Bristol-myers Squibb Compnay

Sterling Winthrop Inc.

University of California

Astrazeneca Ab

Sterling Drug Inc.

Karo Bio Ab

William N Washburn

Philip Michael Sher

Saleem Ahmad

Wei Meng

Bruce A Ellsworth

Lee H Latimer

Gang Wu

Khehyong Ngu

Andres S Hernandez

Carl R Illig

Jeffrey A Robl

Barbara Boland Lussier

Pratik Devasthale

Kathleen M Poss

Guohua Zhao

Edward A Dennis

Ashvinikumar V Gavai

Gregory S Bisacchi

Denis E Ryono

Philip D Stein

Alexander L Weis

Kishore V Renduchintala

James F List

Radhakrishnan Sridhar

Sharon N Bisaha

Frederick T Fiedorek

Jean Whaley

Jun Li

Jollie D Godfrey, Jr

Mark C Manfredi

Lawrence J Kennedy

Peter T Cheng

Johan Malm

Alexandra A Nirschl

Steven J Walker

Wei Wang

Haixia Wang

Chong-qing Sun

Amarendra B Mikkilineni

Neeraj Garg

Rajesh Babulal Gandhi

Murugaiah Andappan Murugaiah Subbaiah

Terry Stouch

Arvind Mathur

James Mignone

Carl B Illig

Thomas Ericsson

Mario Maldonado

Mahmoud Rahimi-Ghadim

Venkatramana M Rao

Zhenghua Wang

Barbara B Lussier

Mario Maidonado

Ravindar N Girotra

Konrad Koehler

The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are melanin concentrating hormone receptor-1 (MCHR1) antagonists which may be used as medicaments. 

Pyrrolone or pyrrolidinone melanin concentrating hormone receptor-1 antagonists

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

Methods are provided for treating obesity or causing weight loss in a mammalian subject or patient, wherein a therapeutically effective amount of an SGLT2 inhibitor alone or optionally in combination with another anti-obesity agent, is administered to a mammalian subject or patient. In addition, a pharmaceutical composition is provided which comprises an SGLT2 inhibitor, alone or in combination with another anti-obesity agent, and a pharmaceutically acceptable carrier thereof.

Methods for treating obesity employing an SGLT2 inhibitor

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 I wherein the variables are defined herein.

Azolotriazinone melanin concentrating hormone receptor-1 antagonists

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

The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein all of the variables are defined herein.

Azolopyrrolone melanin concentrating hormone receptor-1 antagonists

The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R, R, R, R, R, W, D, R, Rand Rare defined herein. 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, anxiety or intestinal inflammation, by administration of a therapeutically effective dose of a compound according to Formula I.

Pyrrolone melanin concentrating hormone receptor-1 antagonists

The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R, R, R, R, and Rare defined herein. 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 pyrazinone melanin concentrating hormone receptor-1 antagonists and methods

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

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. where R, R, R, A, R, R, R, R5and Rare as defined herein.

Non-basic melanin concentrating hormone receptor-1 antagonists

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Titusville, NJ, United States of America

William N Washburn