- Synthesis and structure-activity relationships of pyrimidine derivatives as potent and orally active FGFR3 inhibitors with both increased systemic exposure and enhanced in vitro potency
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Fibroblast growth factor receptor 3 (FGFR3) is an attractive therapeutic target for the treatment of patients with bladder cancer harboring genetic alterations in FGFR3. We identified pyrimidine derivative 20b, which induced tumor regression following ora
- Kuriwaki, Ikumi,Kameda, Minoru,Iikubo, Kazuhiko,Hisamichi, Hiroyuki,Kawamoto, Yuichiro,Kikuchi, Shigetoshi,Moritomo, Hiroyuki,Kondoh, Yutaka,Terasaka, Tadashi,Amano, Yasushi,Tateishi, Yukihiro,Echizen, Yuka,Iwai, Yoshinori,Noda, Atsushi,Tomiyama, Hiroshi,Nakazawa, Taisuke,Hirano, Masaaki
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- NITROGEN-CONTAINING AROMATIC HETEROCYCLIC COMPOUND
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Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.
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Paragraph 0338; 0378
(2014/05/25)
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