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    • 25. 发明申请
    • PHARMACEUTICAL COMPOUNDS
    • 药物化合物
    • US20110098290A1
    • 2011-04-28
    • US12902658
    • 2010-10-12
    • Brian John WilliamsMarian WilliamsMartyn Frederickson
    • Brian John WilliamsMarian WilliamsMartyn Frederickson
    • A61K31/496C07D403/10C07D403/14C07D413/14A61K31/5377A61P35/00
    • C07D295/155C07D209/44
    • The invention provides a compound of the formula (1): or a salt, solvate, N-oxide or tautomer thereof; wherein either R1 is R1a and R2 is R2a; or R1 is R1b and R2 is R2b; provided that in each case at least one of R1 and R2 is other than hydrogen; R1a and R2a are the same or different and each is selected from hydrogen, C1-4 alkyl, C2-4 alkenyl and C2-4 alkynyl wherein the C1-4 alkyl is optionally substituted by C1-2 alkoxy; R1b and R2b are the same or different and are selected from hydrogen, C(O)NR4R5, C(O)R6 and C(O)OR6 where R6 is C1-4 alkyl, R4 and R5 are both C1-4 alkyl, or NR4R5 forms a 4 to 7 membered saturated heterocyclic ring optionally containing a second heteroatom ring member selected from O, N or S and oxidised forms of N and S, the heterocyclic ring being optionally substituted by one or two C1-4 alkyl groups and/or one or two oxo groups; and R3 is a group D: wherein the asterisk denotes the point of attachment to the isoindoline ring; but excluding acetic acid 5-acetoxy-4-isopropyl-2-[5-(4-methyl-piperazin-1-ylmethyl)-1,3-dihydro-isoindole-2-carbonyl]-phenyl ester.
    • 本发明提供式(1)化合物或其盐,溶剂合物,N-氧化物或其互变异构体; 其中R1是R1a,R2是R2a; 或R1为R1b且R2为R2b; 条件是在每种情况下,R 1和R 2中的至少一个不是氢; R1a和R2a相同或不同,各自选自氢,C 1-4烷基,C 2-4烯基和C 2-4炔基,其中C 1-4烷基任选被C 1-2烷氧基取代; R1b和R2b相同或不同,并且选自氢,C(O)NR4R5,C(O)R6和C(O)OR6,其中R6是C1-4烷基,R4和R5都是C1-4烷基或 NR4R5形成任选地含有选自O,N或S的第二杂原子环成员和氧化形式的N和S的4至7元饱和杂环,杂环任选被一个或两个C 1-4烷基和/或 一个或两个氧代基团; 并且R 3是基团D:其中星号表示与异二氢吲哚环的连接点; 但不包括乙酸5-乙酰氧基-4-异丙基-2- [5-(4-甲基 - 哌嗪-1-基甲基)-1,3-二氢 - 异吲哚-2-羰基] - 苯酯。
    • 26. 发明授权
    • Pharmaceutical compounds
    • 药物化合物
    • US08383619B2
    • 2013-02-26
    • US12902658
    • 2010-10-12
    • Martyn FredericksonMarian Williams
    • Brian John WilliamsMartyn Frederickson
    • A61K31/5377A61K31/496C07D413/14C07D403/14C07D403/06
    • C07D295/155C07D209/44
    • The invention provides a compound of the formula (1): or a salt, solvate, N-oxide or tautomer thereof; wherein either R1 is R1a and R2 is R2a; or R1 is R1b and R2 is R2b; provided that in each case at least one of R1 and R2 is other than hydrogen; R1a and R2a are the same or different and each is selected from hydrogen, C1-4 alkyl, C2-4 alkenyl and C2-4 alkynyl wherein the C1-4 alkyl is optionally substituted by C1-2 alkoxy; R1b and R2b are the same or different and are selected from hydrogen, C(O)NR4R5, C(O)R6 and C(O)OR6 where R6 is C1-4 alkyl, R4 and R5 are both C1-4 alkyl, or NR4R5 forms a 4 to 7 membered saturated heterocyclic ring optionally containing a second heteroatom ring member selected from O, N or S and oxidized forms of N and S, the heterocyclic ring being optionally substituted by one or two C1-4 alkyl groups and/or one or two oxo groups; and R3 is a group D: wherein the asterisk denotes the point of attachment to the isoindoline ring; but excluding acetic acid 5-acetoxy-4-isopropyl-2-[5-(4-methyl-piperazin-1-ylmethyl)-1,3-dihydro-isoindole-2-carbonyl]-phenyl ester.
    • 本发明提供式(1)化合物或其盐,溶剂合物,N-氧化物或其互变异构体; 其中R1是R1a,R2是R2a; 或R1为R1b且R2为R2b; 条件是在每种情况下,R 1和R 2中的至少一个不是氢; R1a和R2a相同或不同,各自选自氢,C 1-4烷基,C 2-4烯基和C 2-4炔基,其中C 1-4烷基任选被C 1-2烷氧基取代; R1b和R2b相同或不同,并且选自氢,C(O)NR4R5,C(O)R6和C(O)OR6,其中R6是C1-4烷基,R4和R5都是C1-4烷基或 NR4R5形成任选地含有选自O,N或S的第二杂原子环成员和氧化形式的N和S的4至7元饱和杂环,杂环任选被一个或两个C 1-4烷基和/或 一个或两个氧代基团; 并且R 3是基团D:其中星号表示与异二氢吲哚环的连接点; 但不包括乙酸5-乙酰氧基-4-异丙基-2- [5-(4-甲基 - 哌嗪-1-基甲基)-1,3-二氢 - 异吲哚-2-羰基] - 苯酯。