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31. 发明授权

US5688809A 5-heteroarylindole derivatives 失效
标题翻译： 5-杂吲哚衍生物
公开(公告)号：US5688809A
公开(公告)日：1997-11-18
申请号：US687555
申请日：1996-10-07
申请人： John E. Macor
发明人： John E. Macor
IPC分类号： C07D487/04 , A61K31/415 , A61K31/435 , A61K31/505 , A61P25/02 , A61P25/08 , A61P25/20 , A61P25/28 , C07D209/08 , C07D401/12 , C07D403/04 , C07D471/04 , A61K31/44
CPC分类号： C07D403/04 , C07D471/04
摘要： The present invention relates to compounds of the formula ##STR1## The present invention also relates to intermediates for the preparation of compounds of the formula I, pharmaceutical compositions and method of use.
摘要翻译： PCT No.PCT / IB94 / 00407 Sec。 371日期1996年10月7日第 102（e）日期1996年10月7日PCT 1994年12月8日PCT公布。公开号WO95 / 21836 日期：1995年8月17日本发明涉及式I化合物本发明还涉及制备式I化合物，药物组合物和使用方法的中间体。

32. 发明授权

US5594014A Indole derivatives as 5-HT1 agonists 失效
标题翻译：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。

33. 发明授权

US5545644A Indole derivatives 失效
标题翻译：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。

34. 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。

35. 发明申请

US20130096130A1 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).

36. 发明申请

US20120108596A1 Aza-Bicyclic Amine N-Oxide Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligand Pro-Drugs 有权
标题翻译：氮杂双环胺氧化物作为α-7烟碱乙酰胆碱受体配体药物
公开(公告)号：US20120108596A1
公开(公告)日：2012-05-03
申请号：US13097153
申请日：2011-04-29
申请人： Kimberley A. Lentz , Rex Denton , James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Robert A. Mate , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor , Matthew D. Hill , Haiquan Fang
发明人： Kimberley A. Lentz , Rex Denton , James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Robert A. Mate , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor , Matthew D. Hill , Haiquan Fang
IPC分类号： A61K31/4725 , A61P25/18 , A61P25/28 , A61K31/439 , A61K31/498 , A61K31/506 , A61K31/444 , A61K31/497 , C07D498/20 , C07D519/00
CPC分类号： C07D498/10
摘要： The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are prodrugs for ligands, agonists, and partial agonists for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
摘要翻译：本公开内容通常涉及式I化合物，包括其盐，以及使用该化合物的组合物和方法。这些化合物是用于烟碱型α7受体的配体，激动剂和部分激动剂的前药，并且可用于治疗中枢神经系统的各种疾病，特别是情感和神经变性疾病。

37. 发明申请

US20110251223A1 CGRP Receptor Antagonists 有权
标题翻译： 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）。

38. 发明申请

US20100099684A1 Quinuclidine Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands 有权
标题翻译：奎宁环化合物作为α-7烟碱乙酰胆碱受体配体
公开(公告)号：US20100099684A1
公开(公告)日：2010-04-22
申请号：US12607354
申请日：2009-10-28
申请人： James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
发明人： James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
IPC分类号： A61K31/499 , C07D239/12 , C07D241/36 , C07D401/14 , A61K31/498 , A61K31/444 , A61P25/28
CPC分类号： A61K31/506 , A61K31/439 , C07D498/20 , C07D519/00
摘要： The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
摘要翻译：本公开提供式I化合物，包括其盐，以及使用该化合物的组合物和方法。这些化合物是烟碱型α7受体的配体，可用于治疗中枢神经系统的各种疾病，特别是情感和神经退行性疾病。

39. 发明授权

US5578612A Indole derivatives 失效
标题翻译：吲哚衍生物
公开(公告)号：US5578612A
公开(公告)日：1996-11-26
申请号：US469258
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： A61K31/00 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/4045 , A61K31/4427 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61P1/00 , A61P1/08 , A61P3/00 , A61P3/04 , A61P9/00 , A61P9/08 , A61P9/12 , A61P11/00 , A61P17/00 , A61P19/00 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/30 , A61P27/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07D401/06 , C07D403/06
CPC分类号： C07D401/06 , A61K31/40 , C07D403/06
摘要： Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, X and n are as defined in the claims and the pharmaceutically acceptable salts thereof are new. 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, 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 hypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of dihalogenated intermediate is also disclosed.
摘要翻译：其中R 1，R 2，R 3，X和n如权利要求中所定义并且其药学上可接受的盐的式Ⅰ的化合物是新的。这些化合物是有用的精神治疗药物，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性高血压药和血管扩张剂。还公开了通过二卤化中间体的过渡金属催化环化形成吲哚的方法。

40. 发明授权

US5559129A Indole derivatives 失效
公开(公告)号：US5559129A
公开(公告)日：1996-09-24
申请号：US466645
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 , A61K37/40
CPC分类号： A61K31/40 , C07D401/06 , C07D403/06
摘要： Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, X and n are as defined in the claims and the pharmaceutically acceptable salts thereof are new. 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, 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 hypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of dihalogenated intermediate is also disclosed.

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