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BICYCLIC DERIVATIVES AND THEIR APPLICATION AS MODULATORS OF ION CHANNELS

机译:双环导数及其在离子通道调节剂中的应用

摘要

1. The compound of formula I:! ! or a pharmaceutically acceptable salt thereof,! where the ring Z is a 5-7 membered unsaturated or aromatic ring containing at least one heteroatom in the ring selected from O, S, N or NH; ! wherein ring Z may optionally be fused to ring A, which is an optionally substituted 5-7 membered unsaturated or aromatic ring; and! ring Z or ring Z together with the aforementioned condensed ring A may be substituted by a number z of substituents Rz; ! z is 0-4; ! each Rz element is independently selected from R1, R2, R3, R4, or R5; ! q is 0-2; ! Q means a bond or a C1-C6 straight or branched alkylidene chain in which one or two non-adjacent methylene units of Q are optionally and independently substituted by -CO-, -CS-, -COCO-, -CONR2, -CONR2NR2-, -CO2-, - OCO-, -NR2CO2-, -O-, -NR2CONR2-, -OCONR2-, -NR2NR2-, -NR2NR2CO-, -NR2CO-, -S-, -SO-, -SO2-, -NR2-, -SO2NR2- , -NR2SO2-, -NR2SO2NR2- or the spirocycloalkylene part; ! RQ means a C1-6 aliphatic group, a 3-8 membered saturated, partially unsaturated or fully unsaturated monocyclic ring containing 0-3 heteroatoms independently selected from O, S, N or NH, or an 8-12 membered saturated, partially unsaturated or a completely unsaturated bicyclic ring system containing 0-5 heteroatoms independently selected from O, S, N or NH; ! wherein the RQ element may optionally be substituted with 1-4 substituents independently selected from R1, R2, R3, R4 or R5; ! RM and RN independently mean R2; ! R1 is oxo, = NN (R6) 2, = NN (R7) 2, = NN (R6R7), R6 or (CH2) n-Y; ! n is 0, 1 or 2; ! Y is halogen, CN, NO2, CF3, OCF3, OH, SR6, S (O) R6, SO2R6, NH2, NHR6, N (R6) 2, NR6R8, COOH, COOR6 or OR6; either! two elements of R1 at adjacent atoms in the ring taken together form 1,2-methylenedioxy or 1,2-ethylenediox�
机译:1.式I的化合物:! !或其药学上可接受的盐!其中环Z是5-7元不饱和或芳族环,在环中含有至少一个选自O,S,N或NH的杂原子; !其中环Z可以任选地稠合至环A,该环是任选取代的5-7元不饱和或芳族环;和!环Z或环Z与上述稠合环A一起可被多个z的取代基Rz取代; ! z为0-4; !每个Rz元素独立地选自R1,R2,R3,R4或R5; ! q是0-2; ! Q是指键或C 1 -C 6直链或支链亚烷基链,其中Q的一个或两个不相邻的亚甲基单元任选地并且独立地被-CO-,-CS-,-COCO-,-CONR2,-CONR2NR2-取代。 ,-CO2-,-OCO-,-NR2CO2-,-O-,-NR2CONR2-,-OCONR2-,-NR2NR2-,-NR2NR2CO-,-NR2CO-,-S-,-SO-,-SO2-,- NR 2-,-SO 2 NR 2-,-NR 2 SO 2-,-NR 2 SO 2 NR 2-或螺环亚烷基部分; ! RQ是指C 1-6脂族基团,含有0-3个独立地选自O,S,N或NH的杂原子的3-8元饱和,部分不饱和或完全不饱和的单环,或8-12元饱和,部分不饱和或3-8元的单环。含有0-5个独立地选自O,S,N或NH的杂原子的完全不饱和双环系统; !其中RQ元素可以任选地被1-4个独立地选自R1,R2,R3,R4或R5的取代基取代; ! RM和RN独立地表示R2; ! R1是氧代,= NN(R6)2,= NN(R7)2,= NN(R6R7),R6或(CH2)n-Y; ! n为0、1或2; ! Y是卤素,CN,NO 2,CF 3,OCF 3,OH,SR 6,S(O)R 6,SO 2 R 6,NH 2,NHR 6,N(R 6)2,NR 6 R 8,COOH,COOR 6或OR 6;要么!环中相邻原子上的R1的两个元素一起形成1,2-亚甲二氧基或1,2-亚乙二氧基。

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