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1.发明授权SUBSTITUTED (4-AMINOCYCLOHEXEN-1-YL)PHENYL AND (4-AMINOCYCLOHEXEN-1-YL)PYRIDINYL COMPOUNDS AS 5-HT1F AGONISTS 有权取代基（4-氨基环戊烯-1-基）苯基和（4-氨基环己烷-1-基）吡啶基缬氨二醛5-HT1F AGONISTEN
公开(公告)号：EP1697305B1
公开(公告)日：2007-08-15
申请号：EP04816953.6
申请日：2004-12-06
IPC分类号： C07C233/80 , C07D213/75 , A61K31/165 , A61K31/44 , A61P25/06
CPC分类号： C07D213/73 , C07C233/80 , C07C2601/16 , C07C2601/18 , C07D213/61 , C07D213/75
摘要： The present invention relates to compounds of formula (I) or a pharmaceutically acceptable acid addition salt thereof, where; X is -C(R4)= or -N=; Ar is phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R1 and R2 are independantly hydrogen or C1-C3 alkyl; R3 is hydrogen, fluoro, or methyl; when X is -C(R4)=, R4 is hydrogen, fluoro, or methyl, provided that no more than one of R3 and R4 may be other than hydrogen; and R5 is hydrogen, methyl, or ethyl. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting dural protein extravasation, and for the treatment or prevention of migraine in a mammal.
摘要翻译： 本发明涉及式I化合物或其药学上可接受的酸加成盐，其中： X是-C（R 4） - 或-N-; Ar是苯基，取代的苯基，杂环或取代的杂环; R 1和R 2独立地是氢或C 1 -C 3烷基; R 3是氢，氟或甲基; 当X是-C（R 4） - ）时，R 4是氢，氟或甲基，条件是R 3不超过一个 >和R 4可以不同于氢; R 5是氢，甲基或乙基。 本发明的化合物可用于活化5-HT 1F受体，抑制硬脑膜蛋白质外渗，以及治疗或预防哺乳动物偏头痛。
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2.发明公开SUBSTITUTED (4-AMINOCYCLOHEXEN-1-YL)PHENYL AND (4-AMINOCYCLOHEXEN-1-YL)PYRIDINYL COMPOUNDS AS 5-HT1F AGONISTS 有权取代的（4- AMINOCYCLOHEXEN -1-基）苯基和（4- AMINOCYCLOHEXEN -1-基）吡啶基化合物作为5-HT1F激动剂
公开(公告)号：EP1697305A1
公开(公告)日：2006-09-06
申请号：EP04816953.6
申请日：2004-12-06
IPC分类号： C07C233/80 , C07D213/75 , A61K31/165 , A61K31/44 , A61P25/06
CPC分类号： C07D213/73 , C07C233/80 , C07C2601/16 , C07C2601/18 , C07D213/61 , C07D213/75
摘要： The present invention relates to compounds of formula (I) or a pharmaceutically acceptable acid addition salt thereof, where; X is -C(R4)= or -N=; Ar is phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R1 and R2 are independantly hydrogen or C1-C3 alkyl; R3 is hydrogen, fluoro, or methyl; when X is -C(R4)=, R4 is hydrogen, fluoro, or methyl, provided that no more than one of R3 and R4 may be other than hydrogen; and R5 is hydrogen, methyl, or ethyl. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting dural protein extravasation, and for the treatment or prevention of migraine in a mammal.
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公开(公告)号：EP2318375A1
公开(公告)日：2011-05-11
申请号：EP09790351.2
申请日：2009-07-14
发明人： KHILEVICH, Albert , LIU, Bin , MAYHUGH, Daniel, Ray , SCHKERYANTZ, Jeffrey, Michael , ZHANG, Deyi
IPC分类号： C07D233/92 , A61K31/4164 , A61P25/00
CPC分类号： C07D233/92
摘要： The present invention provides certain imidazole carboxamide derivatives, pharmaceutical compositions thereof, methods of using the same for preparing a medicament useful in the treatment of conditions associated with the mGluR
2 receptor, such as depression and anxiety, and processes of the following Formula (I) for preparing the same.摘要翻译： 本发明提供某些咪唑甲酰胺衍生物，其药物组合物，其用于制备可用于治疗与mGluR 2受体相关的病症（例如抑郁和焦虑）的药物的方法，以及下式（I）的方法： 为了准备它。
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4.发明公开6-SUBSTITUTED 2,3,4,5-TETRAHYDRO-1H-BENZO [D]AZEPINES AS 5-HT2C RECEPTOR AGONISTS 有权6-取代的-2,3,4,5-四氢-1H-苯并[d]氮杂作为对5-HT2C受体激动剂
公开(公告)号：EP1720836A1
公开(公告)日：2006-11-15
申请号：EP05723397.5
申请日：2005-02-18
发明人： ALLEN, John, Gordon , BRINER, Karin , COHEN, Michael, Philip , GALKA, Christopher, Stanley , HELLMAN, Sarah, Lynne , MARTINEZ-GRAU, Maria Angeles , REINHARD, Matthew, Robert , RODRIGUEZ, Michael, John , ROTHHAAR, Roger, Ryan , TIDWELL, Michael, Wade , VICTOR, Frantz , WILLIAMS, Andrew Caerwyn , ZHANG, Deyi , BOYD, Steven, Armen , CONWAY, Richard, Gerard , DEO, Arundhati, S. , LEE, Wai-Man , SIEDEM, Christopher, Stephen , SINGH, Ajay ,
IPC分类号： C07D223/16 , C07D401/12 , C07D417/12 , C07D413/12 , C07D403/12 , C07D409/12 , C07D405/12 , C07D413/14 , C07D417/06 , C07D403/06 , A61K31/55 , A61P25/22 , A61P25/24 , A61P25/30 , A61P3/04
CPC分类号： C07D223/16 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12
摘要： The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT 2C receptor agonists for the treatment of 5-HT 2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where: R 6 is -S-L-R 15 and other substituents are as defined in the specification.
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公开(公告)号：EP1492786B1
公开(公告)日：2006-10-04
申请号：EP03721402.0
申请日：2003-03-27
发明人： COHEN, Michael Philip , KOHLMAN, Daniel Timothy , LIANG, Sidney Xi , MANCUSO, Vincent , VICTOR, Frantz , XU, Yao-Chang , YING, Bai-Ping , ZACHERL, DeAnna, Piatt , ZHANG, Deyi
IPC分类号： C07D401/06 , C07D409/14 , C07D401/14 , A61K31/44 , A61P25/06
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to compounds of formula I:or pharmaceutically acceptable acid addition salts thereof, where;R1 is C1-C6 alkyl, substituted C1-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C3 alkyl, substituted C3-C7 cycloalkyl-C1-C3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle;R2 is hydrogen, C1-C3 alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II II;R3 is hydrogen or C1-C3 alkyl; R4 is hydrogen, halo, or C1-C3 alkyl;R5 is hydrogen or C1-C3 alkyl; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.
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6.发明公开6-N-LINKED HETEROCYCLE-SUBSTITUTED 2,3,4,5-TETRAHYDRO-1H-BENZO[d]AZEPINES AS 5-HT2C RECEPTOR AGONISTS 有权6-N连接的杂环基取代的2,3,4,5-四氢-1H-苯并[d]氮杂作为5-HT2C受体激动剂
公开(公告)号：EP1924578A2
公开(公告)日：2008-05-28
申请号：EP06802905.7
申请日：2006-09-01
发明人： BRINER, Karin , CAMP, Anne, Marie , CORNELL, Alan , MAZANETZ, Michael, Philip Eli Lilly and Company Limited , ROTHHAAR, Roger, Ryan , VICTOR, Frantz , WILLIAMS, Andrew, Caerwyn , ZHANG, Deyi
IPC分类号： C07D403/04 , C07D405/14 , C07D409/14 , C07D223/16 , C07D401/14 , A61K31/55 , A61P25/24
CPC分类号： C07D403/04 , C07D223/16 , C07D401/14 , C07D405/14 , C07D409/14
摘要： The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H- benzo[d]azepines of Formula I as selective 5-HT2C receptor agonists for the treatment of 5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: Formula (I) where: R6 is selected from the group consisting of (a, b, c, d, e) and other substituents are as defined in the specification.
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7.发明公开SUBSTITUTED 2-CARBONYLAMINO-6-PIPERIDINAMINOPYRIDINES AND SUBSTITUTED 1-CARBONYLAMINO-3-PIPERIDINAMINOBENZENES AS 5-HT1F AGONISTS 有权作为5-HT1F激动剂的取代的2-羰基氨基-6-哌啶氨基吡啶和取代的1-羰基氨基-3-哌啶子基氨基苯甲酸
公开(公告)号：EP1663971A1
公开(公告)日：2006-06-07
申请号：EP04780442.2
申请日：2004-09-03
发明人： BLANCO-PILLADO, Maria-Jesus , COHEN, Michael, Philip , FILLA, Sandra, Ann , HUDZIAK, Kevin, John , KOHLMAN, Daniel, Timothy , BENESH, Dana, Rae , VICTOR, Frantz , XU, Yao-Chang , YING, Bai-Ping , ZACHERL, DeAnna, Piatt , ZHANG, Deyi
IPC分类号： C07D211/58 , C07D401/14 , C07D401/12 , C07D401/06 , A61K31/444 , A61K31/4436 , A61K31/4439 , A61K31/4409
CPC分类号： C07D211/58 , A61K31/4468 , A61K31/4523 , C04B35/632 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14
摘要： ABSTRACT The present invention relates to compounds of formula I: (I) or a pharmaceutically acceptable acid addition salt thereof, where; X is C(R3c= or N=; R1 is C2-C6 alkyl, substituted C2-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 n-alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II (II) provided that when R1 is C2-C6 alkyl or substituted C2-C6 alkyl, R2 is hydrogen or methyl; R3a, R3b, and, when X is C(R3c)=, R3c, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R3a, R3b, and R3c may be other than hydrogen; R4 is hydrogen or C1-C3 alkyl; R5 is hydrogen, C1-C3 alkyl, or C3-C6 cycloalkylcarbonyl, provided that when R3a is other than hydrogen, R5 is hydrogen; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal.
摘要翻译： 摘要本发明涉及式I的化合物：（I）或其药学上可接受的酸加成盐，其中： X是C（R 3c =或N =; R 1是C 2 -C 6烷基，取代的C 2 -C 6烷基，C 3 -C 7环烷基，取代的C 3 -C 7环烷基，苯基，取代的苯基，杂环或取代的杂环; R 2是氢， C3烷基，C3-C6环烷基-C1-C3烷基或式II（II）的基团，条件是当R1是C2-C6烷基或取代的C2-C6烷基时，R2是氢或甲基; R3a，R3b ，并且当X是C（R 3c）=，R 3c时，各自独立地是氢，氟或甲基，条件是R 3a，R 3b和R 3c中不超过一个可以不是氢; R 4是氢或C 1 -C 3 烷基; R 5为氢，C 1 -C 3烷基或C 3 -C 6环烷基羰基，条件是当R 3a不为氢时，R 5为氢; R 6为氢或C 1 -C 6烷基;且n为1至6的整数。 本发明化合物可用于活化5-HT1F受体，抑制神经元蛋白质外渗，并用于治疗或预防哺乳动物的偏头痛。
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公开(公告)号：EP2318375B1
公开(公告)日：2012-09-19
申请号：EP09790351.2
申请日：2009-07-14
发明人： KHILEVICH, Albert , LIU, Bin , MAYHUGH, Daniel, Ray , SCHKERYANTZ, Jeffrey, Michael , ZHANG, Deyi
IPC分类号： C07D233/92 , A61K31/4164 , A61P25/00
CPC分类号： C07D233/92
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9.发明授权(PIPERIDINYLOXY)PHENYL, (PIPERIDINYLOXY)PYRIDINYL, (PIPERIDINYLSULFANYL)PHENYL AND (PIPERIDINYLSULFANYL)PYRIDINYL COMPOUNDS AS 5-HT 1F AGONISTS 有权（PIPERIDINYLOXY）苯基 - （（PIPERIDINYLOXY）PYRIDINYL-，（PIPERIDINYLSULFANYL）PHENYL- UND（PIPERIDINYLSULFANYL）PYRIDINYLVERBINDUNGEN ALS 5-HT1F-AGONISTEN
公开(公告)号：EP1626958B1
公开(公告)日：2012-06-27
申请号：EP04759769.5
申请日：2004-04-14
发明人： BLANCO-PILLADO, Maria-Jesus , BENESH, Dana, Rae , FILLA, Sandra, Ann , HUDZIAK, Kevin, John , MATHES, Brian, Michael , KOHLMAN, Daniel, Timothy , YING, Bai-Ping , ZHANG, Deyi , XU, Yao-Chang
IPC分类号： C07D211/44 , C07D211/54 , C07D401/12 , C07D409/12 , A61K31/445 , A61P25/06
CPC分类号： C07D401/12 , C07D211/44 , C07D211/46 , C07D211/54 , C07D401/14 , C07D409/12 , C07D409/14
摘要： The present invention relates to compounds of formula 1: and pharmaceutically acceptable acid addition sails thereof. The compounds of the present invention are useful for activating 5-HTIF receptors, inhibiting neuronal protein extravasation, and for the treatment or preverition of migraine in mammals, particularly humans.
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10.发明公开(PIPERIDINYLOXY)PHENYL, (PIPERIDINYLOXY)PYRIDINYL, (PIPERIDINYLSULFANYL)PHENYL AND (PIPERIDINYLSULFANYL)PYRIDINYL COMPOUNDS AS 5-HT 1F AGONISTS 有权（哌啶基氧基）苯基，（哌啶基氧基）吡啶基，（PIPERIDINYLSULFANYL）苯基和（PIPERIDINYLSULFANYL）PYRIDINYLVERBINDUNGEN ALS 5- HT1F-激动剂
公开(公告)号：EP1626958A1
公开(公告)日：2006-02-22
申请号：EP04759769.5
申请日：2004-04-14
发明人： BLANCO-PILLADO, Maria-Jesus , BENESH, Dana, Rae , FILLA, Sandra, Ann , HUDZIAK, Kevin, John , MATHES, Brian, Michael , KOHLMAN, Daniel, Timothy , YING, Bai-Ping , ZHANG, Deyi , XU, Yao-Chang
IPC分类号： C07D211/44 , C07D211/54 , C07D401/12 , C07D409/12 , A61K31/445 , A61P25/06
CPC分类号： C07D401/12 , C07D211/44 , C07D211/46 , C07D211/54 , C07D401/14 , C07D409/12 , C07D409/14
摘要： The present invention relates to compounds of formula 1: and pharmaceutically acceptable acid addition sails thereof. The compounds of the present invention are useful for activating 5-HTIF receptors, inhibiting neuronal protein extravasation, and for the treatment or preverition of migraine in mammals, particularly humans.
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