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1. 发明授权

US07220862B2 Calcitonin gene related peptide receptor antagonists 有权
标题翻译：降钙素基因相关肽受体拮抗剂
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。

2. 发明授权

US07314883B2 Anti-migraine treatments 有权
标题翻译：抗偏头痛治疗
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，

3. 发明授权

US07842808B2 Anti-migraine spirocycles 有权
标题翻译：抗偏头痛螺旋
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。

4. 发明授权

US07569578B2 Heterocyclic anti-migraine agents 有权
标题翻译：杂环类抗偏头痛药
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。

5. 发明授权

US07754732B2 Spirocyclic anti-migraine compounds 有权
标题翻译：螺环抗偏头痛化合物
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。

6. 发明授权

US07470680B2 Constrained compounds as CGRP-receptor antagonists 有权
标题翻译：约束化合物作为CGRP受体拮抗剂
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。

7. 发明申请

US20070259851A1 CONSTRAINED COMPOUNDS AS CGRP-RECEPTOR ANTAGONISTS 有权
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.

8. 发明授权

US08481546B2 CGRP receptor antagonist 有权
标题翻译： 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。

9. 发明申请

US20120059017A1 CGRP Receptor Antagonist 有权
标题翻译： CGRP受体拮抗剂
公开(公告)号：US20120059017A1
公开(公告)日：2012-03-08
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： 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。

10. 发明授权

US07449586B2 Processes for the preparation of CGRP-receptor antagonists and intermediates thereof 有权
标题翻译：制备CGRP受体拮抗剂及其中间体的方法
公开(公告)号：US07449586B2
公开(公告)日：2008-11-11
申请号：US11291670
申请日：2005-12-01
申请人： Prasad V. Chaturvedula , Xiaojan Han , Xiang-Jun J. Jiang
发明人： Prasad V. Chaturvedula , Xiaojan Han , Xiang-Jun J. Jiang
IPC分类号： C07D231/56
CPC分类号： C07D471/04 , C07D231/56 , C07D401/12 , C07D401/14
摘要： The invention relates to novel processes for the preparation of small molecule antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”) and intermediates thereof.
摘要翻译：本发明涉及制备降钙素基因相关肽受体（“CGRP受体”）及其中间体的小分子拮抗剂的新方法。

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