Donald M Graham

US Patent:

6849636, Feb 1, 2005

Filed:

Dec 18, 2003

Appl. No.:

10/739716

Inventors:

Sherman T. Waddell - Westfield NJ, US
Gina M. Santorelli - Oceanport NJ, US
Milana M. Maletic - Summit NJ, US
Aaron H. Leeman - Westfield NJ, US
Xin Gu - Scotch Plains NJ, US
Donald W. Graham - Mountainside NJ, US
James M. Balkovec - Martinsville NJ, US
Susan D. Aster - Teaneck NJ, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 314196
C07D24908
C07D40104
C07D40304
C07D41302

US Classification:

514256, 514311, 514340, 514364, 514365, 514383, 544333, 546167, 5462724, 548131, 548203, 5482662, 5482664, 5482668, 5482672, 5482678, 5482694

Abstract:

Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

US Patent:

7504402, Mar 17, 2009

Filed:

Dec 14, 2004

Appl. No.:

11/011889

Inventors:

Sherman T. Waddell - Westfield NJ, US
Gina M. Santorelli - Oceanport NJ, US
Milana M. Maletic - Summit NJ, US
Aaron H. Leeman - Westfield NJ, US
Xin Gu - Scotch Plains NJ, US
Donald W. Graham - Mountainside NJ, US
James M. Balkovec - Martinsville NJ, US
Susan D. Aster - Teaneck NJ, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31/4196
C07D 249/08
C07D 401/04
C07D 403/04
C07D 413/02

US Classification:

514256, 514311, 514340, 514364, 514365, 514383

Abstract:

Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

US Patent:

8026264, Sep 27, 2011

Filed:

May 26, 2004

Appl. No.:

10/558454

Inventors:

Sherman T. Waddell - Westfield NJ, US
Gina M. Santorelli - Oceanport NJ, US
Milana M. Maletic - Summit NJ, US
Aaron H. Leeman - Westfield NJ, US
Xin Gu - Scotch Plains NJ, US
Donald W. Graham - Mountainside NJ, US
James M. Balkovec - Martinsville NJ, US
Susan D. Aster - Teaneck NJ, US

Assignee:

Merck Sharp and Dohme Corp. - Rahway NJ

International Classification:

A61K 31/4196
C07D 249/08

US Classification:

514383, 5482622

Abstract:

Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

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:

20090181994, Jul 16, 2009

Filed:

Feb 3, 2009

Appl. No.:

12/364902

Inventors:

Sherman T. Waddell - Westfield NJ, US
Gina M. Santorelli - Oceanport NJ, US
Milana M. Maletic - Summit NJ, US
Aaron H. Leeman - Westfield NJ, US
Xin Gu - Scotch Plains NJ, US
Donald W. Graham - Mountainside NJ, US
James M. Balkovec - Martinsville NJ, US
Susan D. Aster - Teaneck NJ, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31/4196
C07D 249/08
A61K 31/506
A61P 25/28

US Classification:

514275, 5482694, 514383

Abstract:

Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

US Patent:

51324636, Jul 21, 1992

Filed:

Jun 12, 1991

Appl. No.:

7/713895

Inventors:

Donald W. Graham - Mountainside NJ
John C. Chabala - Westfield NJ
Tesfaye Biftu - Parlin NJ
Michael N. Chang - Newtown PA
Yuan-Ching P. Chiang - Piscataway NJ
Shu S. Yang - Bridgewater NJ
Kathryn L. Thompson - Westfield NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07C31714
C07C31722

US Classification:

568 33

Abstract:

Novel 1,3-Diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediated by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.

US Patent:

40790690, Mar 14, 1978

Filed:

May 9, 1977

Appl. No.:

5/794771

Inventors:

Donald W. Graham - Mountainside NJ
Edward F. Rogers - Middletown NJ
Wallace T. Ashton - Clark NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31505
C07D52100

US Classification:

2602564F

Abstract:

5-Deazariboflavin, its phosphate ester and nontoxic salts thereof and its novel bis(loweralkoxymethylene) derivatives have antiprotozoal and antiparasitic activity. They are particularly useful for controlling cecal and/or intestinal coccidiosis when administered in minor quantities to animals, in particular to poultry, usually in admixture with animal sustenance. The compounds are included in compositions useful for the prevention and treatment of coccidiosis in poultry.