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Nitrogen bonded directly to the 1,3-diazine at 2-position by a single bond

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.)

514256000 - 1,3-diazines (e.g., pyrimidines, etc.)

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Entries
DocumentTitleDate
20130045986NOVEL COMPOUNDS AS MODULATORS OF GPR-119 - The present invention relates to novel compounds of formula (A) and (B) as modulators of GPR-119, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of GPR-119 mediated diseases or disorders with them.02-21-2013
20080269269Crystalline Forms of 4-Methyl-N- [3-(4-Methyl-Imidazol-1-Yl)-5-Trifluoromethyl-Phenyl]-3- (4-Pyridin-3-Yl-Pyrimidin-2-Ylamino) -Benzamide - Polymorphic forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base and salts thereof are prepared by various processes.10-30-2008
20120184574INDOLE DERIVATIVES AND METHODS FOR ANTIVIRAL TREATMENT - The present invention is directed to compounds and forms and pharmaceutical compositions thereof useful for treating a viral infection, or for affecting viral activity by modulating viral replication.07-19-2012
20120184575TOPICAL ADMINISTRATION CARRIER COMPOSITION AND THERAPEUTIC FORMULATIONS COMPRISING SAME - A topical administration carrier composition including water, glycerin and polysorbate, suitable for use in formulations with active ingredient compositions containing active ingredients such as minoxidil that are susceptible to systemic penetration, and solvents that are susceptible to evaporative loss, when the active ingredient composition is topically applied to the body. The carrier formulation retards the evaporative losses of the solvent component(s) and systemic migration losses of the active ingredient composition, to provide sustained topical action, in relation to formulations lacking the carrier composition of the invention.07-19-2012
20090181994TRIAZOLE DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE-1 - Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.07-16-2009
20090192181PYRIMIDINYL AMIDE COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 - Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.07-30-2009
20110195985COMPOUNDS FOR THE TREATMENT OF LYSOSOMAL STORAGE DISEASES - A method of treating a lysosomal storage disease comprises administering a pyrimethamine derivative to a subject in need thereof.08-11-2011
20110195986PYRROLONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS - The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I08-11-2011
20100087467Compositions Useful As Inhibitors of Protein Kinases - The present invention provides compounds of formula I:04-08-2010
20130210848NEW SALT OF A PYRIMIDIN DERIVATIVE - The present invention relates to a salt of a pyrimidin derivative of the acid (3R,5S,6E)-7-[4-(4-fluorophenyl)-2-(N-methylmethanesulfonamide)-6-(propan-2-yl)pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic, to a method for preparing same and to the use thereof in formulating pharmaceutical formulations.08-15-2013
20100076002Method of Treating Atherosclerosis, Dyslipidemias and Related Conditions and Pharmaceutical Compositions - A method of treating atherosclerosis is disclosed wherein nicotinic acid or another nicotinic acid receptor agonist is administered to the patient in combination with a DP receptor antagonist. The DP receptor antagonist is administered to reduce, prevent or eliminate flushing that may otherwise occur.03-25-2010
20100076001IMIDAZOLIDINONYL AMINOPYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER - The present invention provides novel imidazolidinonyl aminopyrimidine compounds believed to have clinical use for treatment of cancer through inhibiting Plk1. wherein: R03-25-2010
20120245189CRYSTALLINE CDC7 INHIBITOR SALTS - The present invention relates to novel crystalline salts of a CDC7 or CDC7/CDKs inhibitor, to a novel crystal form of the corresponding free base, to a process for their preparation, to hydrates, solvates and polymorphs of such new salt forms, to their use in therapy and to pharmaceutical compositions containing them. Such crystal salts are selected from L-asparate, hemifumarate, hydrochloride, maleate, mesylate, sulfate, L-tartrate or phosphate salts of 5-(2-amino-pyrimidin-4-yl)-2-(2,4-dichloro-phenyl)-1H-pyrrole-3-carboxylic acid amide.09-27-2012
20130079363COMBINATIONS OF PYRIMETHANIL AND MONOTERPENES - The present invention relates to combinations of pyrimethanil, or a salt thereof, and a monoterpene, or a salt thereof, which provide an improved biocidal effect. More particularly, the present invention relates to compositions comprising a combination of pyrimethanil, or a salt thereof, together with a monoterpene selected from thymol and β-thujaplicin in respective proportions to provide a synergistic biocidal effect. Compositions comprising these combinations are useful for the protection of any living or non-living material, such as crops, plants, fruits, seeds, objects made of wood, thatch or the like, engineering material, biodegradable material and textiles against deterioration due to the action of microorganisms such as bacteria, fungi, yeasts, algae, virusses, and the like.03-28-2013
20090258888Pyrimidine Derivatives - This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly cancer.10-15-2009
20130040977Pro-Neurogenic Compounds - This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.02-14-2013
20130040976INDAZOLE INHIBITORS OF THE WNT SIGNAL PATHWAY AND THERAPEUTIC USES THEREOF - Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states.02-14-2013
20100041687HYDROBROMIDE SALT OF AN ANTI-HIV COMPOUND - Solid dispersions and dosage forms comprising the hydrobromide salt of a diarylpyrimidine derivative, useful as an anti-HIV agent.02-18-2010
201000996942-ANILINO-4-HETEROARYL PYRIMIDINE DERIVATIVES, AND PREPARATION THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS, AND IN PARTICULAR IKK INHIBITORS - The disclosure relates to a compound of formula (I):04-22-2010
20130210847PROCESS FOR THE PREPARATION OF NILOTINIB - The present invention relates a process for the preparation of a compound of formula (I):08-15-2013
201001447722,2,2-TRI-SUBSTITUTED ACETAMIDE DERIVATIVES AS GLUCOKINASE ACTIVATORS, THEIR PROCESS AND PHARMACEUTICAL APPLICATION - Compounds of the present disclosure are 2,2,2-tri-substituted acetamide derivatives of formula (I), its polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, useful as Glucokinase activator. Processes of their preparation are also described in the disclosure. The disclosure also describes method to characterize partial glucokinase activators.06-10-2010
20080287477Novel Compounds as Modulators of Ppar - Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.11-20-2008
20100041688REVAPRAZAN-CONTAINING SOLID DISPERSION AND PROCESS FOR THE PREPARATION THEREOF - The present invention provides a solid dispersion in which revaprazan particles are surface-modified with a water-soluble polymer, a water-soluble saccharide, a surfactant, or a mixture thereof and a process for preparing the same. The present invention also provides a pharmaceutical composition containing the solid dispersion and a process for preparing the pharmaceutical composition.02-18-2010
20090156623N-ARYL PIPERIDINE SUBSTITUTED BIPHENYLCARBOXAMIDES - N-aryl piperidine substituted biphenylcarboxamides compounds of formula (I)06-18-2009
200901566222,4-PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES - The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.06-18-2009
20090156621HCV INHIBITORS - The present invention relates to compounds that are useful in the treatment of viruses belonging to Flaviviridae, including flaviviruses, pestiviruses, and hepaciviruses. The invention includes compounds useful for the treatment or prophylaxis of dengue fever, yellow fever, West Nile virus, and HCV.06-18-2009
20100105712CHEMICAL COMPOUNDS - Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.04-29-2010
20100105711Organic Compounds - The present invention relates to a compound of formula (I)04-29-2010
20090286821INHIBITORS OF TYROSINE KINASES - The invention relates to compounds of formula11-19-2009
20090105287Inhibitors of Dihydrofolate Reductase With Antibacterial Antiprotozoal, Antifungal and Anticancer Properties - The compositions and methods described herein discloses the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as 04-23-2009
20100093776Organic Compounds and Their Uses - The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases.04-15-2010
20090124647Indole Derivatives as Antitumoral Compounds - Antitumoural compounds of general formula (I); wherein Ar is an heterocyclic group of formula (a) and R05-14-2009
20090124646SUBSTITUTED INDOLYL ALKYL AMINO DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I)05-14-2009
20120165355METHODS AND COMPOSITIONS FOR TREATING CANCERS - This invention provides a combination of antagonists of the hedgehog signaling pathway with a BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with protein tyrosine kinases such as, for example, Src, BCR-ABL and c-kit.06-28-2012
20120165354TREATMENT METHOD - The present invention relates to methods of treating age-related macular degeneration in a patient by administration of pazopanib or pharmaceutically acceptable salts or solvates thereof.06-28-2012
20130090347ETHYNYL DERIVATIVES - The present invention relates to ethynyl derivatives of formula I04-11-2013
20090306117ROSUVASTATIN ZINC SALT - The present invention is related to rosuvastatin zinc salt of the Formula (I), process for preparation thereof and medicinal products containing said salt. Rosuvastatin zinc salt according to the present invention is prepared by reacting rosuvastatin with a zinc alcoholate, zinc enolate or an inorganic or organic zinc salt and isolating the thus obtained rosuvastatin zinc salt (2:1).12-10-2009
20090306115Phenyl ethyne compounds - In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted or unsubstituted six membered heterocyclic ring that includes at least two nitrogen atoms. The ring additionally includes four carbon atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon triple bond. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system. Invention compounds may also act as insecticides, and as fungicides. Pharmaceutical compositions containing invention compounds also have wide utility.12-10-2009
20090306116PYRIMIDINE DERIVATIVES FOR THE INHIBITION OF IGF-IR TYROSINE KINASE ACTIVITY - A compound of formula (I) wherein the substituents are as defined in the text for use in inhibiting insulin-like growth factor 1 receptor activity in a warm blooded animal such as man.12-10-2009
20130165462HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.06-27-2013
20090093508THERAPEUTIC OR PROPHYLACTIC AGENT FOR ALLERGIC DERMATITIS - A therapeutic or prophylactic agent for allergic dermatitis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for allergic dermatitis according to the present invention has high therapeutic or prophylactic effect.04-09-2009
20090093507CDK INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The compounds of the invention may further act as HDAC inhibitors.04-09-2009
20090093506Copper antagonist compositions - Pharmaceutical compositions having a pharmaceutically acceptable copper antagonist compound(s) or a pharmaceutically acceptable salt or prodrug thereof, including copper (II) antagonists, and a pharmaceutically acceptable 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor or a pharmaceutically acceptable salt or prodrug thereof, articles and kits and delivery devices containing such compositions, tablets and capsules and formulations containing such compositions, and methods of use for treatment of subjects, including humans, who have or are at risk for various diseases, disorders, and conditions.04-09-2009
20130072510Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine H4 receptor - Benzoimidazol-2-yl pyrimidines and pyrazines, pharmaceutical compositions and methods for H03-21-2013
20130072509PTEROSTILBENE AND STATIN COMBINATION FOR TREATMENT OF METABOLIC DISEASE, CARDIOVASCULAR DISEASE, AND INFLAMMATION - A pharmaceutical composition is provided comprising a therapeutically effective amount of pterostilbene, a therapeutically effective amount of a statin compound, and a pharmaceutically acceptable carrier. The embodiments of the pharmaceutical compositions can have lipid lowering properties, or alternatively can have properties that can treat oxidative stress, by decreasing inflammation or inflammatory processes contributing to neurodegenerative diseases. A method of lowering lipid levels in an individual is also provided, comprising administering to the individual in need of such treatment a pharmaceutical composition including a therapeutically effective amount of pterostilbene, a therapeutically effective amount of a statin compound, and a pharmaceutically acceptable carrier, wherein lipid levels are decreased.03-21-2013
20130059873PHARMACEUTICAL COMPOSITIONS AS INHIBITORS OF DIPEPTIDYL PEPTIDASE-IV (DPP-IV) - The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.03-07-2013
20110015218AZA-BICYCLOHEXYL SUBSTITUTED INDOLYL ALKYL AMINO DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I)01-20-2011
20110015217Pro-Neurogenic Compounds - This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death.01-20-2011
200902704332,3-DIHYDRO-IMINOISOINDOLE DERIVATIVES - A compound represented by the following general formula (1), or a salt thereof has serine protease inhibiting activity, and particularly excellent inhibiting activity against clotting factor VIIa. This compound or a salt thereof is useful as therapeutic and/or prophylactic agents for diseases associated with thrombus formation.10-29-2009
20090012108SALT OF 4-[[4-[[4-(2-CYANOETHENYL)-2,6-DIMETHYLPHENYL]AMINO]-2-PYRIMIDINYL]AMINO]BENZONITRILE - The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethyl-phenyl]amino]-2-pyrimidinyl]amino]benzonitrile and to processes for their preparation.01-08-2009
20100087464PROTEIN KINASE INHIBITORS AND METHODS FOR USING THEREOF - The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of TrkA, TrkB, TrkC, Abl, Bcr-Abl, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKCα, Raf, ROCK-II, Rsk1, and SGK kinases, or a combination thereof.04-08-2010
20080306100PHENYLAMINOPYRIMIDINE DERIVATIVES AS INHIBITORS OF BCR-ABL KINASE - The present invention relates to novel intermediates useful for the preparation of novel phenylaminopyrimidine derivatives, novel phenylaminopyrimidine derivatives. Pharmaceutical composition containing the novel phenylaminopyrimidine derivatives and processes for their preparation. The invention particularly relates to novel Phenyl pyrimidine amine derivatives of the general formula (I). The novel compounds of the formula 1 can be used in the therapy of Chronic Myeloid Leukemia (CML). Since the IC12-11-2008
20120238593HETEROCYCLIC COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.09-20-2012
20130165464HETEROARYLS AND USES THEREOF - This invention provides compounds of formula IB:06-27-2013
20080293751Tetralin and indane derivatives and uses thereof - Compounds of the formula I:11-27-2008
20080293750Susceptibility Gene for Myocardial Infarction, Stroke, Paod and Methods of Treatment - Linkage of myocardial infarction (MI) and a locus on chromosome 13q12 is disclosed. In particular, the FLAP gene within this locus is shown by genetic association analysis to be a susceptibility gene for MI and ACS, as well as stroke and PAOD. Pathway targeting for treatment and diagnostic applications in identifying those who are at risk of developing MI, ACS, stroke or PAOD, in particular are described. The invention also provides for compositions comprising a leukotriene synthesis inhibitor and a stating and methods of using these compositions to reduce C-reactive protein in a human subject at risk of MI, ACS, stroke and/or PAOD.11-27-2008
20130165461METHODS OF TREATING HEART FAILURE - Methods of treating heart failure by administration of beneficial agents to the heart.06-27-2013
20130165463INHIBITION OF FOCAL ADHESION KINASE FOR CONTROL OF SCAR TISSUE FORMATION - The formation of scars at a wound site is reduced by contacting the wound site with an effective dose of an inhibitor of focal adhesion kinase (FAK) activity or expression. Blockade of FAK is sufficient to prevent mechanical and inflammatory stimuli from activating MCP-1 pathways. In addition to these chemokine-mediated mechanisms, inhibition of FAK may control fibrosis by blocking fibroblast collagen production. Pharmacologic blockade of FAK significantly reduces scar formation in vivo.06-27-2013
20130165465Crystalline Forms of 4-Methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyr- idin-3-yl-pyrimidin-2-ylamino)-benzamide - Crystalline forms of 4-methyl-N-3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base and salts thereof are prepared by various processes.06-27-2013
20110118292METHOD OF TREATING ATHEROSCLEROSIS, DYSLIPIDEMIAS AND RELATED CONDITIONS - A method of treating atherosclerosis is disclosed wherein nicotinic acid or another nicotinic acid receptor agonist is administered to the patient in combination with a DP receptor antagonist. The DP receptor antagonist is administered to reduce, prevent or eliminate flushing that may otherwise occur.05-19-2011
20110294840HYDRAZIDE COMPOUND AND USE OF THE SAME IN PEST CONTROL - There is provided a hydrazide compound having a controlling effect on pests represented by the formula (1): wherein, G is a 5-membered heterocyclic group, M is an oxygen atom or a sulfur atom, Q12-01-2011
20090111839Process for Preparing Amorphous Rosuvastatin Calcium of Impurities - A pure amorphous form of rosuvastatin calcium substantially free from alkali metal impurities is disclosed. A process of preparing a pure amorphous form of rosuvastatin calcium is disclosed, which comprises hydrolysis of C04-30-2009
20110281901PHARMACEUTICAL COMPOSITIONS AND METHODS OF MAKING SAME - Pharmaceutical compositions that include an amount of an acid addition salt of pazopanib equivalent to about 5 mg/mL pazopanib, about 2.0 to about 13.0% w/w of a modified cyclodextrin suitable for use in an ophthalmic formulation, and pH adjusting agent as well as methods of making the same are described.11-17-2011
20100190812NILOTINIB HCL CRYSTALLINE FORMS - Crystalline forms of Nilotinib HCl are described.07-29-2010
20100099693NEW COMBINATION FOR USE IN THE TREATMENT OF INFLAMMATORY DISORDERS - There is provided combination products comprising (a) ramatroban, or a pharmaceutically-acceptable salt or solvate thereof and (b) a statin, or a pharmaceutically-acceptable salt or solvate thereof. Such combination products find particular utility in the treatment of atherosclerosis and related conditions.04-22-2010
20110281902COMBINATIONS COMPRISING A PROTEIN KINASE INHIBITOR BEING A PYRIMIDYLAMINOBENZAMIDE COMPOUND AND A HSP90 INHIBITOR SUCH AS 17-AAG - The invention provides a pharmaceutical combination comprising: 11-17-2011
20090118316Methods for Augmenting Bone - The present invention relates to methods of stimulating osteoblast function with a PYK2 inhibitor in subjects with osteoporosis, bone fractures, non-unions, pseudoarthroses, periodontal disease or other disorders of bone metabolism. Optionally, the method further comprises administration of a second therapeutic bone agent. The present invention also relates to methods to identify a PYK2 inhibitor effective as a therapeutic bone agent comprising administering a test agent to an osteoblast-like cell and determining if osteoblast function is stimulated. Optionally, the identifying method further comprises contacting the test agent with PYK2 and determining if PYK2 activity is inhibited.05-07-2009
20120289527MONO-HYDROCHLORIC SALTS OF AN INHIBITOR OF HISTONE DEACETYLASE - This invention provides novel crystalline forms of mono-HCl salts and a mono-HCl salt hydrate of JNJ-26481585, an inhibitor of histone deacetylases. The invention also relates to processes for production of these forms, to intermediates used in these processes, to pharmaceutical compositions comprising these forms, and to the use of these forms in medical treatment for instance as a medicine to inhibit proliferative conditions, such as cancer and leukemia.11-15-2012
20110301186USE OF HAPTOGLOBIN GENOTYPING IN DIAGNOSIS AND TREATMENT OF CARDIOVASCULAR DISEASE - This invention is directed to methods and compositions for the treatment of cardiovascular disorders. Specifically, the invention is directed to compositions comprising vitamin E, statins and/or glutathione peroxidase mimetics; methods of treating diabetic patients expressing the Hp-2-2 haptoglobin genotype; a method of inhibiting or suppressing a cardiovascular disorder in a diabetic subject, treating cardiovascular disease in subjects exhibiting the Haptoglobin Hp-2-2 genotype; and methods of treating cardiovascular disease in subjects exhibiting the Haptoglobin Hp-2-2 genotype.12-08-2011
20120015967PYRIMIDINE AND PYRIDINE DERIVATIVES AS POSH AND POSH-AP INHIBITORS - Pyridine and pyrimidine derivatives inhibit ubiquitination of human polypeptides, particularly of POSH and POSH-associated proteins such as HERPUD1, and can be used as medicaments for treatment of viral infections caused by virus such as HIV and for treatment of neurological disorders or diseases.01-19-2012
20110098315PHARMACEUTICAL COMPOSITIONS OF ROSUVASTATIN CALCIUM - This invention is related to pharmaceutical compositions of rosuvastatin or pharmaceutically acceptable salts thereof especially calcium salt with sodium carbonate anhydrous which has effects on dissoltion profiles in 0.1 N HCI medium provided that using of sodium carbonate anhydrous should be presence in the range of from about 0.5% to about 2% by weight.04-28-2011
20110112125Novel hair growth composition - A water-soluble minoxidil composition for topical use significantly enhances the transdermal delivery of the drug in comparison with that of Rogaine. The composition contains minoxidil, water, enhancer, and polymer. The percentage of water in the composition may be up to 95%.05-12-2011
20100035906Dipyridyl-dihydropyrazolones and their use - The present application relates to novel dipyridyl-dihydropyrazolones, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.02-11-2010
20110190328ACID ADDITION SALTS OF (3,5-BIS TRIFLUOROMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3YL-PYRIMIDIN-2YLAMINO)-PHENYL]- -BENZAMIDE - The present invention relates to acid addition salts of the pharmaceutically active compound (3,5-Bistrifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide(I):08-04-2011
20090286820(R)-PHENYL(HETEROCYCLE)METHANOL-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM AND METHODS OF THEIR USE - Multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use are described. Compounds described include those of formula I:11-19-2009
20090099219ALKYNYLPYRIMIDINES AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME - The invention relates to alkynylpyrimidines according to the general formula (I):04-16-2009
20100069417NOVEL PHENYL(4-PHENYLPYRIMIDIN-2-YL)AMINE DERIVATIVES, THEIR PREPARATION, AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND IN PARTICULAR AS IKK INHIBITORS - The disclosure relates to a compound of formula (I):03-18-2010
20090170884FUNGICIDAL ACTIVE SUBSTANCE COMBINATION - Active compound combinations comprising an oxime ether derivative of the formula (I)07-02-2009
20100035907NEW 2,4-DIANILINOPYRIMIDINES, PREPARATION THEREOF AS DRUGS, PHARMACEUTICAL COMPOSITIONS AND USE THEREOF ESSENTIALLY AS IKK INHIBITORS - The disclosure relates to a compound of formula (I):02-11-2010
20090062320Method of Treating Disorders Mediated by the Fibroblast Growth Factor Receptor - The disclosure includes a method of treating a warm-blooded animal having a disorder mediated by the fibroblast growth factor receptor (FGFR), in particular 8p11 myelo-proliferative syndrome (EMS), pituitary tumors, retinoblastoma, synovial sarcoma, chronic obstructive pulmonary disease (COPD), seborrheic keratosis, obesity, diabetes and related disorders, autosomal dominant hypophosphatemic Rickets (ADHR), X-chromosome linked hypophosphatemic rickets (XLH), tumor-induced osteomalacia (TIO) and fibrous dysplasia of the bone (FD), as well as to a method of promoting localized neochondrogenesis, as well as a method of treating hepatocellular carcinoma, lung cancer, especially pulmonary adnocarcinoma, oral squameous cell carcinoma, or esophageal squameous cell carcinoma, or any combination of two or more such diseases.03-05-2009
20100267755PYRIMIDINE DERIVATIVES - The invention provides the compounds of formula (I)10-21-2010
20110124670Use of Pyrimidylaminobenzamide Derivatives for the Treatment of Fibrosis - The invention relates to the use of a pyrimidylaminobenzamides of formula I05-26-2011
20080318989Pyrimidine Kinase Inhibitors - The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula (I) wherein ring A, X, Y, Z, R12-25-2008
20120035198Antiviral Compounds and Methods of Using Thereof - Disclosed herein are compounds which exhibit antiviral activity against a plurality of viruses belonging to different families such as Bornaviridae, Filoviridae, Paramyxoviridae, Rhabdoviridae, Arenaviridae, Bunyaviridae, Orthomyxoviridae, and Poxviridae. Thus, methods of preventing, inhibiting, or reducing the viral activity of various viruses are provided as well as methods of treating viral infections.02-09-2012
20100087465HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS - Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. The compounds of the invention are orally active.04-08-2010
20100087462METHODS FOR PREDICTING AND DETECTING INTOLERANCE TO AN HYPOLIPIDEMIC AGENT - The invention describes methods and tools for the identification of drug intolerance into subjects receiving an hypolipidemic agent. The invention further describes methods and tools for the prediction of drug intolerance in subjects in need of hypolipidemic agents. Some aspects of the invention are based on the assessment of the subject plasma glycerol concentrations. Some aspects of the invention are based on the assessment of the subject HDL-triglycerides concentration. Some other aspects are based on the identification of hepatic lipase gene variants in a subject genome.04-08-2010
20100087463PHARMACEUTICAL COMPOSITIONS COMPRISING NILOTINIB OR ITS SALT - A pharmaceutical composition, especially capsules. comprising granules containing nilotinib or a salt thereof with at least one pharmaceutically acceptable excipient. The granules may be produced by a wet granulation process.04-08-2010
20120108617METHODS AND COMPOSITIONS INVOLVING (S)-BUCINDOLOL - Disclosed is bucindolol substantially free of its R-stereoisomer. Also disclosed are pharmaceutical compositions that include bucindolol substantially free of its R-stereoisomer or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. Also disclosed are methods of treating a patient that involve administering to the patient a therapeutically effective amount of a composition of the present invention. Formula (I).05-03-2012
20090054474Novel pyrimidine compound having benzyl(pyridylmethyl)amine structure and medicament comprising the same - A compound represented by the following general formula (I) or a salt thereof, or a solvate thereof:02-26-2009
20090036476BENZIMIDAZOLE DERIVATIVES AND THEIR USE FOR MODULATING THE GABAA RECEPTOR COMPLEX - This invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith.02-05-2009
20090170885NAPHTHYRIDINE DERIVATIVES AS POTASSIUM CHANNEL MODULATORS - This invention provided compounds of formula I07-02-2009
20080207658Pharmaceutical Combination of Bcr-Abl and Raf Inhibitors - The invention provides a pharmaceutical combination comprising: a) a pyrimidylaminobenzamide compound, and b) a RAF kinase inhibitor and a method for treating or preventing a proliferative disease using such a combination, wherein compound a) has the following general Formula: (I).08-28-2008
20080207659INHIBITORS OF PHOSPHODIESTERASE TYPE 4 - The present invention relates to inhibitors of phosphodiesterase (PDE) type 4.08-28-2008
20090270434AZACYCLOALKANE DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. 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; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.10-29-2009
20090042920CARBONYLAMINO-DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I)02-12-2009
20090042919METHOD FOR MODULATING GPR119 G PROTEIN-COUPLED RECEPTOR AND SELECTED COMPOUNDS - A method of modulating the activity of the GPR119 G protein-coupled receptor comprising administering to a mammalian patient in need thereof a therapeutically effective amount of at least one compound of Formula I or Formula IA and, optionally, an additional therapeutic agent.02-12-2009
20100113492Substituted Aminopyrimidines as Cholecystokinin-1 Receptor Modulators - Certain novel substituted aminopyrimidines are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.05-06-2010
20100298366CHEMOKINE RECEPTOR BINDING COMPOUNDS - The present invention relates to chemokine receptor binding compounds, pharmaceutical compositions and their use. More specifically, the present invention relates to modulators of chemokine receptor activity, preferably modulators of CCR5. These compounds demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).11-25-2010
20080275073CRYSTALLINE FORMS AND POLYMORPHS OF N-(3-(DIMETHYLAMINO)PROPYL)-4-(4-(3-FLUORO-4-METHOXYPHENYL) PYRIMIDIN-2-YLAMINO) BENZENESULFONAMIDE AS PHARMACEUTICALLY ACCEPTABLE SALTS - The present invention relates to one or more crystalline forms and polymorphs of compounds of formula I:11-06-2008
20080249120Pharmaceutical compositions - A pharmaceutical composition in solid form containing at least a therapeutically effective amount of one or more statins in the free acid form is disclosed.10-09-2008
20130217715DERIVATIVES OF PYRAZOLOPHENYL-BENZENESULFONAMIDE COMPOUNDS AND USE THEREOF AS ANTITUMOR AGENTS - Substituted pyrazolophenyl-benzenesulfonamide compounds of formula (I) are described, wherein m, R1, R2, R3, and R4 are defined in the description, which modulate the activity of protein kinases, These compounds find utility in treating diseases caused by deregulated protein kinase activity, such as cancer and cell proliferative disorders.08-22-2013
20080207660PHOSPHODIESTERASE 4 INHIBITORS - Selective PDE4 inhibition is achieved by aryl and heteroaryl pyrazole compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds such as rolipram and show selectivity with regard to inhibition of other classes of PDEs.08-28-2008
20080269268Substituted Phenylamino-Pyrimidines - The invention relates to substituted phenylaminopyrimidines, to a process for their preparation and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases in humans and animals, in particular cardiovascular disorders.10-30-2008
20110207759METHOD FOR TREATMENT OF ATHEROSCLEROTIC DISEASE - A method of effecting regression of atherosclerotic disease in a patient whose plasma lipid concentrations are at levels considered normal or optimal. The method involves treating the patient with a combination of a 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitor and niacin. Disease regression has been observed over periods as short as 14 months, preferably 8 months.08-25-2011
200902644522-(Phenylamino)-Pyrimidin-5-Amides As Cannabinoid 2 Receptors Modulators for the Treatment of Immune or Inflammatory Disorders - The present invention relates to novel pyrimidine derivatives such as compounds of the formula (I):10-22-2009
20080269270Triol form of rosuvastatin and synthesis of rosuvastatin - Provided is a rosuvastatin triol and its use as a reference standard for analysis of rosuvastatin. Also provided are methods for preparation of rosuvastatin.10-30-2008
20120196886COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-furancarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.08-02-2012
20090030023PYRIMIDINE COMPOUNDS AND MEDICINAL COMPOSITION THEREOF - A compound represented by the following formula (I), a salt, or a solvate thereof:01-29-2009
20090181993HIV INHIBITING 5-HETEROCYCLYL PYRIMIDINES - HIV replication inhibitors of formula (I), N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein -a07-16-2009
200901819952-ANILINO-4-AMINOALKYLENEAMINOPYRIMIDINES - The present invention relates to 2-arylamino-4-(aminoalkylene)aminopyrimidines inhibitors which are inhibitors and therefore inhibit Protein Kinase C-alpha (PKC-α). The PKC-α inhibitors of the present invention are important for improving myocardial intracellular calcium cycling, resulting in improved myocardial contraction and relaxation performance and thereby slowing the progression of heart failure. The present invention further relates to compositions comprising said 2-arylamino-4-(aminoalkylene)amino-pyrimidines and to methods for controlling, abating, or otherwise slowing the progression of heart failure.07-16-2009
20090054475HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS - Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. The compounds of the invention are orally active.02-26-2009
20090005406Cancer Treatment Method - The present invention relates to a method of treating cancer in a mammal by administration of pyrimidine derivatives. In particular, the method relates to a method of treating cancer by administration of 5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide or a salt or solvate thereof.01-01-2009
20080234302Novel Processes for Preparing Amorphous Rosuvastatin Calcium and a Novel Polymorphic Form of Rosuvastatin Sodium - Provided are processes for preparing amorphous rosuvastatin calcium from crystalline rosuvastatin calcium by simple precipitation processes. Also provided is a novel polymorphic form of rosuvastatin sodium, processes for preparing thereof and pharmaceutical compositions thereof.09-25-2008
20080318988Pyrimidylaminobenzamide Derivatives For the Treatment of Neurofibromatosis - The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF, and to a method of treating non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF.12-25-2008
20090209566Spirocyclic Compounds - The present invention relates to a novel class of substituted spirocyclic compounds, represented by the following structural Formula: I Wherein A, B and D are independently selected from CR08-20-2009
20090030024THIAZOLES AS FUNGICIDES - Use of compounds of the formula (I),01-29-2009
20090082380DEUTERIUM-ENRICHED ROSUVASTATIN - The present application describes deuterium-enriched rosuvastatin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-26-2009
20120289528METHOD OF TREATING PROLIFERATIVE DISORDERS AND OTHER PATHOLOGICAL CONDITIONS MEDIATED BY BCR-ABL, C-KIT, DDR1, DDR2 OR PDGF-R KINASE ACTIVITY - The present invention relates to a regimen for the administration of a pyrimidylaminobenzamide of formula I11-15-2012
20110224244Adamantyl Benzamide Derivatives - Embodiments of the present invention provide adamantyl benzamide derivtives and pharmaceutical compositions comprising adamantyl benzamide derivatives. Methods of use of such compounds and compositions to modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) in a subject are also provided.09-15-2011
20110230507Piperidine GPCR Agonists - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of diabetes and obesity.09-22-2011
20090192180Alpha-7 Nicotinic Receptor Agonists and Statins In Combination - Combinations of α7-nAChR agonists and statins, pharmaceutical compositions containing the same and methods of using the same useful for treatment or prophylaxis of neurological degenerative diseases.07-30-2009
20110230508Novel Forms of a Fused Pyrrolocarbazole Compound - Alternative chemical and/or solid state forms of Compound I, processes to reproducibly make them and methods of treating patients using them.09-22-2011
20080262009CRYSTALLINE POLYMORPHS OF N-(3-(DIMETHYLAMINO)PROPYL)-4-(4-(3-FLUORO-4-METHOXYPHENYL) PYRIMIDIN-2-YLAMINO) BENZENESULFONAMIDE AS ACETATE SALTS - The present invention relates to methods for preparing one or more crystalline forms and polymorphs of a compound of formula I:10-23-2008
20080262008CRYSTALLINE FORMS AND POLYMORPHS OF N-(3-(DIMETHYLAMINO)PROPYL)-4-(4-(3-FLUORO-4-METHOXYPHENYL) PYRIMIDIN-2-YLAMINO) BENZENESULFONAMIDE AS SUCCINATE SALTS - The present invention relates to methods for preparing and manufacturing a crystalline form or polymorph of a compound of formula I:10-23-2008
20080262007Hiv Inhibiting 5-Substituted Pyrimidines - HIV replication inhibitors of formula10-23-2008
20090203720Methods for inhibiting cell growth - Cell growth is inhibited and/or cell death is induced in a cell by administering an RXR agonist and an inhibitor of casein kinase 1α. A cell or a tissue can be screened for enhanced susceptibility to cell death or interference with cell growth. Conditions characterized by uncontrolled cell growth or proliferation, such as a cancer, can be treated with inhibitors of casein kinase 1α.08-13-2009
20120077833ACID ADDITION SALTS OF (3,5-BIS TRIFLUOROMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3YL-PYRIMIDIN-2YLAMINO)-PHENYL]- -BENZAMIDE - The present invention relates to acid addition salts of the pharmaceutically active compound (3,5-Bistrifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide(I):03-29-2012
20120077832BESYLATE SALT OF A BTK INHIBITOR - The present invention provides a salt form, and compositions thereof, useful as an inhibitor of one or more protein kinases and which exhibits desirable characteristics for the same.03-29-2012
20110144142Methods of Reducing Hair Loss and/or Facilitating Hair Growth and/or Regrowth - The present disclosure relates to methods of retarding hair loss or facilitating hair growth and/or regrowth. More specifically, the present disclosure relates to methods of using the disclosed compositions to increase the rate of terminal hair growth and/or regrowth in a mammal.06-16-2011
20110144141Hair Growth and/or Regrowth Compositions - The present disclosure relates to compositions containing certain pyrimidine compounds such as minoxidil and/or certain pyrimidine sulfate (inner salt) compounds such as minoxidil sulfate and especially compositions containing pyrimidine compounds in combination with an admixtures comprising at least one antioxidant, at least one organic acid and a select fatty acid mixture. The present disclosure also relates to use of the compositions to grow and/or regrow hair and/or prevent hair loss in mammals and particularly in humans.06-16-2011
20090221619NOVEL MATERIALS AND METHODS FOR THE PRODUCTION THEREOF - The present invention relates to, inter alia, methods for the treatment of wallboards with fungicides and the treated wallboards. In particular, the invention relates to the treatment of wallboards with synergistic combinations of an anilinopyrimidine fungicide and other fungicides. The invention also provides the treatment of building materials with synergistic mixtures containing an anilinopyrimidine fungicide. More specifically the anilinopyrimidine fungicide is cyprodinil.09-03-2009
20110118291SUBSTITUTED INDOLYL-ALKYL-AMINO-DERIVATIVES AS INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (1)05-19-2011
20120196885NEW HISTONE DEACETYLASE INHIBITORS BASED SIMULTANEOUSLY ON TRISUBSTITUTED 1H-PYRROLES AND AROMATIC AND HETEROAROMATIC SPACERS - The present invention refers to compounds derived from trisubstituted 1H-pyrrole rings and aromatic rings, which have the following formula (I):08-02-2012
20090253724THERAPEUTIC OR PROPHYLACTIC AGENT FOR LEUKEMIA - A therapeutic or prophylactic agent for leukemia is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for leukemia according to the present invention shows the excellent absorbability and in vivo stability when orally administered, and exhibits prominent therapeutic or prophylactic effects.10-08-2009
20090253723PROTEIN KINASE INHIBITORS - Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.10-08-2009
20110003838Whitening Agent And Skin External Preparation - The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a compound represented by formula (1) or a pharmacologically acceptable salt thereof:01-06-2011
20100152219PYRAZOLE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSINE KINASES - Compounds of formula (I): and their use in the inhibition of Trk activity are described.06-17-2010
20100152218COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY - The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.06-17-2010
200900760472-Substituted Hydroxylaminopyrimidine, Method for the Production and the Use Thereof in the Form of Pesticides - 2-Substituted pyrimidines of the formula I,03-19-2009
20090048282PYRIMIDINE SULFONAMIDE ANALOGS AND THEIR USE AS AGONISTS OF THE WNT-BETA-CATENIN CELLULAR MESSAGING SYSTEM - The present invention relates to pyrimidine sulfonamide analogs, methods of making pyrimidine sulfonamide analogs, compositions comprising a pyrimidine sulfonamide analog, and methods for treating canonical Wnt-β-catenin cellular messaging system-related disorders comprising administering to a subject in need thereof an effective amount of a pyrimidine sulfonamide analog.02-19-2009
20090048281Organic Compounds - Compounds of Formula (I); in salt or zwitterionic form wherein R02-19-2009
20100184789INHIBITORS OF PROTEIN KINASES - The present invention relates to inhibitors of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to methods of preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases comprising the administration of an effective amount of at least one inhibitor of cyclin-dependent kinases.07-22-2010
20100184791COMPOUNDS AND COMPOSITIONS AS C-KIT AND PDGFR KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFRα and PDGFRβ kinases.07-22-2010
20100160361TREATMENT OF MAJOR ADVERSE CARDIAC EVENTS AND ACUTE CORONARY SYNDROME USING SECRETORY PHOSPHOLIPASE A2 (SPLA2) INHIBITOR OR SPLA2 INHIBITOR COMBINATION THERAPIES - Administration of sPLA06-24-2010
20100184792Co-Crystals of Pyrimethanil and Dithianon - The present invention relates to co-crystals of pyrimethanil and dithianon, which, in a X-ray powder diffractogram at 25° C. show at least three of the following reflexes: 07-22-2010
20100216828METHODS AND COMPOSITIONS FOR TREATING CANCERS - This invention provides a combination of antagonists of the hedgehog signaling pathway with a BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with protein tyrosine kinases such as, for example, Src, BCR-ABL and c-kit.08-26-2010
20090076046Compounds modulating c-fms and/or c-kit activity and uses therefor - Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.03-19-2009
20130217714Non-Flushing Niacin Analogues, and Methods of Use Thereof - One aspect of the present invention relates to substituted pyridines and pharmaceutically acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels.08-22-2013
20110112127COMPOUNDS 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, or forms thereof are active on Fms protein kinase, or on Fms and Kit protein kinase, or on Fms and Flt-3 protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinase, Kit protein kinase, or Flt-3 protein kinase including rheumatoid arthritis, osteoarthritis, multiple sclerosis, Alzheimer's disease, Parkinson's disease, glomerulonephritis, interstitial nephritis, Lupus nephritis, tubular necrosis, diabetic nephropathy, renal hypertrophy, acute myeloid leukemia, melanoma, multiple myeloma, metastatic breast cancer, prostate cancer, pancreatic cancer, neurofibromatosis, brain metastases, and gastrointestinal stromal tumors.05-12-2011
20100210673PYRIMIDYLAMINOBENZAMIDE DERIVATIVES FOR SYSTEMIC MASTOCYTOSIS - The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of systemic mastocytosis.08-19-2010
20100120807COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.05-13-2010
20090286819Process for Preparing the Calcium Salt of Rosuvastatin - An improved process for manufacture of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium salt, which is useful for the production of a pharmaceutical useful in the treatment of, inter alia, hypercholesterolemia, hyperlipoproteinemia and atherosclerosis, is described.11-19-2009
20090325989INDAZOLYL DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATING AGENTS - This invention relates to novel indazolyl derivatives useful as potassium channel modulating agents, and their use in the preparation of pharmaceutical compositions.12-31-2009
200901494874,5-DIPHENYL-PYRIMIDINYLAMINO SUBSTITUTED CARBOXYLIC ACIDS, METHOD FOR THE PRODUCTION AND USE THEREOF AS MEDICAMENTS - This invention relates to a compound of formula I,06-11-2009
20090318484Inhibitors of JNK - The invention relates to prodrugs of JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses prodrugs of JNK inhibitors, as described below in formula I:12-24-2009
20130131094PYRIMIDINE DERIVATIVES AS POSH AND POSH-AP INHIBITORS - Pyrimidine deriviatives are ubiquination inhibitors that inhibit the ubiquitin ligase activity, particularly of POSH polypeptides, are useful for the treatment of viral infections and neurological disorders.05-23-2013
20130131095ADMINISTRATION OF PYRIDINEDICARBOXYLIC ACID COMPOUNDS FOR STIMULATING OR INDUCING THE GROWTH OF HUMAN KERATINOUS FIBERS AND/OR ARRESTING THEIR LOSS - The invention relates to the use in a composition for caring for human hair or eyelashes of an effective amount of a pyridinedicarboxylic acid derivative of general formula (I) or of one of its salts,05-23-2013
20130131097TOPICAL TREATMENT FOR CHEMOTHERAPY INDUCED EYELASH LOSS OR HYPOTRICHOSIS USING PROSTAMIDE F2 ALPHA AGONISTS - The present invention is directed to compositions and methods for the treatment of post-chemotherapeutic hypotrichosis. More specifically, the present invention is directed to the use of compositions comprising bimatoprost for the treatment of post-chemotherapeutic hypotrichosis which may be applied before, during and after receiving chemotherapeutic treatment.05-23-2013
20100298364 SALTS 756 - The invention provides salts of 4-(dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate, pharmaceutical compositions containing them and their use in therapy.11-25-2010
20130137712Salts of 4-Methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-- 3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide - Salts of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide are prepared by various processes.05-30-2013
20090069360Organic Compounds - The present invention relates to the discovery that certain compounds inhibit, regulate and/or modulate tyrosine and serine/threonine kinase and kinase-like proteins, such as RAF kinase, a serine/threonine kinase that functions in the MAP kinase signaling pathway, and is concerned with compositions which contain these compounds, and methods of using them to treat tyrosine and serine/threonine kinase and kinase-like dependent diseases, such as angiogenesis, cancer and cardiac hypertrophy.03-12-2009
20090069357DEUTERIUM-ENRICHED ICLAPRIM - The present application describes deuterium-enriched iclaprim, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-12-2009
20090069356USE OF ANILINOPYRIMIDINES IN WOOD PROTECTION - The present invention relates to the use of the anilinopyrimidines pyrimethanil, cyprodinil and mepanipyrim for the protection of wood and wood materials against wood destroying and wood discolouring fungi.03-12-2009
20130143908METHOD FOR PREPARING ROSUVASTATIN CALCIUM INTERMEDIATE - A method for preparing a rosuvastatin calcium intermediate represented by formula I. The method includes: hydrolyzing an ester compound represented by formula II (in which, R represents C1-C5) in the presence of a metal compound to obtain a carboxylic acid compound represented by formula III; and reducing the carboxylic acid compound in the presence of a reductant.06-06-2013
20100240687METHOD FOR CHECKING AND CONTROLLING THE MAMMALIAN LACTIC ACID FERMENTATION PROCESS/AEROBIC GLUCOSE FERMENTATION METABOLIC PATHWAY IN MAMMALIAN ORGANISM - The method for qualitative and quantitative detecting of the extend of use and the correct process flow of the mammalian aerobic glucose fermentation metabolic pathway (mam-aGF) in a mammalian individual is characterized in that the enzyme TKTL1 is used as indicator and target molecule and the structural and/or functional parameter of said TKTL1 in a biological sample of said individual (patient) are taken as indication for the qualitative and quantitative run of the mam-aGF in the cells and/or tissue of said individual (patient). In combination with the use of inhibitors and activators of the mam-aGF the method is further suitable for checking and controlling the mam-aGF in an individual (patient).09-23-2010
20110003836Pro-Neurogenic Compounds - This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protection from neuron cell death.01-06-2011
20100240686CHEMICAL COMPOUNDS - Compounds of formula (I):09-23-2010
20110245284Alkoxy- and Alkylthio-Substituted Anilinopyrimidines - Alkoxy- and alkylthio-substituted anilinopyrimidines of the formula (I)10-06-2011
20110028503COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY - Compounds I and II as well as salts and pharmaceutical compositions containing them are useful for treating diseases and/or disorders of the eye.02-03-2011
20110034496POST-HARVEST TREATMENT - The present invention relates to methods for the protection of harvested fruit, cutflowers or vegetables against decay caused by certain storage diseases or disorders expressed in storage conditions. In particular the invention relates to the application of certain fungicidal active compounds to protect harvested fruit, cutflowers or vegetables against phytopathogenic fungi.02-10-2011
20110034495Method of Modulating Stress-Activated Protein Kinase System - A series of thieno[2,3-b]pyridin-6(7H)-one derivatives, substituted in the 2-position by a carbonyl- or sulfonyl-linked pyrrolidin-1-yl or related moiety, being inhibitors of p38 MAP kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.02-10-2011
20110034497INDAZOLE INHIBITORS OF THE WNT SIGNAL PATHWAY AND THERAPEUTIC USES THEREOF - Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states.02-10-2011
20110039873SUBSTITUTED PYRAZOLO[1,5-a] PYRIDINE COMPOUNDS HAVING MULTI-TARGET ACTIVITY - The substituted pyrazolo[1,5-a]pyridine compounds in accordance with Formula 1 are strong inhibitors of phosphodiesterase and c-Jun N-terminal kinase activity.02-17-2011
20110112126ENZYME INHIBITING COMPOUNDS - The present invention is directed to compounds that are specifically structured to provide enzyme inhibition. In specific embodiments, the enzyme inhibiting compounds exhibit antifolate activity. Particularly, the inventive compounds are formed of an antifolate residue that is active in inhibiting one or more of TS, DHFR, GAR, FPGS, and AICAR Tfase. The enzyme inhibiting compounds are useful in a variety of methods of treatment, including treating abnormal cell proliferation and treating inflammation.05-12-2011
20110130415PROTEIN KINASE C INHIBITORS AND USES THEREOF - This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.06-02-2011
20110212983PLATELET ADP RECEPTOR INHIBITORS - Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.09-01-2011
20110245283Methods for predicting the response to statins - The invention provides methods for optimizing therapeutic efficacy for treating hypercholesterolemia in a subject having a cardiovascular disease (CVD), comprising (a) determining subject characteristics that affect the likelihood of reaching a goal level of low density lipoprotein (LDL); and (b) obtaining success probabilities of a variety of statin treatments for reaching said goal level of LDL using said subject characteristics and a multivariate model; and (c) administrating the optimal statin treatment with the highest success probability of step (b) to said subject thereby optimizing therapeutic efficacy for treating hypercholesterolemia in said subject.10-06-2011
20110082164POLYCYCLIC COMPOUNDS AS LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS - Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.04-07-2011
20110130416PHARMACEUTICAL COMPOSITION FOR TREATING HYPERTENSION AND METABOLIC SYNDROME AND USE THEREOF - The present invention provides a pharmaceutical composition comprising the following active ingredients: 1) amlodipine or a pharmaceutically acceptable salt thereof, 2) pioglitazone or a pharmaceutically acceptable salt thereof, and 3) rosuvastatin or a pharmaceutically acceptable salt thereof. The present invention also provides use of the pharmaceutical composition in preparing a medicament for treating hypertension or metabolic syndrome. The pharmaceutical composition of the present invention can treat hypertension or metabolic syndrome, while effectively controlling the incidence of associated cardiovascular diseases and more potently improving survival prognosis in hypertensive patients. When blood pressure is lowered to desired level, the risk factors such as cardiovascular diseases are rectified, metabolic disorders and prognosis of patients are improved, and survival rate of hypertensive patients is raised.06-02-2011
20110245285PROCESS FOR PREPARATION OF ROSUVASTATIN ACETONIDE CALCIUM - The present invention is in relation to a process for preparation of HMG-CoA reductase inhibitor. More particularly, the present invention provides a process for preparation of (3R,5S,6E) 6-{2-[4-(4-Fluoro-phenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-vinyl}-2,2-dimethyl-[1,3]dioxan-4-yl)-acetic acid, calcium salt (Rosuvastatin acetonide calcium) which is used for treating hypercholesterolemia.10-06-2011
20100179178PYRIMIDINE DERIVATIVES AS POSH AND POSH-AP INHIBITORS - Pyrimidine deriviatives are ubiquination inhibitors that inhibit the ubiquitin ligase activity, particularly of POSH polypeptides, are useful for the treatment of viral infections and neurological disorders.07-15-2010
20090312353Methods and compositions for treating liquid tumors - The application relates to a method of using compositions having anti-alpha-4 integrin and/or anti-alpha-9 integrin activity to inhibit liquid tumor growth, malignancies thereof and/or development of metastases thereof that involve expression of an alpha-4 integrin and/or alpha-9 integrin. Pharmaceutical compositions and combination therapies (for example, with chemotherapies) for the inhibition of liquid tumor growth, malignancies thereof and/or development of metastases thereof are also provided.12-17-2009
201000694183-HETEROARYL (AMINO OR AMIDO)-1-(BIPHENYL OR PHENYLTHIAZOLYL) CARBONYLPIPERIDINE DERIVATIVES AS OREXIN RECEPTOR INHIBITORS - The invention relates to piperidine compounds of formula (I) wherein X-R03-18-2010
20100063081CPCR Agonists - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.03-11-2010
20100056552COMBINATION FOR USE IN THE TREATMENT OF INFLAMMATORY DISORDERS - There is provided combination products comprising (a) suplatast, or a pharmaceutically-acceptable salt or solvate thereof; and (b) a statin, or a pharmaceutically-acceptable salt or solvate thereof. Such combination products find particular utility in the treatment of atherosclerosis and related conditions.03-04-2010
20090215804FUMARATE OF 4- [[4- [[4- (2-CYANOETHENYL) -2,6-DIMETHYLPHENYL)AMINO] -2-PYRIMIDINYL]AMINO]BENZONITRILE - The present invention relates to the fumarate salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile, pharmaceutical compositions comprising as active ingredient said salt and to processes for their preparation.08-27-2009
20090215806Rosuvastatin calcium with a low salt content - Provided is rosuvastatin calcium with a low salt by product content and processes for preparing such rosuvastatin calcium.08-27-2009
200902158054-Heteroaryl Pyrimidine Derivatives and use thereof as Protein Kinase Inhibitors - The present invention relates to compounds of formula (I) or formula (II), or pharmaceutically acceptable salts thereof. Further aspects relate to pharmaceutical compositions comprising compounds according to the invention, and the use of said compounds in the preparation of a medicament for treating a variety of disorders, including proliferative disorders, viral disorders, stroke, etc.08-27-2009
20130158059NILOTINIB SALTS AND CRYSTALLINE FORMS THEREOF - Nilotinib salts and crystalline forms thereof have been prepared and characterized.06-20-2013
20110152303Chemical Compounds - Novel diarylpyrimidine derivatives and pharmaceutically acceptable salts, solvates or hydrates thereof, designed to inhibit HIV reverse transcriptase, are provided, and a pharmaceutical composition containing the same, especially an anti-HIV agent. More specifically, novel diarylpyrimidine derivatives that are derivatives of the HIV reverse transcriptase inhibitor TMC278 of formula (106-23-2011
20120035197Novel Use of Fibrates - The present invention, which is applicable in the pharmaceutical industry, relates to the use of fibrates, in particular fenofibrate, especially in the form of a solid oral composition, for the manufacture of a drug for the treatment of sleep apnea, sleep apnea syndrome, in particular obstructive sleep apnea or obstructive sleep apnea syndrome.02-09-2012
20110251222SULFONE-SUBSTITUTED ANILINOPYRIMIDINE DERIVATIVES AS CDK INHIBITORS, THE PRODUCTION THEREOF, AND USE AS A MEDICINE - The invention relates to sulphone-substituted anilinopyrimidine derivatives of the formula (I),10-13-2011
20110251221PYRIMIDINYLPIPERIDINYLOXYPYRIDINONE ANALOGUES AS GPR119 MODULATORS - Novel compounds of structure Formula I:10-13-2011
20110098314STATINS FOR THE TREATMENT OF OCULAR HYPERTENSION AND GLAUCOMA - The use of HMG-CoA reductase inhibitors (e.g., statins) to treat glaucoma, control intraocular pressure, preserve the trabecular meshwork, protect against ocular neurodegeneration and/or protect against glaucomatous retinopathy is described. The preferred HMG-CoA reductase inhibitors, which are statins having an RI value of 0.2 to 0.7 (e.g., pravastatin), are administered via topical application to the affected eye(s) of the patient.04-28-2011
20110082165PYRROLIDINE GPR40 MODULATORS - The present invention provides compounds of Formula (I):04-07-2011
20110152302Novel dicyclanil-based shelf stable aqueous suspension and non-aqueous solution pour-on and spray-on formulations useful for the prevention and treatment of insect infestation in animals - This invention relates to topically active compositions, including pour-on and spray-on formulations, comprising insect growth regulator (IGR) insecticides prepared as aqueous suspension formulations, or as non-aqueous solution formulations, and to the methods of making these formulations, and to methods of using these formulations for the treatment and/or prevention of insect infestation in animals.06-23-2011
20110071177FUNGICIDAL ACTIVE SUBSTANCE COMBINATION - Methods of controlling fungi with an active compound combination that includes trifloxystrobin and pyrimethanil.03-24-2011
20090253722AQUEOUS PHARMACEUTICAL FORMULATION - The invention concerns a stable aqueous pharmaceutical composition comprising 5-[(2RS)-2-cyclopropyl-7,8-dimethoxy-2H-1-benzopyran-5-ylmethyl]-pyrimidine-2,4-diamine in form of the water soluble methanesulfonic acid salt, a physiological sodium chloride solution, ethanol and Povidone 12 PF, the liquid having a pH of over and above 4.8, but not higher than 5.2, and wherein the oxygen amount is controlled to be 0.8 ppm or less; which can be sterilized by filtration and/or by heated treatment, stored for longer time periods and which can be use for bolus injection or diluted for i.v. infusion.10-08-2009
20100311776Novel sEH Inhibitors and their Use - The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I:12-09-2010
20100261743NOVEL SEH INHIBITORS AND THEIR USE - The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I:10-14-2010
20120202834GLUCAGON RECEPTOR MODULATORS - The present invention provides a compound of Formula (I)08-09-2012
20120202835COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.08-09-2012
20100004274Stable pharmaceutical compositions comprising a pyrimidine-sulfamide - Stable pharmaceutical compositions include the compound of the below formula, or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof:01-07-2010
20120202836METHOD OF TREATING PROLIFERATIVE DISORDERS AND OTHER PATHOLOGICAL CONDITIONS MEDIATED BY BCR-ABL, C-KIT, DDR1, DDR2 OR PDGF-R KINASE ACTIVITY - The present invention relates to a regimen for the administration of a pyrimidylaminobenzamide of formula I as defined herein for the treatment of proliferative disorders, particularly solid and liquid tumors, and other pathological conditions mediated by the Bcr-AbI oncoprotein, the cell transmembrane tyrosine kinase receptor c-Kit, DDR1 (discoidin domain receptor 1), DDR2 (discoidin domain receptor 2) or PDGF-R (platelet derived growth factor receptor) kinase activity.08-09-2012
20110257211Small-Molecule Choline Kinase Inhibitors as Anti-Cancer Therapeutics - Small molecule choline kinase inhibitors having the following formula:10-20-2011
20090005407PARTICULATE (3'-CHLOROBIPHENYL-4-YL)(1-(PYRIMIDIN-2-YL)PIPERIDIN-4-YL)METHANONE AND METHODS OF ITS USE - Particulate (3′-chlorobiphenyl-4-yl)(1-(pyrimidin-2-yl)piperidin-4-yl)methanone is disclosed. Also disclosed are pharmaceutical formulations and dosage forms comprising particulate (3′-chlorobiphenyl-4-yl)(1-(pyrimidin-2-yl)piperidin-4-yl) and methods of their use.01-01-2009
20080312263PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF ATHEROSCLEROSIS - The present invention relates to the use, 12-18-2008
20080255171Combination of Nilotinib with Farnesyl Transferase Inhibitors - The invention provides a pharmaceutical combination comprising: 10-16-2008
20080255169Sulphonamide Derivatives - The invention relates to sulphonamide derivatives of formula (I),10-16-2008
20080255172PYRIMIDINE DERIVATIVES - A compound of the following formula:10-16-2008
20110053968AMINOPYRIMIDINE INHIBITORS OF TYROSINE KINASE - The present invention relates to new aminopyrimidine inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof03-03-2011
20110071176PHARMACEUTICAL COMPOSITION COMPRISING OMEGA-3 FATTY ACID AND HYDROXY-DERIVATIVE OF A STATIN AND METHODS OF USING SAME - In various embodiments, the present invention provides compositions and methods for treating and/or preventing a cardiovascular-related disease in subject in need thereof.03-24-2011
20120302589PHARMACEUTICAL COMPOSITIONS COMPRISING EPA AND A CARDIOVASCULAR AGENT AND METHODS OF USING THE SAME - The present invention relates to, inter alia, pharmaceutical compositions comprising EPA and one or more cardiovascular agents, and to therapeutic methods for treating various diseases and disorders using the same.11-29-2012
20120302588METHOD OF ENHANCING HAIR GROWTH - Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include bimatoprost and minoxidil in a vehicle for topical application to the skin of a mammal, e.g. a human, whereby the combination of bimatoprost and minoxidil produces a faster onset of hair growth in humans or other mammals and wherein said composition brings about a synergestic result of faster onset of hair growth as compared to compositions comprising bimatoprost and minoxidil, alone.11-29-2012
20100298365TOPICAL ADMINISTRATION CARRIER COMPOSITION AND THERAPEUTIC FORMULATIONS COMPRISING SAME - A topical administration carrier composition including water, glycerin and polysorbate, suitable for use in formulations with active ingredient compositions containing active ingredients such as minoxidil that are susceptible to systemic penetration, and solvents that are susceptible to evaporative loss, when the active ingredient composition is topically applied to the body. The carrier formulation retards the evaporative losses of the solvent component(s) and systemic migration losses of the active ingredient composition, to provide sustained topical action, in relation to formulations lacking the carrier composition of the invention.11-25-2010
20110136842Substituted Dihydroisoquinolinone and Isoquinolinedione Derivatives as Calcium Channel Blockers - A series of disubstituted dihydroisoquinolinone and isoquinolinedione derivatives represented by Formula I, or pharmaceutically acceptable salts thereof are presented. 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.06-09-2011
20110136840ANTI-INFECTIVE AGENTS - The present invention relates to the use of molecules having a spacer unit, linker and recognition unit(s) for the treatment and prevention of various diseases, disorders and conditions. In particular, the present invention provides compounds useful in preventing or treating infectious diseases and diseases, disorders or conditions related thereto. Further, the present invention relates to methods for preventing or treating diseases, disorders or conditions involving recognition and binding of carbohydrate structures.06-09-2011
20100222373Crystalline Form of Bis [(E)-7-[4-(4-fluoro-phenyl)-6-isopropyl-2-[methyl(methyl-sulfonyl)amino] pyrimidin-5-yl] (3R,5S)-3,5-dihydroxyhept-6-enoic acid] Calcium Salt - Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described.09-02-2010
20100324076Novel sEH Inhibitors and their Use - The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I:12-23-2010
20100324075THERAPEUTIC USE OF CARBOXYL ESTER LIPASE INHIBITORS - Compounds, pharmaceutical compositions, and their methods of use in raising serum HDL levels in subjects in need thereof are provided. Also provided are compounds, pharmaceutical compositions, and their methods of use in increasing reverse cholesterol transport in subjects in need thereof. Finally, methods for treating disease by raising serum HDL levels and increasing reverse cholesterol transport are provided.12-23-2010
20100179179INHIBITORS OF THE MUTANT FORM OF KIT - The present invention relates to the treatment of KIT dependent diseases that are characterized by a mutant form of KIT whereby the mutant KIT is identified and an appropriate inhibitor of the mutant KIT is administered.07-15-2010
20110178111LONG-TERM TREATMENT OF SYMPTOMATIC HEART FAILURE - The main object here is the use of omega-3 polyunsaturated fatty acids (as ethyl esters, hereinafter called “n-3 PUFA”) as a medicament, either alone or in combination with other therapeutic agents, for reducing mortality for a cardiovascular cause, in particular arrhythmia or for reducing hospitalization for any cause, in particular a cardiovascular cause and for the daily administration to patients with symptomatic heart failure (HF) for more than 3.5 years.07-21-2011
20090176813AQUEOUS SUSPENSIONS OF TMC278 - This invention concerns pharmaceutical compositions for administration via intramuscular or subcutaneous injection, comprising micro- or nanoparticles of the NNRTI compound TMC278, suspended in an aqueous pharmaceutically acceptable carrier, and the use of such pharmaceutical compositions in the treatment and prophylaxis of HIV infection.07-09-2009
20090209567Rosuvastatin and salts thereof free of rosuvastatin alkylether and a process for the preparation thereof - The present invention provides rosuvastatin and intermediates thereof having a low level of alkylether impurity and processes for the preparation thereof.08-20-2009
20100190811PYRIMIDINE DERIVATIVES AND COMPOSITIONS AS C-KIT AND PDGFR KINASE INHIBITORS - The invention provides a novel class of pyrimidine derivatives, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFRα and PDGFRβ kinases.07-29-2010
20110190327METHOD FOR MODULATING GPR119 G PROTEIN-COUPLED RECEPTOR AND SELECTED COMPOUNDS - A method of modulating the activity of the GPR119 G protein-coupled receptor comprising administering to a mammalian patient in need thereof a therapeutically effective amount of at least one compound of Formula I or Formula IA and, optionally, an additional therapeutic agent.08-04-2011
20110136841SUBSTITUTED INDOLYL ALKYL AMINO DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I)06-09-2011
20100022569INHIBITORS OF TYROSINE KINASES - The present invention relates to the use of pyrimidylaminobenzamide compounds for the preparation of a drug for the treatment of diseases that respond to modulation of Ephrin receptor kinase, especially EphB4, activity, especially for the curative and/or prophylactic treatment of proliferative diseases, and to a method of treating diseases that respond to modulation of kinase activity, especially Ephrin receptor kinase activity.01-28-2010
20100016345PYRIMIDINYL SULFONAMIDE COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 - Disclosed are compounds, which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, Crohn's disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.01-21-2010
20100016344AMINO HETEROCYCLIC LINKED PYRIMIDINE DERIVATIVES - Macrocyclic benzofused pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions and disorders using such compounds and compositions are described herein.01-21-2010
20090221620GENTIC POLYMORPHISMS ASSOCIATED WITH STROKE, METHODS OF DETECTION AND USES THEREOF - The present invention provides compositions and methods based on genetic polymorphisms that are associated with vascular diseases such as stroke. In particular, the present invention relates to genetic polymorphisms that have utility for such uses as predicting disease risk or predicting an individual's response to a treatment such as statins, including groups of polymorphisms that may be used as a signature marker set for such uses, as well as nucleic acid molecules containing the polymorphisms, variant proteins encoded by such nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and proteins, and methods of using the nucleic acid and proteins as well as methods of using reagents for their detection.09-03-2009
20080207657Use Of Minoxidil Sulfate As An Anti-Tumor Drug - The invention relates to compositions, methods and kits for the treatment of cancer. ATP-dependent potassium channel agonists, salts thereof, or chemical analogs thereof, for example, minoxidil sulfate, have been found to possess anti-neoplastic properties. Administering minoxidil sulfate may prolong the life of a cancer patient; for example, a patient with a brain tumor.08-28-2008
20100160360JNK MODULATORS - Compounds of formula I modulate JNK:06-24-2010
20090099220ANTIMALARIAL COMPOUNDS WITH FLEXIBLE SIDE-CHAINS - The present invention relates to novel compounds that are inhibitors of wild type and mutant dihydrofolate reductase (DHFR) of 04-16-2009
20090137617USE OF HAPTOGLOBIN GENOTYPING IN DIAGNOSIS AND TREATMENT OF CARDIOVASCULAR DISEASE - This invention is directed to methods and compositions for the treatment of cardiovascular disorders. Specifically, the invention is directed to compositions comprising vitamin E, statins and/or glutathione peroxidase mimetics; methods of treating diabetic patients expressing the Hp-2-2 haptoglobin genotype; a method of inhibiting or suppressing a cardiovascular disorder in a diabetic subject, treating cardiovascular disease in subjects exhibiting the Haptoglobin Hp-2-2 genotype; and methods of treating cardiovascular disease in subjects exhibiting the Haptoglobin Hp-2-2 genotype.05-28-2009
20100234407PREVENTIVES/REMEDIES FOR MYELOMA TUMOR AND METHOD FOR DIAGNOSING THE SAME - The present invention provides a preventive or therapeutic drug for a myeloma tumor and osteoclastic bone loss associating therewith, the drug containing as an active ingredient an osteopontin-production regulator or inhibitor; a screening method for a preventive or therapeutic drug for a myeloma tumor, characterized by determining osteopontin production regulatory or inhibitory effect; as well as a diagnostic kit for a myeloma tumor, characterized by including a reagent for measuring blood osteopontin level, and a diagnostic method.09-16-2010
20100216827ARYL GPR120 RECEPTOR AGONISTS AND USES THEREOF - Aryl GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.08-26-2010
20120041010PHARMACEUTICAL COMBINATION OF (E)-7-[4-(4-FLUOROPHENYL)-6-ISOPROPYL-2-[METHYL(METHYLSULFONYL)AMINO]PYRI- MIDIN-5-YL] (3R,5S)-3,5-DIHYDROXYHEPT-6-ENOIC ACID AND CANDESARTAN - The present invention relates to a new use of a statin drug in the improvement of diabetic neuropathy, specifically in improving nerve conduction velocity and nerve blood flow in patients suffering diabetes, in particular to pharmaceutical combinations of the statin drug and other agents known to improve diabetic neuropathy such as an aldose reductase inhibitor (ARI), an angiotensin converting enzyme (ACE) inhibitor or an angiotensin II (AII) antagonist which combinations are useful in the prevention and treatment of the complications of diabetes02-16-2012
20110306625COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.12-15-2011
20090069359Topical and transdermal treatments using urea formulation - Various medical conditions, some previously treated by injection or surgery, are effectively treated by a topical application of a composition of urea and a chemotherapeutic agent. Such agents include sclerosing agents, vasodilators, botulinum toxin and minoxidil. Conditions as diverse as spider veins, erectile dysfunction, facial wrinkles, hair loss and baldness can be effectively treated with the compositions.03-12-2009
20090099221PYRIDYL-AND PYRIMIDINYL-SUBSTITUTED PYRROLE-, THIOPHENE-AND FURANE-DERIVATIVES AS KINASE INHIBITORS - The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R04-16-2009
20090042918Pyridopyrimidinone Inhibitors of PIM-1 and/or PIM-3 - Compounds of formula (I), useful for inhibiting PIM-I and/or PIM-3: and pharmaceutically acceptable salts thereof, wherein Y, Z, R02-12-2009
20090093505Imazalil compositions comprising alkoxylated amines - The present invention relates to the use of alkoxylated amines to enhance the activity of fungicidal formulations comprising the fungicidal compound imazalil. It also relates to formulations comprising imazalil and alkoxylated amines. These formulations are useful to protect materials, plants, fruits or seeds against fungi.04-09-2009
20120041012SUBSTITUTED SPIROCYCLIC AMINES USEFUL AS ANTIDIABETIC COMPOUNDS - Substituted spirocyclic amines of structural formula I are selective antagonists of the somatostatin sub-type receptor 5 (SSTR5) and are 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.02-16-2012
20120041011SUBSTITUTED BENZOFUSED DERIVATIVES AND THEIR USE AS VANILLOID RECEPTOR LIGANDS - The present invention relates to substituted benzofused derivatives, which can he used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.02-16-2012
20100184790PYRROLO[2,3-B]PYRIDINE COMPOUNDS, AZAINDOLE COMPOUNDS USED FOR SYNTHESIZING SAID PYRROLO[2,3-B]PYRIDINE COMPOUNDS, METHODS FOR THE PRODUCTION THEREOF, AND USES THEREOF - The invention relates to pyrrolo[2,3-b]pyridine compounds and azaindole compounds used for the synthesis thereof. The invention also relates to methods for the production thereof and the uses thereof. Said novel pyrrolo[2,3-b]pyridine compounds according to the invention have great antiproliferative, apoptotic, and neuroprotective activities. The invention particularly applies to the pharmaceutical field.07-22-2010
20080262010CRYSTALLINE POLYMORPHS OF N-(3-(DIMETHYLAMINO)PROPYL)-4-(4-(3-FLUORO-4-METHOXYPHENYL) PYRIMIDIN-2-YLAMINO) BENZENESULFONAMIDE AS D-GLUCORONATE SALTS - The present invention relates to methods for preparing one or more crystalline polymorphs of a compound of formula I:10-23-2008
20080280932COMPOSITIONS AND METHODS FOR TREATING VASCULAR, AUTOIMMUNE, AND INFLAMMATORY DISEASES - The disclosure provides methods and compositions for the treatment of vascular, autoimmune and inflammatory diseases using a combination of an inosine monophosphate dehydrogenase (IMPDH) inhibitor and a HMG CoA reductase inhibitor.11-13-2008
20090082379Novel Cyclic Urea Derivatives, Preparation Thereof and Pharmaceutical Use Thereof as Kinase Inhibitors - Compounds of formula (I):03-26-2009
20100081679DIAMINOPYRIMIDINES AS FUNGICIDES - Use of diaminopyrimidines of the formula (I)04-01-2010
20120004253Novel Fused Pyrrolocarbazoles - The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.01-05-2012
20110166169NOVEL HSP90 INHIBITORY CARBAZOLE DERIVATIVES, COMPOSITIONS CONTAINING SAME AND USE THEREOF - The invention relates to the novel substances in Formula (I): wherein Het is a heterocycle optionally substituted by one or a plurality of radicals R1 or R′1; R is selected from the group comprising Formula (A′), (B), (C), (D), or (E), with R1 and/or R′1 selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxyl, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalcoxy, alkylhio, or carboxy that is free or esterified by an alkyl, carboxamide, CO—NH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—S02-alkyl, S(0)2-NHalkyl, or S(02)-N(alkyl)2 radical; all these radicals are optionally substituted; W1, W2, and W3 independently are CH or N; X is 0, S, NR2, C(O), S(O), or S(0)2; Z is optionally substituted H, Hal, -0-R2 or —NH—R2 with R2 being H, alkyl, cycloalkyl, or heterocycloalkyl; and these substances are all isomeric forms and salts thereof, used as drugs.07-07-2011
20120015969NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION - The present invention relates to a compound of Formula (I): wherein: R01-19-2012
20120015968USE OF PYRIMIDYLAMINOBENZAMIDE DERIVATIVES FOR THE TREATMENT OF DISORDERS MEDIATED BY THE LEUCINE ZIPPER-AND STERILE ALPHA MOTIF-CONTAINING KINASE (ZAK) - The invention relates to the use of a pyrimidylaminobenzamide derivative of formula I01-19-2012
20120022090NOVEL SUBSTITUTED BENZOXAZOLE, BENZIMIDAZOLE, OXAZOLOPYRIDINE AND IMIDAZOPYRIDINE DERIVATIVES AS GAMMA SECRETASE MODULATORS - The present invention is concerned with novel substituted benzoxazole, benzimidazole, oxazolopyridine and imidazopyridine derivatives of Formula (I)01-26-2012
20120022092PROTEIN KINASE C INHIBITORS AND USES THEREOF - This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.01-26-2012
20120022091KEY INTERMEDIATES FOR THE SYNTHESIS OF ROSUVASTATIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF - The present invention relates in general to the field of organic chemistry and in particular to the preparation of N-(4-(4-fluorophenyl)-6-isopropyl-5-methylpyrimidin-2-yl)-N-methylmethanesulfonamide (I), N-(4-(4-fluorophenyl)-5-(bromomethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (II) and N-(4-(4-fluorophenyl)-5-(hydroxymethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (III), key intermediates in preparation of Rosuvastatin.01-26-2012
20110077261PREVENTION OF HIV-INFECTION - This invention relates to the use of a parenteral formulation comprising the NNRTI TMC278 for the long term prevention of HIV infection in a subject at risk of being infected by HIV, which comprises the intermittent administration of the said formulation at long time intervals.03-31-2011
20120059022Crystalline Form of Bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]- pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoicacid] Calcium Salt - Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described.03-08-2012
201100925274 (Pyrrolopyridinyl)pyrimidin-2-ylamine derivatives - Compounds of the formula (I), in which R04-21-2011
20110092528PIPERIDINYL COMPOUNDS THAT SELECTIVELY BIND INTEGRINS - The invention is directed to piperidinyl compounds that selectively bind integrin receptors and methods for treating an integrin mediated disorder.04-21-2011
20110105543NOVEL TRIARYL DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS - This invention relates to novel triaryl derivatives, formula (I), a stereoisomer thereof or a mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein all of X, Y and Z represent CH; or one or two of X, Y and Z represent N; and the others of X, Y and Z represent CH; and R05-05-2011
20090131463NOVEL COMPOUNDS - The invention provides compounds of formula05-21-2009
20100249164MODULATION OF SLEEP WITH NR2B RECEPTOR ANTAGONISTS - An NR2B receptor antagonist is useful, alone or in combination with other agents, for promoting wakefulness, treating narcolepsy, excessive daytime sleepiness, enhancing cognition, treating sleepiness associated with Alzheimer's disease, Parkinson's disease, fibromyalgia, chronic pain, sleep disorders, autism and attention deficit hyperactivity disorder.09-30-2010
20120232105PHARMACEUTICAL COMPOSITION FOR INHIBITING OSTEOCLAST GROWTH - A pharmaceutical composition for inhibiting osteoclast growth is disclosed in the present invention. The pharmaceutical composition includes a compound represented by a formula (I), and a pharmaceutically acceptable salt and carrier:09-13-2012
20120136018QUINOLINES - The present invention relates to 2-aminoquinolines of formula I05-31-2012
20100173924NOVEL HETEROCYCLE COMPOUNDS AND USES THEREOF - The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula (I): which penetrate the blood-brain barrier, inhibit the formation and accumulation of beta-amyloid, and are useful in the treatment of neurodegenerative diseases, particularly Alzheimer's disease. Further, the compounds of the present invention inhibit certain kinases, thereby being useful for the treatment of cancers of the central nervous system.07-08-2010
20120172386Combinations Comprising a VEGF Receptor Inhibitor - A composition comprising a VEGF receptor inhibitor and a penetration enhancer and uses thereof.07-05-2012
20120172385ORTHO SUBSTITUTED PYRIMIDINE COMPOUNDS AS JAK INHIBITORS - The invention relates to compounds of formula (I)07-05-2012
20120172384HETEROCYCLYLAMINOPYRIMIDINES AS KINASE INHIBITORS - The invention relates to compounds of formula (I)07-05-2012
20090069358Use of IKappaB-Kinase Inhibitors in Pain Therapy - The present invention relates to the use of IκB-kinase Inhibitors and methods for the prophylaxis and therapy for treating pain comprising administering such compounds.03-12-2009
20100048595USE OF ARCHAEA TO MODULATE THE NUTRIENT HARVESTING FUNCTIONS OF THE GASTROINTESTINAL MICROBIOTA - The invention generally relates to the use of archaea to modulate nutrient harvesting in a subject. In particular, the invention provides methods that use archaea to modulate the nutrient harvesting functions of the microbiota in the subject's gastrointestinal tract.02-25-2010
20100048598TOPICAL COMPOSITIONS COMPRISING 5-ALPHA REDUCTASE INHIBITORS - The present invention relates to topical compositions comprising 5α-reductase inhibitors. The present invention also includes processes for preparation of such topical compositions and methods of using them.02-25-2010
20100048597Organic Compounds and Their Uses - The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases.02-25-2010
20100048596Indole Derivatives as Antitumoral Compounds - Antitumoural compounds of general formula (I); wherein Ar is an heterocyclic group of formula (a) and R02-25-2010
20120178770SUBSTITUTED PYRIMIDINYLPYRROLOPYRIDINONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS - Pyrimidinylpyrrolopyridinone 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.07-12-2012
201001739234 (PYRROLOPYRIDINYL)PYRIMIDINYL-2-AMINE DERIVATIVES - Compounds of the formula I in which R07-08-2010
20100010026STATIN AND OMEGA-3 FATTY ACIDS FOR REDUCTION OF APO-B LEVELS - Methods of utilizing a combined administration or a unit dosage of a combination of an HMG-CoA inhibitor and omega-3 fatty acids for the reduction of apolipoprotein-B levels. The methods are especially useful in the treatment of patients with hypertriglyceridemia or hypercholesterolemia or mixed dyslipidemia, coronary heart disease (CHD), vascular disease, atherosclerotic disease and related conditions, and for the prevention or reduction of cardiovascular, cardiac, and vascular events.01-14-2010
20100010025Pyrimidine Derivatives - Disclosed are pyrimidine derivatives having interesting pharmacological properties.01-14-2010
201002922624 (PYRROLO[2,3-C]PYRIDINE-3-YL)PYRIMIDIN-2-AMINE DERIVATIVES - Compounds of the formula (I), in which R11-18-2010
20120220615SUBSTITUTED INDOLYL ALKYL AMINO DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I)08-30-2012
20120083504Reverse Amide Compounds As Protein Deacetylase Inhibitors And Methods Of Use Thereof - The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.04-05-2012
20120225899Compounds and Compositions as Protein Kinase Inhibitors - The present invention provides compounds of Formula I or II:09-06-2012
20120225898HAIR GROWTH AND/OR REGROWTH COMPOSITIONS - The present disclosure relates to compositions containing certain pyrimidine compounds such as minoxidil and/or certain pyrimidine sulfate (inner salt) compounds such as minoxidil sulfate and especially compositions containing pyrimidine compounds in combination with an admixtures comprising at least one antioxidant, at least one organic acid and a select fatty acid mixture. The present disclosure also relates to use of the compositions to grow and/or regrow hair and/or prevent hair loss in mammals and particularly in humans.09-06-2012
20120225897HAIR GROWTH AND/OR REGROWTH COMPOSITIONS - The present disclosure relates to compositions containing certain pyrimidine compounds such as minoxidil and/or certain pyrimidine sulfate (inner salt) compounds such as minoxidil sulfate and especially compositions containing pyrimidine compounds in combination with an admixtures comprising at least one antioxidant, at least one organic acid and a select fatty acid mixture. The present disclosure also relates to use of the compositions to grow and/or regrow hair and/or prevent hair loss in mammals and particularly in humans.09-06-2012
20120190700NOVEL 4-AMINO-N-HYDROXY-BENZAMIDES FOR THE TREATMENT OF CANCER - The present invention provides compounds of formula07-26-2012
20090018152Aminophenyl Derivatives as Novel Inhibitors of Histone Deacetylase - This invention comprises the novel compounds of formula (I)01-15-2009
20090018153Substituted Indolyl-Alkyl-Amino-Derivatives as Inhibitors of Histone Deacetylase - This invention comprises the novel compounds of formula (I) wherein R01-15-2009
20090018151Topical Treatment of Peripheral diabetic complications - This invention relates to agents for treating, ameliorating, or preventing diabetic complications specifically diabetic neuropathy and skin ulceration by topical application of materials containing one or more arterial or venous dilation components and one or more fast sodium channel inhibitors. Particularly, the invention relates to treating or ameliorating agents that contain minoxidil and its related congeners, which have both potassium channel agonist properties and nitric oxide agonist properties as an active ingredient and which are effective against diabetic complications such as neuropathy, peripheral circulation disorders and skin ulcerations. Unique methods of delivery including delivery through impregnated socks or gloves to match the distribution of pain are also noted.01-15-2009
200900181505-Ht2b Receptor Antagonists - Compounds of formulae: (I), (II), (IIIa), (IIIb), (IVa) and (IVb): or a pharmaceutically acceptable salt thereof, for use as pharmaceuticals, in particular for the treatment of a condition alleviated by antagonism of a 5-HT01-15-2009
20110124669Modulators of Cellular Adhesion - The present invention provides compounds having formula (I):05-26-2011
20120264773ORGANIC COMPOUNDS - The present invention provides a compound of formula (I):10-18-2012
20120232106TREATMENT FOR DISCOID LUPUS - Compounds I and II as well as salts and pharmaceutical compositions containing them are useful for treating diseases and/or disorders of the skin, such as cutaneous lupus, for example acute cutaneous lupus erythematosus, subacute cutaneous lupus erythematosus, or discoid lupus erythematosus. In certain embodiments, the compounds are provided in topical compositions.09-13-2012
20120232107NON-PEPTIDE ANTAGONISTS OF GASTRIN RELEASING PEPTIDE - This invention relates, e.g., to methods for inhibiting or stimulating an activity of an adrenomedullin (AM) or gastrin releasing peptide (GRP) peptide hormone, comprising contacting the peptide with a small molecule, non-peptide, modulatory agent of the invention. Complexes of these modulatory agents with other components, such as the peptides or blocking antibodies specific for the peptides, are also described, as are pharmaceutical compositions comprising the modulatory agents, and methods for using the modulatory agents to diagnose or treat patients.09-13-2012
20080306099COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY - The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.12-11-2008
20100324077COMBINATIONS OF ANILINOPYRIMIDINES AND PYRION COMPOUNDS - The present invention relates to combinations of an anilinopyrimidine, or a salt thereof, and a pyrion compound, or a salt thereof, which provide an improved biocidal effect. More particularly, the present invention relates to compositions comprising a combination of an anilinopyrimidine, or a salt thereof, selected from the group consisting of pyrimethanil, cyprodinil or mepanipyrim, together with a pyrion compound selected from 1-hydroxy-2-pyridinone, ciclopirox, ciclopirox olamine, piroctone, piroctone olamine, rilopirox, pyrion disulfide, sodium pyrithione and zinc pyrithione in respective proportions to provide a synergistic biocidal effect. Compositions comprising these combinations are useful for the protection of any living or non-living material, such as crops, plants, fruits, seeds, objects made of wood, thatch or the like, engineering material, biodegradable material and textiles against deterioration due to the action of microorganisms such as bacteria, fungi, yeasts, algae, virusses, and the like.12-23-2010
200803002661-(Hetero)Aryl-3-Amino-Pyrrolidine Derivatives for Use as Mglur3 Antagonists - The present invention relates to compounds of the Formula (I) which are useful for treating conditions associated with mGluR3 receptors, such as depression, schizophrenia and migraine, pharmaceutical compositions thereof, and methods of using the same.12-04-2008
20080300267Compounds and Compositions as Protein Kinase Inhibitors - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the CDKs, Aurora, Jak2, Rock, CAMKII, FLT3, Tie2, TrkB, FGFR3 and KDR kinases.12-04-2008
20080300268HETEROCYCLIC COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.12-04-2008
20110003837MODIFIED RELEASE FORMULATIONS OF HMG COA REDUCTASE INHIBITORS - Modified release formulations of HMG Co-A reductase inhibitors, which provide reduced incidence of rhabdomyolysis, renal toxicity and other side effects by increasing hepatic bioavailability and decreasing systemic availability upon oral administration. The modified release pharmaceutical formulation comprises a therapeutically effective amount of HMG CoA reductase inhibitor or a pharmaceutically acceptable salt(s), polymorph(s), solvate(s), hydrate(s), prodrug or metabolite thereof, one or more release modifying agent(s) and one or more pharmaceutically acceptable excipient(s), wherein the modified release formulation provides reduced incidence of adverse effects and improved efficacy when compared to the immediate release formulation upon oral administration.01-06-2011
20110046170NOVEL PYRIMIDINE-PYRIDINE DERIVATIVES - The invention relates to novel pyrimidine-pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.02-24-2011
20120270891Salts of 4-Methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-- 3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide - Salts of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide are prepared by various processes.10-25-2012
20120270892Aminopyrimidine Kinase Inhibitors - Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1γ), casein kinase 2 (CK2), Pim-1, Pim-2, Pim-3, the TGFβ pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1γ), casein kinase 2 (CK2), Pim-1, Pim-2, Pim-3, the TGFβ pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.10-25-2012
20100234408PYRIMIDYLAMINOBENZAMIDE DERIVATIVES FOR THE TREATMENT OF NEUROFIBROMATOSIS - The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF, and to a method of treating non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF.09-16-2010
20100234406COMPOUNDS AND COMPOSITIONS AS C-KIT AND PDGFR KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFR and PDGFR kinases.09-16-2010
20120277258Chemical Compounds - Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.11-01-2012
20120277259SUBSTITUTED BENZOFUSED DERIVATIVES AND THEIR USE AS VANILLOID RECEPTOR LIGANDS - The present invention relates to substituted benzofused derivatives, which can be used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.11-01-2012
20100204255BICYCLIC DERIVATIVES AS MODULATORS OF ION CHANNELS - The present invention relates to bicyclic compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.08-12-2010
20110294841NOVEL STATIN PHARMACEUTICAL COMPOSITIONS AND RELATED METHODS OF TREATMENT - The invention provides novel omega-3 oil formulations of one or more statins. These formulations are readily bioavailable. Notably, because the formulations of the invention contain an omega-3 oils as the major ingredient, they not only provide an antihypercholesterolemic effect due to the statin active ingredient, they also provide recommended daily dosages of omega-3 oils (i.e., approximately 1 gram of omega-3 oil per day), or a portion thereof. The invention also provides novel salts of one or more statins.12-01-2011
20100204254Use of statins in the prevention and treatment of radiation injury and other disorders associated with reduced endothelial thrombomodulin - The present invention discloses statins (3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors) consistently and significantly increased endothelial cell thrombomodulin protein and functional activity. Statins also abrogated the downregulation of thrombomodulin that occurs in response to radiation injury. These results indicate that preserving or restoring endothelial thrombomodulin expression and function by statins may be useful in a variety of disorders associated with widespread endothelial dysfunction such as sepsis, adult respiratory distress syndrome, and normal tissue radiation injury.08-12-2010
20100168144INHIBITORS OF PROTEIN KINASES - The present invention relates to inhibitors of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to methods of preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases comprising the administration of an effective amount of at least one inhibitor of cyclin-dependent kinases. formula (I).07-01-2010
20130012532CYCLOPROPANECARBOXYLIC ACID DERIVATIVE - A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R01-10-2013
20130012531TREATMENT METHOD - The present invention is directed to methods of treating disorders of ocular angiogenesis or vascular leakage in a patient by administration of suitable inhibitors, including pazopanib or pharmaceutically acceptable salts or hydrates thereof.01-10-2013
20100130523MONO-HYDROCHLORIC SALTS OF AN INHIBITOR OF HISTONE DEACETYLASE - This invention provides novel crystalline forms of mono-HCl salts and a mono-HCl salt hydrate of JNJ-26481585, an inhibitor of histone deacetylases. The invention also relates to processes for production of these forms, to intermediates used in these processes, to pharmaceutical compositions comprising these forms, and to the use of these forms in medical treatment for instance as a medicine to inhibit proliferative conditions, such as cancer and leukemia.05-27-2010
20100130522COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES - The invention relates to certain compounds according to Formula (I):05-27-2010
20130018065PROCESSES FOR THE PREPARATION OF KEY INTERMEDIATE FOR THE SYNTHESIS OF ROSUVASTATIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOFAANM Andrensek; SamoAACI LjubljanaAACO SIAAGP Andrensek; Samo Ljubljana SIAANM Anzel; JolandaAACI LjubljanaAACO SIAAGP Anzel; Jolanda Ljubljana SIAANM Hocevar; MarjetaAACI LjubljanaAACO SIAAGP Hocevar; Marjeta Ljubljana SIAANM Casar; ZdenkoAACI LjubljanaAACO SIAAGP Casar; Zdenko Ljubljana SI - The present invention relates in general to the field of organic chemistry and in particular to a process for the preparation of 5-((E)-2-((2S,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-methanesulfonylamino)pyrimidine (RSVL) as well as a process for preparing crystalline 5-((E)-2-((2S,4R)-4-(tert-butyldimethylsilyloxy)-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVLTBS) useful as key intermediates for the preparation of rosuvastatin or pharmaceutically acceptable salts thereof.01-17-2013
20130018066HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS - Disclosed are compounds of the formula I01-17-2013
20110160237Substituted Heterocyclic Compounds - The present invention relates to substituted heterocyclic compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted heterocyclic 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
20110160236Treating Vascular Events with Statins by Inhibiting PAR-1 and PAR-4 - The present invention relates to new methods for treating and/or preventing vascular events by inhibiting G-coupled Protease Activating Receptor (PAR)-1 and/or PAR-4 with the administration of statins. In one embodiment, individuals who are at risk for vascular events, but have cholesterol levels (e.g., total cholesterol or Low Density Lipoprotein) in normal ranges, are treated with statins.06-30-2011
20130023548Crystalline Forms of 4-Methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyr- idin-3-yl-pyrimidin-2-ylamino)-benzamide - Crystalline forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base and salts thereof are prepared by various processes.01-24-2013
20130023550PHARMACEUTICAL COMPOSITIONS AND METHODS OF MAKING SAME - Pharmaceutical compositions that include about 10 mg pazopanib/mL of the composition and about 2 to about 13% w/w of a modified cyclodextrin as well as methods of making the same are described.01-24-2013
20130023549Pharmaceutical Compositions Comprising Nilotinib or Its Salt - A pharmaceutical composition, especially capsules, comprising granules containing nilotinib or a salt thereof with at least one pharmaceutically acceptable excipient. The granules may be produced by a wet granulation process.01-24-2013
20080255170Process for the Synthesis of Rosuvastatin Calcium - Present invention represents process for the preparation of HMG-CoA reductase inhibitors, in particular rosuvastatin calcium introducing L-malic acid as the source of chirality for the side chain.10-16-2008
20130172378Combination of BRAF and VEGF Inhibitors - A novel combination comprising the VEGFR inhibitor 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, with a B-Raf inhibitor, particularly N-(3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl)-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of VEGFR and/or B-Raf is beneficial.07-04-2013
20080249121INTERMEDIATES AND A PROCESS EMPLOYING THE INTERMEDIATES FOR THE PREPARATION OF (3-TRIFLUOROMETHYLSULFONYL)-N-[4-METHYL-3-(4-PYRIDIN-3YL-PYRIMIDIN-2YLAMINO)-PHENYL]-BENZAMIDE - This invention relates to a process for the preparation of (3-trifluoromethylsulfonyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide (formula (I)) starting from 4-methyl-2-nitro-aniline (formula (II)) through intermediates (3-trifluoromethylsulfonyl)-N-[4-methyl-3-nitrophenyl]-benzamide (formula (III)), (3-trifluoromethylsulfonyl)-N-[3-amino-4-methylphenyl]-benzamide (formula (IV)) and (3-trifluoromethylsulfonyl)-N-[3-guanidino-4-methylphenyl]-benzamide (formula (V)). This invention also relates to processes for the preparation of these intermediates. The compound of formula (I), also known as AN-024, is:10-09-2008
20100087466NOVEL SMALL MOLECULE DNAK INHIBITORS - Methods of inhibiting HSP70 proteins, agents causing the inhibition of HSP70 proteins, and the effects of such inhibition on cell proliferation. Anti-microbial agents comprising small molecules, or pharmaceutical salts thereof, disclosed herein and further methods of use thereof are also disclosed. The disclosed small molecules, or pharmaceutical salts thereof, are effective in inhibiting microbial chaperone activity in microbes, such as homologs of HSP70. The disclosed small molecules, or pharmaceutical salts thereof, are also effective for the therapeutic treatment of cancer.04-08-2010
20090012107Antiviral Compounds and Methods of Using Thereof - Disclosed herein are compounds which exhibit antiviral activity against a plurality of viruses belonging to different families such as Bornaviridae, Filoviridae, Paramyxoviridae, Rhabdoviridae, Arenaviridae, Bunyaviridae, Orthomyxoviridae, and Poxviridae. Thus, methods of preventing, inhibiting, or reducing the viral activity of various viruses are provided as well as methods of treating viral infections.01-08-2009
20080227800Pyrimidylaminobenzamide Derivatives for Hypereosinophilic Syndrome - The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of FIP1L1-PDGFRα-induced or TEL-PDGFRβ-induced myeloproliferative diseases, especially for the curative and/or prophylactic treatment of hypereosinophilic syndrome and hypereosinophilic syndrome with resistance to imatinib, and to a method of treating hypereosinophilic syndrome, chronic eosinophilic leukemia and hypereosinophilic syndrome with resistance to imatinib, or other diseases associated with FIP1L1-PDGFRα, TEL-PDGFRβ or similar mutations that activate PDGFR.09-18-2008
20080227799CXCR4 Antagonists Including Heteroatoms for the Treatment of Medical Disorders - The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor for the treatment of proliferative conditions mediated by CXCR4 receptors. The compounds provided interfere with the binding of SDF1 to the receptor. These compounds are particularly useful for treating or reducing the severity of hyperproliferative diseases by inhibiting metastasis.09-18-2008
20110263628N-HYDROXYAMIDE DERIVATIVES AND USE THEREOF - The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.10-27-2011
20130178491FUNGICIDAL COMPOSITION - A composition comprising (i) a compound of formula (I)07-11-2013
20130096149HETEROARYL COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The present invention provides compounds of Formula I:04-18-2013
20130123289CERTAIN AMINO-PYRIMIDINES, COMPOSITIONS THEREOF, AND METHODS FOR THEIR USE - Provided are compounds of Formula I:05-16-2013
201301310968-HYDROXY-QUINOLINE DERIVATIVES - The invention relates to compounds of the general formula (I) and their pharmaceutically acceptable salts (in which formula R05-23-2013
20100280056IDENTIFICATION OF SUBJECTS LIKELY TO BENEFIT FROM STATIN THERAPY - Methods are provided herein to determine if a subject is a candidate for treatment with an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGCR). The method includes determining the presence of at least one polymorphism in the HMGCR gene in a sample from a subject. The presence of at least one polymorphism indicates that the subject is a candidate for treatment with a statin, for example to decrease risk of or treat cancer, cardiovascular disease, diabetes, obesity, inflammatory disease, or auto-immune disease.11-04-2010
20130158057AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS - Compounds of the formula I:06-20-2013
20130158058HYPERCHOLESTEROLEMIA AND TENDINOUS INJURIES - This invention provides compositions and methods of inhibiting, suppressing, or treating a tendinous or musculoskeletal soft tissue injury. The invention further provides a method of ameliorating symptoms associated with a tendinous or musculoskeletal soft tissue injury. Additionally, the invention provides methods for evaluating the risk of developing a tendinous or musculoskeletal soft tissue injury.06-20-2013
20080200489Combination of Organic Compounds - The invention provides a pharmaceutical combination comprising: 08-21-2008
20080200488Combinations Comprising a Protein Kinase Inhibitor Being a Pyrimidylaminobenzamide Compound and a Hsp90 Inhibitor Such as 17-Aag - The invention provides a pharmaceutical combination comprising: 08-21-2008
20080200487Salts of 4-Methyl-N-[3-(4-Methyl-Imidazol-1-Yl)-5-Trifluoromethyl-Phenyl]-3-(4-Pyridin-3-Yl-Pyrimidin-2-Ylamino)-Benzamide - Salts of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide are prepared by various processes.08-21-2008
20080200486Combination Of Organic Compounds - The invention provides a pharmaceutical combination comprising: 08-21-2008
20110275655PYRIMIDINECARBOXAMIDE DERIVATIVES AS INHIBITORS OF SYK KINASE - The present invention relates to the compound of formula (I):11-10-2011
20110275654LONG TERM TREATMENT OF HIV-INFECTION WITH TMC278 - This invention relates to the use of a parenteral formulation comprising an anti-virally effective amount of TMC278 or a pharmaceutically acceptable acid-addition salt thereof, and a carrier, for the manufacture of a medicament for the treatment of a subject being infected with HIV, wherein the formulation is to be administered intermittently at a time interval of at least one week.11-10-2011
20110237612Thienylamino pyrimidines for use as Fungicides - Thienylaminopyrimidines of the formula (I)09-29-2011
20130150393Statin Bioavailability Enhancement Delivery Composition - A composition for increasing the bioavailability of a statin active pharmaceutical ingredient (“API”) in humans and animals, wherein that composition includes a statin API selected from the group consisting of atorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, and simvastatin, a first water soluble surfactant having a cloud point greater than about 37° C., a second water soluble surfactant having a cloud point greater than about 37° C., wherein a mixture of the first surfactant and the second surfactant comprises a cloud point less than about 37° C.06-13-2013
20100311775Novel sEH Inhibitors and Their Use - The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I:12-09-2010
20100317680PYRIMIDINE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts,12-16-2010
20100317679SUBSTITUTED ARYL-FUSED SPIROCYCLIC AMINES - Substituted Aryl-fused Spirocyclic Amines of the formula (I): are provided, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).12-16-2010
20100317678HYDROXAMATES AS INHIBITORS OF HISTONE DEACETYLASE - Compounds of formula (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers:12-16-2010
20130184300Methods of Treating Traumatic Brain Injury Using Pro-Neurogenic Compounds - This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death.07-18-2013
20130184301Methods of Treating Post-Traumatic Stress Disorder Using Pro-Neurogenic Compounds - This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death.07-18-2013
20110288110METHODS FOR TREATING DISORDERS ASSOCIATED WITH HYPERLIPIDEMIA IN A MAMMAL - The invention is directed to methods for treating hyperlipidemia in a mammal. The methods involve combination therapies using a microsomal triglyceride transfer protein (MTP) inhibitor (for example, BMS-201038 and implitapide) and a HMG-CoA reductase inhibitor (for example simvastatin or atorvastatin). Co-administration of the MTP inhibitor with the HMG-CoA reductase inhibitor produces a therapeutic benefit, for example, a reduction in the concentration of cholesterol and/or triglycerides in the blood stream, but with fewer or reduced side effects than when higher dosages of the MTP inhibitor are used during monotherapy to provide the same or similar therapeutic benefit.11-24-2011
20130123290Pyrimidylaminobenzamide Derivatives for Treatment of Neurofibromatosis - The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF, and to a method of treating non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF.05-16-2013
20090298860ANTIFUNGAL WALLBOARDS AND BUILDING MATERIALS AND METHODS FOR THE PRODUCTION THEREOF - The present invention relates to, inter alia, methods for the treatment of wallboards with fungicides and the treated wallboards. In particular, the invention relates to the treatment of wallboards with a fungicidally effective amount of difenoconazole. The invention also provides for the treatment of wallboards with synergistic combinations of difenoconazole and other fungicides. The invention also provides the treatment of building materials with difenoconazole and synergistic mixtures containing difenoconazole.12-03-2009
20110312985NARINGENIN COMPLEXES AND METHODS OF USE THEREOF - The invention relates to methods of treatment of hepatitis C, dyslipidemia, insulin resistance, and inflammation, with flavonoid-sugar complexes.12-22-2011
20130190339Pro-Neurogenic Compounds - This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death.07-25-2013
20130190340Small-Molecule-Targeted Protein Degradation - Certain aspects of the invention relate to compounds, compositions and methods that are useful for treating or preventing a disease in a subject by enhancing the degradation of a protein. In other aspects, said compounds can be useful research tools for investigating protein degradation. In other aspects, said compounds are useful research tools for investigating protein function. In certain embodiments, the degraded protein is implicated in a disease or disorder whose pathology is related at least in part to the excessive expression of the protein or the expression of a mutant form of the protein.07-25-2013
20120029004NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION - The present invention relates to a compound of Formula (I): wherein: R02-02-2012
20120029003GALECTIN-3 AND STATIN THERAPY - Described herein are materials and methods for predicting and monitoring a heart failure patient's physiological response to treatment with a statin. More specifically, the present invention relates to the endogenous protein galectin-3 and its use as a predictor of response to treatment with 3-hydroxy-3-methylglutaryl coenzyme-A reductase inhibitors, or statins.02-02-2012
20120029002BENZIMIDAZOLE AND PYRAZOLOPYRIDINE DERIVATIVES FOR TREATING AND/OR PREVENTING CARDIOVASCULAR DISEASES - The present application relates to novel fused, heteroatom-bridged pyrazole and imidazole derivatives, to processes for their preparation, to their use, alone or in combination, for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.02-02-2012
20120029001METHOD OF TREATMENT OF NEPHROGENIC DIABETES INSIPIDUS - Nephrogenic diabetes insipidus is treated with statins.02-02-2012
20130197017COMBINATIONS COMPRISING A PROTEIN KINASE INHIBITOR BEING A PYRIMIDYLAMINOBENZAMIDE COMPOUND AND A HSP90 INHIBITOR SUCH AS 17-11G - The invention provides a pharmaceutical combination comprising: 08-01-2013
20130197018Synergistic Fungicidal Active Substance Combinations - Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1)08-01-2013
20130203792CO-CRYSTALS OF PYRIMETHANIL OR CYPRODINIL - The present invention relates to co-crystals of cyprodinil or pyrimethanil and a co-crystal forming compound which has at least one imide and/or oxime functional group.08-08-2013

Patent applications in class Nitrogen bonded directly to the 1,3-diazine at 2-position by a single bond