发明名称 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
摘要 <p>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>, R2>H, A, OH, OA, CN, halo, COR or CH2R; R3>A, 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.</p>
申请公布号 DE10353657(A1) 申请公布日期 2005.06.23
申请号 DE2003153657 申请日期 2003.11.17
申请人 MERCK PATENT GMBH 发明人 HOELZEMANN, GUENTER;CRASSIER, HELENE;SCHIEMANN, KAI;BOETTCHER, HENNING;HEINRICH, TIMO;LEIBROCK, JOCHIM;AMSTERDAM, CHRISTOPH VAN;BARTOSZYK, GERD;SEYFRIED, CHRISTOPH
分类号 A61K31/404;A61K31/4523;A61P25/00;C07D401/12;C07D405/12;C07D405/14;(IPC1-7):C07D405/12;A61K31/452 主分类号 A61K31/404
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