公开(公告)号：EP0787009A1

公开(公告)日：1997-08-06

申请号：EP95940622.0

申请日：1995-11-06

申请人： ARIZONA BOARD OF REGENTS, A BODY CORPORATE OF THE STATE OF ARIZONA acting for and on behalf of ARIZONA STATE UNIVERSITY

发明人： PETTIT, George R. ,  SRIRANGAM, Jayaram K.

IPC分类号： A61K38 ,  A61P35 ,  C07D207 ,  C07K5 ,  C07K7

CPC分类号： C07D207/08 ,  A61K38/00 ,  C07K5/0205 ,  C07K7/02

摘要： The sea hare Dolabella auricularia has yielded many structurally distinct peptides which possess antineoplastic activity. Presently the compound denominated 'dolastatin 10' represents the most important of such peptides because of its demonstrated potential as an anticancer drug. The present invention relates to the systematic creation of seven unique pentapeptides by selectively coupling a tripeptide-trifluoroacetate salt with a preselected dipeptide trifluoroacetate salt which provide active molecules capable of emulating the measured therapeutic effect of dolastatin 10.

公开(公告)号：EP0787009B1

公开(公告)日：2004-01-21

申请号：EP95940622.4

申请日：1995-11-06

申请人： ARIZONA BOARD OF REGENTS, A BODY CORPORATE OF THE STATE OF ARIZONA acting for and on behalf of ARIZONA STATE UNIVERSITY

发明人： PETTIT, George R. ,  SRIRANGAM, Jayaram K.

IPC分类号： C07K5/00 ,  C07K5/02 ,  A61K38/04 ,  C07D207/08

CPC分类号： C07D207/08 ,  A61K38/00 ,  C07K5/0205 ,  C07K7/02

摘要： The sea hare Dolabella auricularia has yielded many structurally distinct peptides which possess antineoplastic activity. Presently the compound denominated 'dolastatin 10' represents the most important of such peptides because of its demonstrated potential as an anticancer drug. The present invention relates to the systematic creation of seven unique pentapeptides by selectively coupling a tripeptide-trifluoroacetate salt with a preselected dipeptide trifluoroacetate salt which provide active molecules capable of emulating the measured therapeutic effect of dolastatin 10.