ДЖУНГ Дональд (US),МАТТЕУЧЧИ Марк (US),КРОЛЛ Стюарт (US)
申请号：
RU2013147744/15
公开号：
RU2013147744A
申请日:
2012.04.13
申请国别(地区):
RU
年份:
2015
代理人:
摘要：
1. An oral composition comprising a prodrug of Formula I, hypoxia activatable, gdeYpredstavlyaet is O, S, NR, NCORili NSORRpredstavlyaet is C-alkyl, C-Sgeteroalkil, aryl or heteroaryl r and are independently selected from the group consisting of 2-haloalkyl, 2- alkilsulfoniloksialkila, 2-geteroalkilsulfoniloksialkila, 2-arilsulfoniloksialkila and 2-geteroalkilsulfoniloksialkila R d formula LZ L represents C (Z) each Zpredstavlyaet independently hydrogen, halogen, C-alkyl, C-Sgeteroalkil, aryl, heteroaryl, S-cycloalkyl, heterocyclyl, C-C acyl, C-Sgeteroatsil, aroyl or heteroaroyl or L represents: ,,,,,,, or, Zpredstavlyaet biovosstanavlivaemuyu a group having a formula selected from the group consisting of: and, each X b is independently N or CR Hpredstavlyaet is NR, S or O each R is independently C-alkyl, C-Sgeteroalkil, C cycloalkyl, heterocyclyl, aryl or heteroaryl and R are independently hydrogen, halogen, cyano, CHF, CF, COH, amino, C- alkyl, C-Sgeteroalkil, C-cycloalkyl, alkoxy-C, C-Salkilamino, C-Sdialkilamino, aryl, CON (R), C-Sacile, C-Sgeteroatsil, aroyl or heteroaroyl, or a pharmaceutically acceptable salt thereof, wherein the oral composition is a modified vysvobozhdeniem.2. The composition with modified release according to claim 1, which is a tabletku.3. The composition with modified release according to claim 1, which comprises mikrochastitsy.4. The composition with modified release according to claim 1, which comprises a matrix for controlled vysvobozhdeniya.5. The composition with modified release according to claim 1, further comprising yadro.6. composite1. Пероральная композиция, содержащая пролекарство Формулы I, активируемое гипоксией,гдеY2 представляет собой О, S, NR6, NCOR6 или NSO2R6R6 представляет собой С1-С6алкил, C1-С6гетероалкил, арил или гетероарилR3 и R4 независимо выбраны из группы, состоящей из 2-галогеналкила, 2-алкилсульфонилоксиалкила, 2-гетероалкилсульфонилоксиалкила, 2-арилсульфонилоксиалкила и 2-гетероалкилсульфонилоксиалкилаR1 и
