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41. 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).

42. 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）。

43. 发明授权

US08026257B2 Substituted heterocyclic ethers and their use in CNS disorders 有权
公开(公告)号：US08026257B2
公开(公告)日：2011-09-27
申请号：US12165967
申请日：2008-07-01
申请人： Andrew P. Degnan , George O. Tora , Derek J. Denhart , Vivekananda M. Vrudhula , John E. Macor , Joanne J. Bronson
发明人： Andrew P. Degnan , George O. Tora , Derek J. Denhart , Vivekananda M. Vrudhula , John E. Macor , Joanne J. Bronson
IPC分类号： C07D413/14 , C07D401/12 , A61K31/5377 , A61K31/4439
CPC分类号： C07D401/12
摘要： The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.

44. 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。

45. 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。

46. 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.

47. 发明授权

US5498626A Acylaminoindole derivatives as 5-ht1 agonists 失效
标题翻译：酰基氨基吲哚衍生物作为5-ht1激动剂
公开(公告)号：US5498626A
公开(公告)日：1996-03-12
申请号：US295792
申请日：1994-09-14
申请人： John E. Macor
发明人： John E. Macor
IPC分类号： A61K31/40 , A61K31/395 , A61K31/404 , A61K31/4427 , A61K31/445 , A61P3/04 , A61P9/12 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/20 , A61P25/24 , A61P25/26 , C07D401/06 , C07D403/06 , C07D403/14
CPC分类号： C07D403/06 , C07D403/14
摘要： ##STR1## Compounds of formula (I) where n is 0, 1, or 2; m is 0 or 1; Y and W are each an amino acid residue; R
1 is hydrogen, C
1 -C
6 alkyl, C
3 -C
6 alkenyl, C
3 -C
6 alkynyl, aryl, C
1 -C
3 alkylaryl, or C
1 -C
3 alkylheteroaryl, and --(CH
2 )
p R
3 ; R
2 is CF
3 , C
1 -C
6 alkyl, aryl, C
1 -C
3 alkylaryl, and --OR
5 ; R
3 is cyano, trifluoromethyl, or --OR
4 ; R
4 is hydrogen, C
1 -C
6 alkyl, C
1 -C
3 alkylaryl, or aryl; R
5 is C
1 -C
6 alkyl, C
1 -C
3 alkylaryl, or aryl; R
6 is hydrogen, --OR
7 , or --NHCOR
7 ; R
7 is hydrogen, C
1 to C
6 alkyl, aryl or C
1 to C
3 alkyl-aryl; p is 1, 2, or 3; and the above aryl groups and the aryl moieties of the above alkyl-aryl groups are independently selected from phenyl and substituted phenyl, wherein said substituted phenyl may be substituted with one to three groups selected from C
1 to C
4 alkyl, halogen, hydroxy, cyano, carboxamide, nitro, and C
1 to C
4 alkoxy and the pharmaceutically acceptable salts thereof. These compounds are useful in treating migraine and other disorders. These compound are useful psychotherapeutics and are potent serotonin (5-HT
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 / 01807 Sec。 371日期：1994年9月14日 102（e）1994年9月14日PCT 1993年3月4日PCT公布。出版物WO93 / 21180 PCT （I）其中n为0,1或2的式（I）化合物; m为0或1; Y和W各自为氨基酸残基; R 1是氢，C 1 -C 6烷基，C 3 -C 6烯基，C 3 -C 6炔基，芳基，C 1 -C 3烷基芳基或C 1 -C 3烷基杂芳基，和 - （CH 2）p R 3; R2是CF3，C1-C6烷基，芳基，C1-C3烷基芳基和-OR5; R3是氰基，三氟甲基或-OR4; R4是氢，C1-C6烷基，C1-C3烷基芳基或芳基; R5是C1-C6烷基，C1-C3烷基芳基或芳基; R6是氢，-OR7或-NHCOR7; R 7为氢，C 1至C 6烷基，芳基或C 1至C 3烷基 - 芳基; p为1,2或3; 并且上述芳基和上述烷基 - 芳基的芳基部分独立地选自苯基和取代的苯基，其中所述取代的苯基可以被一至三个选自C 1 -C 4烷基，卤素，羟基，氰基，甲酰胺，硝基和C1至C4烷氧基及其药学上可接受的盐。这些化合物可用于治疗偏头痛和其他疾病。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，疼痛和慢性阵发性血尿素和头痛相关血管疾病和由血清素能神经传递缺陷引起的其他疾病。该化合物也可用作中枢作用的抗高血压药和血管扩张剂。

48. 发明申请

US20120028994A1 COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION 有权
标题翻译：用于还原β-淀粉样生成的化合物
公开(公告)号：US20120028994A1
公开(公告)日：2012-02-02
申请号：US13013373
申请日：2011-01-25
申请人： Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
发明人： Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
IPC分类号： A61K31/517 , C07D401/14 , A61P35/00 , A61P25/28 , A61P25/00 , A61P27/02 , C07D403/12 , C07D401/12
CPC分类号： A61K31/517 , A61K31/519 , A61K31/5377 , C07D239/70 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D407/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D491/052 , C07D491/08 , C07D491/107 , C07D491/113
摘要： The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
摘要翻译：本公开提供了一系列式（I）的化合物，其调节和淀粉样蛋白肽（＆bgr; -AP）产生，并且可用于治疗阿尔茨海默氏病和其它受β-淀粉状蛋白肽（＆bgr; -AP）生产。

49. 发明申请

US20110124662A1 Substituted Carbamate Derivatives as Modulators of Corticotropin-Releasing Factor Receptor Activity 有权
标题翻译：取代氨基甲酸酯衍生物作为促肾上腺皮质激素释放因子受体活性的调节剂
公开(公告)号：US20110124662A1
公开(公告)日：2011-05-26
申请号：US13055885
申请日：2009-07-29
申请人： Richard A. Hartz , Vijay T. Ahuja , John E. Macor
发明人： Richard A. Hartz , Vijay T. Ahuja , John E. Macor
IPC分类号： A61K31/497 , C07D401/14 , C07D401/12 , A61P25/22 , A61P25/24
CPC分类号： C07D241/22 , C07D401/12 , C07D401/14
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 CRF receptor antagonists and may be useful for treating disorders associated with abnormal CRF levels or aberrant functioning of CRF receptors.
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。化合物是CRF受体拮抗剂，可用于治疗与CRF异常异常或CRF受体异常功能相关的疾病。

50. 发明授权

US07601751B2 Indole acetic acid acyl guanidines as β-secretase inhibitors 有权
标题翻译：吲哚乙酸酰基胍作为β-分泌酶抑制剂
公开(公告)号：US07601751B2
公开(公告)日：2009-10-13
申请号：US11508481
申请日：2006-08-23
申请人： Lorin A. Thompson, III , Jianliang Shi , F. Christopher Zusi , Michael F. Dee , John E. Macor
发明人： Lorin A. Thompson, III , Jianliang Shi , F. Christopher Zusi , Michael F. Dee , John E. Macor
IPC分类号： A61K31/404 , A61K31/5377 , C07D209/04 , C07D413/12 , C07D241/04
CPC分类号： C07D209/18
摘要： There is provided a series of substituted acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, and R8 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
摘要翻译：提供一系列式（I）的取代酰基胍或立体异构体; 或其药学上可接受的盐，其中如本文所定义的R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8，其药物组合物和使用方法。这些化合物通过β-分泌酶抑制淀粉样蛋白前体蛋白（APP）的加工，更具体地抑制Aβ-肽的产生。本公开涉及可用于治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物，例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。

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