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The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Patent No.:

US 7329683 B1

PDFFull Text
Date of Patent:
Feb. 12, 2008

Filed:

Jan. 28, 2003

11-β-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia

Applicants:

James M. Balkovec, Martinsville, NJ (US);

Rolf Thieringer, Highland Park, NJ (US);

Steven S. Mundt, Hamilton, NJ (US);

Anne Hermanowski-vosatka, Kinnelon, NJ (US);

Donald W. Graham, Mountainside, NJ (US);

Gool F. Patel, Califon, NJ (US);

Susan D. Aster, Teaneck, NJ (US);

Sherman T. Waddell, Westfield, NJ (US);

Steven H. Olson, Clark, NJ (US);

Milana Maletic, Summit, NJ (US);

Inventors:

James M. Balkovec, Martinsville, NJ (US);

Rolf Thieringer, Highland Park, NJ (US);

Steven S. Mundt, Hamilton, NJ (US);

Anne Hermanowski-Vosatka, Kinnelon, NJ (US);

Donald W. Graham, Mountainside, NJ (US);

Gool F. Patel, Califon, NJ (US);

Susan D. Aster, Teaneck, NJ (US);

Sherman T. Waddell, Westfield, NJ (US);

Steven H. Olson, Clark, NJ (US);

Milana Maletic, Summit, NJ (US);

Assignee:

Merck & Co., Inc., Rahway, NJ (US);

Attorneys:

Phillipe L. Durette

Richard C. Billups

Heidi M. Struse

Primary Examiner:

Taofiq Solola

Int. Cl.
CPC ...
A61K 31/4196 (2006.01); C07D 249/16 (2006.01);
U.S. Cl.
CPC ...
Abstract

Compounds having Formula (I), including pharmaceutically acceptable salts and prodrugs thereof: are selective inhibitors of the 11β-HSD1 enzyme. They inhibit the 11β-HSD1-mediated conversion of cortisone and other 11-keto-glucocorticoids to cortisol and other 11β-hydroxy-glucocorticoids. The 11β-HSD1 inhibitors therefore decrease the amount of cortisol in target tissues, thereby modulating the effects of cortisol. Modulation of cortisol may be effective in controlling non-insulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM or with excess cortisol in the body

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