Bristol-myers Squibb Compnay

E. R. Squibb Sons, Inc.

Bristol-myers Squibb

Harvard College

Other

E. R. Squibbs & Sons, Inc.

University of Pennsylvania

Jeffrey A Robl

Jun Li

Richard B Sulsky

Lawrence G Hamann

David R Magnin

Joseph Anthony Tino

James J Li

Andres S Hernandez

Scott A Biller

David John Augeri

Haixia Wang

Lawrence J Kennedy

Khehyong Ngu

Chong-qing Sun

Donald S Karanewsky

William N Washburn

Tammy C Wang

John K Dickson

Xiang-Yang Ye

R Michael Lawrence

Saleem Ahmad

Michael A Poss

Yan Shi

James Clifford Sutton

Rajeev S Bhide

Louis John Lombardo

Zhen-Wei Cai

Rex A Parker

Ligang Qian

Stephanie Barbosa

Ligaya Simpkins

Ying Wang

Dean A Wacker

David S Weinstein

David A Betebenner

William A Slusarchyk

Mark E Salvati

Shung C Wu

Chongqing Sun

Yingzhi Bi

Chenkou Wei

Zheming Ruan

Christopher Blair Cooper

Michael A Galella

Stephen P O'Connor

Alexandra Holubec

Haris Jamil

Bruce L Jacobson

Krishna Kodukula

Jie Jack Li

Yan-Ting Huang

Chunhong He

Ramesh N Patel

Joel C Barrish

David R Kronenthal

Hao Zhang

Pratik Devasthale

Edward W Petrillo, Jr

Denis E Ryono

Steven P Seitz

Philip D Stein

Bang-Chi Chen

Ronald L Hanson

Jay A Markwalder

Peter T W Cheng

Mark C Manfredi

Shiwei Tao

David J Carini

Steven J Walker

Xinhua Qian

Gokhan S Hotamisligil

Sutjano Jusuf

David S Yoon

Thomas Caulfield

Zhiwei Guo

Rajendra P Deshpande

Stephen G Swartz

Laxma Reddy Kolla

Mark S Kirby

Reginald O Cann

Ashish Khanna

Zhenghua Wang

Jollie D Godfrey

John R Wetterau

Henry M Holava

John E Lawson

Daru Young Sharp

Richard A Partyka

Richard E Gregg

Peter TW Cheng

Stephen P O'CONNOR

Ligaya M Simpkins

The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.

Cyclopropanecarboxylic acid GPR120 modulators

Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R, R, R, R, R, R, R, R, R, R, and Rare defined herein, are provided which are TGR5 G protein-coupled receptor modulators. TGR5 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring TGR5 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the TGR5 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds. 

Bicyclic nitrogen containing heteroaryl TGR5 receptor modulators

Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, D, Di, E, J, L, n, Q, Rand Rare defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds. 

Bicyclic heteroaryl compounds as GPR119 modulators

Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, L, m, n, o, p, R, R, R, Rand Rare defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds. 

Benzofuranyl analogues as GPR119 modulators

The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I. 

Substituted thieno[3,2-d]pyrimidinones as MCHR1 antagonists and methods for using them

MCHR1 antagonists are provided having the following Formula I: wherein all of the variables are defined herein. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.

Pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists

Novel compounds are provided which are 1 1-beta-hydroxysteroid dehydrogenase type I inhibitors. 1 1-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 1 1-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: W-L-Z or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, L are defined herein and Z is selected from the following bicyclic heteroaryl groups: (a), (b), (c), (d). 

Substituted [1,2,4]triazolo[4,3-A]pyrazine 11-beta-hydroxysteroid dehydrogenase inhibitors

Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds of formula I: or stereoisomers or pharmaceutically acceptable salts thereof, wherein G, Q, X, Y, R, R, and Rare defined herein.

Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors

Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula where A method is also provided for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor *or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.

Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method

Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure formula (I) enantiomers, diastereomers, solvates, salts, tautomers or prodrugs thereof wherein, A, W, X, Y and Rare defined herein. 

Pyridone/hydroxypyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors

Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, or salts thereof, wherein A, W, X and Z are defined herein.

Cyclic 11-beta hydroxysteroid dehydrogenase type 1 inhibitors

Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof wherein W, L, R, R, Rand Rare defined herein.

The present invention provides compounds having the following Formula IA and IB, which are useful as MCHR1 antagonists, and includes prodrugs and pharmaceutically acceptable salts thereof: 

Substituted thieno[3,2-D]pyrimidines as melanin concentrating hormone receptor-1 antagonists

Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein R, Rand Rare defined herein.

Triazine 11-beta hydroxysteroid dehydrogenase type 1 inhibitors

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Newtown, PA, United States of America

Jeffrey A Robl