Elan Pharmaceuticals, Inc.

Cymabay Therapeutics, Inc.

David W G Wone

Michael A Pleiss

Jay S Tung

Darren B Dressen

Jing Wu

Albert W Garofalo

Ashley C Guinn

Jiangao Song

Xin Chen

Jingyuan Ma

R Jeffrey Neitz

Imad Nashashibi

Phuongly Pham

Aaron Robert Novack

Martin Neitzel

Dong-Fang Shi

Jennifer Marugg

Jeffrey D Johnson

Lee H Latimer

Charles A McWherter

John Alan Tucker

Xueyan Wang

Brian Edward Lavan

Jennifer Sealy

Scott A Jenkins

The present disclosure relates to compounds that act as agonists of, or otherwise modulate the activity of, GPR131 and to their use in the treatment of various diseases. In particular embodiments, the structure of the compounds is given by Formula I: wherein the variables are as described herein. Related compositions, formulations and methods for the preparation of compounds of formula I are also described.

Bicyclic agonists of GPR131 and uses thereof

Chemical compounds which act as agonists of, or otherwise modulate the activity of, GPR131 are disclosed. Related compositions, formulations and methods of use are also described.

Agonists of GPR131 and uses thereof

This invention is directed to acylated amino acid amidyl pyrazoles and related compounds of Formula I. The invention is also directed to a pharmaceutical formation comprising such compound or in a pharmaceutically acceptable salt form thereof. The invention is further directed to a method for inhibiting &#x3b2;-amyloid peptide release and/or synthesis, a method for inhibiting &#x3b3;-secretase activity, and a method for treating neurological disorders associated with &#x3b2;-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.

Acylated amino acid amidyl pyrazoles and related compounds

Disclosed are compounds that are bradykinin Breceptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin Breceptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action.

[object Object]

Disclosed are compounds of formula I and II that are bradykinin Breceptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin Breceptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action. 

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Newark, CA, United States of America

David W G Wone