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    Urinary incontinence ameliorating dibenz- b,e- -oxepin and -thiepin derivatives, compositions, and method of use therefor
    1.
    发明授权
    Urinary incontinence ameliorating dibenz- b,e- -oxepin and -thiepin derivatives, compositions, and method of use therefor 失效
    尿失禁改善二苯并b，e-氧化皮蛋白和硫蛋白衍生物，组合物及其使用方法

    公开(公告)号：US4645758A

    公开(公告)日：1987-02-24

    申请号：US820428

    申请日：1986-01-17

    申请人： Nils-Erik Willman ,  Bengt C. H. Sjogren ,  Lennart G. Nordh ,  Gustav L. Persson ,  Goran H. Sjoholm

    发明人： Nils-Erik Willman ,  Bengt C. H. Sjogren ,  Lennart G. Nordh ,  Gustav L. Persson ,  Goran H. Sjoholm

    IPC分类号： C07D493/10 ,  A61K31/00 ,  A61K31/335 ,  A61K31/38 ,  A61P13/02 ,  A61P15/00 ,  C07D313/12 ,  C07D337/12 ,  C07D405/06 ,  C07D493/04 ,  C07D493/14 ,  C07D493/20 ,  C07D493/22 ,  C07D495/04 ,  C07D495/10 ,  C07D495/14 ,  C07D495/20 ,  C07D495/22 ,  C07D498/10 ,  C07D498/20 ,  C07D498/22 ,  A61K31/36

    CPC分类号： C07D405/06 ,  C07D313/12 ,  C07D337/12

    摘要： The invention concerns:Novel dibenz/b,e/oxepin and dibenz/b,e/thiepin compounds having the general formula: ##STR1## wherein X is O or S,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are each selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulponyl, halogen, trifluoromethyl, trifluoromethylthio, lower dialkylsulphonamido, nitro, hydroxy, cyano, carbamyl, carboxy, lower alkoxycarbonyl, amino, N-lower alkylamino, N,N-diloweralkylamino, lower acylamido, lower alkanesulfonamido and lower acyl and, when on adjacent carbon atoms at the positions 2 and 3 and/or 8 and 9, two of the substituents R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4 taken together may form a methylenedioxy group;R.sup.5 and R.sup.6 are the same or different and are selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aralkyl, lower hydroxyalkyl, lower aminoalkyl, lower alkylaminoalkyl, lower dialkylaminoalkyl, lower alkoxyalkyl and together with the nitrogen atom, R.sup.5 and R.sup.6 may form a 5- or 6- membered ring, such as pyrrolidine, piperidine, morpholine, piperazine, and N-lower alkyl or N-hydroxy lower alkyl substituted rings such as N-alkylpiperazine or N-hydroxyalkyl piperazine or the like,R.sup.7 is hydrogen or lower alkyl; optionally in the form of addition salts with pharmaceutically acceptable inorganic or organic acids and optionally in the form of essentially pure enantiomers.The invention also includes compositions containing the novel compounds, processes for their preparation and a method of treatment therewith.The compounds have pharmacological effects.

    摘要翻译： 本发明涉及：具有以下通式的新型二苯并/ b，e /氧杂七环素和二苯并/ b，e /硫氮烯化合物：其中X为O或S，R 1，R 2，R 3和R 4的化合物相同或 不同的并且各自选自氢，低级烷基，低级烯基，低级炔基，低级环烷基，低级烷氧基，低级烷硫基，低级烷基亚磺酰基，低级烷基亚磺酰基，卤素，三氟甲基，三氟甲硫基，低级二烷基磺酰胺基，硝基，羟基，氰基 ，氨基甲酰基，羧基，低级烷氧基羰基，氨基，N-低级烷基氨基，N，N-二低级烷基氨基，低级酰基酰氨基，低级链烷磺酰氨基和低级酰基，当在位置2和3和/或8和9相邻的碳原子上时， 取代基R 1和R 2或R 3和R 4一起可以形成亚甲二氧基; R5和R6相同或不同，选自氢，低级烷基，低级烯基，低级炔基，低级环烷基，芳烷基，低级羟基烷基，低级氨基烷基，低级烷基氨基烷基，低级二烷基氨基烷基，低级烷氧基烷基， 氮原子，R5和R6可以形成5-或6-元环，例如吡咯烷，哌啶，吗啉，哌嗪和N-低级烷基或N-羟基低级烷基取代的环，例如N-烷基哌嗪或N-羟基烷基哌嗪 R 7为氢或低级烷基; 任选地以与药学上可接受的无机酸或有机酸加成盐的形式，并且任选地以基本上纯的对映异构体的形式。 本发明还包括含有新化合物的组合物，其制备方法及其处理方法。 该化合物具有药理作用。