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    • 9. 发明授权
    • CGRP receptor antagonist
    • CGRP受体拮抗剂
    • US08481546B2
    • 2013-07-09
    • US13038550
    • 2011-03-02
    • Prasad V. ChaturvedulaGene M. DubowchikJohn E. Macor
    • Prasad V. ChaturvedulaGene M. DubowchikJohn E. Macor
    • C07D401/14A61K31/496
    • C07D401/14C07K5/0806
    • 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.
    • 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。