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1,4-diazine as one of the cyclos

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514183000 - Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI

514247000 - Hetero ring is six-membered consisting of two nitrogens and four carbon atoms (e.g., pyridazines, etc.)

514248000 - Polycyclo ring system having a 1,2- or 1,4-diazine as one of the cyclos

Patent class list (only not empty are listed)

Deeper subclasses:

Class / Patent application numberDescriptionNumber of patent applications / Date published
514250000 At least three rings in the polycyclo ring system 167
Entries
DocumentTitleDate
20130029996SPECIAL COMPOSITION FOR THE USE THEREOF AS A DRUG - The present invention relates to a composition containing at least one polyphenol, at least one polyethylene glycol and/or a functional equivalent and at least one glycol ether and/or a functional equivalent for application as a medicinal product.01-31-2013
20130029995Substituted Bicyclic Aromatic Carboxamide and Urea Compounds as Vanilloid Receptor Ligands - Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).01-31-2013
20130029994N-(IMIDAZOLIDIN-2-YLIDENE)QUINOLINE DERIVATIVES AS MODULATORS OF ALPHA 2 ADRENERGIC RECEPTORS - The present invention relates to novel N-(imidazolidin-2-ylidene)quinoline derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.01-31-2013
20130029993AZAINDOLYLPHENYL SULFONAMIDES AS SERINE/THREONINE KINASE INHIBITORS - The present invention encompasses compounds of general formula (I)01-31-2013
20100022548USE OF N-HETEROCYCLYLMETHYLBENZAMIDES IN THERAPEUTICS - The invention relates to use of compositions in therapeutics containing a compound having general formula (I):01-28-2010
20120184558Crystalline Salt Forms of a 5,6,7,8-Tetrahydro-1,2,4-Triazolo[4,3-a]Pyrazine Derivative - This invention provides novel crystalline acid salt forms of 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine, i.e. sitagliptin, to processes for their preparation and isolation, and to pharmaceutical compositions comprising the same.07-19-2012
20100056532COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.03-04-2010
20080207628METHODS OF PREVENTING AND REDUCING THE SEVERITY OF STRESS-ASSOCIATED CONDITIONS - The present invention provides a method of preventing or reducing the severity of a stress-associated condition in a subject by systemically administering to the subject an effective amount of brimonidine or a pharmaceutically acceptable salt, ester, amide, sterioisomer or racemic mixture thereof. Stress-associated conditions that can be treated according to a method of the invention include, but are not limited to, dyspepsia, tachycardias other than tachycardia associated with myocardial ischemia, panic attack, non-inflammatory dermatological conditions, disorders of muscle contraction, sensory hypersensitivity associated with migraine, and behavioral disorders.08-28-2008
20090054441Process For The Preparation of an Optically Active 5H-Pyrrolo [3,4-B] Pyrazine Derivative - A substantially pure dextrorotatory isomer of zopiclone or a pharmaceutically acceptable salt thereof and crystalline forms thereof are provided. Also provided is a process for its preparation and pharmaceutical compositions containing same.02-26-2009
20100160331NOVEL CARBAMOYLOXY ARYLALKAN ARYLPIPERAZINE COMPOUND, PHARMACEUTICAL COMPOSITIONS COMPRISING THE COMPOUND AND METHOD FOR TREATING PAIN, ANXIETY AND DEPRESSION BY ADMINISTERING THE COMPOUND - There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.06-24-2010
20100152192FUSED IMIDAZOLE CARBOXAMIDES AS TRPV3 MODULATORS - The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.06-17-2010
20110195969AMIDE COMPOUNDS AS BOOSTERS OF ANTIVIRALS - The present invention relates to compounds that have CYP450 inhibiting properties and are therefore useful as boosters of certain drugs, i.e. they are able to increase at least one of the pharmacokinetic variables of certain drugs when co-administered. The invention further provides the use of said compounds as improvers of the bioavailability of certain drugs. Methods for the preparation of the compounds of the invention and pharmaceutical compositions comprising these compounds are also provided.08-11-2011
20130085144DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE AS MEDICAMENT - The present invention relates to a compound of following formula (I):04-04-2013
20130210829APPLICATION OF 5-HT6 RECEPTOR ANTAGONISTS FOR THE ALLEVIATION OF COGNITIVE DEFICITS OF DOWN SYNDROME - Methods for treating Down syndrome and improving cognitive function of a patient with an intellectual disability are disclosed. 5-hydroxytryptamine sub-receptor six (5-HT08-15-2013
20120245178CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR - Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.09-27-2012
20120245176NOVEL PIPERAZINE ANALOGS WITH SUBSTITUTED HETEROARYL GROUPS AS BROAD-SPECTRUM INFLUENZA ANTIVIRALS - A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof:09-27-2012
201000937405,6,7,8-TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE DERIVATIVES - The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I), wherein X represents CH04-15-2010
20130040956PROCESS FOR THE PREPARATION OF STABLE, CRYSTALLINE (6S)-N(5)-METHYL-5,6,7,8-TETRAHYDROFOLIC ACID - A process for the preparation of the stable, amorphous calcium salt of (6S)-N(5)-methyl-5,6,7,8-tetrahydrofolic acid of the formula V,02-14-2013
20130079348COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.03-28-2013
20090023742THIAZOLONES FOR USE AS PI3 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using substituted thiazolones. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of substituted thiazolones.01-22-2009
20100099683COMPOUNDS THAT INHIBIT HUMAN DNA LIGASES AND METHODS OF TREATING CANCER - Methods for treating cancer using compounds that inhibit human DNA ligases. Methods for using compounds that inhibit human DNA ligases to provide insights into the reaction mechanisms of human DNA ligases, for example to identify the human DNA ligase involved in different DNA repair pathways. Screening methods for compounds that inhibit human DNA ligases.04-22-2010
20090156606OPTICAL CORRECTION - The present disclosure describes compositions which improve visual acuity and to methods for their use.06-18-2009
20100105692Dipterinyl Calcium Pentahydrate (DCP) and Therapeutic Methods Based Thereon - Provided herein is dipterinyl calcium pentahydrate (DCP) and therapeutic methods based thereon. Also provided herein is the compound dipterinyl calcium pentahydrate (DCP) or an analog or polymorph thereof.04-29-2010
20100105691METFORMIN FOLATE AND PREPARATION OF THE SAME - The present invention discloses a novel biguanidine compound, i.e. folacin-metformin, and its manufacture with inorganic salt of metformin as raw material. Compared with metformin, the compound has the same clinic curative effect, such as lowering blood sugar, curing poly-cystic ovary syndrome (PCOS), losing weight and so on, without resulting in the increase of homocysteine concentration, even with a little decrease of homocysteine concentration in some cases.04-29-2010
201002491391,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS - The present invention relates to compounds of formula I09-30-2010
20090124627COMPOSITIONS FOR SLEEPING DISORDERS - Provided herein is a method for treating, preventing, or ameliorating a disorder such as insomnia or another sleeping disorder using a composition that contains an effective amount of one or more compounds.05-14-2009
20090124626Pharmaceutical agent comprising insulin resistance improving agent - To provide a method for treating diabetes which has an excellent hypoglycemic action and causes minimal adverse drug reactions, there is provided a medicine comprising a DPP-IV inhibitor and an insulin sensitizer in combination.05-14-2009
20120165335CDK INHIBITORS - The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer.06-28-2012
20110003822P2X3 RECEPTOR ANTAGONISTS FOR TREATMENT OF PAIN - The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.01-06-2011
20090042892Cetp Inhibitors - Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B is a cyclic group other than phenyl, and B has a cyclic substituent at a position that is ortho to the position at which B is connected to the remainder of the structure of Formula (I). The 5-membered ring of Formula (I) has a second cyclic substituent in addition to B.02-12-2009
20090042890Heteroaryl compounds, compositions thereof, and methods of treatment therewith - Provided herein are Heteroaryl Compounds having the following structure:02-12-2009
20100004252SUBSTITUTED TETRAHYDROPYRROLOPYRAZINE COMPOUNDS AND THE USE THEREOF IN THE TREATMENT AND/OR INHIBITION OF PAIN - Substituted tetrahydropyrrolopyrazine compounds corresponding to the formula I:01-07-2010
20100004251Dopamine-Agonist Combination Therapy For Improving Sleep Quality - The present invention generally relates to pharmaceutical compositions comprising a dopamine agonist and sedative agent. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine. In a preferred embodiment, the sedative agent is optically pure (S)-zopiclone or optically pure (S)—N-desmethylzopiclone. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine; and the sedative agent is optically pure (S)-zopiclone or optically pure (S)—N-desmethylzopiclone. The pharmaceutical compositions of the invention are useful in the treatment of restless-leg syndrome and periodic-limb-movement disorder, as well as various sleep disorders. In addition, the present invention relates to a method of treating a patient suffering from restless-leg syndrome, periodic-limb-movement disorder, a sleep abnormality, or insomnia, comprising coadministering a therapeutically effective amount of a dopamine agonist and a therapeutically effective amount of a sedative agent. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine. In a preferred embodiment, the sedative agent is optically pure (S)-zopiclone or optically pure (S)—N-desmethylzopiclone. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine; and the sedative agent is optically pure (S)-zopiclone or optically pure (S)—N-desmethylzopiclone.01-07-2010
20100004249Bicyclic heterocyclic compound and use thereof - The present invention provides a bicyclic heterocyclic compound having a serotonin 5-HT01-07-2010
20080300251Derivatives of 3-Azabicyclo[3.1.0] Hexane as Dipeptidyl Peptidase-IV Inhibitors - The present invention relates to novel 3-azabicyclo[3.1.0]hexane derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the said compounds. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.12-04-2008
201300903403,4-DIHYDROPYRROLO[1,2-A]PYRAZINE-2,8(1H)-DICARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - Compounds corresponding to the general formula (I)04-11-2013
20090306088SUBSTITUTED HETEROARYL PYRIDOPYRIMIDONE DERIVATIVES - A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof are disclosed and claimed.12-10-2009
20090306087Compounds and Methods for Kinase Modulation, and Indications Therefor - Compounds and salts thereof, formulations thereof conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Raf protein kinases, including melanoma, colorectal cancer, thyroid cancer, ovarian cancer, cholangiocarcinoma, pain or polycystic kidney disease.12-10-2009
20090306086COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds active on Fms and/or Kit protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of Fms and/or Kit protein kinases.12-10-2009
20090042893KINASE INHIBITORS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE - Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions comprising them and methods of their use.02-12-2009
20130072494INHIBITORS OF JUN N-TERMINAL KINASE - The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula:03-21-2013
20130072493N-[4-(1H-PYRAZOLO[3,4-b]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS - The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula I,03-21-2013
20130072495FUSED BICYCLIC KINASE INHIBITORS - Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as but not limited to tumors driven at least in part by at least one of RON, MET, IR, IGF-1R, or ALK. This Abstract is not limiting of the invention.03-21-2013
20130059856AGONISTS OF GPR131 AND USES THEREOF - Chemical compounds which act as agonists of, or otherwise modulate the activity of, GPR131 are disclosed. Related compositions, formulations and methods of use are also described.03-07-2013
20130059857METHODS AND COMPOSITIONS FOR SAFE AND EFFECTIVE TREATMENT OF TELANGIECTASIA - Improved methods and compositions for safe and effective treatment of telangiectasia or a symptom associated with telangiectasia in a subject are described. The methods involve topically applying to an affected skin area a topical composition comprising about 0.3% to about 10% by weight of brimonidine and a pharmaceutically acceptable carrier.03-07-2013
20130059858BENZOFURANYL ANALOGUES AS GPR119 MODULATORS - Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, where-in A, L, m, n, o, p, R03-07-2013
20110015200NITROGEN-CONTAINING BYCYCLIC COMPOUNDS ACTIVE ON CHRONIC PAIN CONDITIONS - The invention refers to compounds of general formula (I) wherein the R groups are, independently, H, C01-20-2011
20110015199GPR119 Agonists - GPR119 agonist compounds of the formula:01-20-2011
20110065713Benzazole Derivatives, Compositions, and Methods of Use as B-Secretase Inhibitors - The present invention is directed to benzazole compounds that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which BACE is involved.03-17-2011
20090270405QUINUCLIDINE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.10-29-2009
20090270404OXYMETHYLENE ARYL COMPOUNDS AND USES THEREOF - Use of oxymethylene aryl GPR119 agonists and DPP IV inhibitors for the treatment of diabetic diseases, including Type II diabetes and other diseases associated with poor glycemic control are provided.10-29-2009
20090270403NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINYL DERIVATIVE AND ITS MEDICAL USE - This invention relates to a novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivative and its use in the manufacture of pharmaceutical compositions. The compound of the invention is found to be a cholinergic ligand at the nicotinic acetylcholine receptors.10-29-2009
20090270402Novel triazolopyridazines - The present invention is directed to novel compounds of formula (I)10-29-2009
20090270401USE OF A DIHYDROIMIDAZOPYRAZOINE DERIVATIVE FOR TREATING OR PREVENTING PAIN - The invention relates to the use of (1R)-1-[({(2R)-2-amino-3-[(8S)-8-(cyclohexylmethyl)-2-phenyl-5,6-dihydroimidazo[1,2-a]pyrazine-7(8H)-yl]-3-oxopropyl}dithio)methyl]-2-[(8S)-8-(cyclohexylmethyl)-2-phenyl-5,6-dihydroimidazo[1,2-a]pyrazine-7(8H)-yl]-2-oxoethylamine or an pharmaceutically acceptable salt thereof for preparing a drug for preventing or treating pain.10-29-2009
20090270400PAINKILLING ASSOCIATION COMPRISING A DIHYDROIMIDAZOPYRAZINE DERIVATIVE - The invention relates to a product comprising (1R)-1-[(({2R)-2-amino-3-[(8S)-8-(cyclohexylmethyl) -2-phenyl-5,6-dihydroimidazo [1,2-a]pyrazin-7(8H)-yl]-3-oxopropyl}dithio)methyl]-2-[(8S)-8-(cyclohexylmethyl) -2-phenyl-5,6-dihydrolmidazo[1,2-a]pyrazin-7(8H)-yl]-2-oxoethylamine in association with an analgesic agent selected from morphine, the similar or a morphine derivative, sodium channel inhibitors, non-steroidal antiflammatory agents (AINS), glutamatergic system inhibitors, tricycle antidepressants and gabaergic derivatives for simultaneous therapeutic use which is separated or out over the time for pain treatment or prevention.10-29-2009
20130065905NITROGEN-CONTAINING HETEROCYCLIC COMPOUND HAVING INHIBITORY EFFECT ON PRODUCTION OF KYNURENINE - The present invention provides a nitrogen-containing heterocyclic compound or a pharmaceutically acceptable salt thereof having an inhibitory effect on the production of kynurenine, represented by formula (I):03-14-2013
201300659023-(HETEROARYL-AMINO)-1,2,3,4-TETRAHYDRO-9H-CARBAZOLE DERIVATIVES AND THEIR USE AS PROSTAGLANDIN D2 RECEPTOR MODULATORS - The present invention relates to 3-(heteroaryl-amino)-1,2,3,4-tetrahydro-9H-carbazole derivatives of the formula (I),03-14-2013
20130065903Method of Improving Diastolic Dysfunction - A method of treating, preventing, reversing, or ameliorating diastolic dysfunction includes reducing S-glutathionylated myosin binding protein-C (MyBP-C) level by administering to a host in need thereof a therapeutically effective amount of tetrahydrobiopterin (BH03-14-2013
20130065904Combinations of Eszopiclone and Trans 4-(3,4-Dichlorophenyl)-1,2,3,4-Tetrahydro-N-Methyl-1-Napthalenamine or Trans 4-(3,4-Dichlorophenyl)-1,2,3,4-Tetrahydro-1-Napthalenamine, and Methods of Treatment of Menopause and Mood, Anxiety, and Cognitive Disorders - One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., menopause, mood disorders, anxiety disorders, or cognitive disorders. The first component of the pharmaceutical composition is a sedative eszopiclone. The second component of the pharmaceutical composition is trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-napthalenamine or trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine. The present invention also relates to a method of treating menopause, perimenopause, mood disorders, anxiety disorders, and cognitive disorders.03-14-2013
20090258879METHOD FOR TREATING CANCER, RHEUMATOID ARTHRITIS AND OTHER MEDICAL DISEASES BY UTILIZING MODIFIED VIRUS VIRIONS TO INSERT MEDICATIONS INTO TARGETED CELLS - A safer, more effective treatment of many medical diseases may be approached by a method utilizing modified viruses as vehicles to transport medically therapeutic drug molecules to specific cells in the body with the intent to have the drug exert an effect only on those cells to which the modified virus delivers the drug. The modified virus or virus-like structures make contact with specific target cells by means of the modified virus's exterior probes or virus-like structures' exterior probes. Once the exterior probes engage a target cell's receptors, the modified virus or virus-like structure inserts into the target cell the quantity of medically therapeutic drug molecules it is carrying. By delivering the medically therapeutic drug only to specific cells in the body it is assured the drug reaches the site in the body it will be most beneficial and the occurrence of unwanted side effects due the drug are significantly minimized.10-15-2009
20110046144IMIDAZOPYRAZINOL DERIVATIVES FOR THE TREATMENT OF CANCERS - Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein X02-24-2011
20090233935Methods for Fabrication of Antimicrobial Surfaces - A method for rendering a carboxyl-containing polymer surface resistant to microbial growth, the method comprising: (i) reacting the carboxyl-containing polymer surface with a metal borohydride in a solvent system comprising a water-soluble alcohol having one to three hydroxy groups and one to four carbon atoms, and optionally up to about fifty percent water, in a temperature range having a minimum of about 60° C. and a maximum of about 80° C., and for an amount of time sufficient for reducing carboxyl groups on the carboxyl-containing polymer surface to surface hydroxymethyl groups without altering the nature of the bulk of the polymer; and either: (iia) converting hydroxy groups of the surface hydroxymethyl groups to leaving groups and displacing the leaving groups with one or a combination of antimicrobial agents; or (iib) displacing the hydrogen atoms of the hydroxy groups of the surface hydroxymethyl groups with one or a combination of antimicrobial agents.09-17-2009
20120115874PYRAZINE DERIVATIVES, PROCESS FOR MANUFACTURE AND USE THEREOF - The present invention provides pyrazine derivatives of formula I05-10-2012
20090005386Methods for Modulating Ion Channels - In one embodiment, the invention provides an ion having the formula: (I) In another embodiment, the invention provides a method for modulating potassium, sodium, and cyclic nucleotide-modulated ion channels in a mammal in need thereof. In a further embodiment, the invention provides a method for modulating ligand-gated ion channels or transient receptor potential channels in a mammal in need thereof. The methods comprise administering an ion having the formula described above.01-01-2009
20080318965Derivatives of Alpha2-Adrenergic Receptor Agonist - The present invention relates to alpha12-25-2008
20120238580MALEATE SALTS OF 6-(5-CHLORO-2-PYRIDYL)-5-[(4-METHYL-1-PIPERAZINYL)CARBONYLOXY]-7-OXO-6,7-- DIHYDRO-5H-PYRROLO[3,4-b]PYRAZINE - A novel maleate salt of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-09-20-2012
20120238579New Compounds 806 - The present invention relates to new compounds of formula (I) and to pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof.09-20-2012
20130165447Inhibitors of PDE10 - PDE10 inhibitors having the general formula (I)06-27-2013
20080293727Novel sulfonamide inhibitors of aspartyl protease - The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.11-27-2008
20080293726Combinations of Eszopiclone and Trans 4-(3,4-Dichlorophenyl)-1,2,3,4-Tetrahydro-N-Methyl-1-Napthalenamine or Trans 4-(3,4-Dichlorophenyl)-1,2,3,4-Tetrahydro-1-Napthalenamine, and Methods of Treatment of Menopause and Mood, Anxiety, and Cognitive Disorders - One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., menopause, mood disorders, anxiety disorders, or cognitive disorders. The first component of the pharmaceutical composition is a sedative eszopiclone. The second component of the pharmaceutical composition is trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-napthalenamine or trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine. The present invention also relates to a method of treating menopause, perimenopause, mood disorders, anxiety disorders, and cognitive disorders.11-27-2008
20110034470Inhibitors of JNK - The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I:02-10-2011
20080287447Methods for preparing eszopiclone - Methods for the preparation of crystalline eszopiclone free base in water, in the absence of organic solvents, are provided. The methods are more environmentally acceptable than prior art methods, and produce eszopiclone free base essentially free of residual organic solvent.11-20-2008
20120101106Tetrahydronapthyridine Orexin Receptor Antagonists - The present invention is directed to tetrahydronapthyridine and tetrahydropyridopyrazine compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.04-26-2012
20080280913TETRAHYDROTRIAZOLOPYRAZINE DERIVATIVES AND USES THEREOF - This invention relates to novel substituted tetrahydrotriazolopyrazines and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an enzyme inhibitor of dipeptidyl-peptidase IV (DPP-IV).11-13-2008
20080293728Complexes Comprising alpha2-Adrenergic Receptor Agonists and Compositions - A complex comprises at least an α11-27-2008
20110281882Compositions and Methods for Treating, Controlling, Reducing, or Ameliorating Inflammatory Pain - A composition for treating, controlling, reducing, or ameliorating inflammatory pain comprises a dissociated glucocorticoid receptor agonist (“DIGRA”), a prodrug thereof, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable ester thereof. The composition can comprise an additional anti-inflammatory agent and can be formulated for topical application, injection, or implantation. It may be used in a method of managing post-surgical ocular pain such that it has lower risk of eliciting adverse side effects seen with other therapeutic agents.11-17-2011
20110281880METHODS OF ADMINISTERING TETRAHYDROBIOPTERIN, ASSOCIATED COMPOSITIONS, AND METHODS OF MEASURING - The present invention is directed to treatment methods of administering tetrahydrobiopterin, including in oral dosage forms, in intravenous formulations, and with food. Also disclosed herein are biopterin assays for measuring the amount of biopterin and metabolites of biopterin in a sample.11-17-2011
20110281879SULFONYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS - The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.11-17-2011
20080269227Pyridine Methylene Azolidinones and Use Thereof Phosphoinositide Inhibitors - The present invention is related to fused pyridine methylene azolidinone derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.10-30-2008
20090247532Crystalline polymorph of sitagliptin phosphate and its preparation - The present invention is directed to a novel polymorph form of crystalline sitagliptin phosphate, named as Form V herein. The present invention further provides processes for preparations of Form V, pharmaceutical composition comprising Form V and its use in therapy. Form V can be prepared from recrystallizing sitagliptin phosphate in a mixture of methanol and water, a mixture of acetone and water, or from distillation of a mixture of organic solvents and water followed by recrystallization in the remaining aqueous solution.10-01-2009
20100267731USE OF TRANSFORMING GROWTH FACTOR-B RECEPTOR INHIBITORS TO SUPPRESS OCULAR SCARRING - A pharmaceutical composition useful in the prevention of subconjunctival scarring that may occur after GFS comprising an effective amount of an ALK-5 inhibitor. Also disclosed is a method of treating disorder or condition of other ocular scarring or fibrosis including corneal haze and PVR that may develop after ocular surgery or injury comprising applying an amount of a pharmaceutical composition including an ALK-5 inhibitor to a post-surgical or injury site.10-21-2010
20120289512Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme - The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.11-15-2012
20090197889SYNTHESIS AND ANTI-PROLIFERATIVE EFFECT OF BENZIMIDAZOLE DERIVATIVES - This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated.08-06-2009
20110118267Method and Kit for Treating or Preventing Psoriasis - Methods and kits for treating or preventing psoriasis or a symptom associated with psoriasis in a subject are described. The methods involve topical applications to the subject a therapeutically effective amount of an α2 adrenergic receptor agonist, such as brimonidine.05-19-2011
20100311759ANTIPARASITIC AGENT FOR FISH AND METHOD OF CONTROLLING PROLIFERATION OF FISH PARASITES - An antiparasitic agent for fish containing an inhibitor of folate synthesis and/or an inhibitor of folate activation as the active substance(s). A combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is preferable, and a sulfonamide is preferable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist, etc., can be used as the inhibitor of folate activation.12-09-2010
20090054440Quinoline derivatives as neurokinin receptor antagonists - The present invention relates to substituted quinoline hydrazides of Formula (I): wherein R02-26-2009
20090048260Use of pyrrolopyrazine derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells - The invention relates to the use of pyrrolopyrazine derivatives for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells, said derivatives being of formula (I): where R2 and R3 independently=H, C1-C6 straight or branched chain optionally-substituted alkyl, R6=an aromatic ring Ar or cycloalkyl, optionally substituted, said cycloalkyl optionally substituted by an aryl group which may equally be substituted, R7=H, C1-C6 alkyl, (alk.)02-19-2009
20090306085HCV PROTEASE INHIBITORS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.12-10-2009
20110301171Inhibitors of JNK - Compounds of formula I12-08-2011
20110301168CYCLOALKANE[B]AZAINDOLE ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS - Described herein are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.12-08-2011
20110301172COMBINATION OF DPP-IV INHIBITOR, PPAR ANTIDIABETIC AND METMORFORMIN - The invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, which comprises; 12-08-2011
20110301169Therapies for Treating Cancer Using Combinations of COX-2 Inhibitors and Antimetabolites - A method for treating a subject having cancer, comprising administering to the subject, a therapeutically effective amount of a combination comprising a 1,2-diphenylpyrrole derivative or the respective pharmaceutically acceptable salt, solvate, polymorph or prodrug and an anti-metabolite.12-08-2011
20110166147IMIDAZOPYRAZINE COMPOUNDS - Novel imidazopyrazine compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a viral infection, in particular a HCV, HRV, Sb and/or CVB in a patient in need thereof.07-07-2011
20110288098NOVEL COMPOUNDS - This invention relates to imidazopyrazine substituted piperidine derivatives and their use as pharmaceuticals.11-24-2011
201002922413,5-SUBSTITUTED-1,3-OXAZOLIDIN-2-ONE DERIVATIVES - The present invention is directed to 3,5-disubstituted-1,3-oxazolidin-2-one derivatives which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neuro-ological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.11-18-2010
20090281108PRENATAL DIETARY SUPPLEMENT - The present invention relates to a prenatal dietary supplement comprising at least one omega-3 fatty acid, at least one omega-6 fatty acid; folic acid; lutein; and at least one proanthocyanidin.11-12-2009
20080207626STABLE TABLET FORMULATION - The present invention is directed to a stable solid formulations of tetrahydrobiopterin, processes for producing them, and treatment methods using such formulations.08-28-2008
20110294817N-[PIPERAZINYL HETARYL]ARYLSUFONAMIDE COMPOUNDS WITH AFFINITY FOR THE DOPAMINE D3 RECEPTOR - The invention related to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula (I) in which Q is a bivalent, 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents R12-01-2011
20090298839ADRB2 GENE POLYMORPHISM ASSOCIATED WITH INTRAOCULAR PRESSURE RESPONSE TO TOPICAL BETA-BLOCKERS - The invention provides a single nucleotide polymorphism (SNP) rs1042714 in the human ADRB2 gene (Gln27Glu) associated with a clinically meaningful reduction in intraocular pressure (IOP) in a human following treatment with a topical beta-blocker. Nucleic acids comprising the SNP are used to screen glaucoma-afflicted individuals to thereby provide an improved method for genotype-based prescribing of beta-blockers in glaucoma management.12-03-2009
20110301170Inhibitors of JNK - Compounds of formula I12-08-2011
20110112101TREATMENT FOR OCULAR-RELATED DISORDERS - A treatment for ocular related disorders, such as macular degeneration, and preferably age-related macular degeneration, diabetic retinopathy, and diabetic macular edema is disclosed, using a compound of Formula I.05-12-2011
20090076013DEUTERIUM-ENRICHED SITAGLIPTIN - The present application describes deuterium-enriched sitagliptin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20090030004SPECIFIC SALT, ANHYDROUS AND CRYSTALLINE FORM OF A DIHYDROPTERIDIONE DERIVATIVE - The present invention relates to a specific salt of a dihydropteridione derivative, namely the trihydrochloride salt of the compound N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide, to its crystallisation in the form of an hydrate with water, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.01-29-2009
20080242668Dimeric Azacyclic Compounds and Their Use - This invention relates to azacyclic derivatives according of formula (I) and their use as pharmaceuticals. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or. disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the′ termination of abuse of chemical substances. Formula (I) Aza-X′-A′-Y′-L-Y-A″-X″-Aza Aza:Azabicyclic group A′,A″:Aromatic monocyclic and/or polycyclic, carbocyclic and/or heterocyclic group Y′,Y″: Linker or absent (covalent bond) L: Monocyclic or polycyclic, carbocyclic or heterocyclic group or is absent X′,X″: Linker or absent (covalent bond)10-02-2008
20090054442METHOD OF ADMINISTERING OPHTHALMIC FLUIDS - A method is provided of treating an eye with ophthalmologically active compounds, particularly with intra-ocular pressure lowering (IOP) compounds, where a dose of 5-15 microliters is delivered at a standard concentration.02-26-2009
20100004250PTERIDINE DERIVATIVES AS POLO-LIKE KINASE INHIBITORS USEFUL IN THE TREATMENT OF CANCER - Compounds of formula (I) are inhibitors of Polo-like kinases (PLKs), and are useful, inter alia, in the treatment of proliferative diseases:01-07-2010
20100022547Compounds and Methods for Treating Mammalian Gastrointestinal Parasitic Infections - One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of 01-28-2010
20100035884KINASE INHIBITOR - The invention is directed to a compound of formula (I):02-11-2010
20090275586HETEROCYCLIC INHIBITORS OF PDE4 - The present invention is directed to potent and selective heterocyclic compounds, useful as inhibitors of phosphodiesterase 4 (PDE4), compositions comprising the same, and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of PDE4 activity are also provided, as well as methods for the treatment of inflammatory diseases and other diseases in which PDE4 or one of its isoforms may play a role.11-05-2009
20090099190Kinase inhibitors useful for the treatment of proliferative diseases - The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferrably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.04-16-2009
20090048261Pharmaceutical Composition for Treatment of Ocular Hypertension - The present invention is related to the pharmaceutical industry in general and in particular with the pharmaceutical industry of production of ophthalmic compositions. More specifically, the present invention relates to the pharmaceutical industry of production of ophthalmologic compositions for the treating of ocular hypertension. The advantage of the present invention against the present state of the technique is the fulfilling of a synergic effect of its components for the decreasing of ocular hypertension with no antagonistic effect between its components. The present invention consists of a pharmaceutical composition for the treatment of ocular hypertension characterized by comprising a pharmacologically effective amount of dorzolamide, with a pharmacologically effective amount of timolol and a pharmacologically effective amount of brimonidine.02-19-2009
20100113461SUBSTITUTED HETEROCYCLIC COMPOUNDS - The present invention relates to compounds that are late sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I):05-06-2010
20100113460Organic Compounds - Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them.05-06-2010
201002861511-OXA-3-Azaspiro[4,5]Decan--2-One Derivatives For The Treatment Of Eating Disorders - The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof,11-11-2010
200900053883-Heteroaryl-3,9-Diazabicyclo[3.3.1]Nonane Derivatives as Nicotinic Acetylcholine Receptor Agonists - This invention relates to novel 3,9-diazabicyclo[3.3.1]nonane derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.01-01-2009
201001207791-(ARYLSULFONYL)-4-(PIPERAZIN-1-YL)-1H-BENZIMIDAZOLES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS - The invention relates to 1-(arylsulfonyl)-4-(piperazin-1-yl)-1H-benzimidazole compounds of the Formula I:05-13-2010
20100120774Substituted Pyrano [2,3-b] Pyridinamine compounds as beta-secretase modulators and methods of use - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I05-13-2010
20100280036Modulation of Pathogenicity - The present invention relates to the use of compounds of the general Formula (I):11-04-2010
20100286152N-PHENYL HYDRAZIDES AS MODULATORS OF THE GHRELIN RECEPTOR - The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof,11-11-2010
20100120778QUINOXALINE-BASED LXR MODULATORS - Disclosed are quinoxaline-based modulators of Liver X receptors (LXRs) and related methods. The modulators include compounds of formula (I):05-13-2010
20100125077Polymorphs of Brimonidine Pamoate - A brimonidine pamoate polymorph exhibits characteristics disclosed herein. The polymorph is included in a composition, device, or implant for use in the treatment or control of elevated intraocular pressure or in the neuroprotection of components of a neurological tissue to prevent progressive degeneration of such components. In particular, such a composition, device, or implant can be used to provide neuroprotection to cells and components of the optic nerve system.05-20-2010
20120065209TETRAHYDRO-IMIDAZO[1,5-a]PYRAZINE DERIVATIVES SALTS, PREPARATION METHODS AND MEDICINAL USE THEREOF - Pharmaceutically acceptable salts of (R)-7-[3-amino-4-(2,4,5-trifluorophenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-formic acid, their preparation methods, compositions containing the said pharmaceutical salts and their use as medicaments, especially as dipeptidyl peptidase IV (DPP-IV) inhibitors are disclosed.03-15-2012
20120035180PHARMACEUTICAL COMPOSITION FOR TREATING CANCER COMPRISING CHLORIN E6-FOLIC ACID CONJUGATE COMPOUND AND CHITOSAN - The present invention relates to a pharmaceutical composition for the treatment of cancer comprising a chlorin e6-folic acid conjugate compound and chitosan, and more particularly, to a pharmaceutical composition for photodynamic therapy of solid tumors comprising the novel chlorin e6-folic acid conjugate compound or a pharmaceutically acceptable salt thereof and chitosan, in which the novel compound is prepared by linking chlorin e6 to folic acid, and effectively produces singlet oxygen in various media and has much better tumor selectivity than the known porphyrin-based photosensitizers, thereby being used effectively in photodynamic treatment for malignant tumors.02-09-2012
20100120775Farnesoid X Receptor Agonists - The present invention provides novel substituted isoxazole compounds, pharmaceutical compositions, therapeutic uses and processes for preparing the same.05-13-2010
20100324049DIARYL KETIMINE DERIVATIVE HAVING ANTAGONISM AGAINST MELANIN-CONCENTRATING HORMONE RECEPTOR - [Problems] To provide an antagonist of a melanin-concentrating hormone receptor, which is useful as a medicine for a central nervous system disease, a cardiovascular disease or a metabolic disease.12-23-2010
20100087441Prognostic Method - A method for prognosing a rheumatoid arthritis phenotype using the outcomes of selected single nucleotide polymorphisms (SNPs) and clinical variables. A method for genotyping multiple rheumatoid arthritis associated genetic variations comprising use of a DNA microrarray. A microarray for use in the described methods.04-08-2010
20100249141NOVEL INHIBITORS OF FOLIC ACID-DEPENDENT ENZYMES - The invention relates to compounds of the formula I, or pharmaceutically acceptable salts thereof:09-30-2010
20100087440Phosphatidylinositol 3-Kinase Inhibitors and Methods of Their Use - The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.04-08-2010
20090176790PTERIN ANALOGS - Disclosed herein are analogs of tetrahydrobiopterin, compositions containing the same, and methods of treating an individual suffering from a condition responsive to tetrahydrobiopterin by administration of the analog. These analogs are contemplated for use wherever tetrahydrobiopterin is currently used to treat conditions responsive to tetrahydrobiopterin therapies.07-09-2009
20090258881ARYL-SUBSTITUTED POLYCYCLIC AMINES, METHOD FOR THE PRODUCTION THEREOF, AND USE THEREOF AS A MEDICAMENT - The invention relates to aryl-substituted polycyclic amines of the formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof;10-15-2009
201301903184,7-DIHYDRO-PYRAZOLO[1,5-a]PYRAZIN-6-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) - The present invention relates to novel 4,7-dihydro-pyrazolo[1,5-a]pyrazin-6-yl-amine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.07-25-2013
20100099681SUBSTITUTED 5-AMINOPYRAZOLES AND USE THEREOF - The present application relates to novel substituted 5-aminopyrazoles, methods of production thereof, use thereof alone or in combinations for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases.04-22-2010
20100099682ACETYLENE DERIVATIVES - The invention provides compounds of formula (I)04-22-2010
20100099680PTERIDINONE DERIVATIVES AS P13-KINASES INHIBITORS - New compounds of Formula (1) are provided which by virtue of their pharmaceutical activity as PI3-kinase modulators may be used in the therapeutic field for the treatment of inflammatory or allergic diseases. Examples of these include inflammatory and allergic respiratory complaints, inflammatory diseases of the gastro-intestinal tract and motor apparatus, inflammatory and allergic skin diseases, inflammatory eye diseases, diseases of the nasal mucosa, inflammatory or allergic conditions involving autoimmune reactions or inflammations of the kidney.04-22-2010
20110172236SUBSTITUTED ARYL SULFONE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS - A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.07-14-2011
20100125078QUINAZOLINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS - The present invention relates to a compounds of formula I05-20-2010
20090105264Substituted Nicotinamide Compounds - The present invention relates to a novel class of substituted nicotinamides. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.04-23-2009
200803122427-ARYL-3, 9-DIAZABICYCLO(3.3.1)NON-6-ENE DERIVATIVES AND THEIR USE AS RENIN INHIBITORS IN THE TREATMENT OF HYPERTENSION, CARDIOVASCULAR OR RENAL DISEASES - The invention relates to novel 3,9-diazabicyclo[3.3.1]nonene derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors or renin.12-18-2008
20090286798FUSED PYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - Novel[1.2.4]triazolo[1,5-a]pyrazine and imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following:11-19-2009
20090088438NEW TYROSINE DERIVATIVES AS PPARy MODULATORS - Compounds of general formula I,04-02-2009
20100280037CRYSTALLINE FORM OF A DIHYDROPTERIDIONE DERIVATIVE - The present invention relates to a crystalline form a dihydropteridione derivative, namely a crystalline form of the free base N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.11-04-2010
20100280038METHODS OF TREATMENT OF CHRONIC PAIN USING ESZOPICLONE - The invention relates to the use of eszopiclone for the treatment of low-level, chronic pain and fatigue associated with pain.11-04-2010
20120295913BICYCLIC PYRAZOLE COMPOUNDS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS - In one aspect, the invention relates to bicyclic pyrazole compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.11-22-2012
20090036455ARYLPIPERAZINE DERIVATIVE AND USE THEREOF AS 5-HT1A RECEPTOR LIGANDS - Novel substituted arylpiperazine derivatives with activity as 5-hydroxytryptamine 1A (5-HT02-05-2009
20100099685CRYSTALLINE FORMS OF (6R)-L-ERYTHRO-TETRAHYDROBIOPTERIN DIHYDROCHLORIDE - Crystal forms of (6R)-L-erythro-tetrahydrobiopterin dihydrochloride, hydrates and solvates and processes for their preparation are provided. These crystal forms are either intermediates for the preparation of stable polymorphic form B or are suitable for solid formulations.04-22-2010
20080242669METHODS RELATING TO THE TREATMENT OF FIBROTIC DISORDERS - The invention provides α-mimetic structure of formula (I), wherein A is —(C═O)—(CHR10-02-2008
20080275051Preparation of High Purity Substituted Quinoxalines - The present invention comprises an improved process for the preparation of substituted quinoxaline I by cyclization of the corresponding dianiline.11-06-2008
20080275052HETEROBICYCLIC COMPOUNDS USEFUL AS KINASE INHIBITORS - A compound of Formula (I)11-06-2008
201200590123-(4-AMINOPHENYL)-2-FURANCARBOXYLIC ACID DERIVATIVE AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - Disclosed is a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof:03-08-2012
20080280912Novel Diazabicycylic Aryl Derivatives and Their Medical Use - This invention relates to novel diazabicyclic aryl derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.11-13-2008
20110207737SUBSTITUTED BICYCLIC AMINES FOR THE TREATMENT OF DIABETES - Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.08-25-2011
20080287446Sulfonyl Containing Compounds as Cysteine Protease Inhibitors - The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.11-20-2008
20080287449AZA-TRIPEPTIDE HEPATITIS C SERINE PROTEASE INHIBITORS - The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof:11-20-2008
20080287448Diacyl indazole derivatives as lipase and phospholipase inhibitors - The invention relates to diacyl indazole derivatives of general formulae (I) or (II) and to the pharmaceutically acceptable salts thereof:11-20-2008
20080306076MODULATION OF CHEMOSENSORY RECEPTORS AND LIGANDS ASSOCIATED THEREWITH - The present invention provides screening methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors as well as modifiers capable of modulating chemosensory receptors and their ligands.12-11-2008
20080306079External preparation for allergic diseases - The invention presents an external preparation for allergic diseases containing 3′-hydroxymethyl-4-hydroxypyrrolido [1,2-f]2′,5′-pipera-zinedione as an active ingredient. This compound has a prophylactic and therapeutic effect of allergic diseases, and the external preparation of the invention can be used in prophylaxis and treatment of various allergic diseases (for example, atopic dermatitis, urticaria, allergic rhinitis, allergic conjunctivitis, pollinosis, allergic asthma, and others).12-11-2008
20080306077Oxadiazole Derivatives and Their Use as Metabotropic Glutamate Receptor Potentiators 842 - Compounds of Formula I:12-11-2008
20080306075Pharmaceutical Compositions For Transdermal Delivery - The present invention relates to a pharmaceutical composition for transdermal administration comprising a conjugate of methotrexate and PTD (protein transduction domain). In accordance with the present invention, the methotrexate, which is widely used for the treatment of psoriasis, rheumatoid and inflammation, etc., can be delivered transdermally to a local part of a patient body, in order to minimize the side effect of the methotrexate.12-11-2008
20080312240Bicyclic Piperazines as Metabotropic Glutatmate Receptor Antagonists - The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof:12-18-2008
20130217695BETA-AMINO HETEROCYCLIC DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES - The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.08-22-2013
20080293725Prognostic Molecular Markers - The present invention relates to the use of ecteinascidin 743 in patients having certain levels of molecular markers who can predict the outcome of chemotherapy, in particular in patients having low levels of BRCA1 expression.11-27-2008
20090312335Hiv Integrase Inhibitors - Substituted hydroxytetrahydropyrrolopyrazinone and substituted hydroxytetrahydro-pyrazolopyrazinone compounds of Formula (I) are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein R12-17-2009
20120295914COMBINATION OF ADRENERGIC RECEPTOR AGONIST ALPHA-1 OR ALPHA-2, PREFERABLY BRIMONIDINE WITH FILLERS, PREFERABLY HYALURONIC ACID - A combination of a quantity of adrenergic receptor agonist α-1 or α-2, and preferably product known as brimonidine, with fillers, and preferably with hyaluronic acid, for decreasing skin or cutaneous reactions is described.11-22-2012
20080207623Peptide-enhanced corneal drug delivery - Improved methods and preparations are provided for ocular administration of therapeutic drugs. The preparations include respective quantities of a drug and a peptide which enhances transport of the drug across ocular tissues. The drug and peptide components may be separately administered or used as a mixture. The preferred peptide is NC-1059 (Seq. ID No. 1).08-28-2008
20080269228HYDRAZIDE-CONTAINING HEPATITIS C SERINE PROTEASE INHIBITORS - The present invention relates to novel hydrazide-containing compounds of Formula I or Formula II, including pharmaceutically acceptable salts, esters, or prodrugs thereof which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.10-30-2008
20080269229Novel 8-aza-bicyclo[3.2.1]octane derivatives and their use as monoamine neurotransmitter re-uptake inhibitors - This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors.10-30-2008
20090264436CB-1 receptor modulator formulations - Described herein are solid, stable pharmaceutical formulations of cannabinoid receptor inverse agonists, such as taranabant, and processes of making such formulations. Additionally, described herein are solid stable pharmaceutical formulations of cannabiniod inverse agonists, such as taranabant, and an additional therapeutic agent, as well as processes for making such pharmaceutical formulations.10-22-2009
20090264435Novel Aryl- and Heteroarylpiperazines - Novel aryl- and heteroarylpiperazines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.10-22-2009
20100137324RHO-KINASE INHIBITORS - Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.06-03-2010
20100137323BENZO-FUSED COMPOUNDS FOR USE IN TREATING METABOLIC DISORDERS - The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I:06-03-2010
20100137325BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - The invention provides compounds of formula I:06-03-2010
20100298335Preparations and Methods for Ameliorating or Reducing Presbyopia - This application relates to the use of one or more parasympathomimetic drugs in combination with one or more alpha agonists to create optically beneficial miosis to, for example, temporarily treat presbyopia. The invention provides a pharmaceutical preparation comprising a therapeutically effective amount of one or more parasympathomimetic drugs or cholinesterase inhibitors, or a pharmaceutically acceptable salt thereof, in combination with one or more alpha agonists or antagonists, or a pharmaceutically acceptable salt thereof. The invention further provides for a method for treating, ameliorating or reducing presbyopia of a patient having an eye, comprising administering to said eye a pharmaceutically effective amount of the ophthalmic preparation.11-25-2010
20090030005Combinations for the treatment of cancer - This invention is in the field of pharmaceutical agents and specifically relates to combinations, compositions, uses and methods for treating cancer.01-29-2009
20090030002Heterocyclic compounds and their uses - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelodysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.01-29-2009
20090088439Diazinane Compounds - The present invention relates to novel compounds of the general formula (I)04-02-2009
20100144743COMPOSITIONS AND METHODS FOR INHIBITION OF TYROSINE KINASES - Compositions for inhibiting the catalytic activity of tyrosine kinases comprising compounds represented by Formulas (I), (II), and (III). Methods for treating proliferative diseases comprising administering a therapeutically effective amount of the above compositions.06-10-2010
20120035182METHODS OF TREATMENT OF CHRONIC PAIN USING ESZOPICLONE - The invention relates to the use of eszopiclone for the treatment of low-level, chronic pain and fatigue associated with pain.02-09-2012
20090082357Prolyl Hydroxylase Inhibitors - The invention described herein relates to certain bicyclic heteroaromatic N-substituted glycine derivatives of formula (I)03-26-2009
20090124625NOVEL ALKYNYL DERIVATIVES AS MODULATORS OF METATROPIC GLUTAMATE RECEPTORS - The present invention relates to novel compounds of formula (I) wherein W, n, X and W′ are defined in the description; invention compounds are modulators of metabotropic glutamate receptors—subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.05-14-2009
20110224216Methods of Treating or Preventing Acute Erythema - A method of treating or preventing acute erythema in a human in need thereof by topical administration of an effective amount of an alpha adrenergic receptor agonist or pharmaceutically acceptable salt thereof is claimed. The preferred alpha adrenergic receptor agonist is brimonidine. A method of preventing secondary inflammation caused by acute erythema by topical administration of an effective amount of an alpha adrenergic receptor agonist or a pharmaceutically acceptable salt thereof is also claimed.09-15-2011
20090005390NOVEL QUINUCLIDINE DERIVATIVES AND THEIR USE - This invention relates to novel quinuclidine derivatives and their use as pharmaceuticals. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.01-01-2009
20090005387QUINOXALINYL MACROCYCLIC HEPATITIS C VIRUS SERINE PROTEASE INHIBITORS - The present invention relates to compounds, including compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof:01-01-2009
20090005385Treatment or Prevention of Cancer or Cardiovascular Disease with Methenyltetrahydrofolate Synthetases - The present invention relates to a method of screening test substances for chemotherapeutic activity or for efficacy in treating cardiovascular disease by providing one or more cells transformed with a nucleic acid molecule encoding methenyltetrahydrofolate synthetase, contacting the cells with test substance(s), and identifying those test substances which modulate methenyltetrahydrofolate synthetase expression as candidates for such therapeutic use. Another aspect of the present invention relates to a method of measuring folate status in a sample by measuring methenyltetrahydrofolate synthetase expression or activity and/or catecholamine activity in the sample, all of which are correlated to folate status in the sample. The present invention can also be used to treat or prevent cancer or cardiovascular disease in a subject by administering to the subject a substance which modulates methenyltetrahydrofolate synthetase expression or activity and/or catecholamine activity.01-01-2009
20090176789Diazaspirodecane orexin receptor antagonists - The present invention is directed to diazaspirodecane compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.07-09-2009
20090118295CHEMICAL COMPOUNDS - The use of a compound of formula I wherein Y is a single bond, C═O, C═S or S(O)05-07-2009
20080318962Fungicides Based on Nitrogen-Containing Heterocycles - The compound of the general formula (I), wherein W, X, Y, Z, R, R12-25-2008
200803189631-[6,7-Substituted Alkoxyquinoxalinyl) Aminocarbonyl]-4-(Hetero) Arylpiperazine Derivatives - The present invention relates to novel quinoxaline-piperazine compounds, 1-[(6,7-substituted alkoxyquinoxalinyl)aminocarbonyl]-4-(hetero)arylpiperazine derivatives and their pharmaceutically acceptable salts, a process for their preparation thereof, and compositions containing such compounds. Therapeutic methods for the treatment of hyperproliferative disorders, including cancers, by administering quinoxalin-piperazine compounds are also included.12-25-2008
20100004248Use of a Nitric Oxide Synthase Modulator for the Treatment of Cardiac Indications - The invention features compositions and methods for modulating NOS that are useful for the prevention and treatment of cardiac diseases and disorders, including cardiac hypertrophy and cardiac dilation. In particular, the invention provides compositions comprising tetrahydrobiopterin (BH4), alone or in combination with one or more additional compounds.01-07-2010
20090325970AZA-INDOLES AND RELATED COMPOUNDS HAVING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR ANTAGONIST BIOLOGICAL ACTIVITY - The present invention provides compounds are disclosed herein having the formula:12-31-2009
20090209545Besylate Salts of 6-(5-Chloro-2-Pyridyl)-5-[(4-Methyl-1-Piperazinyl)Carbonyloxy]-7-oxo-6,7-- dihydro-5H-Pyrrolo[3,4-b]Pyrazine - A novel besylate salt of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-08-20-2009
20090258880Substituted Tetrahydropyrrolopyrazine Compounds and the Use Thereof in Pharmaceutical Compositions - Substituted tetrahydropyrrolopyrazine compounds corresponding to formula I10-15-2009
20090082358Vanilloid receptor ligands and their use in treatments - Bicyclic 3,4-fused piperidine compounds, and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotizing agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.03-26-2009
20090082356Pyrazine Derivatives and Use as P13k Inhibitors - The present invention is related to pyrazine derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.03-26-2009
20110224215PRE-SURGICAL TREATMENT - The invention relates to a method of reducing post-surgical bleeding and/or bruising in a patient scheduled to be subjected to a surgical procedure and a patient that was subjected to a surgical procedure. The method involves topically applying to the area and the surrounding area of skin of the patient where the surgical procedure will be or was performed, a pharmaceutical composition comprising an effective amount of brimonidine or a pharmaceutically acceptable salt thereof, prior to performing the surgical procedure and/or following the surgical procedure.09-15-2011
20090076012Modulation of pathogenicity - The present invention relates to the use of compounds of the general Formula (I):03-19-2009
201102304927-PHENYLALKYL SUBSTITUTED 2-QUINOLINONES AND 2-QUINOXALINONES AS POLY(ADP-RIBOSE) POLYMERASE INHIBITORS - The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I)09-22-2011
201102304916-SUBSTITUTED 2-QUINOLINONES AND 2-QUINOXALINONES AS POLY(ADP-RIBOSE) POLYMERASE INHIBITORS - The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I)09-22-2011
20090203704Quinoxaline Derivative, and Light-Emitting Element, Light-Emitting Device, and Electronic Device Using Quinoxaline Derivative - An object is to provide a novel quinoxaline derivative. Another object is to provide a light-emitting element with low driving voltage. Still another object is to provide a light-emitting element with low power consumption. Yet another object is to provide a light-emitting device and an electronic device each having low power consumption by using such a light-emitting element. A quinoxaline derivative is provided which has a structure in which at least one of carbon at a 2-position and carbon at a 3-position of quinoxaline, and carbon of a pyridine ring are bound via an arylene group.08-13-2009
20090209544Aminotetrahydropyrans as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes - The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.08-20-2009
20090105263HETEROBICYCLIC COMPOUNDS AS GLUCOKINASE ACTIVATORS - Compounds of Formula (I):04-23-2009
20090105266Organic compounds - The present invention relates to novel benzimidazole derivatives, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them, wherein the compounds have the formula (I):04-23-2009
20080318964DEUTERIUM-ENRICHED ESZOPICLONE - The present application describes deuterium-enriched eszopiclone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.12-25-2008
20080261989Quinoxaline Inhibitors of the Hedgehog Signalling - The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I wherein A is a carbocycle or heterocycle; X is alkylene, NR10-23-2008
20090093488Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors - The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with an IGF-1R kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an IGF-1R kinase inhibitor, comprising assessing whether the tumor cell has undergone an epithelial to mesenchymal transition (EMT), by determining the expression level of epithelial and/or mesenchymal biomarkers, wherein tumor cells that have undergone an EMT are substantially less sensitive to inhibition by IGF-1R kinase inhibitors. Improved methods for treating cancer patients with IGF-1R kinase inhibitors that incorporate the above methodology are also provided. Additionally, methods are provided for the identification of new biomarkers that are predictive of responsiveness of tumors to IGF-1R kinase inhibitors. Furthermore, methods for the identification of agents that restore the sensitivity of tumor cells that have undergone EMT to inhibition by IGF-1R kinase inhibitors are also provided. pErk, HER3 and pHER are also demonstrated to be effective biomarkers for predicting sensitivity of tumor cells to IGF-1R kinase inhibitors.04-09-2009
20090203703Thienopyrimidine Derivatives - This invention provides thienopyrimidine derivatives of the formula,08-13-2009
20090197888FLUORINATED TRIPEPTIDE HCV SERINE PROTEASE INHIBITORS - The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof:08-06-2009
20090209543FOLATES, COMPOSITIONS AND USES THEREOF - The present invention relates to folates, compositions and uses thereof; In particular, this invention describes a crystalline or amorphous compound which is a substituted or unsubstituted folate or a reduced folate, or the natural or unnatural isomers thereof, of at least one organic base, as well as compositions and uses thereof. The compounds of the invention show a long lasting stability as well as a peculiarly high water-solubility.08-20-2009
20110144116DERIVATIVES OF (BRIDGED PIPERAZINYL)-1-ALKANONE AND USE THEREOF AS p75 INHIBITORS - The present invention relates to derivatives of ((phenyl)-3,6-dihydropyridin-1-yl)(bridged piperazinyl)-1-alkanone derivatives and ((phenyl)-2,5-dihydropyrrol-1-yl) (bridged piperazinyl)-1-alkanone corresponding to Formula (I):06-16-2011
20110144117Pharmaceutical Dosage Form Containing Tetrahydrobiopterin - Pharmaceutical dosage form comprising tetrahydrobiopterin, or a metabolic precursor thereof, comprising an aqueous solution of tetrahydrobiopterin, or a metabolic precursor thereof, and an antioxidant in a dispensing container and a dosing means for the dosed dispensation of the aqueous solution, as well as the use of an antioxidant for stabilizing an aqueous solution of tetrahydrobiopterin, or a metabolic precursor thereof, for a storage period of more than at least one month.06-16-2011
20090221594STABLE PHARMACEUTICAL COMPOSITIONS OF 5, 10 METHYLENETRAHYDROFOLATE - The invention provides a stable lyophilized composition of 5,10 methylenetetrahydrofolate suitable for use in the treatment of cancer and other therapies. The composition comprises 5,10-MTHF in combination with citric acid and ascorbic acid, with the ratio of citric acid to ascorbic acid from about 0.75:1 to about 2.25:1 by weight, and the ratio of total citric acid and ascorbic acid to 5,10-MTHF from about 1.4:1 to about 3.4:1 by weight. Prior to lyophilization, the solution is adjusted to an essentially neutral pH.09-03-2009
20090221593TRIAZOLE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS - The present invention relates to novel compounds of formula (I) or a salt thereof:09-03-2009
20090221591Selective Inhibitors of Human Corticosteroid Synthases - The invention relates to compounds for selectively inhibiting human corticosteroid synthases CYP1 1 B1 and CYP1 1 B2, and to the production and use thereof for treating hypercortisolism, diabetes mellitus, hyperaldosteronism, cardiac insufficiency, myocardial fibrosis, depression, age-related cognitive decline and metabolic syndrome.09-03-2009
20090221595Crystalline form of sitagliptin - A Sitagliptin crystalline form characterized by PXRD pattern having any 5 peaks selected from the group consisting of 7.4, 11.5, 16.7, 17.7, 18.9, 24.1, 24.5, 27.0, 28.5 and 28.8±0.2 degrees 2-theta, wherein any combination of peaks selected includes the peak at 7.4±0.2 degrees two theta, processes for preparing said Sitagliptin crystalline form, and pharmaceutical compositions thereof, are provided.09-03-2009
20100273802NEW PURINE DERIVATIVES HAVING, IN PARTICULAR, ANTI-PROLIFERATIVE PROPERTIES, AND THEIR BIOLOGICAL USES - This invention provides 2-, 6, and 9-substituted purine derivatives, particularly 2(1-R hydroxymethylpropylamino)-6-benzylamino-9-isopropyl purine, having, in particular, antiproliferative properties, and suitable for use as pharmaceutical compositions and herbicidal compositions. Also provided are pharmaceutical compositions and herbicidal compositions comprising the 2-, 6, and 9-substituted purine derivatives, and methods of treatment using the 2-, 6, and 9-substituted purine derivatives.10-28-2010
20100160330NOVEL BICYCLIC HETEROCYCLES USEFUL AS SELECTIVE ANDROGEN RECEPTOR MODULATORS - The present invention is directed to novel bicyclic heterocycles, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.06-24-2010
20100160329USE OF CONDENSED PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISEASES - The invention relates to the use of a compound of the formula (I), or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for use in modulating an immune or inflammatory response: wherein: Z=O or S; n=1-3; R06-24-2010
200901246282-benzylaminodihydropteridinones, process for their manufacture and use thereof as medicaments - The present invention relates to new 2-benzylaminodihydropteridinones of general formula (I)05-14-2009
20100152191CYCLOPROPYL PYRROLIDINE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to cyclopropyl proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.06-17-2010
20100160332a2-Adrenoceptor Ligands - The adrenergic receptors or adrenoceptors are a family of G-protein coupled receptors split into α and β subclasses. The adrenoceptors have important roles in regulating a myriad of physiological conditions and their malfunction has been implicated in the pathophysiology of a number of diseases. Disclosed herein are a series of novel compounds which are ligands of the alpha2-adrenoceptor (α06-24-2010
20090018139Treatment of CRTH2-mediated diseases and conditions - The present invention provides indole derivatives that antagonize prostaglandin D01-15-2009
20090018138Treatment of CRTH2-mediated diseases and conditions - The present invention provides indole derivatives that antagonize prostaglandin D01-15-2009
20090048262COMBINATION OF 10-PROPARGYL-10-DEAZAAMINOPTERIN AND ERLOTINIB FOR THE TREATMENT OF NON-SMALL CELL LUNG CANCER - The present invention relates to compositions comprising a combination of 10-propargyl-10-deazaminopterin and an EGFR Kinase inhibitor, including erlotinib, for treatment of non-small cell lung cancer, and methods of treatment for non-small cell lung cancer in a patient in need thereof comprising administering for combination of 10-propargyl-10-deazaminopterin and an EGFR Kinase inhibitor, including erlotinib, for treatment of non-small cell lung cancer.02-19-2009
20090298841QUINOLINE DERIVATIVES AND THEIR USE AS 5-HT6 LIGANDS - The present invention relates to novel quinoline compounds having pharmacological activity, to processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.12-03-2009
20090298838Method for Determination of Effective Dose of Methotrexate - Problems: Provided are a test method of determining an effective dose of methotrexate in each patient and a method for treatment of rheumatoid arthritis.12-03-2009
20100184773Germline Polymorphisms in the Angiogenic Pathway Predict Tumor Recurrence in Cancer Therapy - The invention provides compositions and methods for determining the likelihood of successful treatment with pyrimidine based antimetabolites and platinum-based alkylating agents. The methods comprise determining the identity of one or more genomic polymorphism present in a predetermined region of a gene of interest and correlating the polymorphism to the predictive response and treatment options. Patients identified as responsive are then treated with the appropriate therapy.07-22-2010
20100184772SULFONAMIDE SUBSTITUTED PYRAZOLINE COMPOUNDS, THEIR PREPARATION AND USE AS CB1 MODULATORS - The present invention relates to substituted pyrazoline compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.07-22-2010
20110201614CYCLIC GLYCYL-2-ALLYL PROLINE IMPROVES COGNITIVE PERFORMANCE IN IMPAIRED ANIMALS - Embodiments of this invention provide methods for therapeutic use of cyclic G-2-Allyl Proline to treat cognitive disorders as well as manufacture of medicaments including tablets, capsules, injectable solutions that are useful for treatment of such conditions.08-18-2011
20090298840Hydrates and polymorphs of 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pterid- inyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament - Disclosed are hydrates and polymorphs of 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, processes for preparing them and their use as pharmaceutical compositions.12-03-2009
20100261725COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.10-14-2010
20100160333NOVEL 3,9-DIAZABICYCLO[3.3.1]NONANE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - 3,9-diazabicyclo[3.3.1]nonane derivatives, useful as monoamine neurotransmitter re-uptake inhibitors. Also, use of these compounds in a method for therapy and in pharmaceutical compositions comprising the compounds. The 3,9-diazabicyclo[3.3.1]nonane derivatives have the formula06-24-2010
20100184774METHODS OF TREATMENT - This invention relates to a method of treating a disease state selected from: Alzheimer's disease, Down's syndrome, mental retardation, memory defects, memory loss, pancreatic cancer, bone resorption disease, osteoporosis, sickle cell anemia, chronic kidney disease, diabetes, depression, and subsets of depression including: alcoholism, anxiety, obsessive compulsive disorder, panic disorder, chronic pain, obesity, senile dementia, migraine, bulimia, anorexia, social phobia, pre-menstrual syndrome (PMS), adolescent depression, trichotillomania, dysthymia and substance abuse, in a mammal in need thereof, including a human, which comprises administering to such mammal a therapeutically effective amount of a selected substituted thiazol compound. The invention also relates to a method of enhancing cognition in a mammal in need thereof which comprises administering to such mammal a therapeutically effective amount of a selected substituted thiazol compound.07-22-2010
20110059976PYRIDO PYRIMIDINONES, DIHYDRO PYRIMIDO PYRIMIDINONES AND PTERIDINONES USEFUL AS RAF KINASE INHIBITORS - The present invention provides compounds having the formula:03-10-2011
20100216802PTERIDINE DERIVATIVES AS POLO-LIKE KINASE INHIBITORS USEFUL IN THE TREATMENT OF CANCER - Compound of formula (I) are inhibitors of Polo-like kinases (PLKs), and are useful in treatment of cell proliferative diseases:08-26-2010
20100179157THERAPEUTIC AGENT FOR CEREBRAL INFARCTION - The present invention provides a novel therapeutic drug for cerebral infarction, which contains a piperazine compound as an active ingredient.07-15-2010
20100240666FUSED PYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - Novel fused pyrazine compounds are disclosed that have a formula represented by the following:09-23-2010
20100216803ORNITHINE DERIVATIVE - Provided is a compound which is useful as a therapeutic agent for chronic renal insufficiency and a therapeutic agent for diabetic nephropathy.08-26-2010
20100216805MODULATION OF NEUROGENESIS USING D-CYCLOSERINE COMBINATIONS - The disclosure provides compositions and methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure provides compositions and methods based on the use of D-cycloserine in combination with the neurogenic agent, which synergistically stimulates or activates the formation of new nerve cells.08-26-2010
20100216801THIAZOLONES FOR USE AS PI3 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using substituted thiazolones. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of substituted thiazolones.08-26-2010
20100227867Compounds, Formulations, and Methods for Treating or Preventing Inflammatory Skin Disorders - In methods, compounds, and topical formulations for treatment of inflammatory skin disorders incorporating compounds represented by the formulas below:09-09-2010
20100216804Long Circulating Nanoparticles for Sustained Release of Therapeutic Agents - The present disclosure is directed in part to a biocompatible nanoparticle composition comprising a plurality of non-colloidal long circulating nanoparticles, each comprising a α-hydroxy polyester-co-polyether and a therapeutic agent, wherein such disclosed compositions provide a therapeutic effect for at least 12 hours.08-26-2010
20100240667CRYSTALLINE FORMS OF (6R)-L-ERYTHRO-TETRAHYDROBIOPTERIN DIHYDROCHLORIDE - Crystal forms of (6R)-L-erythro-tetrahydrobiopterin dihydrochloride, hydrates and solvates and processes for their preparation are provided. These crystal forms are either intermediates for the preparation of stable polymorphic form B or are suitable for solid formulations.09-23-2010
20090042891Pyrazine Derivatives Useful as Adenosine Receptor Antagonists - The present disclosure relates to a compound of formula (I)02-12-2009
20100130503NEW FLUORENE DERIVATIVES, COMPOSITIONS CONTAINING THE SAME AND USE THEREOF AS INHIBITORS OF THE PROTEIN CHAPERONE HSP 90 - The present invention relates to compounds of formula (I):05-27-2010
20130217694METHOD OF REDUCING THE SEVERITY OF INFLAMMATORY DERMATOLOGICAL CONDITIONS - The present invention provides a method of reducing the severity of one or more symptoms of an inflammatory dermatological condition in a subject, comprising topically administering to the skin of a subject in need of such reduction an effective amount of brimonidine or a pharmaceutically acceptable salt, ester, amide, stereoisomer or racemic mixture thereof.08-22-2013
20100113459Gene Polymorphisms as Predictors of Tumor Progression and Their Use in Cancer Therapy - The invention provides compositions and methods for determining the likelihood of successful treatment with a pyrimidine based antimetabolite chemotherapy drug and a platinum based chemotherapy drug, such as 5-FU/oxaliplatin. The methods comprise determining the genomic polymorphism present in a predetermined region of a gene of interest and correlating the polymorphism to the predictive response. Patients identified as responsive are then treated with the appropriate therapy.05-06-2010
20110112102METHOD OF TREATING CANCER USING A NEUROPEPTIDE Y 5R (NP Y5R) ANTAGONIST - The present invention relates to methods for treating cancer by administering a therapeutically effective amount of compound of formula (I), such as selective NPY5R antagonist MK-0557 (trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H), 1′-cyclohexane]-4′-carboxamide), or a pharmaceutically acceptable salt thereof, to a subject in need thereof The methods can further comprise administering a chemotherapeutic agent to the subject in need thereof.05-12-2011
20100222354AMPA Receptor Antagonists and Aldose Reductase Inhibitors for Neuropathic Pain - The invention provides methods for treating and/or preventing neuropathic pain by administering to patients therapeutically effective amounts of AMPA receptor antagonists and aldose reductase inhibitors. The neuropathic pain may be diabetic neuropathy. The invention also provides kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists and aldose reductase inhibitors. The AMPA receptor antagonists may be, for example, 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one. The aldose reductase inhibitor may be, for example, ranirestat.09-02-2010
20100222356Furazano '3, 4-B! Pyrazines and Their Use as Anti-Tumor Agents - The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.09-02-2010
20100222355QUINOLIZIDINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to spiropiperidine compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.09-02-2010
20080312243IMIDAZOLES AND TRIAZOLES, THEIR PREPARATION, AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to imidazoles and triazoles of general formula12-18-2008
20120142693CRYSTALLINE COMPOUND OF 7-[(3R)-3-AMINO-1-OXO-4-(2, 4, 5-TRIFLUORPHENYL)BUTYL]-5, 6, 7, 8-TETRAHYDRO-3-(TRI FLUORMETHYL)-1, 2, 4 -TRIAZOLO[4,3-A]PYRAZIN - A crystalline compound of 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine (INN: Sitagliptin) of formula 106-07-2012
20120142692ANTIFOLATE COMBINATIONS - The present invention provides combinations of active agents, such combinations comprising one or more antifolate compounds. The particularly can include methotrexate and one or more further antifolate compounds. In specific embodiments, the combinations are useful for treating certain conditions, such as rheumatoid arthritis. The invention also provides articles useful to provide the combinations in desirable dosage forms and combinations. The combinations further may be useful in the treatment of further conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis.06-07-2012
20110130404QUINOXALINEDIONE DERIVATIVES - The present invention relates to compounds of formula (I)06-02-2011
20110028483INDOLES, 1H-INDAZOLES, 1,2-BENZISOXAZOLES, AND 1,2-BENZISOTHIAZOLES, AND PREPARATION AND USES THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.02-03-2011
20100197694Compositions and methods for treatment of diseases and conditions with increased vascular permeability - The invention provides compositions and methods for treating diseases and conditions through reducing vascular permeability, selectively inhibiting VEGF-induced postcapillary venular leakage, and/or selectively reducing spread of viral and/or bacterial pathogens. The provided compositions and methods utilize low concentrations of selective α-2 adrenergic receptor agonists having a binding affinity of 300 fold or greater for α-2 over α-1 adrenergic receptors. The compositions preferably comprise brimonidine and/or dexmedetomidine.08-05-2010
20100197692BICYCLIC HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Bicyclic heteroaromatic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis.08-05-2010
20100197691SOLUBLE EPOXIDE HYDROLASE INHIBITORS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT - Compounds of the Formula: (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating hypertension, diabetes, inflammation, atherosclerosis, pain, and the like are disclosed. Pharmaceutical compositions and methods of use are also included.08-05-2010
20090286797Novel Quinoxaline Derivatives and Their Medical Use - This invention relates to novel quinoxaline derivatives having medical utility, to use of the quinoxaline derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the quinoxaline derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to positive modulation of AMPA receptor mediated synaptic responses.11-19-2009
20100197693NOVEL BENZENESULFONAMIDES AS CALCIUM CHANNEL BLOCKERS - The present application relates to calcium channel inhibitors comprising compounds of formula (I), formula (II), formula (III), or formula (IV),08-05-2010
20090221592Dodecylsulfate Salt Of A Dipeptidyl Peptidase-Iv Inhibitor - The dodecylsulfate salt of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-09-03-2009
20120245177CRYSTALLINE LEVOFOLINIC ACID AND PROCESS FOR ITS PREPARATION - The present invention relates to stable crystalline (6S)—N(5)-formyl-5,6,7,8-tetrahydrofolic acid, commonly referred to as levofolinic acid, in essentially pure 6S diastereomeric form, and to a process for its preparation.09-27-2012
20090318456SUBSTITUTED PTERIDINES FOR THE TREATMENT AND PREVENTION OF VIRAL INFECTIONS - Tri-substituted pteridines and tetra-substituted pteridines exhibit a significant and selective activity against certain types of viral infections, in particular they selectively inhibit the replication of the hepatitis C virus, and are useful for the prevention and treatment of such infections.12-24-2009
20090181974Composition for slowing down the development of alzheimer's disease - The invention relates to a composition comprising: vegetable oil containing at least one linoleic acid and at least one linolenic acid, vitamin E, and vitamin B9 (or folates), whereby the linoleic acid/linolenic acid weight ratio is between 3 and 5. The inventive composition is intended to slow down the development of Alzheimer's disease and to improve the patient's quality of life. Said composition is intended to be incorporated in a vector that can be assimilated by the human body, preferably by means of dietary intake.07-16-2009
20090111817Combinations of Eszopiclone and an Antidepressant - One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., menopause, mood disorders, anxiety disorders, or cognitive disorders. The first component of the pharmaceutical composition is a sedative eszopiclone. The second component of the pharmaceutical composition is an antidepressant. The present invention also relates to a method of treating menopause, perimenopause, mood disorders, anxiety disorders, and cognitive disorders.04-30-2009
20110039857PIPERIDINE AND PYROOLIDINE COMPOUNDS - The invention relates to piperidine and pyrrolidine compounds of formula (I)02-17-2011
20100298333COMBINATION THERAPY FOR THE TREATMENT OF DIABETES AND CONDITIONS RELATED THERETO AND FOR THE TREATMENT OF CONDITIONS AMELIORATED BY INCREASING A BLOOD GLP-1 LEVEL - The present invention concerns combination of an amount of a GPR119 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-1 level in a subject over that provided by the amount of the GPR119 agonist or the amount of the DPP-IV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-1 level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-1 secretagogues.11-25-2010
20130131073FUSED-IMIDAZOYL COMPOUNDS USEFUL AS ANTIMICROBIAL AGENTS - Disclosed are methods of treating microbial infections, comprising administering a compound of Formula (I) Formula I wherein R05-23-2013
20100298334N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS - The present invention relates to N-(hetero)aryl-pyrrolidine derivatives of Formula I:11-25-2010
20100305135AHCY HYDROLASE INHIBITORS FOR TREATMENT OF HYPER HOMOCYSTEINEMIA - The present invention is directed to AHCY inhibitors of formula (I) which are useful in the treatment of diseases characterized by high homocysteine levels, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases characterized by high homocysteine levels.12-02-2010
20100305134SPECIFIC INHIBITORS OF PTERIDINE REDUCTASE WITH ANTIPARASITIC ACTION - The processes for the preparation of alkyl derivatives of N-[4-(2,4-diaminopteridin-6-ylmethylamino)benzoyl]-N-piperidin-2-carboxylic acid and N-[4-(2,4-diaminopteridin-6-ylmethylamino)benzoyl]-N-piperidin-4-carboxylic acid and of N-[4-(2,4-diaminopteridin-6-ylmethylamino)benzoyl]-N-pyrrolidin-2-carboxylic acid and N-[4-(2,4-diaminopteridin-6-ylmethylamino)benzoyl]-N-pyrrolidin-4-carboxylic acid. Their specific properties of inhibition versus Pteridine reductase of parasitic species. The processes for the preparation of alkyl derivatives of 1[4-(quinoxalin-2-ylamino)benzoyl]piperidin-mono and di-carboxylic acid and alkyl derivatives of 1-[4-(quinoxalin-2-ylamino)benzoyl]pyrrolidin-mono and di-carboxylic acid. The specific properties of inhibition versus Pteridine reductase of parasitic species. The processes for the preparation of alkyl derivatives of 4-(6,7-dimethoxy-quinoxalin-2-ylmethoxy)benzoic acid and alkyl derivatives of 2-(phenylsulfanil)-quinoxalin-5,7-diamine and their specific properties of inhibition versus Pteridine reductase of bacterial species. The pharmaceutical composition and their use in the treatment and prevention of parasitic infections caused by 12-02-2010
201301376963,4-DIHYDRO-2H-PYRROLO[1,2-A]PYRAZIN-1-ONE DERIVATIVES FOR THE MODULATION OF THE ACTIVITY OF PROTEIN KINASES - Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.05-30-2013
20130143891Methods for Treating Methotrexate-Resistant Disorders with 10-Propargyl-10-Deazaaminopterin - The present invention relates to a method for treating a methotrexate-resistant disorder in an individual, wherein the method comprises administering to the individual an effective amount of 10-propargyl-10-deazaminopterin or its pharmaceutically acceptable salts.06-06-2013
20090036457Utilities of olefin derivatives - Compounds having an activity to enhance the expression of apoAI are provided. Compounds of formula (I):02-05-2009
20100324054AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES - The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.12-23-2010
20100009994L-Malate Salts of 6-(5-Chloro-2-Pyridyl)-5-[(4-Methyl-1-Piperazinyl)Carbonyloxy]-7-Oxo-6,7-- Dihydro-5H-Pyrrolo[3,4-b]Pyrazine - A novel L-malate salt of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) is provided.01-14-2010
20110039856POLYMORPHS OF A C-MET/HGFR INHIBITOR - This invention relates to polymorphs of 2-[4-(3-Quinolin-6-ylmethyl-3H-[1,2,3]triazolo[4,5-b]pyrazin-5-yl)-pyrazol-1-yl]-ethanol that are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to compositions including such salts and polymorphs, and to methods of using such compositions in the treatment of abnormal cell growth in mammals, especially humans.02-17-2011
20110034469Heterocyclic Compound - The present invention provides a compound represented by the formula02-10-2011
20110118268NOVEL 1,4-DIAZA-BICYCLO[3.2.1]OCTANE DERIVATIVES USEFUL AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS - This invention relates to novel 1,4-diaza-bicyclo[3.2.1]octane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. (formula)05-19-2011
20110245258NOVEL ANTIMICROBIALS - The present invention relates to novel phenyl oxazolidinone compounds of formula I, their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of formula I or their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of formula I and methods of using them. The compounds of the present invention are useful as antimicrobial agents, effective against a number of aerobic and/or anaerobic Gram positive and/or Gram negative pathogens such as multi drug resistant species of 10-06-2011
201101121035-HYDROXYPYRIMIDINE-4-CARBOXAMIDE COMPOUND - The present invention provides compounds which promote erythropoietin production. Compounds represented by the following general formula (1) or pharmacologically acceptable salts thereof are provided:05-12-2011
20110118271Kinase Inhibitors Useful For The Treatment Of Proliferative Diseases - The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferrably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.05-19-2011
20110245257HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.10-06-2011
20110245255PURINE COMPOUNDS - A compound of the formula:10-06-2011
20110118270HETEROCYCLIC DERIVATIVES THAT ARE USED IN THE TREATMENT OF NEURODEGENERATIVE DISEASES - The present invention relates to compounds of Formula (I) below, to their pharmaceutically acceptable salts and to their isomers or mixtures of isomers: HetAr—X—CHR05-19-2011
20100144744FUSED HETEROCYCLIC 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS - Novel compounds are provided which are 1 1-beta-hydroxysteroid dehydrogenase type I inhibitors. 1 1-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 1 1-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: W-L-Z or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, L are defined herein and Z is selected from the following bicyclic heteroaryl groups: (a), (b), (c), (d).06-10-2010
20100144745Pyrrolopyrazinyl Urea Kinase Inhibitors - The present invention relates to the use of novel pyrrolopyrazinyl urea derivatives of Formula I,06-10-2010
20090069333FUNGICIDES - This invention relates to novel derivatives of pyridopyrazines and pyridopyridazines, to processes for preparing them, to intermediate chemicals used in their manufacture, to compositions containing them and to methods of using them to combat fungi, especially fungal infections of plants. The fungicidal compounds have the general formula (1) wherein R, R03-12-2009
20100137322NOVEL N-(8-HETEROARYLTETRAHYDRONAPHTALENE-2YL) OR N-(5-HETEROARYLCHROMANE-3-YL) CARBOXAMIDE DERIVATIVES FOR THE TREATMENT OF PAIN - The present invention relates to new compounds of formula (I) and to pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof.06-03-2010
20120035181ANTIPARASITIC AGENT FOR FISH AND METHOD OF CONTROLLING PROLIFERATION OF FISH PARASITES - A method of controlling proliferation of fish parasites comprising the administration of 1 to 50 mg/kg fish body weight/day of an inhibitor of folate synthesis and/or an inhibitor of folate activation to fish continuously for 1 to 2 weeks. Using a combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is preferable, and a sulfonamide is preferable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist, etc., can be used as the inhibitor of folate activation. The antiparasitic agent is able to exterminate fish parasites via oral administration. It is particularly effective against parasites belonging to the ciliate group among fish parasites.02-09-2012
20100029658HETEROCYCLIC DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF - The present invention relates to novel quinoxaline, quinazoline and phthalazine derivatives as well as multimeric derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds for the treatment and prevention of brain damage resulting from brain injury, especially secondary brain damage due to traumatic brain injury (TBI). The compounds of the invention are also useful in treating and preventing neurodegenerative diseases.02-04-2010
20100216800Treatment of Type 2 Diabetes With a Combination of DPIV Inhibitor and Metformin or Thiazolidinedione - This invention relates to a therapeutic method for glycaemic control, in particular to a method for the treatment of type 2 diabetes, comprising the administration of a DPIV inhibitor together with metformin or a thiazolidinedione.08-26-2010
20110136815SOLID ORAL FILM DOSAGE FORMS AND METHODS FOR MAKING SAME - Improved pharmaceutical solid oral film dosage forms for the buccal and/or sublingual delivery of pharmaceutical, nutraceutical or cosmetic ingredients are endowed with instant hydration potential and complete dissolution potentially enabling the active ingredient to become immediately available for enhanced buccal and/or sublingual absorption and/or reduced absorption through the gastrointestinal route. The improved delivery systems for solubilizing and stabilizing pharmaceutically active ingredients exhibit enhanced stability by the use of a combination of crystallization inhibitors, which together can maintain the active ingredient in a desired plurality of particles in an effective size range within a polymeric film matrix.06-09-2011
20110245256USE OF A PKC INHIBITOR - The present invention demonstrates that chronic active BCR signaling through CD79A/B confers a strong dependence on downstream PKCb kinase signaling. Hence, provided herein is a method for inhibiting the growth of B-cell lymphoma having chronic active B-cell-receptor signaling, or inhibiting the growth of cancers with molecular lesions that lead to chronic active BCR signaling, by administering to a patient in need of such treatment a therapeutically effective amount of a PKC inhibitor or a use of a PKC inhibitor to inhibit the growth of B-cell lymphoma having chronic active B-cell-receptor signaling or to inhibit the growth of cancers with molecular lesions that lead to chronic active BCR signaling.10-06-2011
20090312336DIHYDROPTERIDINE COMPOUNDS AS ANTI PROLIFERATIVE AGENTS - Compounds of formula (I), or optionally the pharmacologically acceptable acid addition salts thereof, and their use in the inhibition of PLK activity are described.12-17-2009
20110152271Compositions and methods for ophthalmic delivery of nasal decongestants - The invention provides compositions and methods for treating nasal congestion through ophthalmic delivery. The provided compositions and methods utilize low concentrations of selective α-2 adrenergic receptor agonists. The compositions preferably include brimonidine.06-23-2011
200900364563,9-DIAZABICYCLO[3.3.1]NONANE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - This invention relates to novel 3,9-diazabicyclo[3.3.1]nonane derivatives useful as monoamine neurotransmitter re-uptake inhibitors.02-05-2009
20100056531ALKYL-SUBSTITUTED 3' COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY - The present disclosure provides compounds having affinity for the 5-HT03-04-2010
20100056530GLUCOKINASE ACTIVATORS - Provided are compounds of Formula I wherein R03-04-2010
20110178091ARYLPIPERAZINE-CONTAINING PYRROLE 3-CARBOXAMIDE DERIVATIVES FOR TREATING DEPRESSIVE DISORDERS - The present invention relates to novel arylpiperazine-containing pyrrole 3-carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof which is useful for preventing or treating depressive disorders. The present invention also provides a method for preparing the arylpiperazine-containing pyrrole 3-carboxamide derivatives or the pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating depressive disorders.07-21-2011
201101780894-PHENOXY-NICOTINAMIDE OR 4-PHENOXY-PYRIMIDINE-5-CARBOXAMIDE COMPOUNDS - This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula07-21-2011
2010005653318F-LABELLED FOLATES - The present invention is directed towards new 03-04-2010
20090170858Methods and Compositions Containing Natural Folates for Protecting Against Radiation Damage - Disclosed are methods for protecting a subject from harmful effects of ionizing radiation. The method includes administering to the subject an effective amount of at least one reduced folate. Also disclosed are radioprotective compositions that include a first radioprotective agent and a second radioprotective agent, where the first radioprotective agent is a reduced folate. Methods for protecting a subject from harmful effects of ultraviolet radiation are also disclosed.07-02-2009
20090215785Pyrrolopyrazine kinase inhibitors - The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I,08-27-2009
20090215784Maleate Salts of 6-(5-Chloro-2-Pyridyl)-5-[(4-Methyl-1-Piperazinyl)Carbonyloxy]-7-oxo-6,7-- dihydro-5H-Pyrrolo[3,4-b]Pyrazine - A novel maleate salt of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) is provided.08-27-2009
20100063057COMPOSITIONS AND METHODS FOR DELIVERY OF ANTI-CANCER AGENTS - The present invention relates to compositions comprising 5-fluorouracil, or a pharmaceutically acceptable salt or analogue thereof, folinic acid, or a pharmaceutically acceptable salt thereof and a cyclodextrin, or a pharmaceutically acceptable salt or derivative thereof. The invention also relates to methods for the treatment of cancer using such compositions.03-11-2010
20100069393METHOD OF TREATMENT AND AGENTS USEFUL FOR SAME - The present invention relates generally to therapeutic agents, formulations comprising them and their use in the treatment, amelioration and/or prophylaxis of glioma brain tumours and related conditions. The therapeutic agent comprises two fused 6-membered rings with at least a nitrogen at position 1 and a hydroxyl at position 8.03-18-2010
20110082149METABOLICALLY INERT ANTIFOLATES FOR TREATING DISORDERS OF ABNORMAL CELLULAR PROLIFERATION AND INFLAMMATION - The present invention provides compositions and methods for the treatment of disorders of abnormal cell proliferation and/or inflammation, such as psoriasis and inflammatory bowel disease, in a human or other host animals.04-07-2011
20100249140SOLID STATE FORMS OF SITAGLIPTIN SALTS - Solid state forms of Sitagliptin salts, processes for preparing the solid state forms, and pharmaceutical compositions thereof, are provided.09-30-2010
20110152272Treatment Of Incontinence - The present invention relates to the use of agonists of 5-HT2C receptors for the treatment of urinary incontinence, preferably mixed incontinence or stress urinary incontinence. The invention also relates to the use of antagonists of 5-HT2C receptors for the treatment of urine retention. The present invention also relates to a method of treatment of incontinence, to assays to screen for compounds useful in the treatment of incontinence, and to methods of preparing compositions for the treatment of urinary incontinence.06-23-2011
20110251200ARYL GUANIDINE F1F0-ATPASE INHIBITORS AND RELATED METHODS - The invention provides to a family of aryl guanidine-based F10-13-2011
20110098307CRYSTALLINE OF ESZOPICLONE, ITS COMPOSITION, PREPARATION AND USES THEREOF - The present invention discloses a crystalline form of S-zopiclone having a powder X-Ray diffraction spectrum excited by Cu-Ka radiation with characteristic peaks expressed in terms of 28 at about 11.08°, about 12.38°, about 15.86°, about 17.88°, about 19.98° and about 20.58°; a DSC thermogram with a peak at about 207.7° C. and an infrared absorption spectrum (IR) with characteristic peaks at about 3078 cm04-28-2011
20110098306Uses of tetrahydrobiopterin, sepiapterin and derivatives thereof - The present invention discloses that diabetic rats showed a reduction in nitrergic relaxation of the gastric, impaired nNOS dimerization, decreased BH4 and GTPCH1 levels and thus, are more susceptible to develop diabetic gastroparesis. The use of tetrahydrobiopterin and its derivatives and sex steroid hormones as disclosed herein provides a novel strategy for therapeutic intervention of diabetic gastroparesis and any other gut-related diseases. Additionally, the present invention also discloses methods to determine risk of developing gastroparesis in an individual that are drawn to detecting variations in the activity and levels of GCH gene and in gene encoding sex steroid hormone receptor.04-28-2011
20090088437INDOLES, 1H-INDAZOLES, 1,2-BENZISOXAZOLES, AND 1,2-BENZISOTHIAZOLES, AND PREPARATION AND USES THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.04-02-2009
20110046145Quinolizidinone M1 Receptor Positive Allosteric Modulators - The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.02-24-2011
20100130502Compounds, Formulations, and Methods for Treating or Preventing Inflammatory Skin Disorders - In methods, compounds, and topical formulations for treatment of inflammatory skin disorders incorporating compounds represented by the formulas below:05-27-2010
20110152279MACROCYCLIC INDOLE DERIVATIVES USEFUL AS HEPATITIS C VIRUS INHIBITORS - Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein Y, R06-23-2011
20110152275AGENT FOR MAINTENANCE OF INDUCED REMISSION - Disclosed is a method for maintaining induced remission of an immune disease, which can alleviate or reduce any serious side effect and the burdens exerted on a patient suffering from the same. The method comprises carrying out the remission induction for an immune disease by the use of a biological agent or a nucleic acid synthesis-inhibitory agent and then using an agonist for sphingosine-1-phosphate receptor to the patient.06-23-2011
20110152270SUBSTITUTED TETRAZOL-1-YL-PHENOXYMETHYL-THIAZOL-2-YL-PIPERIDINYL-PYRIMIDINE SALTS - Crystalline salts of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine, compositions thereof, methods for their preparation, and methods for their use are disclosed.06-23-2011
20110071154PYRROLIDIN-3-YLMETHYL-AMINE AS OREXIN ANTAGONISTS - The present invention is concerned with novel sulfonamides of formula I03-24-2011
20110251201Sustained release intraocular implants and methods for preventing retinal dysfunction - Biocompatible intraocular implants include an alpha-2 adrenergic receptor agonist and a polymer associated with the alpha-2 adrenergic receptor agonist to facilitate release of the alpha-2 adrenergic receptor agonist into an eye for an extended period of time. The alpha-2 adrenergic receptor agonist may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants may be placed in an eye to prevent the occurrence of one or more ocular conditions, or to reduce one or more symptoms of an ocular condition, such as an ocular neurosensory disorder and the like.10-13-2011
20090023741ARYL/HETARYLAMIDES AS MODULATORS OF THE EP2 RECEPTOR - The present invention relates to aryl/hetarylamide derivatives of the general formula I, process for their preparation, and the use thereof for the manufacture of pharmaceutical compositions for the treatment of disorders and indications connected with the EP01-22-2009
20110257189PYRROLOPYRAZINONE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts,10-20-2011
20080249100PTERIDINONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses pteridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I:10-09-2008
20110152278SYNTHESIS AND ANTI-PROLIFERATIVE EFFECT OF BENZIMIDAZOLE DERIVATIVES - This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated.06-23-2011
201102512021,3-Dihydro-imidazo[4,5-c]quinolin-2-ones as Lipid Kinase Inhibitors - The invention relates to novel organic compounds of formula (I)10-13-2011
20110212971DIKETO FUSED AZOLOPIPERIDINES AND AZOLOPIPERAZINES AS ANTI-HIV AGENTS - Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketo fused azolopiperidine and azolopiperazine derivatives that possess unique antiviral activity are provided. These compounds are useful for the treatment of HIV and AIDS.09-01-2011
20100099684Quinuclidine Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.04-22-2010
20110178090SUBSTITUTED-QUINOXALINE-TYPE BRIDGED-PIPERIDINE COMPOUNDS AND THE USES THEREOF - Compounds of Formula (I):07-21-2011
20110152277HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.06-23-2011
20110152274Preparations and Methods for Ameliorating or Reducing Presbyopia - This application relates to the use of one or more parasympathomimetic drugs in combination with one or more alpha agonists to create optically beneficial miosis to, for example, temporarily treat presbyopia. The invention provides a pharmaceutical preparation comprising a therapeutically effective amount of one or more parasympathomimetic drugs or cholinesterase inhibitors, or a pharmaceutically acceptable salt thereof, in combination with one or more alpha agonists or antagonists, or a pharmaceutically acceptable salt thereof. The invention further provides for a method for treating, ameliorating or reducing presbyopia of a patient having an eye, comprising administering to said eye a pharmaceutically effective amount of the ophthalmic preparation.06-23-2011
20120202820PHARMACEUTICAL COMPOSITION HAVING THE ACTIVE SUBSTANCES METFORMIN AND SITAGLIPTIN OR VILDAGLIPTIN - The present invention relates to a pharmaceutical composition that comprises the active substance metformin in combination with one of the active substances sitagliptin or vildagliptin. The present invention further relates to a method of production of said pharmaceutical composition.08-09-2012
20090253706Methods and Compositions for the Treatment of Rheumatoid Arthritis and Other Inflammatory Diseases - Compositions and methods for the treatment of inflammatory diseases are disclosed.10-08-2009
20120277238PHARMACEUTICAL COMPOSITION CONTAINING FUSED HETERO-RING DERIVATIVE - The present invention provides a compound which indicates a histamine H4 receptor modulating activity.11-01-2012
20080306074Compositions Comprising Addl Receptors, Related Compositions, and Related Methods - Disclosed and claimed herein are compositions comprising ADDL receptors, related compositions, and related methods. ADDL receptors are typically, but perhaps not exclusively, localized at the post-synaptic density (PSD) of neuronal cells. Related compositions include, but are not limited to, compounds that affect, positively or negatively, ADDL binding to neuronal cells, either via one or more receptors localized at the post-synaptic density (PSD) or otherwise. Related methods include, but are not limited to, procedures to screen for compounds that affect, either positively or negatively, ADDL binding to neuronal cells, either via one or more receptors localized at the post-synaptic density (PSD) or otherwise. Other related methods include, but are not limited to, prevention and treatment of ADDL-related diseases, such as Alzheimer's disease, mild cognitive impairment, Down's syndrome, and the like, using compositions that inhibit, block, or otherwise interfere with ADDL binding to one or more receptors localized at the post-synaptic density of neuronal cells.12-11-2008
20110257188Compositions and methods for the treatment of nasal conditions - The invention provides compositions and methods for treating nasal congestion. The provided compositions and methods utilize low concentrations of selective α-2 adrenergic receptor agonists. The compositions preferably include brimonidine.10-20-2011
20110288095THIOPHENE-CARBOXAMIDES USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.11-24-2011
20080214550Novel inhibitors of folic acid-dependent enzymes - The invention relates to compounds of the formula I, or pharmaceutically acceptable salts thereof:09-04-2008
20100311760HETEROCYCLIC ANTIVIRAL COMPOUNDS - Compounds having the formula I wherein12-09-2010
20080255131N-(HETEROARYL)-1H-INDOLE-2-CARBOXAMIDE DERIVATIVES AND THEIR USE AS VANILLOID TRPV1 RECEPTOR LIGANDS - The invention concerns therapeutic uses of compounds of general formula (I), wherein n, X10-16-2008
20100331337Quercetin-Containing Compositions - This invention relates to a composition containing quercetin, vitamin B3, vitamin C, and folic acid. Also disclosed is a method of using the composition for enhancing physical or mental performance or treating various diseases or disorders.12-30-2010
20100331336PROTECTIVE EFFECT OF HIGH DOSE FOLATE ON MYCARDIAL ISCHEMIA - The present invention relates to the use of high dose of folic acid, or an equivalent dose one of its biological active derivatives to blunt myocardial dysfunction during ischemia and to ameliorate post-reperfusion injury. The invention specially relates to an early treatment by the application of a high dose of at least 200 mg folic acid, or an equivalent dose of a derivative during active ischemia, before the reperfusion.12-30-2010
20080207624Therapeutic Agent for Bh4-Responsive Hyperphenylalaninemia - A pharmaceutical preparation containing sapropterin hydrochloride can be used to administer sapropterin hydrochloride, an effective therapeutic agent for the treatment of tetrahydrobiopterin-responsive hyperphenylalaninemia, to patients of a wide range of ages, ranging from infants to adults, in a single preparation. One specific example is a pharmaceutical preparation for the treatment of BH4-responsive hyperphenylalaninemia provided in the form of granule, fine granule, or dry syrup, comprising sapropterin hydrochloride as an active ingredient; a flavoring agent; a coloring agent which is stable to acid and oxidation; and ascorbic acid or L-cysteine hydrochloride as a stabilizer, wherein the preparation has a moisture content (weight loss on drying) of 0.9% or less. Also provided is the pharmaceutical preparation in which the amount of sapropterin hydrochloride is from 2.5 to 20 wt %.08-28-2008
20110053946Aryl-Quinolyl Compounds and Their Use - The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain aryl-quinolyl compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.03-03-2011
20110053944SUBSTITUTED DIHYDROPTERIDIN-6-ONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS - Dihydropteridin-6-one derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.03-03-2011
20110028482ISOXAZOLINES AS INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provides isoxazoline FAAH inhibitors of the formula (I):02-03-2011
20100286153COMBINATION THERAPY FOR THE TREATMENT OF DIABETES AND CONDITIONS RELATED THERETO AND FOR THE TREATMENT OF CONDITIONS AMELIORATED BY INCREASING A BLOOD GLP-1 LEVEL - The present invention concerns combination of an amount of a GPR119 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-1 level in a subject over that provided by the amount of the GPR119 agonist or the amount of the DPP-IV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-1 level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-1 secretagogues.11-11-2010
20110112100Hepatitis C Virus Inhibitors - The present invention relates to compounds of the formula (I)05-12-2011
20120302575Methods for Preventing Oxidative Stress Injury of a Tissue by a Folate-Tempol Conjugate. - The present disclosure is generally related to methods of preventing oxidative stress injury induced by renal is-chemia-reperfusion by a Folate-TEMPOL conjugate.11-29-2012
20120302574Methods of Preventing and Reducing the Severity of Stress-Associated Conditions - The present invention provides a method of preventing or reducing the severity of a stress-associated condition in a subject by systemically administering to the subject an effective amount of brimonidine or a pharmaceutically acceptable salt, ester, amide, sterioisomer or racemic mixture thereof. Stress-associated conditions that can be treated according to a method of the invention include, but are not limited to, dyspepsia, tachycardias other than tachycardia associated with myocardial ischemia, panic attack, non-inflammatory dermatogical conditions, disorders of muscle contraction, sensory hypersensitivity associated with migraine, and behavioral disorders.11-29-2012
20120302573METHODS OF INHIBITING PRO MATRIX METALLOPROTEINASE ACTIVATION - This invention relates to methods for preventing, treating or ameliorating an MMP9 and/or MMP13 mediated syndrome, disorder or disease comprising administering to a subject in need thereof an effective amount of a compound listed in the examples section of this specification, or a form, composition or medicament thereof. Disorders treated and/or prevented include rheumatoid arthritis.11-29-2012
20120302572USE OF EMT GENE SIGNATURES IN CANCER DRUG DISCOVERY, DIAGNOSTICS, AND TREATMENT - The present invention provides diagnostic methods for assessing the EMT status of tumor cells, and for predicting the effectiveness of treatment of a cancer patient with an EGFR or IGF-1R kinase inhibitor, utilizing an EMT gene signature index score. The present invention further provides methods for treating patients with cancer that incorporate these methods.11-29-2012
20100324050INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.12-23-2010
20100324052NOVEL PIPERIDINE CARBOXYLIC ACID AMINE DERIVATIVES - The invention relates to novel piperidine carboxylic acid amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of these novel compounds, pharmaceutical compositions comprising such compounds and especially the use of such compounds as inhibitors of renin.12-23-2010
20100324051NOVEL COMPOUNDS AS OPIOID RECEPTOR MODULATORS - The present invention is directed to novel opioid receptor modulators of Formula (I).12-23-2010
20100179156Antimicrobial compositions - The present invention is directed to providing antimicrobial surfaces containing 1,4-diazoniabicyclo[2.2.2]octane and hydrocarbon groups and/or chains. More specifically, the present invention is directed to antimicrobial compositions wherein the hydroxyl groups on polyols are replaced by 1,4-diazoniabicyclo[2.2.2]octane. The invention is also directed to methods of making antimicrobial compositions containing polyols.07-15-2010
20100113462SUBSTITUTED BENZOYLAMINO-INDAN-2-CARBOXYLIC ACIDS AND RELATED COMPOUNDS - The present invention relates to novel compounds of the formula I:05-06-2010
20100113463PTERIDINONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses pteridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I:05-06-2010
20110190307Assay - The present invention provides zebrafish based methods for the identification of compounds potentially useful in the treatment of motor neuron degenerative diseases (MNDDs), compounds identified by these methods and compositions, methods and medicaments for treating MNDDs.08-04-2011
20110190306Inhibitors of PLK - Compounds of formula (I) are PLK inhibitors, useful for the treatment of cell proliferative diseases: wherein R08-04-2011
20090186899Substituted Sulfonamide Compounds - Substituted sulfonamide compounds corresponding to the formula I07-23-2009
20100190798PHARMACEUTICAL COMPOSITION COMPRISING RACEMIC AMINOPTERIN - There is disclosed a pharmaceutical composition comprising racemic aminopterin or pharmaceutically acceptable salts thereof. There is further disclosed a method to treat a disorder in a patient comprising administering a therapeutically effective amount of racemic aminopterin or pharmaceutically acceptable salts of racemic aminopterin. More particularly, there is disclosed a method for treating disorders modulated by at least dihydrofolate reductase activity, such as cancers and inflammatory disorders, wherein the method comprises administering to a patient in need thereof a therapeutically effective amount of racemic aminopterin or a pharmaceutically acceptable salt thereof.07-29-2010
20110190308NOVEL CYCLIC AZABENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS - The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.08-04-2011
20110190305Optically Pure Diastereomers of 10-Propargyl-10-Deazaaminopterin and Methods of Using Same - The present invention relates to diastereomers of 10-propargyl-10-deazaminopterin, compositions comprising optically pure diastereomers of 10-propargyl-10-deazaminopterin, in particular the two (R,S) diastereomers about the C10 position. Methods of preparation of these diastereomers, compositions containing them, and their use for the treatment of conditions related to inflammatory disorders and cancer are also disclosed.08-04-2011
20100137326NOVEL 4-CYANO, 4-AMINO, AND 4-AMINOMETHYL DERIVATIVES OF PYRAZOLO[1,5-a]PYRIDINES, PYRAZOLO[1,5-c]PYRIMIDINES AND 2H-INDAZOLE COMPOUNDS AND 5-CYANO, 5-AMINO, AND 5-AMINOMETHYL DERIVATIVES OF IMIDAZO[1,2-a]PYRIDINES, AND IMIDAZO[1,5-a]PYRAZINES AS CYCLIN DEPENDENT KINASE INHIBITORS - In its many embodiments, the present invention provides a novel class of 4-cyano, 4-amino, and 4-aminomethyl derivatives of pyrazolo[1,5-a]pyridine, pyrazolo[1,5-c]pyrimidine, and 2H-Indazole compounds and 5-cyano, 5-amino, and 5-aminomethyl derivatives of imidazo[1,2-a]pyridine and imidazo[1,5-a]pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.06-03-2010
20110152276SUBSTITUTED PYRROLO[2,3-D]PYRIMIDINES AS ANTIFOLATES - The present invention is directed to antifolate compounds having the structure06-23-2011
20100063055CONDENSED TETRAHYDROQUINOLINE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES - The problem of the present invention is to provide a compound having a GR selective binding activity, which shows less action on other nuclear receptors such as progesterone receptor (PR), mineralocorticoid receptor (MR) and the like. The present invention provides a condensed tetrahydroquinoline compound represented by the following formula (I)03-11-2010
20100029663Compositions and methods for reducing activation of alpha-1 receptors - The invention generally relates to compositions and methods for reducing activation of a-1 adrenergic receptors. The compositions comprise highly selective a-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.02-04-2010
20100029664PYRROLIDIN-3-YLMETHYL-AMINE AS OREXIN ANTAGONISTS - The present invention is concerned with novel sulfonamides of formula I02-04-2010
20100029662Vasoconstriction compositions and methods of use - The invention generally relates to compositions for inducing vasoconstriction. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.02-04-2010
20100029661Anesthetic compositions and methods of use - The invention generally relates to anesthetic compositions comprising low doses of a selective a-2 adrenergic receptor agonists in combination with anesthetic agents. The invention also relates to methods of using these compositions; in particular, the use of these compositions in humans to enhance the efficacy of a local peripheral anesthetic injection. The compositions and the methods are particularly useful in regional block anesthetic injections, and more particularly, in dental anesthetic injections.02-04-2010
20100029659Preferential vasoconstriction compositions and methods of use - The invention generally relates to compositions and methods for preferential vasoconstriction of smaller blood vessels relative to larger blood vessels. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.02-04-2010
20100029657Bridged, Bicyclic Heterocyclic or Spiro Bicyclic Heterocyclic Derivatives of Pyrazolo[1, 5-A]Pyrimidines, Methods for Preparation and Uses Thereof - Compounds of formula A:02-04-2010
20100029660Compositions and methods for reversing rebound hyperemia - The invention generally relates to compositions and methods for inducing vasoconstriction with low incidence of rebound hyperemia. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.02-04-2010
20110218203TREATMENT OF RHEUMATOID ARTHRITIS WITH A COMBINATION OF LAQUINIMOD AND METHOTREXATE - This invention provides a method of treating a subject afflicted with rheumatoid arthritis comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof and an amount of methotrexate, wherein the amounts when taken together are effective to treat the subject. This invention also provides laquinimod or pharmaceutically acceptable salt thereof for use in combination with methotrexate in treating a subject afflicted with rheumatoid arthritis. This invention also provides a pharmaceutical composition comprising an amount of laquinimod or pharmaceutically acceptable salt thereof and an amount of methotrexate for use in treating a subject afflicted with rheumatoid arthritis.09-08-2011
20100016326CONCENTRATED METHOTREXATE SOLUTIONS - Concentrated methotrexate solutions are described which are suitable for the use of an active substance in the production of a parenterally administered medicament for the treatment of inflammatory autoimmune diseases. The methotrexate is added to a pharmaceutically acceptable solvent at a concentration of more than 25 mg/ml. The invention also relates to a ready-made syringe and a carpule containing such a pharmaceutical solution formulation, as well as a pen injector comprising such a carpule and/or a ready-made syringe.01-21-2010
20100016328PTERIN ANALOGS - Disclosed herein are analogs of tetrahydrobiopterin, compositions containing the same, and methods of treating an individual suffering from a condition responsive to tetrahydrobiopterin by administration of the analog. These analogs are contemplated for use wherever tetrahydrobiopterin is currently used to treat conditions responsive to tetrahydrobiopterin therapies.01-21-2010
20100016327QUINOLINE COMPOUNDS - [Object] To provide a novel LXRβ agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease.01-21-2010
20110053945SALTS OF 6-(5-CHLORO-2-PYRIDYL)-5-[(4-METHYL-1-PIPERAZINYL)CARBONYLOXY]-7-- OXO-6,7-DIHY-DRO-5H-PYRROLO[3,4-B]PYRAZINE - Novel mesylate, (R)-mandelate, succinate, citrate, fumarate, D-malate, D-tartrate, sulfate and L-tartrate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.03-03-2011
20090105265Pharmaceutical Compositions of Combinations of Dipeptidyl Peptidase-4 Inhibitors With Metformin - Disclosed are pharmaceutical compositions comprising fixed-dose combinations of a dipeptidyl peptidase-4 inhibitor and metformin, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes with such pharmaceutical compositions.04-23-2009
20100120776Carbocysteine medical foods - Medical foods containing carbocysteine and designed for buccal absorption; useful for treating conditions that benefit from administration of an antioxidant, immunostimulant, and/or mucoregulator, such as COPD.05-13-2010
20100240665BIOLOGICAL MARKERS PREDICTIVE OF ANTI-CANCER RESPONSE TO INSULIN-LIKE GROWTH FACTOR-1 RECEPTOR KINASE INHIBITORS - The present invention provides diagnostic methods for predicting the effectiveness of treatment of a cancer patient with an IGF-1R kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an IGF-1R kinase inhibitor, comprising assessing whether the tumor cell expresses certain sensitivity or resistance biomarkers, or genomic classifiers. Improved methods for treating cancer patients with IGF-1R kinase inhibitors that incorporate this methodology are also provided.09-23-2010
20090312337COMPOSITIONS CONTAINING ALPHA-2-ADRENERGIC AGONIST COMPONENTS - Compositions useful for improving effectiveness of alpha-2-adrenergic agonist components include carrier components, alpha-2-adrenergic agonist components, solubility enhancing components which aid in solubilizing the alpha-2-adrenergic agonist components. In one embodiment, the alpha-2-adrenergic agonist components include alpha-2-adrenergic agonists. In another embodiment, the solubility enhancing components include carboxymethylcellulose.12-17-2009
20110118269FUSED PYRAZINE COMPOUNDS AS THEIR SALTS, USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - Novel salts of a [1.2.4]triazolo[1,5-a]pyrazine compound according to Formula I:05-19-2011
20090192166METHOD FOR AUGMENTING THE EFFECTS OF SEROTONIN REUPTAKE INHIBITORS - A method of treating a subject for a serotonergic neurotransmission dysregulation disorder, comprises administering the subject a serotonin enhancer (e.g., a serotonin reuptake inhibitor) in an amount effective to treat the disorder; and concurrently administering the subject 5-hydroxytryptophan in an amount effective to enhance the activity of the serotonin enhancer, (e.g., serotonin reuptake inhibitor). In preferred embodiments the disorder is depression, anxiety, or substance abuse.07-30-2009
20080312241Cicletanine and PKC inhibitors in the treatment of pulmonary and cardiac disorders - Embodiments of the present invention are related to novel therapeutic drugs, drug combinations, and associated methods for treating or preventing pulmonary disease, including pulmonary hypertension, pulmonary fibrosis, asthma and COPD, and heart failure, together with other pulmonary and cardiovascular diseases and their complications. More particularly, aspects of the present invention are related to the use of cicletanine and ruboxistaurin as monotherapies or in combination with other agents for treatment of disease. Cicletanine may be used as pure (+) or (−) enantiomers or as a racemic or non-racemic mixture of those enantiomers.12-18-2008
20100190797CRYSTALLINE POLYMOPHIC FORMS OF ZOPICLONE, PROCESSES FOR THEIR PREPARATION AND THEIR PHARMACEUTICAL COMPOSITIONS - Disclosed are processes for the preparation of crystalline polymorphic forms of zopiclone and their pharmaceutical compositions for use as a sedative.07-29-2010
20100120777Treatment of T-Cell Lymphoma using 10-propargyl-10-deazaaminopterin - T cell lymphoma is treated by administering to a patient suffering from T cell lymphoma a therapeutically effective amount of 10-propargyl-10-deazaaminopterin. Remission is observed in human patients, even with drug resistant T cell lymphoma at weekly dosages levels as low as 30 mg/m05-13-2010
20100286154ANTIHELMINTIC PASTE - The present invention is concerned with an anthelmintic paste in form of an aqueous suspension, comprising a veterinarily effective amount each of praziquantel and a macrocyclic lactone selected from avermectins, milbemycins and derivatives thereof; a cyclodextrin; a thickener; and water. The suspension formulations of the present invention are useful for controlling endoparasites in warm-blooded animals such as companion animals.11-11-2010
20110152273FUSED HETEROAROMATIC PYRROLIDINONES - Disclosed are compounds of Formula 1,06-23-2011
20090076014Methods of Administering Tetrahydrobiopterin, Associated Compositions, And Methods of Measuring - The present invention is directed to treatment methods of administering tetrahydrobiopterin, including in oral dosage forms, in intravenous formulations, and with food. Also disclosed herein are biopterin assays for measuring the amount of biopterin and metabolites of biopterin in a sample.03-19-2009
20100227868TREATMENT METHODS WITH BRIMONIDINE - Disclosed herein are therapeutic methods related to brimonidine.09-09-2010
20090325969METHOTREXATE ADJUVANTS TO REDUCE TOXICITY AND METHODS FOR USING THE SAME - Methods are provided for using methotrexate (MTX) active agents in which reduced host toxicity is observed. Aspects of the methods include administering to a subject an effective amount of an MTX active agent in conjunction with a MTX toxicity-reducing adjuvant, such as a 2,2′-anhydropyrimidine, a derivative thereof or a uridine phosphorylase inhibitor. Also provided are compositions and kits that find use in practicing embodiments of the invention. The methods and compositions find use in a variety of applications, including the treatment of a variety of different disease conditions.12-31-2009
20120040988DERIVATIVES OF 6,7-DIHYDRO-3H-OXAZOLO[3,4-a]PYRAZINE-5,8-DIONE - The present invention describes a series of derivatives of 6,7-dihydro-3H-oxazolo[3,4-a]pyrazine-5,8-dione, mixtures thereof, their pharmaceutically acceptable salts, which are inhibitors of PDE-5, possessing vasodilatator properties and relaxing effects. In particular, the derivative (R)-3-(1,3-benzodioxol-5-yl)-1-(1H-indol-3-yl)-7-methyl-6,7-dihydro[1,3]oxazolo[3,4-a]pyrazine-5,8-dione, its enantiomer (S)-3-(1,3-benzodioxol-5-yl)-02-16-2012
201200409892-HYDROXYETHYL-1H-QUINOLIN-2-ONE DERIVATIVES AND THEIR AZAISOSTERIC ANALOGUES WITH ANTIBACTERIAL ACTIVITY - The invention relates to antibacterial compounds of formula I02-16-2012
20080207625Synthesis and Purification of Pteroic Acid and Conjugates Thereof - Methods for purifying pteroic acid, analogs of pteroic acid, and derivatives of pteroic acid are described. Methods for synthesizing and purifying conjugates of vitamins, including FITC conjugates of folic acid, folic acid analogs, and derivatives of folic acid and folic acid analogs are also described. Purified forms of pteroic acid, derivatives and analogs of pteroic acid, and conjugates thereof are also described.08-28-2008
201101055145,6,7,8-TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE COMPOUNDS - The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I) wherein R05-05-2011
20110105513AMINO-QUINOXALINE AND AMINO-QUINOLINE COMPOUNDS FOR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS - Compounds of the Formula (I), where W represents CH or N; and Q represents —CN, —C(═NOH)NH05-05-2011
20120208821ALPHA ADRENERGIC RECEPTOR MODULATORS - Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor. The compounds can include a naphthalene, a quinoline, a benzoimidazole or an isoquinoline as a core structure. Methods of making, using and formulating these compounds are described.08-16-2012
20090030003AMINO-HETEROCYCLIC COMPOUNDS - The invention provides PDE9-inhibiting compounds of Formula (I),01-29-2009
20120046296PALATABLE DUCTILE CHEWABLE VETERINARY COMPOSITION - The present invention is directed to palatable ductile chewable veterinary composition for oral administration. The composition is capable of killing endo-parasites and ecto-parasites and/or can be used for treating prophylactic or curative animal diseases, and it is useful for the treatment of any warm-blooded non-human animal, including herd animals, like horses, cattle, sheep or poultry and preferably pets like dogs and cats. It consists basically of (A) an effective amount of one or more ingredients that are active against animal pests, pathogens or animal diseases; (B) meat flavoring; (C) partially gelatinized starch; (D) a softener; and (E) up to 9% water.02-23-2012
20120046295COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.02-23-2012
20100286155ADRENOCORTICAL CARCINOMA TREATMENT - A method of treating adrenocortical carcinoma with OSI-906.11-11-2010
20120004238L-methylfolate treatment for psychiatric or neurologic disorders - Provided herein are methods of treating neuropsychiatric disorders or improving the symptoms associated therewith administering a medical food, such as L-methylfolate, to a subject having the disorder. The neuropsychiatric disorder may be an autism spectrum disorder or attention deficit disorder with or without hyperactivity (ADD/ADHD). The L-methylfolate may be administered as an adjunct to other therapeutic agents effective to treat the disorder. The subject preferably may be a child and also may have a single nucleotide polymorphism in the MTHFR gene associated with reduced expression of MTHFR enzyme. Also provided is a method of increasing the de novo synthesis of neurotransmitters in vivo by transporting a methyl-donating compound across the blood-brain barrier in a subject.01-05-2012
20100035885COMPOSITIONS FOR MANIPULATING THE LIFESPAN AND STRESS RESPONSE OF CELLS AND ORGANISMS - Provided herein are methods and compositions for modulating the activity of sirtuin deacetylase protein family members; p53 activity; apoptosis; lifespan and sensitivity to stress of cells and organisms. Exemplary methods comprise contacting a cell with an activating compound, such as a flavone, stilbene, flavanone, isoflavone, catechin, chalcone, tannin or anthocyanidin; or an inhibitory compound, such as a sphingolipid, e.g., sphingosine.02-11-2010
20100324053TRISUBSTITUTED 1,2,4 TRIAZOLES - The present invention relates to 1-aryl-3-aniline-5-alkyl-1,2,4-triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I).12-23-2010
20120010211PHARMACEUTICAL COMPOSITION FOR TREATMENT OF TYPE 2 DIABETES - The present invention provides a pharmaceutical composition for the treatment of 2 type diabetes, wherein the pharmaceutical composition contains (R)-7-[3-amino-4-(2,4,5-trifluoro-phenyl)-butyryl]-3-trifluoromethyl-5,6, 7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-carboxylic acid methyl ester or its pharmaceutically acceptable salts and metformin or its pharmaceutically acceptable salts (such as hydrochlorate), preparation method thereof and method of treating 2 type diabetes with the composition.01-12-2012
20110166152HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Heteroaromatic compounds of structural formula (I) are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; Type 2 diabetes; insulin resistance; hyperglycemia; Metabolic Syndrome; neurological disease; cancer; and liver steatosis.07-07-2011
20110166150Anhydrous Crystal Form Of Ovrepitant Maleate - The invention relates to anhydrous crystalline orvepitant maleate (Form 1), pharmaceutical formulations comprising the same, its use in therapy and processes for preparing the same.07-07-2011
20110166149PTERIDINE DERIVATIVES FOR TREATING RESPIRATORY DISEASE - The invention provides methods and compositions for treating asthma and/or COPD. For example, provided herein are compositions that include a kinase inhibiting agent such as 6,7-bis(3-hydroxyphenyl)-pteridine-2,4-diamine or pharmaceutically acceptable salts thereof; and a surfactant.07-07-2011
20110166151GLUCOCORTICOID RECEPTOR AGONIST COMPRISING 1,2,3,4-TETRAHYDROQUINOXALINE DERIVATIVES CONTAINING PHENYL GROUP HAVING SULFONIC ACID ESTER STRUCTURE INTRODUCED THEREIN AS SUBSTITUENT - The object aims to find a novel pharmacological activity of a novel 1,2,3,4-tetrahydroquinoxaline derivative which contains, as a substituent, a phenyl group having a sulfonic acid ester structure introduced therein. A compound represented by general formula (1) or a salt thereof is useful as a glucocorticoid receptor agonist, particularly as a therapeutic agent for diseases against which a glucocorticoid receptor agonist (e.g., a steroid) is believed to be effective, such as inflammatory bone/joint diseases, inflammatory ophthalmic diseases (inflammatory ophthalmic diseases in the anterior or posterior segment of an eye). R07-07-2011
20110166148TREATMENT OF INFLAMMATION USING ALPHA 7 RECEPTOR-BINDING CHOLINERGIC AGONISTS - A method of treating a patient suffering from pancreatitis comprising treating said patient with a therapeutically effective amount of a cholinergic agonist selective for an α7 nicotinic receptor in an amount sufficient to decrease the amount of the proinflammatory cytokine that is released from a macrophage wherein said condition is acute pancreatitis. The compounds of the present invention include a quaternary analog of cocaine; (1-aza-bicyclo[2.2.2]oct-3-yl)-carbamic acid 1-(2-fluorophenyl)-ethyl ester; a compound of formula (I), a compound of formula (II), a compound of formula (III), a compound of formula (IV), and an oligonucleotide or mimetic capable of attenuating the symptoms of acute pancreatitis wherein the oligonucleotide or mimetic consists essentially of a sequence greater than 5 nucleotides long that is complementary to an mRNA of an α7 cholinergic receptor. The variables of formulae (I), (II), (III) and (IV) are described herein.07-07-2011
20120015952Inhibitors of NF-KB - The invention relates to compounds of formulae (1) and (2):01-19-2012
20120015951Polymorphs of Brimonidine Pamoate - A brimonidine pamoate polymorph exhibits characteristics disclosed herein. The polymorph is included in a composition, device, or implant for use in the treatment or control of elevated intraocular pressure or in the neuroprotection of components of a neurological tissue to prevent progressive degeneration of such components. In particular, such a composition, device, or implant can be used to provide neuroprotection to cells and components of the optic nerve system.01-19-2012
20120015950CARBAMATE DERIVATIVES OF ALKYL-HETEROCYCLES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - Compound corresponding to general formula (I): in which R01-19-2012
20120022072PTERIN ANALOGS - Disclosed herein are analogs of tetrahydrobiopterin, compositions containing the same, and methods of treating an individual suffering from a condition responsive to tetrahydrobiopterin by administration of the analog. These analogs are contemplated for use wherever tetrahydrobiopterin is currently used to treat conditions responsive to tetrahydrobiopterin therapies.01-26-2012
20120059011PHARMACEUTICAL COMPOSITIONS OF COMBINATIONS OF DIPEPTIDYL PEPTIDASE-4 INHIBITORS WITH PIOGLITAZONE - This invention relates to pharmaceutical compositions comprising fixed-dose combinations of a dipeptidyl peptidase-4 inhibitor and pioglitazone, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes with such pharmaceutical compositions.03-08-2012
20120157459NOVEL 3-HYDROXY-5-ARYLISOTHIAZOLE DERIVATIVE06-21-2012
20110009416PH INDEPENDENT FORMULATIONS OF 6-(5-CHLORO-2-PYRIDYL)-5-[(4-METHYL-1-PIPERAZINYL)CARBONYLOXY]-7-OXO-6,7-- DIHYDRO-5H-PYRROLO[3,4-b]PYRAZINE - Pharmaceutical compositions of zopiclone [(6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine)] that render the aqueous solubility/dissolution of the free base independent of the pH of the gastrointestinal tract are disclosed. The compositions are useful for oral administration.01-13-2011
20120065210SUBSTITUTED HEXAHYDROPYRROLO[1,2-C]IMIDAZOLONES - There are provided compounds of formula I03-15-2012
20120108599METHODS AND COMPOSITIONS FOR THE TREATMENT OF METABOLIC DISORDERS - The present invention is directed to a novel methods and compositions for the therapeutic intervention in hyperphenylalaninemia. More specifically, the specification describes methods and compositions for treating various types of phenylketonurias using compositions comprising BH4. Combination therapies of BH4 and other therapeutic regimens are contemplated.05-03-2012
20120108598SITAGLIPTIN SYNTHESIS - The present invention relates to novel processes for the preparation of enantiomerically enriched β-amino acid derivatives such as β-amino esters useful for the synthesis of enantiomerically enriched biologically active molecules such as sitagliptin. The key step involves the resolution of the racemate with mandelic acid.05-03-2012
20120108597Azaquinazolinediones Chymase Inhibitors - Disclosed are small molecule inhibitors of the formula (I), which are useful in treating various diseases and conditions involving chymase.05-03-2012
20120108596Aza-Bicyclic Amine N-Oxide Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligand Pro-Drugs - The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are prodrugs for ligands, agonists, and partial agonists for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.05-03-2012
20120065211ALKOXY TETRAHYDRO-PYRIDOPYRIMIDINE PDE10 INHIBITORS - The present invention is directed to alkoxy tetrahydro-pyridopyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.03-15-2012
20120122875Salts of Methyl (R)-7-[3-Amino-4-(2,4,5-Trifluoro-Phenyl)-Butyryl]-3-Trifluoromethyl-5,6,- 7,8-Tetrahydro-Imidazo[1,5-A]Pyrazine-1-Carboxylate - The pharmaceutically acceptable salts of methyl (R)-7-[3-amino-4-(2,4,5-trifluoro-phenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-05-17-2012
200803060783,9-Diazabicyclo [3.3.1] Nonane Derivatives and Their Use as Monoamine Neurotransmitter Re-Uptake Inhibitors - This invention relates to novel 3,9-diazabicyclo[3.3.1]nonane derivatives useful as monoamine neurotransmitter re-uptake inhibitors.12-11-2008
20110092510DPP-IV INHIBITORS FOR USE IN THE TREATMENT OF NAFLD - The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing non alcoholic fatty liver diseases (NAFLD).04-21-2011
20090170859Viral Polymerase Inhibitors - An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I:07-02-2009
20110065714SUBSTITUTED QUINAZOLINES - This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 03-17-2011
20120309766QUINOXALINE CARBOXAMIDE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS - The invention relates to compounds of formula (I)12-06-2012
201203097655-ANILINOIMIDAZOPYRIDINES AND METHODS OF USE - The invention relates to a method of inhibiting abnormal cell growth or treating a hyperproliferative disorder in a mammal comprising administering to said mammal a therapeutically effective amount of an imidazopyridine of formula I with anti-hyperproliferative activity.12-06-2012
20120309764Heteroaromatic aryl triazole derivatives as PDE10A enzyme inhibitors - This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.12-06-2012
20120122877Compositions for Treating Bacterial Infections - The present invention is antibiotic compositions having the ability to disrupt a MazEF complex in 05-17-2012
20120122876PYRIDOPYRAZINONES DERIVATIVES INSULIN SECRETION STIMULATORS, METHODS FOR OBTAINING THEM AND USE THEREOF FOR THE TREATMENT OF DIABETES - The present invention relates to pyridopyrazinone derivatives of formula (I), wherein X, Y, Z1 W, A and R1 are as defined in claim 05-17-2012
20120122874COMBINATION OF A SEDATIVE AND A NEUROTRANSMITTER MODULATOR, AND METHODS FOR TREATING DEPRESSION - One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., insomnia and/or depression. The first component of the pharmaceutical composition is a GABA receptor modulating compound. The second component of the pharmaceutical composition is a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a 5-HT05-17-2012
20100093743CARBAMIC ACID COMPOUNDS COMPRISING A BICYCLIC HETEROARYL GROUP AS HDAC INHIBITORS - This invention pertains to certain carbamic acid compounds of the following formula, which inhibit HDAC (histone deacetylase) activity wherein: A is independently an unsubstituted or substituted bicyclic C04-15-2010
20100093742PTERIN ANALOGS - Disclosed herein are analogs of tetrahydrobiopterin, compositions containing the same, and methods of treating an individual suffering from a condition responsive to tetrahydrobiopterin by administration of the analog. These analogs are contemplated for use wherever tetrahydrobiopterin is currently used to treat conditions responsive to tetrahydrobiopterin therapies.04-15-2010
20100093741CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS - Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of obesity, sarcopenia, wasting syndrome, frailty, cachexia, muscle spasm, post-surgical and post-traumatic muscle weakness, neuromuscular disease, and other indications.04-15-2010
20120316175SOLID STATE FORMS OF SITAGLIPTIN SALTS - Solid state forms of Sitagliptin salts, processes for preparing the solid state forms, and pharmaceutical compositions thereof, are provided.12-13-2012
20090131446Fused pyrazine compounds useful for the treatment of degenerative and inflmmatory diseases - Novel fused pyrazine compounds are disclosed that have a formula represented by the following:05-21-2009
20090131445Furazano '3, 4-B! Pyrazines and Their Use as Anti-Tumor Agents - The present invention provides novel compounds of the formula (I) and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.05-21-2009
20090137596G-PROTEIN INHIBITOR - A subject of the invention is a product comprising at least one Cdc25 phosphatase inhibitor in combination with at least one other anti-cancer agent for a therapeutic use which is simultaneous, separate or spread over time in the treatment of cancer.05-28-2009
20110183989SATURATED BICYCLIC HETEROCYCLIC DERIVATIVES AS SMO ANTAGONISTS - The present invention relates to compounds of formula I: and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of the Sonic Hedgehog pathway, in particular Smoantagonists. Thus the compounds of this invention are useful for the treatment of diseases associated with abnormal hedgehog pathway activation, including cancer, for example basal cell carcinoma, medulloblastoma, prostate, pancreatic, breast, colon, bone and small cell lung cancers, and cancers of the upper GI tract.07-28-2011
20110183988COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on each of B-Raf, B-Raf V600E and c-Raf-1 protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including melanoma, glioma, glioblastoma, pilocytic astrocytoma, liver cancer, biliary tract cancer, cholangiocarcinoma, colorectal cancer, lung cancer, bladder cancer, gallbladder cancer, breast cancer, pancreatic cancer, thyroid cancer, kidney cancer, ovarian cancer, adrenocortical cancer, prostate cancer, gastrointestinal stromal tumors, medullary thyroid cancer, tumor angiogenesis, acute myeloid leukemia, chronic myelomonocytic leukemia, childhood acute lymphoblastic leukemia, plasma cell leukemia, and multiple myeloma.07-28-2011
20110183987Stereoselective Synthesis of Bicyclic Heterocycles - The present invention relates to a process for the stereoselective preparation of compounds of formulae (1A) and (1B)07-28-2011
20120165337TETRAHYDROQUINOXALINE UREA DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF - The invention relates to compounds of formula (I), where: A is a bond, an oxygen atom, or an 06-28-2012
20120165336Color Change Time Indicator for Packaging System - Disclosed in certain embodiments is a pharmaceutical packaging system comprising: a receptacle comprising an openable seal for accessing the interior of the receptacle; a pharmaceutical dosage form contained in the receptacle; and an activatable color-changing material, wherein upon activation, the material exhibits a visually discernible color change upon the lapsing of a predetermined time period.06-28-2012
201201723665,6,7,8-TETRAHYDROIMIDAZO[1,2-A]PYRAZINE DERIVATIVES AS P2X7 MODULATORS - The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof:07-05-2012
20120214816METHODS AND COMPOSITIONS FOR SAFE AND EFFECTIVE TREATMENT OF ERYTHEMA - Improved methods and compositions for safe and effective treatment of erythema or a symptom associated with erythema in a subject are described. The methods involve topically applying to an affected skin area a topical composition comprising about 0.4% to about 0.6% by weight of brimonidine and a pharmaceutically acceptable carrier.08-23-2012
20120214817UROTENSIN II RECEPTOR ANTAGONISTS - The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.08-23-2012
20100048576PYRIDOPYRAZINES AND DERIVATIVES THEREOF AS ALK AND c-MET INHIBITORS - The present invention provides a compound of Formula I02-25-2010
20100048577Method for treating benign prostate hyperplasia using resveratrol - The invention relates to the discovery that resveratrol, and substituted forms of resveratrol, are effective in alleviating benign prostate hyperplasia. Formulations containing the resveratrol or resveratrol derivative, lack omega-3 fatty acids, and also contain no other compounds which activate SIRT1 and PGCα.02-25-2010
20100305133Prolyl Hydroxylase Inhibitors - The invention described herein relates to certain quinoxaline-5-carboxamide derivatives of formula (I)12-02-2010
20100009996METHODS AND COMPOSITIONS FOR THE TREATMENT OF METABOLIC DISORDERS - The present invention is directed to a novel methods and compositions for the therapeutic intervention in hyperphenylalaninemia. More specifically, the specification describes methods and compositions for treating various types of phenylketonurias using compositions comprising BH4. Combination therapies of BH4 and other therapeutic regimens are contemplated.01-14-2010
20100009998Compositions and Methods Employing Aminopterin - The present invention relates to pharmaceutical compositions containing the antifolate aminopterin, processes for making the compositions, and methods of using them to treat disorders in adult and pediatric patients. Pharmaceutical compositions substantially free of impurities are provided comprising a therapeutically effective amount of aminopterin, or a pharmaceutically acceptable salt thereof. Relative to the teachings of the prior art, the disclosed methods and compositions provide unexpected improvements that include a greater interpatient oral bioavailability in pediatric patients, a smaller interpatient coefficient of variation of oral bioavailability, a smaller mean intrapatient coefficient of variation of oral bioavailability, a greater therapeutic index, a smaller coefficient of variation of toxicity, efficacy in combination therapy, and efficacy of certain polyglutamated metabolites.01-14-2010
20100009997METHOD OF TREATING A METABOLIC OR NEUROPSYCHIARTY DISORDER WITH A BH4 DERIVATIVE PRODRUG - Low dose therapeutic methods for use of BH4 derivatives to treat BH4-responsive disorders, such as hyperphenylalanemia and neuropsychiatric diseases, and combination therapies of BH4 derivatives and other therapeutic regimens, are described.01-14-2010
20100009995Maleate Salts of 6-(5-Chloro-2-Pyridyl)-5-[(4-Methyl-1-Piperazinyl)Carbonyloxy]-7-oxo-6,7-- dihydro-5H-Pyrrolo[3,4-b]Pyrazine - A novel maleate salt of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) is provided.01-14-2010
20100009993Diketo Fused Azolopiperidines and Azolopiperazines as Anti-HIV Agents - Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketo fused azolopiperidine and azolopiperazine derivatives that possess unique antiviral activity are provided. These compounds are useful for the treatment of HIV and AIDS.01-14-2010
20100009992AMPK MODULATORS - The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II):01-14-2010
20100292240SULFONAMIDE COMPOUNDS - Certain sulfonamide compounds are dual CCK1/CCK2 inhibitors useful in the treatment of CCK1/CCK2 mediated diseases.11-18-2010
20120220598Besylate Salts of 6-(5-Chloro-2-Pyridyl)-5-[(4 Methyl-1-Piperazinyl)Carbonyloxy]-7-oxo-6, 7-dihydro-5H-Pyrrolo[3,4-b]Pyrazine - A novel besylate salt of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) is provided.08-30-2012
20120220597L-MALATE SALTS OF 6-(5-CHLORO-2-PYRIDYL)-5-[(4-METHYL-1-PIPERAZINYL)CARBONYLOXY]-7-OXO-6,7-- DIHYDRO-5H-PYRROLO[3,4-B]PYRAZINE - A novel L-malate salt of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) is provided.08-30-2012
20120220596CYSTEINE AND CYSTINE PRODRUGS TO TREAT SCHIZOPHRENIA AND REDUCE DRUG CRAVINGS - The present invention provides cysteine and cystine prodrugs for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing prodrugs and methods of using the prodrugs and compositions for treatment of schizophrenia and drug addiction.08-30-2012
20090318457Methods of Using hydrates and polymorphs of 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pterid- inyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide - Disclosed are hydrates and polymorphs of 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, processes for preparing them and their use as pharmaceutical compositions.12-24-2009
20120083499NOVEL BENZENESULFONAMIDES AS CALCIUM CHANNEL BLOCKERS - The present application relates to calcium channel inhibitors comprising compounds of formula (I), formula (II), formula (III), or formula (IV),04-05-2012
20120225884BRIDGED PIPERIDINE DERIVATIVES - The present invention relates to compounds of formula I09-06-2012
20120190685NOVEL PHENYLIMIDAZOLE DERIVATIVE AS PDE10A ENZYME INHIBITOR - This invention provides the compound 5,8-Dimethyl-2-[2-(1-methyl-4-phenyl-1H-imidazol-2-yl)-ethyl]-[1,2,4]thazolo[1,5-a]pyrazine and pharmaceutically acceptable acid addition salts thereof.07-26-2012
20110124650STABLE CRYSTALLINE SALTS OF ANTIFOLATE COMPOUNDS - The present invention provides stable crystalline polymorphic forms of antifolate compounds, particularly (S)-2-{4-[2-(2,4-diamino-quinazolin-6-yl)-ethyl]-benzoylamino}-4-methylene-pentanedioic acid, dipotassium salt, and methods of preparation thereof The polymorphs may be in the form of hydrates. The invention further provides pharmaceutical compositions comprising the polymorphs and methods of treatment using the polymorphs. The polymorphs are useful in the treatment of multiple conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis, and the polymorphs may be administered alone in or combination with on or more further active agents.05-26-2011
20120232084PYRROLIDIN-3-YLMETHYL-AMINE AS OREXIN ANTAGONISTS - The present invention is concerned with novel sulfonamides of formula I09-13-2012
20120264760Compounds and Methods for Treating Mammalian Gastrointestinal Parasitic Infections - One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of 10-18-2012
20120232083FLUORO-PYRIDINONE DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS - The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.09-13-2012
20100331335Inhibitors of Jun N-Terminal Kinase - The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula:12-30-2010
20080300252EMBEDDING ANTIBIOTIC COMPOUNDS IN SOLID POLYMERS - The present invention is directed to providing antimicrobial compositions consisting of a polymeric material and, embedded therein, an antimicrobial compound. The antimicrobial compound contains at least one quaternary ammonium group, at least one hydrocarbon chain comprising a minimum of 10 carbon atoms and a maximum of 24 carbon atoms, and one or more anions to balance the charge of the quaternary ammonium groups. The invention is also directed to a method of making antimicrobial compositions containing an antimicrobial compound embedded in a polymeric material.12-04-2008
20110003823Compositions and methods for treatment of diseases and conditions associated with vasodilation and/or vascular leakage - The invention provides compositions and methods for treating diseases and conditions, including systemic diseases and conditions, through an intravenous administration of a selective α-2 adrenergic receptor agonists having a binding affinity of 300 fold or greater for α-2 over α-1 adrenergic receptors. The amounts of the selective α-2 adrenergic receptor agonists are substantially lower than the amounts normally used to cause sedation. The compositions preferably include dexmedetomidine.01-06-2011
20110009417PYRIDOPYRAZINONES DERIVATIVES INSULIN SECRETION STIMULATORS, METHODS FOR OBTAINING THEM AND USE THEREOF FOR THE TREATMENT OF DIABETES - The present invention relates to pyridopyrazinone derivatives of formula (I), wherein X, Y, Z, W, A and R1 are as defined in claim 1, as insulin secretion stimulators. The invention also relates to the preparation and use of these pyridopyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.01-13-2011
20120270880PYRROLO [2,3-D] PYRAZIN-7-YLPYRIMIDINE COMPOUNDS - Pyrrolo[2,3-d]pyrazin-7-ylpyrimidine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.10-25-2012
20120270879Heterocyclic Compounds As CCR1 Receptor Antagonists - Disclosed are CCR1 receptor antagonists of the formula (I) wherein Ar1, Ar2, R1-R3, X and L are disclosed herein. Also disclosed are compositions, methods of making and using compounds of the formula (I).10-25-2012
20110212969SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I):09-01-2011
20120322806QUINOXALINEDIONE DERIVATIVES - The present invention relates to compounds of formula (I)12-20-2012
20120322805PHARMACEUTICAL COMPOSITIONS OF SEMI-ORDERED DRUGS AND POLYMERS - A solid composition of a low-solubility drug and a concentration-enhancing polymer has a portion of the drug in a semi-ordered state.12-20-2012
20120129866METHODS FOR PREVENTING OR TREATING METABOLIC DISEASES, INFLAMMATORY DISEASES, AUTOIMMUNE DISEASES, ALLERGIC DISEASES, CENTRAL NERVOUS SYSTEM DISEASES, CARDIOVASCULAR DISEASES, HOMEOSTASIS-RELATED DISEASES OR GLAUCOMA - A method for preventing or treating a metabolic disorder, an inflammatory disease, an autoimmune disease, an allergic disease, a central nervous system disease, a cardiovascular disease, a homeostasis-related disease or glaucoma, involving administering a compound or a salt thereof, the compound having the following formula (1)05-24-2012
20100234387Sulfonylated Tetrahydroazolopyrazines and their Use as Pharmaceuticals - Sulfonylated tetrahydroazolopyrazine compounds corresponding to the formula I09-16-2010
20100234386QUINOXALINE DERIVATIVES AS PI3 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using quinoxaline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoxaline derivatives.09-16-2010
20100234385Compsition Containing Biopterin and Method for Using The Same - It is thought that applications and use of tetrahydrobiopterin (BH4), which is used as a pharmaceutical, will expand due to its superior efficacy. However, in addition to BH4 being extremely expensive, since it is unstable with respect to oxidation, applications other than pharmaceuticals are considered to be difficult. Further, it is difficult for BH4 to permeate through a blood-brain barrier, so that BH4 concentrations in the brain tend not to increase under the present conditions. Biopterins are oxidized form of BH4, stable to oxidation, easy to handle, and can be produced inexpensively. The inventors found that administration of biopterin can be expected to demonstrate effects equal to or greater than those of administration of BH4. On the basis of the result, it was first clarified that administration of a composition containing biopterin causes increase in BH4 concentration in the body (especially BH4 concentration in the brain, which is difficult to be increased by BH4 administration) to demonstrate sufficient actions.09-16-2010
201002343843, 9-DIAZABICYCLO(3.3.1)NON-3-YL-ARYL METHANONE DERIVATIVES AS NICOTINIC ACETYLCHOLINE RECEPTOR AGONISTS - This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.09-16-2010
20120277237NOVEL ALKYNYL DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel compounds of formula I wherein W, n, X and W′ are defined in the description; invention compounds are modulators of metabotropic glutamate receptors—subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.11-01-2012
20120277240SUBSTITUTED AMINOTETRAHYDROTHIOPYRANS AND DERIVATIVES THEREOF AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES - The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.11-01-2012
20120277239Compositions and Methods for Improving Night Vision - The invention provides compositions and methods for improving night vision without inducing redness or significant tachyphylaxis. The provided compositions and methods utilize low concentrations of selective α-2 adrenergic receptor agonists. The compositions preferably include brimonidine.11-01-2012
20120277241Compounds, Formulations, and Methods for Treating or Preventing Inflammatory Skin Disorders - In methods, compounds, and topical formulations for treatment of inflammatory skin disorders incorporating compounds represented by the formulas below:11-01-2012
201102452595-Amino-2-(1-Hydroxy-Ethyl)-Tetrahydropyran Derivatives - The invention relates to antibacterial compounds of formula I10-06-2011
20100204238BICYCLIC NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS FOR USE AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses bicyclic nitrogen-containing heterocyclic compounds for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, oily skin conditions, metabolic syndrome, and the like.08-12-2010
20100204237Hydroxypyrimidinone derivatives having inhibitory activity against HIV integrase - Compounds of Formula (1), pharmaceuticals containing the same, especially anti-HIV agents having anti viral activity, especially inhibitory activity against HIV integrase,08-12-2010
20100204236Substituted imidazoles as bombesin receptor subtype-3 modulators - Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.08-12-2010
20120329803Dihydropteridinones, method for production and use thereof - The present invention relates to new dihydropteridinones of general formula (12) wherein the groups R12-27-2012
20120329805PREPARATIONS AND METHODS FOR AMELIORATING OR REDUCING PRESBYOPIA - This application relates to the use of one or more parasympathomimetic drugs in combination with one or more alpha agonists to create optically beneficial miosis to, for example, temporarily treat presbyopia. The invention provides a pharmaceutical preparation comprising a therapeutically effective amount of one or more parasympathomimetic drugs or cholinesterase inhibitors, or a pharmaceutically acceptable salt thereof, in combination with one or more alpha agonists or antagonists, or a pharmaceutically acceptable salt thereof. The invention further provides for a method for treating, ameliorating or reducing presbyopia of a patient having an eye, comprising administering to said eye a pharmaceutically effective amount of the ophthalmic preparation.12-27-2012
20120329804Pyridopyrazindione Derivative and its Use as an Antiulcer Drug - The invention relates to the fields of the chemical and pharmaceutical industry and medicine and concerns a novel compound which can be used as an antiulcer agent. The compound is 9-(quinonyl-2)-2-p-ethoxyphenylethyl-4,5,6,7,8,9,10,11-octahydropyrido[1,2-a]pyrazindione-1,4 of formula (I), or pharmaceutically acceptable complex derivatives thereof. The compound can be used as an antiulcer agent.12-27-2012
20120329802METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.12-27-2012
20110319419Methotrexate Adjuvants to Reduce Toxicity and Methods for Using the Same - Methods are provided for using methotrexate (MTX) active agents in which reduced host toxicity is observed. Aspects of the methods include administering to a subject an effective amount of an MTX active agent in conjunction with a MTX toxicity-reducing adjuvant, such as a 2,2′-anhydropyrimidine, a derivative thereof or a uridine phosphorylase inhibitor. Also provided are compositions and kits that find use in practicing embodiments of the invention. The methods and compositions find use in a variety of applications, including the treatment of a variety of different disease conditions.12-29-2011
20120101105ARYL SUBSTITUTED CARBOXAMIDE DERIVATIVES AS CALCIUM OR SODIUM CHANNEL BLOCKERS - The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as Na04-26-2012
20120101104TOPICAL GEL COMPOSITIONS AND METHODS OF USE - Improved topical gel compositions, such as those containing brimonidine, for the treatment of skin disorders are described. The gel compositions contain carbomer and paraben, and are substantially free of paraben crystalline particles after an extended period of storage.04-26-2012
201201011037-PHENOXYCHROMAN CARBOXYLIC ACID DERIVATIVES - Compounds of Formula I: (I) in which A, A04-26-2012
20100168118Methods to Treat Cancer with 10-propargyl-10-deazaaminopterin and Methods for Assessing Cancer for Increased Sensitivity to 10-propargyl-10-deazaaminopterin - The present invention relates to a method for assessing the sensitivity of a patient's cancer to treatment with 10-propargyl-10-deazaminopterin and a method for selecting a patient for treatment of cancer with 10-propargyl-10-deazaminopterin, by determining the amount of a selected polypeptide expressed by the cancer and comparing the amount with the amount of the selected polypeptide expressed by a reference cancer, wherein the polypeptide includes a member of folate pathways within cells and may include at least one of reduced folate carrier-1 enzyme (RFC-1), dihydrofolate reductase (DHFR), folylpoly-gamma-glutamate synthetase (FPGS), thymidylate synthase (TS), γ-glutamyl hydrolase (GGH), and glycinamide ribonucleotide formyltransferase (GARFT). The present invention also relates to the use of 10-propargyl-10-deazaminopterin in the treatment of multiple myeloma.07-01-2010
20120135997PHARMACEUTICAL COMPOSITION COMPRISING A LACTAM OR BENZENESULFONAMIDE COMPOUND - The present invention provides, for example, the following compounds as a pharmaceutical composition for treating diseases induced by production, secretion or deposition of amyloid β proteins.05-31-2012
20100168117A PROCESS FOR THE PREPARATION OF THE STABLE, AMORPHOUS CALCIUM SALT OF (6S)-N(5)-METHYL-5,6,7,8-TETRAHYDROFOLIC ACID - A process for the preparation of an aqueous solution of the calcium salt of (6S)-N(5)-methyl-5,6,7,8-tetrahydrofolic acid, whereby (6S)-5,6,7,8-tetrahydrofolic acid having a content of the corresponding (6R)-diastereoisomer in the range from 4% by weight to 8% by weight is methylated in water comprises: treating the methylated reaction mixture with calcium chloride; crystallizing the calcium salt of (6RS)-N(5)-methyl-5,6,7,8-tetrahydrofolic acid from the resulting aqueous solution; and obtaining an aqueous solution of the calcium salt of (6S)-N(5)-methyl-5,6,7,8-tetrahydrofolic acid.07-01-2010
20100130500METHODS AND COMPOSITIONS FOR THE TREATMENT OF PULMONARY HYPERTENSION OF THE NEWBORN - The present invention is directed to a novel methods and compositions for the therapeutic intervention in persistent pulmonary hypertension of the newborn (PPHN). More specifically, the specification describes methods and compositions for treating various types of PPHN using compositions comprising BH4. Combination therapies of BH4 and other therapeutic regimens are contemplated.05-27-2010
20100130504BETA-AMINO HETEROCYCLIC DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES - The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.05-27-2010
20100130501NOVEL 3-AMINO-PYRROLO[3,4-C]PYRAZOLE-5(1H, 4H, 6H) CARBALDEHYDE DERIVATIVES - The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: (A) and (B) wherein A, B, R05-27-2010
201300180522-PYRIDYL SUBSTITUTED IMIDAZOLES AS ALK5 AND/OR ALK4 INHIBITORS - The present invention provides a novel 2-pyridyl substituted imidazole derivative, or a pharmaceutically acceptable salt or solvate thereof, which selectively inhibits the transforming growth factor-β (TGF-β) type I receptor (ALK5) and/or the activin type I receptor (ALK4); a pharmaceutical composition comprising same as an active ingredient; and a use of the 2-pyridyl substituted imidazole derivative for the manufacture of a medicament for preventing or treating a disease mediated by ALK5 and/or ALK4 receptors in a mammal.01-17-2013
20110136816COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.06-09-2011
20110160216Thymidylate Synthase Haplotype is Associated with Tumor Recurrence in Stage II and Stage III Colon Cancer Patients - The invention provides compositions and methods for determining the likelihood of tumor recurrence following treatment with 5-FU based adjuvant therapy for Stage II or Stage III colon cancer patients. After determining if a patient is less likely to experience tumor recurrence once treated, the invention also provides methods for treating these patients.06-30-2011
20110160215Substituted Triazolo-Pyrazine Compounds - The present invention relates to substituted triazolo-pyrazine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted triazolo-pyrazine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.06-30-2011
20110160214Compositions and methods for eye whitening - The invention provides compositions and methods for whitening of eyes. The provided compositions and methods utilize low concentrations of selective α-2 adrenergic receptor agonists. The compositions preferably include brimonidine.06-30-2011
20130023537PYRIDOPYRAZINONES DERIVATIVES INSULIN SECRETION STIMULATORS, METHODS FOR OBTAINING THEM AND USE THEREOF FOR THE TREATMENT OF DIABETES - The present invention relates to pyridopyrazinone derivatives of formula (I), wherein X, Y, Z1 W, A and R1 are as defined in claim 01-24-2013
20130023536FIXED DOSE COMBINATION OF BIMATOPROST AND BRIMONIDINE - The present invention is directed to compositions comprising combinations of brimonidine and bimatoprost useful for lowering intraocular pressure in a patient and for the treatment of glaucoma01-24-2013
20080255130Bicyclic Nitrogen-containing Heterocyclic compounds for use as Stearoyl CoA Desaturase inhibitors - The present invention discloses bicyclic nitrogen-containing heterocyclic compounds for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, oily skin conditions, metabolic syndrome, and the like.10-16-2008
20130172358Compounds, Formulations, and Methods for Treating or Preventing Inflammatory Skin Disorders - In methods, compounds, and topical formulations for treatment of inflammatory skin disorders incorporating compounds represented by the formulas below:07-04-2013
20130172359Compounds, Formulations, and Methods for Treating or Preventing Inflammatory Skin Disorders - In methods, compounds, and topical formulations for treatment of inflammatory skin disorders incorporating compounds represented by the formulas below:07-04-2013
20080249101BENZOIMIDAZOLE, TETRAHYDRO-QUINOXALINE, BENZOTRIAZOLE, DIHYDRO-IMIDAZO[4,5-c] PYRIDINONE AND DIHYDRO-ISOINDOLONE DERIVATIVES - This invention relates to compounds of the formula10-09-2008
200802490997-Phenylalkyl Substituted 2-Quinolinones and 2-Quinoxalinones as Poly(Adp-Ribose) Polymerase Inhibitors - The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I)10-09-2008
20080227789DIAMINOTHIAZOLES USEFUL AS AXL INHIBITORS - Diaminothiazoles and pharmaceutical compositions containing them are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the diaminothiazoles in treating diseases or conditions associated with Axl activity are also disclosed.09-18-2008
20080227787Use of New Lipoxygenase Inhibitors - There is provided a use of a compound of formula (I), wherein R09-18-2008
20080227786Novel Crystalline Salts of a Dipeptidyl Peptidase-IV Inhibitor - Novel crystalline salts of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-&agr; amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel salts, processes to prepare these salts and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.09-18-2008
20130131072Methods for Optimizing Clinical Responsiveness to Methotrexate Therapy Using Metabolite Profiling and Pharmacogenetics - The present invention provides methods for optimizing clinical responsiveness to chemotherapy in an individual through genotypic analysis of polymorphisms in at least one gene. The methods of the present invention may further comprise determining the level of at least one long-chain methotrexate polyglutamate (MTXPG) in a sample obtained from the individual. The present invention also provides methods for generating a pharmacogenetic index for predicting clinical responsiveness to chemotherapy in an individual through genotypic analysts of polymorphisms in at least one gene. In addition, the present invention provides methods for optimizing therapeutic efficacy of chemotherapy in an individual by calculating the level of at least one long-chain MTXPG in a sample obtained from the individual.05-23-2013
20080221113SUBSTITUTED HEXAHYDROPYRAZINO [1,2-A] PYRIMIDINE-4,7-DIONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS - Substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives, processes for their preparation and their use as medicaments09-11-2008
20080221112New utilities of amide compounds - Compounds having an activity to enhance the expression of apoAI are provided, which are used as medicaments.09-11-2008
20080221111Combination of a Pd4 Inhibitor and a Tetrahydrobiopterin Derivative - The invention describes the use of a PDE4 inhibitor in combination with BH4 or a BH4 derivative for the prevention and/or treatment of respiratory diseases.09-11-2008
20130172357Compositions and Methods for Treatment of Glaucoma - The invention provides α-2 adrenergic receptor agonist compositions and methods for treating glaucoma and other intraocular conditions. The preferred α-2 agonist used in the inventive compositions and methods is dexmedetomidine.07-04-2013
20130172360DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE AS MEDICAMENT - The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.07-04-2013
20130096131OPTICAL CORRECTION - The present disclosure describes compositions which improve visual acuity and to methods for their use.04-18-2013
20130096130CGRP Receptor Antagonists - The disclosure generally relates to the novel compounds of formula I, including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).04-18-2013
20130102612TOPICAL DERMAL BRIMONIDINE COMPOSITIONS - The present invention provides topical dermal compositions comprising an effective amount of brimonidine or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier selected from the group consisting of drops, creams, gels and ointments, wherein the composition is suitable for application to skin.04-25-2013
20130102613TREATMENT OF CANCER WITH TOR KINASE INHIBITORS - Provided herein are methods for treating or preventing a solid tumor, non-Hodgkin lymphoma or multiple myeloma in a patient, comprising administering an effective amount of a TOR kinase inhibitor to a patient having a solid tumor, non-Hodgkin lymphoma or multiple myeloma.04-25-2013
20130116261NANOPARTICLES FOR ENCAPSULATION OF COMPOUNDS, THE PRODUCTION AND USES THEREOF - The present invention relates to nanoparticles for the encapsulation of compounds, the obtaining and uses thereof. The nanoparticles comprise a zein matrix and a basic amino acid. Said nanoparticles can encapsulate a water-soluble or fat-soluble biologically active compound. It is applicable in the food, pharmaceutical and cosmetic sectors and in the nanotechnology sector.05-09-2013
20130116260FUSED HETEROAROMATIC PYRROLIDINONES AS SYK INHIBITORS - Disclosed are compounds of Formula 1,05-09-2013
20130116259COMBINATION THERAPY FOR TREATING OR PREVENTING AN INFLAMMATORY SKIN DISORDER - Methods and compositions for improved treatment and prevention of an inflammatory skin disorder or a sign and/or symptom associated with the skin disorder are described. The methods involve topical application to the skin a combination of a therapeutically effective amount of an α2 adrenergic receptor agonist, such as brimonidine, and a therapeutically effective amount of a non-steroidal anti-inflammatory agent, such as diclofenac.05-09-2013
20130203760Polymorphs of Brimonidine Pamoate - A brimonidine pamoate polymorph exhibits characteristics disclosed herein. The polymorph is included in a composition, device, or implant for use in the treatment or control of elevated intraocular pressure or in the neuroprotection of components of a neurological tissue to prevent progressive degeneration of such components. In particular, such a composition, device, or implant can be used to provide neuroprotection to cells and components of the optic nerve system.08-08-2013
20130131071USE OF PTERIDINE DERIVATIVES FOR THE TREATMENT OF INCREASED INTRACRANIAL PRESSURE, SECONDARY ISCHEMIA, AND DISORDERS ASSOCIATED WITH AN INCREASED LEVEL OF CYTOTOXIC REACTIVE OXYGEN SPECIES - The present invention relates to the use of pteridine derivatives for the treatment of increased intracranial pressure, secondary ischemia, and disorders associated with an increased level of cytotoxic reactive oxygen species.05-23-2013
201301310701-Aryl or 1- Heteroaryl-Pyrido(B)indoles and Uses Thereof - Provided are 1-aryl or 1-heteroaryl substituted beta-carboline compounds or indole analogs thereof having the structure:05-23-2013
20130131069METHOD FOR TREATMENT OF SOLID MALIGNANCIES INCLUDING ADVANCED OR METASTATIC SOLID MALIGNANCIES - The present invention relates to the use of Volasertib or a salt thereof or the hydrate thereof for treating patients suffering from solid malignancies including advanced or metastatic solid malignancies comprising a high frequency administration of Volasertib according to a specific dosage schedule.05-23-2013
20130178477METHODS OF TREATING DIABETIC NEUROPATHY USING BENZENESULFONAMIDES - This invention is directed to methods of treating diabetic neuropathy, particularly, diabetic peripheral neuropathy, in a patient in need of treatment thereof.07-11-2013
20130178476METHOTREXATE COMPOSITION - A Methotrexate composition for oral administration is provided comprising a pharmaceutically acceptable salt of Methotrexate and an aqueous carrier agent. The Methotrexate salt is substantially or completely soluble in the aqueous carrier agent, forming an aqueous solution. There is also provided a method of manufacturing a Methotrexate composition for oral administration, comprising mixing a pharmaceutically acceptable salt of Methotrexate with an aqueous carrier agent until the Methotrexate salt is substantially or completely soluble in the carrier agent to form an aqueous solution.07-11-2013
20080207627METHODS OF PREVENTING AND REDUCING THE SEVERITY OF STRESS-ASSOCIATED CONDITIONS - The present invention provides a method of preventing or reducing the severity of a stress-associated condition in a subject by systemically administering to the subject an effective amount of brimonidine or a pharmaceutically acceptable salt, ester, amide, sterioisomer or racemic mixture thereof. Stress-associated conditions that can be treated according to a method of the invention include, but are not limited to, dyspepsia, tachycardias other than tachycardia associated with myocardial ischemia, panic attack, non-inflammatory dermatogical conditions, disorders of muscle contraction, sensory hypersensitivity associated with migraine, and behavioral disorders.08-28-2008
20130143890CO-CRYSTAL INTERMEDIATES OF ROSUVASTATIN AND METHODS OF USING SAME - Methods for the preparation of Rosuvastatin by co-crystals of Rosuvastatin or intermediates are provided. Also provided are co-crystals, pharmaceutical compositions which include such co-crystals and methods for treating conditions associated with hypercholesterolemia by administering such compositions.06-06-2013
200802004716' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY - The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I):08-21-2008
20080200470Diaza- or Thiazadione Derivatives With Neuroprotective Activity - The present invention relates to certain derivatives of cycloalkanediones invariably substituted with a chroman-2-yl, 2-quinolyl or —O-phenyl residue which are serotonin (5-hydroxytryptamine, 5-HT) 5-HT08-21-2008
20110212970COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.09-01-2011
20110224217METHODS OF TREATMENT USING HETEROARYL COMPOUNDS AND COMPOSITIONS THEREOF - Provided herein are Heteroaryl Compounds having the following structure:09-15-2011
20110251203USE OF PKC INHIBITORS IN DIABETIC COMPLICATIONS - The present invention pertains “to the use of a PKC inhibitor in the manufacture of a medicament in the treatment or prevention of diabetic complications, where in the PKC inhibitor is one of 3-(1.H.-indol-3-yl)-4-[2-(4-methyl-piperazin-1-yl)-quinazolin-4-yl]-pyrrole-2,5-dione, 3-(1.H.-indol-3-yl)-4-[2-(piperazin-1-yl)-quinazolin-4-yl]-pyrrole-2,5-dione, 3-[3-(4,7-Diaza-spiro [2.5]oct-7-yl)-isoquinolin-1-yl]-4-(7-methyl-1H-indol-3-yl)-pyrrole-2,5-dione or a pharmaceutically acceptable salt thereof.10-13-2011
20110275644BIOLOGICAL MARKERS PREDICTIVE OF ANTI-CANCER RESPONSE TO INSULIN-LIKE GROWTH FACTOR-1 RECEPTOR KINASE INHIBITORS - The present invention provides diagnostic methods for predicting the effectiveness of treatment of a cancer patient with an IGF-1R kinase inhibitor that inhibits both IGF-1R and IR kinases. Methods are provided for identifying patients with cancer who are likely to benefit from treatment with an IGF-1R kinase inhibitor that inhibits both IGF-1R and IR kinases. Methods are also provided for identifying patients with cancer who are likely to benefit from treatment with an IGF-1R kinase inhibitor that inhibits both IGF-1R and IR kinases, but who would likely not respond to therapy with an anti-IGF-1R antibody. Methods are also provided for identifying patients with cancer who are more likely to benefit from treatment with anti-IGF-1R antibody. Improved methods for treating cancer patients with IGF-1R kinase inhibitors that incorporate these methods are also provided.11-10-2011
20110275643AROYLQUINOLINE COMPOUNDS - A serious of nitro heterocyclic derivatives including a structure of formula (I) are provided. In formula (I), P, Q and R1 to R8 are defined in the specification. The derivatives disclosed in the present invention are characterized in inhibiting tubulin polymerization, and treating cancers and other tubulin polymerization-related disorders with a suitable pharmaceutical acceptable carrier.11-10-2011
20110257190CRYSTALLINE FORMS - The disclosure relates to crystalline forms of 2-[4-(7-ethyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)-phenyl]-propan-2-ol, characterized by physico-chemical data described herein.10-20-2011
20130150371Inhibitors of PDE10 - PDE10 inhibitors having the general formula (I)06-13-2013
201301503724-PHENOXY-NICOTINAMIDE OR 4-PHENOXY-PYRIMIDINE-5-CARBOXAMIDE COMPOUNDS - This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula06-13-2013
20100292239NOVEL MICROBIOCIDES - Compounds of the formula (I), in which the substituents are as defined in claim 11-18-2010
20100317668SUBSTITUTED PYRANO [2,3-B] PYRIDINAMINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I12-16-2010
201003176671-aryl-or 1-heteroaryl-pyrido[B]indoles and uses thereof - Provided herein are 1-aryl or 1-heteroarylsubstituted phenanthrene diketo acid compounds. These compounds comprise a β-carboline ring structure substituted at C1 with an aryl or heteroaryl moiety and individually substituted at C3-C8 and N9 with a C12-16-2010
20100317666Composition Comprising An NK-1 Receptor Antagonist And An SSRI For The Treatment Of Tinnitus And Hearing Loss - The present invention relates to methods for treating a subject suffering from tinnitus, hearing loss, or tinnitus and hearing loss comprising administering to the subject an effective amount of an NK1 receptor antagonist alone, or in combination with an effective amount of a selective serotonin reuptake inhibitor. Compositions and pharmaceutical formulations are also provided.12-16-2010
20130184282IP RECEPTOR AGONIST HETEROCYCLIC COMPOUNDS - The present invention provides heterocyclic derivatives which activate the IP receptor, processes for preparing them, pharmaceutical compositions comprising said derivatives and uses thereof. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients.07-18-2013
20120283265COMPOUNDS USEFUL FOR TREATING AIDS - The present invention relates to compound Formula (I) wherein: Formula (II) means a pyridazine, a pyrimidine or a pyrazine group, R independently represent a hydrogen atom, a halogen atom or a group chosen among a CN group, a hydroxyl group, a COOR11-08-2012
20120283264Oxazolidinones as Modulators of MGLUR5 - The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.11-08-2012
20130158040DIAZAINDOLE INHIBITORS OF CRAC - Disclosed are compounds of Formula (I):06-20-2013
20130158041Tyrosine Kinase Inhibitors - The present invention relates to pyridazinthione derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.06-20-2013
20130184283METHOD FOR TREATING PSORIASIS - Methods and kits for treating or preventing psoriasis or a symptom associated with psoriasis in a subject are described. The methods involve topical applications to the subject a therapeutically effective amount of an α2 adrenergic receptor agonist.07-18-2013
20130184281USE OF PTERIDINE DERIVATIVES FOR THE TREATMENT OF INCREASED INTRACRANIAL PRESSURE, SECONDARY ISCHEMIA, AND DISORDERS ASSOCIATED WITH AN INCREASED LEVEL OF CYTOTOXIC REACTIVE OXYGEN SPECIES - The present invention relates to the use of pteridine derivatives for the treatment of increased intracranial pressure, secondary ischemia, and disorders associated with an increased level of cytotoxic reactive oxygen species.07-18-2013
20110281881NOVEL SUBSTITUTED BICYCLIC HETEROCYCLIC COMPOUNDS AS GAMMA SECRETASE MODULATORS - The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I)11-17-2011
20110288099COMPOSITIONS WITH REDUCED HEPATOTOXICITY - Pharmaceutical compositions of hepatotoxic compounds are provided in which the hepatotoxicity of the compounds is mitigated by including quantities of nicotinamide and methionine in the composition. Folic acid also can be included to further mitigate the hepatotoxic effects. The hepatotoxic compounds can include acetaminophen, methotrexate, atorvastatin, simvastatin, niacin, flucanozole, divalproex sodium, and valproic acid.11-24-2011
20110288097Pyrrolopyrazine Kinase Inhibitors - The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I,11-24-2011
20110288096METHODS AND COMPOSITIONS FOR TREATING OR PREVENTING ERYTHEMA - Methods and products for treating or preventing erythema or a symptom associated with erythema in a subject are described. The methods involve topically applying to an affected skin area a topical aqueous gel composition comprising about 0.01% to about 10% by weight of at least one α-adrenergic receptor agonist and a pharmaceutically acceptable carrier.11-24-2011
20130190315SUBSTITUTED BENZALDEHYDE COMPOUNDS AND METHODS FOR THEIR USE IN INCREASING TISSUE OXYGENATION - Provided are substituted benzaldehydes and derivatives thereof that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions comprising the modulators, and methods for their use in treating disorders mediate by hemoglobin and disorders that would benefit from increased tissue oxygenation.07-25-2013
20130190316SUBSTITUTED HETEROARYL ALDEHYDE COMPOUNDS AND METHODS FOR THEIR USE IN INCREASING TISSUE OXYGENATION - Provided are substituted heteroaryl aldehydes and derivatives thereof that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions comprising the modulators, and methods for their use in treating disorders mediate by hemoglobin and disorders that would benefit from increased tissue oxygenation.07-25-2013
20130190317COMBINATION OF COMPOUNDS FOR TREATING OR PREVENTING SKIN DISEASES - The invention relates to a combination of compounds for treating skin diseases and particularly rosacea and ocular rosacea. It is the combination of a compound selected from azelaic acid and salts thereof with a compound of the alpha-1 or alpha-2 adrenergic receptor agonist family. The invention also relates to a product in the form of a kit containing: (a) a first composition comprising a compound selected from azelaic acid and salts thereof, and (b) a second composition different from the first one and comprising a compound of the alpha-1 or alpha-2 adrenergic receptor agonist family, as a combination product for application thereof as a medicament for treating and/or preventing skin diseases and in particular rosacea and ocular rosacea, wherein said first and second compositions can be applied simultaneously, separately or with a time delay.07-25-2013
20120010210L-Methylfolate Treatment for Psychiatric or Neurologic Disorders - Provided herein are methods of treating neuropsychiatric disorders or improving the symptoms associated therewith administering a medical food, such as L-methylfolate, to a subject having the disorder. The neuropsychiatric disorder may be an autism spectrum disorder or attention deficit disorder with or without hyperactivity (ADD/ADHD). The L-methylfolate may be administered as an adjunct to other therapeutic agents effective to treat the disorder. The subject preferably may be a child and also may have a single nucleotide polymorphism in the MTHFR gene associated with reduced expression of MTHFR enzyme. Also provided is a method of increasing the de novo synthesis of neurotransmitters in vivo by transporting a methyl-donating compound across the blood-brain barrier in a subject.01-12-2012
20120028985COMBINATIONAL THERAPY FOR TREATING AUTOIMMUNE DISEASE - The present invention relates to the treatment and prevention of immunological and inflammatory disorders with a compound of formula (I) in combination with methotrexate,02-02-2012
20130197000DRUG AND FOOD/DRINK FOR PREVENTING OR IMPROVING CEREBRAL DYSFUNCTION08-01-2013
20130197002BRIMONIDINE FOR TREATING VISUAL DISORDERS MEDIATED BY CENTRAL VISUAL PROJECTIONS FROM THE EYE - The present invention relates to a method for treating visual disorders mediated by lateral geniculate nucleus, superior colliculus and the visual cortex by administering to a patient in need of such treatment, compounds acting at the alpha 2 adrenergic receptor.08-01-2013
20130197003METHODS AND COMPOSITIONS FOR TREATING OR PREVENTING ERYTHEMA - Methods and products for treating or preventing erythema or a symptom associated with erythema in a subject are described. The methods involve topically applying to an affected skin area a topical aqueous gel composition comprising about 0.01% to about 10% by weight of at least one α-adrenergic receptor agonist and a pharmaceutically acceptable carrier.08-01-2013
20130197004Optically Pure Diastereomers of 10-Propargyl-10-Deazaaminopterin and Methods of Using Same for the treatment of cancer - The present invention relates to diastereomers of 10-propargyl-10-deazaminopterin, compositions comprising optically pure diastereomers of 10-propargyl-10-deazaminopterin, in particular the two (R,S) diastereomers about the C10 position. Methods of preparation of these diastereomers, compositions containing them, and their use for the treatment of conditions related to inflammatory disorders and cancer are also disclosed.08-01-2013
20130197001SUBSTITUTED HETEROCYCLIC COMPOUNDS - The present invention relates to compounds that are late sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I):08-01-2013
200900053892,5 Diaza-Bicyclo [2.2.1] Heptane Derivatives as Calcium Channel Blockers - 2,5-diaza-bicyclo[2.2.1]heptane derivatives represented by Formula (I), or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.01-01-2009
20130102611IP RECEPTOR AGONIST HETEROCYCLIC COMPOUNDS - The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed. Examples of compounds of the invention include the compounds according to Formula Ia, or a pharmaceutically acceptable salt thereof, and the compounds of the examples.04-25-2013
20130203761Polymorphs of Brimonidine Pamoate - A brimonidine pamoate polymorph exhibits characteristics disclosed herein. The polymorph is included in a composition, device, or implant for use in the treatment or control of elevated intraocular pressure or in the neuroprotection of components of a neurological tissue to prevent progressive degeneration of such components. In particular, such a composition, device, or implant can be used to provide neuroprotection to cells and components of the optic nerve system.08-08-2013
20100063056BIPYRIDINE CARBOXAMIDE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to bipyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.03-11-2010
20120095010TRICYCLIC DELTA-OPIOID MODULATORS - The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic δ-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.04-19-2012
20120095009SYNTHESIS AND ANTI-PROLIFERATIVE EFFECT OF BENZIMIDAZOLE DERIVATIVES - This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated. In particular, the disclosure provides for substituted imidazo[4,5-b]pyrazine compounds having the general formula04-19-2012
20120095008COMPOSITION AND METHODS FOR THE TREATMENT OF WOUNDS - The present invention is directed to a wound composition comprising an effective amount of phenytoin and an effective amount of vitamin C. The present invention is further directed to a method of treating a wound in a patient comprising administering an effective amount of phenytoin and an effective amount of vitamin C to the wound.04-19-2012
20130210826METHODS FOR TREATING PAIN - The present invention features methods and compositions for preventing, reducing, or treating a traumatic, metabolic, or toxic peripheral nerve lesion or pain including neuropathic pain, inflammatory, and nociceptive pain by administering to a mammal a compound that reduces expression or activity of BH4. This reduction may be achieved by reducing activity of a BH4 synthetic enzyme, including GTP cyclohydrolase, sepiapterin reductase, or dihydropteridine reductase; antagonizing the cofactor function of BH4 or BH4-dependent enzymes; or blocking BH4 binding to membrane bound receptors. The invention provides methods for diagnosing pain or a peripheral nerve lesion in a mammal by measuring levels of BH4 or its metabolites in biological sample or the levels or activity of any one of the BH4 synthetic enzyme in tissue samples of a mammal. Disclosed are screening methods that use BH4 or BH4 synthetic enzymes, BH4-dependent enzymes, and BH4-binding receptors to identify therapeutics for the treatment, prevention, or reduction of pain.08-15-2013
20130210827NOVEL BENZENESULFONAMIDES AS CALCIUM CHANNEL BLOCKERS - The present application relates to calcium channel inhibitors comprising compounds of formula (I), formula (II), formula (III), or formula (IV),08-15-2013
20130210828STRUCTURE, SYNTHESIS, AND APPLICATIONS FOR POLY (PHENYLENE) ETHYNYLENES (PPEs) - The present disclosure provides novel poly(phenylene ethynylene) (PPE) compounds, methods for synthesizing these compounds, and materials and substances incorporating these compounds. The various PPEs show antibacterial, antiviral and antifungal activity.08-15-2013