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Exactly three ring nitrogens in the bicyclo ring system

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

514277000 - Hetero ring is six-membered consisting of one nitrogen and five carbon atoms

514279000 - Polycyclo ring system having the six-membered hetero ring as one of the cyclos

514299000 - Bicyclo ring system having the six-membered hetero ring as one of the cyclos

514300000 - Plural hetero atoms in the bicyclo ring system

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Entries
DocumentTitleDate
20090036482Imidazopyridine-derivatives as inductible no-synthase inhibitors - The compounds of Formula (I)02-05-2009
20090318494PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS - The invention provides a compound of formula (I) or a salt thereof:12-24-2009
20110190336AZABENZIMIDAZOLONES - Compounds are provided having the general structure of formula I:08-04-2011
20110195992NEW COMPOUNDS II - The present invention relates to compounds of formula (I),08-11-2011
20130085156NOVEL 2-PYRIDINECARBOXAMIDE DERIVATIVES - The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I):04-04-2013
20090215818THIOZOLIDINEDIONE DERIVATIVES AS PI3 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using thiozolidinedione derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of thiozolidinedione derivatives.08-27-2009
20120178780RAF KINASE INHIBITORS - Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.07-12-2012
20120178779FUSED HETEROCYCLIC COMPOUND AND USE THEREOF - A fused heterocyclic compound of formula (1):07-12-2012
20090221631IMIDAZOPYRIDINONES - The invention relates to imidazopyridinones, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.09-03-2009
20100076014MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF - Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein (Ia) is heterocycle or heteroaryl; J, Ja, E, F, G, Ma, M, Q, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.03-25-2010
20120208839NEW COMPOUNDS - This invention relates to compounds of formula I08-16-2012
201001057235-PHENYL-6-PYRIDIN-4-YL-1,3-DIHYDRO-2H-IMIDAZO[4,5-b]PYRIDIN-2-ONE DERIVATIVES USEFUL AS A2B ADENOSINE RECEPTOR ANTAGONISTS - The present disclosure relates to compounds of formula (I):04-29-2010
20100087478HIF-1 Inhibitors - HIF-1 inhibitors and methods of their use are provided. In particular, 2,2-dimethylbenzopyran based compounds and methods of their use, for example in the treatment or prevention of hypoxia-related pathologies are provided.04-08-2010
20100093788HETEROCYCLIC BENZIMIDAZOLES AS TRPM8 MODULATORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows:04-15-2010
20120165367AZAINDAZOLES USEFUL AS INHIBITORS OF KINASES - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.06-28-2012
20100069431IMIDAZOPYRIDINE COMPOUNDS - Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of formula (I) wherein the variables are as defined herein.03-18-2010
20090306129SUBSTITUTED PYRAZOLO [3,4-B] PYRIDINES AS PHOSPHODIESTERASE INHIBITORS - The present invention relates to phosphodiesterase (PDE) type IV selective inhibitors. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type IV selective inhibitors are provided. Prepared compounds correspond to structure XIV Formula (XIV).12-10-2009
20090093516TRIAZOLOPYRIDINE 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS - Novel compounds are provided which are 11 -beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds of formula I:04-09-2009
20090076070HETERO COMPOUND - [Problems] To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P03-19-2009
20110021559AMINOPYRIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.01-27-2011
20120115903Substituted Heteroaromatic Carboxamide and Urea Compounds as Vanilloid Receptor Ligands - Substituted heteroaromatic carboxamide and urea compounds corresponding to formula (i)05-10-2012
201201159023H-Imidazo [4, 5-B] Pyridine- 6 -Carboxamides As Anti-Inflammatory Agents - There are provided compounds of formula (I), wherein R05-10-2012
20130165478PYRAZOLOPYRIDINONE DERIVATIVES AS LPA RECEPTOR ANTAGONISTS - The present invention relates to novel pyrazolopyridinone derivatives according to formula (I) and a process of manufacturing thereof. These pyrazolopyridinone derivatives can be used as LPA receptor antagonists for the treatment of various herein disclosed diseases.06-27-2013
20110060002CONGLOMERATES OF TENATOPRAZOLE POTASSIUM SALTS - The invention relates to conglomerates of tenatoprazole potassium salts of the following general formula (I), that consist of an equimolar mixture of enantiomers having R and S configurations and capable of crystallisation in the form of a conglomerate, wherein said salts are selected from tenatoprazole dehydrated potassium salt, tenatoprazole potassium dimethanolate, tenatoprazole potassium diethanolate and tenatoprazole potassium ethylene-glycolate. The invention also relates to a pharmaceutical composition containing such salt, and to the use of said salt.03-10-2011
20080269281Novel Beta-Agonists, Method for Producing Them and Their Use as Drugs - Compounds of the formula10-30-2008
20090076069DEUTERIUM-ENRICHED APIXABAN - The present application describes deuterium-enriched apixaban, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20080312272ARYLOAZOL-2-YL CYANOETHYLAMINO COMPOUNDS, METHOD OF MAKING AND METHOD OF USING THEREOF - The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives of formula (I):12-18-2008
20100029709NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - A novel [1,2,4]triazolo[1,5-a]pyridine compound is disclosed that has a formula represented by the following:02-04-2010
20100029710COMPOUNDS HAVING BOTH ANGIOTENSIN II RECEPTOR ANTAGONISM AND PPARy ACTIVATING ACTIVITIES - Compounds of following formula (I) are provided that have both angiotensin II receptor antagonist activity and PPARy agonist activity. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment of diseases with the compounds including type 2 diabetes, insulin resistance, hyperinsulinemia, hyperlipidemia, hypertriglyceridemia, metabolic syndrome, congestive heart failure, and hypertension.02-04-2010
20090099228PYRAZOLO-TETRAHYDRO PYRIDINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS - The invention relates to novel pyrazolo-tetrahydropyridines compounds and their use as orexin receptor antagonists.04-16-2009
201001135073-Tetrazolyl Indazoles, 3-Tetrazolyl Pyrazolopyridines, and use Thereof - The present application relates to novel 3-tetrazolylindazole and 3-tetrazolylpyrazolo[3,4-b]-pyridine derivatives, processes for their preparation, their use alone or in combination for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.05-06-2010
20090082392Substituted Carboxylic Acids - The present invention relates to compounds and pharmaceutically acceptable salts of formula (I):03-26-2009
20100120840Heterocyclic benzylamino derivatives, their manufacture and use as pharmaceutical agents - Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.05-13-2010
20100280065PERHARIDINES AS CDK INHIBITORS - The invention relates to trisubstituted or tetrasubstituted imidazo[4,5b]pyridines, to their uses as well as to a process for manufacturing them.11-04-2010
20100286192NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS - Compounds of Formula I:11-11-2010
20120065227TRIAZOLOPYRIDINONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses triazolopyridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I:03-15-2012
20120035209Hydroxy Substituted 1H-Imidazopyridines and Methods - Hydroxy substituted 1H-imidazo[4,5-c]pyridin-4-amines, with a hydroxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.02-09-2012
20100249181HIV Protease Inhibiting Compounds - A compound of the formula09-30-2010
201002861912-Arylthiazole Derivatives as CXCR3 Receptor Modulators - The invention encompasses compounds of Formula I or pharmaceutically acceptable salts thereof, which are modulators of the CXCR3 chemokine receptor function useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.11-11-2010
20100125089ENANTIOMERICALLY ENRICHED ARYLOAZOL-2-YL CYANOETHYLAMINO COMPOUNDS, METHOD OF MAKING AND METHOD OF USING THEREOF - The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives substantially enriched in an enantiomer of formula (I):05-20-2010
20090143422P38 INHIBITORS AND METHODS OF USE THEREOF - This invention relates to inhibitors of p38 and methods of utilizing the inhibitors and pharmaceutical compositions thereof in the treatment and prevention of various disorders mediated by p38.06-04-2009
20080207682Phenylurea Derivatives As Inhibitors Of Tyrosine Kinases For The Treatment Of Tumour Diseases - Compounds of the formula (I), in which R08-28-2008
20080207683BIARYL-SUBSTITUTED TETRAHYDRO-PYRAZOLO-PYRIDINE MODULATORS OF CATHEPSIN S - Biaryl-substituted tetrahydro-pyrazolo-pyridine compounds are described, which are useful as cathepsin S modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by cathepsin S activity, such as psoriasis, pain, multiple sclerosis, atherosclerosis, and rheumatoid arthritis.08-28-2008
20080207684Kinase inhibitors and methods for using the same - Compounds of formula I:08-28-2008
20090111848Halogenated Pyrazolo[1,5-A]Pyrimidines, Processes, Uses, Compositions and Intermediates - The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R04-30-2009
20090042931Tricyclic Angiotensin II Agonists - There is provided compounds of formula I,02-12-2009
20110172266PYRAZOLO PYRIDINE DERIVATIVES AS NADPH OXIDASE INHIBITORS - The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).07-14-2011
20080242695Certain Chemical Entities, Compositions, and Methods - Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of muscle weakness and/or cachexia, as part of a rehabilitation or conditioning exercise regimen, or in the treatment of fraility, post-polio syndrome, obesity, sarcopenia, wasting syndrome, muscle spasm, and other indications.10-02-2008
20080275078Pyrazolo[3,4-B] Pyridine Compounds and Their Use as Pde4 Inhibitors - The invention provides a compound of formula (I) or a salt thereof:11-06-2008
20080312271AZABENZIMIDAZOLYL COMPOUNDS - Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I12-18-2008
20080269280OXO-IMIDAZOLIDINES AS MODULATORS OF CHEMOKINE RECEPTORS - Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.10-30-2008
20090163539ENANTIOMER OF TENATOPRAZOLE AND THE USE THEREOF IN THERAPY - This invention relates to optically active substances of tenatoprazole, (+) and (−) -5-methoxy-2-{(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl}-1H-imidazo[4,5-b]pyridine. The compound and pharmaceutical compositions thereof are useful for anti-ulcer agent.06-25-2009
20080234314FUSED AMINO PYRIDINE AS HSP90 INHIBITORS - The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.09-25-2008
20090326003PYRAZOLO (3, 4-B) PYRIDINE DERIVATIVES AS PDE4 INHIBITORS - The present invention provides a compound of formula (I) or a salt thereof (in particular, a pharmaceutically acceptable salt thereof):12-31-2009
20130217722NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - A novel imidazolopyridine according to Formula I, able to inhibit JAK as disclosed, this compound may be prepared as a pharmaceutical composition, 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, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.08-22-2013
20130217723Pharmaceutical Composition Combining Tenatoprazole and an Anti-Inflammatory Agent - The invention relates to a novel pharmaceutical combination. The inventive pharmaceutical composition comprises a combination of tenatoprazole and one or more anti-inflammatory agents selected from non-steroid anti-inflammatory agents and cyclooxygenase-2 inhibitors. The invention is suitable for the treatment of painful and inflammatory manifestations.08-22-2013
20090197910NOVEL VIRAL REPLICATION INHIBITORS - The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one benzimidazole conjugates derivative having the general formula (I). The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula and their use as a medicine or to treat or prevent viral infections.08-06-2009
20090197911LONIDAMINE ANALOGUES AND TREATMENT OF POLYCYSTIC KIDNEY DISEASE - Lonidamine derivatives can be useful in methods of treating, inhibiting, and/or preventing polycystic kidney disease (PKD). Accordingly, lonidamine derivatives can be administered in a therapeutically effective amount for inhibiting, and/or preventing polycystic kidney disease (PKD) in the subject. This can include administering a therapeutically effective amount of the lonidamine derivatives for inhibiting CFTR and/or Hsp90 or biological pathway thereof. Also, the method can include administering the lonidamine derivatives in a therapeutically effective amount for inhibiting ErbB2, Src, Raf-1, B-Raf, MEK, Cdk4, NKCC1, or combinations thereof. For example, the therapeutically effective amount of the lonidamine derivatives can be configured so as to provide a concentration in or adjacent to a kidney cell of about 0.25 uM or more or less.08-06-2009
20090062330TREATMENT OF PROGRESSIVE NEURODEGENERATIVE DISEASE WITH IBUDILAST - Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine).03-05-2009
20120077841METHODS FOR CANCER THERAPY AND STEM CELL MODULATION - The present invention relates to a method of modulating pluripotency and/or self-renewing characteristics of a stem/progenitor cell. The method comprises administering to the respective cell a compound of the general formula (I)03-29-2012
20090209578CHEMICAL COMPOUNDS - The present invention provides compounds of formula (I) wherein R08-20-2009
20090221632Bicyclo-Pyrazoles and Pharmaceutical Compositions Comprising Them - Bicyclo-pyrazole compounds of formula (I), as herein defined, are useful for treating diseases linked to disregulated protein kinases.09-03-2009
20090239899Triazolopyridinylsulfanyl Derivatives As P38 Map Kinase Inhibitors - A compound of formula (I), or a pharmaceutical acceptable salt and/or solvate (including hydrate) thereof;09-24-2009
20090253737CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS - Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of neuromuscular disorders, conditions having muscle wasting, claudication, frailty, metabolic syndrome, muscle atrophy associated with disuse, and muscle fatigue, and other indications.10-08-2009
20090258897Substituted benzimidazoles - Disclosed herein are substituted benzimidazole-based proton pump modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.10-15-2009
20100152230HYDROXY SUBSTITUTED 1H-IMIDAZOPYRIDINES AND METHODS - Hydroxy substituted 1H-imidazo[4,5-c]pyridin-4-amines, with a hydroxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.06-17-2010
20100168159HETERO COMPOUND07-01-2010
20110060003LONIDAMINE ANALOGUES FOR FERTILITY MANAGEMENT - Fertility management can include: administering to the subject one or more doses of a compound according to Formula I so as to reduce fertility in the subject. Fertility management can also include administering an effective amount of the compound to: impair Sertoli cell function in a male subject; inhibit spermatogenesis in the subject; reduce testis weight in the subject; reduce ovary weight in a female subject; reduce serum progesterone in the female subject; impair ovarian follicle function in the female subject; causing reversible fertility in the subject. In order to return fertility, the method can include ceasing administration of the compound to the subject so as to return fertility in the subject. The compound can be administered for irreversibly sterilizing the subject.03-10-2011
20130123297PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING OSTEOPOROSIS OR OBESITY COMPRISING PHENYLTETRAZOLE DERIVATIVE - A pharmaceutical composition comprising a phenyltetrazole derivative of formula (I) or a pharmaceutical acceptable salt thereof is effective in preventing or treating osteoporosis, obesity, diabetes, or hyperlipidemia, by regulating protein TAZ.05-16-2013
20100216835Method For Modulating Microbial Quorum Sensing - The present invention provides compositions and methods for modulating bacterial quorum sensing using antagonist or agonist compounds. Further, the present invention provides methods of treating or preventing microbial damages and diseases, in particular for diseases where there is an advantage in inhibiting quorum sensing regulated phenotypes of pathogens.08-26-2010
20110112138MULTI-CYCLIC CINNAMIDE DERIVATIVES - The present invention provides a compound represented by the formula (I):05-12-2011
20090247571Certain Chemical Entities, Compositions and Methods - Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of obesity, sarcopenia, wasting syndrome, frailty, cachexia, muscle spasm, post-surgical and post-traumatic muscle weakness, neuromuscular disease, and other indications.10-01-2009
20100331359NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - A compound is disclosed that has a formula represented by the following:12-30-2010
20090253738TRIAZOLOPYRIDINONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses triazolopyridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I:10-08-2009
20110009444N-AZABICYCLIC CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - This disclosure relates to compounds of formula (I):01-13-2011
20110009445NEUROPROTECTANTS - Methods of protecting cells against cytotoxic insults are provided. The methods involve administering a composition including a CpG oligonucleotide to a subject. The methods are applicable to the protection of neural and non-neural cells. For example, methods of protecting a neural cell against excitotoxic brain injury are provided. Methods for preparing medicaments for the prophylactic treatment of excitotoxic injury, ischemia and/or hypoxia are also provided. Also provided are compositions for use in the described methods.01-13-2011
20110034506TRIAZOLOPYRIDINE COMPOUNDS USEFUL AS DGAT1 INHIBITORS - Disclosed are triazolopyridine compounds of the following Formula (I); or stereoisomers or salts thereof. Also, disclosed are methods of using the compound in the treatment of obesity, dyslipidemia, diabetes and atherosclerosis, and to pharmaceutical compositions comprising at least one compound of Formula (I) or a stereoisomer or pharmaceutically acceptable salt thereof.02-10-2011
20110039884Imidazopyridinones - The invention relates to imidazopyridinones, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.02-17-2011
20110152313SYNTHESIS OF AGELADINE A AND ANALOGS THEREOF - The invention describes a one pot process for synthesizing a compound of structure (I), or a tautomer thereof. A compound of structure (II), or a tautomer thereof, and an aldehyde of structure R06-23-2011
20120035208PYRAZOLOPYRIDINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Compounds of Formula (I), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer or inflammation mediated by lipid kinases. Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.02-09-2012
20100063088Raf Kinase Inhibitors - Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.03-11-2010
20090215817Novel Triazolopyridine Compounds for the Treatment of Inflammation - This invention is directed generally to triazolopyridine compounds that generally inhibit p38 kinase, TNF, and/or cyclooxygenase activity. Such triazolopyridine include compounds generally corresponding in structure to the following formula:08-27-2009
20100120841BENZIMIDAZOLE COMPOUND AND PHARMACEUTICAL USE THEREOF - Provided is an ORL-1 receptor agonist having improved bioavailability based on superior metabolic stability and strong and high selectivity, as compared to conventional compounds. A compound represented by the formula (I)05-13-2010
20110077268KINASE INHIBITORS AND METHODS OF USE - The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating lipid kinases such PB kinases, tryosine kinases and protein kinases such as mTOR. Also provided in the present invention are methods of using these compositions to modulate these kinases especially for therapeutic applications.03-31-2011
20110060004Imidazo-Pyridine Derivatives as Activin-Like Receptor Kinase (ALK4 or ALK5) Inhibitors - Compounds of formula (I): in free or salt or solvate form, where X, R03-10-2011
20110152314USE OF TENATOPRAZOLE FOR THE TREATMENT OF GASTROESOPHAGEAL REFLUX DISEASE - The invention relates to a novel therapeutic application of tenatoprazole. Tenatoprazole and the salts thereof can be used in the production of a medicament for the treatment of atypical and esophageal symptoms of gastroesophageal reflux, gastrorrhagia and dyspepsia.06-23-2011
20100048611TETRAHYDROPYRROLOPYRIDINE, TETRAHYDROPYRAZOLOPYRIDINE, TETRAHYDRO-IMIDAZOPYRIDINE AND TETRAHYDROTRIAZOLOPYRIDINE DERIVATIVES AND USE THEREOF - The invention relates to novel tetrahydropyrrolopyridine, tetrahydropyrazolopyridine, tetrahydroimidazopyridine and tetrahydrotriazolopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders02-25-2010
20120122919PHARMACEUTICAL COMPOSITION COMBINING TENATOPRAZOLE AND A HISTAMINE H2-RECEPTOR ANTAGONIST - The invention relates to a novel pharmaceutical combination. The inventive pharmaceutical composition, which is intended for the treatment of pathologies linked to gastric hyperacidity, comprises a combination of tenatoprazole and one or more histamine H2-receptor antagonists preferably selected from cimetidine, ranitidine, famotidine and nizatidine. The invention is particularly suitable for the treatment of duodenal and gastric ulcers and the symptoms of, and lesions caused by, gastroesophageal reflux.05-17-2012
20090298866Indole Compounds - The present application relates to compounds of formula (I) or a pharmaceutically acceptable derivative thereof: formula (I) wherein X, R12-03-2009
20120202846MOLECULAR TARGET OF NEUROTOXICITY - The present invention relates to the fields of biology, genetics and medicine. In particular it concerns new methods for the detection, characterisation and/or treatment (or management) of neurodegenerative diseases, particularly amyotrophic lateral sclerosis. The invention equally concerns methods for identifying or screening compounds active in these diseases. The invention further concerns the compounds, genes, cells, plasmids or compositions useful for implementing the hereinabove methods. In particular, the invention describes the role of PDE4B in these diseases and its use as a therapeutic, diagnostic or experimental target.08-09-2012
200901183255-Thioxylopyranose Compounds - 5-thioxylose compounds, especially 5-thioxylopyranose compounds, a process for their preparation, and their use for treating and/or inhibiting thromboses, especially venous thromboses. The compounds correspond to formula I:05-07-2009
20080319005Phenylacetamides Suitable as Protein Kinase Inhibitors - The invention relates to compounds of the formula (I) wherein the moieties R1, R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, and salts thereof, as well as their use, methods of use for them and method of their synthesis, and the like. The compounds are protein kinase inhibitors and can, inter alia, be used in the treatment of various proliferative diseases.12-25-2008
20080255185SMALL-MOLECULE MODULATORS OF TRP-P8 ACTIVITY - Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.10-16-2008
20120302598IMIDAZOPYRIDINONES - The invention relates to imidazopyridinones, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.11-29-2012
20100004281VIRAL INHIBITORS - The present invention relates to imidazo[4,5-c]pyridine compounds and pharmaceutical compositions for the treatment or prevention of viral infections, wherein the imidazo[4,5-c]pyridine compounds have the formula:01-07-2010
20100190820MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF - Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1 and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I): its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein the group X is O or (R07-29-2010
20110190337SUBSTITUTED PYRAZOLOPYRIDINES, COMPOSITIONS CONTAINING THEM, METHOD FOR THE PRODUCTION THEREOF, AND THEIR USE - The disclosure relates to substituted pyrazolo-pyridines, compositions containing them, methods for the production thereof, and to their use as medicaments, in particular, as anticancer agents.08-04-2011
20100004280Substituted imidazoles as bombesin receptor subtype-3 modulators - Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.01-07-2010
20090023771PHARMACEUTICAL COMPOSITION COMPRISING A PROTON PUMP INHIBITOR AND PROTEIN COMPONENT - The present disclosure relates to, inter alia, pharmaceutical compositions comprising a H01-22-2009
20090286827NOVEL BI-ARYL AMINES - The present invention relates to novel bi-aryl amines of formula (I) and to pharmaceutically acceptable prodrugs, salts, solvates, hydrates, and N-oxides thereof and to pharmaceutical compositions comprising them, methods of their use, and methods of their preparation.11-19-2009
20120059030HETEROCYCLIC COMPOUND AND USE THEREOF - The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and/or a superior γ-secretase modulation activity, and use thereof. A compound represented by the formula (I):03-08-2012
20090209577Novel Triazolopyridine Compounds - This invention is directed generally to triazolopyridine compounds that generally inhibit p38 kinase, TNF, and/or cyclooxygenase activity. Such triazolopyridine include compounds generally corresponding in structure to the following formula:08-20-2009
20100184801FUSED AMINO PYRIDINES FOR THE TREATMENT OF BRAIN TUMORS - The present invention relates to the use of compounds with fused amino pyridine core for the treatment of malignancies associated with brain and lung. The oral administration of compounds of the instant application results in effective brain penetration and provides for non-intrusive treatment of brain and lung tumors.07-22-2010
20120059029SELECTIVE INTEGRIN INHIBITORS - This invention provides methods for selectively antagonizing the α4β1 integrin heterodimer in a subject in need thereof, and preferably in a human subject. The methods of the invention utilize conjugates comprising two or more α4β1 small molecule antagonists covalently attached to a biocompatible polymer. These methods of selectively inhibiting α4β1 may be used modulate both normal and pathological biological processes mediated at least in part through α4β1 activity.03-08-2012
20090137624Chemical Compounds - This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.05-28-2009
20110092539INDANE DERIVATIVES AS AMPA RECEPTOR MODULATORS - The present invention relates to a heterocyclic derivative according to formula (I); wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.04-21-2011
20120208840Condensed Ring Pyridine Compounds As Subtype-Selective Modulators Of Sphingosine-1-Phosphate-2 (S1P2) Receptors - The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity, wherein these compounds selected from the group consisting of wherein A, B, C, D, X, Y, Z and R08-16-2012
20110077267TRIAZOLOPYRIDINE COMPOUND, AND ACTION THEREOF AS PROLYL HYDROXYLASE INHIBITOR OR ERYTHROPOIETIN PRODUCTION-INDUCING AGENT - The present invention provides a triazolopyridine compound having a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability. The present invention relates to a compound represented by the following formula [I]:03-31-2011
20120309784TRIAZOLOPYRIDINE KINASE INHIBITORS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - A novel [1,2,4]triazolo[1,5-a]pyridine compound is disclosed that has a formula represented by the following:12-06-2012
20120316197USE OF EP4 RECEPTOR ANTAGONISTS IN THE TREATMENT OF IL-23 MEDIATED DISEASES - This invention relates to a compound with EP4 antagonistic activity, or a pharmaceutically acceptable salt with EP4 receptor antagonistic activities, which is useful in the treatment of immune disease or allergy. This invention also relates to a compound of formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof with EP4 receptor antagonistic activities, which is useful in the treatment of immune disease or allergy. This invention also relates to a pharmaceutical composition for the treatment of immune disease or allergy which comprises a therapeutically effective amount of a compound of formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof. Further this invention relates to a method for the treatment of immune disease or allergy in an animal subject including a mammalian subject, which comprises administering to the animal subject including a mammalian subject a compound of the formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof.12-13-2012
20110184016PREVENTION AND TREATMENT OF ITCH WITH CYSTEINE PROTEASE INHIBITION - Embodiments of the invention relates to methods of preventing itch in a subject using a therapeutically effective amount of a cysteine protease inhibitor. The itch is not associated with psoriasis and atopic dermatitis. The itch is also a non-histamine mediated itch. The inhibitor are directed to the cathepsin selected from the group consisting of cathepsin B, C, F, J, K, H, L, P, Q, S, W, X, V, and Z.07-28-2011
20110184015NOVEL DERIVATIVES OF PYRROLOINDOLE WHICH ARE INHIBITORS OF HSP90, COMPOSITIONS CONTAINING SAME, AND USE THEREOF - Pyrroloindoles of formula (I) are provided wherein Het is an aromatic or partially unsaturated, monocyclic or bicyclic heterocycle containing between 1 and 4 heteroatoms N, O or S, optionally substituted by R1 or R′1 which are the same or different; R is X-(A-B)n-CONH2, X-(A-B)n-O—CONH2, X-(A-B)n-NH—CONH2, X—(CH2)m-heterocycloalkyl, X(CH2)m-aryl and X—(CH2)m-heteroaryl wherein X is —O—C(O), —NH—C(O), NH—CS, —NH—CO—CH2-O—; —NH—COCH2-S—CH2-CO—NH—; —NH—CO—(CH2)2-SO2-; and —NH—CO—CH2-N(CH3)-CO—; A and B are the same or different and are each independently a single bond, CH2, CH-alkyl, and CH-aralkyl; n=1,2 and m=0, 1; R1 and/or R′1 are H, halogen, CF3, nitro, cyano, alkyle, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, and carboxy, free or esterified by an alkyl, carboxamide, CONH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—SO2-alkyl, S(O)2-NHalkyl, and S(O2)-N(alkyl)2 group, all of said alkyl, alcoxy and alkylthio groups being optionally substituted themselves, said products being in all isomer forms and salts, as medicaments.07-28-2011
20120165368PYRAZOLOPYRIDINE KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.06-28-2012
20100173934COMBINATIONS OF THERAPEUTIC AGENTS FOR TREATING CANCER - The invention relates to a combination comprising a microtubule active agent; and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; methods of treatment comprising said combination; processes for making said combination; and a commercial package comprising said combination.07-08-2010
20120172392AMINE-BASED AND AMIDE-BASED INHIBITORS OF SEMICARBAZIDE-SENSITIVE AMINE OXIDASE (SSAO) ENZYME ACTIVITY AND VAP-1 MEDIATED ADHESION USEFUL FOR TREATMENT OF DISEASES - Compositions and methods are disclosed for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1). The compounds disclosed are amine-containing and amide-containing compounds. The compounds and compositions are useful for treatment of diseases, including inflammation, inflammatory diseases and autoimmune disorders.07-05-2012
20120252838TETRAHYDROTRIAZOLOPYRIDINE COMPOUNDS AS SELECTIVE MGLU5 RECEPTOR POTENTIATORS USEFUL FOR THE TREATMENT OF SCHIZOPHRENIA - The present invention provides certain tetrahydrotriazolopyridine derivatives, pharmaceutical compositions thereof, methods of using the same and processes for preparing the same. Formula (I) wherein R10-04-2012
20110190335NITROGENATED 5-MEMBERED HETEROCYCLIC COMPOUND - The purpose of the present invention is to provide a glucokinase activator which is useful as a pharmaceutical agent such as agents for the prophylaxis or treatment of diabetes, obesity and the like, and the like.08-04-2011
20100048612BICYCLIC HETEROCYCLES AS CANNABINOID-1 RECEPTOR MODULATORS - The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formula:02-25-2010
20120178778PYRAZOLOPYRIDINES - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.07-12-2012
20120220623THE ENANTIOMER OF TENATOPRAZOLE AND THE USE THEREOF IN THERAPY - This invention relates to optically active substances of tenatoprazole, (+) and (−)-5-methoxy-2-{(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl}-1H-imidazo[4,5-b]pyridine. The compound and pharmaceutical compositions thereof are useful for anti-ulcer agent.08-30-2012
20120220624PYRAZOLO [3,4-B] PYRIDIN-4-ONE KINASE INHIBITORS - The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer.08-30-2012
20120225904New 7-Phenyl-[1,2,4]triazolo[4,3-a]Pyridin-3(2H)-One Derivatives - This disclosure is directed to, inter alis, new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), to processes for their preparation, to pharmaceutical compositions comprising them, and to their use in therapy.09-06-2012
20090018158CRYSTAL FORMS OF AN IMIDAZOLE DERIVATIVE - The invention relates to the essentially pure Λ/-[({2-[4-(2-Ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1 -yl)phenyl]ethyl}amino)carbonyl]-4-methylbenzenesulfonamide Polymorph Forms A and B and to processes for the preparation of, compositions containing and to the uses of, such crystal forms.01-15-2009
20110003848Polymorphic Form Of A [1,2,4]Triazole[4,3-A] Pyridine Derivative For Treating Inflammatory Diseases - The present invention relates to a polymorphic form B of Λ/[3-tert-butyl-1-(3-chloro-4-hydroxyphenyl)-1H-pyrazol-5-yl]-N-{2-[(3-{2-[(2-hydroxyethyl)sulfanyl]phenyl}[1,2,4]triazolo[4,3-a]pyridin-6-yl)sulfanyl]benzyl}urea (I) as de-fined herein. This polymorph is useful in the treatment of various conditions, particularly in the treatment of inflammatory conditions such as chronic obstructive pulmonary disease.01-06-2011
20090247570PHARMACEUTICALS - The present invention relates to the use of a CCR5 antagonist in an HIV infected patient to enhance their immune reconstitution and so treat to HIV related opportunistic conditions resulting from the immunocompromised state of the HIV patient. The invention also allows treatment with a CCR5 antagonist of patients having a CXCR4 using viral population since such patients will also benefit from an increase in their CD4 and/or CD8 cell count.10-01-2009
20120322821GHRELIN RECEPTOR AGONIST FOR TREATMENT OF CACHEXIA - The present invention relates to use of a compound of the present invention or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt, for the manufacture of a medicament for the treatment of cachexia. The invention also relates to a method for the treatment of cachexia, comprising administering the compound of the present invention or a pharmaceutical composition comprising the same to a human or an animal. The invention further relates to use of said compound, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt, in combination with one or more second active agents. Moreover, the invention relates to a pharmaceutical composition and a kit comprising the compound of the present invention or a pharmaceutically acceptable salt thereof, for the treatment of said disease.12-20-2012
20090203732Thiazolones for Use as P13 Kinase Inhibitors - Invented is a method of inhibiting the activity/function of PI3 kinases using substituted thiazolones. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of substituted thiazolones.08-13-2009
20100130543PYRAZOLE CARBOXAMIDE INHIBITORS OF FACTOR XA - The present invention relates to new pyrazole carboxamide inhibitors of factor Xa, pharmaceutical compositions thereof, and methods of use thereof.05-27-2010
20100130542Composition Comprising a Combination of Omeprazole and Lansoprazole, and a Buffering Agent, and Methods of Using Same - The present disclosure relates to pharmaceutical compositions comprising omeprazole, lansoprazole and sodium bicarbonate. Methods of using such compositions are also provided05-27-2010
20080255186Pyrazolo[3,4-B]Pyridine Compound, and Its Use as a Pde4 Inhibitor - The invention provides N-{[1,6-diethyl-4-(tetrahydro-2H-pyran-4-ylamino)-1H-pyrazolo[3,4-b]pyridin-5-yl]methyl}-3-methyl-5-isoxazolecarboxamide10-16-2008
20100087477SELECTIVE GLYCOSIDASE INHIBITORS - The present invention provides glucoimidazole derivatives and methods of making them. The compounds can be used to inhibit the activity of O-GlcNAcase enzymes, including both bacterial OGA (bOGA) and human OGA (hOGA) and can be selective, showing low inhibition of hexosaminidases. The compounds can be used to study the role of the O-GlcNAcase modification in human or animal cells. Furthermore the compounds can have therapeutic uses in the treatment of diseases mediated by the activity of O-GlcNAcase enzymes including type II diabetes, Alzheimers disease, and cancer.04-08-2010
20080221154HIV-INTEGRASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS FOR THEIR USE - Bicyclic hydroxamate compounds represented by the Formula I:09-11-2008
20130178497FUSED TRIAZOLES FOR THE TREATMENT OR PROPHYLAXIS OF MILD COGNITIVE IMPAIRMENT - The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and/or a superior γ-secretase modulation activity, and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.07-11-2013
20130096155TRIAZOLOPYRIDINE COMPOUND, AND ACTION THEREOF AS PROLYL HYDROXYLASE INHIBITOR OR ERYTHROPOIETIN PRODUCTION-INDUCING AGENT - The present invention provides a triazolopyridine compound having a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability. The present invention relates to a compound represented by the following formula [I]:04-18-2013
20130102629ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by formula (I)04-25-2013
20130123296LONIDAMINE ANALOGUES FOR FERTILITY MANAGEMENT - Fertility management can include: administering to the subject one or more doses of a compound according to Formula I so as to reduce fertility in the subject. Fertility management can also include administering an effective amount of the compound to: impair Sertoli cell function in a male subject; inhibit spermatogenesis in the subject; reduce testis weight in the subject; reduce ovary weight in a female subject; reduce serum progesterone in the female subject; impair ovarian follicle function in the female subject; causing reversible fertility in the subject. In order to return fertility, the method can include ceasing administration of the compound to the subject so as to return fertility in the subject. The compound can be administered for irreversibly sterilizing the subject.05-16-2013
20130143914UREA DERIVATIVES AND THEIR THERAPEUTIC USE IN THE TREATMENT OF, INTER ALIA, DISEASES OF THE RESPIRATORY TRACT - Compounds of formula (I) are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory wherein R06-06-2013
20130143915TRIAZOLOPYRIDINES AS TYK2 INHIBITORS - The present invention relates to compounds of Formula (I), wherein R06-06-2013
20130131103Methods and Compositions For Improved Nerve Conduction Velocity - The present invention provides methods and compositions for the effective treatment of impaired nerve signal conduction. Compositions including selective AT05-23-2013
20100317689Prodrugs of proton pump inhibitors including the 1h-imidazo[4,5-b] pyridine moiety - The compounds of formulas (I), (II), (III) and (IV), where the symbols are as defined in the specification are prodrugs of proton pump inhibitors. The R12-16-2010
201202832881-(5-TERT-BUTYL-2-PHENYL-2H-PYRAZOL-3-YL)-3-[2-FLUORO-4-(1-METHYL-2-OXO-2,- 3-DIHYDRO-1H-IMIDAZO[4,5-B]PYRIDIN-7-YLOXY)-PHENYL]-UREA AND RELATED COMPOUNDS AND THEIR USE IN THERAPY - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (I) (for convenience, collectively referred to herein as “IP compounds”), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterised by (e.g., driven by) mutant RAS (“mutant RAS cancer”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer.11-08-2012
20110312992Inhibitors of C-Kit and Uses Thereof - Compounds and methods useful as inhibitors of c-Kit are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of c-Kit and processes for synthesizing these compounds are also described herein.12-22-2011
20130190350Mediators of Hedgehog Signaling Pathways, Compositions and Uses Related Thereto - The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.07-25-2013
20130203803Azaindazole Amide Compounds As CCR1 Receptor Antagonists - Disclosed are CCR1 inhibitor compounds of the formula (I): which are useful in the treatment of autoimmune and other diseases. Also disclosed a pharmaceutical compositions containing the same, and methods of making and using same.08-08-2013
20120302599KAT ll INHIBITORS - Compounds of Formula I:11-29-2012
20120088788SUBSTITUTED IMIDAZOLES AS BOMBESIN RECEPTOR SUBTYPE-3 MODULATORS - Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.04-12-2012
20120095038SYNTHESIS AND ANTI-PROLIFERATIVE EFFECT OF BENZIMIDAZOLE DERIVATIVES - This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated. In particular, the disclosure provides for substituted imidazo[4,5-c]pyridine compounds having the general formula04-19-2012
20120095037SYNTHESIS AND ANTI-PROLIFERATIVE EFFECT OF BENZIMIDAZOLE DERIVATIVES - This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated. In particular, the disclosure provides for substituted imidazo[4,5-b]pyridine compounds having the general formula04-19-2012
20120095036NOVEL SUBSTITUTED INDAZOLE AND AZA-INDAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS - The present invention is concerned with novel substituted indazole and aza-indazole derivatives of Formula (I)04-19-2012

Patent applications in class Exactly three ring nitrogens in the bicyclo ring system