Millennium Pharmaceuticals Limited

Abbott Laboratories Corporation

James A Brown

Michael A Patane

Susan Laurene Acton

Natalie Alysia Dales

Bing Guan

Timothy D Ocain

Alexandra E Gould

Andrew J Souers

Philip R Kym

Anil Vasudevan

Matthew J LaMarche

Rajesh R Iyengar

Martin P Maguire

Su-Jen Lai

Mathew M Mulhern

Michael E Solomon

Christopher Blackburn

Courtney A Cullis

Dariusz Wodka

Ju Gao

John K Lynch

Jennifer C Freeman

Alain Stricker-Krongrad

Mary Katherin Verzal

Vivek J Kadambi

Jennifer L Che

ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include compounds of formula (I):Z-&#x39b;&#x2003;&#x2003;(I)Wherein Z is a zinc coordinating moiety and &#x39b; is an amino-acid mimicking moiety, and pharmaceutically acceptabale salts thereof. Methods of using the inhibitors and pharmaceutical compositions containing the inhibitors to treat a body weight disorder, to decrease appetite, to increase muscle mass, to decrease body fat, to treat diabetes and to treat a state associated with altered lipid metabolism, are also described.

ACE-2 modulating compounds and methods of use thereof

This invention provides compounds that are antagonists of melanin concentrating hormone receptor-1 (MCH-R1). The compounds are represented by formula I:where m is zero or one, n is zero to two, Y is oxygen or &#x2014;N(R)&#x2014;, R, R, R, R, R, Rand Ring A are defined in the specification. Coumarin and quinolone compounds where Rand Rtogether form a fused benzo ring are preferred. The invention also provides compounds of formula VI where the coumarin moiety is replaced by a quinazolinone ring. The compounds are useful for treating MCH-R1-related disorders, particularly overweight conditions including obesity.

Antagonists of melanin concentrating hormone receptor

ACE-2 inhibiting compounds and methods of use thereof

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Framingham, MA, United States of America

James A Brown