Compounds of Structure I, and salts, tautomers, stereoisomers, and mixtures thereof may be used in methods of inhibiting checkpoint kinase 1 in subjects, in methods for inducing cell cycle progression, and in methods for increasing apoptosis in cells. Such compounds may be used to prepare pharmaceutical compositions and may be used in conjunction with DNA damaging agents.
Inhibition of FGFR3 and treatment of multiple myeloma
申请人:Cai Shaopei
公开号:US20050261307A1
公开(公告)日:2005-11-24
Methods of inhibiting fibroblast growth factor receptor 3 and treating various conditions mediated by fibroblast growth factor receptor 3 are provided that include administering to a subject a compound of Structure I, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I have the following structure where and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting fibroblast growth factor receptor 3 and for use in treating conditions mediated by fibroblast growth factor receptor 3 such as multiple myeloma.
Methods of treating cancer include contacting a cancer cell with 4-amino-5-fluoro-3-(5-piperazin-1-yl-1H-benzimidazol-2-yl)quinolin-2(1H)-one, 4-amino-5-fluoro-3-[5-(4-methyl-4-oxidopiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one, tautomers thereof, pharmaceutically acceptable salts thereof, pharmaceutically acceptable salts of the tautomers thereof, or a mixture thereof.
Pharmaceutically acceptable salts of quinolinone compounds having improved pharmaceutical properties
申请人:Cai Shaopei
公开号:US20050209247A1
公开(公告)日:2005-09-22
A lacate salt of a compound of Formula I or a tautomer of the compound, wherein Formula I has the following structure and R
1
-R
9
and R
12
-R
14
are as defined herein
A method for synthesizing a 4-amino substituted quinolinone includes reacting a substituted or unsubstituted 2-benzimidazolyl-2-acetate with a substituted or unsubstituted 2-aminobenzonitrile in the presence of a base or an acid. A 4-amino substituted quinolinone compound is formed by the reaction, and the 4-amino substituted quinolinone compound comprises a benzimidazole group.