专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

31. 发明申请

WO1993011106A1 INDOLE DERIVATIVES 审中-公开
标题翻译： INDOLE DORIVATIVES
公开(公告)号：WO1993011106A1
公开(公告)日：1993-06-10
申请号：PCT/US1992008306
申请日：1992-10-06
申请人： PFIZER, INC. , MACOR, John, E.
发明人： PFIZER, INC.
IPC分类号： C07D209/16
CPC分类号： C07D401/04 , C07D209/16 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D417/14 , C07D473/34
摘要： Compounds of formula (I) wherein Z is (a) or (b); R1 is (c), (d), (e) or (f); X is O, NH or S; A, B, D, E, and F are each independently C, N, O, or S; R2, R3, R4, R5 and R6 are each independently hydrogen, C1 to C6 alkyl, aryl, C1 to C3 alkyl-aryl, halogen, cyano, nitro, -NR7R8, -(CH2)mOR9, -SR9, -SO2R9, -SO2NR7R8, -NR7SO2R8, -NR7CO2R9, -NR7COR9, -CONR7R8, or -CO2R9; one of R2 and R3, R3 and R4, R4 and R5, or R5 and R6 may be taken together to form a five- to seven-membered alkyl ring, a six-membered aryl ring, a five- to seven-membered heteroalkyl ring having 1 heteroatom of N, O, or S, or a five- or six-membered heteroaryl ring having 1 or 2 heteroatoms of N, O, or S; R7 and R8 are each independently hydrogen, C1 to C6 alkyl, -(CH2)qR10, C1 to C3 alkyl-aryl, aryl, or may be taken together to form a four- to six-membered ring; R9 is hydrogen, C1 to C6 alkyl, C1 to C3 alkyl-aryl, aryl, or -(CH2)wR11; R10 and R11 are each independently -OH, -OR12, -CO2R12, -CONHR12, or cyano; R12 is hydrogen, C1 to C6 alkyl, aryl, or C1 to C6 alkyl-aryl; R13 is hydrogen, -OR14, or -NHCOR14; R14 is C1 to C6 alkyl, or C1 to C3 alkyl-aryl; n is 0, 1, or 2; m is 1, 2, or 3; q is 2, 3, or 4; w is 2, 3, or 4; the above aryl groups and the aryl moieties of the above alkyl-aryl groups are independently phenyl or substituted phenyl, wherein said substituted phenyl may be substituted with one to three of C1 to C4 alkyl, halogen, hydroxy, cyano, carboxamido, nitro, and C1 to C4 alkoxy; and a broken line represents an optional double bond, and the pharmaceutically acceptable salts thereof. These compounds are useful psychotherapeutics and are potent serotonin (5-HT1) 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.
摘要翻译：其中Z为（a）或（b）的式（I）化合物; R1为（c），（d），（e）或（f）; X是O，NH或S; A，B，D，E和F各自独立地为C，N，O或S; R2，R3，R4，R5和R6各自独立地为氢，C1至C6烷基，芳基，C1至C3烷基 - 芳基，卤素，氰基，硝基，-NR7R8 - ，（CH2）mOR9，-SR9，-SO2R9， SO 2 NR 7 R 8，-NR 7 SO 2 R 8，-NR 7 CO 2 R 9，-NR 7 COR 9，-CONR 7 R 8或-CO 2 R 9; R 2和R 3中的一个，R 3和R 4，R 4和R 5或R 5和R 6可以一起形成五元至七元烷基环，六元芳环，五至七元杂烷基环具有1个N，O或S杂原子，或具有1或2个N，O或S杂原子的五元或六元杂芳基环; R 7和R 8各自独立地为氢，C 1至C 6烷基， - （CH 2）q R 10，C 1至C 3烷基 - 芳基，或可一起形成四至六元环; R 9为氢，C 1至C 6烷基，C 1至C 3烷基 - 芳基，或 - （CH 2）w R 11; R 10和R 11各自独立地为-OH，-OR 12，-CO 2 R 12，-CONHR 12或氰基; R 12是氢，C 1至C 6烷基，芳基或C 1至C 6烷基 - 芳基; R 13是氢，-OR 14或-NHCOR 14; R14是C1-C6烷基或C1-C3烷基 - 芳基; n为0,1或2; m为1,2或3; q是2,3或4; w为2,3或4; 上述芳基和上述烷基 - 芳基的芳基部分独立地为苯基或取代的苯基，其中所述取代的苯基可被一至三个C1至C4烷基，卤素，羟基，氰基，甲酰氨基，硝基和 C1至C4烷氧基; 虚线表示任选的双键及其药学上可接受的盐。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作用的抗高血压药和血管扩张剂。

32. 发明申请

WO2011044212A1 MODULATORS OF G PROTEIN-COUPLED RECEPTOR 88 审中-公开
标题翻译： G蛋白偶联受体的调节剂88
公开(公告)号：WO2011044212A1
公开(公告)日：2011-04-14
申请号：PCT/US2010/051597
申请日：2010-10-06
申请人： BRISTOL-MYERS SQUIBB COMPANY , LEXICON PHARMACEUTICALS, INC. , BI, Yingzhi , DZIERBA, Carolyn, Diane , BRONSON, Joanne, J. , FINK, Cynthia , GREEN, Michael , KIMBALL, David , MACOR, John, E. , KWON, Soojin , ZHANG, Yulian , ZIPP, Greg
发明人： BI, Yingzhi , DZIERBA, Carolyn, Diane , BRONSON, Joanne, J. , FINK, Cynthia , GREEN, Michael , KIMBALL, David , MACOR, John, E. , KWON, Soojin , ZHANG, Yulian , ZIPP, Greg
IPC分类号： C07D213/56 , C07D241/12 , A61K31/4418 , A61K31/4965 , A61P3/00 , A61P25/00
CPC分类号： C07D213/56 , C07D241/12
摘要： The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.
摘要翻译：本公开一般涉及可以调节G蛋白偶联受体88的化合物，包含这些化合物的组合物，以及调节G蛋白偶联受体88的方法。

33. 发明申请

WO2011044195A1 MODULATORS OF G PROTEIN-COUPLED RECEPTOR 88 审中-公开
公开(公告)号：WO2011044195A1
公开(公告)日：2011-04-14
申请号：PCT/US2010/051572
申请日：2010-10-06
申请人： BRISTOL-MYERS SQUIBB COMPANY , LEXICON PHARMACEUTICALS, INC. , BI, Yingzhi , DZIERBA, Carolyn, Diane , BRONSON, Joanne, J. , CARSON, Kenneth , CIANCHETTA, Giovanni , DONG, Li , FINK, Cynthia , GREEN, Michael , KIMBALL, David , MACOR, John, E. , KWON, Soojin , WANG, Jiancheng , ZHANG, Yulian , ZIPP, Greg
发明人： BI, Yingzhi , DZIERBA, Carolyn, Diane , BRONSON, Joanne, J. , CARSON, Kenneth , CIANCHETTA, Giovanni , DONG, Li , FINK, Cynthia , GREEN, Michael , KIMBALL, David , MACOR, John, E. , KWON, Soojin , WANG, Jiancheng , ZHANG, Yulian , ZIPP, Greg
IPC分类号： C07D333/24 , A61K31/381 , C07C233/06 , A61P3/00 , A61P25/00
CPC分类号： C07D333/24 , C07C233/60 , C07C2601/02
摘要： The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.

34. 发明申请

WO2009131926A1 QUINUCLIDINE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS 审中-公开
标题翻译：喹啉化合物作为ALPHA-7非丁醇乙酰胆碱受体配体
公开(公告)号：WO2009131926A1
公开(公告)日：2009-10-29
申请号：PCT/US2009/041076
申请日：2009-04-20
申请人： BRISTOL-MYERS SQUIBB COMPANY , COOK II, James, H. , MCDONALD, Ivar, M. , KING, Dalton , OLSON, Richard, E. , WANG, Nenghui , IWUAGWU, Christiana, I. , ZUSI, F., Christopher , MACOR, John, E.
发明人： COOK II, James, H. , MCDONALD, Ivar, M. , KING, Dalton , OLSON, Richard, E. , WANG, Nenghui , IWUAGWU, Christiana, I. , ZUSI, F., Christopher , MACOR, John, E.
IPC分类号： C07D498/20 , A61K31/439 , A61P25/28
CPC分类号： 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 α 7 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α受体的配体，可用于治疗中枢神经系统各种疾病，特别是情感和神经退行性疾病。

35. 发明申请

WO2009009411A1 SUBSTITUTED HETEROCYCLIC ETHERS AND THEIR USE IN CNS DISORDERS 审中-公开
标题翻译：替代性异位症患者及其在CNS疾病中的使用
公开(公告)号：WO2009009411A1
公开(公告)日：2009-01-15
申请号：PCT/US2008/069133
申请日：2008-07-03
申请人： BRISTOL-MYERS SQUIBB COMPANY , DEGNAN, Andrew P. , TORA, George O. , DENHART, Derek J. , VRUDHULA, Vivekananda M. , MACOR, John E. , BRONSON, Joanne J.
发明人： DEGNAN, Andrew P. , TORA, George O. , DENHART, Derek J. , VRUDHULA, Vivekananda M. , MACOR, John E. , BRONSON, Joanne J.
IPC分类号： C07D401/12 , A61K31/33 , A61P25/00
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.
摘要翻译：本发明包括式（I）的化合物，包括药学上可接受的盐，其药物组合物及其在治疗CNS障碍中的用途。

36. 发明申请

WO2005095383A1 HETEROCYCLIC CGRP ANTAGONISTS FOR THE TREATMENT OF MIGRAINE 审中-公开
标题翻译：异位CGRP拮抗剂用于治疗MIGRAINE
公开(公告)号：WO2005095383A1
公开(公告)日：2005-10-13
申请号：PCT/US2005/010330
申请日：2005-03-28
申请人： BRISTOL-MYERS SQUIBB COMPANY , DEGNAN, Andrew P. , HAN, Xiaojun , DUBOWCHIK, Gene M. , MACOR, John E.
发明人： DEGNAN, Andrew P. , HAN, Xiaojun , DUBOWCHIK, Gene M. , MACOR, John E.
IPC分类号： C07D401/14
CPC分类号： C07D401/14
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。

37. 发明申请

WO2004026237A3 COMPOUNDS FOR THE TREATMENT OF PREMATURE EJACULATION 审中-公开
标题翻译：用于治疗预防性呕吐的化合物
公开(公告)号：WO2004026237A3
公开(公告)日：2004-07-01
申请号：PCT/US0329055
申请日：2003-09-15
申请人： SQUIBB BRISTOL MYERS CO , DENHART DEREK JOHN , DITTA JONATHAN L , KING DALTON , MACOR JOHN E , MARCIN LAWRENCE R , MATTSON RONALD J , MENG ZHAOXING
发明人： DENHART DEREK JOHN , DITTA JONATHAN L , KING DALTON , MACOR JOHN E , MARCIN LAWRENCE R , MATTSON RONALD J , MENG ZHAOXING
IPC分类号： A61K20060101 , A61K31/416 , A61K31/4184 , C07D209/14 , C07D403/02
CPC分类号： C07D209/14
摘要： The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds [INSERT CHEMICAL STRUCTURE HERE] (I) useful for the treatment of premature ejaculation, depression, attention deficit hyperactivity disorder, obsessive-compulsive disorder, post-traumatic stress disorder and substance abuse disorders.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐或溶剂合物，以及包含所述化合物的药学上可接受的制剂[用于治疗早泄，抑郁，注意缺陷多动症，强迫症的化学结构（I） - 压力障碍，创伤后应激障碍和药物滥用障碍。

38. 发明申请

WO2004026236A2 CYCLOPENTYL INDOLE DERIVATIVES 审中-公开
标题翻译：环戊基吲哚衍生物
公开(公告)号：WO2004026236A2
公开(公告)日：2004-04-01
申请号：PCT/US2003/028989
申请日：2003-09-15
申请人： BRISTOL-MYERS SQUIBB COMPANY , KING, Dalton , DESKUS, Jeffrey, A. , MACOR, John, E. , MATTSON, Ronald, J. , MENG, Zhaoxing , SLOAN, Charles, P.
发明人： KING, Dalton , DESKUS, Jeffrey, A. , MACOR, John, E. , MATTSON, Ronald, J. , MENG, Zhaoxing , SLOAN, Charles, P.
IPC分类号： A61K
CPC分类号： C07D209/30 , C07D209/42 , C07D403/08
摘要： The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds of Formula (I) useful for the treatment of premature ejaculation, depression, attention deficit hyperactivity disorder, obsessive-compulsive disorder, post-traumatic stress disorder and substance abuse disorders.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐或溶剂化物和包含所述式（I）化合物的药学上可接受的制剂，其用于治疗早泄，抑郁症，注意力不集中多动症，强迫症，创伤后应激障碍和物质滥用障碍。

39. 发明申请

WO0220489A3 QUINOLINE INHIBITORS OF cGMP PHOSPHODIESTERASE 审中-公开
标题翻译： cGMP磷酸二酯的喹啉抑制剂
公开(公告)号：WO0220489A3
公开(公告)日：2002-06-06
申请号：PCT/US0126130
申请日：2001-08-21
申请人： SQUIBB BRISTOL MYERS CO , BI YINGZHI , YU GUIXUE , ROTELLA DAVID P , MACOR JOHN E
发明人： BI YINGZHI , YU GUIXUE , ROTELLA DAVID P , MACOR JOHN E
IPC分类号： A61K31/47 , A61K31/4709 , A61K31/4745 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , A61P1/00 , A61P3/06 , A61P3/10 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/08 , A61P15/00 , A61P15/10 , A61P15/12 , A61P27/06 , A61P27/16 , A61P37/08 , A61P43/00 , C07D215/42 , C07D215/48 , C07D215/54 , C07D401/04 , C07D401/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07D491/06
CPC分类号： C07D405/12 , A61K31/47 , A61K31/4709 , C07D215/42 , C07D215/48 , C07D215/54 , C07D401/04 , C07D401/12 , C07D417/12 , C07D491/10
摘要： Compounds of the formula (1) are useful as inhibitors of cGMP PDE especially Type 5.
摘要翻译：式（1）化合物可用作cGMP PDE抑制剂，特别是5型。

40. 发明申请

WO1995021836A1 5-HETEROARYLINDOLE DERIVATIVES AS BENZODIAZEPINE RECEPTOR SITE AGONISTS AND ANTAGONISTS 审中-公开
标题翻译：作为苯二氮卓类受体位点激动剂和拮抗剂的5-异构体衍生物
公开(公告)号：WO1995021836A1
公开(公告)日：1995-08-17
申请号：PCT/IB1994000407
申请日：1994-12-08
申请人： PFIZER INC. , MACOR, John, E.
发明人： PFIZER INC.
IPC分类号： C07D403/04
CPC分类号： C07D403/04 , C07D471/04
摘要： The present invention relates to compounds of formula (I). The present invention also relates to intermediates for the preparation of compounds of formula (I), pharmaceutical compositions and method of use.
摘要翻译：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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式