Kirin Beer Kabushiki Kaisha

Kyowa Hakko Kirin Co., Limited

Tatsushi Osawa

Yasunari Fujiwara

Atsushi Miwa

Tsuyoshi Nishitoba

Terufumi Senga

Kazuhide Nakamura

Tetsuya Yoshino

Teruyuki Sakai

Kazuo Kubo

Tatsuo Nakajima

Toshiyuki Shimizu

Hideko Murooka

An objective of the present invention is to provide compounds having potent antitumor activity. The compounds of the present invention are represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein X&#x2550;CH or N; Z&#x2550;O or S; L=O or S; M=CRR, wherein Rand R&#x2550;H, alkyl, or alkoxy, NRwherein R&#x2550;H or alkyl; R, R, and R&#x2550;H or optionally substituted alkoxy; R&#x2550;H; R&#x2550;H, halogen, alkoxy or the like; and R=alkyl optionally substituted by &#x2014;R, -T-R, or &#x2014;NRRwherein T=O, S, or NH; R=an optionally substituted carbocyclic or heterocyclic ring; and R=alkyl or an optionally substituted carbocyclic or heterocyclic ring, or &#x2014;NRRwherein Rand R&#x2550;H, optionally substituted alkyl, or an optionally substituted carbocylic or heterocyclic ring, or optionally substituted carbocyclic or heterocyclic ring.

Quinoline derivative and quinazoline derivative inhibiting self-phosphorylation of hepatocytus proliferator receptor, and medicinal composition containing the same

An objective of the present invention is to provide novel compounds which have inhibitory activity against autophosphorylation of an FGF receptor family and, when orally or intraveneously administered, can suppress the growth of cancer cells. The compounds of the present invention are represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein X represents CH or N; Z represents O or S; Q represents NR, CRR, carbonyl, O, S(&#x2550;O)m, wherein m is 0 to 2, or urea; Rto Reach independently represent H, OH, halogen, nitro, amino, alkyl, alkoxy or the like in which the alkyl and alkoxy groups are optionally substituted; Rrepresents H; Rto Reach independently represent H, halogen, alkyl, or alkoxy; and Rrepresents an optionally substituted carbocyclic or heterocyclic group.

Quinoline or quinazoline derivatives inhibiting auto-phosphorylation of fibroblast growth factor receptors

An objective of the present invention is to provide compounds having potent antitumor activity. The compounds of the present invention are represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein X=CH or N; Z=O or S; L=O or S; M=CRR, wherein Rand R=H, alkyl, or alkoxy, NRwherein R=H or alkyl; R, R, and R=H or optionally substituted alkoxy; R=H; R=H, halogen, alkoxy or the like; and R=alkyl optionally substituted by &#x2014;R, -T-R, or &#x2014;NRRwherein T=O, S, or NH; R=an optionally substituted carbocyclic or heterocyclic ring; and R=alkyl or an optionally substituted carbocyclic or heterocyclic ring, or &#x2014;NRRwherein Rand R=H, optionally substituted alkyl, or an optionally substituted carbocylic or heterocyclic ring, or optionally substituted carbocyclic or heterocyclic ring.

Quinoline derivative and quinazoline derivative inhibiting self-phosphorylation of hepatocytus prolifertor receptor and medicinal composition containing the same

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

Growing community of inventors

Takasaki, Japan

Tatsushi Osawa