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    • 1. 发明授权
    • N-Aryl-N'-(phenyl- or phenoxy-alkyl)-piperazines and salts thereof
    • N-芳基-N {40-(苯基 - 或苯氧基 - 烷基) - 哌嗪及其盐
    • US4100282A
    • 1978-07-11
    • US793736
    • 1977-05-04
    • Ernst-Otto RenthAnton MentrupKurt SchrommPeter Danneberg
    • Ernst-Otto RenthAnton MentrupKurt SchrommPeter Danneberg
    • A61K31/495C07D207/26C07D207/27C07D279/02
    • C07D207/27A61K31/495
    • Compounds of the formula ##STR1## wherein R is phenyl; phenyl having one or two 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, chlorine and trifluoromethyl; naphthyl; tetrahydronaphthyl; indanyl; pyridyl; isoquinolyl; or thiazolyl;R.sub.1 is ##STR2## where R.sub.3 is hydrogen, alkyl of 1 to 4 carbon atoms,R.sub.4 and R.sub.5 are each hydrogen or alkyl of 1 to 4 carbon atoms, 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, antiphlogistics, analgesics, antihistaminics and anticholesteremics.
    • 其中R是苯基的式“IMAGE”的化合物; 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,氯和三氟甲基; 萘基; 四氢萘基; 茚满基 吡啶基 异喹啉基 或噻唑基; R1是,其中R3是氢,1-4个碳原子的烷基,R4和R5分别是氢或1-4个碳原子的烷基,Q是氧或两个氢,R2是氢,1-4个 碳原子数为1〜4的烷氧基或卤素,A为单碳 - 碳键或-OCH2-,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, 并且M IS为0,1,2,3,4或5,但当R6为羟基时为0以及非毒性,药理学上可接受的酸添加量; 化合物作为它们的有效作为CNS抑制剂,肾上腺素,消炎药,镇痛药,抗组胺药和抗胆碱血症有用。
    • 5. 发明授权
    • N-Aryl-N'-(phenyl-or phenoxy-alkyl)-piperazines and salts thereof
    • N-芳基-N {40-(苯基 - 或苯氧基 - 烷基) - 哌嗪及其盐
    • US3941789A
    • 1976-03-02
    • US427367
    • 1973-12-21
    • Ernst-Otto RenthAnton MentrupKurt SchrommPeter Danneberg
    • Ernst-Otto RenthAnton MentrupKurt SchrommPeter Danneberg
    • C07D233/72A61K31/415A61K31/4166A61K31/495A61K31/505A61K33/44A61P3/06A61P9/02A61P9/12A61P11/00A61P11/08A61P25/00A61P25/02A61P25/04A61P25/20A61P29/00A61P43/00C07D207/26C07D207/27C07D211/76C07D239/10C07D275/02C07D279/02C07D295/092C07D295/135C07D401/12C07D403/12C07D417/12C07D241/02
    • C07D207/27A61K31/495C07D295/088C07D295/135
    • 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.
    • 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。