Kirin Beer Kabushiki Kaisha

Kazuo Kubo

Toshiyuki Isoe

Yasunari Fujiwara

Teruyuki Sakai

Rika Nagao

Kazumasa Hasegawa

Hideko Murooka

Tsuyoshi Nishitoba

Tatsushi Osawa

Tatsuo Nakajima

Toshiyuki Shimizu

Shinichiro Kato

Hiroaki Ohno

Tuyoshi Nishitoba

Shinichi Ohyama

Yoshiko Kobayashi

An objective of the present invention is to provide compounds which have inhibitory activity against autophosphorylation of macrophage colony-stimulating factor receptors. The compounds of the present invention are represented by formula (I) and salt and solvate thereof: wherein X represents CH or N; Z represents O or S; R, R, and Rrepresent H, optionally substituted alkoxy or the like; Rrepresents H; R, R, R, and Rrepresent H, halogen, alkyl, alkoxy, trifluoromethyl or the like; Rand Rrepresent H, alkyl or the like; and any one of Rand Rrepresents H with the other representing alkyl and Rrepresents an optionally substituted carbocyclic or heterocyclic ring or the like, or Rrepresents H and Rand Rcombine together to form a bicyclic carbocyclic ring.

Quinoline derivatives and quinazoline derivatives inhibiting autophosphorylation of macrophage colony stimulating factor receptor

An object of the present invention is to provide compounds having potent antitumor activity. The compounds according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein X and Z represent CH or N; Y represents O or S; R, R, and Rrepresent H, alkoxy or the like; Rrepresents H; R, R, R, and Rrepresent H, halogen, alkoxy or the like; Rand Rrepresent H, alkyl or the like; and Rrepresents optionally substituted azolyl.

Quinoline derivatives and quinazoline derivatives having azolyl group

An object of the present invention is to provide compounds which have antitumor activity and do not change cytomorphosis. Disclosed are compounds represented by formula (I) and a pharmaceutically acceptable salts and solvates thereof and pharmaceutical compositions comprising said compounds: wherein X and Z each independently represent CH or N; Rto Rrepresent H, substituted alkoxy, unsubstituted alkoxy or the like; Rrepresents H; Rto Rrepresent H, halogen, alkyl, alkoxy, alkylthio, nitro, or amino, provided that Rto Rdo not simultaneously represent H; Rand Rrepresent H, alkyl, or alkylcarbonyl; and Rrepresents alkyl, alkenyl, alkynyl, or aralkyl.

Quinoline derivatives and quinazoline derivatives

The present invention relates to a process for producing a 4-quinolone derivative, comprising allowing an o-aminoacetophenone derivative to react with a formic acid in an aprotic solvent in the presence of a suitable base, and adding a protic solvent to the reaction mixture. This is a simple process for producing 4-quinolone derivatives, applicable to large-scale commercial production.

Process for producing quinolone derivatives

Quinoline and quinazoline derivatives inhibiting platelet-derived growth

Growing community of inventors

Takasaki, Japan

Kazuo Kubo