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公开(公告)号:US07842808B2
公开(公告)日:2010-11-30
申请号:US11620308
申请日:2007-01-05
申请人: Prasad V. Chaturvedula , Ling Chen , Rita Civiello , Andrew P. Degnan , Gene M. Dubowchik , Xiaojun Han , Xiang Jun J. Jiang , Guanglin Luo , John E. Macor , Graham S. Poindexter , George O. Tora
发明人: Prasad V. Chaturvedula , Ling Chen , Rita Civiello , Andrew P. Degnan , Gene M. Dubowchik , Xiaojun Han , Xiang Jun J. Jiang , Guanglin Luo , John E. Macor , Graham S. Poindexter , George O. Tora
IPC分类号: C07D471/10 , C07D471/20 , C07D471/22 , C07D487/10 , A61K31/4375 , A61P11/00 , A61P11/06 , A61P25/06
CPC分类号: A61K49/0008 , A01K67/0275 , A01K2207/15 , A01K2217/00 , A01K2217/05 , A01K2227/106 , A01K2267/0306 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D473/34 , C07D487/04 , C07D487/14 , C07D491/113 , C07D498/10 , C07D519/00 , C12N15/8509 , G01N33/566 , G01N2500/10 , G01N2800/2807
摘要: The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
摘要翻译: 本发明涉及作为降钙素基因相关肽受体(“CGRP受体”)拮抗剂的式(I)化合物,包含它们的药物组合物,鉴定它们的方法,使用它们的治疗方法及其在治疗治疗中的用途 神经源性血管舒张,神经源性炎症,偏头痛和其他头痛,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和慢性阻塞性肺疾病(COPD)以及其他治疗可以通过 CGRP受体的拮抗作用。
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公开(公告)号:US07569578B2
公开(公告)日:2009-08-04
申请号:US11004706
申请日:2004-12-03
申请人: Guanglin Luo , Ling Chen , Andrew P. Degnan , Gene M. Dubowchik , John E. Macor , George O. Tora , Prasad V. Chaturvedula
发明人: Guanglin Luo , Ling Chen , Andrew P. Degnan , Gene M. Dubowchik , John E. Macor , George O. Tora , Prasad V. Chaturvedula
IPC分类号: A61K31/517 , C07D239/95 , A61K31/497 , C07D403/04
CPC分类号: C07D471/10 , C07D401/14 , C07D413/14
摘要: The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
摘要翻译: 本发明涉及作为降钙素基因相关肽受体(“CGRP受体”)拮抗剂的式(I)化合物,包含它们的药物组合物,鉴定它们的方法,使用它们的治疗方法及其在治疗治疗中的用途 神经源性血管舒张,神经源性炎症,偏头痛和其他头痛,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和慢性阻塞性肺疾病(COPD)以及其他治疗可以通过 CGRP受体的拮抗作用。
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公开(公告)号:US07314883B2
公开(公告)日:2008-01-01
申请号:US11620291
申请日:2007-01-05
申请人: Ling Chen , Prasad V. Chaturvedula , Rita Civiello , Andrew P. Degnan , Gene M. Dubowchik , Xiaojun Han , Xiang Jun J. Jiang , George N. Karageorge , Guanglin Luo , John E. Macor , Graham S. Poindexter , George O. Tora
发明人: Ling Chen , Prasad V. Chaturvedula , Rita Civiello , Andrew P. Degnan , Gene M. Dubowchik , Xiaojun Han , Xiang Jun J. Jiang , George N. Karageorge , Guanglin Luo , John E. Macor , Graham S. Poindexter , George O. Tora
IPC分类号: A61K31/4427 , A61K31/496 , A61K31/517 , A61P11/00 , A61P11/06 , A61P25/06 , C07D487/14 , C07D487/22
CPC分类号: A61K49/0008 , A01K67/0275 , A01K2207/15 , A01K2217/00 , A01K2217/05 , A01K2227/106 , A01K2267/0306 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/10 , C07D487/04 , C07D487/14 , C07D491/10 , C12N15/8509 , G01N33/566 , G01N2500/10 , G01N2800/2807
摘要: The present invention relates to methods of treating neurogenic vasodilation, neurogenic inflammaton, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors using pharmaceutical compositions comprising compounds of Formula (I)
摘要翻译: 本发明涉及治疗神经源性血管舒张,神经源性炎症,偏头痛等头痛,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和慢性阻塞性肺病(COPD)等的治疗方法 使用包含式(I)化合物的药物组合物可以通过CGRP受体的拮抗作用来治疗其,
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公开(公告)号:US07220862B2
公开(公告)日:2007-05-22
申请号:US10729155
申请日:2003-12-05
申请人: Prasad V. Chaturvedula , Ling Chen , Rita Civiello , Andrew P. Degnan , Gene M. Dubowchik , Xiaojun Han , Xiang Jun J. Jiang , George N. Karageorge , Guanglin Luo , John E. Macor , Graham Poindexter , George Tora
发明人: Prasad V. Chaturvedula , Ling Chen , Rita Civiello , Andrew P. Degnan , Gene M. Dubowchik , Xiaojun Han , Xiang Jun J. Jiang , George N. Karageorge , Guanglin Luo , John E. Macor , Graham Poindexter , George Tora
IPC分类号: C07D487/14 , C07D487/22 , A61K31/4427 , A61K31/496 , A61K31/517 , A61P11/00 , A61P11/06 , A61P25/06
CPC分类号: A61K49/0008 , A01K67/0275 , A01K2207/15 , A01K2217/00 , A01K2217/05 , A01K2227/106 , A01K2267/0306 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/10 , C07D487/04 , C07D487/14 , C07D491/10 , C12N15/8509 , G01N33/566 , G01N2500/10 , G01N2800/2807
摘要: The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
摘要翻译: 本发明涉及作为降钙素基因相关肽受体(“CGRP受体”)拮抗剂的式(I)化合物,包含它们的药物组合物,鉴定它们的方法,使用它们的治疗方法及其在治疗治疗中的用途 神经源性血管舒张,神经源性炎症,偏头痛和其他头痛,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和慢性阻塞性肺疾病(COPD)以及其他治疗可以通过 CGRP受体的拮抗作用。
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公开(公告)号:US08481546B2
公开(公告)日:2013-07-09
申请号:US13038550
申请日:2011-03-02
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。
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公开(公告)号:US07470680B2
公开(公告)日:2008-12-30
申请号:US11742626
申请日:2007-05-01
申请人: Prasad V. Chaturvedula , Stephen E. Mercer , Haiquan Fang , Xiaojun Han , Guanglin Luo , Gene M. Dubowchik , Graham S. Poindexter
发明人: Prasad V. Chaturvedula , Stephen E. Mercer , Haiquan Fang , Xiaojun Han , Guanglin Luo , Gene M. Dubowchik , Graham S. Poindexter
IPC分类号: C07D487/04 , C07D401/14 , C07D519/00 , A61K31/55 , A61P25/06
CPC分类号: C07D487/04
摘要: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of 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), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
摘要翻译: 本发明包括受限制的双环和三环CGRP受体拮抗剂,鉴定它们的方法,包含它们的药物组合物及其用于治疗偏头痛和其他头痛,神经源性血管舒张,神经源性炎症,热损伤,循环休克,冲洗的方法 与更年期,气道炎症性疾病如哮喘和慢性阻塞性肺疾病(COPD)相关的其它病症以及其治疗可以通过CGRP受体的拮抗作用来实现。
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公开(公告)号:US20070259851A1
公开(公告)日:2007-11-08
申请号:US11742626
申请日:2007-05-01
申请人: Prasad V. Chaturvedula , Stephen E. Mercer , Haiquan Fang , Xiaojun Han , Guanglin Luo , Gene M. Dubowchik , Graham S. Poindexter
发明人: Prasad V. Chaturvedula , Stephen E. Mercer , Haiquan Fang , Xiaojun Han , Guanglin Luo , Gene M. Dubowchik , Graham S. Poindexter
IPC分类号: A61K31/55 , C07D471/02 , A61K31/519 , A61K31/517 , A61K31/4747 , A61K31/4745 , A61K31/4709 , C07D487/02
CPC分类号: C07D487/04
摘要: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of 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), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
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公开(公告)号:US20120059017A1
公开(公告)日:2012-03-08
申请号:US13038550
申请日:2011-03-02
IPC分类号: A61K31/497 , A61P35/00 , A61P25/06 , C07D401/14 , A61P25/00
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。
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公开(公告)号:US07754732B2
公开(公告)日:2010-07-13
申请号:US11620253
申请日:2007-01-05
申请人: Prasad V. Chaturvedula , Gene M. Dubowchik , Xiang Jun J. Jiang , John E. Macor , Graham S. Poindexter , Shikha Vig
发明人: Prasad V. Chaturvedula , Gene M. Dubowchik , Xiang Jun J. Jiang , John E. Macor , Graham S. Poindexter , Shikha Vig
IPC分类号: C07D487/10 , A61K31/4427 , A61K31/496 , A61K31/517 , A61P11/00 , A61P11/06 , A61P25/06 , C07D487/20
CPC分类号: A61K49/0008 , A01K67/0275 , A01K2207/15 , A01K2217/00 , A01K2217/05 , A01K2227/106 , A01K2267/0306 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/10 , C07D487/04 , C07D487/14 , C07D491/10 , C12N15/8509 , G01N33/566 , G01N2500/10 , G01N2800/2807
摘要: The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
摘要翻译: 本发明涉及作为降钙素基因相关肽受体(“CGRP受体”)拮抗剂的式(I)化合物,包含它们的药物组合物,鉴定它们的方法,使用它们的治疗方法及其在治疗治疗中的用途 神经源性血管舒张,神经源性炎症,偏头痛和其他头痛,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和慢性阻塞性肺疾病(COPD)以及其他治疗可以通过 CGRP受体的拮抗作用。
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公开(公告)号:US07049323B2
公开(公告)日:2006-05-23
申请号:US10813870
申请日:2004-03-30
IPC分类号: C07D401/02 , A61K31/44
CPC分类号: C07K5/06139 , A61K31/397 , A61K31/40 , A61K31/435 , A61K38/00 , C07K5/06191
摘要: Novel azetidinyl and pyrrolidinyl compounds are ligands of melanocortin-4 receptors and are useful for treating conditions responsive to the modulation of melanocortin-4 receptors such as obesity, diabetes, and sexual dysfunction.
摘要翻译: 新的氮杂环丁烷基和吡咯烷基化合物是黑皮质素-4受体的配体,并且可用于治疗对黑皮质素-4受体如肥胖,糖尿病和性功能障碍的调节的反应。
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