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    • 5. 发明授权
    • Condensed diazepinones and medicaments containing these compounds
    • 浓缩二氮杂酮和含有这些化合物的药物
    • US5179090A
    • 1993-01-12
    • US779203
    • 1991-10-18
    • Klaus RudolfWolfhard EngelWolfgang EberleinGunter TrummlitzGerhard MihmHenri DoodsNorbert Mayer
    • Klaus RudolfWolfhard EngelWolfgang EberleinGunter TrummlitzGerhard MihmHenri DoodsNorbert Mayer
    • C07D487/18C07D519/00
    • C07D487/18C07D519/00
    • Condensed diazepinones of general formula I ##STR1## in which]B represents one of the divalent groups ##STR2## X is a .dbd.CH-- group or a nitrogen atom,R represents a lower alkyl radical, which may optionally be further substituted by a phenyl optionally carrying halogen, methyl or methoxy,R.sup.4 and R.sup.5 represent hydrogen, halogen or lower alkyl,R.sup.6 is hydrogen, chlorine or methyl,R.sup.7 and R.sup.8 denote lower alkyl, R.sup.8 also additionally denotes halogen, andm, n, o and p represent the numbers 0, 1, 2 or 3 with the following limitations: the sum of m+n and the sum of o+p each denote the numbers 1, 2 or 3, the sum of n+o and the sum of m+p each denote the numbers 1, 2, 3, 4 or 5, wherein, however, the sum of m+n+o+p must always be greater than 2, andA.sup.1, A.sup.2, A.sup.3 and A.sup.4 denote hydrogen, or, for the case where m, n, o and p each denote the number 1, A.sup.1 and A.sup.2 together or A.sup.3 and A.sup.4 together represent an ethylene bridge,are suitable for the treatment of cholinergically induced spasms and motility disorders of the gastrointestinal tract and in the region of the evacuating bile ducts, for the symptomatic treatment of cystitis and of spasms from urelithiasis, for the treatment of relative incontinence, for the symptomatic treatment of bronchial asthma and bronchitis, and for the treatment of ischaemic heart diseases. The compounds are characterized by good selectivity.
    • (I)其中] + E,crc / B /表示二价基团之一的通式I的缩二氮杂酮类(I)其中一个二价基团(S)(T) V)X是= CH-基或氮原子,R表示低级烷基,其可以任选地被任选地带有卤素,甲基或甲氧基的苯基进一步取代,R4和R5代表氢,卤素或低级烷基,R6 是氢,氯或甲基,R7和R8表示低级烷基,R8还另外表示卤素,m,n,o和p表示数字0,1,2或3,具有以下限制:m + n和 o + p的和表示数字1,2或3,n + o和m + p之和各自表示数字1,2,3,4或5,其中,然而, m + n + o + p必须始终大于2,A1,A2,A3和A4表示氢,或者对于m,n,o和p分别表示数字1,A1和A2一起或A3 和A4一起代表乙烯桥,适合于处理o f胆碱能诱发胃肠道的痉挛和运动障碍以及排空胆管区域,用于膀胱炎和尿毒症痉挛的症状治疗,用于治疗相对失禁,用于支气管哮喘和支气管炎的症状治疗, 并用于治疗缺血性心脏病。 该化合物的特征在于良好的选择性。