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1.发明公开3-AMINOPIPERIDINES AND 3-AMINOQUINUCLIDINES AS INHIBITORS OF MONOAMINE UPTAKE 审中-公开3氨基哌啶和3 aminoquinuclidines AS MONO阿明记录抑制剂
公开(公告)号：EP1638560A1
公开(公告)日：2006-03-29
申请号：EP04751759.4
申请日：2004-05-25
发明人： BEADLE, Christopher, David , CASES-THOMAS, Manuel, Javier , CLARK, Barry, Peter Eli Lilly and Company Limited , GALLAGHER, Peter, Thaddeus , MASTERS, John, Joseph , TIMMS, Graham, Henry Eli Lilly and Company , WALTER, Magnus, Wilhelm , WHATTON, Maria, Ann Eli Lilly and Company Limited , WOOD, Virginia, Ann Eli Lilly and Company Limited , GILMORE, Jeremy Eli Lilly and Company Limited
IPC分类号： A61K31/439 , C07D453/02 , A61K31/4462 , C07D211/56 , C07D405/12
CPC分类号： C07D405/12 , C07D211/56 , C07D453/02
摘要： The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, which are useful for the inhibition of the uptake of one or more physiologically active monoamines (serotonin, norepinephrine, and dopamine).
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公开(公告)号：EP2201002B1
公开(公告)日：2012-03-07
申请号：EP08836911.1
申请日：2008-09-30
IPC分类号： C07D401/14 , C07D403/12 , A61K31/497 , A61P25/00
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14
摘要： The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is C(H)= or -N= and R1-7 are as defined herein.
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3.发明公开(THIENO[2,3-b][1,5]BENZOXAZEPIN-4-YL)PIPERAZIN-1-YL COMPOUNDS AS DUAL ACTIVITY H1 INVERSE AGONISTS/5-HT2A ANTAGONISTS 有权（噻吩并[2,3-B] [1,5]苯并恶嗪-4-基）哌嗪-1-基] - 缬氨酸二氢卟吩连接物H1-反相激动剂/ 5-HT2A-拮抗剂
公开(公告)号：EP2943498A1
公开(公告)日：2015-11-18
申请号：EP14701636.4
申请日：2014-01-08
IPC分类号： C07D498/04 , A61K31/55 , A61P25/00
CPC分类号： C07D498/04
摘要： A dual H1 inverse agonist/5-HT2A receptor antagonist of the formula: [Formula I], its uses, and methods for its preparation are described.
摘要翻译： 描述了下式的双H1逆激动剂/ 5-HT2A受体拮抗剂：[式I]，其用途及其制备方法。
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4.发明授权(THIENO[2,3-B][1,5]BENZOXAZEPIN-4-YL)PIPERAZIN-1-YL COMPOUNDS AS DUAL ACTIVITY H1 INVERSE AGONISTS/5-HT2A ANTAGONISTS 有权（噻吩并[2,3-B] [1,5]苯并氮杂-4-基）哌嗪-1-基化合物作为双重活性H1反向激动剂/ 5-HT2A拮抗剂
公开(公告)号：EP2943498B1
公开(公告)日：2017-09-06
申请号：EP14701636.4
申请日：2014-01-08
IPC分类号： C07D498/04 , A61K31/55 , A61P25/00
CPC分类号： C07D498/04
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5.发明公开SUBSTITUTED [(5H-PYRROLO[2,1-c] [1,4]BENZODIAZEPIN-11-YL)PIPERAZIN-1-YL]-2,2-DIMETHYLPROPANOIC ACID COMPOUNDS AS DUAL ACTIVITY H1 INVERSE AGONISTS/5-HT2A ANTAGONISTS 有权取代的[（5H-吡咯并[2,1-C] [1,4]苯并二氮杂-11-基）哌嗪-1-基] -2,2-二DIMETHYLPROPANSÄUREVERBINDUNGENALS双作用H1-逆激动剂/拮抗剂5-HT2A
公开(公告)号：EP2683719A1
公开(公告)日：2014-01-15
申请号：EP12701824.0
申请日：2012-01-25
发明人： CAMP, Anne, Marie , GALLAGHER, Peter, Thaddeus , SANDERSON, Adam, Jan , LEDGARD, Andrew, James , COATES, David, Andrew
IPC分类号： C07D487/04 , A61K31/5517 , A61P25/20
CPC分类号： C07D487/04
摘要： A dual H1/5-HT
2A receptor antagonist of the formula:, its uses, and methods for its preparation are described.-
6.发明授权2-[4-(PYRAZOL-4-YLALKYL)PIPERAZIN-1-YL]-3-PHENYL PYRAZINES AND PYRIDINES AND 3-[4-(PYRAZOL-4-YLALKYL)PIPERAZIN-1-YL]-2-PHENYL PYRIDINES AS 5-HT7 RECEPTOR ANTAGONISTS 有权2- [4-（吡唑-4-基） - 哌嗪-1-基] -3-苯基]吡啶-3-基] -3- [4-（吡唑-4-基） - 哌嗪-1-基] -2 - [ - 苯基 - 吡啶ALS 5-HT7-REZEPTORANTAGONISTEN
公开(公告)号：EP2155717B1
公开(公告)日：2012-10-24
申请号：EP08747748.5
申请日：2008-05-07
发明人： BADESCU, Valentina, O. , CAMP, Anne, Marie , CLARK, Barry, Peter , COHEN, Michael, Philip , FILLA, Sandra, Ann , GALLAGHER, Peter, Thaddeus , HELLMAN, Sarah, Lynne , MAZANETZ, Michael, Philip , PINEIRO-NUNEZ, Marta, Maria , SCHAUS, John, Mehnert , SPINAZZE, Patrick, Gianpietro , WHATTON, Maria, Ann
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/14 , C07D417/14 , A61K31/497 , A61P25/00
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
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7.发明公开3-ARYLOXY/THIO-2,3-SUBSTITUTED PROPANAMINES AND THEIR USE IN INHIBITING SEROTONIN AND NOREPINEPHRINE REUPTAKE 审中-公开3-芳氧基/ THIO-2,3-取代丙烷胺和它们的使用抑制血清素和去甲肾上腺素的回收
公开(公告)号：EP1587781A1
公开(公告)日：2005-10-26
申请号：EP03777543.4
申请日：2003-10-24
发明人： BOULET, Serge, Louis , FILLA, Sandra, Ann , GALLAGHER, Peter, Thaddeus , HUDZIAK, Kevin, John , JOHANSSON, Anette, Margareta , KARANJAWALA, Rushad, E. , MASTERS, John, Joseph , MATASSA, Victor , MATHES, Brian, Michael , RATHMELL, Richard, Edmund , WHATTON, Maria, Ann , WOLFE, Chad, Nolan
IPC分类号： C07C217/62 , C07C217/64 , C07C323/32 , C07D275/04 , C07D307/86 , C07D333/54 , C07D333/56 , A61K31/381 , A61K31/137 , A61K31/343 , A61K31/425 , A61P25/06 , A61P25/18 , A61P25/24
CPC分类号： C07D275/04 , C07C217/16 , C07C217/30 , C07C217/48 , C07C323/32 , C07D307/86 , C07D333/54 , C07D333/62 , C07D475/04
摘要： There is provided a compound of formula (I) wherein A is selected from -O- and -S-; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n- where n is 0, 1 or 2, -CF3, -CN and -CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n- where n is 0, 1 or 2, nitro, acetyl, -CF3, -SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1-C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereofwith the proviso that when Y is optionally substituted phenyl or optionally substituted 1,3-benzodioxolyl and Z is OR3 and X is optionally substituted phenyl then A is -S-.
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8.发明授权SUBSTITUTED [(5H-PYRROLO[2,1-c] [1,4]BENZODIAZEPIN-11-YL)PIPERAZIN-1-YL]-2,2-DIMETHYLPROPANOIC ACID COMPOUNDS AS DUAL ACTIVITY H1 INVERSE AGONISTS/5-HT2A ANTAGONISTS 有权取代的[（5H-吡咯并[2,1-C] [1,4]苯并二氮杂-11-基）哌嗪-1-基] -2,2-二DIMETHYLPROPANSÄUREVERBINDUNGENALS双作用H1-逆激动剂/拮抗剂5-HT2A
公开(公告)号：EP2683719B1
公开(公告)日：2015-03-18
申请号：EP12701824.0
申请日：2012-01-25
发明人： CAMP, Anne, Marie , GALLAGHER, Peter, Thaddeus , SANDERSON, Adam, Jan , LEDGARD, Andrew, James , COATES, David, Andrew
IPC分类号： C07D487/04 , A61K31/5517 , A61P25/20
CPC分类号： C07D487/04
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公开(公告)号：EP2201002A1
公开(公告)日：2010-06-30
申请号：EP08836911.1
申请日：2008-09-30
IPC分类号： C07D401/14 , C07D403/12 , A61K31/497 , A61P25/00
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14
摘要： The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is C(H)= or -N= and R1-7 are as defined herein.
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10.发明授权4-AMINO-PIPERIDINE DERIVATIVES AS MONOAMINE UPTAKE INHIBITORS 有权4- AMINOPIPERIDINDERIVATE AS MONO AMIN记录抑制剂
公开(公告)号：EP1735302B1
公开(公告)日：2010-06-16
申请号：EP05722890.0
申请日：2005-02-11
发明人： BOULET, Serge, Louis , CLARK, Barry, Peter , FAIRHURST, John , GALLAGHER, Peter, Thaddeus , JOHANSSON, Anette, Margareta , WHATTON, Maria, Ann , WOOD, Virginia, Ann
IPC分类号： C07D409/12 , C07D405/12 , C07D401/12 , C07D417/12 , C07D513/04 , A61K31/435 , A61P25/00
CPC分类号： C07D513/04 , A61K31/454 , A61K31/4545 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention provides compounds of formula (I) where n, R1, R2, R3, R4, R5 and Heteroaryl are defined herein. The compounds are inhibitors of the uptake of one or more monoamines selected from serotonin, norepinephrine and dopamine and, as such, may be useful in the treatment of disorders of the central and/or peripheral nervous system.
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