Neurocrine Biosciences, Inc.

Other

Keith M Wilcoxen

Chen Chen

James R McCarthy

Charles Q Huang

Mustapha Haddach

Terence J Moran

Raymond Stanley Gross

Thomas R Webb

Richard Christopher Oglesby

Fabio C Tucci

Yun-Fei Zhu

R Scott Struthers

Yinghong Gao

Patrick J Connors

Mustapha Hadduch

This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein Ris NRRor OR; Ris Calkyl, Calkyloxy or Calkylthio; Ris hydrogen, Calkyl, Calkylsulfonyl, Calkylsulfoxy or Calkylthio; Ris hydrogen, Calkyl, mono- or di(Ccycloalkyl)methyl, Ccycloalkyl, Calkenyl, hydroxyCalkyl, CalkylcarbonyloxyCalkyl or CalkyloxyCalkyl; Ris Calkyl, mono- or di(Ccycloalkyl)methyl, ACH, CalkyloxyCalkyl, hydroxyCalkyl, Calkenyl, thienylmethyl, furanylmethyl, CalkylthioCalkyl, morpholinyl, mono- or di(Calkyl)aminoCalkyl, di(Calkyl)amino, CalkylcarbonylCalkyl, Calkyl substituted with imidazolyl; or a radical of formula &#x2014;Alk&#x2014;O&#x2014;CO&#x2014;Ar; or Rand Rtaken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).

Pyrazolopyrimidines as CRF receptor antagonists

Methods of making substituted pyrazolopyrimidines generally and, more particularly, N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-&#x3b1;]-pyrimidin-7-yl}phenyl)acetamide. Such compounds have utility over a wide range of indications, including treatment of insomnia. In the practice of the present invention, improved techniques which do not require use and/or isolation of the pyrazole intermediate are disclosed, as well as improved techniques for making the reaction intermediates themselves. Such techniques offer significant advantages, including enhanced efficiency, particularly in the context of large scale manufacture.

Synthesis of substituted pyrazolopyrimidines

CRF antagonistic pyrazolo&lsqb;4,3-b&rsqb;pyridines

CRF antagonistic quino-and quinazolines

CRF antagonistic quino- and quinazolines

Methods of making substituted pyrazolopyrimidines generally and, more particularly, N-methyl-N-(3-&lcub;3-&lsqb;2-thienylcarbonyl&rsqb;-pyrazol-&lsqb;1,5-&agr;&rsqb;pyrimidin-7-yl&rcub;phenyl)acetamide. Such compounds have utility over a wide range of indications, including treatment of insomnia. In the practice of the present invention, improved techniques which do not require use and/or isolation of the pyrazole intermediate are disclosed, as well as improved techniques for making the reaction intermediates themselves. Such techniques offer significant advantages, including enhanced efficiency, particularly in the context of large scale manufacture.

Gonadotropin-releasing hormone receptor antagonists and methods relating thereto

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San Diego, CA, United States of America

Keith M Wilcoxen