Non-calcemic, antiproliferative, transcriptionally active sulfur-containing analogs of 1&agr;, 25-dihydroxy vitamin D3

US6380408B1 · kind B1 · utility

Assignee

• THE JOHNS HOPKINS UNIVERSITY · US

Inventors

• Gary H. Posner · Baltimore, US
• Jae Kyoo Lee · Andover, US
• Qiang Wang · Philadelphia, US
• Kenneth R. Crawford · Baltimore, US
• Gyoonhee Han · Daejeon, KR

Key dates

• Filing date: Mar 31, 2000
• Grant date: Apr 30, 2002
• Expiry date: Mar 31, 2020

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Novel sulfur-containing analogs of 1&agr;,25-dihydroxy vitamin D3 are provided. These analogs are synthesized in a convergent manner by joining A-ring and C,D ring fragments. Each analog with 1&agr;,3&bgr;-substituent stereochemistry shows a pharmacologically desirable combination of high antiproliferative and high transcriptional activities in vitro and also low calcemic activity in vivo.