Inventors list

Assignees list

Classification tree browser

Top 100 Inventors

Top 100 Assignees


Ring nitrogen shared by two of the cyclos

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

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

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.)

514231200 - Morpholines (i.e., fully hydrogenated 1,4- oxazines)

514231500 - Additional hetero ring attached directly or indirectly to the morpholine ring by nonionic bonding

514232800 - Polycyclo ring system having the additional hetero ring as one of the cyclos

Patent class list (only not empty are listed)

Deeper subclasses:

Entries
DocumentTitleDate
20130029982HETEROCYCLIC COMPOUNDS AND USES THEREOF - Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.01-31-2013
20100120761Bicyclic Heterocyclic Compounds as FGFR Inhibitors - The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.05-13-2010
20130029981COMPOUNDS, COMPOSITIONS, AND METHODS FOR CONTROLLING BIOFILMS - The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-01-31-2013
20120184546[1,2,4]TRIAZOLO [1,5-C]PYRIMIDINE DERIVATIVES AS HSP90 MODULATORS - The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine derivatives of formula (I) which inhibit the activity of Heat Shock Protein Hsp90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, methods of treating diseases and the pharmaceutical compositions comprising these compounds.07-19-2012
20130085141SUBSTITUTED OCTAHYDROPYRROLO[1,2-a]PYRAZINE SULFONAMIDES AS CALCIUM CHANNEL BLOCKERS - The present application relates to: (a) compounds of Formula (I):04-04-2013
20130085142SUBSTITUTED OCTAHYDROPYRROLO[1,2-a]PYRAZINES AS CALCIUM CHANNEL BLOCKERS - The present application relates to: (a) compounds of Formula (I):04-04-2013
20130085143AMINOACID DERIVATIVES, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES AS INHIBITORS OF ONCOGENIC SIGNALS BY THE MET FAMILY - Novel amino acids derivatives, in particular some amino acid amides derivatives, their process of preparation and their use for inhibiting Met-triggered disorders, in particular cancer.04-04-2013
20100029636Lck inhibitors - The invention relates to novel pyrazolo[1,5-A]pyrimidine compounds of Formula I02-04-2010
20100075958PYRROLOTRIAZINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS - This invention relates to pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis.03-25-2010
20120245164DIPHENYL-PYRAZOLOPYRIDINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF AS NUCLEAR RECEPTOR NOT MODULATORS - The invention relates to a formula (I), in which R is a hydrogen or halogen atom or a (C1-C6)alkyl group; X is one or more substituents selected from a hydrogen or halogen atom, a (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkoxy, cyano, hydroxy, or hydroxy(C1-C6)alkyl group; Y is a hydrogen or halogen atom or a (C1-C6)alkyl group; R1 is an NR2R3 or OR4 group; R2 and R3 independently are a hydrogen atom, a (C1-C6)alkyl, hydroxy(C1-C6)alkyl or oxo(C1-C6)alkyl group or R2 and R3, together with the nitrogen atom supporting the same, form a heterocycle optionally substituted by a (C1-C6)alkyl, hydroxy or oxo group; and R4 is a (C1-C6)alkyl, hydroxy(C1-C6)alkyl, or oxo(C1-C6)alkyl group, in the base or acid addition salt state. Said formula can be used therapeutically for treating or preventing diseases linked to the nuclear receptors Nurr-1, also known as NR4A2, NOT, TINUR, RNR-1, and HZF3.09-27-2012
20090270388FUSED AZOLE-PYRIMIDINE DERIVATIVES - The present invention relates to novel fused azolepyriimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity.10-29-2009
20130040946SUBSTITUTED IMIDAZOPYRIMIDINES AND TRIAZOLOPYRIMIDINES - The invention relates to substituted imidazo- and triazolopyrimidines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of haematological disorders, preferably of leucopenias and neutropenias.02-14-2013
20090209531Pyrimido-Benzimidazole Derivatives and the Use Thereof in the Form of Agonists and Antagonists of Melanocortin Receptors - The invention relates to novel pyrimido-benzimidazole derivatives. Said products exhibit a good affinity for certain melanocortin receptor sub-types, in particular MC4 receptors. Said products represent a particular interest for treating pathological disorders and diseases associated with one or several melanocortin receptors. Pharmaceutical compositions containing said products and the use thereof for a drug preparation are also disclosed.08-20-2009
20100048556QUINOXALINE DERIVATIVES - The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I)02-25-2010
20100105676FUSED HETEROCYCLIC COMPOUNDS USEFUL AS KINASE MODULATORS - Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, [PLEASE INSERT CHEMICAL STRUCTURE HERE] (I) are useful as kinase modulators, including Btk modulation, wherein R1, R2, R4, Q, Y, A and D are as defined herein.04-29-2010
20100105677INDAZOLES, BENZOTHIAZOLES, BENZOISOTHIAZOLES, BENZISOXAZOLES, AND PREPARATION AND USES THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.04-29-2010
2010010567511 BETA-HSD1 MODULATORS - A compound according to Formula I: 04-29-2010
20100093718 Compounds - The invention relates to new bicyclic heterocyclic derivative compounds of Formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer The compounds of Formula (I) are inhibitors of FGFR, VEGFR or PDGFR.04-15-2010
20090124612Fused 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
20110003807Thiazole derivatives - The present invention relates to a compound represented by the formula (I) or (I′):01-06-2011
20090093476PYRROLO[1,2-A]QUINOXALINE DERIVATIVES AS ADENOSINE A3 RECEPTOR MODULATORS AND USES THEREOF - The present invention provides new compounds displaying high affinity for adenosine A04-09-2009
20090093475Oxo-substituted imidazo[1,2b]pyridazines, their preparation and use as pharmaceuticals - The invention relates to novel inhibitors of kinases of the general formula (I):04-09-2009
201300598442-PHENYL SUBSTITUTED IMIDAZOTRIAZINONES AS PHOSPHODIESTERASE INHIBITORS - The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.03-07-2013
20110015192SIRTUIN MODULATING COMPOUNDS - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. 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 related 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 benfit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.01-20-2011
20130059845BICYCLIC AGONISTS OF GPR131 AND USES THEREOF - The present disclosure relates to compounds that act as agonists of, or otherwise modulate the activity of, GPR131 and to their use in the treatment of various diseases. In particular embodiments, the structure of the compounds is given by Formula I:03-07-2013
20130059846COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS - The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases.03-07-2013
20090170844Spiro Tetracyclic Compound - Disclosed is an anti-coagulant which has extremely excellent inhibitory effect on FXa and an extremely poor inhibitory effect on hERG channel, and can be administered through the oral route. Specifically, disclosed is a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof.07-02-2009
20130065893IMIDAZOLE DERIVATIVES AS ALDOSTERONE SYNTHASE INHIBITORS - The present invention provides a compound of formula (I) or pharmaceutically acceptable salt thereof, wherein the variables R03-14-2013
20110021521FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I:01-27-2011
20110021520OXAZINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS - The invention relates to novel heterocyclic compounds of the formula01-27-2011
20110021519TETRAHYDROPTERIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.01-27-2011
20110021518PYRROLOTRIAZINE DERIVATIVES USEFUL FOR TREATING CANCER THROUGH INHIBITION OF AURORA KINASE - This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly Cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly Cancer.01-27-2011
20090012080Sirtuin modulating compounds - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. 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 related 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.01-08-2009
20090012079Triazolopyridine Compounds - A compound of formula (Ia): or a pharmaceutically acceptable salt and/or solvate (including hydrate) thereof, or a compound of formula (Ib): or a pharmaceutically acceptable salt and/or solvate (including hydrate) thereof, and the use of a compound of formula (Ia) or (Ib) in the treatment of a TNF-mediated disease, disorder, or condition, or a p38-mediated disease, disorder, or condition, in particular the allergic and non-allergic airway diseases, more particularly obstructive or inflammatory airways diseases, preferably chronic obstructive pulmonary disease.01-08-2009
20090012078Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases - Novel fused pyrazine compounds are disclosed that have a formula represented by the following:01-08-2009
20120238565TRIAZOLOPYRIDINE COMPOUNDS AND THEIR USE AS ASK INHIBITORS - The present invention relates to triazolopyridine compounds according to Formula (I), their use as medicament, for treating autoimmune disorders, inflammatory diseases, cardiovascular diseases and/or neurodegenerative diseases and a process for their preparation.09-20-2012
20120238564IMIDAZO PYRAZINES - Compounds of formula09-20-2012
20130165437NOVEL DIHYDROPYRIMIDINOISOQUINOLINONES AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS. - A compound according to Formula Ia:06-27-2013
20080293713Inhibitors of Diacylglycerol O-acyltransferase Type 1 Enzyme - The present invention relates to compounds of formula (I):11-27-2008
20090156594HETEROCYCLIC KINASE MODULATORS - The present disclosure provides heterocyclic protein kinase modulators and methods of using these compounds to treat diseases mediated by kinase activity.06-18-2009
20120101094INDAZOLES, BENZOTHIAZOLES, AND BENZOISOTHIAZOLES, AND PREPARATION AND USES THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.04-26-2012
20120101093SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS BETA-SECRETASE INHIBITORS - The present invention is directed to substituted imidazo[1,2-a]pyridine derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which BACE is involved.04-26-2012
20090099167Organic compounds - The invention relates to the use of pyrazolo[1,5a]pyrimidin-7-yl amine compounds and salts thereof in the treatment of kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, novel pyrazolo[1,5a]pyrimidin-7-yl amine compounds, and a process for the preparation of the novel pyrazolo[1,5a]pyrimidin-7-yl amine compounds.04-16-2009
20090099168HIV Integrase inhibitors - Pyridopyrazine- and pyrimidopyrazine-dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dihydroxypyridine carboxamides are of Formula I:04-16-2009
20110281863IMIDAZO[1,2-B]PYRIDAZINE AND PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS - The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II):11-17-2011
20110136803Triazolophthalazines - The compounds of formula (I)06-09-2011
20120289503AQUEOUS SOLUTION COMPRISING 3 - QUINUCLIDINONES FOR THE TREATMENT HYPERPROLIFERATIVE, AUTOIMMUNE AND HEART DISEASE - A liquid composition that is an aqueous solution of a compound of formula (I), wherein the aqueous solution has a pH from about 3.0 to about 5.0. The liquid composition may be used in the treatment of a disorder selected from hyperproliferative diseases, autoimmune diseases and heart diseases.11-15-2012
20090170845USE OF IMIDAZO[2,1-b]-1,3,4-THIADIAZOLE-2-SULFONAMIDE COMPOUNDS TO TREAT NEUROPATHIC PAIN - Disclosed herein are methods and compositions for treating and/or prophylaxis of neuropathic pain in a subject. The methods comprise administering to the subject suffering from neuropathic pain, a therapeutically effective amount of a compound, according to Formula I:07-02-2009
20110301160Inhibitors of P38 and Methods of Using the Same - In general, the present invention relates to compounds capable of inhibiting p38 in vivo or in vitro, and methods for treating conditions associated with p38 activity or cytokine activity.12-08-2011
20110294800HYPOGLYCEMIC DIHYDROPYRIDONES - The present invention provides, inter alia, a compound of formula I: wherein the substituent designations are indicated in the Specification. The present invention also provides pharmaceutical compositions comprising a compound of formula I, and methods of treatment or prevention of diabetes or hyperglycemia in a patient, and of normalizing blood glucose levels in a subject, by administering an effective amount of a compound of formula I.12-01-2011
20110294801MACROCYCLICS PYRIMIDINES AS AURORA KINASE INHIBITORS - Macrocyclic derivative compounds that inhibit protein kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed kinase activity such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.12-01-2011
20090286778MACROCYCLIC COMPOUNDS AND THEIR USE AS KINASE INHIBITORS - The present invention relates to macrocyclic compounds of Formula I:11-19-2009
20110034456IMIDAZOPYRIDAZINES AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS - The invention relates to novel compounds of formula I02-10-2011
20100035874Organic compounds - There are described pyrazolo[5.1-b]oxazole derivatives useful as corticotropin releasing factor (CRF02-11-2010
20100113441SUBSTITUTED IMIDAZOPYRIMIDINES AND TRIAZOLOPYRIMIDINES - The invention relates to substituted imidazopyrimidines and triazolopyrimidines, to methods for the production thereof, and to the use of same for producing medicaments for the treatment and/or prophylaxis of diseases, especially haematological diseases, preferably leucopenia and neutropenia.05-06-2010
20110263593NOVEL IMIDAZO[1,2-a]PYRIMIDINE DERIVATIVES, METHOD FOR THE PREPARATION THEREOF, USE THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE, IN PARTICULAR AS MET INHIBITORS - The disclosure concerns imidazo[1,2-a]pyrimidine derivatives of formula (I) and isomers and pharmaceutically acceptable salts thereof. Methods for preparing the compounds, pharmaceutical compositions, and methods of treatment also are disclosed.10-27-2011
20100063046TETRACYCLIC IMIDAZOLE ANALOGS - The present invention provides tetracyclic imidazole analogs which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing these compounds, and methods of using the same.03-11-2010
20090149455Use of Triazolopyrimidines for Controlling Plant Diseases on Legumes - The triazolopyrimidines of the general formula (I)06-11-2009
200901494562-Pyrimidinyl Pyrazolopyridine ErbB Kinase Inhibitors - The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.06-11-2009
20090143376Fused Heterocyclic Compounds and Their Use as Sirtuin Modulators - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. 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 related to aging or stress, diabetes, obesity, neurodegenerative diseases, chemotherapeutic induced neuropathy, neuropathy associated with an ischemic event, polyglutamine diseases, ocular diseases and/or disorders, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.06-04-2009
20100120763IMIDAZO[5,1-C][1,2,4]BENZOTRIAZINE DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASES - The invention relates to imidazo[5,1-c][1,2,4]benzotriazine derivatives of formula I:05-13-2010
20120035172Purinone 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.02-09-2012
20100130488Pyrazolo-Pyrimidines as Casein Kinase II (CK2) Modulators - A compound according to Formula (I) or a pharmaceutically acceptable salt thereof, wherein R05-27-2010
20100120762Triazine derivatives as inhibitors of phosphodiesterases - The invention relates to triazine derivatives of formula (I):05-13-2010
20100298314NOVEL JNK INHIBITORS - Disclosed are substituted imidazo[1,2-a]pyridines, imidazo[1,2-a]pyrazines, imidazo[1,2-c]pyrimidines and imidazo[1,2-d]triazines compounds of the formula: (1.0) Also disclosed are methods for treating JNK1 and ERK mediated diseases using the compounds of formula 1.0.11-25-2010
20100249127SUBSTITUTED INDOLO-PYRIDINONE COMPOUNDS - The present invention relates to substituted indolo-pyridinone compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted indolo-pyridinone compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.09-30-2010
20110172227ALKYL 3-((2-AMIDOETHYL)AMINO)-8-AZABICYCLO[3.2.1]OCTANE-8-CARBOXYLATE ANALOGS AS SELECTIVE M1 AGONISTS AND METHODS OF MAKING AND USING SAME - In one aspect, the invention relates to compounds having a general structure:07-14-2011
20090163489Inhibitors of PI3 kinase - The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof, that inhibit phosphoinositide 3-kinase;06-25-2009
20090286779PYRAZOLOPYRIMIDINES AS LIPID KINASE INHIBITORS - The invention relates to novel—at least 3,5-disubstituted-pyrazolo[1,5-a]pyrimidines of the formula I,11-19-2009
20100113442TRIAZOLOPYRIDINES AS PHOSPHODIESTERASE INHIBITORS FOR TREATMENT OF DERMAL DISEASES - The present invention relates to a compound according to formula (I), wherein X and Y are either C and N or N and C; Z is CH05-06-2010
20110269754COMPOUNDS AND COMPOSITIONS FOR REDUCING LIPID LEVELS - Compositions comprising extracts or isolated or purified compounds from plants of the genus 11-03-2011
20080287434New amino-alkyl-amide derivatives as CCR3 receptor ligands - The invention relates to a compound of the general formula (I),11-20-2008
20080261970Sufonamides and Uses Thereof - Compounds of formula (I), including methods of making and methods of using are described in formula (I).10-23-2008
20130217682PYRAZOLOPYRIMIDINYL INHIBITORS OF UBIQUITIN-ACTIVATING ENZYME - Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I:08-22-2013
20100324037PHARMACOKINETICALLY IMPROVED COMPOUNDS - A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided:12-23-2010
201100094044-ARYL-2-ANILINO-PYRIMIDINES - The present invention relates to compounds of Formula (Ia) or (Ib), the N-oxide forms, pharmaceutically acceptable addition salts, quaternary amines, stereoisomers, tautomers, racemics, metabolites, prodrugs, hydrates, or solvates thereof,01-13-2011
20080312225Triazolophthalazines - The compounds of formula (I)12-18-2008
20100137300Indolizine Acetic Acid Derivatives as CRTH2 Antagonists - The specific compounds of this list: {7-cyano-2-methyl-1-[4-(morpholine-4-sutfonyl)benzyl]indolizin-3-yl}acetic acid, {1-(3-chloro-4-ethanesulfonylbenzyl)-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-[3-chloro4-(morpholine-4-sulfonyl)benzyl]-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-(3-chloro-4-ethanesulfonylphenylsulfanyl)-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-[3-chloro-4-(morpholine-4-sutfonyl)phenylsutfanyl]-7-cyano-2-methylindolizin-3-yl}acetic acid, {7-cyano-1-(6-fluoroquinolin-2-ylmethyl)-2-methylindolizin-3-yl}acetic acid are ligands of the CRTH2 receptor and are useful in the treatment of respiratory diseases.06-03-2010
20120142680HETEROALKYL LINKED PYRIMIDINE DERIVATIVES - The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to heteroalkyl linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other conditions or disorders associated with kinases.06-07-2012
20120196855OXYGEN LINKED PYRIMIDINE DERIVATIVES - The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases.08-02-2012
20110207728COMPOUNDS FOR TREATING RESPIRATORY SYNCYTIAL VIRUS INFECTIONS - The present invention relates to compounds of formula (I)08-25-2011
20110144100TRIAZOLOPYRIDINE COMPOUNDS AS PIM KINASE INHIBITORS - Compounds of Formula (I): I in which B, R06-16-2011
20090163488FUSED HETEROCYCLE DERIVATIVES AND USE THEREOF - A compound represented by the formula (I):06-25-2009
20090275577IMIDAZOPYRIDINE AND IMIDAZOPYRIMIDINE DERIVATIVES AS ANTIBACTERIAL AGENTS - Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I as disclosed herein can be used in a variety of applications including use as antibacterial agents.11-05-2009
20090005372Triazolophthalazines - The compounds of formula I01-01-2009
20090005374IMIDAZOPYRIDINYL THIAZOLYL HISTONE DEACETYLASE INHIBITORS - A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.01-01-2009
20090318437SUBSTITUTED PYRAZOLO[1,5-a] PYRIDINE COMPOUNDS AND THEIR METHODS OF USE - The present invention is directed to substituted pyrazolo[1,5-a]pyridines and related methods for their synthesis and use.12-24-2009
20090105242Triazolopyridine compounds useful for the treatment of degenerative & inflammatory diseases - Novel triazolopyridine compounds are disclosed that have a formula represented by the following:04-23-2009
20090105243Pyrrolo-Triazine Aniline Compounds Useful As Kinase Inhibitors - Compounds having the formula (I),04-23-2009
20090221570Uses of 2-Phenyl-Substituted Imidazotriazinone Derivatives for Treating Pulmonary Hypertension - The present invention relates to the use of PDE 5 inhibitors generally and in particular of known 2-phenyl-substituted imidazotriazinone derivatives for manufacturing medicaments for the treatment of pathological states which can be treated by raising cGMP levels in certain tissues, such as, for example, of, for example: primary pulmonary hypertension, secondary pulmonary hypertension, pulmonary arterial hypertension, portopulmonary hypertension, hepatopulmonary syndrome, pulmonary hypertension caused by medicaments (amphetamines), interstitial lung disease, pulmonary hypertension occurring with HIV, thromboembolic pulmonary hypertension, pulmonary hypertension in children and neonates, pulmonary hypertension induced by atmospheric hypoxia (altitude sickness), COPD, emphysema, chronic bronchial asthma, mucoviscidosis-related pulmonary hypertension, right heart failure, left heart failure and global failure, and which can be treated by raising cGMP levels in certain tissues, such as, for example, isolated systiolic hypertension (ISH) and hardening of blood vessels, specifically of arterial blood vessels, and combination of PDE 5 inhibitors generally and in particular of known 2-phenyl-substituted imidazotriazinone derivatives with further therapeutic agents in the said indications.09-03-2009
20120077810Inhibitors Of AKT Activity - The instant invention provides for substituted fused pyrimidine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.03-29-2012
20120077809PYRIMIDOPYRIDAZINE DERIVATIVES USEFUL AS P38 MAPK INHIBITORS - A compound formula (IA) or (IB), or a pharmaceutically acceptable thereof; wherein the substituents are defined as in the claims, and their use as P38 MAP kinase.03-29-2012
20090221571HIV INTEGRASE INHIBITORS - Pyridopyrimidine carboxamide compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication:09-03-2009
2009024751511 Beta-HSD1 Modulators - A compound according to Formula A:10-01-2009
20100160311Fungicidal Azolopyrimidines, Process for Their Preparation and Their Use For Controlling Harmful Fungi, and Also Compositions Comprising Them - The present invention relates to azolopyrimidines of the formula I06-24-2010
201001603102,4 (4,6) PYRIMIDINE DERIVATIVES - The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z06-24-2010
20090075999OXYGEN LINKED PYRIMIDINE DERIVATIVES - The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases.03-19-2009
20090048244PYRROLOTRIAZINE COMPOUNDS AS KINASE INHIBITORS - The present invention provides compounds of formula I02-19-2009
20130123254PHARMACEUTICALLY ACCEPTABLE MGLUR5 POSITIVE ALLOSTERIC MODULATORS AND THEIR METHODS OF IDENTIFICATION - The present invention relates to mGluR5 positive allosteric modulators (PAM) and methods for identifying pharmaceutically acceptable compounds with high tolerability and safety, which method comprises the use of at least one non-competitive mGluR5 allosteric modulator which has a shift factor measured at 10 uM glutamate concentration below 3.0,05-16-2013
20120142681HETEROCYCLIC HYDRAZONE COMPOUNDS - The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).06-07-2012
20100216786NEW COMPOUNDS - The present invention relates to the adenosine A08-26-2010
20100240648HEXAHYDRO-PYRROLO-ISOQUINOLINE COMPOUNDS - Certain hexahydro-pyrrolo-isoquinoline compounds are histamine H09-23-2010
20100240647Treatment of Alzheimer's Disease and Related Conditions - Compounds of formula (I) inhibit microtubule affinity regulating kinase (MARK), and hence are suitable for treating diseases associated with abnormal phosphorylation of tau.09-23-2010
201001521804-oxo-4,5-dihydropyrrolo[1,2-A)quinoxaline derivatives as inhibitors of poly(ADP-ribose) polymerase (PARP) - The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.06-17-2010
20130217683INDAZOLES, BENZOTHIAZOLES, BENZOISOTHIAZOLES, BENZISOXAZOLES, AND PREPARATION AND USE THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.08-22-2013
20100210642ACETYLENYL-PYRAZOLO-PYRIMIDINE DERIVATIVES - The present invention relates to compounds of formula (I):08-19-2010
20100210641Organic Compounds - Compounds of formula I: in free or salt or solvate form, where R08-19-2010
20100210640BENZAMIDE DERIVATIVES, THEIR PREPARATION AND USES IN MEDICINE THEREOF - The present invention discloses novel benzamide derivatives represented by general formula (I), their preparation, pharmaceutical compositions containing the derivatives and their use as medicament, especially as a 5-HT08-19-2010
20100222340SUBSTITUTED PYRIDO [1,2-a] ISOQUINOLINE DERIVATIVES - The present invention relates to compounds of formula (I)09-02-2010
20100222339Thiazole pyrazolopyrimidines CRF1 receptor antagonists - The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and use thereof as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological diseases, and metabolic syndrome.09-02-2010
200902867775,6,Fused Pyrrolidine Compounds Useful as Tachykinin Receptor Antagonists - The present invention is directed to certain 5,6-fused pyrrolidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.11-19-2009
20100197682Organic Compounds - 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 proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.08-05-2010
20090258872USE OF ARYL-SUBSTITUTED POLYCYCLIC AMINES AS MEDICAMENTS - The invention relates to therapeutic use of aryl-substituted polycyclic amines of the formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof;10-15-2009
20090048246COMPOUNDS, COMPOSITIONS AND METHODS FOR REDUCING LIPID LEVELS - Compositions comprising extracts or isolated or purified compounds from plants of the genus 02-19-2009
20130131057NEW BICYCLIC COMPOUNDS AS PI3-K AND MTOR INHIBITORS - There is provided compounds of formula (I), wherein A05-23-2013
20110039842COMPOUNDS HAVING ANTIVIRAL PROPERTIES - The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.02-17-2011
20110130396IMIDAZOTHIADIAZOLE DERIVATIVES - Novel imidazo[2,1-b][1,3,4]thiadiazole derivatives of formula (I)06-02-2011
20110118256IMIDAZO [1,2-A] PYRIDIN-3-YL-ACETIC ACID HYDRAZIDES, PROCESSES, USES AND COMPOSITIONS - The invention provides novel imidazo[1,2-a]pyridin-3-yl-acetic acid hydrazides of formula (I) wherein R05-19-2011
20110118255PYRAZOLO[1,5-a]PYRIMIDINES USEFUL AS JAK2 INHIBITORS - The present invention relates to compounds of formula (I) useful as selective inhibitors of JAK2 kinase. The invention also provides pharmaceutical acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various diseases, conditions or disorders. The invention also provides processes for preparing the compounds of the invention.05-19-2011
20110086851SUBSTITUTED QUINAZOLINES AND THEIR USES FOR MYEOLOPROLIFIC AND THROMBOTIC DISEASES - This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 04-14-2011
20110086850RADIOSENSITIZATION OF TUMORS WITH INDAZOLPYRROLOTRIAZINES FOR RADIOTHERAPY - Provided herein is a method of radiosensitizing a tumor in a subject, which comprises administering to the subject a radiosensitizing amount of an indazolpyrrolotriazine of Formula I. Also provided herein is a method of treating a tumor in a subject, which comprises the steps of administering to the subject a radiosensitizing amount of an indazolpyrrolotriazine of Formula I, and a therapeutically effective fraction of radiation.04-14-2011
20110212957INDAZOLES, BENZOTHIAZOLES, AND BENZOISOTHIAZOLES, AND PREPARATION AND USES THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.09-01-2011
20120035171BICYCLIC HETEROCYCLYL DERIVATIVES AS FGFR KINASE INHIBITORS FOR THERAPEUTIC USE - The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.02-09-2012
20100197681Triazolopyridine Compounds and Their Use as Ask Inhibitors - The present invention relates to triazolopyridine compounds according to Formula (I), their use as medicament, for treating autoimmune disorders, inflammatory diseases, cardiovascular diseases and/or neurodegenerative diseases and a process for their preparation.08-05-2010
20110178077Anti-infective compounds - The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.07-21-2011
20110098291ANTAGONIST OF SMOOTHENED - Described herein are compounds, pharmaceutical compositions and methods for the inhibition of Hedgehog signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human and veterinary diseases and disorders.04-28-2011
20110251191USE OF SUBSTITUTED 2, 3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINES FOR THE TREATMENT OF MYELOMA - The present invention relates to the use of 2,3-dihydroimidazo[1,2-c]quinazoline compounds, and of pharmaceutical compositions containing such compounds, for the treatment or prophylaxis of multiple myeloma, as a sole agent or in combination with other one or more other active ingredients.10-13-2011
20110152257ETHYNYL COMPOUNDS USEFUL FOR TREATMENT OF CNS DISORDERS - The present invention relates to ethynyl compounds of formula06-23-2011
20120302565KINASE 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.11-29-2012
20110077243Triazolopyridine Compounds Useful As Kinase Inhibitors - A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula (I), and methods of treating conditions associated with the activity of p38 kinase.03-31-2011
20120302564(1,2,4)TRIAZOLO[4,3-A]QUINOXALINE DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASES - The invention relates to (1,2,4)triazolo[4,3-a]quinoxaline derivatives which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases.11-29-2012
20120202807AZABICYCLOALKANE DERIVATIVES, PREPARATION THEREOF AND USE THEREOF IN THERAPY - The invention relates to compounds of the general formula (I):08-09-2012
20090005373SUBSTITUTED SULFONAMIDO-MACROCYCLES AS TIE2 INHIBITORS AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME - The invention relates to substituted sulfonamido-macrocycles according to the general formula (I):01-01-2009
20110212956Pyrazolopyrimidines for treating CNS disorders - Substituted pyrazolopyrimidine derivatives of formula (I)09-01-2011
201000565112- [ (2-SUBSTITUTED) -IND0LIZIN-3-YL] -2-OXO-ACETAMIDE DERIVATIVES AS ANTIFUNGAL AGENTS - The invention provides compounds of formula (I), and pharmaceutically acceptable salts thereof wherein: R1, R2, R3, R4, R5, R6, R7, X and X03-04-2010
201101522561,2,4-TRIAZOLO[4,3-c]PYRIMIDIN-3-ONE AND PYRAZOLO[4,3-e]-1,2,4-TRIAZOLO[4,3-c]PYRIMIDIN-3-ONE COMPOUNDS FOR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS - Compounds of the Formula I wherein R06-23-2011
20090318436Fused 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.12-24-2009
20110257171NOVEL IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, METHOD FOR THE PREPARATION THEREOF, USE THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE IN PARTICULAR AS MET INHIBITORS - The invention relates to the novel products of formula (I): in which: Ra is H, Hal, aryl or heteroaryl, which are optionally substituted; Rb is H, Rc, —COORc-CO-Rc or —CO—NRcRd; where Rc is alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd is H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.10-20-2011
20110288087FUSED RING COMPOUND AND USE THEREOF - Provided is a novel compound represented by the following formula11-24-2011
20110288086POLYCYCLIC QUINAZOLINES, PREPARATION THEREOF, AND USE THEREOF - At least one active pharmaceutical ingredient is chosen from polycyclic quinazolines of formula V,11-24-2011
20110288085IMIDAZOPYRIDINE AND IMIDAZOPYRAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS - A compound of Formula (I) or Formula (II) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) or Formula (II), and methods of treating conditions associated with the activity of p38 kinase.11-24-2011
20100311740IMIDAZOPYRIDINE DERIVATIVES AS ACID PUMP ANTAGONISTS - This invention relates to newly identified imidazopyridine compounds of formula (I), to the use of such compounds in treating GERD and the like.12-09-2010
20100227860DISALT INHIBITORS OF IL-12 PRODUCTION - This invention relates to disalt nitrogen-heteroaryl inhibitors of IL-12 production, and related methods and pharmaceutical compositions.09-09-2010
20110053930INHIBITORS OF THE BMP SIGNALING PATHWAY - The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation.03-03-2011
20110053929IMIDAZO-, PYRAZOLOPYRAZINES AND IMIDAZOTRIAZINES AND THEIR USE - The invention relates to substituted imidazo-, pyrazolopyrazines and imidazotriazines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of hematological disorders, preferably of leukopenias and neutropenias.03-03-2011
20100286140TRIAZOLOPHTHALAZINES - The compounds of formula I11-11-2010
20100305118PYRIMIDINE INHIBITORS OF KINASE ACTIVITY - Described herein are compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof,12-02-2010
20110082136INHIBITORS OF JANUS KINASES - The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.04-07-2011
201102571733 (3-Pyrimidin-2-ylbenzyl)-1,2,4-triazolo[4,3-b]pyridazine derivatives - Compounds of the formula (I), in which R10-20-2011
201102571723-(3-Pyrimidine-2-yl-benzyl)-[1,2,4] triazolo[4,3-b]pyrimidine derivatives - Compounds of the formula I, in which R10-20-2011
20110082135INHIBITORS OF AKT ACTIVITY - The instant invention provides for substituted [1,2,4]triazolo[4,3-a]-1,5-naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity, especially Akt1 by administering the compound to a patient in need of treatment of cancer.04-07-2011
20110178078SUBSTITUTED 3-ARYLSULFONYL-PYRAZOLO[1,5-A]PYRIMIDINES, SEROTONIN 5-HT6 RECEPTOR ANTAGONISTS AND METHODS FOR THE PRODUCTION AND USE THEREOF - The invention relates to the novel substituted 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines of the general formula 1, pharmaceutically acceptable salts and/or hydrates thereof, serotonin 5-HT07-21-2011
20120309754PYRAZOLOPYRIMIDINE COMPOUNDS AND THEIR USE AS PDE10 INHIBITORS - The present invention relates to a compound represented by formula [I]: wherein: R12-06-2012
20090176778Certain nitrogen containing bicyclic chemical entities for treating viral infections - Provided are certain chemical entities, pharmaceutical compositions, and methods of treatment of a member of the flaviviradae family of viruses such as hepacivirus (Hepatitis C or HCV).07-09-2009
20110190289Imidazolothiadiazoles for Use as Protein Kinase Inhibitors - There is provided compounds of formula (I), wherein Z, M, R08-04-2011
20100029637Chymase Inhibitors - Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase.02-04-2010
20110218196COMPOUNDS OF ESTROGEN-RELATED RECEPTOR MODULATORS AND THE USES THEREOF - The compounds according to formula (VIII), their pharmaceutically acceptable acid or base addition salts, and the uses thereof. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for preparing medicaments for modulating estrogen related receptors (ERR), and treating metabolic diseases, such as high blood fat, fatty liver, hyperglycemia, diabetes, obesity. The substituents of the formula are defined in the description.09-08-2011
20100016303NOVEL PHENYLIMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS - This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.01-21-2010
20100016300Imidazoacridine Compounds for Treating FLT3-Mediated Disorders - A method of treating a FLT3-mediated condition in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof: (I), The conditions that can be treated by the compounds of the present invention and the definitions for the variables in formula (I) are provided herein.01-21-2010
20100016301Inhibitors of bruton's tyrosine kinase - This application discloses 6-Phenyl-imidazo[1,2-a]pyridine and 6-Phenyl-imidazo[1,2-b]pyridazine derivatives according to generic Formulae I-V:01-21-2010
20100029638FUSED HETEROCYCLYC INHIBITOR COMPOUNDS - The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.02-04-2010
20100197684SUBSTITUTED HETEROCYCLIC COMPOUNDS - The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I):08-05-2010
20090176777Imidazo (1,2-a)Pyridin-3-YL-Acetic Acid Hydrazides, Proesses for Their Preparation and Pharmaceutical Uses Thereof - The invention provides novel imidazo[1,2-a]pyridin-3-yl-acetic acid hydrazides of formula (I) wherein R07-09-2009
20110065700POLYSUBSTITUTED DERIVATIVES OF 6-HETEROARYLIMIDAZO[1,2-a]PYRIDINES, AND PREPARATION AND THERAPEUTIC USE THEREOF - Compounds of formula (I):03-17-2011
20110065699POLYSUBSTITUTED DERIVATIVES OF 2-ARYL-6-PHENYL-IMIDAZO[1,2-a]PYRIDINES, AND PREPARATION AND THERAPEUTIC USE THEREOF - Compounds of formula (I):03-17-2011
20120040979IMIDAZO[1,2-B]PYRIDAZINES, PROCESSES, USES, INTERMEDIATES AND COMPOSITIONS - The invention provides novel imidazo[1,2-b]pyridazines of formula (I) and pharmaceutically acceptable salts, polymorphs, hydrates, tautomers, solvates and stereoisomers thereof.02-16-2012
20100035875TRIAZOLOPYRIDINE JAK INHIBITOR COMPOUNDS AND METHODS - A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R02-11-2010
20090069315Use of Pyrazolo(1,5A)Pyrimidin-7-YL Amine Derivatives in the Treatment of Neurological Disorders - The invention relates to methods of using the compounds of the invention, including pyrazolo[1,5a]pyrimidin-7-yl amine compounds and salts thereof, as well as pharmaceutical compositions comprising the same, in the treatment of Eph receptor-related (e.g., neurological) injuries and disorders. The invention also relates to modulating the activity of an Eph receptor in a cell, stimulating neural regeneration, and reversing neuronal degeneration, by administering a compound of the invention to a cell or subject in an effective amount.03-12-2009
20120046282METHODS AND COMPOUNDS FOR ANTIMICROBIAL INTERVENTION - The present invention provides Wall Teichoic Acid biosynthesis inhibitors such as compound 1835F03 (targocil) and related synthetic analogs. The invention also provides pharmaceutical compositions thereof and methods for treating bacterial infection and the suppression of growth of bacterial cells by administering a Wall Teichoic Acid biosynthesis inhibitor. The invention is particularly useful for the treatment of Methicillin-resistant 02-23-2012
20120004223COMPOUNDS, COMPOSITIONS AND METHODS FOR REDUCING LIPID LEVELS - The present technology relates to compounds of Formulas (V) and (VI) and methods of making and using such compounds. Methods of use include prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Compounds disclosed herein also lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression, inhibit PCSK9 expression, and activate AMP-activated protein kinase.01-05-2012
20120004222CB2 RECEPTOR LIGANDS FOR THE TREATMENT OF PAIN - The present invention relates to compounds represented by Formula (I) and Formula (II):01-05-2012
20120208810NOVEL 1,2,3,4-TETRAHYDRO-PYRIMIDO(1,2-A)PYRIMIDIN-6-ONE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL USE THEREOF - The invention relates to the novel materials of formula (I), where: R08-16-2012
20110166133FUSED NITROGEN CONTAINING HETEROCYCLES AND COMPOSITIONS THEREOF AS KINASE INHIBITORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Ros, KDR, FMS, C-FMS, FLT3, c-Kit, JAK2, JAK3, Aurora, PDGFR, Lck, TrkA, TrkB, TrkC, IGF-IR, ALK4, ALK5 and ALK or combinations thereof.07-07-2011
20090099166C10-substituted camptothecin analogs - The novel C10-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW<600).04-16-2009
20120058999Substituted Tetrahydropyrrolopyrazine Compounds - Tetrahydropyrrolopyrazine compounds, methods for their preparation, pharmaceutical compositions containing such compounds, and a method of using such compounds for the treatment of pain and other conditions mediated at least partially by Bradykinin 1 receptors (B1R).03-08-2012
20080300245Pyrazolo[1,5-A]Pyridine-3-Carboxylic Acids as Ephb and Vegfr2 Kinase Inhibitors - The invention relates to novel pyrazolo[1,5a]pyridine-3-carboxylic acid compounds of the formula12-04-2008
20120071474INHIBITORS OF PI3 KINASE - The present invention relates to compounds of Formula I, II or III or a pharmaceutically acceptable salt thereof;03-22-2012
20120157451RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF - Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.06-21-2012
201100924983-(3-PYRIMIDIN-2-YLBENZYL)-1,2,4-TRIAZOLO[4,3-B]PYRIDAZINE DERIVATIVES AS MET KINASE INHIBITORS - Compounds of the formula (I), in which R04-21-2011
20110092497IMIDAZOLOPYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following:04-21-2011
20100197683FUSED RING COMPOUND AND USE THEREOF - Provided is a novel compound represented by the following formula08-05-2010
20120135987NOVEL PHENYLIMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS - This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.05-31-2012
20120135986Bicyclic Heteroaryl Compounds - This invention relates to compounds of the general formula:05-31-2012
20100093719PHARMACOKINETICALLY IMPROVED COMPOUNDS - A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided:04-15-2010
20090131425INHIBITORS OF PROTEIN KINASES - Compounds that inhibit Aurora-kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.05-21-2009
201101839713,4-DIHYDRO-2H-PYRAZINO[1,2-A]INDOL-1-ONE DERIVATIVES ACTIVE AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM - Compounds which are 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.07-28-2011
20120129850IMIDAZOLOTHIAZOLE COMPOUNDS FOR THE TREATMENT OF DISEASE - Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.05-24-2012
20120165326DERIVATIVES OF 6-(6-SUBSTITUTED-TRIAZOLOPYRIDAZINE-SULFANYL) 5-FLUORO BENZOTHIAZOLES AND 5-FLUORO BENZIMIDAZOLES, PREPARATION THEREOF, USE THEREOF AS DRUGS, AND USE THEREOF AS MET INHIBITORS - The invention relates to novel products of the formula (I) where: (II) is a single or double bond; F is a fluorine atom, Ra is H, HaI, alkoxy, O-cycloalkyl, —O— heterocycloalkyl; —NH-heterocycloalkyl, heteroaryl, phenyl, NHCOalk NHCOcycloalk or NR1 R2; X is S, SO or SO2, A is NH or S; W is H, alkyl, or COR with R being cycloalkyl; alkyl optionally substituted by NR3R4, alkoxy, hydroxy, phenyl, heteroaryl or heterocycloalkyl; alkoxy optionally substituted by NR3R4, i.e. a O—(CH2)n-NR3R4 radical, an O-phenyl or an O—(CH2)n-phenyl radical, with phenyl optionally substituted and n=1 to 4; or the NR1 R2 radical; R1 is H or alk and R2 is H, cycloalkyl or alkyl; R3 and R4 are H, alk, cycloalkyl, heteroaryl or phenyl; R1, R2 and/or R3, R4 form a cycle together with N optionally containing O, S, N and/or NH; heterocycloalkyl, heteroaryl and phenyl and cycles all being optionally substituted; wherein said products can be in any isomer or salt form, and can be used as drugs, in particular as MET inhibitors.06-28-2012
20100048557Triazolopyridine JAK Inhibitor Compounds and Methods - A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R02-25-2010
20100048555IMIDAZOTHIAZOLE DERIVATIVES AS MARK INHIBITORS - Compounds of formula (I): are inhibitors of MARK, and hence useful for treatment of disorders involving 10 hyperphosphorylation of tau.02-25-2010
201201787512-ARYLIMIDAZO[1,2-B]PYRIDAZINE, 2-PHENYLIMIDAZO[1,2-A]PYRIDINE, AND 2-PHENYLIMIDAZO[1,2-A]PYRAZINE DERIVATIVES - Disclosed are compounds of formula (I):07-12-2012
20100273792MACROCYCLIC INDOLES AS HEPATITIS C VIRUS INHIBITORS - The present invention relates to inhibitors of HCV replication of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof,10-28-2010
20100009985THERAPEUTICALLY USEFUL SUBSTITUTED HYDROPYRIDO [3,2,1-ij] QUINOLINE COMPOUNDS - Disclosed herein are compounds represented by the structural formula:01-14-2010
20100286139AMINO PYRAZOLE COMPOUND - The present invention provides amino pyrazole compounds useful in the treatment of chronic myeloproliferative disorders and various cancers, e.g., glioblastoma, breast cancer, multiple myeloma, prostate cancer, and leukemias.11-11-2010
20100292232NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS - Disclosed herein are antiviral agents, in particular non-nucleoside reverse transcriptase inhibitors (NNRTIs) of the formula11-18-2010
20100292231Indazole Compounds for Treating Inflammatory Disorders, Demyelinating Disorders and Cancers - Compounds of formula (I) or formula (Ia) and a method of treating a patient suffering from certain inflammatory disorders, demyelinating disorders, FLT3-mediated disorders, CSF-1R-mediated disorders, cancers and leukemias, comprising administering to said patient a therapeutically effective amount of a compound of formula (I) or formula (Ia) or a pharmaceutically acceptable salt thereof.11-18-2010
20120220582IMIDAZOPYRAZINE SYK INHIBITORS - Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.08-30-2012
20120083492IMIDAZOPYRAZINES FOR USE AS KINASE INHIBITORS - There is provided compounds of formula (I), wherein R04-05-2012
20090018127Ergoline Derivatives - Disclosed are ergoline derivatives, Formula (I), wherein either each of R01-15-2009
20090018128Compounds - The present invention relates to novel pyrrolopyrazine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor.01-15-2009
20110124640FUSED HETEROCYCLIC COMPOUNDS USEFUL AS KINASE MODULATORS - Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation, wherein R05-26-2011
20120232075Fused Pyrazine Compounds Useful for the Treatment of Degenerative and Inflammatory Diseases - Novel fused pyrazine compounds are disclosed that have a formula represented by the following:09-13-2012
20120232076QUINOLIZIDINONE CARBOXAMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.09-13-2012
20110003808OCTAHYDROQUINOLIZINES FOR ANTIDIABETIC TREATMENT - This invention relates to novel octahydroquinolizines for treatment or prevention of diabetes mellitus and its complications, for treatment or prevention of hyperlipidemia, for treatment of diabetic dyslipidemia, for treatment or prevention of the metabolic syndrome, for treatment of diseases related to metabolic dysfunction, for treatment of obesity or obesity-related diseases. The invention also includes pharmaceutical compositions and kits comprising these compounds alone or in combination with other drugs or compounds aiming towards an improved treatment or prevention of the aforementioned diseases or syndromes in humans or animals.01-06-2011
20110003806Heteroaryls and uses thereof - This invention provides compounds of formula IA or IB:01-06-2011
20110046130TETRAHYDRONAPHTHYRIDINES AND AZA DERIVATIVES THEREOF AS HISTAMINE H3 RECEPTOR ANTAGONISTS - The invention relates to compounds of formula (I), wherein X02-24-2011
20100227861IMIDAZO[1,2-beta]PYRIDAZINE AND PYRAZOLO[1,5-alpha]PYRIMIDINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS - The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II):09-09-2010
20120277225INHIBITORS OF BRUTON'S TYROSINE KINASE - Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.11-01-2012
20120277224HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK - Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.11-01-2012
20110251192AMIDE COMPOUNDS, THEIR PHARMACEUTICAL COMPOSITIONS, THEIR PREPARATION METHOD AND THEIR USES - The present invention pertains to the field of pharmaceutical chemistry and discloses 8-(3-aminopropyl)-3-exo-8-azabicyclo[3.2.1]octane-3-amino amide compounds represented by formula I, the pharmaceutical compositions, the preparation method and the use thereof. Such compounds or pharmaceutically acceptable salts thereof can be used as an antagonist of CCR5 in preparing medicaments for treating diseases mediated by CCR5, particularly HIV infection, asthma, rheumatoid arthritis, autoimmune diseases and chronic obstructive pulmonary diseases (COPD).10-13-2011
201103194062-PYRIDYL SUBSTITUTED IMIDAZOLES AS THERAPEUTIC ALK5 AND/OR ALK4 INHIBITORS - This invention relates to 2-pyridyl substituted imidazoles which are inhibitors of the transforming growth factor-β (TGF-β) type I receptor (ALK5) and/or the activin type I receptor (ALK4), methods for their preparation, and their use in medicine, specifically in the treatment and prevention of a disease state mediated by these receptors.12-29-2011
20110319408Methods of Treating Fibrosis, Cancer and Vascular Injuries - This invention relates to use of inhibitors of the transforming growth factor-β (TGF-β) type I receptor (ALK5) and/or the activin type I receptor (ALK4) in treating, preventing, or reducing fibrosis, cancer, and vascular injuries.12-29-2011
20110319407INDAZOLES, BENZOTHIAZOLES, BENZOISOTHIAZOLES, BENZISOXAZOLES, AND PREPARATION AND USE THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.12-29-2011
20100152181AMINO PYRAZOLE COMPOUND - The present invention provides amino pyrazole compounds useful in the treatment of chronic myeloproliferative disorders and various cancers, e.g., glioblastoma, breast cancer, multiple myeloma, prostate cancer, and leukemias.06-17-2010
20090131426SOLID FORMS COMPRISING N-(5-TERT-BUTYL-ISOXAZOL-3-YL)-N'-UREA, COMPOSITIONS THEREOF, AND USES THEREWITH - Solid forms comprising N-(5-tert-butyl-isoxazol-3-yl)-N′-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders are disclosed.05-21-2009
20130012506ANTI-INFECTIVE PYRIDO (1,2-A) PYRIMIDINES - The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.01-10-2013
20100173906Substituted 3,4,6,7-Tetrahydro-5H-1,2a,4a,8-Tetraazacyclopenta[cd]Phenalenes and Methods - Substituted 3,4,6,7-tetrahydro-5H-1,2a,4a,8-tetraazacyclopenta[cd]phenalene-9-amines, pharmaceutical compositions containing the compounds or salts thereof, intermediates, methods of making the compounds or salts thereof, and methods of use of these compounds or salts thereof or pharmaceutical compositions as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.07-08-2010
20100130489IMIDAZOLO-HETEROARYL DERIVATIVES WITH ANTIBACTERIAL PROPERTIES - The invention relates to Imidazolo-heteroaryl derivatives of formula (I). The compounds inhibit the activity of the Dlta enzyme of Gram-positive bacteria and are useful to treat Gram-positive bacterial infections. Furthermore the application discloses method for assessing the Dlta inhibitory activity of tested molecules and a method for measuring the efficacy of molecules in inhibiting bacteria proliferation in vitro.05-27-2010
20120149699IMIDAZO[1,2-a]PYRIDINE SULFONAMIDES 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:06-14-2012
20130023530NOVEL NK-3 RECEPTOR SELECTIVE ANTAGONIST COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN NK-3 RECEPTORS MEDIATED DISORDERS - The present invention is directed to novel compounds of formula I01-24-2013
20110263594NOVEL TRIAZOLO(4,3-A)PYRIDINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF, USE THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE, IN PARTICULAR AS MET INHIBITORS - The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, —COORc-CO-Rc or —CO—NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.10-27-2011
20110263592IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - Imidazo[1,2-α]pyridine derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT10-27-2011
20130172338OXYGEN LINKED PYRIMIDINE DERIVATIVES - The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases.07-04-2013
20130096113HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF - Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFRβ kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.04-18-2013
20130096114PHARMACOKINETICALLY IMPROVED COMPOUNDS - A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided:04-18-2013
20130116249INDOLIZINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to compounds corresponding to formula (I):05-09-2013
20130116250IMIDAZOPYRIDINE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to compounds corresponding to formula (I):05-09-2013
20110275628NOVEL PYRAZOLE-3-CARBOXAMIDE DERIVATIVE HAVING 5-HT2B RECEPTOR ANTAGONIST ACTIVITY - Disclosed is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, which is useful as a selective antagonist of a 5-HT11-10-2011
20110275627INDOLIZINE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I):11-10-2011
20110237582PYRIDO[3,4-B]INDOLES AND METHODS OF USE - This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.09-29-2011
20130150362NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS - The present invention relates to certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrimidine compounds.06-13-2013
20130150360INHIBITORS OF BRUTON'S TYROSINE KINASE - This application discloses compounds according to generic Formula I:06-13-2013
20130150361KINASE INHIBITORS - Compounds of formula (I):06-13-2013
20100292233DIHYDRO-1H-PYRROLO[1,2-A]INDOL-1-YL CARBOXYLIC ACID DERIVATIVES WHICH ACT AS S1P1 AGONISTS - The present invention relates to certain (1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl carboxylic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, sepsis, myocardial infarction, ischemic stroke, acne, microbial infections or diseases and viral infections or diseases.11-18-2010
20100298315NOVEL 6-TRIAZOLOPYRIDAZINESULFANYL BENZOTHIAZOLE AND BENZIMIDAZOLE DERIVATIVES, METHOD FOR PRODUCTION THEREOF AND APPLICATION AS MEDICAMENTS AND PHARMNACEUTICAL COMPOSITIONS AND NOVEL USE AS MET INHIBITORS - The disclosure relates to compounds of formula (I):11-25-2010
20130184273BICYCLIC PYRIMIDINES - Compounds of formula (I), which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.07-18-2013
20130158025NOVEL COMPOUND ACTING AS A CANNABINOID RECEPTOR-1 INHIBITOR - Disclosed is a novel compound acting as a cannabinoid receptor 1 inhibitor, a prodrug thereof, an isomer thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof. The novel compound or the like is useful for preventing or treating diseases mediated by the cannabinoid receptor-1.06-20-2013
20110312957IMIDAZOPYRIDINES AND IMIDAZOPYRIMIDINES AS HIV-I REVERSE TRANSCRIPTASE INHIBITORS - The invention provides compounds of formula A or B which are useful in the treatment of a subject infected with HIV.12-22-2011
20130190308PYRIDO[3,4-B]INDOLES AND METHODS OF USE - This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.07-25-2013
20120028975SUBSTITUTED TRIAZOLOPYRIDINES AND ANALOGS THEREOF - The present invention relates to substituted triazolopyridines and analogs thereof, the use of the compounds as phosphodiesterase 10 (PDE10) inhibitors for the treatment of PDE10-modulated disorders, to pharmaceutical compositions comprising the compounds.02-02-2012
20120028974TRIAZOLOPYRIDINES AS PHOSPHODIESTERASE INHIBITORS FOR TREATMENT OF DERMAL DISEASES - The present invention relates to a compound according to formula I, wherein R02-02-2012
201301969843-AMINO-5-PHENYL-56-DIHYDRO-2H-[1,4]OXAZINES - The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I08-01-2013
20130196986TRIAZOLOPYRAZINONES AS P2X7 RECEPTOR ANTAGONISTS - The invention provides certain 3,7-disubstituted-[1,2,4]triazolo[4,3-a]pyrazin-8(7H)-ones of the Formula (I), and their pharmaceutically acceptable salts, wherein R08-01-2013
20130196985HETEROCYCLIC ALKYNYL BENZENE COMPOUNDS AND MEDICAL COMPOSITIONS AND USES THEREOF - The heterocyclic alkynyl benzene compounds of formula (I), their pharmaceutically acceptable salts and stereoisomers thereof, as well as application in preparing drugs for preventing or treating tumors. The compounds can overcome the clinically induced resistance against Gleevec.08-01-2013
20090048245Imidazolopyridine compounds useful for the treatment of degenerative and inflammatory diseases - Novel imidazolopyridine compounds are disclosed that have a formula represented by the following:02-19-2009
201302037542-Aryl Imidazo[1,2-a]Pyridine-3-Acetamide Derivatives, Preparation Methods and Uses Thereof - Disclosed are 2-arylimidazo[1,2-08-08-2013
20100016302Inhibitors of bruton's tyrosine kinase - This application discloses 6-Phenyl-imidazo[1,2-a]pyrazine derivatives according to generic Formulae I-V:01-21-2010
20120094996Imidazo [2, 1-B] [1, 3, 4] Thiadiazole Derivatives - There is provided compounds of formula (I): wherein R04-19-2012
201200949952-AZA-BICYCLO[2.2.1]HEPTANE COMPOUNDS AND USES THEREOF - This invention relates to 2-aza-bicyclo[2.2.1]heptane compounds (and salts thereof), the process for making such a compound and pharmaceutical compositions comprising such a compound. The invention also relates to the use of the compounds for modulating the glycine transporter 1 (GlyT1) and for the treatment of psychosis, cognitive disorders, bipolar disorders, depression disorders, anxiety disorders, post-traumatic stress disorders and pain.04-19-2012

Patent applications in class Ring nitrogen shared by two of the cyclos