Donald J Graham

US Patent:

8178546, May 15, 2012

Filed:

Apr 14, 2010

Appl. No.:

12/759737

Inventors:

Susan D. Aster - Teaneck NJ, US
James M. Balkovec - Martinsville NJ, US
Donald W. Graham - Mountainside NJ, US
Xin Gu - Scotch Plains NJ, US
Nancy J. Kevin - East Brunswick NJ, US
Gool F. Patel - Califon NJ, US
Mitree Ponpipom - Branchburg NJ, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

C07D 249/08

US Classification:

5142664

Abstract:

2,5-Diaryl-1,2,4-triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase Type 1 enzyme (11β-HSD-1). The compounds are useful for the treatment of diabetes, hyperglycemia, obesity, insulin resistance, atherosclerosis, dyslipidemia, hyperlipidemia, hypertension, and Metabolic Syndrome. Also disclosed are novel compounds of structural formula II which are inhibitors of 11β-HSD-1.

US Patent:

20080255216, Oct 16, 2008

Filed:

Mar 25, 2005

Appl. No.:

10/593010

Inventors:

Susan D. Aster - Teaneck NJ, US
James M. Balkovec - Martinsville NJ, US
Donald W. Graham - Mountainside NJ, US
Xin Gu - Scotch Plains NJ, US
Nancy J. Kevin - East Brunswick NJ, US
Gool F. Patel - Califon NJ, US
Mitree Ponpipom - Branchburg NJ, US

International Classification:

A61K 31/4196
C07D 249/08
A61P 3/04
A61P 9/12
A61P 9/10
A61P 3/10
C07D 403/02

US Classification:

514383, 5482622, 5482664

Abstract:

2,5-Diaryl-1,2,4-triazole derivatives of structural formula I are selective inhibitors of the 11&bgr;-hydroxysteroid dehydrogenase Type 1 enzyme (11&bgr;-HSD-1). The compounds are useful for the treatment of diabetes, hyperglycemia, obesity, insulin resistance, atherosclerosis, dyslipidemia, hyperlipidemia, hypertension, and Metabolic Syndrome. Also disclosed are novel compounds of structural formula II which are inhibitors of 11&bgr;-HSD-1.

US Patent:

58860053, Mar 23, 1999

Filed:

May 6, 1997

Appl. No.:

8/817965

Inventors:

Susan D. Aster - Teaneck NJ
Donald W. Graham - Mountainside NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A01N 4342
C07D22102

US Classification:

514284

Abstract:

Compounds of the formula ##STR1## are inhibitors of 5. alpha. -reductase and are useful alone or in combination with other active agents for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.

US Patent:

57417954, Apr 21, 1998

Filed:

Oct 17, 1996

Appl. No.:

8/732953

Inventors:

Susan D. Aster - Teaneck NJ
Donald W. Graham - Mountainside NJ
Derek J. Von Langen - Fanwood NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31715

US Classification:

514284

Abstract:

Compounds of the formula I ##STR1## are inhibitors of 5. alpha. -reductase, and are useful for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, prostatic carcinoma, prostatitis and benign prostatic hyperplasia.

US Patent:

54380618, Aug 1, 1995

Filed:

Jul 16, 1993

Appl. No.:

8/093107

Inventors:

Jeffrey P. Bergman - Ridgefield Park NJ
Donald W. Graham - Mountainside NJ
Gary H. Rasmusson - Watchung NJ
Richard L. Tolman - Warren NJ
Derek Von Langen - Fanwood NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D22118
A61K 3144

US Classification:

514284

Abstract:

Compounds of the formula I ##STR1## wherein R. sub. 1 hydrogen or methyl; R. sub. 2 is methyl; R. sub. 3 hydrogen, Alk-R. sub. 4, X-Alk, C. sub. 1-6 -X-Alk, XCO-Alk, CN, CO-Alk, CO-Ar, CO-O-Alk, CO-NH-Alk, CO-NH-Ar, CO-NH-Het and CO-N(Alk). sub. 2 ; Alk is C. sub. 1-12 straight or branched alkyl; Ar is phenyl, Het is piperidinyl, piperizinyl, pyrrolidinyl, pyrrolyl, furanyl or thienyl and X is O, N or S. Such compounds are useful in the treatment of pathologic conditions that benefit from blockade of isozymes of 5. alpha. -reductase.