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N-biphenylcarbonyl- and N-phenylpyridylcarbonyl-substituted di- and tricyclic azepines and diazepines as vasopressin agonists

机译:N-联苯基羰基和N-苯基吡啶基羰基取代的二环和三环阿塞品和二氮杂苯为加压素激动剂

摘要

A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or -(CHSUB2/SUB)SUBn/SUB; wherein R is hydrogen or (CSUB1/SUB-CSUB6/SUB) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (CSUB1/SUB-CSUB6/SUB) lower alkyl, halogen, cyano, CFSUB3/SUB, hydroxy, (CSUB1/SUB-CSUB6/SUB) lower alkoxy, (CSUB1/SUB-CSUB6/SUB) lower alkoxy carbonyl, carboxy, -CONHSUB2/SUB, -CONH[(CSUB1/SUB-CSUB6/SUB) lower alkyl], -CON[(CSUB1/SUB-CSUB6/SUB) lower alkyl]SUB2/SUB; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (CSUB1/SUB-CSUB6/SUB) lower alkyl, halogen or (CSUB1/SUB-CSUB6/SUB) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (CSUB1/SUB-CSUB6/SUB) lower alkyl, halogen, cyano, CFSUB3/SUB, hydroxy, (CSUB1/SUB-CSUB6/SUB) lower alkoxy, or (CSUB1/SUB-CSUB6/SUB) lower alkoxy carbonyl, carboxy, -CONHSUB2/SUB, -CONH[(CSUB1/SUB-CSUB6/SUB) lower alkyl], -CON[(CSUB1/SUB-CSUB6/SUB) lower alkyl]SUB2/SUB; or (2) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (CSUB1/SUB-CSUB6/SUB) lower alkyl, (CSUB1/SUB-CSUB6/SUB) lower alkoxy, or halogen; or (3) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (CSUB1/SUB-CSUB6/SUB) lower alkyl, halogen, or (CSUB1/SUB-CSUB6/SUB) lower alkoxy; represents a 5-membered aromatic (unsaturated) heterocyclic ring having one sulfur atom, optionally substituted by (CSUB1/SUB-CSUB6/SUB) lower alkyl, halogen, or (CSUB1/SUB-CSUB6/SUB) lower alkoxy; RSUB1 /SUBis a moiety of the formula and RSUB2/SUB, RSUB3/SUB, RSUB7/SUB, RSUB8 /SUBand RSUB9 /SUBare, independently, selected from a group consisting of hydrogen, (CSUB1/SUB-CSUB3/SUB) lower alkyl, OCHSUB3/SUB, halogen, CFSUB3/SUB, -SCHSUB3/SUB, OCFSUB3/SUB, SCFSUB3/SUB, or CN; or a pharmaceutically acceptable salt, or pro-drug form thereof.
机译:式(I)或(II)的化合物:其中:Y是选自NR或-(CH 2 n 的部分;其中R为氢或(C 1 -C 6 )低级烷基,n为1;代表:(1)任选地被一个或两个独立地选自氢,(C 1 -C 6 )低级烷基,卤素的取代基取代的苯环,氰基,CF 3 ,羟基,(C 1 -C 6 )低级烷氧基,(C 1 - C 6 )低级烷氧基羰基,羧基,-CONH 2 ,-CONH [(C 1 -C 6 )低级烷基],-CON [(C 1 -C 6 )低级烷基] 2 ;或(2)具有一个氮原子的六元芳香族(不饱和)杂环,其任选被(C 1 -C 6 )低级烷基,卤素或(C 1 -C 6 )低级烷氧基;代表:(1)任选地被一个或两个独立地选自氢,(C 1 -C 6 )低级烷基,卤素的取代基取代的苯环,氰基,CF 3 ,羟基,(C 1 -C 6 )低级烷氧基或(C 1 -C 6 )低级烷氧基羰基,羧基,-CONH 2 ,-CONH [(C 1 -C 6 )低级烷基],-CON [(C 1 -C 6 )低级烷基] 2 ;或(2)具有一个氮原子的5元芳香族(不饱和)杂环,其任选被(C 1 -C 6 )低级烷基取代,(C 1 -C 6 )低级烷氧基或卤素; (3)具有一个氮原子的六元芳香族(不饱和)杂环,其任选被(C 1 -C 6 )低级烷基,卤素或( C 1 -C 6 )低级烷氧基;表示具有一个硫原子的5元芳族(不饱和)杂环,可选地被(C 1 -C 6 )低级烷基,卤素或(C 1 -C 6 )低级烷氧基; R 1 是下式的组成部分,R 2 ,R 3 ,R 7 ,R 8 和R 9 独立地选自氢(C 1 -C 3 )低级烷基,OCH 3 ,卤素,CF 3 ,-SCH 3 ,OCF 3 ,SCF 3 < / SUB>或CN;或其药学上可接受的盐或其前药形式。

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