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

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

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

514210010 - Hetero ring is four-membered and includes at least one ring nitrogen

514210190 - Additional hetero ring attached directly or indirectly to the four-membered hetero ring by nonionic bonding

514210200 - The additional hetero ring contains ring nitrogen

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Entries
DocumentTitleDate
20130045965INHIBITORS OF BRUTON'S TYROSINE KINASE - This application discloses compounds according to generic Formula I:02-21-2013
20130029969HETEROCYCLIC COMPOUND - Provided is a compound useful for the prophylaxis or treatment of cancer.01-31-2013
20130029967Fused Imidazo [3,2 - D] Pyrazines as P13 Kinase Inhibitors - There is provided compounds of formula (I), wherein A01-31-2013
20130029968INDAZOLES - The present invention relates to compounds of formula (I):01-31-2013
20120184526COMPOUNDS AND COMPOSITIONS AS SYK KINASE INHIBITORS - Provided herein are a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated Syk kinase activity.07-19-2012
201201845251,2,3-TRIAZOLO [4,3-A] PYRIDINE DERIVATIVES AND THIER USE FOR THE TREATMENT OF PREVENTION OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS - The present invention relates to novel triazolo[4,3-07-19-2012
20120184524PYRAZOLOPYRIDINE 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.07-19-2012
20090143353ANTIFUNGAL BICYCLIC HETERO RING COMPOUNDS - A 1,6-β-glucan synthetase inhibitor is provided, having potent growth inhibition and having excellent safety.06-04-2009
20090192138 COMPOUNDS - The invention provides novel deazaxanthine and deazahypoxanthine compounds. The compounds may be useful in the therapy of diseases and conditions in which dipeptidylpeptidase-IV (DPP-IV) is implicated.07-30-2009
201101959492-BENZOTHIOPHENYL- AND 2-NAPHTHYL-OXAZOLIDINONES AND THEIR AZAISOSTERE ANALOGUES AS ANTIBACTERIAL AGENTS - The invention relates to antibacterial compounds of formula (I)08-11-2011
20100113415EPHA4 RTK INHIBITORS FOR TREATMENT OF NEUROLOGICAL AND NEURODEGENERATIVE DISORDERS AND CANCER - The present invention is directed to compounds of generic formula (I)05-06-2010
20130079330Fused Thiazole Derivatives as Kinase Inhibitors - A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.03-28-2013
20130079329INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/Beta-CATENIN SIGNALING PATHWAY INHIBITORS - Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.03-28-2013
20130029966SUBSTITUTED OXINDOLE DERIVATIVES, MEDICAMENTS CONTAINING SAID DERIVATIVES AND USE THEREOF - The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R01-31-2013
20130040934SPIROCYCLIC COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS AND DIAGNOSTIC PROBES - The invention relates to new triazines (G=Q=U are N), pyrimidines (two out of G, Q and U are N), and pyridopyrimidines (one of G and U together with R2 forms an anullated pyridine ring) of formula (I) carrying a spirocyclic substituent, wherein E02-14-2013
20090186869Antiviral compounds - The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.07-23-2009
20120264737Heterocyclic Modulators of Lipid Synthesis - Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.10-18-2012
20100041636NOVEL KINASE INHIBITORS - The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts thereof. The Formula (I) compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1 and IGFR-1, thereby making them useful as anti-cancer agents. The formula (I) compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.02-18-2010
20100041635OXINDOLE COMPOUNDS - The invention provides compounds that inhibit PIM kinases and Flt3 kinase, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation.02-18-2010
20100105654SUBSTITUTED QUINAZOLINONE COMPOUNDS - A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the structures VA, VB, VIIA and VIIB where the values of the variables are defined herein.04-29-2010
20100105656TRIAZOLOPYRAZINE DERIVATIVES - The invention relates to compounds of the formula I04-29-2010
20100105655NOVEL COMPOUNDS 515 - There is provided novel pyrimidine derivatives of formula (I)04-29-2010
20100105653PYRROLOPYRIMIDINE COMPOUNDS AND THEIR USES - The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.04-29-2010
20100105652PURINES AS CYSTEINE PROTEASE INHIBITORS - Substituted heteroaryl nitrile salt of Formula I,04-29-2010
20100120741HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE - The present invention relates to compounds and methods which may be useful as inhibitors of H05-13-2010
20120214791Imidazo[5,1-f][1,2,4]Triazines for the Treatment of Neurological Disorders - The present invention relates to compounds of the Formula08-23-2012
20100331307THERAPEUTIC COMPOUNDS AND COMPOSITIONS - Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.12-30-2010
20100093698AMINOTRIAZOLOPYRIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH - Provided herein are Heteroaryl Compounds of formula (I):04-15-2010
20090197864Furo- and Thieno [3,2-c] Pyridines - Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula I, and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET.08-06-2009
201000693525- [4-(AZETIDIN-3-YLOXY)-PHENYL]-2-PHENYL-5H-THIAZOLO[5,4-C] PYRIDIN-4-ONE DERIVATIVES AND THEIR USE AS MCH RECEPTOR ANTAGONISTS - The present invention relates to a melanin concentrating hormone antagonist compound of formula I: wherein “ - - - ” is absent or is optionally a bond; q is 1 or 2; R03-18-2010
20100069351SPIRO COMPOUND AND USE THEREOF - The present invention aims to provide a novel SCD inhibitor.03-18-2010
20100130468INDOLE CARBOXAMIDES AS IKK2 INHIBITORS - The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I):05-27-2010
201001304692, 6-NAPHTHRIDINE DERIVATIVES - The present invention relates to novel organic compounds comprising a naphthyridine which may be mediators of a selective subset of kinases belonging to the AGC kinase family, such as for example PKC, PKD, PKN-1/2, CDK-9, MRCK-beat, PASK, PRKX, ROCK-I/II or mediators of other kinases, the selectivity of which would be depending on the structural variation thereof.05-27-2010
20090093454Chemical Compounds - The present invention provides compounds of Formula (I) comprising:04-09-2009
20130072470NOVEL TRICYCLIC COMPOUNDS - The invention provides compounds of Formula (I)03-21-2013
20110015175Bicyclic Compounds for the Reduction of Beta-Amyloid Production - The present disclosure provides a series of compounds of the formula (I)01-20-2011
20130059836PYRAZOLOPYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER - Compound of Formula (I): are described, along with pharmaceutically acceptable salts thereof, compositions containing the same, and methods of use thereof in the treatment of cancer.03-07-2013
20090270362BICYCLIC MGLUR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME - In one aspect, the invention relates to bicyclic MGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.10-29-2009
200902703632-Aryl- and 2-Heteroarylthiazolyl Compounds, Methods for Their Preparation and Use Thereof - The present invention discloses fused bicyclic 2-aryl- or 2-heteroarylthiazolyl compounds and their pharmaceutically acceptable salts and esters thereof, which are useful for inhibiting the growth of cancerous cells, inhibiting human breast carcinoma tumor growth in particular and to treat diseases or disorders associated with securin, including elevated securin levels.10-29-2009
20130065883Triazolo [4, 5- B] Pyridin Derivatives - There is provided compounds of formula (I), wherein R03-14-2013
20130065881Tricyclic Compounds for Use as Kinase Inhibitors - There is provided compounds of formula (I), wherein R03-14-2013
20130065882VLA-4 inhibitory drug - This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof:03-14-2013
20110021495QUINAZOLES USEFUL AS MODULATORS OF ION CHANNELS - The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.01-27-2011
20110021493SUBSTITUTED TRICYCLIC COMPOUNDS AND METHODS OF USE THEREOF - 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
20110046110QUINOLINES AND RELATED ANALOGS 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, 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.02-24-2011
20120115846QUINAZOLINEDIONE DERIVATIVES, PREPARATION THEREOF AND VARIOUS THERAPEUTIC USES THEREOF. - The subject matter of the invention is quinazolinedione derivatives of formula (I), methods for obtaining same and therapeutic uses thereof, such as cancer, diabetes, muscle diseases, bone diseases, cardiovascular diseases, central nervous system diseases, peripheral nervous system diseases, inter alia.05-10-2012
20090012056Quinoline Compounds Capable of Binding the Cb2 and/or the 5-Ht6 Receptor - The present invention relates to novel quinoline derivatives such as compounds of the formula (I) which possess antagonist potency for the 5-HT01-08-2009
20090012055Organic compounds - Novel substituted piperidines of the general formulae (I) and (II)01-08-2009
20130165424DISPIROPYRROLIDINE DERIVATIVES - A compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R06-27-2013
20120238545TRICYCLIC PYRAZOL AMINE DERIVATIVES - This invention relates to compounds of Formula (I*) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers.09-20-2012
20120238544THIENO- AND FURO-PYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR - Thieno- and furo-pyrimidine compounds are described, which are useful as H09-20-2012
20120238543Antiviral Compounds - Novel compounds, methods, and compositions for treating various viral infections are described. In some embodiments the novel compounds of the invention are 3-oxo-phenothiazine derivatives; more specific embodiments include 3-oxo-phenothiazine derivatives having substituents at the 1-, 7-, and 9-positions of the phenothiazine parent ring. In other embodiments, the invention provides compositions and methods for treating viral infections, especially HIV.09-20-2012
20120238542AMINOPYRAZOLOQUINAZOLINES - Compounds of general formula (I)09-20-2012
20080293688AMINOAZACYCLYL-3-SULFONYLINDAZOLES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS - The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.11-27-2008
20090082332PURINE DERIVATIVES FOR THE TREATMENT OF VIRAL OR ALLERGIC DISEASES AND CANCERS - The present invention provides compounds of formula (I)03-26-2009
20100280002AMINOPYRIDINE-DERIVATIVES AS INDUCTIBLE NO-SYNTHASE INHIBITORS - The compounds of Formula (I)11-04-2010
20100292207SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS - Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.11-18-2010
20100317650IMIDAZOPYRIDINE DERIVATIVES USEFUL AS INOS INHIBITORS - The compounds of formula (I)12-16-2010
20110281841Kinase Inhibitors - The present invention provides a new group of protein kinase inhibitors, pyrropyrimidine and pyrazolopyrimidine derivatives, and pharmaceutically acceptable salts and prodrugs thereof that are useful for treating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrropyrimidine and pyrazolopyrimidine derivatives.11-17-2011
20110281843SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS - Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.11-17-2011
20110281842PYRROLOPYRIDINE AND PYRROLOPYRIMIDINE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts,11-17-2011
20110144085TRIAZOLOPYRIDINE COMPOUNDS AS PIM KINASE INHIBITORS - Compounds of Formula (I), in which A, B, R06-16-2011
20110144083Xanthine Derivatives, the Preparation Thereof and Their Use as Pharmaceutical Compositions - The present invention relates to substituted xanthines of general formula06-16-2011
201002676894-AZETIDINYL-1-PHENYL-CYCLOHEXANE ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula (I):10-21-2010
20110301146GLYCOGEN SYNTHASE KINASE-3 BETA INHIBITORS CONTAINING 7-HYDROXY-BENZOIMIDAZOLE-4-YL-METHANONE DERIVATIVES - GSK-3beta inhibitors comprising 7-Hydroxy-benzoimidazole-4-yl-methanone Derivatives are provided. For example, the inhibitors have following general formula (I).12-08-2011
20110301144Kinase Antagonists - The present invention provides novel compounds that are antagonists of PI3 kinase, PI3 kinase and tyrosine kinase, PI3 kinase and mTOR, or PI33 kinase, mTOR and tyrosine kinase.12-08-2011
20110028452PYRIDO[4,3-d]PYRIMIDIN-4(3H)-ONE DERIVATIVES AS CALCIUM RECEPTOR ANTAGONISTS - The present invention is directed to novel pyrido[4,3-d]pyrimidin-4(3H)-one derivatives and pharmaceutically acceptable salts thereof of structural formula I02-03-2011
20110301145PYRIDAZINONES, METHOD OF MAKING, AND METHOD OF USE THEREOF - Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.12-08-2011
20110166124TRICYCLIC SPIROCYCLE DERIVATIVES AND METHODS OF USE - The present invention relates to novel Tricyclic Spirocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Spirocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or aired fasting glucose.07-07-2011
20110288069Benzodiazepine and Pyridodiazepine Derivatives - The present application relates to benzodiazepine and pyridodiazepine derivatives of formula (I)11-24-2011
20110294781PYRAZOLO-PYRIMIDINE COMPOUNDS - The present invention has searched for a variety of compounds which show IL-12/IL-23 production-inhibitory activities and herein provides a pharmaceutical composition and an agent for preventing or treating IL-12/IL-23 excess production-related diseases, which comprise the compound.12-01-2011
20110294780SUBSTITUTED THIAZOLIDINEDIONE INDAZOLES, INDOLES AND BENZOTRIAZOLES AS ESTROGEN-RELATED RECEPTOR-a MODULATORS - The present invention relates to compounds of Formula (I),12-01-2011
20100298290Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture - The invention is directed to Compounds of Formula I:11-25-2010
20090281076Azetidine Derivatives as G-Protein Coupled Receptor (GPR119) Agonists - Compounds of formula (I) or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful for the treatment of diabetes and as peripheral regulators of satiety, e.g. for the treatment of obesity and metabolic syndrome.11-12-2009
20100035858Novel Compositions and Methods for Binding and Inhibiting 5-HT4 Receptor - The present invention relates to compositions that bind to 5-HT4 receptors and inhibit proliferation of activated lymphocytes. The invention also provides methods for inhibiting proliferation and inducing cell death in activated immune cells, as well methods for treating diseases associated with activated immune cells by administering 5-HT4 receptor ligands.02-11-2010
20090253679NEW IMIDAZOLONE DERIVATIVES, PREPARATION THEREOF AS DRUGS, PHARMACEUTICAL COMPOSITIONS, AND USE THEREOF AS PROTEIN KINASE INHIBITORS, IN PARTICULAR CDC7 - The present invention relates to imidazolone derivatives of formula (I)10-08-2009
20100113416JANUS KINASE INHIBITORS FOR TREATMENT OF DRY EYE AND OTHER EYE RELATED DISEASES - Methods, kits, and compositions for treating dry eye disorders and other related eye diseases are provided, wherein the methods, kits, and compositions utilize a JAK inhibitor.05-06-2010
20110263561Novel pyrrolidone derivatives for use as MetAP-2 inhibitors - Compounds of the formula (I), in which R, X, Y, Z, R10-27-2011
20100113417Substituted Spiroamine Compounds - Substituted spiroamine compounds corresponding to the formula (I)05-06-2010
20090149441DERIVATIVES OF IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS - The present invention is related to a compound of formula (I):06-11-2009
20110269739KINASE INHIBITORS - The present invention provides a new group of protein kinase inhibitors, pyrido[4,3,-d]pyrimidin-5-one derivatives, and pharmaceutically acceptable salts thereof that are useful for intreating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrido[4,3,-d]pyrimidin-5-one derivatives.11-03-2011
20110201595OXAZOLIDINYL ANTIBIOTICS - The invention relates to antibacterial compounds of formula I08-18-2011
20090149440NOVEL PYRIDONECARBOXYLIC ACID DERIVATIVES OR SALTS THEREOF - The present invention provides an agent which exhibits excellent antibacterial activity, low toxicity, improved bioavailability, and low binding rate to serum proteins. The present invention is directed to a pyridonecarboxylic acid derivative represented by formula (1):06-11-2009
20120190666Heteroaryl Compounds as PIKK Inhibitors - The present invention provides compounds that are PIKK inhibitors, more specifically, mTOR and/or PI3Kα kinase inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of kinases, specifically PI3 kinases, more specifically, mTOR and/or PI3Kα, such as cancer. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.07-26-2012
201102635667-Hydroxy-benzoimidazole-4-yl-methanone Derivatives and PBK Inhibitors Containing the Same - 7-Hydroxy-benzoimidazole-4-yl-methanone Derivatives, which are useful for PBK inhibitors, are provided.10-27-2011
20110263563Ansamycin Hydroquinone Compositions - Aspects of the present invention provide compositions comprising a sulfur containing compound and a compound of the formula (I); and also provide methods of their preparation and use.10-27-2011
20120035154Modulators of Cellular Adhesion - The present invention provides compounds having formula (I):02-09-2012
201002676884-AZETIDINYL-1-HETEROARYL-CYCLOHEXANE ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula (I).10-21-2010
20090258855BICYCLIC TRIAZOLES AS PROTEIN KINASE MODULATORS - The present disclosure provides bicyclic triazole protein kinase modulators and methods of using these compounds to treat diseases mediated by kinase activity.10-15-2009
20090275557Novel Composition for Treatment of Diseases Related to Activated Lymphocytes - The present invention relates to inhibiting proliferation and inducing apoptosis in activated lymphocytes, including T cells and B cells. The invention also provides compositions and methods for inhibiting proliferation and inducing apoptosis in activated lymphocytes, as well methods for treating diseases associated with activated lymphocytes by administering 5-HT receptor antagonists.11-05-2009
20090143355Substituted aryl-amine derivatives and methods of use - Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds of Formula I and II06-04-2009
20110269741NOVEL COMPOSITIONS AND METHODS OF USE - Described herein are novel enzyme inhibitors. In some embodiments the enzyme inhibitors are integrase inhibitors, particularly HIV integrase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV integrase as a method of treating or preventing HIV, AIDS or related disorders.11-03-2011
20090275558SUBSTITUTED SULFONAMIDE COMPOUNDS - Substituted sulfonamide compounds corresponding to formula I11-05-2009
20090281075ISOMERIC PURINONES AND 1H-IMIDAZOPYRIDINONES AS PKC-THETA INHIBITORS - A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKCθ inhibitors, and their methods of use are disclosed. The genus is represented by the formula I:11-12-2009
20090286768SUBSTITUTED IMIDAZOPYR- AND IMIDAZOTRI-AZINES - Fused pyridine-based bicyclic compounds having the structure of Formula I, as defined herein, pharmaceutically acceptable salts thereof, preparation, compositions, and disease treatment therewith. This abstract does not define or limit the invention.11-19-2009
20090042856PYRIDAZINONE DERIVATIVES USED FOR THE TREATMENT OF PAIN - A pyridazinone derivative compound shown by the following formula (I): wherein R02-12-2009
20110172204COMPOUNDS AND THEIR USE - A compound of the formula:07-14-2011
20110172203Substituted Imidazopyridinyl-Aminopyridine Compounds - The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.07-14-2011
20120295885INHIBITORS OF BRUTON'S TYROSINE KINASE - This application discloses compounds according to generic Formula I:11-22-2012
20130190290Substituted phenylimidazopyrazoles and their use - The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.07-25-2013
20080261945Compounds Having Activity at Nk3 Receptor and Uses Thereof in Medicine - The present invention relates to compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof:10-23-2008
20080280879SUBSTITUTED HETEROCYCLIC DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS - Compounds of the general Formula I, wherein X11-13-2008
20080280878Methods and Compositions for Treating Chronic Lymphocytic Leukemia - Novel method of treating chronic lymphocytic leukemia by the administering of HSP90 inhibitors, particularly ansamycins, more particularly I 7-allylamino-I 7-demethoxygetdanarnycin (17-AAG).11-13-2008
20080287415Bicycloheteroaryl compounds as P2X7 modulators and uses thereof - Compounds are disclosed that have a formula represented by the following:11-20-2008
20080287414Mitotic Kinesin Inhibitors - The present invention relates to tricyclic pyrazoles according to Formula (I) that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.11-20-2008
20100280001IMIDAZOQUINOLINES WITH IMMUNO-MODULATING PROPERTIES - The present invention provides compounds of formula (I)11-04-2010
20090318411PURINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Purine 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 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.12-24-2009
20100249100QUINAZOLINES USEFUL AS MODULATORS OF ION CHANNELS - The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.09-30-2010
20100249099PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLE SULFONAMIDES AND THEIR USE IN CANCER THERAPY - Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g., compounds of Formulae IA, IB, and IC, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.09-30-2010
20130217671QUINOLINE DERIVATIVES AND MELK INHIBITORS CONTAINING THE SAME - The present invention directs a compound represented by formula (I).08-22-2013
20100249098OXYPIPERIDINE DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to novel Oxypiperidine Derivatives, pharmaceutical compositions comprising the Oxypiperidine Derivatives and the use of the Oxypiperidine Derivatives for treating or preventing treating allergy, an allergy-induced airway response, congestion, hypotension, a cardiovascular disease, a gastrointestinal disorder, obesity, a sleep disorder, pain, diabetes, a diabetic complication, impaired glucose tolerance, impaired fasting glucose or a central nervous system (CNS) disorder.09-30-2010
20120270854Antiviral Compounds - Compounds and methods for preventing and treating viral infections are provided. In some embodiments, novel compounds broad-spectrum antiviral activity are provided. In more specific embodiments, the compounds and methods are effective against viruses such as Venezuelan Equine Encephalitis, West Nile Virus, and Hepatitis C.10-25-2012
20110207713PYRIDO[3,2-d]PYRIMIDINE PI3K DELTA INHIBITOR COMPOUNDS AND METHODS OF USE - Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. 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.08-25-2011
20080269191Compounds for Nonsense Suppression, Use of These Compounds for the Manufacture of a Medicament for Treating Somatic Mutation-Related Diseases - The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.10-30-2008
200902644063-METHYL-IMIDAZO[1,2-B]PYRIDAZINE DERIVATIVES - The invention relates to compounds of formula (I) and salts thereof10-22-2009
20110269742Serotonin 5-HT2B Receptor Inhibitors - Disclosed are Serotonin 5-HT2B receptor inhibitors of the formula I. Also disclosed are methods of making and methods of using these compounds.11-03-2011
20110207714SEROTONIN RECEPTOR MODULATORS - The biphenyic compounds of formula (I) are serotonin modulators useful in the treatment of serotonin-mediated diseases.08-25-2011
20120196846ANTI-RSV COMPOUNDS - The present invention relates to anti-RSV compounds of Formula (I) and methods for use of the compounds in the treatment and prevention of RSV infection.08-02-2012
20090029966COMBINATION THERAPY WITH PARP INHIBITORS - The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with temozolomide (TMZ).01-29-2009
20090163471Tropane compounds - A compound according to Formula I or II:06-25-2009
20090163472MINERALOCORTICOID RECEPTOR ANTAGONISTS AND METHODS OF USE - The present invention provides a compound of Formula (I):06-25-2009
20090137550Novel Compounds - This invention relates to a novel group of 8-Alkyl/Aryl-4-aryl-2-N-(alkylamino)-N″-substituted-N′-cyanoguanidino-8H-pyrido[2,3-d]pyrimidin-7-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and pharmaceutical compositions for use in such therapy.05-28-2009
20100016280Low Dosage Serotonin 5-HT2A Receptor Agonist To Suppress Inflammation - Activation of 5-HT01-21-2010
20090186870Therapeutic Agents - 802 - A compound of formula I07-23-2009
20080318926Methods of Treating Mood Disorders Using Pyridyloxymethyl and Benzisoxazole Azabicyclic Derivatives - An aminomethylpyridyloxymethyl/benzisoxazole substituted azabicyclic compound, a pharmaceutical composition comprising same, and a method of treating a mood disorder selected from the group consisting of Somatization Disorder, Borderline Personality Disorder, Narcissistic Personality Disorder, Suicidal Ideation, and Antisocial Personality Disorder.12-25-2008
20110230464PURINE DERIVATIVES USEFUL AS P13 KINASE INHIBITORS - This invention provides a compound which is a purine of formula (Ia) or (Ib): and the pharmaceutically acceptable salts thereof that are inhibitors of PI3K and a selective for the p110δ isoform, which is a class Ia PI3 kinase, over other class Ia PI3 kinases and over class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.09-22-2011
20100004220Indenoisoquinolinone Analogs and Methods of Use Thereof - The present invention relates to Indenoisoquinolinone Analogs, compositions comprising an effective amount of an Indenoisoquinolinone Analog and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes mellitus, a diabetic complication, reoxygenation injury resulting from organ transplantation, an ischemic condition, a neurodegenerative disease, renal failure, a vascular disease, a cardiovascular disease, cancer, a complication of prematurity, cardiomyopathy, retinopathy, nephropathy, neuropathy, erectile dysfunction or urinary incontinence, comprising administering to a subject in need thereof an effective amount of an Indenoisoquinolinone Analog.01-07-2010
20090325926PYRROLO[3,2-D] PYRIMIDINES AS DPP-IV INHIBITORS FOR THE TREATMENT OF DIABETES MELLITUS - The present invention relates to substituted pyrrolo[3,2-d]pyrimidines of formula (I), wherein R1 and R2 are defined as in claim 12-31-2009
20090325927Benzofuro- and benzothienopyrimidine modulators of the histamine H4 receptor - Benzofuro- and benzothienopyrimidine compounds are described, which are useful as H12-31-2009
200903259286,6-Bicyclic Ring Substituted Heterobicyclic Protein Kinase Inhibitors - Compounds of the formula12-31-2009
20090023704Novel Compounds 737 - The present invention relates to novel xanthine compounds of the general formula (I)01-22-2009
201101440846 SUBSTITUTED 2- HETEROCYCLYLAMINO PYRAZINE COMPOUNDS AS CHK-1 INHIBITORS - The present invention is directed to compounds of formula (I),06-16-2011
20090054397PYRAZOLE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE COMPOUND - The present invention provides a novel compound having an excellent JNK inhibitory effect. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.02-26-2009
20090105210Bicyclic Pyrimidines as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes - The present invention is directed to novel substituted bicyclic pyrimidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.04-23-2009
20110230465VIRAL POLYMERASE INHIBITORS - Compounds of formula I:09-22-2011
20110224190PIPERIDIN-4-YL AZETIDINE DERIVATIVES AS JAK1 INHIBITORS - The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.09-15-2011
20090105212NOVEL ADENINE COMPOUND - A novel adenine compound represented by the formula (1):04-23-2009
20090105211INHIBITORS OF HEDGEHOG PATHWAY - The present invention is directed to a compound of Formula I04-23-2009
20090105213Lactam compounds useful as protein kinase inhibitors - The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.04-23-2009
20090203665HETEROCYCLIC-SUBSTITUTED PHENYL METHANONES - The present invention relates to compounds of formula I08-13-2009
20080261946Pyrimidine Compounds for the Treatment of Inflammatory Disorders - The present invention relates to novel pyrimidine compounds, for the modulation of the histamine H4 receptor and the treatment or prevention of conditions mediated by the histamine H4 receptor. The invention also relates to the preparation of such compounds.10-23-2008
20080261944Indole Derivatives as Antiviral Agents - The present invention relates to indole compounds of the formula (I): wherein R10-23-2008
20080261947FUSED PYRIDAZINE DERIVATIVE COMPOUNDS AND DRUGS CONTAINING THESE COMPOUNDS AS THE ACTIVE INGREDIENT - Fused pyridazine derivatives represented by formula (I) or pharmaceutically acceptable salts thereof (wherein each symbol has the meaning as defined in the specification.).10-23-2008
20080261943PYRROLOPYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE - The subject invention provides compounds having the structure:10-23-2008
20090197863BENZOXAZOLE CARBOXAMIDE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) - A compound having the structure set forth in Formula (I) or Formula (II):08-06-2009
20120077799HETEROCYCLIC COMPOUND AND USE THEREOF - Provided is a compound represented by the formula (I):03-29-2012
20090093455QUINOLONE ANALOGS AND METHODS RELATED THERETO - The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.04-09-2009
20090247505SPIRO(5.5)UNDECANE DERIVATIVES - The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.10-01-2009
20090247504Indazole Derivatives for Treatment of Alzheimer's Disease - Compounds of formula (IA) and (IB) are inhibitors of MARK, and hence are suitable for treatment of Alzheimer's disease.10-01-2009
20090258853Somatostatin Agonists - This invention relates to compounds which are agonists of somatostatin and selective toward somatostatin receptor subtype SSTR2. The compounds are useful in the treatment and prevention of diabetes, and diabetes-related pathologies, including retinopathy, neuropathy and nephropathy. Many of the compounds are orally active. Thus, it is an object of this invention to describe such compounds. It is a further object to describe the specific preferred stereoisomers of the somatostatin agonists. A still further object is to describe processes for the preparation of such compounds. Another object is to describe methods and compositions which use the compounds as the active ingredient thereof.10-15-2009
20090286767SUBSTITUTED QUINOLIN-4-YLAMINE ANALOGUES - Substituted quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.11-19-2009
20090048228Heterocycle Derivatives As Histone Deacetylase (Hdac) Inhibitors - The present invention relates to compounds of formula I:02-19-2009
20100261704THERAPEUTIC AGENTS 928 - A compound (2S)-2-[1-(2,6-dichlorophenyl)pyrazolo[4,5-e]pyrimidin-4-yl]oxy-3-(3-hydroxyazetidin-1-yl)-N-(5-methylpyrazin-2-yl)propanamide is useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK or GK), leading to a decreased glucose threshold for insulin secretion.10-14-2010
20100184739Modulators of ATP-Binding Cassette Transporters - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.07-22-2010
20110059946DUAL ACTION ANTIBIOTICS - The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:03-10-2011
20110237565HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE - The present invention relates to compounds and methods which may be useful as inhibitors of H09-29-2011
20130123237NOVEL CYCLIC AZABENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS - Novel compounds of structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.05-16-2013
20100216767QUINAZOLINES FOR PDK1 INHIBITION - The invention provides novel compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.08-26-2010
20100216768N-SUBSTITUTED AZAINDOLES AND METHODS OF USE - The invention relates to N-substituted azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to N-substituted azaindolyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.08-26-2010
20100137280AZETIDIN COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR - The present invention relates to compounds of formula (I)06-03-2010
20100152159IMIDAZOPYRAZINE 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.06-17-2010
20100144702INDOLE COMPOUND - The purpose of the present invention is to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like. The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein R06-10-2010
201201968476,6-Bicyclic Ring Substituted Heterobicyclic Protein Kinase Inhibitors - Compounds of the formula08-02-2012
20100041634N-(amino-heteroaryl)-1H-pyrrolopyridine-2-carboxamides derivatives preparation thereof and their use in therapy - The invention relates to compounds of the general formula (I):02-18-2010
20120142670N-(amino-heteroaryl)-1H-pyrrolopyridine-2-carboxamides derivatives preparation thereof and their use in therapy - The invention relates to compounds of the general formula (I):06-07-2012
20120142669N-(amino-heteroaryl)-1H-pyrrolopyridine-2-carboxamides derivatives preparation thereof and their use in therapy - The invention relates to compounds of the general formula (I):06-07-2012
20100197656COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISEASES - Dihydrothienopyrimidines of formula 108-05-2010
20120245144BENZOXAZEPIN COMPOUNDS SELECTIVE FOR PI3K P110 DELTA AND METHODS OF USE - Benzoxazepin Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. 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.09-27-2012
201202451423-OXO-2,3-DIHYDRO-1H-ISOINDOLE-4-CARBOXAMIDES AS PARP INHIBITORS - There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating, diseases utilizing pharmaceutical compositions comprising these compounds.09-27-2012
20090318410IMIDAZOPYRIDAZINES AS LIPID KINASE INHIBITORS - The invention relates to novel compounds of the formula I,12-24-2009
20080287416Organic Compounds - There are provided according to the invention compounds of formula (I)11-20-2008
20100222325Inhibitors of Bruton's Tyrosine Kinase - This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-III:09-02-2010
20100298291FUSED BICYCLIC-SUBSTITUTED AMINES AS HISTAMINE-3 RECEPTOR LIGANDS - Compounds of formula (I)11-25-2010
20130131043PYRAZOLE COMPOUNDS AS JAK INHIBITORS - The invention relates to compounds of formula (I)05-23-2013
20130131044SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.05-23-2013
20090075970Thieno-and furo-pyrimidine modulators of the histamine H4 receptor - Thieno- and furo-pyrimidine compounds are described, which are useful as H03-19-2009
20130143865PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof.06-06-2013
20100331304Compounds Which Modulate The CB2 Receptor - Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.12-30-2010
20100331308OXAZOLIDINONE DERIVATIVES - The invention relates to compounds of Formula (I)12-30-2010
20100222322Non-Nucleoside Reverse Transcriptase Inhibitors - Indole compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein R09-02-2010
20110009380QUINOLINE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR - The present invention relates to novel quinoline compounds. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT01-13-2011
20110245230PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof.10-06-2011
20110009381SOLUBILIZED THIAZOLOPYRIDINES - Provided herein are novel sirtuin-modulating compounds Structural Formula (I): 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.01-13-2011
20100179122Non-Nucleoside Reverse Transcriptase Inhibitors - Compounds of Formula (I): are HIV reverse transcriptase inhibitors, wherein R07-15-2010
20100179123THIENOPYRIMIDINES USEFUL AS AURORA KINASE INHIBITORS - The present invention provides compounds having the formula:07-15-2010
20110039823OXAZOLIDINONE ANTIBIOTICS - The invention relates to compounds of formula (I) wherein U, V, W, X, R1, R2, R3, R4, R5, R6, A, B, D, E, G, m, and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention.02-17-2011
20110245229DIHYDROPYRAZOLOPYRIMIDINONE DERIVATIVES - The invention relates to compounds represented by the general formula (I) and the like. In the formula, Ar10-06-2011
20100152158Substituted Disulfonamide Compounds - Substituted disulfonamide compounds corresponding to formula I:06-17-2010
20110086840N-7 SUBSTITUTED PURINE AND PYRAZOLOPYRIMINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - The present invention relates to compounds of Formula I:04-14-2011
20100222323IMIDAZOPYRAZINE 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.09-02-2010
20090093456NOVEL MCH RECEPTOR ANTAGONISTS - The present invention relates to a melanin concentrating hormone antagonist compound of formula (1): wherein R04-09-2009
201202451433-0X0-2,3-DIHYDRO-1H-ISOINDOLE-4-CARBOXAMIDES WITH SELECTIVE PARP-1 INHIBITION - There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.09-27-2012
20090258852Inhibitors of Checkpoint Kinases - The instant invention provides for compounds which comprise benzoisoquinolinones and aza derivatives that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.10-15-2009
20090312305BICYCLIC COMPOUNDS HAVING ACTIVITY AT THE CXCR4 RECEPTOR - A compound represented by the structural formula:12-17-2009
201000693547-AZAINDOLE DERIVATIVES AND THEIR USE IN THE INHIBITION OF C-JUN N-TERMINAL KINASE - The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof, the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof in the inhibition of c-Jun N-terminal kinase (JNK) activity and the use in medicine and particularly in the treatment of neurodegenerative disorders, inflammatory diseases and/or and autoimmune diseases. The invention also provides processes for the manufacture of said compounds of formula (I) or a pharmaceutically acceptable salt thereof and compositions containing them.03-18-2010
201000564914'-AMINO CYCLIC COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY - The present disclosure provides compounds having affinity for the 5-HT03-04-2010
20130158003HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF - Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.06-20-2013
20100063026ANTIBACTERIAL QUINOLINE DERIVATIVES - The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib):03-11-2010
20130158005PYRIMIDINE DERIVATIVES AS FAK INHIBITORS - Compounds of the formula (I), in which R06-20-2013
20100069353INHIBITORS OF HIV REPLICATION - The present invention relates to compounds of formula (I) wherein R03-18-2010
20100069355Analogs of Indole-3-Carbinol and Their Use as Agents Against Infection - Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.03-18-2010
20110152243NOVEL THIENOPYRROLE COMPOUNDS - The invention provides a compound of Formula (I)06-23-2011
20120149682HETEROCYCLIC-SUBSTITUTED PYRROLOPYRIDINES AND PYRROLOPYRIMIDINES AS JAK INHIBITORS - The present invention provides heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines of Formula I:06-14-2012
20120149681CYCLOBUTYL SUBSTITUTED PYRROLOPYRIDINE AND PYRROLOPYRIMIDINE DERIVATIVES AS JAK INHIBITORS - The present invention provides cyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I:06-14-2012
201101522422,3-Substituted Fused Pyrimidin -4 (3H)-Ones as VR1 Antagonists - A compound of formula (I), wherein W is formula (1); A is a benzene ring, a fÊve-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S atom is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; n is zero, one, two or three; when n is zero or one, V is CH06-23-2011
20110077235APOPTOSIS SIGNAL-REGULATING KINASE 1 INHIBITORS - The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula (I); wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.03-31-2011
20120035155INDOLE-2-CARBOXAMIDE DEIVATIVE - To provide an indole compound having a human QRFP receptor antagonistic activity and useful as a preventive or a remedy for various disorders. A compound of a formula (I) or a pharmaceutically-acceptable salt thereof is provided: [wherein, R02-09-2012
20110009382Substituted Benzimidazoles, Benzothiazoles and Benzoxazoles - Substituted benzimidazoles, benzothiazoles and benzoxazoles, processes for their preparation, pharmaceutical compostions containing these compounds and the use of these compounds for treating or inhibiting disorders or disease states mediated at least in part by bradykinin receptor 1 (BR1).01-13-2011
20100311715ALPHA CARBOLINES AND USES THEREOF - This invention provides alpha-carboline compounds of formula I:12-09-2010
20100298289HETEROBICYCLIC COMPOUNDS AS HISTAMINE H4-RECEPTOR ANTAGONISTS - The present invention concerns heterobicyclic compounds of formula (I) processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.11-25-2010
20100261703SALT AND CRYSTALLINE FORMS THEREOF OF A DRUG - A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.10-14-2010
20120202788AZABENZOTHIAZOLE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R08-09-2012
20090186871Tyrosine kinase inhibitors - The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.07-23-2009
20080275022Substituted Quinazolones as Anti-Cancer Agents - The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.11-06-2008
20120302547NOVEL MCH RECEPTOR ANTAGONISTS - The present invention relates to a melanin concentrating hormone antagonist compound of formula (I) wherein R11-29-2012
20080255086Heterocyclic Derivatives - The present invention relates to a heterocyclic derivative according to formula I10-16-2008
20120149680KINASE 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.06-14-2012
20110053909Compounds - 801 - Spirocyclic amide derivatives of formula I03-03-2011
20110028450Ring-annulated dihydropyrrolo[2,1-alpha]isoquinolines - The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I02-03-2011
20100286119N-(Aminoheteroaryl)-1H-indole-2-carboxamide derivatives, and preparation and therapeutic application thereof - The invention concerns compounds of general formula (I):11-11-2010
20100298288CETP INHIBITORS DERIVED FROM BENZOXAZOLE ARYLAMIDES - Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis Atherosclerosis and its clinical consequences, coronary heart disease (CHD), stroke and penpheral vascular disease, represent a truly enormous burden to the health care systems of the industrialized world In formula I, A-B is an arylamide moiety11-25-2010
20100305093Inhibitors of mTOR and Methods of Making and Using - The invention is directed to Compounds of Formula I:12-02-2010
20100324018PHARMACEUTICAL COMPOSITIONS HAVING IMPROVED DISSOLUTION PROFILES FOR POORLY SOLUBLE DRUGS - Pharmaceutical compositions having improved dissolution profiles for drugs therein is disclosed.12-23-2010
20100324017ACYLGUANIDINE DERIVATIVE - An object of the present invention is to provide a novel and excellent agent for treating or preventing dementia, schizophrenia and the like, based on the 5-HT12-23-2010
20110086841N-9 SUBSTITUTED PURINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - The present invention relates to compounds of Formula I:04-14-2011
20100179124THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS - A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.07-15-2010
20100222324Substituted Indole Compounds - Substituted indole compounds corresponding to the formula I:09-02-2010
20120309741QUINOXALINE CARBOXAMIDE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS - The invention relates to compounds of formula (I)12-06-2012
20120309740Pharmaceutical Compositions Having Improved Dissolution Profiles For Poorly Soluble Drugs - Pharmaceutical compositions having improved dissolution profiles for drugs therein is disclosed.12-06-2012
20100190769THIAZOLOPYRIMIDINES AND THEIR USE AS INHIBITORS OF PHOSPHATIDYLINOSITOL-3 KINASE - Thiazolopyrimidines of formula (I): wherein W represents a thiazole ring; R07-29-2010
20100190770COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY - Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.07-29-2010
20110190262Aryl-and Heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use - The present invention relates to compounds defined by formula I08-04-2011
20110190265METHODS AND COMPOSITIONS FOR TREATING BACTERIAL INFECTIONS BY INHIBITING QUORUM SENSING - The present invention provides methods for treating bacterial infections in a subject comprising administering to the subject a sub-growth inhibiting amount of a 5′-Methylthioadenosine/S-adenosyl homocysteine nucleosidase (MTAN) inhibitor. The present invention further provides pharmaceutical compositions comprising a sub-bacterial-growth inhibiting amount of a 5′-Methylthioadenosine/S-adenosyl homocysteine nucleosidase (MTAN) inhibitor and a pharmaceutically acceptable carrier.08-04-2011
20110190264COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS - The invention relates to triazine and pyrimidine derivatives having Formula (1) or (2), and methods for using such compounds. For example, the compounds of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, c-ros oncogene (ROS), insulin-like growth factor (IGF-IR), and/or insulin receptor (InsR) or a combination thereof.08-04-2011
20110190263COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds of Formula (I): pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.08-04-2011
20110152244PYRROLOPYRIMIDINE COMPOUNDS AND THEIR USES - The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.06-23-2011
20100063025Substituted isoquinoline and isoquinolinone derivatives as inhibitors of RHO-Kinase - The invention relates to 6-substituted isoquinoline and isochinolone derivatives of the formula (I)03-11-2010
201101902665,6,6a,7,8,9-HEXAHYDRO-2H-PYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) - Provided herein are compounds having the structure set forth in Formula (I):08-04-2011
20110201594PYRIDO [2,3-D] PYRIMIDINES AND THEIR USE AS KINASE INHIBITORS - The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.08-18-2011
20100029611S1P1 receptor agonists and use thereof - The present invention relates to compounds of Formula (I):02-04-2010
20100022507AMINOPYRIMIDINES 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.01-28-2010
20110218184QUINOLONE ANALOGS AND METHODS RELATED THERETO - The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.09-08-2011
20110218185AZOLOTRIAZINONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS - The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I09-08-2011
20100016279BICYCLIC DERIVATIVES FOR USE IN THE TREATMENT OF ANDROGEN RECEPTOR ASSOCIATED CONDITIONS-155 - The invention concerns bicyclic compounds of Formula I01-21-2010
20100311713Novel Azetidine Compounds Useful in the Treatment of Functional Gastrointestinal Disorders, Ibs and Functional Dyspepsia - The present invention relates to new azetidine compounds, to pharmaceutical compositions containing them and the use of said compounds in the treatment of functional gastrointestinal disorders, IBS and functional dyspepsia. The compounds are neurokinin (NK) antagonists. The present invention further relates to processes for the preparation of the compounds.12-09-2010
20130012492FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present disclosure 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:01-10-2013
20110306592CYCLOHEXYL-AZETIDINYL ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula (I).12-15-2011
20100210623THERAPEUTIC COMPOUNDS - The present invention relates to pyrazine substituted pyrrolopyridines which are inhibitors of JAK kinases (JAK1, JAK2, JAK3 and/or TYK2) and/or PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer.08-19-2010
20120040957Novel Bicyclic Antibiotics - Compounds of formula (I) wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; R1 and R2, independently of one another, represent hydrogen or a substituent selected from hydroxy, halogen, carboxy, amino, C1-C6alkylamino, di(C1-C6alkyl)amino, mercapto, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylamino-carbonyloxy, C2-C6alkenyl, C2-C6alkynyl, C1-C6alkylcarbonyloxy, C1-C6alkyl-sulfonyloxy, C1-C6heteroalkylcarbonyloxy, C5-C6heterocyclyl-carbonyloxy, C1-C6heteroalkyl, C1-C6heteroalkoxy, wherein heteroalkyl, heteroalkoxy groups or heterocyclyl comprise 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, in which substituents the alkyl moieties are unsubstituted or further substituted by halogeno, cyano, hydroxy, C1-C4alkoxy, C1-C4alkylcarbonyl, C1-C4alkoxycarbonyl, unsubstituted or substituted phenoxy or phenylcarbonyl, unsubstituted or substituted C5-C6heterocyclyl or carboxy; A1 represents a divalent group of one of the formulae —O—(CH02-16-2012
20120040958INDOLE CARBOXAMIDES AS IKK2 INHIBITORS - The invention is directed to novel indole carboxamide compounds. Specifically, the invention is directed to compounds according to formula (I):02-16-2012
20100210622HETEROCYCLIC COMPOUNDS AND METHODS OF USE - In one aspect, the present invention provides for a compound of Formula I08-19-2010
201200409604-AZETIDINYL-1-PHENYL-CYCLOHEXANE ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula (I):02-16-2012
20120065188SUBSTITUTED HETEROCYCLIC DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS - Compounds of the general Formula I, wherein X03-15-2012
20090312304ORGANIC COMPOUNDS - 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4-substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula I,12-17-2009
20100190768NOVEL FUSED PYROLE DERIVATIVE - The present invention relates to a compound represented by the formula (1) which is useful as a glucocorticoid receptor function regulating agent, an anti-inflammatory agent or an antidiabetic agent, or a pharmaceutically acceptable salt thereof:07-29-2010
20110021498INDOLYL- PYRIDONE DERIVATIVES HAVING CHECKPOINT KINASE 1 INHIBITORY ACTIVITY - Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R01-27-2011
20110021497AMINO TRIAZOLES AS PI3K INHIBITORS - The invention relates to compounds of formula (I)01-27-2011
20110021496THIENOPYRIMIDINE DERIVATIVES AS P13K INHIBITORS - Thienopyrimidines of formula (I) wherein W and R01-27-2011
20110021494NOVEL TETRAHYDRO-FUSED PYRIDINES AS HISTONE DEACETYLASE INHIBITORS - The compounds of formula (I), wherein ring D and ring E together form a fused ring system selected from formula (II), (III), (IV), (V), (VI), (VII), and the salts of these compounds are novel, effective inhibitors of histone deacetylases.01-27-2011
20120065187HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE - The present invention relates to compounds and methods which may be useful as inhibitors of H03-15-2012
201200409598-METHOXY-9H-ISOTHIAZOLO[5,4-B]QUINOLINE-3,4-DIONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS - The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B:02-16-2012
20110071133BICYCLIC ARYL AND BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.03-24-2011
20110071132SUBSTITUTED OXINDOLE DERIVATIVES, DRUGS CONTAINING SAID DERIVATIVES AND THE USE THEREOF - The invention relates to novel oxindol derivative of general formula (I), wherein substituents R03-24-2011
20110071131Substituted Spirocyclic Piperidine Derivatives as Histamine-3 (H3) Receptor Ligands - The present invention provides compounds of Formula (I):03-24-2011
201100711302-AMINOBENZIMIDAZOLES FOR TREATING NEURODEGENERATIVE DISEASES - The invention relates to 2-aminobenzimidazoles useful in treating disorders that are mediated by A03-24-2011
20100152160NOVEL BENZODIOXANE AND BENZOXAZINE DERIVATIVES USEFUL AS CC CHEMOKINE RECEPTOR LIGANDS - The present invention relates to benzodioxane and benzoxazine derivatives that act as ligands for CC chemokine receptors, such as CCR1. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.06-17-2010
20090270364SUBSTITUTED PYRIMIDINE DERIVATIVES - The present application describes substituted pyrimidine compounds of formula (I)10-29-2009
20120065186ANTIMICROBIAL COMPOSITIONS - The present invention relates to antimicrobial compositions and more specifically compositions of quinolone carboxylic acid derivatives. These compositions have improved solubility, stability, and tolerability. These compositions are useful for intravenous administration for treating, preventing, or reducing the risk of infection.03-15-2012
20120252780BICYCLIC PYRIDINES AND ANALOGS 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, 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.10-04-2012
20120252779HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS JAK INHIBITORS - The invention relates to compounds of formula (I)10-04-2012
20120208792PROTEIN KINASE MODULATORS - The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate Pim kinase activity and/or FMS-like tyrosine kinase (Flt) activity. The invention also relates in part to methods for using such molecules.08-16-2012
20120046269Novel Amino Azaheterocyclic Carboxamides - The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.02-23-2012
20090258854Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amines as modulators of leukotriene A4 hydrolase - Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.10-15-2009
201003117141H-IMIDAZO[4,5-c]QUINOLINONE COMPOUNDS - The invention relates to the use of 1H-imidazo[4,5-c]quinolinone compounds and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c]quinolinone compounds for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H-imidazo[4,5-c]quinolinone compounds to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c]quinolinone compounds, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1H-imidazo[4,5-c]quinolinone compounds; and a process for the preparation of the novel 1H-imidazo[4,5-c]quinolinone compounds.12-09-2010
20120208793THIENO- AND FURO-PYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR - Thieno- and furo-pyrimidine compounds are described, which are useful as H08-16-2012
20100190771AMINO-HETEROCYCLIC COMPOUNDS - The invention provides PDE9-inhibiting compounds of Formula (I),07-29-2010
20120010193CGRP RECEPTOR ANTAGONISTS - Compounds of Formula (I) (wherein variables A01-12-2012
20120010192Fused Heterocyclic Compounds as Ion Channel Modulators - The present disclosure 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:01-12-2012
20120010191PYRIDONE AND AZA-PYRIDONE COMPOUNDS AND METHODS OF USE - Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.01-12-2012
20110166123NOVEL COMPOSITIONS AND METHODS OF USE - Described herein are novel enzyme inhibitors. In some embodiments the enzyme inhibitors are integrase inhibitors, particularly HIV integrase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV integrase as a method of treating or preventing HIV, AIDS or related disorders.07-07-2011
20120252782Xanthine Derivatives, the Preparation Thereof and Their Use as Pharmaceutical Compositions - The present invention relates to substituted xanthines of general formula10-04-2012
20120252783Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions - The present invention relates to substituted xanthines of general formula10-04-2012
20120022043PYRAZOLOPYRIMIDINE JAK INHIBITOR COMPOUNDS AND METHODS - The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R01-26-2012
20120058988CARBAZOLE AND CARBOLINE KINASE INHIBITORS - The present invention provides compounds of Formula (I)03-08-2012
20120270855THIENO- AND FURO-PYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR - Thieno- and furo-pyrimidine compounds are described, which are useful as H10-25-2012
20110028451Dihydrobenzoindazoles - The invention relates to benzoindazole derivatives according to general Formula I02-03-2011
20120157439RAF 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, prodrugs 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
20110092479PYRAZOLE [3, 4-B] PYRIDINE RAF INHIBITORS - Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs 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.04-21-2011
201201085698-AZA Tetracycline Compounds - The present invention is directed to a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.05-03-2012
20120157437VLA-4 INHIBITORY DRUG - This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof:06-21-2012
20120157435Antiviral Compounds - Compounds and methods for preventing and treating viral infections are provided. In some embodiments, novel compounds broad-spectrum antiviral activity are provided. In more specific embodiments, the compounds and methods are effective against viruses such as Venezuelan Equine Encephalitis, West Nile Virus, and respiratory viruses including the common cold.06-21-2012
20120071461Substituted Benzamide Compounds - Substituted benzamide compounds corresponding to formula (I)03-22-2012
201201574365,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-a]PYRAZINE DERIVATIVES AS P2X7 MODULATORS - The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof:06-21-2012
20120157434Antimicrobial heterocyclic compounds for treatment of bacterial infections - The present invention provides heterocyclic compounds of the following formula I:06-21-2012
20110092481QUINOLINE OR ISOQUINOLINE SUBSTITUTED P2X7 ANTAGONISTS - The present invention is related to novel compounds of formula (I) having P2X7 antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans. (I)04-21-2011
20110092480Substituted Heterocyclic Derivatives and Their Pharmaceutical Use and Compositions - Compounds of the general Formula I, wherein X04-21-2011
20110092478DIAZABENZO[DE] ANTHRACEN-3-ONE COMPOUNDS AND METHODS FOR INHIBITING PARP - The present invention relates to diazabenzo[de]anthracen-3-one compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.04-21-2011
20120252778PYRAZOLO PYRIMIDINE DERIVATIVES - The present invention relates to pyrazolo pyrimidine derivatives, to methods of preparing these, to combinations and pharmaceutical composition comprising these, and to their use in the treatment of diseases and disorders which may for example involve autoimmune diseases, angiogenesis, pain, and/or inflammatory diseases.10-04-2012
20090253678MACROCYCLIC PYRIMIDINE DERIVATIVES - Macrocyclic pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions, and disorders using such compounds and compositions are described herein.10-08-2009
20120157438PYRANYL ARYL METHYL BENZOQUINAZOLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to pyranyl aryl methyl benzoquinazolinone 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.06-21-2012
20090143354P2X7 Receptor Antagonists and Their Use - The invention provides compounds of formula (IA), processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.06-04-2009
20120309739AKT / PKB INHIBITORS - The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.12-06-2012
20110105464PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE - Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.05-05-2011
201000936962-AMINO PYRIMIDINE COMPOUNDS - The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, their synthesis, and their use as HSP-90 inhibitors.04-15-2010
20100093697Substituted Imidazopyridine Derivatives As Melanocortin-4 Receptor Antagonists - The present invention relates to substituted imidazopyridine derivatives as melanocortin-4 receptor (MC-4R) modulators, in particular as melanocortin-4 receptor antagonists. The antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, amytrophic lateral sclerosis (ALS), anxiety and depression.04-15-2010
20120316152SUBSTITUTED ISOQUINOLINEAND ISOQUINOLINONE DERIVATIVES - A method for the treatment or prevention in a mammal of a disease associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase comprising administering to the mammal in need thereof at least one compound of the formula (I)12-13-2012
20120122842NAMPT AND ROCK INHIBITORS - Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. Disclosed are compounds which inhibit the activity of ROCK, compositions containing the compounds and methods of treating diseases during which ROCK is expressed.05-17-2012
20120122841Biological Markers Predictive Of Anti-Cancer Response To Insulin-like Growth Factor-1 Receptor Kinase Inhibitors - The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with an IGF-1R kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an IGF-1R kinase inhibitor, comprising assessing whether the tumor cell has undergone an epithelial to mesenchymal transition (EMT), by determining the expression level of epithelial and/or mesenchymal biomarkers, wherein tumor cells that have undergone an EMT are substantially less sensitive to inhibition by IGF-1R kinase inhibitors. Improved methods for treating cancer patients with IGF-1R kinase inhibitors that incorporate the above methodology are also provided.05-17-2012
20120122840COMPOUNDS AND THERAPEUTIC USES THEREOF - The invention relates to compounds, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer.05-17-2012
20090131399Imidazopyridine Derivatives Useful as iNOS Inhibitors - The compounds of formula (I)05-21-2009
20090131400IMMUNOSUPPRESSANT COMPOUNDS AND COMPOSITIONS - The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.05-21-2009
20120165309HETERO RING DERIVATIVE06-28-2012
20120214792THIENO- ADN FURO-PYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR - Thieno- and furo-pyrimidine compounds are described, which are useful as H08-23-2012
201201653111H-THIENO[2,3-C]PYRAZOLE DERIVATIVES USEFUL AS KINASE INHIBITORS - Thieno[2,3-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.06-28-2012
20120165310ETHER DERIVATIVES OF BICYCLIC HETEROARYLS - The invention relates to compounds of formula I,06-28-2012
20100331305OXO-HETEROCYCLE FUSED PYRIMIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).12-30-2010
20100331306HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity. The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.12-30-2010
20120232056HETEROCYCLIC 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.09-13-2012
20090291937KINASE 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.11-26-2009
20120178737Tricyclic Heterocyclic Compounds as Phosphoinositide 3-Kinase Inhibitors - Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N-(C07-12-2012
20120258951NOVEL ANTIPLATELET AGENT - The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I:10-11-2012
20100273766SUBSTITUTED OXINDOL DERIVATIVES, MEDICAMENTS CONTAINING SAID DERIVATIVES AND USE THEREOF - The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R10-28-2010
20100273765Rifamycin analogs and uses thereof - The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, 4′- and/or 6′ halo and/or alkoxy analogs, and various 5′ substituents that incorporate a cyclic amine moiety.10-28-2010
20100009963KINASE ANTAGONISTS - The present invention provides novel compounds that are antagonists of PI3 kinase, PI3 kinase and tyrosine kinase, PI3 kinase and mTOR, or PI33 kinase, mTOR and tyrosine kinase.01-14-2010
20100009962Benzyl-substituted quinolone m1 receptor positive allosteric modulators - The present invention is directed to benzyl-substituted quinolone compounds of general formula (I)01-14-2010
20100292208COMPOUNDS WITH TWO FUSED BICYCLIC HETEROARYL MOIETIES AS MODULATORS OF LEUKOTRIENE A4 HYDROLASE - Compounds with two fused bicyclic heteroaryl moieties and their pharmaceutical compositions, and methods of using them as leukotriene A11-18-2010
20120220566Antimicrobial Compounds and Methods of Making and Using the Same - The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.08-30-2012
20120220565PYRIDYL-AMINE FUSED AZADECALIN MODULATORS - The present invention provides a novel class of pyridyl-amine fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.08-30-2012
20120225856FUSED RING AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS - The present invention provides a novel class of fused ring azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.09-06-2012
20120258952Substituted N-(1H-Indazol-4-yl)Imidazo[1,2-a]Pyridine-3-Carboxamide Compounds as cFMS Inhibitors - Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which R10-11-2012
20120258950PYRROLO[2,3-d]PYRIMIDINE TROPOMYSIN-RELATED KINASE INHIBITORS - The present invention relates to compounds of Formula (I)10-11-2012
20110124628APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.05-26-2011
20110124627MODULATORS OF TOLL-LIKE RECEPTORS - The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds.05-26-2011
20120264739CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR - Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.10-18-2012
20120264738DISPIROPYRROLIDINE DERIVATIVES - A compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R10-18-2012
20120232055HYDROXYLATED AND METHOXYLATED PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I:09-13-2012
20120232054PYRROLOTRIAZINE COMPOUNDS - A compound of formula (I):09-13-2012
20080300234PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH - The present invention relates to a compound of the formula 112-04-2008
20110003790PYRIDO [4, 3-D] PYRIMIDINONE DERIVATIVES AS KINASE INHIBITORS - The invention provides a class of compounds of Formula (I), 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 Syk, ZAP70, KDR, FMS, FLT3, c-Kit, RET, TrkA, TrkB, TrkC, IGR-IR, AIk, c-FMS, or combinations thereof.01-06-2011
201100037895-AMINOCYCLYLMETHYL-OXAZOLIDIN-2-ONE DERIVATIVES - The invention relates to antibacterial compounds of formula I01-06-2011
20120322788Compouds - The present invention relates to spirocyclic amide derivatives of the formula I,12-20-2012
20120270856HETEROARYLOXY QUINAZOLINE DERIVATIVES - Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc.10-25-2012
20110160183INHIBITORS OF AKT ACTIVITY - The instant invention provides for substituted naphthyridine 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.06-30-2011
20100234347Substituted Pteridines substituted with a Four-Membered Heterocycle - The invention relates to novel pteridines of formula (1),09-16-2010
20120277210SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT - A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.11-01-2012
20110263562BICYCLIC COMPOUND - The present invention provides to a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy.10-27-2011
20120329777Amino-Heterocyclic Compounds - The invention provides PDE9-inhibiting compounds of Formula (I),12-27-2012
20120329776HETEROCYCLIC COMPOUNDS AND USES THEREOF - Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the isoquinolone entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.12-27-2012
20120329778BICYCLIC HETEROCYCLES, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS, THEIR USE AND PROCESSES FOR PREPARING THEM - The present invention relates to bicyclic heterocycles of general formula12-27-2012
20110319381DERIVATIVES OF AZASPIRANYL-ALKYLCARBAMATES OF 5-MEMBER HETEROCYCLIC COMPOUNDS, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to a compound of the general formula (I) in which R12-29-2011
20120101084Biological Markers Predictive of Anti-Cancer Response to Insulin-Like Growth Factor-1 Receptor Kinase Inhibitors - The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with an IGF-1R kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an IGF-1R kinase inhibitor, comprising assessing whether the tumor cell has undergone an epithelial to mesenchymal transition (EMT), by determining the expression level of epithelial and/or mesenchymal biomarkers, wherein tumor cells that have undergone an EMT are substantially less sensitive to inhibition by IGF-1R kinase inhibitors. Improved methods for treating cancer patients with IGF-1R kinase inhibitors that incorporate the above methodology are also provided. Additionally, pErk, HER04-26-2012
20100222321Inhibitors of akt activtiy - The instant invention provides for substituted naphthyridine 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.09-02-2010
20130012493NOVEL SPIRO IMIDAZOLONE DERIVATIVES AS GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE - The present invention relates to compounds of the general formula (I): wherein ring A, ring B, G, R01-10-2013
20120149684AKT INHIBITORS - The present invention provides AKT inhibitors of the formula: Formula I The present invention also provides pharmaceutical compositions comprising compounds of Formula I, uses of compounds of Formula I and method of using compounds of Formula I.06-14-2012
20120149683SUBSTITUTED AMINOPIPERIDINES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES - The present invention is directed to novel substituted aminopiperidines of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-ÏV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.06-14-2012
20130018037Compounds - 801 - Spirocyclic amide derivatives of formula I01-17-2013
20130018039IMIDAZOLYL-IMIDAZOLES AS KINASE INHIBITORS - Disclosed are compounds having the formula: wherein R01-17-2013
20130018034AZETIDINYL PHENYL, PYRIDYL OR PYRAZINYL CARBOXAMIDE DERIVATIVES AS JAK INHIBITORS - The present invention provides azetidinyl phenyl, pyridyl, or pyrazinyl carboxamide derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAKs) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.01-17-2013
20130018038CHEMICAL COMPOUNDS - The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I:01-17-2013
20130018036SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS - Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.01-17-2013
20130018035COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.01-17-2013
20130018033RAF 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, prodrugs 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.01-17-2013
20100125062PYRIDINE AND PYRIMIDINE DERIVATIVES AS PHOSPHODIESTERASE 10 INHIBITORS - Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.05-20-2010
20130172316New azetidine derivatives, pharmaceutical compositions and uses thereof - The invention relates to new azetidine derivatives of the formula I07-04-2013
20080227769Compounds for the Treatment of Hepatitis C - The invention encompasses compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.09-18-2008
20110263564PYRIDINE, BICYCLIC PYRIDINE AND RELATED ANALOGS 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, 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.10-27-2011
20110263565COMPOUNDS - The present invention encompasses compounds of general formula (1), wherein R10-27-2011
20080221078Use of a CB1 Antagonist for Treating Side Effects and Negative Symptoms of Schizophrenia - The present invention discloses and claims a method of treating cognition deficits in a patient suffering from schizophrenia by administering to said patient a therapeutically effective amount of a CB1 receptor antagonist as described herein. In another aspect, this invention also discloses and claims a combination of one or more CB1 receptor antagonists and of one or more antipsychotic agents useful in the treatment of psychiatric disorders. The combination of this invention provides synergistic results in that the combination improves positive and negative symptoms of schizophrenia, weight gain and catalepsy.09-11-2008
20080221077Ansamycin formulations and methods of use thereof - Provided herein, inter alia, are solid forms of geldanamycin analogs, pharmaceutical compositions comprising a geldanamycin analog and a crystallization inhibitor, methods of making and using such compositions. Additionally, provided are methods for the treatment of cancer, a neoplastic disease state and/or a hyperproliferative disorder, and methods of inhibiting Heat Shock Protein 90 (“Hsp90”).09-11-2008
20130178461INHIBITORS OF BRUTON'S TYROSINE KINASE - This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I:07-11-2013
20130178462COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION - The present disclosure provides a series of compounds of the formula (I)07-11-2013
20130178459TRICYCLIC COMPOUNDS AND PBK INHIBITORS CONTAINING THE SAME - Tricyclic compounds are provided. These compounds are PBK inhibitors, and are useful for the treatment of PBK related diseases, including cancer.07-11-2013
20130178460THIENOPYRIMIDINE COMPOUNDS - The present invention relates to the use of novel compounds of Formula I:07-11-2013
20120252781Benzodiazepine Bromodomain Inhibitor - Benzodiazepine compounds of formula (I)10-04-2012
20120252777THIAZOLOPYRIMIDINE COMPOUNDS - The present invention relates to the use of novel pyrrolopyrazine derivatives of formula I:10-04-2012
200802145206-N-Linked Heterocycle-Substituted 2,3,4,5-Tetrahydro-1H-Benzo[d]Azepines as 5-Ht2c Receptor Agonists - The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT09-04-2008
20110269740JAK KINASE MODULATING COMPOUNDS AND METHODS OF USE THEREOF - Provided herein are pyrrolotriazine compounds for treatment of JAK kinase, including JAK2 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.11-03-2011
20130172317TRIAZINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION HAVING AN ANALGESIC ACTIVITY COMPRISING THE SAME - The present invention provides novel compounds having a P2X07-04-2013
20130116234ARYL-QUINOLINE DERIVATIVES - The invention provides novel compounds having the general formula (I)05-09-2013
20130102586SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3, 4-B] PYRIDINE AND PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS - Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds.04-25-2013
20130116236NOVEL [1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES - The invention relates to a compound of formula (I)05-09-2013
20130123236SUBSTITUTED BENZYLSPIROINDOLIN-2-ONE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M1 - In one aspect, the invention relates to substituted benzylspiroindolin-2-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M05-16-2013
20130143864(6,7-DIHYDRO-2-NITRO-5H-IMIDAZOL[2,1-B][1,3]OXAZIN-6YL) AMIDE COMPOUNDS, PREPARATION METHODS AND USES THEREOF - (6,7-Dihydro-2-nitro-5H-imidazo[2,1-b][1,3]oxazin-6-yl)amide compounds of formula (I), and their pharmaceutically acceptable salts, preparation methods and pharmaceutical compositions thereof are disclosed, wherein m and R are defined as in the description. The uses of the compounds in preparing medicaments for treating infectious diseases caused by 06-06-2013
20130158002POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 - The present invention is directed to 5-substituted 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide and 1,3-dihydro[1,2,5]thiadiazolo[3,4-b]pyridine 2,2,-dioxide derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.06-20-2013
20130158004Azetidine Derivatives - Azetidine derivatives of which the following is exemplary06-20-2013
20110224191Substituted Pyrrolo[2,3-b]-Pyridines and -Pyrazines - Compounds of Formula I, as shown below and defined herein: (I) pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by Ron and/or Met.09-15-2011
20110275611CHEMICAL COMPOUNDS - The invention is directed to 6-(4-pyrimidinyl)-1H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R11-10-2011
20110257156GAMMA SECRETASE MODULATORS - In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.10-20-2011
20130150342PYRROLOPYRIMIDINE COMPOUNDS AS INHIBITORS OF CDK4/6 - The invention is directed to novel pyrrolopyrimidine compounds of formula (I) wherein R06-13-2013
20130137677Bicyclic Azaheterocyclic Carboxamides - The invention provides novel bicyclic azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.05-30-2013
20130137676NOVEL [1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES - The invention relates to a compound of formula (I)05-30-2013
200901565777-AMINO ALKYLIDENYL-HETEROCYCLIC QUINOLONES AND NAPHTHYRIDONES - The present invention relates to compounds having a structure according to Formula (I)06-18-2009
20120283241IMIDAZOPYRIDAZINECARBONITRILES USEFUL AS KINASE INHIBITORS - The invention provides compounds of Formula (I)11-08-2012
20120283240Analogs of Indole-3-Carbinol and Their Use as Agents Against Infection - Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.11-08-2012
201202832391H-[1,2,3]TRIAZOLO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES - The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R11-08-2012
20120283238IRAK INHIBITORS AND USES THEREOF - The present invention provides compounds, compositions thereof, and methods of using the same.11-08-2012
20130184253TETRAHYDROPYRIDO-PYRIDINE AND TETRAHYDROPYRIDO-PYRIMIDINE COMPOUNDS AND USE THEREOF AS C5A RECEPTOR MODULATORS - The present invention provides a compound of formula I:07-18-2013
20130184254AZAINDAZOLE COMPOUNDS - Disclosed are azaindazole compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein W is CR07-18-2013
20110312936CYCLOHEXYL-AZETIDINYL ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula I.12-22-2011
201103129351H-Benz Imidazole-5-Carboxamides As Anti-Inflammatory Agents - There are provided compounds of formula (I), wherein R12-22-2011
201103129342-ALKYL-6-CYCLOAMINO-3-(PYRIDIN-4-YL)IMIDAZO[1,2-B]-PYRIDAZINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC APPLICATION THEREOF - The invention relates to 2-alkyl-6-cycloamino-3-(pyridin-4-yl)imidazo[1,2-b]pyridazine derivatives of the general formula (I) where: R12-22-2011
20130190291HETEROCYCLIC COMPOUND AND USE THEREOF - Provided is a compound represented by the formula (I):07-25-2013
20130190292HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS SELECTIVE JAK INHIBITORS - The present invention relates to compounds of formula (I)07-25-2013
20130096103IMIDAZOQUINOLINE COMPOUNDS - The invention provides novel compositions comprising imidazoquinoline compounds. Also provided are methods of administering the compositions in an effective amount to enhance the immune response of a subject. Further provided are novel compositions and methods of administering the compositions in combination with (an)other agent(s).04-18-2013
20110319380Compounds for Treating Disorders Mediated by Metabotropic Glutamate Receptor 5, and Methods of Use Thereof - Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.12-29-2011
20120289497FUSED PYRIDINE DERIVATIVES - Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R11-15-2012
20120289496NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES - The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.11-15-2012
20130116233NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A - The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.05-09-2013
20130116235HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS - Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X05-09-2013
20120028956BICYCLIC MGLUR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME - In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.02-02-2012
20120028955BICYCLIC MGLUR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME - In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.02-02-2012
20130196973BENZODIOXANE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I):08-01-2013
20130196974COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS DISEASE - A compound of formula (I)08-01-2013
20090291938POLO-LIKE KINASE INHIBITORS - Compounds of the following formula are provided for use with kinases:11-26-2009
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200900692896-SUBSTITUTED 2-(BENZIMIDAZOLYL)PURINE AND PURINONE DERIVATIVES FOR IMMUNOSUPPRESSION - The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulae I and II:03-12-2009
20130096104IMIDAZOPYRIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - The invention provides compounds of Formulas Ia-Ib, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R04-18-2013
20120094976NEW CHEMICAL COMPOUNDS - The present invention encompasses compounds of general formula (1)04-19-2012
20120094975PYRIDO [5, 4-D] PYRIMIDINES AS CELL PROLIFERATION INHIBITORS - The present invention encompasses compounds of general formula (1) wherein the groups R04-19-2012
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20130210802IMIDAZOPYRIDINES SYK INHIBITORS - Certain imidazopyridines (I) 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.08-15-2013

Patent applications in class Polycyclo ring system having the additional hetero ring as one of the cyclos