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    • 9. 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。
    • 10. 发明授权
    • Aminoalkyl-substituted benzimidazolidin-2-ones
    • 氨基烷基取代的苯并咪唑烷-2-酮
    • US4215119A
    • 1980-07-29
    • US26608
    • 1979-04-03
    • Anton MentrupKurt SchrommErnst-Otto RenthRichard ReichlWerner TrauneckerWolfgang Hoefke
    • Anton MentrupKurt SchrommErnst-Otto RenthRichard ReichlWerner TrauneckerWolfgang Hoefke
    • 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-Rwherein Q 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 atoms or 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 or 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 to 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 --COHN-- 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是氢或烷基或1至4个碳原子,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中的一个或两个不同于卤素或三氟甲基时,也可以是-NR 3 R 9,其中R 3具有上述定义,R 8是氢, 1至20个碳原子的烷酰基,1至4个碳原子的烷酰基或芳烷基,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至5个碳原子的烷氧基羰基,以及R5和R6, 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 -COOH-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。