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115 条记录 (耗时 0.038 秒)

    Antagonists of calcitonin gene-related peptide
    87.
    发明授权
    Antagonists of calcitonin gene-related peptide 有权
    降钙素基因相关肽的拮抗剂

    公开(公告)号：US06313097B1

    公开(公告)日：2001-11-06

    申请号：US09523472

    申请日：2000-03-10

    申请人： Wolfgang Eberlein ,  Klaus Rudolf ,  Wolfhard Engel ,  Henri Doods ,  Gerhard Hallermayer

    发明人： Wolfgang Eberlein ,  Klaus Rudolf ,  Wolfhard Engel ,  Henri Doods ,  Gerhard Hallermayer

    IPC分类号： A61K31454

    CPC分类号： C07D401/04 ,  A61K38/00 ,  C07D211/58 ,  C07D401/14 ,  C07D471/04 ,  C07K5/06078

    摘要： Compounds of the formula (I) wherein A, R, R1, R2, X1, X2, X3, and Y are as defined herein, and the tautomers and the pharmaceutically acceptable salts thereof, including pharmaceutical compositions containing these compounds, and their use in the selective antagonization of calcitonin gene-related peptide (CGRP) and in the treatment or prophylaxis of migraine or cluster headaches, non-insulin-dependent diabetes mellitus, inflammation, allergic rhinitis, asthma, morphine tolerance, menopausal hot flashes, and diseases characterized by excessive vasodilatation and consequent reduction in blood-flow.

    摘要翻译： 其中A，R，R 1，R 2，X 1，X 2，X 3和Y如本文所定义的式（I）化合物及其互变异构体及其药学上可接受的盐，包括含有这些化合物的药物组合物及其在 降钙素基因相关肽（CGRP）的选择性拮抗和治疗或预防偏头痛或丛集性头痛，非胰岛素依赖型糖尿病，炎症，过敏性鼻炎，哮喘，吗啡耐受，绝经期潮热，以及特征为 过多的血管舒张和血流量的减少。

    Condensed diazepinones and medicaments containing these compounds
    88.
    发明授权
    Condensed diazepinones and medicaments containing these compounds 失效
    浓缩二氮杂酮和含有这些化合物的药物

    公开(公告)号：US5179090A

    公开(公告)日：1993-01-12

    申请号：US779203

    申请日：1991-10-18

    申请人： Klaus Rudolf ,  Wolfhard Engel ,  Wolfgang Eberlein ,  Gunter Trummlitz ,  Gerhard Mihm ,  Henri Doods ,  Norbert Mayer

    发明人： Klaus Rudolf ,  Wolfhard Engel ,  Wolfgang Eberlein ,  Gunter Trummlitz ,  Gerhard Mihm ,  Henri Doods ,  Norbert Mayer

    IPC分类号： C07D487/18 ,  C07D519/00

    CPC分类号： C07D487/18 ,  C07D519/00

    摘要： 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.

    摘要翻译： （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。