公开(公告)号：JPH06501494A

公开(公告)日：1994-02-17

申请号：JP50198193

申请日：1992-07-10

申请人： ERBA CARLO SPA

发明人： BUZZETTI FRANCO ,  LONGO ANTONIO ,  COLOMBO MARISTELLA

IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P35/00 ,  A61P43/00 ,  C07D209/04 ,  C07D209/34 ,  C07D209/56 ,  C07D487/08

公开(公告)号：JP2000204070A

公开(公告)日：2000-07-25

申请号：JP2000040167

申请日：2000-02-17

申请人： ERBA CARLO SPA

发明人： BUZZETTI FRANCO ,  LONGO ANTONIO ,  COLOMBO MARISTELLA

IPC分类号： A61K31/16 ,  A61K31/03 ,  A61K31/19 ,  A61K31/22 ,  A61K31/275 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/425 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61P35/00 ,  A61P43/00 ,  C07C57/42 ,  C07C57/60 ,  C07C59/52 ,  C07C59/54 ,  C07C59/64 ,  C07C69/017 ,  C07C209/42 ,  C07C215/48 ,  C07C233/11 ,  C07C235/34 ,  C07C255/34 ,  C07C255/36 ,  C07C255/37 ,  C07C255/41 ,  C07C255/52 ,  C07C255/53 ,  C07C255/54 ,  C07C327/44 ,  C07C327/48 ,  C07D209/34 ,  C07D215/12 ,  C07D215/14 ,  C07D215/20 ,  C07D215/22 ,  C07D215/227 ,  C07D215/233 ,  C07D215/26 ,  C07D401/06 ,  C07D403/06 ,  C07D417/06

摘要： PROBLEM TO BE SOLVED: To obtain a highly active and low-toxic new compound having specific tyrosine kinase inhibitory activity and useful in treating abnormal proliferation including cancer. SOLUTION: This new compound is a compound of formula I (Y is a group of formula II or formula III; R is a group of formula IV or the like; R3 is OH; R1 is H, a 1-6C alkyl or the like; R2 is H, a halogen or the like; when Y is the group of formula II, n is 0-3, when Y is the group of formula III, n is 0-2; wherein such a condition that, for the group of formula III, only the benzene moiety is substitutable with groups R, OR1 and R2 is satisfied), pref. 2-cyano-3-(2-hydroxynaphth-1-yl)thioacrylamide or the like. The compound of formula I is obtained by condensation reaction of a compound of formula V (e.g. 2-hydroxy-1-naphthaldehyde) with e.g. a compound of the formula NC- CH2-CSNH2 in an inert organic solvent such as ethanol in the presence of a basic catalyst such as piperidine pref. at about 0-100 deg.C followed by, as necessary, e.g. conversion to the corresponding pharmaceutically acceptable salt.