ARRAY BIOPHARMA INC. Patent applications |
Patent application number | Title | Published |
20160137608 | SUBSTITUTED BENZOAZEPINES AS TOLL-LIKE RECEPTOR MODULATORS - Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease. | 05-19-2016 |
20160122316 | SERINE/THREONINE KINASE INHIBITORS - Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt 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. | 05-05-2016 |
20160002232 | SUBSTITUTED N-(1H-INDAZOL-4-YL)IMIDAZO[1,2-a]PYRIDINE-3-CARBOXAMIDE COMPOUNDS AS TYPE III RECEPTOR TYROSINE KINASE INHIBITORS - Compounds useful in the treatment of fibrosis, bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases, pain and burns in a mammal. | 01-07-2016 |
20160002210 | INTERMEDIATES FOR USE IN THE PREPARATION OF INDAZOLE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF - Provided herein are novel processes for preparing a compound of Formula (I) to the use of said compound as an intermediate in novel processes for the synthesis of indazole derivatives, and to indazole intermediates and derivatives prepared by the processes described herein. | 01-07-2016 |
20150322061 | PYRROLOPYRIDINES AS KINASE INHIBITORS - Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers 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. | 11-12-2015 |
20150299182 | CRYSTALLINE FORMS OF (1S)-1-[5-(AMINO)-1,2,4-THIADIAZOL-3-YL]ETHANE-1,2-DIOL - The present invention relates to crystalline polymorph forms of (1S)-1-[5-({3-[(2-methylpyridin-3-yl)oxy]-5-(pyridin-2-ylsulfanyl)pyridin-2-yl}amino)-1,2,4-thiadiazol-3-yl]ethane-1,2-diol, to pharmaceutical compositions comprising such crystalline polymorph forms, and to processes for preparing them. The invention further relates to methods of treatment of diabetes related disorders comprising administering such solid-state forms or compositions thereof to a subject, and to use of such crystalline polymorph forms in the manufacture of medicaments. | 10-22-2015 |
20150232442 | 6-SUBSTITUTED PHENOXYCHROMAN CARBOXYLIC ACID DERIVATIVES - Provided herein are compounds of Formula I: | 08-20-2015 |
20150231117 | ARRY-520 FOR USE IN TREATING CANCER IN A PATIENT WITH LOW AAG - The compound ARRY-520 for use for treating cancer in patients with low [AAG] is provided. | 08-20-2015 |
20150210658 | MITOTIC KINESIN INHIBITORS AND METHODS OF USE THEREOF - This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders. | 07-30-2015 |
20150191490 | MITOTIC KINESIN INHIBTORS AND METHODS OF USE THEREOF - This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders. | 07-09-2015 |
20150087664 | QUINAZOLINE COMPOUNDS AS SERINE/THREONINE KINASE INHIBITORS - Compounds having the formula (I) wherein R | 03-26-2015 |
20150030673 | CRYSTALLINE FORMS OF 1-(3-TERT-BUTYL-1-P-TOLYL-1H-PYRAZOL-5-YL)-3-(5-FLUORO-2-(1-(2-HYDROXYETH- YL)-INDAZOL-5-YLOXY)BENZYL)UREA HYDROCHLORIDE - Provided herein is a hydrogen chloride salt of 1-(3-/t?r/-butyl-1-p-tolyl-1H-pyrazol-5-yl)-3-(5-fluoro-2-(1-(2-hydroxyethyl)-1H-indazol-5-yloxy)benzyl)urea, crystalline forms of 1-(3-½̂butyl-1̂-tolyl-1H-pyrazol-5-yl)-3-(5-fluoro-2-(1-(2-hydroxyethyl)-1H-indazol-5-yloxy)benzyl)urea hydrochloride, processes for the preparation of said crystalline forms, pharmaceutical compositions containing a crystalline form of 1-(3-r | 01-29-2015 |
20140249127 | SERINE/THREONINE KINASE INHIBITORS - Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt 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. | 09-04-2014 |
20140243520 | PYRROLOPYRIDINES AS KINASE INHIBITORS - Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers 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. | 08-28-2014 |
20140243361 | POLYMORPHS OF ARRY-380, A SELECTIVE HERB2 INHIBITOR AND PHARMACEUTICAL COMPOSITIONS CONTIANING THEM - Polymorphs of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine are provided herein. Processes for preparing the polymorphs and pharmaceutical composition comprising the polymorphs are also disclosed. | 08-28-2014 |
20140234376 | Substituted Benzoazepines as Toll-Like Receptor Modulators - Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease. | 08-21-2014 |
20140221443 | NOVEL HYDROGEN SULFATE SALT - The present invention relates to Compound 1 hydrogen sulfate salt and solvates, crystalline forms and amorphous forms thereof, and to processes for their preparation. | 08-07-2014 |
20140221370 | PYRROLOPYRIDINES AS KINASE INHIBITORS - Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers 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. | 08-07-2014 |
20140221342 | 6-SUBSTITUTED PHENOXYCHROMAN CARBOXYLIC ACID DERIVATIVES - Provided herein is a method of treating an allergic inflammatory disease selected from asthma, dermatitis, allergic rhinitis, urticaria, anaphylaxis, angioedemea, allergies, contact hypersensitivity, drug hypersensitivity, and allergic conjunctivitis in a mammal, comprising administering a therapeutically effective amount of a compound of Formula I | 08-07-2014 |
20140194403 | METHOD OF TREATMENT USING SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS - Provided herein are methods for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal, which comprises administering to said mammal in need thereof a therapeutically effective amount of a compound of Formula I: | 07-10-2014 |
20140148436 | AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: | 05-29-2014 |
20140142086 | Substituted Benzoazepines as Toll-Like Receptor Modulators - Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease. | 05-22-2014 |
20140128442 | PREPARATION OF AND FORMULATION COMPRISING A MEK INHIBITOR - The present invention relates to processes for preparing 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, processes for preparing crystallized 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, and intermediates useful therefore. Also provided herein are pharmaceutical compositions comprising this crystallized compound. | 05-08-2014 |
20140100369 | PYRROLOPYRIDINES AS KINASE INHIBITORS - Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers 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. | 04-10-2014 |
20140094603 | MITOTIC KINESIN INHIBITORS AND METHODS OF USE THEREOF - This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders. | 04-03-2014 |
20140088085 | Substituted Benzoazepines As Toll-Like Receptor Modulators - Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, fibrotic disease, cardiovascular disease, infectious disease, inflammatory disorder, graft rejection, or graft-versus-host disease. | 03-27-2014 |
20140080829 | PYRIMIDYL 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. | 03-20-2014 |
20140066453 | SERINE/THREONINE KINASE INHIBITORS - Compounds having the formula I wherein R | 03-06-2014 |
20140045835 | TRIAZOLOPYRIDINE COMPOUNDS AS PIM KINASE INHIBITORS - Provided herein are methods of treating diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases by administering to a mammal in need thereof a therapeutically effective amount of a compound of Formula I: | 02-13-2014 |
20140045817 | TRIAZOLOPYRIDINE COMPOUNDS AS PIM KINASE INHIBITORS - Provided herein is a method of treating a PIM-1 and/or PIM-2 and/or PIM-3 kinase-mediated condition in a mammal, which comprises administering to said mammal a therapeutically effective amount of a compound of Formula I: | 02-13-2014 |
20140023643 | N4-PHENYL-QUINAZOLINE-4-AMINE DERIVATIVES AND RELATED COMPOUNDS AS ERBB TYPE I RECEPTOR TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF HYPERPROLIFERATIVE DISEASES - This invention provides compounds of Formula I | 01-23-2014 |
20140018399 | MITOTIC KINESIN INHIBTORS AND METHODS OF USE THEREOF - This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders. | 01-16-2014 |
20140005418 | 6-SUBSTITUTED PHENOXYCHROMAN CARBOXYLIC ACID DERIVATIVES | 01-02-2014 |
20140005213 | TRIAZOLOPYRIDINE COMPOUNDS AS PIM KINASE INHIBITORS | 01-02-2014 |
20130338140 | SERINE/THREONINE KINASE INHIBITORS - Compounds having the formula I wherein Z, Z | 12-19-2013 |
20130252934 | SERINE/THREONINE KINASE INHIBITORS - Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt 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. | 09-26-2013 |
20130231301 | COMBINATION OF CHECKPOINT KINASE I INHIBITORS AND WEE I KINASE INHIBITORS - A combination of a CHK1 inhibitor and a WEE1 inhibitor are provided. | 09-05-2013 |
20130195971 | PHARMACEUTICAL COMPOSITION 271 - The invention concerns pharmaceutical compositions containing a hydrogen sulphate salt of 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide and solvates, crystalline forms and amorphous forms thereof, to the use of said compositions as a medicament; and to processes for the preparation of said compositions. | 08-01-2013 |
20130143865 | PYRIMIDYL 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 |
20130131039 | 5,7-SUBSTITUTED-IMIDAZO[1,2-C]PYRIMIDINES AS INHIBITORS OF JAK KINASES - Compounds of Formula I: (Formula should be inserted here) and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R | 05-23-2013 |
20130085135 | 5H-CYCLOPENTA[D]PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS - Compounds of Formula I are useful for inhibiting AKT protein kinases. Methods of using compounds of Formula I and stereoisomers 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. | 04-04-2013 |
20130072500 | PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds of Formula I including tautomers, resolved enantiomers, resolved diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. | 03-21-2013 |
20130065908 | DIHYDROFURO PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: | 03-14-2013 |
20130065901 | 2-AMINOPYRIDINE ANALOGS AS GLUCOKINASE ACTIVATORS - Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase. | 03-14-2013 |
20130045286 | PYRROLOPYRIDINES AS KINASE INHIBITORS - Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers 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. | 02-21-2013 |
20130018033 | RAF 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 |
20120329808 | DIHYDROTHIENO PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: | 12-27-2012 |
20120277277 | Methods of Treating a Hyperproliferative Disorder or Inhibiting Cell Growth in a Mammal - Disclosed are methods for inhibiting abnormal cell growth or treating hyperproliferative diseases in mammals, comprising administering to a mammal in heed thereof a pharmaceutical composition comprising 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, or a pharmaceutically acceptable salt thereof, in combination with an effective amount of an anti-tumour agent or in combination with radiation therapy. | 11-01-2012 |
20120277242 | Pyridin-2YL-Amino-1, 2, 4-Thiadiazole Derivatives as Glucokinase Activators for the Treatment of Diabetes Mellitus - Provided are compounds of Formula (I): wherein R | 11-01-2012 |
20120263679 | Combinations Comprising Heterocyclic Inhibitors of MEK and Methods of Use Thereof - Disclosed are combinations comprising (a) a compound of the Formula: | 10-18-2012 |
20120258952 | Substituted 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 R | 10-11-2012 |
20120232055 | HYDROXYLATED 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 |
20120208995 | NOVEL MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS REPLICATION - The embodiments provide compounds of the general Formulae I through general Formula VIII, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. | 08-16-2012 |
20120208801 | Aminodiazepines as Toll-Like Receptor Modulators - Provided are compositions and methods useful for modulation signaling through the Toll-like receptor TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency. | 08-16-2012 |
20120202854 | 4-SUBSTITUTED PHENOXYPHENYLACETIC ACID DERIVATIVES - Compounds of formula (I): | 08-09-2012 |
20120178715 | SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS - Compounds of Formula I: and salts thereof in which R | 07-12-2012 |
20120165317 | 8-SUBSTITUTED BENZOAZEPINES AS TOLL-LIKE RECEPTOR MODULATORS - Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency. | 06-28-2012 |
20120157453 | RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF - Compounds of Formula II are useful for inhibition of Raf kinases. Methods of using compounds of Formula II 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 |
20120157452 | 1H-PYRAZOLO[3,4-B] PYRIDINE COMPOUNDS FOR INHIBITING RAF KINASE - Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. [FORMULA I] | 06-21-2012 |
20120157439 | RAF 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 |
20120114750 | PHARMACEUTICAL COMPOSITION 271 - The invention concerns pharmaceutical compositions containing a hydrogen sulphate salt of 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide and solvates, crystalline forms and amorphous forms thereof, to the use of said compositions as a medicament; and to processes for the preparation of said compositions. | 05-10-2012 |
20120108568 | SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS - Compounds of Formula (I) and salts thereof in which R | 05-03-2012 |
20120101103 | 7-PHENOXYCHROMAN CARBOXYLIC ACID DERIVATIVES - Compounds of Formula I: (I) in which A, A | 04-26-2012 |
20110319632 | PROCESS FOR PREPARING BENZIMIDAZOLE COMPOUNDS - Provided are compounds having Formula VIIIa-1: | 12-29-2011 |
20110319631 | PROCESS FOR PREPARING BENZIMIDAZOLE COMPOUNDS - Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ib-1: | 12-29-2011 |
20110288092 | Heterocyclic Inhibitors of MEK and Methods of Use Thereof - Disclosed are methods of treating hyperproliferative disorders, method of treating inflammatory disorders, and methods of inhibiting MEK activity in a mammal, comprising administering an effective amount of one or more compounds of the Formula V | 11-24-2011 |
20110281874 | 2-AMINOPYRIDINE ANALOGS AS GLUCOKINASE ACTIVATORS - Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase. | 11-17-2011 |
20110275608 | PIPERIDINE-CONTAINING COMPOUNDS AND USE THEREOF - A method for preventing and/or treating a metabolic disease, cerebrovascular disease, etc. which comprises administering to a mammal an effective amount of the compound of the formula (I): | 11-10-2011 |
20110245230 | PYRIMIDYL 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 |
20110195948 | Substituted Pyrazolo[1,5-a]Pyrimidine Compounds as TRK Kinase Inhibitors - Compounds of Formula (I) in which R | 08-11-2011 |
20110183981 | HETEROCYCLIC INHIBITORS OF MEK AND METHODS OF USE THEREOF - Disclosed are compounds of the Formula I | 07-28-2011 |
20110178136 | HETEROCYCLIC INHIBITORS OF MEK AND METHODS OF USE THEREOF - Disclosed are amino acid and phosphate prodrugs of compounds of the Formula V | 07-21-2011 |
20110160221 | PYRIMIDYL 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. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer. | 06-30-2011 |
20110158971 | COMPOSITIONS COMPRISING N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS AND METHODS OF USE THEREOF - Disclosed are pharmaceutical compositions comprising 6-(4-Bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, or a pharmaceutically acceptable salt thereof. Also disclosed are methods of using such compositions for inhibiting abnormal cell growth or treating hyperproliferative diseases in mammals. | 06-30-2011 |
20110144100 | TRIAZOLOPYRIDINE COMPOUNDS AS PIM KINASE INHIBITORS - Compounds of Formula (I): I in which B, R | 06-16-2011 |
20110144085 | TRIAZOLOPYRIDINE COMPOUNDS AS PIM KINASE INHIBITORS - Compounds of Formula (I), in which A, B, R | 06-16-2011 |
20110130406 | PYRAZOLO-PYRIDINES AS TYROSINE KINASE INHIBITORS - Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates 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. | 06-02-2011 |
20110124878 | KINASE INHIBITORS AND METHODS OF USE THEREOF - A compound of Formula II | 05-26-2011 |
20110118235 | SUBSTITUTED BENZOAZEPINES AS TOLL-LIKE RECEPTOR MODULATORS - Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease. | 05-19-2011 |
20110105463 | 6-SUBSTITUTED PHENOXYCHROMAN CARBOXYLIC ACID DERIVATIVES - Compounds of Formula (I): in which A | 05-05-2011 |
20110092485 | SUBSTITUTED BENZOAZEPINES AS TOLL-LIKE RECEPTOR MODULATORS - Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease. | 04-21-2011 |
20110092479 | PYRAZOLE [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 |
20110070317 | PYRROLOPYRIDINES AS KINASE INHIBITORS - Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers 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. | 03-24-2011 |
20110065716 | HYDROXYLATED PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds, including pharmaceutically acceptable salts thereof, comprising the Formula (I): Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases, such as cancer. | 03-17-2011 |
20110053959 | PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds of Formula (I) including tautomers, resolved enantiomers, resolved diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as Akt protein kinase inhibitors and for the treatment of Akt-mediated diseases, for example, hyperproliferative diseases such as cancer. | 03-03-2011 |
20110015204 | PYRIMIDYL 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. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer. | 01-20-2011 |
20110003859 | N- (6-AMINOPYRIDIN-3-YL) -3- (SULFONAMIDO) BENZAMIDE DERIVATIVES AS B-RAF INHIBITORS FOR THE TREATMENT OF CANCER - Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers 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. | 01-06-2011 |
20100331385 | PYRAZOLE UREA DERIVATIVES USED AS KINASE INHIBITORS - Compounds of Formula (I) where R | 12-30-2010 |
20100331283 | Mitotic kinesin inhibitors and methods of use thereof - This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders. | 12-30-2010 |
20100324041 | PYRROLOPYRIDINES AS KINASE INHIBITORS - Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers 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. Formula, (I). | 12-23-2010 |
20100292244 | HYDROXYLATED PYRIMIDYL CYCLOPENTANE AS AKT PROTEIN KINASE INHIBITOR - The present invention provides a compound and pharmaceutically acceptable salts thereof, comprising the Formula I. Also provided are methods of using the compound of this invention as an AKT protein kinase inhibitor and for the treatment of hyperproliferative diseases such as cancer. | 11-18-2010 |
20100280043 | PYRAZOLOPYRIDINES AS KINASE INHIBITORS - Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers 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. | 11-04-2010 |
20100267793 | METHOD OF TREATMENT USING N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS - Disclosed are methods of treating a hyperproliferative disorder or a disease related to vasculogenesis or angiogenesis in a mammal, comprising administering to said mammal an effective amount of a compound of the formula | 10-21-2010 |
20100267710 | N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS - Disclosed are compounds of the Formula I | 10-21-2010 |
20100261718 | N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS - Disclosed are compounds of the Formula | 10-14-2010 |
20100261717 | N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS - Disclosed are compounds of the Formula I | 10-14-2010 |
20100260868 | METHOD OF TREATMENT USING CHECKPOINT KINASE 1 INHIBITORS - Methods of treating cancer by administering a DNA damaging agent and a CHK1 Inhibitor on a dosing regimen are provided. | 10-14-2010 |
20100260714 | COMPOSITIONS COMPRISING N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS AND METHODS OF USE THEREOF - Disclosed are pharmaceutical compositions comprising 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, or a pharmaceutically acceptable salt thereof. Also disclosed are methods of using such compositions for inhibiting abnormal cell growth or treating hyperproliferative diseases in mammals. | 10-14-2010 |
20100234378 | ALKYLSULFONAMIDE-SUBSTITUTED TRIAZOLES AS MATRIX METALLOPROTEASE INHIBITORS - Provided are MMP-2, MMP-3, MMP-9, MMP-12 and/or MMP-13 inhibitors having the Formula (I): wherein R | 09-16-2010 |
20100216989 | METHODS OF SYNTHESIS OF BENZAZEPINE DERIVATIVES - The disclosure describes method of synthesis of substituted benzazepine derivatives. Preferred methods according to the disclosure allow for large-scale preparation of benzazepine compounds having low levels of metal impurities. In some embodiments, preferred methods according to the disclosure also allow for the preparation of benzazepine derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. The methods disclosed herein find utility in synthetic organic chemistry as well as medicinal chemistry. | 08-26-2010 |
20100204240 | Pyridin-2-YL-Amino-1, 2, 4-Thiadiazole Derivatives as Glucokinase Activators for the Treatment of Diabetes Mellitus - Provided are compounds of Formula (I): wherein R | 08-12-2010 |
20100173955 | 4-SUBSTITUTED PHENOXYPHENYLACETIC ACID DERIVATIVES - Compounds of Formula (I): in which R | 07-08-2010 |
20100145065 | PROCESS FOR PREPARING BENZIMIDAZOLE COMPOUNDS - Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-1 and their synthetic intermediates: wherein Z, X | 06-10-2010 |
20100144751 | IMIDAZO[1,2-a]PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS - Compounds of Formula (I): are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class (3) and class (5) receptor tyrosine kinases. Particular compounds of this invention have also been found to be inhibitors of Pim-1. | 06-10-2010 |
20100130748 | SNAR PROCESS FOR PREPARING BENZIMIDAZOLE COMPOUNDS - Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-2 and their synthetic intermediates: wherein X | 05-27-2010 |
20100099713 | 2-AMINOPYRIDINE DERIVATIVES AS GLUCOKINASE ACTIVATORS - Provided are compounds having the Formula I | 04-22-2010 |
20100099697 | Method of Treatment Using Inhibitors of Mitosis - Methods of treating diseases caused by cell division or that are treated by inhibiting mitosis by administering two doses of an inhibitor of mitosis between the biologically effective dose and the maximum tolerated dose in a dosing cycle that allows for the recovery or subsiding of side effects, wherein the second dose is administered 24 to 48 hours after the first dose. | 04-22-2010 |
20100063066 | RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF - Compounds of Formulas (I), (IIA) and (IIIA) are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formulas (I), (IIA) and (IIIA) and stereoisomers 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. | 03-11-2010 |
20100063053 | HETEROCYCLIC INHIBITORS OF MEK AND METHODS OF USE THEREOF - Disclosed are compounds of the Formulas I and V | 03-11-2010 |
20100056530 | GLUCOKINASE ACTIVATORS - Provided are compounds of Formula I wherein R | 03-04-2010 |
20100041719 | MITOTIC KINESIN INHIBITORS AND METHODS OF USE THEREOF - This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment of various disorders. | 02-18-2010 |
20100029633 | IMIDAZO[1,2-A]PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS - Compounds of Formula I: in which A, B, R | 02-04-2010 |
20090297476 | NOVEL PEPTIDE INHIBITORS OF HEPATITIS C VIRUS REPLICATION - The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments provide compounds of the general Formula II, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. | 12-03-2009 |
20090270621 | QUINAZOLINE ANALOGS AS RECEPTOR TYROSINE KINASE INHIBITORS - This invention concerns quinazoline analogs of Formula I: | 10-29-2009 |
20090247526 | GLUCOKINASE ACTIVATORS - Provided are compounds of formula I | 10-01-2009 |
20090246274 | PHARMACEUTICAL COMPOSITION 271 - The invention concerns pharmaceutical compositions containing a hydrogen sulphate salt of 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide and solvates, crystalline forms and amorphous forms thereof, to the use of said compositions as a medicament; and to processes for the preparation of said compositions. | 10-01-2009 |
20090215834 | HETEROCYCLIC INHIBITORS OF MEK AND METHODS OF USE THEREOF - Disclosed are compounds of the Formula V | 08-27-2009 |
20090209554 | Thiazoliums as transketolase inhibitors - The present invention provides N-3′-pyridyl-methyl or N-2′-pyrazinylmethyl thiazolium derivatives of formula (I) which are useful as transketolase inhibitors wherein R | 08-20-2009 |
20090209542 | HETEROCYCLIC INHIBITORS OF MEK AND METHODS OF USE THEREOF - Disclosed are compounds of the Formula I | 08-20-2009 |
20090169510 | NOVEL MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS REPLICATION - The embodiments provide compounds of the general Formulae I through general Formula VIII, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. | 07-02-2009 |
20090156603 | 2-AMINOPYRIDINE ANALOGS AS GLUCOKINASE ACTIVATORS - Provided are compounds of formula I that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes meilitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase. | 06-18-2009 |
20090149459 | P38 INHIBITORS AND METHODS OF USE THEREOF - This invention relates to inhibitors of p38 and methods of utilizing the inhibitors and pharmaceutical compositions thereof in the treatment and prevention of various disorders mediated by p38. | 06-11-2009 |
20090148407 | Novel Macrocyclic Inhibitors of Hepatitis C Virus Replication - The embodiments provide compounds of the general Formulae (I) through general Formula (VIII), as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. | 06-11-2009 |
20090143579 | Heterocyclic Inhibitors of MEK and Methods of Use Thereof - Disclosed are compounds of the Formula I | 06-04-2009 |
20090143422 | P38 INHIBITORS AND METHODS OF USE THEREOF - This invention relates to inhibitors of p38 and methods of utilizing the inhibitors and pharmaceutical compositions thereof in the treatment and prevention of various disorders mediated by p38. | 06-04-2009 |
20090143389 | HETEROCYCLIC INHIBITORS OF MEK AND METHODS OF USE THEREOF - Disclosed are compounds of the Formulas III and IV | 06-04-2009 |
20090136596 | P38 INHIBITORS AND METHODS OF USE THEREOF - This invention relates to inhibitors of p38 and methods of utilizing the inhibitors and pharmaceutical compositions thereof in the treatment and prevention of various disorders mediated by p38. | 05-28-2009 |
20090131435 | HETEROCYCLIC INHIBITORS OF MEK AND METHODS OF USE - Disclosed are compounds of the Formula | 05-21-2009 |
20090048279 | QUINAZOLINE ANALOGS AS RECEPTOR TYROSINE KINASE INHIBITORS - This invention provides quinazoline analogs of Formula I: | 02-19-2009 |
20090048224 | COMPOUNDS AND METHODS OF USE - Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes. | 02-19-2009 |
20090012290 | CYANOGUANIDINES AND CYANOAMIDINES AS ERBB2 AND EGFR INHIBITORS - Cyanoguanidine quinazoline and cyanoamidine quinazolamine derivatives that are useful in the treatment of hyperproliferative diseases are disclosed. Methods of treating hyperproliferative diseases in mammals are also disclosed. | 01-08-2009 |
20080280957 | Heterocyclic Inhibitors of Mek and Methods of Use Thereof - Disclosed are MEK inhibitors useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds. | 11-13-2008 |
20080234251 | 8-Substituted Benzoazepines as Toll-Like Receptor Modulators - Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency. | 09-25-2008 |