首页> 外国专利> New 3-phenyl-1-(phenylsulfonyl)-1,3-dihydro-2H-indol-1-one derivatives, are arginine-vasopressin and/or oxytocin receptor ligands useful e.g. for treating cardiovascular or central nervous system disorders

New 3-phenyl-1-(phenylsulfonyl)-1,3-dihydro-2H-indol-1-one derivatives, are arginine-vasopressin and/or oxytocin receptor ligands useful e.g. for treating cardiovascular or central nervous system disorders

机译:新的3-苯基-1-(苯基磺酰基)-1,3-二氢-2H-吲哚-1-酮衍生物是精氨酸-加压素和/或催产素受体配体,例如可用于例如苯丙氨酸。用于治疗心血管或中枢神经系统疾病

摘要

Piperazino- or homopiperazino-substituted 3-phenyl-1-(phenylsulfonyl)-1,3-dihydro-2H-indol-1-one derivatives (I) are new. Indolone derivatives of formula (I) and their mineral or organic acid addition salts, solvates and/or hydrates are new. n = 1 or 2; X = CH2, O, NH, OCH2, NHCH2 or NHCH2CH2; R1 = halo, 1-4C alkyl or 1-4C alkoxy; R2 = H, halo, 1-4C alkyl, 1-4C alkoxy or CF3; R3 = halo, 1-3C alkyl, 1-3C alkoxy, CF3 or OCF3; R4 = H, halo, 1-3C alkyl or 1-3C alkoxy; R5 = 2-, 3- or 4-pyridinyl, 2-, 4- or 5-pyrimidinyl, 2-pyrazinyl or 3- or 4-pyridazinyl; R6, R7 = 1-4C alkoxy. Independent claims are also included for: (1) the preparation of (I); and (2) new 1-unsubstituted indolone derivative intermediates of formula (IV) and their mineral or organic acid addition salts, as pure optical isomers or their mixture. X' = CH2 or OCH2.
机译:哌嗪子基或高哌嗪子基取代的3-苯基-1-(苯基磺酰基)-1,3-二氢-2H-吲哚-1-酮衍生物(I)是新的。式(I)的吲哚酮衍生物及其无机或有机酸加成盐,溶剂化物和/或水合物是新的。 n = 1或2; X = CH 2,O,NH,OCH 2,NHCH 2或NHCH 2 CH 2; R1 =卤素,1-4C烷基或1-4C烷氧基; R2 = H,卤素,1-4C烷基,1-4C烷氧基或CF3; R3 =卤素,1-3C烷基,1-3C烷氧基,CF3或OCF3; R4 = H,卤素,1-3C烷基或1-3C烷氧基; R5 = 2-,3-或4-吡啶基,2-,4-或5-嘧啶基,2-吡嗪基或3-或4-哒嗪基; R6,R7 = 1-4C烷氧基。独立权利要求还包括:(1)(I)的制备; (2)新的式(Ⅳ)的1-未取代的吲哚酮衍生物中间体及其无机或有机酸加成盐,为纯的旋光异构体或它们的混合物。 X'= CH 2或OCH 2。

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