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    • 3. 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。
    • 10. 发明授权
    • Vasodilating or antidepressant phenalkanolaminoalkyl-substituted
imidazolidinones
    • 血管舒张或抗抑郁药苯烷醇氨基烷基取代的咪唑啉酮
    • US4271158A
    • 1981-06-02
    • US102904
    • 1979-12-13
    • Anton MentrupKurt SchrommErnst-Otto RenthRichard Reichl
    • Anton MentrupKurt SchrommErnst-Otto RenthRichard Reichl
    • C07D215/02A61K31/404A61K31/415A61K31/4166A61K31/4184A61K31/42A61K31/423A61K31/4245A61K31/536A61P9/08A61P9/12A61P11/00A61P25/24A61P25/26C07D215/22C07D215/227C07D223/04C07D233/32C07D233/36C07D235/04C07D235/22C07D235/26C07D263/54C07D263/58C07D265/22C07D265/36C07D405/04C07D405/12C07D413/12A61K31/535
    • C07D215/227C07D233/36C07D235/26C07D263/58C07D265/36Y10S514/929
    • Racemic and optically active compounds of the formulaQ--C.sub.n H.sub.2n --NH--RwhereinQ is ##STR1## where R.sub.1 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, trifluoromethyl or amino,R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atomsor trifluoromethyl,R.sub.1 and R.sub.2, together with each other, are methylenedioxy or ethylenedioxy, andA is --O--, --CH.sub.2 --CH.sub.2 --, or --NR.sub.3 -- where R.sub.3 is hydrogen or alkyl of 1 to 4 carbon atoms,n is an integer from 2 to 6, inclusive, andR is hydrogen, benzyl or ##STR2## where R.sub.4 is hydrogen, methyl or ethyl,R.sub.5, R.sub.6 and R.sub.7, which may be identical to or different from each other, are each hydrogen, halogen, hydroxymethyl, trifluoromethyl, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, nitro, cyano, --CONHR.sub.3, --CONHOH, --COOR.sub.3, R.sub.8 O--, methylsulfonylmethyl or, when one or two of R.sub.5 through R.sub.7 are other than halogen or trifluoromethyl, also--NR.sub.3 R.sub.9, whereR.sub.3 has the meanings defined above,R.sub.8 is hydrogen, alkanoyl of 1 to 20 carbon atoms, alkyl of 1 to 4 carbon atoms, or aralkyl, andR.sub.9 is hydrogen, lower alkanoyl, methanesulfonyl, carbamoyl, dimethylsulfamoyl, or alkoxycarbonyl of 2 or 5 carbon atoms, andR.sub.5 and R.sub.6, together with each other, are --O--CH.sub.2 --O, --O--CH.sub.2 --CH.sub.2 --O--, --CH.dbd.CH--CH.dbd.CH--, --O--CH.sub.2 --CONH--, --CH.sub.2 --CH.sub.2 --CONH-- or --O--CO--NH--, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as vasodilators and CNS- stimulators.
    • 其中Q为氢,卤素,1至4个碳原子的烷基,1至4个碳原子的烷氧基,三氟甲基或氨基,R 2为式Q-C n H 2n-NH-R的外消旋和旋光活性化合物 氢,卤素,1至4个碳原子的烷基,1至4个碳原子的烷氧基或三氟甲基,R 1和R 2彼此一起是亚甲二氧基或亚乙二氧基,A是-O-,-CH 2 -CH 2 - 或 - NR 3 - 其中R 3是氢或1至4个碳原子的烷基,n是2-6的整数,包括2和6,R是氢,苄基或者其中R 4是氢,甲基或乙基,R 5,R 6和R 7 可以相同或不同,分别为氢,卤素,羟甲基,三氟甲基,1至4个碳原子的烷基,1至4个碳原子的烷氧基,硝基,氰基,-CONHR 3,-CONHOH,-COOR 3 ,R8O-,甲基磺酰基甲基,或当R 5至R 7中的一个或两个不是卤素或三氟甲基时,还有-NR 3 R 9,其中R 3具有上述定义,R 8是氢, 1至20个碳原子的芳基,1至4个碳原子的烷基或芳烷基,R 9是氢,低级烷酰基,甲磺酰基,氨基甲酰基,二甲基氨磺酰基或2或5个碳原子的烷氧基羰基,以及R 5和R 6 另一个是-O-CH 2 -O,-O-CH 2 -CH 2 -O - , - CH = CH-CH = CH-,-O-CH 2 -CONH - , - CH 2 -CH 2 -CONH-或-O-CO -NH-和无毒的药学上可接受的酸加成盐。 化合物及其盐可用作血管扩张剂和CNS刺激剂。