This is intended to provide an initial safety assessment of HSD-016 and also to evaluate how the drug is absorbed and eliminated and its effect on the body in healthy subjects.

开始日期2009-03-01

申办/合作机构

Wyeth AB

NCT00740649 / Completed临床1期

Single Ascending Dose Study Of The Safety, Tolerability, Pharmacokinetics, And Pharmacodynamics Of HSD-016 Administered Orally To Healthy Japanese Male Subjects

This is a single ascending dose study of HSD-016 to provide the initial assessment of the safety, tolerability, how the drug is absorbed and eliminated, and it's effect on the body in Japanese male subjects.

开始日期2008-10-01

申办/合作机构

Wyeth AB

NCT00739232 / Completed临床1期

Single Ascending Dose Study of the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of HSD-016 Administered Orally to Healthy Subjects

This is a single ascending dose study of HSD-016 to provide the initial assessment of the safety, tolerability, how the drug is absorbed and eliminated, and its effect on the body.

开始日期2008-09-01

申办/合作机构

Wyeth AB

100 项与 HSD-016 相关的临床结果

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100 项与 HSD-016 相关的转化医学

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100 项与 HSD-016 相关的专利（医药）

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项与 HSD-016 相关的文献（医药）

2011-09-02·The Journal of Organic Chemistry2区 · 化学

Synthesis of Potent and Orally Efficacious 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor HSD-016

2区 · 化学

Article

作者: Massefski, Walter W. ; Xiang, Jason ; Wang, Youchu, ; Wan, Zhao-Kui ; Saiah, Eddine ; Li, Huan-Qiu ; Chenail, Eva ; Kendall, Christopher ; Gingras, Stéphane ; Mansour, Tarek, S.

Cortisol and the glucocorticoid receptor (GR) signaling pathway has been linked to the development of diabetes and metabolic syndrome. In vivo, 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) catalyzes the conversion of inactive cortisone to its active form, cortisol. Existing clinical data have supported 11β-HSD1 as a valid therapeutic target for type 2 diabetes. In our research program, (R)-1,1,1-trifluoro-2-(3-((R)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)propan-2-ol (HSD-016) was discovered to be a potent, selective, and efficacious 11β-HSD1 inhibitor and advanced as a clinical candidate. Herein, a reliable and scalable synthesis of HSD-016 is described. Key transformations include an asymmetric synthesis of a chiral tertiary alcohol via Sharpless dihydroxylation, epoxide formation, and subsequent mild reduction. This route ensured multikilogram quantities of HSD-016 necessary for clinical studies.

100 项与 HSD-016 相关的药物交易

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