公开(公告)号：EP1418177A1

公开(公告)日：2004-05-12

申请号：EP02758042.2

申请日：2002-08-14

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： YUE, J., c/o Shangai Institute of Materia Medica, ,  YANG, S., c/o Shangai Institute of Materia Medica, ,  DING,J., c/o Shangai Institute of Materia Medica, ,  XIAO, D., c/o Shangai Institute of Materia Medica, ,  YUAN, S., c/o Shangai Institute of Materia Medica ,  WU, Yan., c/o Shangai Institute of Materia Medica ,  TONG, Y., c/o Shangai Institute of Materia Medica ,  DONG, Lei, c/o Shangai Institute of Materia Medica

IPC分类号： C07D521/00 ,  A61K31/558 ,  A61P31/10 ,  A61P35/00

CPC分类号： A61K31/365 ,  C07D311/94

摘要： The invention relates to pseudolaric acid-B derivatives of general formula (I), wherein (a) R 1 is cyano, heterocyclyl, COXR' or CON(R") 2 , wherein X is O or NH, R' is H, cycloalkyl, alkyl, heterocyclic alkyl or arylalkyl, each R" is independently alkyl, cycloalkyl or heterocyclicalkyl; (b) R 2 is H, alkylacyl, arylalkylacyl, arylacyl or heterocyclylacyl; (c) R 3 is COXY, amino or halogen, wherein X is O or NH, Y is H, NH 2 , hydroxy, alkyl, cycloalkyl, heterocyclicalkyl, hetroatom-substituted alkyl, tertiary amino-substituted ammonioalkyl, aryl, arylalkyl or polyhydroxyalkyl. The invention also relates to processes for preparing such derivatives and antitumor or antifungal pharmaceutical compositions containing the same.

摘要翻译： 本发明涉及通式（I）的假极酸-B衍生物，其中（a）R 1是氰基，杂环基，COXR'或CON（R“）2，其中X是O或NH，R'是H，环烷基， 烷基，杂环烷基或芳烷基，每个R“独立地为烷基，环烷基或杂环烷基; （b）R2是H，烷基酰基，芳基烷基酰基，芳基酰基或杂环基酰基; （c）R3是COXY，氨基或卤素，其中X是O或NH，Y是H，NH2，羟基，烷基，环烷基，杂环烷基，杂原子取代的烷基，叔氨基取代的氨基烷基，芳基，芳烷基或多羟基烷基。 本发明还涉及制备此类衍生物的方法和含有该衍生物的抗肿瘤或抗真菌药物组合物。