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    • 4. 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。
    • 9. 发明授权
    • (1-Hydroxy-2-amino-alkyl)-substituted benzoxazinones and benzoxazolinones
    • (1-羟基-2-氨基 - 烷基)取代的苯并恶嗪酮和苯并恶唑啉酮
    • US4460581A
    • 1984-07-17
    • US433681
    • 1982-10-12
    • Kurt SchrommAnton MentrupErnst-Otto RenthArmin Fugner
    • Kurt SchrommAnton MentrupErnst-Otto RenthArmin Fugner
    • C07D263/58C07D265/36C07D413/12A61K31/47
    • C07D263/58C07D265/36C07D413/12
    • Compounds of the formula ##STR1## wherein A is a single bond, ##STR2## R.sub.1 is --OH, --0--acyl, chlorine or hydrogen; R.sub.2 is hydrogen, methyl or ethyl;R.sub.3 is ##STR3## m is 2, 3 or 4; n is 1, 2 or 3;R.sub.4 is hydrogen or lower alkyl;R.sub.5 is hydrogen, lower alkyl or, when R.sub.4 is hydrogen, also phenyl;R.sub.6, R.sub.7 and R.sub.8 are each hydrogen or methyl;R.sub.9 is hydrogen, --Ar, --OAr or --NH--CO--Ar;Ar is ##STR4## R.sub.10, R.sub.11 and R.sub.12 which may be identical to or different from each other, are each hydrogen, hydroxyl, methyl, methoxy, halogen, methylenedioxy, --NH--R.sub.13 or --CONH.sub.2 ; andR.sub.13 is hydrogen, acyl or lower alkylsulfonyl;and non-toxic, pharmaceutically acceptable acid addition salts thereof; the compounds as well as their salts are useful for the treatment of asthma, bronchitis, urticaria, conjunctivities, hay fever, colds and cardiovascular disorders, and for relaxation of the uterine musculature.
    • 其中A是单键的式“IMAGE”的化合物,R 1是-OH,-O-酰基,氯或氢; R2是氢,甲基或乙基; R3为 m为2,3或4; n为1,2或3; R4是氢或低级烷基; R5是氢,低级烷基,或当R4是氢时也是苯基; R6,R7和R8各自为氢或甲基; R9是氢,-Ar,-OAr或-NH-CO-Ar; Ar可以相同或不同,分别是氢,羟基,甲基,甲氧基,卤素,亚甲二氧基,-NH-R13或-CONH 2; R 1,R 2, 和R 13是氢,酰基或低级烷基磺酰基; 和无毒的药学上可接受的酸加成盐; 化合物及其盐可用于治疗哮喘,支气管炎,荨麻疹,结膜炎,花粉症,感冒和心血管疾病,以及用于放松子宫肌肉组织。