公开(公告)号：EP1007042A1

公开(公告)日：2000-06-14

申请号：EP98929059.8

申请日：1998-06-12

申请人： Sugen, Inc.

发明人： TANG, Peng, Cho ,  McMAHON, Gerald ,  RAMPHAL, John, Y.

IPC分类号： A61K31/44 ,  A61K31/47 ,  A61K31/53 ,  A61K31/54 ,  A61K31/425 ,  A61K31/445 ,  A61K31/495 ,  A61K31/505 ,  A61K31/535 ,  C07D215/02 ,  C07D237/26 ,  C07D239/02 ,  C07D241/36 ,  C07D249/02 ,  C07D251/72 ,  C07D253/10 ,  C07D261/20

CPC分类号： C07D409/12 ,  C07D417/12 ,  C07D417/14

摘要： The present invention relates to novel heteroaryl compounds and the physiologically acceptable salts and the prodrugs thereof which are expected to modulate the activity of protein tyrosine enzymes which are related to cellular signal transduction, in particular, protein tyrosine phosphatase, and therefore are expected to be useful in the prevention and treatment of disorders associated with abnormal protein tyrosine enzyme related cellular signal transduction such as cancer and diabetes.

公开(公告)号：EP0929520A1

公开(公告)日：1999-07-21

申请号：EP97939480.0

申请日：1997-08-20

申请人： Sugen, Inc.

发明人： TANG, Peng, Cho ,  SUN, Li ,  McMAHON, Gerald ,  HIRTH, Klaus, Peter ,  SHAWVER, Laura, Kay

IPC分类号： A61K31 ,  A61P3 ,  A61P9 ,  A61P35 ,  A61P43 ,  C07D209 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D409 ,  C07D455 ,  C07D471 ,  C07D495 ,  C07F9

CPC分类号： C07D401/06 ,  C07D209/34 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D455/06 ,  C07D495/04

摘要： The present invention relates to organic molecules capable of modulating, regulating and/or inhibiting protein kinase signal transduction. Such compounds are useful for the treatment of diseases related to unregulated protein kinase signal transduction, including cell proliferative diseases such as cancer, atherosclerosis, arthritis and restenosis and metabolic diseases such as diabetes. The present invention features indolinone compounds that potently inhibit protein kinases and related products and methods. Inhibitors specific to the FLK protein kinase can be obtained by adding chemical substituents to the 3-[(indole-3-yl)methylene]-2-indolinone, in particular at the 1' position of the indole ring. Indolinone compounds that specifically inhibit the FLK and platelet derived growth factor protein kinases can harbor a tetrahydroindole or cyclopentano-b-pyrrol moiety. Indolinone compounds that are modified with substituents, particularly at the 5 position of the oxindole ring, can effectively activate protein kinases. This invention also features novel hydrosoluble indolinone compounds that are tyrosine kinase inhibitors and related products and methods.