Triptolide derivatives and their uses

US7626044B2 · kind B2 · utility

Assignees

• SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES · CN
• Shanghai Pharmaceuticals Holding Co., Ltd. · CN

Inventors

• Yuanchao Li · Shanghai, CN
• Jianping Zuo · Shanghai, CN
• Fan Zhang · Lake Barrington, US
• Ru Zhou · Carlsbad, US
• Jian Ding · Shanghai, CN

Key dates

• Filing date: Jan 28, 2003
• Grant date: Dec 1, 2009
• Expiry date: Apr 29, 2024

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P37/08
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Triptolide derivatives of Formula (I), their pharmaceutically acceptable salts and optical isomers, Formula (I):wherein, C5 and C6 are connect with each other by a C-C single bond or double bond; when C5 and C6 are connected with C-C single bond, X and Y represent independently hydrogen, oxygen, hydroxyl, halogen, lower alkyl-oxy, lower alkyl-amino, mercapto, lower alkyl-thio, the group of formula —OCOR, —OSO2OR or —OPO(OH)2, each of which is attached to C5 and C6, R represents —(CH2)nCO2Na, —(CO2)nCO2K, or —(CH2)nCH3, wherein n=1-6; Z represents hydrogen, oxygen, hydroxyl, halogen, lower alkyl-oxy, lower alkyl-amino, mercapto, lower alkyl-thio, the group of formula -OCOR, -OSO2OR or —OPO(OH)2, each of which is linked at C14-position, R represents —(CH2)nCO2Na, —(CO2)nCO2K, or —(CH2)nCH2, wherein n=1-6; wherein, the“______” linked with X, Y, and Z represents the stereochemistry orientations “” or “” , but X and Y cannot both be hydrogen atom at the same time, methods for preparing the triptolides and their use as antiphiogistic agent, immunosuppressive agent or therapeutic agent for other related diseases.