首页> 外国专利> New quinolonyl- or benzopyranonyl-substituted indole derivatives are 5HT(1A)- and/or 5HT(1D)-agonists useful e.g. as anxiolytic, antidepressant, neuroleptic and/or antihypertensive agents

New quinolonyl- or benzopyranonyl-substituted indole derivatives are 5HT(1A)- and/or 5HT(1D)-agonists useful e.g. as anxiolytic, antidepressant, neuroleptic and/or antihypertensive agents

机译:新的喹啉基或苯并吡喃基取代的吲哚衍生物是有用的5HT(1A)-和/或5HT(1D)-激动剂。作为抗焦虑药,抗抑郁药,抗精神病药和/或降压药

摘要

3-(Quinolonyl- or benzopyranonyl-oxyalkylaminoalkyl)-indole derivatives (I) are new. Indole derivatives of formula (I) and their derivatives, solvates and stereoisomers (including mixtures in all proportions) are new. [Image] X : quinolone or benzopyranone derivative group of formula (a)-(d); Z : O or NH; Y : N(R)-(CH2)n or piperidine-1,4-diyl; Q : O or S; R : H or A'; R1, R2H, A, OH, OA, CN, halo, COR or CH2R; R3A, halo, OH, OA, SA, COOH, COOA', CHO, COA', SO2A', NH2NHA, NA2, CH2NA2, NRCOA, NRCOAr, NRCOOA, NRSO2A, NRSO2Ar, CH2NRSO2A, NRCONH2, NRCONHA, NRCONA2, NRCONHAr, CONR2, CONRA, CONA2, SO2NR2, SO2NHA, SO2NA2, CH2SO2NH2, CH2SO2NHA or CH2SO2NA2; A : 1-10C alkyl (optionally having 1 or 2 CH2 groups replaced by CH=CH and optionally substituted by 1-7 F and/or Cl); A' : 1-6C alkyl or benzyl; m : 2-6; n : 1-4; p, r, s : 0-2; An independent claim is also included for the preparation of (I). ACTIVITY : Tranquilizer; Antidepressant; Neuroleptic; Hypotensive; Neuroprotective; Nootropic; Vasotropic; Hypnotic; Anorectic; Cerebroprotective; Antiparkinsonian; Anticonvulsant; Vulnerary; Antimigraine; Antiaddictive; Gynecological; Osteopathic. MECHANISM OF ACTION : 5HT(1A)- and/or 5HT(1D)-agonist; 5-HT reuptake inhibitor.
机译:3-(喹啉基-或苯并吡喃基-氧基烷基氨基烷基)-吲哚衍生物(I)是新的。式(I)的吲哚衍生物及其衍生物,溶剂化物和立体异构体(包括所有比例的混合物)是新的。 [图像] X:式(a)-(d)的喹诺酮或苯并吡喃酮衍生物基团; Z:O或NH; Y:N(R)-(CH 2)n或哌啶-1,4-二基;问:O或S; R:H或A'; R1>,R2> H,A,OH,OA,CN,卤素,COR或CH2R; R3> A,卤素,OH,OA,SA,COOH,COOA',CHO,COA',SO2A',NH2NHA,NA2,CH2NA2,NRCOA,NRCOAr,NRCOOA,NRSO2A,NRSO2Ar,CH2NRSO2A,NRCONH2,NRCONHA,NRCONA ,CONR2,CONRA,CONA2,SO2NR2,SO2NHA,SO2NA2,CH2SO2NH2,CH2SO2NHA或CH2SO2NA2; A:1-10C烷基(任选具有1或2个CH 2基团,被CH = CH取代并且任选被1-7 F和/或Cl取代); A':1-6C烷基或苄基; m:2-6; n:1-4; p,r,s:0-2;还包括独立权利要求以制备(I)。活动:镇静剂;抗抑郁药抗精神病药;降压;具有神经保护作用;促智;变压性催眠;厌食的;脑保护反帕金森病;抗惊厥药;伤药;抗偏头痛;反吸毒妇科整骨疗法。作用机理:5HT(1A)-和/或5HT(1D)-激动剂; 5-HT再摄取抑制剂。

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