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91 条记录 (耗时 0.062 秒)

    Indole derivatives as 5-HT1 agonists
    35.
    发明授权
    Indole derivatives as 5-HT1 agonists 失效
    吲哚衍生物作为5-HT1激动剂

    公开(公告)号：US5594014A

    公开(公告)日：1997-01-14

    申请号：US284662

    申请日：1994-08-19

    申请人： John E. Macor ,  Jolanta T. Nowakowski

    发明人： John E. Macor ,  Jolanta T. Nowakowski

    IPC分类号： A61K31/40 ,  A61K31/404 ,  A61K31/42 ,  A61K31/425 ,  A61P1/00 ,  A61P3/04 ,  A61P9/12 ,  A61P25/04 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D207/20 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

    CPC分类号： C07D413/14 ,  C07D417/14

    摘要： Compounds of the formula (I) where A represents a direct bond, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkenyl; n is 0, 1, or 2; W, X, Y, and Z are each independently oxygen, sulfur, nitrogen or carbon, provided that at least one of W, X, Y, or Z is nitrogen. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain and chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.

    摘要翻译： PCT No.PCT / US93 / 01667 Sec。 371日期：1994年8月19日 102（e）日期1994年8月19日PCT 1993年3月3日PCT公布。 出版物WO93 / 18032 （I）其中A表示直接键的式（I）化合物，C 1 -C 4烷基或C 1 -C 4烯基; n为0,1或2; W，X，Y和Z各自独立地为氧，硫，氮或碳，条件是W，X，Y或Z中的至少一个为氮。 这些化合物是有用的精神治疗药物，是有效的血清素（5-HT1）激动剂，可用于治疗抑郁症，焦虑症，进食障碍，肥胖症，药物滥用，丛集性头痛，偏头痛，疼痛和慢性阵发性血尿素和与血管相关的头痛 疾病，以及其它由缺乏血清素能神经传递引起的疾病。 该化合物也可用作中枢作用的抗高血压药和血管扩张剂。

    Indole derivatives
    36.
    发明授权
    Indole derivatives 失效
    吲哚衍生物

    公开(公告)号：US5545644A

    公开(公告)日：1996-08-13

    申请号：US466644

    申请日：1995-06-06

    申请人： John E. Macor ,  Martin J. Wythes

    发明人： John E. Macor ,  Martin J. Wythes

    IPC分类号： A61K31/40 ,  C07D401/06 ,  C07D403/06

    CPC分类号： C07D401/06 ,  A61K31/40 ,  C07D403/06

    摘要： Compounds of the formula ##STR1## wherein n is 0, 1, or 2; X is hydrogen, chlorine, bromine or iodine; R.sub.1 is hydrogen; R.sub.3 is selected from hydrogen and C.sub.1 to C.sub.6 linear or branched alkyl; and R.sub.2 is as defined in the specification and the pharmaceutically acceptable salts thereof are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of a dihalogenated intermediate is also disclosed.

    摘要翻译： 式（Ⅰ）化合物其中n为0,1或2; X是氢，氯，溴或碘; R1是氢; R3选自氢和C1至C6直链或支链烷基; 和R2如说明书中所定义，其药学上可接受的盐是有用的精神治疗药物，并且是有效的5-羟色胺（5-HT1）激动剂，可用于治疗抑郁症，焦虑症，进食障碍，肥胖症，药物滥用，丛集性头痛， 偏头痛，疼痛，慢性阵发性高血压和与血管疾病相关的头痛，以及由血清素能神经传递缺陷引起的其他障碍。 该化合物也可用作中枢作用的抗高血压药和血管扩张剂。 还公开了通过二卤代中间体的过渡金属催化环化形成吲哚的方法。

    CGRP receptor antagonist
    37.
    发明授权
    CGRP receptor antagonist 有权
    CGRP受体拮抗剂

    公开(公告)号：US08481546B2

    公开(公告)日：2013-07-09

    申请号：US13038550

    申请日：2011-03-02

    申请人： Prasad V. Chaturvedula ,  Gene M. Dubowchik ,  John E. Macor

    发明人： Prasad V. Chaturvedula ,  Gene M. Dubowchik ,  John E. Macor

    IPC分类号： C07D401/14 ,  A61K31/496

    CPC分类号： C07D401/14 ,  C07K5/0806

    摘要： The disclosure generally relates to the compound of formula I, (R)—N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)piperazin-1-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide, including pharmaceutically acceptable salts, which is a CGRP-receptor antagonist. The disclosure also relates to pharmaceutical compositions and methods for using the compound in the treatment of CGRP related disorders including migraine headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, chronic obstructive pulmonary disease (COPD), and cancer.

    摘要翻译： 本发明一般涉及式I化合物，（R）-N-（3-（7-甲基-1H-吲唑-5-基）-1-（4-（1-甲基哌啶-4-基）哌嗪-1-基） 哌啶-1-基）-1-氧代丙-2-基）-4-（2-氧代-1,2-二氢喹啉-3-基）哌啶-1-甲酰胺，包括药学上可接受的盐，其是CGRP-受体拮抗剂。 本公开还涉及用于治疗CGRP相关疾病的药物组合物和方法，包括偏头痛，神经源性血管舒张，神经源性炎症，热损伤，循环休克，与绝经相关的潮红，气道炎症性疾病如哮喘，慢性阻塞性 肺部疾病（COPD）和癌症。

    CGRP Receptor Antagonists
    38.
    发明申请
    CGRP Receptor Antagonists 有权

    公开(公告)号：US20130096130A1

    公开(公告)日：2013-04-18

    申请号：US13439096

    申请日：2012-04-04

    申请人： Guanglin Luo ,  Gene M. Dubowchik ,  John E. Macor ,  Ling Chen

    发明人： Guanglin Luo ,  Gene M. Dubowchik ,  John E. Macor ,  Ling Chen

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： The disclosure generally relates to the novel compounds of formula I, including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).

    CGRP Receptor Antagonists
    39.
    发明申请
    CGRP Receptor Antagonists 有权
    CGRP受体拮抗剂

    公开(公告)号：US20110251223A1

    公开(公告)日：2011-10-13

    申请号：US12902714

    申请日：2010-10-12

    申请人： Guanglin Luo ,  Gene M. Dubowchik ,  John E. Macor

    发明人： Guanglin Luo ,  Gene M. Dubowchik ,  John E. Macor

    IPC分类号： A61K31/437 ,  C07D471/10 ,  A61P25/06 ,  C07D471/04

    CPC分类号： C07D401/12 ,  C07D471/04 ,  C07D471/10 ,  C07D471/20

    摘要： The disclosure generally relates to the novel compounds of formula I, including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).

    摘要翻译： 本公开内容通常涉及式I的新化合物，其包括药学上可接受的盐，其为CGRP受体拮抗剂。 本公开还涉及用于治疗CGRP相关疾病（包括偏头痛和其他头痛，神经源性血管舒张，神经源性炎症，热损伤，循环休克，与更年期相关的潮红，气道炎症性疾病如哮喘）的药物组合物和方法， 和慢性阻塞性肺疾病（COPD）。