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Glucosylceramide synthase inhibitors
专利权人:
ДЖЕНЗИМ КОРПОРЕЙШН (US)
发明人:
БУРКЕ Элиз (US),СЕЛАТКА Кассандра (US),ХЕРТ Брэдфорд (US),МЕТЦ Маркус (US),ЧЖАО Чжун (US),СКЕРЛДЖ Ренато (US),СЯН Ибинь (US),ДЖАНСИЗИКС Кэтрин (US),МАРШАЛЛ Джон (US),ЧЭН Сэн (US),ШОЙЛЕ Рональд (US),КА
申请号:
RU2013146550/04
公开号:
RU2013146550A
申请日:
2012.03.16
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
1. The compound represented by the following structural formula, or a pharmaceutically acceptable salt or prodrug thereof, wherein: n is 1, 2 or 3; m is 0 or 1; p is 0 or 1; t is 0, 1 or 2; y is 1 or 2; z is 0, 1 or 2; E is S, O, NH, NOH, NNO, NCN, NR, NOR or NSOR; X is CR when m is 1, or N when m is 0; X is O, —NH, —CH—, SO, NH — SO; CH (CC) -alkyl or -NR; X is O, -NH, -CH-, CO, -CH (CC) -alkyl, SONH, -CO-NH- or -NR; X is CRR, CHCRR or CH- ( CC) -alkyl-CRR; X is a direct bond, O, S, SO, CRR; (CC) -alkyl, (CC) -alkyloxy, (CC) -alkenyl, (CC) -alkenyloxy; R is (CC) -aryl, (CC) -heteroaryl, (CC) -alkyl, (CC) -heteroaryl - (CC) -alkyl; R is H, CN, (CC) -alkylcarbonyl or (CC) -alkyl; each of R and R is independently —H, (CC) -alkyl optionally substituted with one or more substituents selected from the group consisting of halogen (CC) -alkyl, (CC) -aryl, (CC) -heteroaryl, (CC) -alkyl- (CC) -aryl, halogen- (CC) -aryl and halogen- (CC) -heteroaryl or, optionally, when X is —NR and X is —NR, R and R together with atom the nitrogen to which they are attached form a non-aromatic heterocyclic ring optionally substituted with one or more substituents selected from the group consisting of halogen, (CC) -alkyl, (CC) -aryl, (CC) -heteroaryl, (CC) -alkyl - (CC) -aryl, halogen- (CC) -aryl and halogen- (CC) -heteroaryl; R and R are independently selected from H, (CC) -alkyl, or together with the carbon to which they are attached, they form a spiro A (CC) cycloalkyl ring or a spiro (CC) cycloalkoxyl ring; R is —H, halogen, —CN, (CC) aryl, (CC) aryloxy group (CC) alkyl igruppu; (C-C) -alkyl optionally substituted1. Соединение, представленное следующей структурной формулой,или его фармацевтически приемлемая соль или пролекарство, где:n равно 1, 2 или 3;m равно 0 или 1;p равно 0 или 1;t равно 0, 1 или 2;y равно 1 или 2;z равно 0, 1 или 2;E представляет собой S, O, NH, NOH, NNO, NCN, NR, NOR или NSOR;Xпредставляет собой CR, когда m равно 1, или N, когда m равно 0;Xпредставляет собой O, -NH
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