首页> 外国专利> BASICALLY SUBSTITUTED DITERTIARY UREAS IN THE SERIES OF CONDENSED TRICYCLIC 1,4-DIAZEPIN-5-ONES,THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

BASICALLY SUBSTITUTED DITERTIARY UREAS IN THE SERIES OF CONDENSED TRICYCLIC 1,4-DIAZEPIN-5-ONES,THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

机译:稠合三环1,4-二氮杂-5-酮系列中的基本取代的脲类化合物,其制备及药物成分

摘要

Condensed diazepinones of the general formula I IMAGE in which IMAGE represents one of the divalent radicals IMAGE and X1, X2, A, R1 to R10 and Z have the following meanings: X1 and X2 represent a = CH-group or, if IMAGE assumes the meanings of the abovementioned divalent radicals (S), (U) or (W), both or only X1 or only X2 can also represent a nitrogen atom; A is an alkylene radical having two to seven carbon atoms; which can also be interrupted by an oxygen or sulphur atom or by the methylimino or ethylimino group; Z is a single bond, an oxygen or sulphur atom, the methylene or 1,2-ethylene group; R1 is a lower alkyl radical or the benzyl group; R2 is an alkyl radical having 1 to 7 carbon atoms, which can optionally be further substituted by a hydroxyl group on its 2nd to 7th carbon atom, a cycloalkyl or a cycloalkylmethyl radical, where the cycloalkyl ring can optionally be further substituted by a hydroxyl group; R1 and R2, however, together with the nitrogen atom lying in between, can also form a 4- to 7-membered saturated, monocyclic heterocyclic ring which can optionally be interrupted by an oxygen atom or by the N-CH3 group; R2 can, however, also be linked to A via an alkylene bridge such that, together with the group NR1, a saturated, 5 to 7-membered heterocyclic ring system is formed; R3 is a lower alkyl group, a chlorine atom or a hydrogen atom; R4 is a hydrogen atom or a methyl group; R5 and R6 each denote a hydrogen atom, a fluorine, chlorine or bromine atom or a lower alkyl group; R7 is a hydrogen or chlorine atom or a methyl group; R8 is a hydrogen atom or a lower alkyl radical; R9 is a hydrogen or halogen atom or a lower alkyl group and R10 is a hydrogen atom or a methyl group, where in the case in which IMAGE represents the divalent radical (T) and R7 is hydrogen, R3 cannot be chlorine and Z cannot be sulphur. Processes for their preparation and medicaments which contain these compounds are also described. In view of the lack of gastric acid secretion-inhibiting, salivation-inhibiting and mydriatic influences, the novel diazepinones are suitable as vagal pacemakers for the treatment of bradycardias and bradyarrhythmias in human and veterinary medicine.
机译:通式I 的缩二二氮杂酮,其中代表二价基团和X <1>,X <2>,A,R <1>至R <1> <0>和Z具有以下含义:X <1>和X <2>表示一个= CH-基团,或者,如果假定上述二价基团(S),(U)或(W)的含义,则两者或仅X 1或仅X 2也可以表示氮原子。 A为具有两个至七个碳原子的亚烷基;也可以被氧或硫原子或甲基亚氨基或乙基亚氨基中断; Z为单键,氧或硫原子,亚甲基或1,2-亚乙基; R 1为低级烷基或苄基; R 2为具有1至7个碳原子的烷基,其可任选地被其2至7个碳原子上的羟基,环烷基或环烷基甲基基团进一步取代,其中该环烷基环可进一步被以下基团取代:羟基;然而,R 1和R 2以及位于它们之间的氮原子也可以形成4至7元饱和的单环杂环,其可以任选地被氧原子或被N-中断。 CH3组;然而,R 2也可以通过亚烷基桥与A连接,从而与基团NR 1一起形成饱和的5至7元杂环系统; R 3为低级烷基,氯原子或氢原子; R 4为氢原子或甲基。 R 5和R 6分别表示氢原子,氟,氯或溴原子或低级烷基。 R 7为氢或氯原子或甲基。 R 8为氢原子或低级烷基。在其中代表二价基团(T)的情况下,R 9是氢或卤素原子或低级烷基,并且R 1 <0>是氢原子或甲基。 <7>是氢,R <3>不能是氯,Z不能是硫。还描述了其制备方法和包含这些化合物的药物。考虑到缺乏抑制胃酸分泌,抑制唾液分泌和散瞳的作用,新型二氮杂one酮适合作为迷走神经起搏器,用于治疗人和兽药中的心动过缓和心律失常。

著录项

  • 公开/公告号IL87433A

    专利类型

  • 公开/公告日1991-12-12

    原文格式PDF

  • 申请/专利权人 DR. KARL THOMAE GMBH;

    申请/专利号IL19880087433

  • 发明设计人

    申请日1988-08-12

  • 分类号C07D401/06;C07D401/14;C07D405/06;C07D405/14;C07D413/06;C07D413/14;C07D417/06;C07D417/14;C07D471/04;C07D487/04;C07D487/14;C07D495/04;C07D495/14;A61K31/55;

  • 国家 IL

  • 入库时间 2022-08-22 05:35:15

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