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Bicyclo ring system having the six-membered hetero ring as one of the cyclos (e.g., 1,4-benzoxazines, etc.)

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

514228800 - Hetero ring is six-membered and includes at least nitrogen and oxygen as ring hetero atoms (e.g., monocyclic 1,2- and 1,3-oxazines, etc.)

514229500 - Polycyclo ring system having the six-membered hetero ring as one of the cyclos (e.g., maytansinoids, etc.)

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Entries
DocumentTitleDate
20080300243Amide Derivatives as Ion-Channel Ligands and Pharmaceutical Compositions and Methods of Using the Same - Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.12-04-2008
20130045973AMIDE DERIVATIVES AS ION-CHANNEL LIGANDS AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME - Compounds are disclosed that have a formula represented by the following:02-21-2013
20130045972GLUCOCORTICOID RECEPTOR ANTAGONISTS - The present invention relates to compounds of formula I02-21-2013
20110201607FUSED HETEROCYCLIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to fused heterocyclic compounds of formula (I): which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.08-18-2011
20120184541COMPOUNDS AND METHODS OF USE - In one aspect, the present invention provides for a compound of Formula I07-19-2012
20120184543DIHYDROPTERIDINONE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF - Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defined as in the description, their preparation process, pharmaceutical compositions comprising said derivatives and their use as therapeutical agents, especially as Plk kinase inhibitors are disclosed.07-19-2012
20120184542PYRIDO PYRIMIDINES - Compounds of formula07-19-2012
20090192149Imidazo Compounds - The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R07-30-2009
20100016297ALKYL-SUBSTITUTED 3' COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY - The present disclosure provides compounds having affinity for the 5-HT01-21-2010
20120178749NS1 PROTEIN INHIBITORS - The present invention generally relates to compounds to treat viral infections and methods of their use. In particular, compounds of the present invention inhibit the activity of NS1 protein, thereby mitigating viral infection and, in particular, influenza virus infection. Accordingly, NS1 protein inhibitors and methods of treatment that employ such inhibitors are contemplated by the present invention.07-12-2012
201001603053, 4, 5 - Substituted Piperidine Compounds - 3,4,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4,5-substituted piperidine compound, a method for the manufacture of a 3,4,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis.06-24-2010
20120245162OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I):09-27-2012
20130085138Selective NR2B Antagonists - The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.04-04-2013
20130079338Selective NR2B Antagonists - The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.03-28-2013
20130079339TRPV1 VANILLOID RECEPTOR ANTAGONISTS WITH A BICYCLIC PORTION - The invention discloses compounds of formula I03-28-2013
20130079337PYRAZOLOQUINOLINONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to compounds corresponding to formula (I)03-28-2013
20130029979FUSED BICYCLIC COMPOUND - Fused bicyclic compound having an affinity to mineral corticoid receptor (MR), of formula [I]:01-31-2013
20130029978NOVEL ARYL UREA DERIVATIVE - There is a need for FAAH inhibitors capable of oral administration and having excellent efficacy, particularly agents for the prevention and treatment of pain. Disclosed are novel arylurea compounds represented by formula (I), salts or solvates thereof, and pharmaceutical compositions comprising the same as an active ingredient. The pharmaceutical composition is used primarily for FAAH inhibitors, or agents for prevention and treatment of pain.01-31-2013
20090209528SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUND, THEIR PREPARATION AND USE IN MEDICAMENTS - The present invention relates to substituted tetrahydroisoquinoline compounds of general formula (I), a process for their preparation, medicaments comprising said substituted tetrahydroisoquinoline compounds as well as the use of said substituted tetrahydroisoquinoline compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT08-20-2009
20130040944MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION - Pyrrole compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.02-14-2013
20100063040Sulfonamide Derivative Having PGD2 Receptor Antagonistic Activity - The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases.03-11-2010
20090149454Benzomorpholine derivatives and methods of use - Selected benzomorpholine compounds are effective for prophylaxis and treatment of diseases, such as VEGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.06-11-2009
20100324035Carboxamide Compounds and Their Use - Chemokine receptor antagonists, in particular, compounds of Formula (I-A) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.12-23-2010
20100324034Methods of Using SAHA for Treating HIV Infection - The present invention relates to pharmaceutical preparations and methods for treating individuals infected with the human immunodeficiency virus (HIV). The pharmaceutical preparations comprise SAHA and another anti-viral agent. The invention also relates to methods for treating HIV infected patients, particularly patients with persistent, latent HIV infection of CD412-23-2010
200901565883,4-DIHYDRO-BENZO[E][1,3]OXAZIN-2-ONES - The present invention relates 3,4-dihydro-benzo[e][1,3]oxazin-2-ones which are substituted at the nitrogen atom by unsubstituted or substituted (C06-18-2009
200901565891,2-DI(CYCLIC GROUP)SUBSTITUTED BENZENE DERIVATIVE - A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action and cell infiltration inhibitory action.06-18-2009
20100105670FUNGICIDAL MIXTURES - Disclosed is a fungicidal mixture comprising (a) at least one compound selected from the compounds of Formula 1 N-oxides, and salts thereof,04-29-2010
20100029629ACYCLIC COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY - The present disclosure provides compounds having affinity for the 5-HT02-04-2010
20120214805BRIDGED BICYCLIC PIPERIDINE DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to Bridged Bicyclic Piperidine Derivatives, compositions comprising a Bridged Bi-cyclic Piperidine Derivative, and methods of using the Bridged Bicyclic Piperidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.08-23-2012
20090124609Fused heterocyclic derivatives and methods of use - Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.05-14-2009
20090124608CB2 Receptor Modulators In Neurodegenerative Diseases And Applications Of The Same - Compositions for the treatment of neurodegenerative diseases are disclosed. Methods of treating and monitoring progression of a neurodegenerative disease are disclosed. According to the present invention, a selective CB2 receptor modulator may be administered to a mammal for the treatment of a neurodegenerative disease.05-14-2009
20130090333BENZOXAZINE DERIVATIVES AS CRAC MODULATORS - Compounds of the formula (I):04-11-2013
20090042875SUBSTITUTED HETEROCYCLIC COMPOUNDS AND USES THEREOF - The present invention relates to substituted heterocyclic compounds and compositions comprising a substituted heterocyclic compound. The present invention also relates to methods for preventing or treating various diseases and disorders by administering to a subject in need thereof one or more substituted heterocyclic compounds. In particular, the invention relates to methods for preventing or treating cancer or an inflammatory disorder by administering to a subject in need thereof one or more substituted heterocyclic compounds. The present invention further relates to articles of manufacture and kits comprising one or more substituted heterocyclic compounds.02-12-2009
20090318431BENZOXAZINONE AND BENZOXAZEPINONE OXAZOLIDINONES AS ANTIBACTERIAL AGENTS - The present invention provides a compound of formula (I) wherein X is a structure of the following formula (i), (ii) (iii), or iv G is O, or S; U is —(CR12-24-2009
20130090334AZABENZOXAZINE DERIVATIVES AS CRAC MODULATORS - Compounds of the formula (I):04-11-2013
20090318432Nitrate esters of aminoalcohols - The application relates to novel nitrate ester derivatives of substituted aminoalcohols of the general formula (I), wherein R12-24-2009
20110009399ORGANIC COMPOUNDS - The application relates to trisubstituted piperidines of the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R01-13-2011
20110009398p27 Protein Inducer - The present invention provides a p27 protein inducing agent comprising a compound represented by general formula (11) below or pharmaceutically acceptable salt thereof as an active ingredient:01-13-2011
20090306069AZOLIDINONE-VINYL FUSED-BENZENE DERIVATIVES - The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, graft rejection or lung injuries.12-10-2009
200903060672, 4-DIAMINOPYRIMIDIDE DERIVATES AND THEIR USE FOR THE TREATMENT OF CANCER - The present invention encompasses compounds of general formula (1) wherein Q and R12-10-2009
20090306066PEPTIDE DEFORMYLASE INHIBITORS - The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives, compositions containing them, the use of such compounds in the inhibition of bacterial peptide deformylase (PDF) activity, and in the treatment of bacterial infections. Specifically, the invention is directed to compounds of formula (I):12-10-2009
20090306065AEROSOL FORMULATION FOR INHALATION CONTAINING AN ANTICHOLINERGIC AGENT - The invention relates to specific aqueous aerosol formulations that are devoid of propellant, containing one or more anticholinergic agents of formula (1), in which X represents an anion, and containing at least one pharmacologically compatible organic acid and optionally additional pharmacologically compatible adjuvants and/or complexing agents. The cation of formula (1′) is contained in the preparation at a concentration of between 83 and 94.5 mg per 100 ml of medicament preparation.12-10-2009
20090306064Substituted Piperidines as Renin Inhibitors - Compounds of the general formula (I) in which the meanings of the substituents R12-10-2009
20090306068NOVEL ENANTIOMERIC PURE BETA AGONISTS, MANUFACTURING AND USE AS A MEDICAMENTS THEREOF - The present invention relates to enantiomerically pure compounds of formula 112-10-2009
20090093472ORTHO PYRROLIDINE, BENZYL-SUBSTITUTED HETEROCYCLE CCR1 ANTAGONISTS FOR AUTOIMMUNE DISEASES & INFLAMMATION - Compounds of the formula04-09-2009
20130072480Cyclothiocarbamate Derivatives as Progesterone Receptor Modulators - Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure:03-21-2013
20130072479HETEROCYCLIC COMPOUNDS AND USES THEREOF IN THE TREATMENT OF SEXUAL DISORDERS - Novel heterocyclic compounds, which exhibit a dopamine receptor (preferably a D4 receptor) agonistic activity, and/or a PDE5 inhibitory activity, processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of sexual disorders such as decreased libido, orgasm disorder and erectile dysfunction are disclosed.03-21-2013
20130072478N-(3-(2-AMINO-6,6-DIFLUORO-4,4A,5,6,7,7A-HEXAHYDRO-CYCLOPENTA[E][1,3]OXAZI- N-4-YL)-PHENYL-AMIDES AS BACE1 INHIBITORS - The present invention provides N-(3-(2-amino-6,6-difluoro-4,4a,5,6,7,7a-hexahydro-cyclopenta[e][1,3]oxazin-4-yl)-phenyl)-amides of formula I03-21-2013
20110015190GAMMA SECRETASE MODULATORS - This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R01-20-2011
20110015189METHODS OF MAKING EFAVIRENZ AND INTERMEDIATES THEREOF - The present invention provides a process for the preparation of Efavirenz. A compound of Formula 1 may be prepared by a process comprising cyclizing, in the presence of a first base, a compound of Formula 5 with a haloformate of Formula 6. Other processes are also provided as well as novel compounds prepared by and used in such processes.01-20-2011
200802808955-Amino-4-Hydroxy-7-(1H-Indolmethyl)-8-Methylnonamide Derivatives as Renin Inhibitors for the Treatment of Hypertension - The application relates to novel alkanamides of the general formula (I) where X is —CH11-13-2008
20090291948SULFONAMIDE PERI-SUBSTITUTED BICYCLICS FOR OCCLUSIVE ARTERY DISEASE - Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula11-26-2009
20090270382Soluble epoxide hydrolase inhibitors - Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases.10-29-2009
20090270383Novel Oxabispidine Compounds And Their Use In The Treatment Of Cardiac Arrhythmias - There is provided compounds of formula (I), wherein R10-29-2009
200902703803,4,5-Substituted Piperidines as Renin Inhibitors - The application relates to novel substituted piperidines of the general formula (II) in which R10-29-2009
20130065892HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.03-14-2013
20110021516MONOCYCLIC CGRP RECEPTOR ANTAGONISTS - The present invention is directed to compounds of the formula (I): (wherein variables A01-27-2011
20110021515DIHYROFUROPYRMINDINE COMPOUNDS - The present invention provides mTOR inhibitors of the formula01-27-2011
20110021514AMIDE DERIVATIVES AS ION-CHANNEL LIGANDS AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME - Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.01-27-2011
20110021513MODULATORS OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE - The present invention relates to modulators of IRAK kinase and provides compositions comprising such modulators, as well as methods therewith for treating conditions or diseases mediated by or associated with IRAK kinase.01-27-2011
20090264424VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS - Compounds having the general structure10-22-2009
20090124610PHARMACEUTICAL COMPOUNDS - Compounds of the formula (I), and salts, solvates, tautomers and N-oxide thereof, wherein TG is selected from groups (1) and (2): wherein the asterisk (*) represents the point of attachment of the group E to the group X; R05-14-2009
201201158593,4,5-SUBSTITUTED PIPERIDINES AS RENIN INHIBITORS - The application relates to novel substituted piperidines of the general formula (II) in which R05-10-2012
20120115858Polymorph Form II of Tanaproget - Tanaproget polymorph Form II, processes for preparing tanaproget polymorph Form II, pharmaceutical compositions including tanaproget polymorph Form II, micronized tanaproget polymorph Form II, and processes for converting Form II to tanaproget Form I are provided. Also provided are methods of contraception, hormone replacement therapy, stimulation of food intake and treating or preventing uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, or carcinomas and adenocarcinomas comprising administering polymorph Form II to a mammalian subject.05-10-2012
20120115857Novel Polymorphs of Efavirenz - The present invention relates to novel amorphous and crystalline forms of efavirenz, processes for their preparation and pharmaceutical compositions containing them. In accordance with the present invention efavirenz crude is dissolved in acetone at 25° C.-30° C., the solution is slowly added to water for 30 minutes at 0° C.-5° C., stirred for 1 hour at the same temperature, the separated solid is filtered, washed with water and dried at 55° C.-60° C. for 5 hours to give amorphous efavirenz.05-10-2012
20120035168N-((6-AMINO-PYRIDIN-3-YL)METHYL)-HETEROARYL-CARBOXAMIDES - The invention relates to compound of the formula I02-09-2012
20090012073N-AROYL CYCLIC AMINES - Disclosed are N-aroyl cyclic amine derivatives having the formula:01-08-2009
20120238561MORPHOLINOTHIAZOLES AS ALPHA 7 POSITIVE ALLOSTERIC MODULATORS - The present invention relates to morpholinothiazole derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulators having the capability to increase the efficacy of nicotinic receptor agonists.09-20-2012
20130165436Dihydro-Benzo-Oxazine and Dihydro-Pyrido-Oxazine Derivatives - The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof,06-27-2013
20080293710Aerosol formulation for the inhalation of beta-agonists - The present invention relates to a propellant-free aerosol formulation which [contains] one or more compounds of general formula 111-27-2008
20080293709Novel 2-Amino-Heterocycles Useful in the Treatment of Abeta-Related Pathologies - This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.11-27-2008
20080293708Pyrimidine Derivatives - Novel pyrimidine derivatives of formula I11-27-2008
20110028465AMIDE DERIVATIVES AS ION-CHANNEL LIGANDS AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME - Compounds are disclosed that have a formula represented by the following:02-03-2011
20100273788FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF - The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof.10-28-2010
20110034452TRIAZOLIUM SALTS AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS - The invention relates to novel compounds of formula I02-10-2011
20110319404METHOD FOR TREATING NON-HODKIN'S LYMPHOMA - The present invention relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating non-Hodgkin's lymphoma, in a subject in need thereof.12-29-2011
20090099163GLUCOKINASE ACTIVATORS - Compounds are provided for use with glucokinase that comprise the formula:04-16-2009
20090099164Phenylaminopropanol Derivatives and Methods of Their Use - The present invention is directed to phenylaminopropanol derivatives of formula I:04-16-2009
20110281859NOVEL HETEROCYCLIC COMPOUNDS AS METAP-2 INHIBITORS - Compounds of the formula I, in which D, X, Y, Z, R and R11-17-2011
20110281858AEROSOL FORMULATION FOR THE INHALATION OF BETA AGONISTS - The present invention relates to a propellant-free aerosol formulation which [contains] one or more compounds of general formula (1) wherein the groups R11-17-2011
20110281857PI3K/MTOR KINASE INHIBITORS - 6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidine and 2-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidine derivatives have unexpected drug properties as inhibitors of PI3 and/or mTOR kinases and are useful in treating disorders related to abnormal PI3K/mTOR activities such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.11-17-2011
20100267715Polymorph Form II of Tanaproget - Tanaproget polymorph Form II, processes for preparing tanaproget polymorph Form II, pharmaceutical compositions including tanaproget polymorph Form II, micronized tanaproget polymorph Form II, and processes for converting Form II to tanaproget Form I are provided. Also provided are methods of contraception, hormone replacement therapy, stimulation of food intake and treating or preventing uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, or carcinomas and adenocarcinomas comprising administering polymorph Form II to a mammalian subject.10-21-2010
20100267714MIF MODULATORS - The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.10-21-2010
201002677134,4-DISUBSTITUTED PIPERIDINES - The application relates to 4,4-disubstituted piperidines of the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R10-21-2010
201002491242,3-DIARYL- OR HETEROARYL-SUBSTITUTED 1,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS - The present invention relates to compounds of formula I09-30-2010
20100249123NOVEL BENZAMIDE DERIVATIVES AS MODULATORS OF THE FOLLICLE STIMULATING HORMONE - The present invention provides new compounds of formula I, wherein Q, R09-30-2010
20100190782COMPOUNDS AND METHODS OF USE - In one aspect, the present invention provides for a compound of Formula I07-29-2010
20110124637BENZIMIDAZOLES AND RELATED ANALOGS AS SIRTUIN MODULATORS - Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.05-26-2011
20110301156Vanilloid Receptor Ligands, Pharmaceutical Compositions Containing Them, Process For Making Them, and Use Thereof to Treat Pain and Other Conditions - Vanilloid receptor ligand compounds corresponding to formula I:12-08-2011
20100035871BENZOXAZINE DERIVATIVES AND USES THEREOF - Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided, wherein each of Z, X, R02-11-2010
20110294797REVERSE-TURN MIMETICS AND METHOD RELATING THERETO - Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.12-01-2011
20110301157BICYCLIC AMIDES AS KINASE INHIBITORS - The invention relates to compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.12-08-2011
20100035872PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS - Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.02-11-2010
20090275572FAB I INHIBITORS - Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.11-05-2009
20100267712ISOINDOLINE COMPOUNDS FOR THE TREATMENT OF SPINAL MUSCULAR ATROPHY AND OTHER USES - Disclosed is a compound of Formula (I) in which W and R10-21-2010
20120065197Pyridinylcarboxylic Acid Derivatives as Fungicides - Pyridinylcarboxylic acid derivatives of the formula (I)03-15-2012
20120101090CRYSTAL OF A BENZOXAZINONE COMPOUND - Disclosed is a crystal of 2-hexadecyloxy-6-methyl-4H-3,1-benzoxazin-4-one useful as a preventive or therapeutic agent for obesity and the like. Specifically disclosed is a crystal of 2-hexadecyloxy-6-methyl-4H-3, 1-benzoxazin-4-one having a powder X-ray diffraction pattern in which characteristic peaks appear at powder X-ray diffraction interplanar spacings (d) of around 16.54±0.2, 13.26±0.2, 4.70±0.2, 4.38±0.2, and 3.67±0.2A.04-26-2012
20120035167INDOLE AND BENZOXAZINE DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel indole and benzoxazine derivatives which are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”) and which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.02-09-2012
20100120758REVERSE-TURN MIMETICS AND METHOD RELATING THERETO - Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.05-13-2010
20120316161NOVEL ANTIVIRAL COMPOUNDS - The present invention relates to compounds of formula (A) as defined herein having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.12-13-2012
20110195963NOVEL CARBAMOYLOXY ARYLALKANOYL ARYLPIPERAZINE COMPOUND, PHARMACEUTICAL COMPOSITIONS COMPRISING THE COMPOUND AND METHOD FOR TREATING PAIN, ANXIETY AND DEPRESSION BY ADMINISTERING THE COMPOUND - There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.08-11-2011
20110201606PYRIMIDINE DERIVATIVES - Novel pyrimidine derivatives of formula I08-18-2011
20110201605HETEROARYL SUBSTITUTED PIPERIDINES - The invention relates to compounds of formula08-18-2011
20100081655REVERSE-TURN MIMETICS AND METHOD RELATING THERETO - Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.04-01-2010
20100099670Benzoquinazoline derivatives - A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof:04-22-2010
20100125069Methods of Treating or Preventing Autoimmune Diseases with 2,4-Pyrimidinediamine Compounds - The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.05-20-2010
20090088424METHODS AND COMPOSITIONS FOR CONTROLLING THE BIOAVAILABILITY OF POORLY SOLUBLE DRUGS - Provided are methods and compositions for controlling the bioavailability of poorly soluble drugs, including, for example, efravirenz.04-02-2009
20090088426Substituted 4-Phenyl Piperidines for Use as Renin Inhibitors - Compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which R04-02-2009
20110172221ANNELLATED 4-(INDAZOLYL)-1,4-DIHYDROPYRIDINE DERIVATIVES AND METHODS OF USE THEREOF - This invention relates to novel annellated 4-(indazolyl)-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.07-14-2011
20110172220DISCODERMOLIDE ANALOGUES AND METHODS OF THEIR USE - 6- and 7-substituted coumarin and related 6- and 7-substituted 1H-quinolin-2-one compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the 7-substituted coumarin and related 7-substituted 1H-quinolin-2-one compounds mimic or exceed the high level of pharmacological activity of discodermolide. In other embodiments, their preparation involves more readily available materials, higher yield processes and/or simpler synthetic sequences. In yet other embodiments, the compounds of the invention represent structurally simpler, therapeutically active analogues of discodermolide than heretofore known and may be useful as microtubule stabilizers and, inter alia, for treating and/or preventing cancer and other diseases, disorders, and/or conditions mediated by the stabilization of microtubules.07-14-2011
20090275574NOVEL COMPOUNDS-300 - Compounds of Formula I, or pharmaceutically acceptable salts thereof:11-05-2009
20090275573Imidazolidinone Derivatives as 11B-HSD1 Inhibitors - Compounds of formula11-05-2009
20090281096CYCLOTHIOCARBAMATE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS - Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure:11-12-2009
20090286774PURINONE DERIVATIVES AS HM74A AGONISTS - The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease.11-19-2009
20090291947PROLINE ANALOGS AS LIGANDS FOR CANNABINOID RECEPTORS - The present invention relates to Proline Analog Compounds that are ligands for cannabinoid receptors, compositions comprising a Proline Analog Compound and a pharmaceutically-acceptable carrier, methods of making such Proline Analog Compounds, and methods for treating or preventing a Condition comprising administering an effective amount of a Proline Analog Compound to an animal in need thereof.11-26-2009
20120295902Hetaryl-[1,8]naphthyridine derivatives - Novel hetaryl-[1,8]naphthyridine derivatives of formula (I)11-22-2012
20120295901NOVEL SUBSTITUTED BICYCLIC TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS - The present invention is concerned with novel substituted bicyclic triazole derivatives of Formula (I)11-22-2012
20090062269Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment - The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.03-05-2009
200902988203-SUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINE AND 3-SUBSTITUTED-1H-PYRROLO[3,2-B]PYRIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES - The invention relates to 3-substituted-1H-pyrrolo[2,3-b]pyridine, and 3-substituted-1H-pyrrolo[3,2-b]pyridine compounds of the Formula 1:12-03-2009
20090170839AEROSOL FORMULATION FOR INHALATION CONTAINING AN ANTICHOLINERGIC AGENT - The invention relates to specific aqueous aerosol formulations that are devoid of propellant, containing one or more anticholinergic agents of formula (1), in which X represents an anion, and containing at least one pharmacologically compatible organic acid and optionally additional pharmacologically compatible adjuvants and/or complexing agents. The cation of formula (1′) is contained in the preparation at a concentration of between 830.22 and 904.2 mg per 100 ml of medicament preparation.07-02-2009
20080280896Dipyrrole Compounds, Compositions, and Methods For Treating Cancer or Viral Diseases - The present invention relates to novel Dipyrrole Compounds, compositions comprising a Dipyrrole Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Dipyrrole Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus. The invention also provides screening assays for compounds that can be used in combination with Dipyrrole Compounds for the treatment of cancer or neoplastic disease, inhibition of cancer cell growth, or treatment of viral infections.11-13-2008
20080287428Novel Heterocyclidene Acetamide Derivative - A compound represented by formula (I′):11-20-2008
20080306057P13K Inhibitors for the Treatment of Endometriosis - This invention relates to a method of treating and/or preventing endometriosis comprising administering a PI3K inhibitor. The PI3K inhibitor can also be administered combined with a hormonal suppressor. The invention further relates to the treatment of endometriosis-related infertility.12-11-2008
201202959001,3-OXAZINES AS BACE 1 AND/OR BACE2 INHIBITORS - The present invention provides compounds of formula I11-22-2012
20080249087Heterocylic antiviral compounds - This invention relates to piperidine derivatives of formula I wherein R10-09-2008
20080287427Bicyclic Amides as Kinase Inhibitors - The invention relates to compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising en a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.11-20-2008
20080269208Pyridine Derivatives and Their Use in the Treatment of Psychotic Disorders - There are provided according to the invention novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof:10-30-2008
20100137297SPIROINDALONES - The present invention relates to spiroindalone compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.06-03-2010
20090029981SUBSTITUTED 4-PHENYLPIPERIDINES - The application relates to substituted 4-phenylpiperidines of the general formula and their salts, preferably their pharmaceutically acceptable salts, in which R01-29-2009
20120035169AEROSOL FORMULATION FOR THE INHALATION OF BETA-AGONISTS - The present invention relates to a propellant-free aerosol formulation which [contains] one or more compounds of general formula 102-09-2012
20090137577HETEROCYCLIC COMPOUNDS - Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I05-28-2009
200803189414' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY - The present disclosure provides compounds having affinity for the 5-HT12-25-2008
20080234257SUBSTITUTED PHENETHYLAMINES WITH SEROTONINERGIC AND/OR NOREPINEPHRINERGIC ACTIVITY - Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and/or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, attention deficit hyperactivity disorder, fibromyalgia, irritable bowel syndrome, and/or premature ejaculation are described.09-25-2008
20100004233NOVEL COUMARIN DERIVATIVE HAVING ANTITUMOR ACTIVITY - The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof:01-07-2010
20120094990PHENYLACETIC ACID COMPOUND - A compound represented by formula (I),04-19-2012
20090325950Benzoxazine derivatives and uses thereof - The present invention provides a compound of the formula:12-31-2009
20090325948INHIBITORS OF UNDECAPRENYL PYROPHOSPHATE SYNTHASE - The present invention relates to compounds that are selective and/or potent inhibitors of UPPS. In addition to compounds which inhibit UPPS, the invention also provides pharmaceutical compositions comprising these compounds and methods of using these compounds for treating bacterial disease, such as bacterial infection.12-31-2009
20090325947NITRATE ESTERS OF PIPERIDINES - The application relates to novel nitrate ester derivatives of substituted piperidines of the general formula (I), wherein R12-31-2009
20090023716Benzoxazines and Related Nitrogen-Containing Heterobicyclic Compounds Useful as Mineralocorticoid Receptor Modulating Agents - The present invention relates to a compound, useful as a mineralocorticoid receptor-modulating agent, of the following formula [I]:01-22-2009
20090023717MORPHINE-BRIDGED INDAZOLE DERIVATIVES - The present invention relates to novel morpholine-bridged indazole derivatives which stimulate soluble guanylate cyclase, to process for the preparation thereof, and to the use thereof for producing medicaments, in particular medicaments for the treatment of disorders of the central nervous system.01-22-2009
20110144098AMINO OXAZINE DERIVATIVES - This invention relates to 5,6-dihydro-4H-[1,3]oxazin-2-ylamine compounds of the formula06-16-2011
20090062267L-ALANINE DERIVATIVES AS a5beta1 ANTAGONISTS - The present invention relates to compounds that inhibit a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins.03-05-2009
20090054422New Oxabispidine Compounds For The Treatment Of Cardiac Arrhythmias - There is provided compounds of formula I, wherein R02-26-2009
20090054424Optically active pyridine derivative and a medicament containing the same - An optically active (−)-7-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-5-[(3S)-3-piperidinyl]-1,4-dihydro-2H-pyrido[2,3-d][1,3]oxazin-2-one of the formula:02-26-2009
20090099162Novel Oxabispidine Compounds And Their Use In The Treatment Of Cardiac Arrhythmias - There is provided compounds of formula I, 04-16-2009
20090062270SPIRO 2,4 PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES - The present invention provides methods of treating or preventing autoimmune diseases with spiro 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lupus erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.03-05-2009
20090192150IMINO-IMIDAZO-PYRIDINE DERIVATIVES HAVING ANTITHROMBOTIC ACTIVITY - The invention relates to compounds of the formula I07-30-2009
20110230477COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN TREATING METABOLIC DISORDERS - The present invention is directed to novel compounds of formula (I) and their use in treating metabolic diseases.09-22-2011
20110230476PI3 KINASE INHIBITORS AND USES THEREOF - The present invention provides compounds, compositions thereof, and methods of using the same.09-22-2011
20090054425PROTEIN KINASE INHIBITORS - Compounds, particularly compounds having spleen tyrosine kinase (Syk) inhibition activity, having the following structure:02-26-2009
20090088425GLUCOCORTICOID RECEPTOR ANTAGONISTS - The present invention relates to compounds of formula I04-02-2009
20080261965KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFIC DISEASES AND OTHER PROLIFERATIVE DISEASES - Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant, melanomas, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, leukemias, papillary thyroid carcinoma, non small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocyclosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.10-23-2008
20090197877Antibacterial Compositions - Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C08-06-2009
20090197879VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS - Compounds having the general structure08-06-2009
200902095294,5-DIHYDRO-OXAZOL-2-YL AMINE DERIVATIVES - The present invention relates to a compounds of formula I08-20-2009
20090239856Use of Pyrrolopyridine Compounds for Activating PPAR Receptors and Treatment of Conditions Involving Such Receptors - A method of activating PPAR receptors in a subject, said method comprising administering to said subject an effective PPAR receptor activating amount of a pyrrolopyridine compound corresponding to formula (I):09-24-2009
200902536932H-BENZO[b][1,4]OXAZIN-3(4H)-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I:10-08-2009
20090221566INHIBITORS OF PHOSPHODIESTERASE TYPE-IV - The present invention relates to oxazine derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. Compounds disclosed herein can be useful in the treatment of CMS disorders, AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases especially in humans. Processes for the preparation of disclosed compounds are provided, as well as pharmaceutical compositions containing the disclosed compounds, and their use as phosphodiesterase (PDE) type IV inhibitors.09-03-2009
20090197878SUBSTITUTED BENZO[d][1,3]OXAZIN-2(4H)-ONES AND RELATED DERIVATIVES AND THEIR USES FOR MODULATING THE PROGESTERONE RECEPTOR - Compounds of formula (I), or pharmaceutically acceptable salts thereof, are provided, wherein R08-06-2009
20090253691TRISUBSTITUTED 1,2,4-TRIAZOLES - The present invention relates to 3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I).10-08-2009
20090275571MORPHOLINYL AND PYRROLIDINYL ANALOGS - The present invention relates to morpholinyl, and pyrrolidinyl analogs, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.11-05-2009
20090275570SUBSTITUTED HETEROCYCLES AND THEIR USE AS CHK1, PDK1 AND PAK INHIBITORS - The invention relates to novel compounds of Formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds possess CHK1 kinase inhibitory activity, PDK1 inhibitory activity and Pak kinase inhibitory activity and are accordingly useful in the treatment and/or prophylaxis of cancer.11-05-2009
20100152176Modulators of Muscarinic Receptors - The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.06-17-2010
20100152175Pyridine Derivatives and Their Use in The Treatment of Psychotic Disorders - There are provided according to the invention novel compounds of formula (I) or a pharmaceutically acceptable salt thereof:06-17-2010
20100160306Acylated Piperidine Derivatives as Melanocortin-4 Receptor Agonists - Certain novel 4 alkyl substituted N acylated piperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.06-24-2010
20090270381Non-steroidal progesterone receptor modulators - The present invention relates to non-steroidal progesterone receptor modulators of the general formula I,10-29-2009
20100168095MULTI-CYCLIC CINNAMIDE DERIVATIVES - The present invention provides a compound represented by the formula (I):07-01-2010
20100197679COMPOUNDS - Bicyclic nitrogen containing compounds and their use as antibacterials08-05-2010
20110059957BENZENE OR THIOPHENE DERIVATIVE AND USE THEREOF AS VAP-1 INHIBITOR - The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.03-10-2011
20100216784Compounds for Inhibiting Beta-Amyloid Production and Methods of Identifying the Compounds - Provided are compounds useful for treating diseases associated with a cerebral accumulation of Alzheimer's amyloid, such as Alzheimer's disease. Also provided are methods for screening for such compounds, by measuring capacitative calcium entry in cells which optionally overexpress APP or a fragment thereof. Also provided are methods of treating or reducing the risk of developing β-amyloid production, β-amyloid deposition, β-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and microgliosis associated with cerebral accumulation of Alzheimer's amyloid by administering therapeutically effective amounts of compounds which decrease β-amyloid production and capacitative calcium entry in cells. Further provided are methods for diagnosing diseases associated with cerebral accumulation of Alzheimer's amyloid in animals or humans by administering diagnostically effective amounts of compounds which inhibit capacitative calcium entry in cells.08-26-2010
20100216782HYDROXYBENZAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF HSP90 - This invention provides methods for treating, alleviating or reducing the incidence of a disease or condition comprising or arising from abnormal cell growth in a mammal, which comprise administering to the mammal a compound, salt, hydrate, tautomer or N-oxide according to formula (I):08-26-2010
20090075992Pteridine Derivatives as Nitric Oxide Synthase Activators - The present invention relates to the use of pteridine derivatives as nitric oxide synthase activators. In particular, the derivatives find use in the treatment of diseases associated with endothelial dysfunction such as cardiovascular diseases.03-19-2009
20090075990Aerosol Formulation for Inhalation Containing an Anticholinergic Agent - The invention relates to specific aqueous aerosol formulations that are devoid of propellant, containing one or more anticholinergic agents of formula (1), in which X03-19-2009
20090075989NON-STEROIDAL PROGESTERONE RECEPTOR MODULATORS - The present invention relates to non-steroidal progesterone receptor modulators of the general formula 1,03-19-2009
20100222336SINGLE ENANTIOMER BETA-AGONISTS, METHODS FOR THE PRODUCTION THEREOF AND THE USE THEREOF AS MEDICATION - The present invention relates to single enantiomer compounds of formula (1), where the moieties n, A, R09-02-2010
20100210635RENIN INHIBITORS - Compounds, pharmaceutical compositions, kits and methods are provided for use with Renin that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.08-19-2010
20100210636BENZOXAZINONE DERIVATIVE08-19-2010
20100087427PYRROLIDINE DERIVATIVES FOR THE TREATMENT OF A DISEASE DEPENDING ON THE ACTIVITY OF RENIN - Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I04-08-2010
20100120759AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS - The present invention provides a novel class of azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.05-13-2010
20100222335Process For The Preparation Of N,N'-Disubstituted Oxabispidines - There is provided a process for the preparation of a sulfonic acid salt of formula I, or a solvate thereof, which process comprises hydrogenating a sulfonic acid salt of formula II, or a solvate thereof; in the presence of a solvent system consisting essentially of water, a C09-02-2010
20110130395P13K ISOFORM SELECTIVE INHIBITORS - 2-Morpholin-4-yl-9H-purine and 5-Morpholin-4-yl-3H-[1,2,3]triazolo[4,5-d]pyrimidine derivatives, especially those substituted by 6-heteroaryl, are unexpected PI3 kinase isoform selective inhibitors with good drug properties and are useful in treating disorders related to abnormal PI3K activities such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.06-02-2011
20090163486Novel 2-arylthiazole-4-carboxamide derivatives, their preparation and use as pharmaceuticals - The present invention relates to 2-arylthiazole-4-carboxamide derivatives of the formula (I), the use thereof as medicament for the treatment of various disorders, and processes for the preparation thereof06-25-2009
20120245163TRPV1 Antagonists - Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates, or combinations thereof,09-27-2012
20090156590Vanilloid Receptor Ligands, Pharmaceutical Compositions Containing Them, Process for Making Them, and Use Thereof for Treating Pain and Other Conditions - Vanilloid receptor ligand compounds corresponding to formula I:06-18-2009
20090111802CYCLOCARBAMATE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS - This invention provides compounds of Formula (I):04-30-2009
20090111801SUBSTITUTED PYRAZINONE DERIVATIVES FOR USE AS A MEDICINE - The present invention concerns substituted pyrazinone derivatives according to the general Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 04-30-2009
20100298311TETRAHYDRONAPHTHALENE DERIVATES, PROCESS FOR PREPARING THEM AND THEIR USE AS ANTIINFLAMMATORY AGENTS - The invention relates to multiply substituted tetrahydronaphthalene derivatives of the formula (Ia)11-25-2010
20130131055FUROPYRIDINYL-SUBSTITUTED 1,4-DIHYDROPYRIDINE DERIVATIVES AND METHODS OF USE THEREOF - This invention relates to novel 4-(furo[3,2-c]pyridin-2-yl)-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.05-23-2013
20130137684HAEMATOPOIETIC-PROSTAGLANDIN D2 SYNTHASE INHIBITORS - The present invention generally relates to compounds that inhibit haematopoietic-prostaglandin D05-30-2013
20090036438FIVE-MEMBERED HETEROCYCLES USEFUL AS SERINE PROTEASE INHIBITORS - The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V):02-05-2009
201102129523,4-DIHYDROBENZOXAZINE COMPOUNDS AND INHIBITORS OF VANILLOID RECEPTOR SUBTYPE 1 (VRI) ACTIVITY - A 3,4-dihydrobenzoxazine compound of the present invention is represented by the following formula [1] (wherein X is a nitrogen atom or CR09-01-2011
20100331323SYNTHESIS AND REGIOSELECTIVE SUBSTITUTION OF 6-HALO- AND 6-ALKOXY NICOTINE DERIVATIVES - The present invention provides active compounds for modulating nicotinic acetylcholine receptors and methods of making the same. The methods of preparing the active compounds utilize different intermediate compounds.12-30-2010
20100331322SUBSTITUTED PIPERIDINES AS RENIN INHIBITORS - The present invention relates to compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which R has the meaning explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.12-30-2010
201100094012-AZA-BICYCLO[2.2.1]HEPTANE DERIVATIVES - The invention relates to novel 2-aza-bicyclo[2.2.1]heptane derivatives of formula (I),01-13-2011
20110009400BICYCLIC DERIVATIVES OF AZABICYCLIC CARBOXAMIDES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The disclosure relates to compounds of formula (I):01-13-2011
20110028468COMPOUNDS HAVING NPY Y5 RECEPTOR ANTAGONISTIC ACTIVITY - This invention provides a compound of the formula (I):02-03-2011
20110028464INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION - Compounds of formula I: wherein c, R02-03-2011
20100160304AROMATIC SULFONE COMPOUND AS ALDOSTERONE RECEPTOR MODULATOR - The present invention provides a compound represented by the following formula (I):06-24-2010
20090062268NOVEL INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) - A compound having the structure set forth in Formula (I):03-05-2009
20100286136DIHYDRONAPHTHYRIDINYL AND RELATED COMPOUNDS FOR USE IN TREATING OPHTHALMOLOGICAL DISORDERS - The invention provides methods of using dihydronaphthyridinyl and related compounds to treat opthalmological disorders, such as, wet age-related macular degeneration, diabetic retinopathy, and high myopia. Pharmaceutical compositions and methods of synthesizing the dihydronaphthyridinyl and related compounds are provided.11-11-2010
20110086849 NOVEL BENZOXAZINE BENZIMIDAZOLE DERIVATIVE, A PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, AND AUSE THEREOF - The present invention relates to a novel benzoxazine benzimidazole derivative of formula (1) as an antagonist against a vanilloid receptor-1, a pharmaceutical composition comprising the same as an active ingredient, and a use thereof. The benzoxazine benzimidazole derivative of the present invention may be useful for preventing or treating a disease associated with antagonistic activity of vanilloid receptor-1:04-14-2011
20100216783COMPOSITIONS, SYNTHESIS, AND METHODS OF UTILIZING ARYLPIPERAZINE DERIVATIVES - The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression.08-26-2010
20090312313COMPOUND HAVING TGFBETA INHIBITORY ACTIVITY AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - The present invention provides compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof:12-17-2009
20110098288SULFONAMIDES AS ZAP-70 INHIBITORS - The invention relates to compounds of formula (I)04-28-2011
20110245241HIV Integrase Inhibitors - The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.10-06-2011
20090247512MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS - Inhibitors of HCV replication of formula (I)10-01-2009
20090312312Heterobicyclic Metalloprotease Inhibitors - The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors.12-17-2009
20100069379Bicyclic androgen and progesterone receptor modulator compounds and methods - The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.03-18-2010
201000630425-SUBSTITUTED BENZOXAZINES - The present invention is concerned with 5-substituted benzoxazine derivatives of formula (I)03-11-2010
20100056508AMINE DERIVATIVES AND THEIR USE IN BETA-2-ADRENORECEPTOR MEDIATED DISEASES - The present invention provides compounds of formula (I), wherein k, Ar, R03-04-2010
20100056507PHENYL DERIVATIVES AND THEIR USE AS A MEDICAMENT - The present invention relates to new phenylic derivatives exhibiting a good affinity for certain sub-types of cannabinoid receptors, in particular the CB2 receptors. These derivatives are of particular interest in a method for treating pathological conditions and diseases in which one or more cannabinoid receptors are involved. The invention also relates to pharmaceutical compositions containing said new phenylic derivatives and to methods for the preparation and use thereof.03-04-2010
20100056509HETEROARYL SULFONAMIDES AND CCR2 - Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.03-04-2010
20090215763SUBSTITUTED BENZOXAZINONES - The present invention provides substituted oxazinone compounds, such as substituted benzoxazinones, which exhibit potent renin inhibition activities.08-27-2009
20110251190SPIRO-TETRACYCLIC RING COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and other related conditions. In one embodiment, the compounds have a general Formula I10-13-2011
20110077241HETEROARYL-SUBSTITUTED 1,3-DIHYDROINDOL-2-ONE DERIVATIVES AND MEDICAMENTS CONTAINING THEM - The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R03-31-2011
20120149698NOUVEL COMPOUNDS - The present invention relates to new CGRP-antagonists of general formulae Ia and Ib06-14-2012
20110105491THIAZOLIDINE COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS - The invention relates to thiazolidine derivatives of the formula (I) wherein A, B, and R05-05-2011
20110077242DIAMINOPYRIMIDINES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds and methods for treating diseases mediated by a P2X03-31-2011
20100160307METHOD FOR CONTROLLING PARTICULAR INSECT PESTS BY APPLYING ANTHRANILAMIDE COMPOUNDS - This invention pertains to a method for controlling lepidopteran, homopteran, hemipteran, thysanopteran and coleopteran insect pests comprising contacting the insects or their environment with an arthropodicidally effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof06-24-2010
20120202805PI3K (delta) SELECTIVE INHIBITORS - Novel PI3K, especially PI3K delta isoform, selective inhibitors are disclosed. The compounds are useful in treating disorders related to abnormal PI3K or PI3Kδ activities such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.08-09-2012
20120202803N-[3-(5-AMINO-3,3A,7,7A-TETRAHYDRO-1H-2,4-DIOXA-6-AZA-INDEN-7-YL)-PHENYL]-- AMIDES AS BACE1 AND/OR BACE2 INHIBITORS - The present invention relates to N-[3-(5-Amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides of formula I08-09-2012
20110251189HYPOXIA TARGETED COMPOUNDS FOR CANCER DIAGNOSIS AND THERAPY - The present invention generally relates to oxazine derivative compounds and related compositions and methods for inducing hypoxic tumor cell death, treating cancer and locating a hypoxic tumor in a subject.10-13-2011
20110039840SPIROCYCLIC DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS - This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R02-17-2011
20110039838PYRROLOTRIAZINE COMPOUNDS AS KINASE INHIBITORS - The present invention provides compounds of formula I02-17-2011
20080249086Novel Oxabispidine Compounds And Their Use In The Treatment Of Cardiac Arrhythmias - There is provided compounds of formula I, wherein R10-09-2008
20100280025EQUILIBRATIVE NUCLEOSIDE TRANSPORTER ENT1 INHIBITORS - The present invention is related to novel compounds of formula (I) having equilibrative nucleoside transporter ENT1 inhibiting properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the inhibition of ENT1 receptors in animals, in particular humans.11-04-2010
20100261719CHEMICAL COMPOUNDS - In one aspect, the present invention relates to compounds of Formula (I) and to pharmaceutically acceptable salts thereof, wherein: n is 1 to 4; and R10-14-2010
20110212953Polymorph Form II of Tanaproget - Tanaproget polymorph Form II, processes for preparing tanaproget polymorph Form II, pharmaceutical compositions including tanaproget polymorph Form II, micronized tanaproget polymorph Form II, and processes for converting Form II to tanaproget Form I are provided. Also provided are methods of contraception, hormone replacement therapy, stimulation of food intake and treating or preventing uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, or carcinomas and adenocarcinomas comprising administering polymorph Form II to a mammalian subject.09-01-2011
20110212951HUMAN PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE - The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-β) inhibitors, and to methods for regulating angiogenesis.09-01-2011
20100069378SUBSTITUTED INDANYL SULFONAMIDE COMPOUNDS, THEIR PREPARATION AND USE AS MEDICAMENTS - The present invention refers to new indanyl sulphonamide compounds with general formula (I), as well as to their preparation procedure, their application as medicine and the pharmaceuticals composition which they are made up of. The new compounds of formula (I) show affinity for 5-HT03-18-2010
20120202804FUSED AMINODIHYDRO-OXAZINE DERIVATIVES - A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C08-09-2012
20120302560Novel Benzoic Pyrrolopyridine Derivatives - The present invention relates to compounds of formula:11-29-2012
20090312314HETEROAROMATIC MONOAMIDES AS OREXININ RECEPTOR ANTAGONISTS - The present invention is concerned with novel sulfonamides of formula12-17-2009
20090170840NS1 protein inhibitors - The present invention generally relates to compounds to treat viral infections and methods of their use. In particular, compounds of the present invention inhibit the activity of NS1 protein, thereby mitigating viral infection and, in particular, influenza virus infection. Accordingly, NS1 protein inhibitors and methods of treatment that employ such inhibitors are contemplated by the present invention.07-02-2009
201102129504,4-DISUBSTITUTED PIPERIDINES - The application relates to 4,4-disubstituted piperidines of the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R09-01-2011
200803122224-Benzyledene-Piperidin Derivatives - The present invention relates to new 4-benzylidene-piperidin derivatives of formula (I), useful as NMDA, in a particular NR2B subunit containing receptor antagonists and analgesica.12-18-2008
20090082344Methods and systems for treating disease - Methods and systems described herein are applicable to the identification of pathogens, pathogenic variants and applicable treatments or remedies. In some embodiments, the pathogen or pathogens bears a causal relationship to a disease state.03-26-2009
20090054421Pyrimidothiophene Compounds Having HSP90 Inhibitory Activity - Compounds of formula (I) are HSP90 inhibitors, of utility in the treatment of, for example, cancers: wherein R02-26-2009
20080242662Organic Compounds - The invention relates to substituted 3,4- or higher substituted piperazine compounds, the use thereof for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; pharmaceutical formulations or products comprising said compounds, and/or a method of treatment comprising administering said compounds, a method for the manufacture of said compounds as well as novel intermediates, starting materials and/or partial steps for their synthesis. The compounds are especially of the formula I,10-02-2008
20110257168DERIVATIVES OF OXABISPIDINE AS NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - The present invention relates to compounds of formula (I) that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).10-20-2011
20110257169NOVEL HYDROXY-6-HETEROARYLPHENANTHRIDINES AND THEIR USE AS PDE4 INHIBITORS - Compounds of the formula Ia*****10-20-2011
20080306059Pyrimido [4,5-B] -Oxazines For Use as Dgat Inhibitors - Compounds of formula (I) or salts thereof, wherein A, and R12-11-2008
20080306058Combinations Comprising a Vegf Receptor Inhibitor - A composition comprising a VEGF receptor inhibitor and a penetration enhancer and uses thereof.12-11-2008
20110288084[4-( 1-AMINO-ETHYL) - CYCLOHEXYL ] - METHYL - AMINES AS ANTIBACTERIALS - The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof, to their use in the treatment of bacterial infections, and to their methods of preparation.11-24-2011
20110288083METHOD OF TREATING CANCER BY INHIBITION OF PROTEIN KINASE-LIKE ENDOPLASMIC RETICULUM PROTEIN KINASE - The present invention relates to a method of identifying compounds useful in inhibiting protein kinase-like endoplasmic reticulum protein kinase (PERK). The method comprises providing a first model comprising PERK active domains, where the said active domains are selected from the group consisting of the peptide spanning from amino acid residue Asp144 to amino acid residue Ser191 of SEQ ID NO: 1 and a peptide comprising the amino acid residue at position 7 of SEQ ID NO: 1, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying the compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for inhibiting PERK. The present invention further relates to compounds that can be used for inhibition of PERK, for example human PERK, and methods related to treatment of PERK-mediated diseases.11-24-2011
20110288082METHODS AND COMPOSITIONS FOR INHIBITION OF THE TRANSITIONAL ENDOPLASMIC RETICULUM ATPASE - Compounds of Formulas I-XLIII are identified as direct inhibitors of p97 ATPase or of the degradation of a p97-dependent ubiquitin-proteasome system (UPS) substrate. Methods and compositions are disclosed for inhibiting p97 ATPase and the degradation of a p97-dependent UPS substrate, and for identifying inhibitors thereof11-24-2011
20100311737PYRIMIDO [4,5-B] -OXAZINES FOR USE AS DGAT INHIBITORS - Compounds of formula (I) or salts thereof, wherein A, and R12-09-2010
20100029632BROADSPECTRUM 2-AMINO-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS - The present invention concerns the compounds having the formula02-04-2010
20110053926New Pharmaceutically-Active Compounds for the Treatment of Respiratory Diseases - The present invention relates to the use of the compounds of general formula 103-03-2011
20110053925Hydroxamate-Based Inhibitors of Deacetylases - The present teachings relate to compounds of Formula I:03-03-2011
20110053924SUBSTITUTED PIPERIDINES AS RENIN INHIBITORS - The present invention relates to compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which R has the meaning explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.03-03-2011
20110053923CHEMICAL COMPOUNDS 610 - There is provided pyrimidinyl indole compounds of Formula (I),03-03-2011
20110028466NITROIMIDAZOOXAZINE AND NITROIMIDAZOOXAZOLE ANALOGUES AND THEIR USES - The current invention pertains to nitroimidazooxazine and nitroimidazooxazole analogues, their methods of preparation, and uses of the compounds as treatment for 02-03-2011
20110028462Niacin Receptor Agonists, compositions Containing Such Compounds and Methods of Treatment - A method of treating atherosclerosis and related conditions using compounds of formula I: as well as pharmaceutically acceptable salts and solvates is disclosed. The compounds are useful for treating dyslipidemias, and in particular, reducing serum LDL, VLDL and triglycerides, and raising HDL levels.02-03-2011
20110028467HETEROCYCLIC DERIVATIVES - The present invention relates to heterocyclic derivatives, and more particularly, to novel heterocyclic derivatives useful for the preparation of medicaments for treating diseases related to uric acid.02-03-2011
20100286137Method of Treating Conditions Involving PPAR-Receptors with Indole Compounds - Indole compounds corresponding to the formula (I):11-11-2010
20100286135HETEROCYCLIC AMIDE COMPOUNDS AS PROTEIN KINASE INHIBITORS - The present invention relates to novel heterocyclic amide compounds of Formula I: as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are compositions comprising said compounds, and methods for using said compounds for treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodegenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease.11-11-2010
20100331321Bis-(Sulfonylamino) derivatives for use in therapy - The invention provides compounds of formula (I) wherein R12-30-2010
20110034451TRIAZOLOPYRIDAZINES AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS - The invention relates to novel compounds of formula I02-10-2011
20110263589Method for preventing or treating a glucocorticoid receptor-related disease - A method of preventing or treating a glucocorticoid receptor-related disease involving administering a therapeutically effective amount of a 1,2-dihydroquinoline compound or a pharmaceutically acceptable salt thereof.10-27-2011
20110118249INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION - Compounds of formula (I): wherein c, X, Y, R05-19-2011
20110118250BETA-SECRETASE MODULATORS AND METHODS OF USE - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I05-19-2011
20110118248Heteroaryl sulfonamides and CCR2/CCR9 - Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.05-19-2011
20100298310Thiazole Derivatives as Kinase Inhibitors - A series of thiazole derivatives which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.11-25-2010
20100305115INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION - The present invention relates to compounds of formula (I) wherein c, X, Y, R12-02-2010
20110039839Cyanopyrroles - This invention provides a progesterone receptor antagonist of formula 1 having the structure02-17-2011
20110136798Crystalline Forms Of A Pyridine Derivative - The invention relates to 4-methylbenzenesulfonate salt of the compound of formula (I)06-09-2011
20090176775DERIVATIVES OF UREAS OF PIPERIDINE OR PYRROLIDINE, THEIR PREPARATION AND THEIR THERAPEUTICAL USE - The present invention is related to a compound of formula (I):07-09-2009
20090176773Non-Peptidic Inhibitors of AKAP/PKA Interaction - The invention relates to non-peptidic molecules which modulate, especially inhibit, the interaction of protein kinase A (PKA) and A kinase anchor proteins (AKAP) and to a host or target organism that comprises said non-peptidic compounds or recognition molecules directed to said compounds, such as e.g. antibodies or chelating agents. The invention also relates to a pharmaceutical agent, especially for use in the treatment of diseases that are associated with a disturbance of the cAMP signal path, especially insipid diabetes, hypertonia, pancreatic diabetes, duodenal ulcer, asthma, heart failure, obesity, AIDS, edema, hepatic cirrhosis, schizophrenia and others. The invention also relates to the use of the inventive molecules.07-09-2009
20100190783TRIAZOLONE DERIVATIVES - A Compound represented by the following general formula (1):07-29-2010
20110190284AEROSOL FORMULATIONS FOR THE INHALATION OF BETA-AGONISTS - A pharmaceutical formulation, comprising: 08-04-2011
20110190283Fab I Inhibitors - Compounds of the Formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.08-04-2011
20100029633IMIDAZO[1,2-A]PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS - Compounds of Formula I: in which A, B, R02-04-2010
20100029630REVERSE-TURN MIMETICS AND METHOD RELATING THERETO - Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.02-04-2010
201000296282,4,5-Substituted Piperidines as Renin Inhibitors - SP-P2140 ATE-132—Abstract Novel substituted piperidines of the general formula (I) and (II) with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent.02-04-2010
20100029631CARBOXYLIC ACID COMPOUNDS AND MEDICINAL COMPOSITIONS CONTAINING THE SAME AS THE ACTIVE INGREDIENT - A compound represented by formula (I)02-04-2010
20100022525Arginine Derivatives with NP-I Antagonistic Activity - The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.01-28-2010
20100016296HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.01-21-2010
20100152177COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY - The present disclosure provides compounds having affinity for the 5HT6 receptor which are of the formula (I):06-17-2010
20090075991DEUTERIUM-ENRICHED EFAVIRENZ - The present application describes deuterium-enriched efavirenz, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20120178750Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment - The present invention encompasses compounds of Formula I:07-12-2012
20120040975BRIDGED BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to Bridged Bicyclic Heterocycle Derivatives, compositions comprising a Bridged Bicyclic Heterocycle Derivative, and methods of using the Bridged Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.02-16-2012
20100324036SUBSTITUTED IMIDAZOPYRIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR ANTAGONISTS - The present invention relates to substituted imidazopyridine derivatives as melanocortin-4 receptor (MC-4R) modulators, in particular as melanocortin 4 receptor antagonists. The antagonists are useful for the treatment of disorders and diseases such as cachexia induced by e.g. cancer, chronic kidney disease (CKD) or chronic heart failure (CHF), muscle wasting, anorexia induced by e.g. chemotherapy or radiotherapy, anorexia nervosa, amyotrophic lateral sclerosis (ALS), pain, neuropathic pain, anxiety and depression.12-23-2010
20120208806Hsp90 Inhibitors - The present application provides compounds useful in the inhibition of Hsp90, and hence in the treatment of disease.08-16-2012
20120208805TRIAZOLIUM SALTS AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS - The invention relates to novel compounds of formula I08-16-2012
20110112084Bicyclic androgen and progesterone receptor modulator compounds and methods - The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.05-12-2011
20120040974MIF MODULATORS - The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.02-16-2012
20090054423Niacin receptor agonists, compositions containing such compounds and methods of treatment - The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating dyslipidemias. Pharmaceutical compositions and methods of use are also included.02-26-2009
20090298818PHARMACEUTICAL COMPOUNDS - The invention provides the use of a compound for the manufacture of a medicament for the treatment of pain, wherein the compound is a compound of the formula (VI):12-03-2009
20080280897Aerosol Formulation for Inhalation - The present invention relates to a propellant-free aerosol formulation which contains one or more compounds of general formula 1.11-13-2008
20080275035Nitroimidazole Compounds - The present invention relates to certain nitroimidazole compounds, which have interesting pharmaceutical properties. In particular, the compounds are useful in the treatment and/or prevention of infections such as those caused by 11-06-2008
20090253692CRYSTALLINE FORM OF N-[[4-FLUORO-2-(5-METHYL-1H-1,2,4-TRIAZOL-1-YL)PHENYL]METHYL]-4,6,7,9-TET- RAHYDRO-3-HYDROXY-9,9-DIMETHYL-4-OXO-PYRIMIDO[2,1-C][1,4]OXAZINE-2-CARBOXA- MIDE, SODIUM SALT MONOHYDRATE - Disclosed is a crystalline form of N-[[4-fluoro-2-(5-methyl-1H-1,2,4-triazol-1-yl)phenyl]methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide, sodium salt monohydrate. Also disclosed are at least one pharmaceutical composition comprising at least one crystalline form of N-[[4-fluoro-2-(5-methyl-1H-1,2,4-triazol-1-yl)phenyl]methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide, sodium salt monohydrate, and at least one method of using at least one crystalline form of N-[[4-fluoro-2-(5-methyl-1H-1,2,4-triazol-1-yl)phenyl]methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide, sodium salt monohydrate to treat AIDS or HIV infection.10-08-2009
2011007114617BetaHSD Type 5 Inhibitor - To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17βHSD type 5.03-24-2011
20110071145Raf Modulators And Methods Of Use - The present invention relates to compounds of the Formula I, wherein G, A, X1, X2, X3, Z, E, Y, and X are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Raf. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.03-24-2011
20120004221Antibacterial Compositions - Compounds of formula (I) have antibacterial activity:01-05-2012
20120115860NOVEL DERIVATIVES OF ARYL--METHANONE, THEIR METHOD OF PREPARATION AND THEIR USE AS MEDICINAL PRODUCTS - The present invention concerns compounds of general formula (1) (I) wherein R05-10-2012
20080287429Dissolution of Arterial Cholesterol Plaques by Pharmacologically Induced Elevation of Endogenous Bile Salts - A group of pharmaceutical substances induce elevation of endogenous bile salts and acids via different mechanisms. The elevated circulating bile salts exert a beneficial effect in atherosclerosis by acting both as atherolytic and antiatherogenic agents. The result of the elevated circulating endogenous bile salt is the dissolution of cholesterol/lipidic aggregates of the atherosclerotic plaques.11-20-2008
20120010202POLYMERIZABLE BENZOXAZINE COMPOUNDS WITH INTERFACIAL ACTIVE OR SURFACE ACTIVE PROPERTIES - The invention relates to polymerizable benzoxazine compounds with interfacial active or surface active properties, having at least one polyalkylene oxide structural element, and to a method for producing said compounds. The invention also relates to benzoxazine (co)polymers comprising at least one of said benzoxazine compounds in the polymerized form.01-12-2012
20090298817ANTI-AMNESIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM - The present invention relates to the use of at least one compound of formula (I) as follows:12-03-2009
20110166132Gamma Secretase Modulators - The present invention provides compounds that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.07-07-2011
20120115861AMINOPYRIDINE DERIVATIVES FOR TREATING TUMORS AND INFLAMMATORY DISEASES - Compounds of the formula (I), in which R05-10-2012
20100063041NOVEL PHENYLPROPIONIC ACID DERIVATIVES AS PEROXISOME PROLIFERATOR-ACTIVATED GAMMA RECEPTOR MODULATORS, METHOD OF THE SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - The present invention provides a novel phenylpropionic acid derivative and a PPAR-γ modulator comprising the same as an active ingredient. The phenylpropionic acid derivative of the present invention has modulatory action on function of PPAR-γ and then exhibits hypoglycemic, hypolipidemic and insulin resistance-reducing effects on PPAR-mediated diseases or disorders. Therefore, the present invention is prophylactically or therapeutically effective for diabetes and metabolic diseases.03-11-2010
20090137578ENANTIOMERICALLY PURE BETA AGONISTS, PROCESS FOR THE MANUFACTURE THEREOF AND USE THEREOF AS MEDICAMENTS - Enantiomerically pure compounds of general formula 105-28-2009
20120252800BICYCLIC THIAZOLES AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS - The present invention relates to novel bicyclic thiazoles which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”) and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved.10-04-2012
20120022057BICYCLIC COMPOUNDS AS INHIBITORS OF DIACYGLYCEROL ACYLTRANSFERASE - The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below (I).01-26-2012
201200220584,5-DIHYDRO-1H-PYRAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USES - Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.01-26-2012
20120122862ARGININE DERIVATIVES WITH NP-I ANTAGONISTIC ACTIVITY - The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.05-17-2012
20120122861BICYCLIC AMIDE DERIVATIVES FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES - This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as conditions such as stroke-induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, among others. In a particular aspect, the invention relates to bicyclic amide compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.05-17-2012
20120122860SOLID FORMS OF SULFONAMIDES AND AMINO ACIDS - Solid forms of phenyl sulfonamide compounds of formula (I) active on protein kinases, including Raf protein kinases, are described, as well as methods of using such solid forms to treat diseases and conditions associated with activity of protein kinases, e.g. Raf protein kinases, including pain, polycystic kidney disease, melanoma and colorectal cancer.05-17-2012
20100280023THIAZOLE DERIVATIVES - It is intended to provide an adenosine A11-04-2010
20100280024RENIN INHIBITORS - The present invention relates to renin inhibitors of formula (I), their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (I), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.11-04-2010
20090137576Novel Piperidine Derivative - Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I)05-28-2009
20110028463AMIDE COMPOUNDS - [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. 02-03-2011
20110009397TRIAZONE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.01-13-2011
20120157450Anhydrate Forms Of A Pyridine Derivative - The invention relates to the compound of formula (I) in a crystalline anhydrate form,06-21-2012
20110092495COMPOUNDS FOR THE TREATMENT OF MULTI-DRUG RESISTANT BACTERIAL INFECTIONS - The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans.04-21-2011
20120071471NOVEL BENZOXAZINONE DERIVATIVES USEFUL FOR THE TREATMENT OF CNS DISORDERS - The present invention encompasses novel 1,4-dihydro-3,1-benzoxazin-2-one derivatives, which are surprisingly found to be efficacious in animal models of CNS disorders and, as such, are valuable candidates for the prevention or treatment of CNS (Central Nervous System) diseases or disorders.03-22-2012
20100197678Glucocorticoid Mimetics, Methods of Making Them, Pharmaceutical Compositions and Uses Thereof - Compounds of Formula (IA)08-05-2010
20110065696IMIDAZOYL PYRIDINE COMPOUNDS AND SALTS THEREOF - A compound represented by the formula (I):03-17-2011
201100656972-OXY-BENZOXAZINONE DERIVATIVES FOR THE TREATMENT OF OBESITY - The use of a compound comprising formula (I):03-17-2011
201101054902,3-DIHYDRO-1H-ISOINDOL-1-IMINE DERIVATIVES USEFUL AS THROMBIN PAR-1 RECEPTOR ANTAGONIST - The present invention is directed to novel 2,3-dihydro-1H-isoindol-1-imine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the thrombin PAR-1 receptor antagonists.05-05-2011
20100093717TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of treating or inhibiting angiogenesis in a subject in need thereof and methods for blocking, occluding, or otherwise disrupting blood flow in neo vasculature, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.04-15-2010
20120316160XINAFOATE SALT OF N4-(2,2-DIFLUORO-4H-BENZO[1,4]OXAZIN-3-ONE)-6-YL]-5-FLUORO-N2-[3-(METHYLA- MINOCARBONYLMETHYLENEOXY)PHENYL]2,4-PYRIMIDINEDIAMINE - The present invention relates to the xinafoate salt of N4-[(2,2-difluoro-4H-benzo[1,4]oxazin-3-one)-6-yl]-5-fluoro-N2-[3-(methylaminocarbonylmethyleneoxy)phenyl]-2,4-pyrimidinediamine. This compound is a suitable drug substance and is useful in the treatment of conditions including asthma.12-13-2012
20120316159BICYCLIC RING SYSTEM SUBSTITUTED SULFONAMIDE FUNCTIONALISED PHENOLS AS MEDICAMENTS - This invention relates to bicyclic ring system substituted sulfonamide functionalized phenols of general formula 1,12-13-2012
20120122859METHODS OF USING DIAMINOPYRIMIDINE AS P2X3 AND P2X2/3 RECEPTOR MODULATORS FOR TREATMENT OF RESPIRATORY AND GASTROINTESTINAL DISEASES - Methods for treating respiratory and gastrointestinal diseases mediated by a P2X05-17-2012
20120129847COMPOSITIONS AND METHODS FOR TREATING OCULAR EDEMA, NEOVASCULARIZATION AND RELATED DISEASES - Disclosed are methods for the treatment of diseases or conditions of the eye, especially retinopathies, ocular edema and ocular neovascularization. Non-limiting examples of these diseases or conditions include diabetic macular edema, age-related macular degeneration (wet form), choroidal neovascularization, diabetic retinopathy, retinal vein occlusion (central or branch), ocular trauma, surgery induced edema, surgery induced neovascularization, cystoid macular edema, ocular ischemia, uveitis, and the like.05-24-2012
20120129848Benzo [E] [1,3] Oxazin-4-One Derivatives as Phosphoinositide 3-Kinase Inhibitors - Compounds of formula (I): wherein: W is O, N—H, N-alkyl, N-alkenyl, N-alkynyl, N-aryl, N-heteroaryl or S; each X is independently CH or N; R05-24-2012
20120165324THERAPEUTIC COMPOSITIONS AND RELATED METHODS OF USE - Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.06-28-2012
20120232073FUSED BICYCLIC PYRIMIDINE DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to Fused Bicyclic Pyrimidine Derivatives, compositions comprising a Fused Bicyclic Pyrimidine Derivative, and methods of using the Fused Bicyclic Pyrimidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) in a patient.09-13-2012
20120232070Use of Indole Derivatives as Nurr-1 Activators for the Application Thereof as a Medicament for the Treatment of Parkinson's Disease - Compounds derived from indole, notably useful in therapeutics, selected from: 09-13-2012
20120232069PROCESS FOR PREPARING EFAVIRENZ POLYMORPH - The present invention relates to a process for the preparation of crystalline non-hygroscopic form H1 of efavirenz, and pharmaceutical compositions containing it. In accordance with the present invention efavirenz was dissolved in acetone at 25° C.-30° C., the solution was slowly added to water at 0° C.-5° C., the separated solid was filtered, washed with mixture of acetone and water and dried at 25° C.-35° C. under below 65% relative humidity for 18 hours to give crystalline non-hygroscopic efavirenz form H1.09-13-2012
20090192148Organic Compounds - The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis.07-30-2009
20090176774Compounds and methods of use - Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.07-09-2009
20110207726Inhibitors of Human Cathepsin L, Cathepsin B, and Cathepsin S - The present invention is directed to novel protease inhibitors that are specific for cathepsin L, cathepsin B, and cathepsin S. Accordingly, the present invention encompasses compositions and methods for treating and preventing diseases and disorders associated with cathepsin L, cathepsin B, or cathepsin S function or activity.08-25-2011
200903259495 HT RECEPTOR MEDIATED NEUROGENESIS - The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a 5HTR agent, optionally in combination with one or more other neurogenic agents, to stimulate or activate the formation of new nerve cells.12-31-2009
20100048547PI 3-KINASE INHIBITORS AND METHODS OF THEIR USE - Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases, including proliferative diseases, inflammatory and obstructive airways diseases, allergic conditions, autoimmune and cardiovascular diseases.02-25-2010
20120232072IMIDAZOPYRIDINE DERIVATIVES - The present invention relates to compounds of formula (I),09-13-2012
20100009984AEROSOL FORMULATIONS FOR THE INHALATION OF BETA-AGONISTS - A pharmaceutical formulation, comprising: 01-14-2010
201000099835 HT RECEPTOR MEDIATED NEUROGENESIS - The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a 5HTR agent, in combination with one or more other neurogenic agents, or anti-astrogenic agent, to stimulate or activate the formation of new nerve cells.01-14-2010
20090069312Potassium Channel Inhibitors - The present invention relates to dipyridin-3-ylmethoxy compounds and derivatives thereof having the structure I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.03-12-2009
20100292229TRYPHOSTIN-ANALOGS FOR THE TREATMENT OF CELL PROLIFERATIVE DISEASES - The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. In general aspects, compounds of the present invention are tyrphostin-like in structure. Compounds of the present invention, in certain embodiments, display significant potency by causing, for example, inhibition of Stat3 activation, reduction in c-myc protein levels and/or induction of apoptosis in tumor cells. In general aspects, compounds of the present invention induce one or more of these activities at nanomolar concentrations and typically function through a unique mechanism involving the induction of stress granules that bind specific signaling molecules and prevent them from participating in signal transduction and oncogenesis.11-18-2010
20100292228SUBSTITUTED OXA-DIAZA-SPIRO-[5.5]-UNDECANONE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS - This invention concerns substituted oxa-diaza-spiro-[5.5]-undecanone derivatives having neurokinin antagonistic activity, in particular an NK11-18-2010
20120220579METHODS OF UTILIZING ARYLPIPERAZINE DERIVATIVES - The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.08-30-2012
20120220578GUM RESIN AS A CARRIER FOR TOPICAL APPLICATION OF PHARMACOLOGICALLY ACTIVE AGENTS - Described are pharmacological compositions comprising a gum resin; a pharmacologically active agent and a topically acceptable volatile solvent for the gum resin and active agent. Also described are methods for the transdermal or transmucosal delivery of a pharmacologically active agent using such compositions.08-30-2012
20120220577GLYCINE B ANTAGONISTS - The invention relates to naphthalene derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders.08-30-2012
20120220576Novel Heterocyclic Derivatives - The invention relates to novel heterocyclic compounds of the formula08-30-2012
20120225867ANDROGEN RECEPTOR MODULATING COMPOUNDS - The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.09-06-2012
20120264748DIAZA-SPIRO[5.5]UNDECANES - The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.10-18-2012
201101246362-AZA-BICYCLO[3.1.0]HEXANE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS - The invention relates to novel 2-aza-bicyclo[3.1.0]hexane derivatives of Formula (I) wherein A, B, n and R05-26-2011
20100240644MORPHOLINE DERIVATIVE - The present invention provides a morpholine derivative of the formula [I];09-23-2010
201202320712,3-DIARYL- OR HETEROARYL-SUBSTITUTED 1,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS - The present invention relates to compounds of formula I09-13-2012
20110003803COMPOSITIONS AND METHODS FOR TREATING OPHTHALMIC, OTIC, OR NASAL INFECTIONS - The present invention relates to methods for treating an ophthalmic, otic, or nasal infection comprising treating the infected tissue with a composition comprising finafloxacin or a finafloxacin derivative. The present invention also relates to antimicrobial compositions comprising finafloxacin or a finafloxacin derivative. The compositions are suitable for the treatment of ophthalmic, otic, or nasal infections.01-06-2011
20110046126Use of 2,4-Pyrimidinediamines For the Treatment of Atherosclerosis - Novel methods and compositions for the prevention and treatment of all forms of atherosclerosis with 2,4-pyrimidinediamine compounds are described. Also disclosed is the coating of prosthetic devices, such as stents, with the compounds of the invention for the prevention and/or treatment of restenosis.02-24-2011
20110046125METHOD FOR TREATING INFECTIONS - The present invention relates to compounds for treating or preventing infection that inhibit the activity of Hsp90.02-24-2011
20120270867NOVEL (6-OXO-1,6-DIHYDROPYRIMIDIN-2-YL)AMIDE DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF AS AKT(PKB) PHOSPHORYLATION INHIBITORS - The invention relates to the novel materials of formula (I), where: R1 is an optionally substituted aryl or heteroaryl; R is an H or, when formed with R1, a 5- or 6-member ring fused with an aryl or heretoaryl group optionally containing one or more of O, S, N, NH, and Nalk, being optionally substituted; R2 and R3 are, independently, an H, Hal, or alkyl optionally substituted by one or more Hal; R4 is H; and R5 is an H or alkyl optionally substituted by one or more halogen atoms. Said materials being in any isomeric form and the salts thereof, and are intended for drugs, particularly AKT(PKB) phosphorylation inhibitors.10-25-2012
201002278573,4-DIHYDRO-2H-BENZO[1,4]OXAZINE AND THIAZINE DERIVATIVES AS CETP INHIBITORS - The invention is directed to compounds of Formula (I) described herein useful as CETP inhibitors, compositions containing them, and methods of using them.09-09-2010
20110237577BICYCLIC PEPTIDOMIMETIC INHIBITORS OF ASPARTYL-PROTEASES FOR THE TREATMENT OF INFECTIOUS DISEASES - The present invention refers to 3-aza-bicyclo[3.2.1]octane derivatives of general formula (I) their preparation, use and pharmaceutical compositions useful in the treatment of pathologies associated with microbial pathogens expressing aspartyl-protease activity.09-29-2011
20100249122Kinase Inhibitors for Preventing or Treating Pathogen Infection and Method of Use Thereof - The present invention provides compositions and methods of use thereof to prevent and/or treat pathogenic infection. In particular, the present invention provides the use of kinase inhibitors to inhibit kinases that involve in pathogen-host cell interactions that are associated with or cause pathogenic infections, therefore, to effectively prevent and/or treat pathogenic infections with far less likely to engender resistance as compared to conventional antibiotics and anti-viral drugs. The present invention further provides the use of kinase inhibitors for the treatment of acute pathogenic infections for a short period of time to avoid toxicities that may caused by long term use of these kinase inhibitors.09-30-2010
20100234368CONDENSED RING COMPOUND AND USE THEREOF - The present invention relates to a compound of formula (I)09-16-2010
20120277223INHIBITORS OF DIACYLGLYCEROL O-ACYLTRANSFERASE TYPE 1 ENZYME - The present invention relates to compounds of formula (I):11-01-2012
20110263590Antibacterial Compositions - Compounds of formula (I) have antibacterial activity:10-27-2011
20120329791Substituted Imidazopyridinyl-Aminopyridine Compounds - The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.12-27-2012
20100204218FUSED BICYCLIC COMPOUND - The present invention provides a novel fused bicyclic compound having an affinity to a receptor of mineral corticoid (MR), shown by the formula [I]:08-12-2010
20110319403BICYCLIC COMPOUNDS AS INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE - The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below: formula (I).12-29-2011
20110319402AEROSOL FORMULATION FOR THE INHALATION OF BETA AGONISTS - The present invention relates to a propellant-free aerosol formulation which [contains] one or more compounds of general formula (1) wherein the groups R12-29-2011
20090298819Compositions, Synthesis, And Methods Of Using Piperazine Based Antipsychotic Agents - The present invention provides novel piperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression.12-03-2009
20100168094MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators.07-01-2010
20100168093SUBSTITUTED 3-AMINO-4 -HYDROXY PYRROLIDINES COMPOUNDS, THEIR PREPARATION AND USE AS MEDICAMENTS - The present invention relates to substituted pyrrolidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animal.07-01-2010
20130012504BI-FUNCTIONAL QUINOLINE ANALOGS - Provided are compounds of Formula I:01-10-2013
20100173903Bicyclic amide derivatives for the treatmet of respiratory disorders - This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of disorders of respiration such as overdose of an alcohol, an opiate, an opioid, a barbiturate, an anesthetic, or a nerve toxin. In a particular aspect, the invention relates to bicyclic amide compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.07-08-2010
20100173902Bicyclic amide derivatives for enhancing glutamatergic synaptic responses - This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as conditions such as stroke-induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, obesity hypoventilation syndrome, sudden infant death syndrome, Rett syndrome, spinal cord injury, traumatic brain injury, Cheney-Stokes respiration, Ondines curse, Prader-Willi's syndrome and drowning. In a particular aspect, the invention relates to bicyclic amide compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.07-08-2010
20100173901Substituted Heterocyclic Compounds - The present invention relates to substituted heterocyclic compounds of Formula I:07-08-2010
20130018050BI-FUNCTIONAL PYRAZOLOPYRIDINE COMPOUNDS - This invention provides compounds of the formula:01-17-2013
20130018049Azaindole Compounds and Methods for Treating HIV - Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).01-17-2013
20130023529Methods Involving Aldose Reductase Inhibitors - Embodiments of the invention include methods and compositions involving aldose reductase inhibitors for the treatment of inflammation, including uveitis and asthma.01-24-2013
20080255109Non-peptide GnRH antagonists - Compounds according to general formula 1, wherein A10-16-2008
20080255108NOVEL THIOPHENE SULFOXIMINES, COMPOSITIONS THEREOF, AND METHODS OF TREATING COMPLEMENT-MEDIATED DISEASES AND CONDITIONS - Disclosed are compounds for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade. Said compounds are of Formula I10-16-2008
201301723352,3-DIARYL- OR HETEROARYL-SUBSTITUTED 1,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS - The present invention relates to compounds of formula I07-04-2013
20100087428Novel Potassium Channel Blockers - The present invention provides a compound of formula (I)04-08-2010
20080227776INHIBITORS OF HEMEPROTEIN-CATALYZED LIPID PEROXIDATION - Methods and compounds for the treatment or prevention of oxidative damage in a mammalian subject. The treatment and/or prevention may be on inhibiting heme-induced lipid peroxidation. Also discloses are methods and compounds for treating or preventing isoprostane-mediated tissue damage.09-18-2008
20130172334TRPV1 ANTAGONISTS - Disclosed herein are compounds of formula (I):07-04-2013
20110263588TRICYCLIC COMPOUNDS AS GLUTAMATE RECEPTOR MODULATORS - The present invention relates to compounds that may be negative allosteric modulators of metabotropic receptors-subtype 5, and methods of making and using same.10-27-2011
20080221095Metalloprotease inhibitors containing a heterocyclic moiety - The present invention relates generally to pharmaceutical agents containing a heterocyclic moiety, and in particular, to heterocyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterocyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds with a squaramide or benzoxazinone moiety, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.09-11-2008
20080221094Metalloprotease inhibitors containing a squaramide moiety - The present invention relates generally to pharmaceutical agents containing a heterocyclic moiety, and in particular, to heterocyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterocyclic MMP-13 inhibiting compounds with a squaramide moiety, that exhibit an increased potency and selectivity in relation to currently known MMP-13 inhibitors.09-11-2008
20080221093Metalloprotease inhibitors containing a heterocyclic moiety - The present invention relates generally to pharmaceutical agents containing a heterocyclic moiety, and in particular, to heterocyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterocyclic MMP-13 inhibiting compounds with a benzoxazinone moiety, that exhibit an increased potency and selectivity in relation to currently known MMP-13 inhibitors.09-11-2008
20080221092Heterobicyclic metalloprotease inhibitors - The present invention relates generally to amide containing heterobicyclic containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-3 and/or MMP-13 inhibiting compounds that exhibit an increased potency and selectivity in relation to currently known MMP-13 and MMP-3 inhibitors.09-11-2008
20130172333FORMULATION AND DOSING OF HSP90 INHIBITORY COMPOUNDS - Provided is a pharmaceutical composition comprising a pharmaceutically acceptable organic solvent, a pharmaceutically acceptable surfactant, and a compound according to the following formula: wherein the variables are defined herein. Optionally, the pharmaceutical composition further comprises a co-solvent. Also provided is a method of using the pharmaceutical composition disclosed herein for the treatment of a patient in need thereof.07-04-2013
20130096111Methods Involving Aldose Reductase Inhibitors - Embodiments of the invention include methods and compositions involving aldose reductase inhibitors for the treatment of inflammation, including uveitis and asthma.04-18-2013
201301162468-FLUOROPHTHALAZIN-1(2H)-ONE COMPOUNDS - 8-Fluorophthalazin-1(2h)-one compounds of Formula II where one or two of X05-09-2013
20130116245ALKYLATED PIPERAZINE COMPOUNDS - Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.05-09-2013
20130102596METHOD AND DEVICE FOR ADMINISTERING XINAFOATE SALT OF N4-(2,2-DIFLUORO-4H-BENZO [1,4]OXAZIN-3-ONE)-6-YL]-5-FLUORO-N2-[3- (METHYLAMINOCARBONYLMETHYLENEOXY) PHENYL]2,4-PYRIMIDINEDIAMINE - Disclosed embodiments concern a device for administering a xinafoate salt of N4-[(2,2-difluoro-4H-benzo[1,4]oxazin-3-one)-6-yl]-5-fluoro-N2-[3-(methylaminocarbonylmethyleneoxy)phenyl]-2,4-pyrimidinediamine, or compositions thereof, and a method for making and using the device. Particular disclosed embodiments concern formulating the xinafoate salt for administration via the device.04-25-2013
20130102595TREATMENT OF CANCERS HAVING K-RAS MUTATIONS - The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.04-25-2013
20130123250SPIRO (PIPERIDINE-4,2'-PYRROLIDINE)-1-(3,5-TRIFLUOROMETHYLPHENYL) METHYLCARBOXAMIDES AS NK1 TACHIKYNIN RECEPTOR ANTAGONISTS - Compounds of formula (I) or pharmaceutically acceptable salts thereof05-16-2013
20130158021AMINO ACID-, PEPTIDE-AND POLYPEPTIDE-LIPIDS, ISOMERS, COMPOSITIONS, AND USES THEREOF - Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein:06-20-2013
200802004574-Cyclopropyl-1,2,3,-Thiadiazole Compound, Agrohorticultural Plant Disease Controlling Agent And Method Of Using The Same - The present invention relates to 1,2,3 -thiadiazole compounds represented by formula (I):08-21-2008
20090221567MUSCARINIC RECEPTOR AGONISTS, COMPOSITIONS, METHODS OF TREATMENT THEREOF, AND PROCESSES FOR PREPARATION THEREOF 177 - Compounds of Formula I, or pharmaceutically acceptable salts thereof:09-03-2009
20110275624INDOLE AND BENZOMORPHOLINE DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel compounds, in particular novel indole and benzomorpholine derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.11-10-2011
20110275623BI-FUNCTIONAL PYRAZOLOPYRIDINE COMPOUNDS - This invention provides compounds of the formula:11-10-2011
20110275622BI-FUNCTIONAL QUINOLINE ANALOGS - Provided are compounds of Formula I:11-10-2011
201102375762-AMINOPYRIMIDIN-4-ONE AND 2-AMINOPYRIDINE DERIVATIVES BOTH HAVING BACE1-INHIBITING ACTIVITY - The present invention provides a compound which has an effect of inhibiting amyloid-β production and is useful as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-β proteins. The present invention relates to a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof:09-29-2011
20130150355NOVEL COMPOUNDS - This invention relates to compounds of formula I06-13-2013
20130150354NEW SELECTIVE CCR2 ANTAGONISTS - The present invention relates to novel and selective antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD as well as pain.06-13-2013
20130150356Acyl Piperazine Derivatives as TTX-S Blockers - The present invention relates to acyl piperazine derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.06-13-2013
201003176571H-IMIDAZO[4,5-c]QUINOLINONE DERIVATIVES - The invention relates to the use of 1H-imidazo[4,5-c]quinolinone derivatives and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c]quinolinone derivatives for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H-imidazo[4,5-c]quinolinone derivatives to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c]quinolinone derivative, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1H-imidazo[4,5-c]quinolinone derivatives; and a process for the preparation of the novel 1H-imidazo[4,5-c]quinolinone derivatives.12-16-2010
20130123251BENZOXAZINE DERIVATIVES AND USES THEREOF - The present invention provides a compound of the formula:05-16-2013
20110312954MINERALOCORTICOID RECEPTOR ANTAGONIST AND METHODS OF USE - The present invention provides a compound of the formula: Compound (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising Compound (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly congestive heart failure, hypertension, diabetic nephropathy, or chronic kidney disease, comprising administering Compound (I), or a pharmaceutically acceptable salt thereof.12-22-2011
20110312953ANTHRANILIC ACID DERIVATIVES - The present invention relates to novel anthranilic acid derivatives of the general formula (I)12-22-2011
20110312952NOVEL SPIRO COMPOUNDS USEFUL AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Heteroaromatic compounds 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.12-22-2011
20110312951C-Ring Modified Tricyclic Benzonaphthiridinone Protein Kinase Inhibitors and Use Thereof - Disclosed are C-ring modified tricyclic benzonaphthiridinone compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation.12-22-2011
20120015940NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION - The present invention relates to a compound of Formula (I): wherein: n is 0 or 1; X is O or CH01-19-2012
20120028973NITROIMIDAZOOXAZINES AND THEIR USES IN ANTI-TUBERCULAR THERAPY - The present invention relates to novel nitroimidazooxazines, to their preparation, and to their use as drugs for treating 02-02-2012
20130196982MORPHOLINO SUBSTITUTED UREA DERIVATIVES AS MTOR INHIBITORS - The invention relates to compounds of formula (I)08-01-2013
20130196983MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators.08-01-2013
20090042874ANTIDEPRESSANT HETEROARYL DERIVATIVES OF HETEROCYCLE-FUSED BENZODIOXANS - The invention provides compounds of the Formula:02-12-2009
20130203748Inhibitors of Human Immunodeficiency Virus Replication - The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.08-08-2013
20130203750N,N-SUBSTITUTED 3-AMINOPYRROLIDINE COMPOUNDS USEFUL AS MONOAMINES REUPTAKE INHIBITORS - The present invention provides a pyrrolidine compound of General Formula (1)08-08-2013
20130203749Tetrahydroisoquinolines, pharmaceutical compositions containing them, and their use in therapy - The present invention relates to tetrahydroisoquinoline of the formula (I)08-08-2013
20130096110Pyrazolopyridine, Pyrazolopyrazine, Pyrazolopyrimidine, Pyrazolothiophene and Pyrazolothiazole Compounds as MGLUR4 Allosteric Potentiators, Compositions, and Methods of Treating Neurological Dysfunction - Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.04-18-2013
20120094993N-PYRIDIN-3-YL OR N-PYRAZIN-2-YL CARBOXAMIDES - The present invention relates to compounds of formula I,04-19-2012
20120094992POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS - Compounds of the following formula are provided for use in inhibiting Poly (ADP-ribose) Polymerase (PARP):04-19-2012
201200949911, 4-Benzoxazine Compounds and Derivatives Thereof as Therapeutic Drugs for the Treatment of Neurodegenerative Conditions - The present invention includes compositions and methods for inhibiting kinase activity to protect against neurodegeneration including diseases such as Alzheimer's disease, Parkinson's disease, or Huntington's disease, and conditions such as ischemic stroke comprising the step of providing the subject with a therapeutically affective amount of 1,4-benzoxazine compounds and derivatives thereof.04-19-2012
20130210818Novel Heterocyclic Compounds and Uses Thereof - New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.08-15-2013
20130210819QUINAZOLINE DERIVATIVES - Compounds of the formula I in which R, X, L08-15-2013

Patent applications in class Bicyclo ring system having the six-membered hetero ring as one of the cyclos (e.g., 1,4-benzoxazines, etc.)