发明名称 Melampomagnolide B derivatives as antileukemic and cytotoxic agents
摘要 Melampomagnolide B is disclosed as a new antileukemic sesquiterpene. A biotin-conjugated derivative of melampomagnolide B was prepared to elucidate its mechanism of action. Prodrugs of Melampomagnolide B are disclosed.
申请公布号 US8884027(B2) 申请公布日期 2014.11.11
申请号 US201113279038 申请日期 2011.10.21
申请人 University of Rochester;University of Kentucky Research Foundation 发明人 Crooks Peter A.;Jordan Craig T.;Pei Shanshan;Nasim Shama
分类号 C07D493/04;C07D495/04;C07D519/00 主分类号 C07D493/04
代理机构 Meunier Carlin & Curfman, LLC 代理人 Meunier Carlin & Curfman, LLC
主权项 1. A melampomagnolide B derivative compound of the formula (I): wherein: R is selected from —P(O)(OR1)(OR2); —CH2OP(O)(OR1)(OR2); —C(O)(CR3R4)nX; —CH2OC(O)(CR3R4)nX; —C(O)O(CR3R4)nX; —C(O)NHCH2CH2NH2; —C(O)NHCH2(CH2)2NH2; —C(O)NHCH2(CH2)3NH2; —C(O)NHCH2(CH2)4NH2 and —C(O)(CH2)mC(O)NH(CR3R4)nX; R1, R2 are independently selected from H; Na; K; NH3; unsubstituted C1-C12alkyl, optionally substituted alkenyl, alkynyl, heterocycloalkyl, heteroaryl, cycloalkyl, and aryl; R3, R4 are independently selected from H, NR5R6, OR1, SR1, S(O)R1, SO2R1, optionally substituted C1-C12alkyl, alkenyl, alkynyl, heterocycloalkyl, heteroaryl, cycloalkyl, and aryl; R5, R6 are independently selected from H; optionally substituted C1-C12alkyl, alkenyl, alkynyl, heterocycloalkyl, heteroaryl, cycloalkyl, aryl; —CO2C1-C12alkyl, CO2alkenyl, CO2alkynyl, CO2heterocycloalkyl, CO2heteroaryl, CO2cycloalkyl, CO2aryl; and C1-C12alkylamino; or R5 and R6 optionally together with the nitrogen atom form an optionally substituted 5-12 membered ring, said ring optionally comprising 1 or more heteroatoms; X is selected from NR5R6, NHC(O)R2; NHC(O)OR2; OR1, SR1, halo, trifluoromethyl, optionally substituted C1-C12alkyl, alkenyl, alkynyl, heterocycloalkyl, heteroaryl, cycloalkyl, and aryl; n is 1-6, m is 1-2; or a pharmaceutically acceptable salt or ester thereof.
地址 Rochester NY US