Use of diazepinones for treating disorders of the microcirculation
    43.
    发明授权
    Use of diazepinones for treating disorders of the microcirculation 失效
    二氮嗪酮用于治疗微循环障碍的用途

    公开(公告)号:US5001122A

    公开(公告)日:1991-03-19

    申请号:US353262

    申请日:1989-05-17

    CPC分类号: A61K31/55 Y10S514/921

    摘要: A method for treating shock in a patient, which comprises administering to the patient a therapeutically effective amount of a diazepinone of the general formula: ##STR1## wherein A represents a 5,11-dihydro-6H-pyrido[2,3-b] [1,4] benzodiazepin-6-one group bound in the 11-position; a 5,10-dihydro-11H-dibenzo [b,e] [1,4] diazepin-11-one group bound in the 5-position; a 5,11-dihydro-10H-pyrido [3-2b] [1-4] benzodiazepin-10-one group bound in the 5-position; a 4,9-dihydro-10H-thieno [3,4-b] [1,5] benzodiazpin-10-one group bound in the 4-position, unsubstituted or substituted at the 1- or 3-position or both in the 1- and 3-position by an alkyl group having from 1 to 4 carbon atoms, or in the 3-positionby chlorine, fluorine or bromine; a 6-11-dihydro-5H-pyrido [2,3-b] [1,5] benzodiazepin-5-one group bound in the 11-position; or a 1-methyl-1,4,9,10-tetrahydropyrrolo-[3,2-b] [1,5] benzodiazepin-10-one group bound in the 4-position, unsubstituted or substituted at the 3-position by methyl or methyl or chlorine;R.sub.1 represents a hydrogen atom or an alkyl group having from 1 to 3 carbon atoms;R.sub.2 represents an alkyl group having from 1 to 3 carbon atoms; andn and m each represent an integer from 1 to 3.

    摘要翻译: 一种治疗患者休克的方法,其包括向患者施用治疗有效量的通式如下的二氮杂酮:其中A代表5,11-二氢-6H-吡啶并[2,3-b] 结合在11位的[1,4]苯并二氮杂- 5位结合的5,10-二氢-11H-二苯并[b,e] [1,4]二氮杂-11-酮基; 5位结合的5,11-二氢-10H-吡啶并[3-2b] [1-4]苯并二氮杂-10-酮基; 在4-位上结合的未取代或取代的4,9-二氢-10H-噻吩并[3,4-b] [1,5]苯并二氮杂基-10-酮基或在 通过具有1至4个碳原子的烷基或3-,3-位上的氯,氟或溴取代1-和3-位; 在11位结合的6-11-二氢-5H-吡啶并[2,3-b] [1,5]苯并二氮杂-5-基; 或在4-位上结合的1-甲基-1,4,9,10-四氢吡咯并[3,2-b] [1,5]苯并二氮杂-10-酮基,其未被取代或在3位被 甲基或甲基或氯; R1表示氢原子或具有1至3个碳原子的烷基; R2表示具有1至3个碳原子的烷基; n和m各自表示1〜3的整数。

    Antagonists of calcitonin gene-related peptide
    50.
    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

    IPC分类号: A61K31454

    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。