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

US7329683B2 · kind B2 · utility

Assignee

• MERCK & CO., INC. · US

Inventors

• James M. Balkovec · North Plainfield, US
• Rolf Thieringer · Highland Park, US
• Steven S. Mundt · Hillsborough Township, US
• Anne Hermanowski-Vosatka · New York, US
• Donald W. Graham · Mountainside, US
• Gool F. Patel · Califon, US
• Susan D. Aster · Teaneck, US
• Sherman T. Waddell · Westfield, US
• Steven H. Olson · Millbrae, US
• Milana Maletic · Summit, US

Key dates

• Filing date: Jan 28, 2003
• Grant date: Feb 12, 2008
• Expiry date: Jul 30, 2024

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D513/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

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