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DEUTERED BENZYLBENZENE DERIVATIVES AND METHODS OF APPLICATION
专利权人:
ТЕРАКОС; ИНК. (US)
发明人:
СИД Брайан (US),ЛВ Биньхуа (CN),РОБЕРЖ Жак Й. (CN),ЧЭНЬ Юаньвэй (US),ПЭН Кунь (CN),ДУН Цзяцзя (US),СЮЙ Байхуа (CN),ДУ Цзиянь (CN),ЧЖАН Лили (CN),ТАН Синьсин (CN),СЮЙ Гэ (CN),ФЭН Янь (US),СЮЙ Минь (CN)
申请号:
RU2011105422/13
公开号:
RU2011105422A
申请日:
2009.07.15
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
1. A composition comprising a compound having the structure:! ! or any stereoisomer or tautomer thereof, or any pharmaceutically acceptable prodrug, salt or solvate thereof, where! - each R1, R2, R3, R4 and R5 independently represents —H, —D, a substituent that is optionally deuterated, or a group Q:! ; ! - each R6, R7, R8, R9, R10, R14, R15, R16 and R19 independently represents —H, —D or a substituent that is optionally deuterated; and! - each R11, R12, R13, R17 and R18 independently represents —H, —D or halogen; where! - one of R1, R2, R3, R4 and R5 represents a group Q; and! at least one of R1-R19 is -D or includes -D, wherein said composition has an isotopic enrichment coefficient for deuterium of at least 5.! 2. The composition according to claim 1, where one of R1, R2, R3, R4 and R5 represents a group Q; ! one of the remaining groups R1, R2, R3, R4 and R5 is hydrogen, deuterium, halogen, cyano, nitro, amino, hydroxy, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C10 cycloalkyl, C5 -C10 cycloalkenyl, C1-C6 alkoxy, C3-C10 cycloalkoxy, (C1-C6 alkoxy) C1-C6 alkoxy, C5-C7 cycloalkenyloxy, aryl, heteroaryl, aryloxy, heteroaryloxy, (C2-C4 alkenyl) C1-C3 alkoxy, ( C2-C4 alkynyl) C1-C3 alkoxy, (aryl) C1-C3 alkoxy, (heteroaryl) C1-C3 alkoxy, (C3-C10 cycloalkyl) C1-C3 alkyl, (C3-C10 cycloalkyl) C1-C3 alkoxy, (C5 -C10 cycloalkenyl) C1-C3 alkyl, (C5-C10 cycloalkenyl) C1-C3 alkoxy, (C1-C4 alkoxy) C1-C3 alkyl, (C3-C7 cy cloalkoxy) C1-C3 alkyl, (C3-C7 cycloalkoxy) C2-C4 alkenyl, (C3-C7 cycloalkoxy) C2-C4 alkynyl, (C3-C7 cycloalkoxy) C1-C3 alkoxy, (C1-C4 alkylamino) C1-C3 alkyl , di- (C1-C3 alkylamino) C1-C3 alkyl, tri- (C1-C4 alkyl) silyl-C1-C6 alkyl, tri- (C1-C4 alkyl) silyl-C2-C6 alkenyl, tri- (C1-C4 alkyl) silyl-C2-C6 alkynyl, tri- (C1-C41. Композиция, содержащая соединение, имеющее структуру: ! ! или любой его стереоизомер или таутомер, или любое его фармацевтически приемлемое пролекарство, соль или сольват, где ! - каждый R1, R2, R3, R4 и R5 независимо представляет
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