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    • 6. 发明授权
    • 3,1 Benzoxazin-2-ones and use thereof
    • 3,苯并恶嗪-2-酮及其用途
    • US4341778A
    • 1982-07-27
    • US280349
    • 1981-07-06
    • Anton MentrupKurt SchrommErnst-Otto RenthWolfgang HoefkeWolfram GaidaIlse StrellerArmin Fugner
    • Anton MentrupKurt SchrommErnst-Otto RenthWolfgang HoefkeWolfram GaidaIlse StrellerArmin Fugner
    • C07D265/16A61K31/535A61K31/536A61P9/00A61P9/08A61P9/12A61P11/08A61P13/02A61P15/00C07D265/18C07D265/22
    • C07D265/18
    • The invention relates to compounds of general formula I ##STR1## (wherein R.sub.1 and R.sub.2, which may be the same or different, each represents a hydrogen atom or a (C.sub.1 -C.sub.4) alkyl group;R.sub.3 and R.sub.4, which may be the same or different, each represents a hydrogen, fluorine or chlorine atom or a hydroxy, methyl, ethyl or (C.sub.1 -C.sub.4) alkoxy group, or R.sub.3 together with R.sub.4 represents a methylenedioxy group;R.sub.5 and R.sub.6, which may be the same or different, each represents a hydrogen atom or a methyl group;R.sub.7 represents a group of formula ##STR2## R represents a hydrogen atom or a (C.sub.1 -C.sub.4) alkyl group; R.sub.8 represents a fluorine or chlorine atom or a (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkylthio, hydroxymethyl, CONHR.sub.11, SO.sub.2 NHR.sub.11, OR.sub.12, methoxycarbonyl, ethoxycarbonyl or NHSO.sub.2 CH.sub.3 group;R.sub.9 represents a hydrogen, fluorine or chlorine atom or a OR.sub.12 group;R.sub.10 represents a hydrogen or chlorine atom or an amino, methyl or methoxy group;R.sub.11 represents a hydrogen atom or a methyl, ethyl or hydroxyethyl group;R.sub.12 represents a hydrogen atom or a (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkyl-CO, aryl-CH.sub.2 or aryl-CO group; andn represents 1, 2 or 3) and acid addition salts thereof as well as to processes for their preparation and pharmaceutical compositions containing them. The compounds of the invention possess interesting pharmacological properties in particular displaying hypotensive and selective tocolytic effects.
    • 本发明涉及通式I(I)的化合物(其中R 1和R 2可以相同或不同,各自表示氢原子或(C 1 -C 4)烷基; R 3和R 4可以 相同或不同,各自表示氢,氟或氯原子或羟基,甲基,乙基或(C1-C4)烷氧基,或R3与R4一起代表亚甲二氧基; R5和R6可以相同 或不同的,各自表示氢原子或甲基; R 7表示下式的基团:R表示氢原子或(C 1 -C 4)烷基; R 8表示氟或氯原子或(C 1 -C 4) )烷基,(C1-C4)烷硫基,羟甲基,CONHR11,SO2NHR11,OR12,甲氧基羰基,乙氧基羰基或NHSO2CH3基; R9表示氢,氟或氯原子或OR12基团; R10表示氢或氯原子或氨基, 甲基或甲氧基; R11表示氢原子或甲基,乙基或羟乙基; R12表示a 氢原子或(C 1 -C 4)烷基,(C 1 -C 4)烷基-CO,芳基-CH 2或芳基-CO基团; 和n表示1,2或3)及其酸加成盐以及其制备方法和含有它们的药物组合物。 本发明的化合物具有特别显示降血压和选择性溶瘤作用的有趣的药理学性质。
    • 8. 发明授权
    • 1-aryloxypropanolamines
    • 1-芳氧基丙醇胺
    • US4594344A
    • 1986-06-10
    • US755044
    • 1985-07-15
    • Herbert KoppeWolfgang Abele, deceasedFranz EsserWolfram GaidaWolfgang Hoefke
    • Herbert KoppeWolfgang Abele, deceasedFranz EsserWolfram GaidaWolfgang Hoefke
    • A61K31/54A61P9/12C07D285/30C07D417/12
    • C07D285/30
    • Disclosed are novel compounds having the formula ##STR1## wherein R.sub.1 is a hydrogen or halogen atom, a lower alkyl, lower alkoxy, lower alkoxy lower alkyl, lower alkenyl, lower alkenyl oxy, cyano, hydroxy, trifluoromethyl, nitro, amino, aminocarbonylmethyl, lower monoalkylamino, lower dialkylamino group;R.sub.2 is a hydrogen or halogen atom, cyano, lower alkyl or lower alkoxy or acylamino group;R.sub.3 is a hydrogen or halogen atom, a lower alkyl or lower alkoxy group, while R.sub.2 and R.sub.3 together can also be a butadienyl or methylene dioxy group;R.sub.4 is a hydrogen atom or a lower alkyl group;R.sub.5 is a chlorine atom or a trifluoromethyl group;X is an alkylene group;and the non-toxic, pharmaceutically acceptable acid addition salts thereof.The compounds are suitable for treatment and prophylaxis of hypertension.
    • 公开了具有下式的新化合物:其中R1是氢或卤原子,低级烷基,低级烷氧基,低级烷氧基低级烷基,低级烯基,低级烯基氧基,氰基,羟基,三氟甲基,硝基,氨基,氨基羰基甲基, 低级单烷基氨基,低级二烷基氨基; R2是氢或卤素原子,氰基,低级烷基或低级烷氧基或酰氨基; R3是氢或卤素原子,低级烷基或低级烷氧基,R2和R3一起也可以是丁二烯基或亚甲基二氧基; R4是氢原子或低级烷基; R5是氯原子或三氟甲基; X是亚烷基; 和其无毒的药学上可接受的酸加成盐。 该化合物适用于治疗和预防高血压。