Bristol-Myers Squibb Compnay

Wyeth

Albany Molecular Research, Inc.

Rulin Zhao

Bang-Chi Chen

Joseph E Sundeen

Bei Wang

Richard Eric Mewshaw

Kyoung S Kim

Raj N Misra

Boguslaw Mudryk

S David Kimball

Gary Paul Stack

Katerina Leftheris

Stephen T Wrobleski

Mark E Salvati

Megan Tran

Nicolas Cuniere

Huiping Zhang

Jing Liang

Lucius Rossano

Dau-Ming Hsieh

Adrian David

Jagabandhu Das

Alaric J Dyckman

Chunjian Liu

Hai-Yun Xiao

Michael E Randazzo

Shuang Liu

John V Duncia

Michael G Yang

John T Hynes

Percy H Carter

Wei Meng

Peter Tai Wah Cheng

Zili Xiao

Matthew L Isherwood

Wenge Cui

Min Hu

Paul C Lobben

Rasidul Amin

Yuh-lin Allen Yang

Mark Liu

Hai-Yun Xia

A compound, enantiomer, prodrug, diastereomer, or salt is provided which is an activator of the enzyme glucokinase and thus is believed to be useful in as treating diabetes and related diseases, which compound has the structure (I). A method for treating diabetes and related disease employing the compound, enantiomer, prodrug, diastereomer, or salt is also provided. 

Glucokinase activators and methods of using same

Disclosed are processes for preparing tetrahydroisoquinolines, intermediates useful in the preparation of tetrahydroisoquinolines, processes for preparing such intermediates, and a crystalline form of 6-[(4S)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. Also disclosed are pharmaceutical compositions comprising tetrahydroisoquinolines, methods of using tetrahydroisoquinolines in the treatment of depression and other conditions and methods for obtaining the crystalline form. One such intermediate has the following structure: 

Tetrahydroisoquinolines and intermediates therefor

The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino) pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R, R, R, R, and are as described herein. Compounds that are useful intermediates of the process are also provided herein.

Substituted pyrrolidine-2-one compounds

The invention is directed to processes for preparing 2-aminothiazole-5-carboxamides of formula I 

Process for preparing 2-aminothiazole-5-carboxamides useful as kinase inhibitors

The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R, R,R, R, and are as described herein. Compounds that are useful intermediates of the process are also provided herein.

[object Object]

The present invention relates to compounds having the formula, and pharmaceutically-acceptable salts, prodrugs, solvates, isomers, and/or hydrates thereof, wherein Q is an optionally-substituted phenyl, pyridyl, pyridazinyl, pyrimidinyl, or pyrazinyl ring; Ris alkyl or an amino group as defined herein; and Z is optionally-substituted oxadiazolyl or &#x2014;C(&#x2550;O)NR, wherein Ris lower alkyl or cyclopropyl. The compounds are surprisingly advantageous in preparing pharmaceutical compositions for treating p38 kinase related conditions and/or in methods of treating conditions associated with the activity of p38 kinase in a patient.

Aryl-substituted pyrazole-amide compounds useful as kinase inhibitors

A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds can be useful as factor Xa inhibitors.

Efficient synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones

A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described.  These compounds can be useful as factor Xa inhibitors.

The present invention relates to compounds having the formula, and pharmaceutically-acceptable salts, prodrugs, solvates, isomers, and/or hydrates thereof, wherein Q is an optionally-substituted pyridyl, ring; Ris alkyl or an amino group as defined herein; and Z is optionally-substituted C(&#x2550;O)NR, wherein Ris lower alkyl or cyclopropyl. The compounds are surprisingly advantageous in preparing pharmaceutical compositions for treating p38 kinase related conditions and/or in methods of treating conditions associated with the activity of p38 kinase in a patient.

An improved process for the preparation of certain pyrrolotriazine compounds is disclosed. The compounds exhibit utility as kinase inhibitors.

Process for preparing pyrrolotriazine kinase inhibitors

Compounds of the formulauseful for the treatment of such as depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder (including trichotillomania), social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addition, sexual dysfunction (including premature ejaculation), and related illnesses.

Antidepressant azahetorocyclylmethyl derivatives of 7,8-dihydro-6H-5-oxa-1-aza-phenathrene

Antidepressant azaheterocyclyl methyl derivatives of 7,8-dihydro-6H-5-oxa-1-aza-phenanthrene

This invention relates to novel processes for the preparation of amino isoquinolines, benzylamino isoquinolines, and acid derivatives useful as serine protease inhibtors.

Processes for the preparation of acid derivatives useful as serine protease inhibitors

Compounds of the formulauseful for the treatment of such as depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as premenstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder (including trichotillomania), social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addition, sexual dysfunction (including premature ejaculation), and related illnesses.

Antidepressant azaheterocyclylmethyl derivatives of 7,8-dihydro-6H-5-oxa-1-aza-phenanthrene

Growing community of inventors

Pennington, NJ, United States of America

Rulin Zhao