Neurocrine Biosciences, Inc.

Smithkline Beecham (cork) Ltd

Syntex (u.s.a.) Inc.

Roche Palo Alto LLC

Sb Cork

John Patrick Williams

Manisha Moorjani

Deborah Slee

Neil Ashweek

Mustapha Haddach

Marion Lanier

Daniel Harry Rogers

John Edward Tellew

Long Mao

Michael Schwaebe

Daisy Joe Du Bois

John Saunders

Zhiyong Luo

Dragan Marinkovic

Jane Han Bu

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 may have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in mammals. The CRF receptor antagonists of this invention have the following structure: (I); and pharmaceutically acceptable salts, esters, solvates, stereoisomers and prodrugs thereof, wherein R, R, R, Y, Het, n, o, R, Ar and Rare 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.

Pyrazolo[1,5-alpha]pyrimidinyl derivatives useful as corticotropin-releasing factor (CRF) receptor antagonists

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

CRF receptor antagonists are disclosed which may have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in mammals, such as stroke. The CRF receptor antagonists of this invention have the following structure: and pharmaceutically acceptable salts, esters, solvates, stereoisomers and prodrugs thereof, wherein R, R, n, R, Ar, and Het are as defined herein. Compositions containing a CRF receptor antagonists in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.

Compounds of Formula (I):wherein Aris aryl; Aris hydrogen, cycloalkyl, aryl or heteroaryl; Z is &#x2014;C(&#x2550;O) or a single bond; R, R, R, Rand Rare independently hydrogen or alkyl optionally substituted with hydroxy; alk is an alkylene chain of one to six carbon atoms; X is &#x2014;O&#x2014;, &#x2014;NR(where Ris hydrogen or alkyl), (CRR)(where Rand Rare independently in each occurrence hydrogen or alkyl and m is an integer from 0 to 3), or &#x2014;S(O)(wherein n is an integer from 0 to 2); or prodrugs thereof, and pharmaceutically acceptable salts thereof,are inhibitors of CCR3 useful for treating eosinophil induced diseases such as asthma.

2,5-substituted pyrimidine derivatives-CCR-3 receptor antagonists

This invention relates to certain 3-aminomethylpyrrolidine derivatives of Formula (I): ##STR1## that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Pyrrolidine derivatives-CCR-3 receptor antagonists

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San Diego, CA, United States of America

John Patrick Williams