Synthesis of inhibitors of 11β-hydroxysteroid dehydrogenase type 1

US8487094B2 · kind B2 · utility

Assignee

• Boehringer Ingelheim International GmbH · DE

Inventors

• Keith Fandrick · Sandy Hook, US
• Joe Ju GAO · Southbury, US
• Wenjie Li · Poughkeepsie, US
• Zhi-Hui Lu · Glen Allen, US
• Yongda Zhang · Sandy Hook, US

Key dates

• Filing date: Jul 23, 2009
• Grant date: Jul 16, 2013
• Expiry date: Jan 10, 2030

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/10
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Disclosed are syntheses of 11β-HSD1 inhibitors and corresponding intermediates that are promising for the treatment of a variety of disease states including diabetes, metabolic syndrome, obesity, glucose intolerance, insulin resistance, hyperglycemia, hypertension, hypertension-related cardiovascular disorders, hyperlipidemia, deleterious gluco-corticoid effects on neuronal function (e.g. cognitive impairment, dementia, and/or depression), elevated intra-ocular pressure, various forms of bone disease (e.g., osteoporosis), tuberculosis, leprosy (Hansen's disease), psoriasis, and impaired wound healing (e.g., in patients that exhibit impaired glucose tolerance and/or type 2 diabetes).