Neurocrine Biosciences, Inc.

The Scripps Research Institute

Smithkline Beecham (cork) Ltd

Smithkline Beecham Corporation

Almirall, S.a.

Deborah Slee

John Patrick Williams

Manisha Moorjani

Neil Ashweek

Chi-Huey Wong

Marion Lanier

Yongsheng Chen

Zhiyong Luo

John Edward Tellew

John P Williams

Karen Laslo

Xiaohu Zhang

Binh G Vong

Neil J Ashweek

Xiahou Zhang

Emily Lin

Substituted 1,2,3-triazole compounds are disclosed which have utility in the treatment of a variety of neurological disorders. The compounds provided herein have the general structure: wherein R, R, Rand n are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound provided herein in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for treating neurological disorders in a subject in need thereof.

Substituted triazoles and methods relating thereto

CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure (I), including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, Y, Ar, and het are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same. 

CRF receptor antagonists and methods relating thereto

Combinatorial libraries of HIV and FIV protease inhibitors are characterized by &#x3b1;-keto amide or hydroxyethylamine core structures flanked by on one side by substituted pyrrolidines, piperidines, or azasugars and on the other side by phenylalanine, tyrosine, or substituted tyrosines. The libraries are synthesized via a one step coupling reaction. Highly efficacious drug candidates are identified by screening the libraries for binding and inhibitory activity against both HIV and FIV protease. Drug candidates displaying clinically useful activity against both HIV and FIV protease are identified as being potentially resistive against a loss of inhibitory activity due to development of resistant strains of HIV.

HIV protease inhibitors

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Cardiff, CA, United States of America

Deborah Slee