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SUBSTITUTED INDOL-5-OLA DERIVATIVES AND THEIR THERAPEUTIC APPLICATION
专利权人:
ЭлЭлСи (US);НЭНТ ХОЛДИНГЗ АйПИ
发明人:
ТАО Чуньлинь (US),ВАН Циньвэй (US),ХО Дэвид (US),ПОЛАТ Тулай (US),НАЛЛАН Лаксман (US),СООН-ШИОНГ Патрик (US)
申请号:
RU2015121431
公开号:
RU2015121431A
申请日:
2013.11.05
申请国别(地区):
RU
年份:
2016
代理人:
摘要:
1. The compound of formula (I) :, or a pharmaceutically acceptable derivative or prodrug thereof, wherein R is selected from: (i) hydrogen, amino, alkylamino; (ii) C-C1-6 alkyl, C-C1-6 alkenyl, C-C1-6 alkynyl; (iii) K- Ar, Ar is heteroaryl or aryl, each of which is substituted with 0 to 4 substituents independently selected from: (1) halogen, hydroxy, amino, amide, cyano, —COOH, —SONH, oxo, nitro and alkoxycarbonyl; and (2) C-Ci-alkyl, C-Ci-alkoxy, C-Ci-cycloalkyl, C-Ci-alkenyl, C-Ci-alkynyl, C-Ci-alkanoyl, C-Ci-haloalkyl, Ci-Ci-haloalkoxy, mono- and di- (Ci-Ci-alkyl) amino, Ci C1-6alkylsulfonyl, mono- and di- (C-C1-6alkyl) sulfonamido and mono- and di- (C1-6alkyl) aminocarbonyl; phenyl (CC) alkyl and (4-7 membered heterocycle) C-C1-6 alkyl, each of which is substituted with 0 to 4 secondary substituents independently selected from halogen, hydroxy, cyano, oxo, imino, C-C1-6 alkyl, and C-Salkoxy and C-haloalkyl; K is selected from a) O, S, SO, SO; b) (CH) m, m = 0-3, -O (CH) p, p = 1-3, -S (CH) p, p = 1-3, -N (CH) p, p = 1-3, - (CH) pO, p = 1-3; c) NR, R is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, alkylthio, aryl, arylalkyl; (iv) groups of structural formula (Ia): wherein R 1 is hydrogen, C 1-6 alkyl, oxo; X is CH, when R 1 is hydrogen; or X-R is O; or X is N, R is hydrogen, C 1 -C 6 alkyl, C 1-6 alkenyl, C 1-6 alkynyl, C 1-6 Caryl or heteroaryl, (1-4C-cycloalkyl) 1-4C-alkyl, 1-4C-haloalkyl, 1-4C-alkoxy, 1-4alkylthio, 4 -Salkanoyl, C-Salkoxycarbonyl, C-Salkanoyloxy, mono- and di- (C-Cycloalkyl) aminoC-Salkyl, (4-7 membered heterocycle) C-Calkyl, C-Salkylsulfonyl, mono- and di- (C-Salkyl ) sulfonamido and mono- and di- (C-C1-6alkyl) aminocarbonyl, each of which is substituted with 0 to 4 substituents independently selected from halogen, hydroxy, cyano, amino, -COOH and oxo; Het is selected from any heterocycle which is substituted from0 to 4 substituents independently selected from: (i) C-Calkyl, C-Calkenyl, C-Calkynyl; (ii) halogen, hydroxy, amino, amide,1. Со
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