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1. (WO2018199049) NOVEL DNMT INHIBITOR AS SOLID TUMOR THERAPEUTIC DRUG

Pub. No.:    WO/2018/199049    International Application No.:    PCT/JP2018/016514
Publication Date: Fri Nov 02 00:59:59 CET 2018 International Filing Date: Wed Apr 25 01:59:59 CEST 2018
IPC: A61K 31/706
A61P 35/00
A61P 43/00
Applicants: OHARA PHARMACEUTICAL CO., LTD.
大原薬品工業株式会社
Inventors: SAKO Magoichi
酒向 孫市
USHIJIMA Toshikazu
牛島 俊和
HATTORI Naoko
服部 奈緒子
Title: NOVEL DNMT INHIBITOR AS SOLID TUMOR THERAPEUTIC DRUG
Abstract:
[Problem] To provide, in place of injected agents (such as Vidaza (registered trademark) and Dacogen (registered trademark)) clinically used as therapeutic drugs for high-risk myelodysplastic syndromes, a medicine as a therapeutic drug or a prophylactic drug for various advanced solid tumors, said medicine having high stability with respect to cytidine deaminase which is a hydrolytic metabolic enzyme, being absorbed into the body even by oral administration, and having an effect of being integrated into a nucleic acid biosynthetic route and inhibiting DNA methyltransferases, i.e., DNMTs. [Solution] The aforementioned problem is solved by a novel compound represented by formula (I). (In the formula, R is a hydroxyl group or a hydrogen atom, and R1 and R2 are each a benzyl group that may have a substituent.)