发明名称 N-[3-(5-AMINO-3,3A,7,7A-TETRAHYDRO-1H-2,4-DIOXA-6-AZA-INDEN-7-YL)-PHENYL]-AMIDES AS INHIBITORS OF BACE1 AND(OR) BACE2
摘要 FIELD: pharmaceutics.SUBSTANCE: invention relates to a compound of formula Ia, where Rrepresents a pyridinyl or pyridinyl, substituted with 1-2 substitutes, individually selected from a cyano, a halogen atom, halogen-C-alkoxy, or pyrazinyl, substituted by halogen-C-alkoxy or C-alkynyl-C-alkoxy; Rrepresents F; Ris selected from a group consisting of i) methyl, ii) -CHCHF, iii) -CHCHF; Ris hydrogen; and Ris selected from a group consisting of i) a hydrogen atom, ii) -CF; or its pharmaceutically acceptable salts. Invention also relates to specific compounds of N-[3-(5-amino-3,3A,7,7A-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)phenyl]amide, given in claim. Compound according to invention is intended for use as a therapeutically active substance possessing inhibitory activity on BACE1 and/or BACE2, for preparing a pharmaceutical composition or a medicinal agent.EFFECT: inhibiting properties of N-[3-(5-amino-3,3A,7,7A-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)phenyl]amide with respect to BACE1 and/or BACE2.12 cl, 8 tbl, 22 ex
申请公布号 RU2597308(C2) 申请公布日期 2016.09.10
申请号 RU20130138834 申请日期 2012.02.06
申请人 F. HOFFMANN-LA ROCHE AG 发明人 KHILPERT KHans;KHUMM Roland
分类号 C07D498/04;A61K31/5365;A61P25/28 主分类号 C07D498/04
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