Patent number: 7626044
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 the
Type:
Grant
Filed:
January 28, 2003
Date of Patent:
December 1, 2009
Assignees:
Shanghai Institute of Materia Medica Chinese Academy of Sciences, Shanghai Pharmaceutical (Group) Co., Ltd.
Inventors:
Yuanchao Li, Jianping Zuo, Fan Zhang, Ru Zhou, Jian Ding
Patent number: 7145021
Abstract: The subject invention provides compounds having the structure: wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R2 is H, OH, a photoactivatable moiety, a fluorescent-moiety, or a radioactive moiety; R3 is H or OH; R4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety, or an optically pure enantiomer of the compound or wherein R1 is H or OH; R2 is H, OH, halogen, unsubstituted or substituted, straight or branched (C1–C5) alkyl group, (C2–C5) alkenyl, or a (C2–C5) alkynyl, (C1–C5) alkoxy, (C2–C5) alkenyloxy, or (C2–C5) alkynyloxy, —N3, —COR5, —CONR5R6, —CO2R5, —OCOR5, —NH(OH), —NR5R6, —NHCOR5, —N(OH)COR5, —CH2OR5, —OCH2CO2R5, —CH2SR5, —CH2NR5R6, —SR5, —OSR5, or —NR5SO2R6, where R5 and R6 are each independently hydrogen, substituted or unsubstituted (C1–C5) alkyl, (C2–C5) alkenyl, or (C2–C5) alkynyl, or a cyclo
Type:
Grant
Filed:
March 28, 2003
Date of Patent:
December 5, 2006
Assignee:
The Trustees of Columbia University in the City of New York
Inventors:
Kristian Stromgaard, Makiko Suehiro, Koji Nakanishi, Stine B. Vogensen