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21. 发明申请

US20120329820A1 Pyridinoylpiperidines As 5-HT1F Agonists 有权
标题翻译：吡啶基哌啶作为5-HT1F激动剂
公开(公告)号：US20120329820A1
公开(公告)日：2012-12-27
申请号：US13363895
申请日：2012-02-01
申请人： Michael P. Cohen , Daniel T. Kohlman , Sidney X. Liang , Frantz Victor , Yao-Chang Xu , Bai-Ping Ying , Deanna P. Zacherl , Deyi Zhang
发明人： Michael P. Cohen , Daniel T. Kohlman , Sidney X. Liang , Frantz Victor , Yao-Chang Xu , Bai-Ping Ying , Deanna P. Zacherl , Deyi Zhang
IPC分类号： A61K31/4545 , C07D409/14 , A61K31/506 , C07D405/14 , C07D417/14 , A61P25/06 , C07D401/06 , C07D401/14
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 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.
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： R 1是C 1 -C 6烷基，取代的C 1 -C 6烷基，C 3 -C 7环烷基，取代的C 3 -C 7环烷基，C 3 -C 7环烷基-C 1 -C 3烷基，取代的C 3 -C 7环烷基-C 1 -C 3烷基，苯基，取代的苯基，杂环或取代的杂环; R 2是氢，C 1 -C 3烷基，C 3 -C 6环烷基-C 1 -C 3烷基或式II的基团R 3是氢或C 1 -C 3烷基; R4是氢，卤素或C1-C3烷基; R5是氢或C1-C3烷基; R6是氢或C1-C6烷基; n为1〜6的整数。本发明的化合物可用于激活5-HT1F受体，抑制神经元蛋白质外渗，以及治疗或预防哺乳动物偏头痛。本发明还涉及合成式I化合物中的中间体的方法。

22. 发明申请

US20090209563A1 Pyridinoylpiperidines as 5-HT1F agonists 审中-公开
标题翻译：吡啶基哌啶作为5-HT1F激动剂
公开(公告)号：US20090209563A1
公开(公告)日：2009-08-20
申请号：US12221919
申请日：2008-08-07
申请人： Michael Philip Cohen , Daniel Timothy Kohlman , Sidney Xi Liang , Vincent Mancuso , Yao-Chang Xu
发明人： Michael Philip Cohen , Daniel Timothy Kohlman , Sidney Xi Liang , Vincent Mancuso , Yao-Chang Xu
IPC分类号： A61K31/4545 , C07D401/06 , C07D409/14 , C07D405/14 , C07D401/14 , C07D417/14 , A61K31/506 , 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 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.
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： R 1是C 1 -C 6烷基，取代的C 1 -C 6烷基，C 3 -C 7环烷基，取代的C 3 -C 7环烷基，C 3 -C 7环烷基-C 1 -C 3烷基，取代的C 3 -C 7环烷基-C 1 -C 3烷基，苯基，取代的苯基，杂环或取代的杂环; R 2是氢，C 1 -C 3烷基，C 3 -C 6环烷基-C 1 -C 3烷基或式II的基团R 3是氢或C 1 -C 3烷基; R4是氢，卤素或C1-C3烷基; R5是氢或C1-C3烷基; R6是氢或C1-C6烷基; n为1〜6的整数。本发明的化合物可用于激活5-HT1F受体，抑制神经元蛋白质外渗，以及治疗或预防哺乳动物偏头痛。本发明还涉及合成式I化合物中的中间体的方法。

23. 发明授权

US07291632B2 Substituted 2-carbonylamino-6-piperidinaminopyridines and substituted 1-carbonylamino-3-piperidinaminobenzenes as 5-HT1F agonists 有权
公开(公告)号：US07291632B2
公开(公告)日：2007-11-06
申请号：US10569109
申请日：2004-09-03
申请人： Maria-Jesus Blanco-Pillado , Michael Philip Cohen , Sandra Ann Filla , Kevin John Hudziak , Daniel Timothy Kohlman , Dana Rae Benesh , Frantz Victor , Yao-Chang Xu , Bai-Ping Ying , DeAnna Piatt Zacherl , Deyi Zhang , Brian Michael Mathes
发明人： Maria-Jesus Blanco-Pillado , Michael Philip Cohen , Sandra Ann Filla , Kevin John Hudziak , Daniel Timothy Kohlman , Dana Rae Benesh , Frantz Victor , Yao-Chang Xu , Bai-Ping Ying , DeAnna Piatt Zacherl , Deyi Zhang , Brian Michael Mathes
IPC分类号： A61K31/445 , C07D211/32 , C07D211/72 , C07D421/00
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： 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.

24. 发明申请

US20060287363A1 Substituted 2-carbonylamino-6-piperidinaminopyridines and substituted 1-carbonylamino-3-piperidinaminobenzenes as 5-ht 1f agonists 有权
公开(公告)号：US20060287363A1
公开(公告)日：2006-12-21
申请号：US10569109
申请日：2004-09-03
申请人： Maria-Jesus Blanco-Pillado , Michael Cohen , Sandra Filla , Kevin Hudzlak , Daniel Kohlman , Dana Benesh , Frantz Victor , Yao-Chang Xu , Bai-Ping Ying , DeAnna Zacherl , Deyi Zhang , Brian Mathes
发明人： Maria-Jesus Blanco-Pillado , Michael Cohen , Sandra Filla , Kevin Hudzlak , Daniel Kohlman , Dana Benesh , Frantz Victor , Yao-Chang Xu , Bai-Ping Ying , DeAnna Zacherl , Deyi Zhang , Brian Mathes
IPC分类号： A61K31/4545 , A61K31/454 , C07D403/14
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： 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.

25. 发明申请

US20060211734A1 (Piperidinyloxy)phenyl, (piperidinyloxy)pyridinyl, (piperidinylsulfanyl)phenyl and (piperidinylsulfanyl)pyridinyl compounds as 5-ht1f agonists 失效
标题翻译：（哌啶基氧基）苯基，（哌啶基氧基）吡啶基，（哌啶基硫烷基）苯基和（哌啶基硫烷基）吡啶基化合物作为5-ht1f激动剂
公开(公告)号：US20060211734A1
公开(公告)日：2006-09-21
申请号：US10552131
申请日：2004-04-14
申请人： Maria-Jesus Blanco-Pillado , Dana Benesh , Sandra Filla , Kevin Hudziak , Brian Mathes , Daniel Kohlman , Bai-Ping Ying , Deyl Zhang , Yao-Chang Xu
发明人： Maria-Jesus Blanco-Pillado , Dana Benesh , Sandra Filla , Kevin Hudziak , Brian Mathes , Daniel Kohlman , Bai-Ping Ying , Deyl Zhang , Yao-Chang Xu
IPC分类号： A61K31/4545 , A61K31/454 , C07D401/14 , C07D403/14
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-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or preverition of migraine in mammals, particularly humans.
摘要翻译：本发明涉及式1的化合物及其药学上可接受的酸加成口。本发明的化合物可用于激活5-HT 1F受体，抑制神经元蛋白质外渗，以及在哺乳动物，特别是人中治疗或预防偏头痛。

26. 发明申请

US20050282817A1 Arylpiperazines having activity at the serotonin 1A receptor 审中-公开
公开(公告)号：US20050282817A1
公开(公告)日：2005-12-22
申请号：US11184522
申请日：2005-07-19
申请人： Alexander Godfrey , Daniel Kohlman , John O'Toole , Yao-Chang Xu , Tony Zhang
发明人： Alexander Godfrey , Daniel Kohlman , John O'Toole , Yao-Chang Xu , Tony Zhang
IPC分类号： C07D295/08 , A61K20060101 , A61K31/395 , A61K31/495 , A61K31/496 , A61P1/00 , A61P3/04 , A61P9/00 , A61P15/10 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/34 , A61P43/00 , C07C20060101 , C07C45/00 , C07C45/29 , C07C45/40 , C07C45/51 , C07C45/59 , C07C45/68 , C07C49/355 , C07C49/563 , C07C49/577 , C07C49/583 , C07C49/86 , C07D20060101 , C07D213/74 , C07D295/04 , C07D295/088 , C07D295/092 , C07D295/10 , C07D295/104 , C07D295/108 , C07D401/04 , C07D521/00
CPC分类号： C07D295/088 , A61K31/495 , A61K31/496 , C07C45/004 , C07C45/29 , C07C45/40 , C07C45/515 , C07C45/59 , C07C45/68 , C07C49/563 , C07C49/577 , C07C49/583 , C07C49/86 , C07D213/74 , C07D295/104 , C07D295/108
摘要： A series of aryl piperazine compounds are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.

27. 发明授权

US06946579B2 Arylpiperazines having activity at the serotonin 1A receptor 失效
标题翻译：具有5-羟色胺1A受体活性的芳基哌嗪
公开(公告)号：US06946579B2
公开(公告)日：2005-09-20
申请号：US10613798
申请日：2003-07-02
申请人： Alexander Glenn Godfrey , Daniel Timothy Kohlman , John Cunningham O'Toole , Yao-Chang Xu , Tony Yantao Zhang
发明人： Alexander Glenn Godfrey , Daniel Timothy Kohlman , John Cunningham O'Toole , Yao-Chang Xu , Tony Yantao Zhang
IPC分类号： C07D295/08 , A61K20060101 , A61K31/395 , A61K31/495 , A61K31/496 , A61P1/00 , A61P3/04 , A61P9/00 , A61P15/10 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/34 , A61P43/00 , C07C20060101 , C07C45/00 , C07C45/29 , C07C45/40 , C07C45/51 , C07C45/59 , C07C45/68 , C07C49/355 , C07C49/563 , C07C49/577 , C07C49/583 , C07C49/86 , C07D20060101 , C07D213/74 , C07D295/04 , C07D295/088 , C07D295/092 , C07D295/10 , C07D295/104 , C07D295/108 , C07D401/04 , C07D521/00 , C07C49/312
CPC分类号： C07D295/088 , A61K31/495 , A61K31/496 , C07C45/004 , C07C45/29 , C07C45/40 , C07C45/515 , C07C45/59 , C07C45/68 , C07C49/563 , C07C49/577 , C07C49/583 , C07C49/86 , C07D213/74 , C07D295/104 , C07D295/108
摘要： A series of aryl piperazine compounds are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.
摘要翻译：一系列芳基哌嗪化合物是用于治疗与5-羟色胺1 A受体相关或受其影响的病症的有效药物; 该化合物在该受体上是特别有效的拮抗剂，特别可用于缓解尼古丁和烟草戒断症状。

28. 发明授权

US06664274B1 Piperidine derivatives as serotonine reuptake inhibitors 失效
标题翻译：哌啶衍生物作为血清素再摄取抑制剂
公开(公告)号：US06664274B1
公开(公告)日：2003-12-16
申请号：US10070183
申请日：2002-07-16
申请人： Sidney Xi Liang , Yao-Chang Xu
发明人： Sidney Xi Liang , Yao-Chang Xu
IPC分类号： A61K31444
CPC分类号： C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The present invention provides compounds of formula I and a method of inhibiting the reuptake of serotonin, antagonizing the 5-HT1A receptor and antagonizing the 5-HT2A receptor which comprises administering to a subject in need of such treatment an effective amount of a compound of formula I.
摘要翻译：本发明提供了式I化合物和抑制5-羟色胺再摄取，拮抗5-HT 1A受体和拮抗5-HT 2A受体的方法，其包括向需要这种治疗的受试者施用有效量的式I化合物。

29. 发明授权

US06660859B2 Arylpiperazines having activity at the serotonin 1A receptor 失效
标题翻译：具有5-羟色胺1A受体活性的芳基哌嗪
公开(公告)号：US06660859B2
公开(公告)日：2003-12-09
申请号：US10022043
申请日：2001-12-18
申请人： Daniel Timothy Kohlman , Yao-Chang Xu
发明人： Daniel Timothy Kohlman , Yao-Chang Xu
IPC分类号： C07D295104
CPC分类号： C07D295/088 , A61K31/495 , A61K31/496 , C07C45/004 , C07C45/29 , C07C45/40 , C07C45/515 , C07C45/59 , C07C45/68 , C07C49/563 , C07C49/577 , C07C49/583 , C07C49/86 , C07D213/74 , C07D295/104 , C07D295/108
摘要： Described herein is a series of aryl piperazine compounds of the formula: wherein Ar′ is a mono or bicyclic aryl or heteroaryl radical substituted with one to three substituents selected from the group consisting of hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C5)cycloalkyl, (C3-C8)cycloalkenyl or halo; R1 is hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio; R2 is phenyl, naphthyl or (C3-C12)cycloalkyl substituted with one or two substituents selected from the group consisting of hydrogen (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; R3 is selected from the group consisting of hydrogen (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C5)cycloalkyl, (C3-C8)cycloalkenyl or halo; X is —(C═O)—, —CHOH— or —CH2—; or a pharmaceutically acceptable salt, racemate, optical isomer or solvate thereof.
摘要翻译：本文描述了一系列下式的芳基哌嗪化合物：其中Ar'是被1-3个选自氢，（C 1 -C 6）烷基，（C 1 -C 6）烷基，烷氧基，（C1-C6）烷硫基，（C2-C6）烯基，（C2-C6）炔基，（C1-C6）烷基卤代，（C3-C5）环烷基，（C3-C8）环烯基或卤素; 是（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷硫基; R 2是苯基，萘基或被一个或两个取代基取代的（C 3 -C 12）环烷基，的（C1-C6）烷基，（C1-C6）烷氧基，（C1-C6）烷硫基，（C2-C6）烯基，（C2-C6）炔基，（C1-C6）烷基卤，（C3-C8），（C 3 -C 8）环烯基或卤素; R 3选自氢（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷硫基，（C 2 -C 6）（C 2 -C 6）炔基，（C 1 -C 6）烷基卤代，（C 3 -C 5）环烷基，（C 3 -C 8）环烯基或卤素; X是 - （C = O） - ， - CHOH-或-CH 2 - 药学上可接受的盐，外消旋体，光学异构体或其溶剂合物。

30. 发明授权

US06465453B1 Azepine derivatives having effects on serotonin related systems 失效
公开(公告)号：US06465453B1
公开(公告)日：2002-10-15
申请号：US09701363
申请日：2000-11-28
申请人： Kenneth Lee Hauser , Larry Wayne Hertel , Yao-Chang Xu
发明人： Kenneth Lee Hauser , Larry Wayne Hertel , Yao-Chang Xu
IPC分类号： A61K3155
CPC分类号： C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The present invention provides compounds of formula I and a method of inhibiting the reuptake of serotonin, antagonizing the 5-HT1A receptor and antagonizing the 5-HT2A receptor which comprises administering to a subject in need of such treatment an effective amount of a compound of formula I.

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