Abstract: The present invention discloses and claims compounds of formula (I) and formula (II) as inhibitors of human casein kinase I?, and methods of using the compounds of formula (I) and formula (II) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. The R-group substituents are defined herein and pharmaceutical compositions comprising compounds of formula (I) or formula (II) are also disclosed and claimed.
Type:
Grant
Filed:
February 13, 2007
Date of Patent:
December 8, 2009
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
William Arthur Metz, Jr., Fa-Xiang Ding
Abstract: The present invention discloses and claims compounds of formula (I) as inhibitors of human casein kinase IF, and methods of using said compounds of formula (I) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. Pharmaceutical compositions comprising compounds of formula (I) and methods for the preparation of compounds of formula (I) are also disclosed and claimed.
Type:
Grant
Filed:
December 1, 2004
Date of Patent:
July 22, 2008
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
William A. Metz, Jr., Frank Halley, Gilles Dutruc-Rosset, Yong Mi Choi-Sledeski, Gregory Bernard Poli, David Marc Fink, Gilles Doerflinger, Bao-Guo Huang, Ann Marie Gelormini, Juan Antonio Gamboa, Andrew Giovanni, Joachim E. Roehr, Joseph T. Tsay, Fernando Camacho, William Joseph Hurst, Stephen Wayne Harnish, Yulin Chiang
Abstract: An ethanol solvate form of (−)-cis-2-(2-chlorophenyl)-5,7-dihydroxy-8[4R-(3S-hydroxy-1-methyl)piperidinyl]-4H-1-benzopyran-4-one hydrochloride (Form II), a method of making Form II and a composition comprising Form II.
Abstract: This invention discloses and claims a series of mercaptoacetylamide derivatives of formula I. Also disclosed and claimed are pharmaceutical compositions incorporating these compounds and processes for preparing said compounds.
Type:
Grant
Filed:
April 8, 2002
Date of Patent:
August 5, 2003
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Gary A. Flynn, Barbara A. Anderson, Manfred Gerken, Bernd Jablonka, Heinz-Werner Kleemann, Wolfgang Linz, Werner Seiz, Bernhard Seuring
Abstract: The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula (1):
and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
Abstract: The invention relates to 20&xgr;-fluoropregna-4,17(20)-dien-3-on-21-oic acid ethyl ester, 20&xgr;-fluoro-3&bgr;-hydroxypregna-5,17(20)-dien-21-oic acid ethyl ester, 20&xgr;-fluoro-21-hydroxypregna-4,17 (20)-dien-3-one, 20&xgr;-fluoropregna-5,17(20)-dien-3&bgr;,21-diol and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17,20 lyase, 5&agr;-reductase and C17-hydroxylase, and to the use of these compounds in the treatment of androgen and estrogen mediated or dependent disorders, including benign prostatic hyperplasia, prostate cancer, breast cancer and DHT-mediated disorders such as acne and hirsutism. Treatment of disorders related to the over synthesis of cortisol, for example, Cushing's Syndrome are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide.
Type:
Grant
Filed:
June 21, 2001
Date of Patent:
July 2, 2002
Assignee:
Aventis Pharmaceuticals, Inc.
Inventors:
Norton P. Peet, Philip M. Weintraub, Joseph P. Burkhart, Cynthia A. Gates
Abstract: The invention related to 4-aza-17&bgr;-(cyclopropoxy)-androst-5&agr;-androstan-3-one, 4-aza-17&bgr;-(cyclopropylamino)-androst-4-en-3-one and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17-20 lyase, 5&agr;-reductase and C17&agr;-hydroxylase and to the use of these compounds in the treatment of androgen and estrogen mediated disorders, including benign prostatic hyperplasia, androgen mediated prostate cancer, estrogen mediated breast cancer and to DHT-mediated disorders such as acne. Disorders relating to the oversynthesis of cortisol, for example, Cushing's Syndrome, are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide.
Type:
Grant
Filed:
February 11, 1997
Date of Patent:
April 2, 2002
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
James R. Pribish, Cynthia A. Gates, Philip M. Weintraub
Abstract: The present invention is directed to a method of using a certain compounds which are 2,19-methyleneoxy or 2,19 methylenethio bridged steroids, and related steroidal compounds as inhibitors of the enzyme steroid aromatase, 19-hydroxylase and as treatment for various estrogen dependent/mediated disorders including hormonal dependent breast cancer.
Type:
Grant
Filed:
October 26, 1999
Date of Patent:
November 6, 2001
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Norton P. Peet, J. O'Neal Johnston, Joseph P. Burkhart
Abstract: The present invention relates to novel substituted N-methyl-N-(4-(piperidin-1-yl)-2-(aryl)butyl)benzamide derivatives of the formula
stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonists. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
Type:
Grant
Filed:
June 9, 1999
Date of Patent:
October 2, 2001
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
George P. Maynard, John M. Kane, Larry D. Bratton, Elizabeth M. Kudlacz