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52. 发明授权

US3941789A N-Aryl-N'-(phenyl-or phenoxy-alkyl)-piperazines and salts thereof 失效
标题翻译： N-芳基-N {40-（苯基 - 或苯氧基 - 烷基） - 哌嗪及其盐
公开(公告)号：US3941789A
公开(公告)日：1976-03-02
申请号：US427367
申请日：1973-12-21
申请人： Ernst-Otto Renth , Anton Mentrup , Kurt Schromm , Peter Danneberg
发明人： Ernst-Otto Renth , Anton Mentrup , Kurt Schromm , Peter Danneberg
IPC分类号： C07D233/72 , A61K31/415 , A61K31/4166 , A61K31/495 , A61K31/505 , A61K33/44 , A61P3/06 , A61P9/02 , A61P9/12 , A61P11/00 , A61P11/08 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/20 , A61P29/00 , A61P43/00 , C07D207/26 , C07D207/27 , C07D211/76 , C07D239/10 , C07D275/02 , C07D279/02 , C07D295/092 , C07D295/135 , C07D401/12 , C07D403/12 , C07D417/12 , C07D241/02
CPC分类号： C07D207/27 , A61K31/495 , C07D295/088 , C07D295/135
摘要： Compounds of the formula ##EQU1## wherein R is phenyl; phenyl having one or more substituents attached thereto, said substituents being selected from the group consisting of alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, alkylthio of 1 to 4 carbon atoms, halogen and trifluoromethyl; a bicyclic aromatic or cycloaliphatic-aromatic ring, especially naphthyl, tetrahydronaphthyl or indanyl; or a mono- or bicyclic heterocyclic ring, especially pyridyl, pyrimidyl, isoquinolyl or thiazolyl;R.sub.1 is ##EQU2## where B is ##EQU3## n is 2, 3 or 4, R.sub.3 is hydrogen, alkyl of 1 to 4 carbon atoms or alkanoyl of 1 to 4 carbon atoms,R.sub.4 and R.sub.5, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 4 carbon atoms,p is 0 or 1, andQ is oxygen or two hydrogens,R.sub.2 is hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or halogen,A is a single carbon-to-carbon bond or --OCH.sub.2 --,R.sub.6 is hydrogen, hydroxyl, alkoxy of 1 to 4 carbon atoms or alkanoyloxy of 1 to 4 carbon atoms, andm is 0, 1, 2, 3, 4 or 5, but other than 0 when R.sub.6 is hydroxyl,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as CNS-depressants, adrenolytics, antiphologistics, analgesics, antihistamines and anticholesterols.
摘要翻译：式A-CH-CmH2m-NN-R | R6的化合物，其中R是苯基; 具有一个或多个取代基的苯基，所述取代基选自1至4个碳原子的烷基，1至4个碳原子的烷氧基，1至4个碳原子的烷硫基，卤素和三氟甲基; 双环芳族或脂环族芳族环，特别是萘基，四氢萘基或茚满基; 或单环或双环杂环，特别是吡啶基，嘧啶基，异喹啉基或噻唑基; R 1（CH 2）p R 4角度-N（CH 2）n或Q = CR 5 ANGLE || B -NN-R3角度C平行O其中B为O O平行角-C-或-S-，n为2,3或 4，R3为氢，1〜4个碳原子的烷基或1〜4个碳原子的烷酰基，R4和R5可以相同或不同，分别为氢或1-4个碳原子的烷基，P IS 0 OR 1，Q为氧或两个氢，R 2为氢，1至4个碳原子的烷基，1至4个碳原子的烷氧基或卤素，A为单个碳 - 碳键或-OCH 2 - R6为氢，羟基，1〜4个碳原子的烷氧基或1〜4个碳原子的烷酰氧基，M为0,1,2,3,4或5，但当R6为羟基时，为0以及非毒性其药理学可接受的酸添加剂; 化合物作为它们的有效成分可用作CNS抑制剂，肾上腺素，抗病毒药物，镇痛药，抗组胺药和抗胆固醇。

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