公开(公告)号：US20090099155A1

公开(公告)日：2009-04-16

申请号：US10598302

申请日：2005-09-09

申请人： John Gordon Allen ,  Karin Briner ,  Michael Philip Cohen ,  Christopher Stanley Galka ,  Sarah Lynne Hellman ,  Maria Angeles Martinez-Grau ,  Matthew Robert Reinhard ,  Michael John Rodriguez ,  Roger Ryan Rothaar ,  Michael Wade Tidwell ,  Frantz Victor ,  Andrew Caerwyn Williams ,  Deyi Zhang ,  Steven Armen Boyd ,  Richard Gerard Conway ,  Arundhati S. Deo ,  Wai-Man Lee ,  Christopher Stephen Siedem ,  Ajay Singh ,  Michael Philip Mazanetz

发明人： John Gordon Allen ,  Karin Briner ,  Michael Philip Cohen ,  Christopher Stanley Galka ,  Sarah Lynne Hellman ,  Maria Angeles Martinez-Grau ,  Matthew Robert Reinhard ,  Michael John Rodriguez ,  Roger Ryan Rothaar ,  Michael Wade Tidwell ,  Frantz Victor ,  Andrew Caerwyn Williams ,  Deyi Zhang ,  Steven Armen Boyd ,  Richard Gerard Conway ,  Arundhati S. Deo ,  Wai-Man Lee ,  Christopher Stephen Siedem ,  Ajay Singh ,  Michael Philip Mazanetz

IPC分类号： A61K31/55 ,  C07D223/16 ,  C07D417/12 ,  C07D401/12 ,  A61P3/04 ,  A61P25/22 ,  C07D409/12 ,  C07D403/12 ,  C07D405/12

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-benzoazepines 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: where: R6 is -C≡C-R10, -O-R12, -S-R14, or -NR24R25; and other substituents are as defined in the specification.

摘要翻译： 本发明提供式I的6-取代2,3,4,5-四氢-1H-苯并吖庚因作为选择性5-HT 2C受体激动剂用于治疗5-HT2C相关疾病，包括肥胖，强迫症/强迫症，抑郁症和 焦虑：其中：R6为-C≡C-R10，-O-R12，-S-R14或-NR24R25; 和其它取代基如说明书中所定义。

公开(公告)号：US20080300407A1

公开(公告)日：2008-12-04

申请号：US12220225

申请日：2008-07-22

申请人： Michael Philip Cohen ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Vincent Mancuso ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  DeAnna Piatt Zacherl ,  Deyi Zhang

发明人： Michael Philip Cohen ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Vincent Mancuso ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  DeAnna Piatt Zacherl ,  Deyi Zhang

IPC分类号： C07D401/14 ,  C07D401/06

CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

摘要： The 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基团; R3是氢或C1-C3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。

公开(公告)号：US20080214520A1

公开(公告)日：2008-09-04

申请号：US11995212

申请日：2006-09-01

申请人： Karin Briner ,  Anne Marie Camp ,  Alan Cornell ,  Michael Philip Mazanetz ,  Roger Ryan Rothhaar ,  Frantz Victor ,  Andrew Caerwyn Williams ,  Deyi Zhang

发明人： Karin Briner ,  Anne Marie Camp ,  Alan Cornell ,  Michael Philip Mazanetz ,  Roger Ryan Rothhaar ,  Frantz Victor ,  Andrew Caerwyn Williams ,  Deyi Zhang

IPC分类号： A61K31/397 ,  C07D223/16 ,  A61P3/04 ,  A61P25/24 ,  A61P25/00 ,  A61K31/55

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.

摘要翻译： 本发明提供式I的6-取代的2,3,4,5-四氢-1H-苯并[d]吖庚因，作为选择性5-HT 2C受体激动剂用于治疗5-HT 相关的疾病包括肥胖症，强迫症/强迫症，抑郁症和焦虑症：式（I）其中：R 6选自（a，b，c ，d，e）和其它取代基如说明书中所定义。

公开(公告)号：US20070270466A1

公开(公告)日：2007-11-22

申请号：US11810388

申请日：2007-06-04

申请人： Maria-Jesus Blanco-Pillado ,  Michael Cohen ,  Sandra Filla ,  Kevin Hudziak ,  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 Hudziak ,  Daniel Kohlman ,  Dana Benesh ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  DeAnna Zacherl ,  Deyi Zhang ,  Brian Mathes

IPC分类号： A61K31/4468 ,  A61K31/4523 ,  A61P25/06

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: or a pharmaceutically acceptable acid addition salt thereof, wherein 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 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 5HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal.

公开(公告)号：US20070078169A1

公开(公告)日：2007-04-05

申请号：US10576762

申请日：2004-12-06

申请人： Daniel Kohlman ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  Deyi Zhang

发明人： Daniel Kohlman ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  Deyi Zhang

IPC分类号： A61K31/4439 ,  A61K31/44 ,  A61K31/277 ,  A61K31/165

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 independently 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。

公开(公告)号：US5821242A

公开(公告)日：1998-10-13

申请号：US868638

申请日：1997-06-04

申请人： Joseph Matthew Colacino ,  Beverly Ann Heinz ,  Louis Nickolaus Jungheim ,  Shawn Christopher Miller ,  Wayne Alfred Spitzer ,  Joseph Chiou-chung Tang ,  Mark Joseph Tebbe ,  Frantz Victor

发明人： Joseph Matthew Colacino ,  Beverly Ann Heinz ,  Louis Nickolaus Jungheim ,  Shawn Christopher Miller ,  Wayne Alfred Spitzer ,  Joseph Chiou-chung Tang ,  Mark Joseph Tebbe ,  Frantz Victor

IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61P31/12 ,  C07D235/30 ,  C07D235/22 ,  C07D235/08

CPC分类号： C07D235/30

摘要： The present application provides a series of benzimidazole compounds which inhibit the growth of picornaviruses, such as rhinoviruses, enteroviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus and flaviviruses such as hepatitis C and bovine diarrheal virus.

摘要翻译： 本申请提供了一系列苯并咪唑化合物，其抑制微小核糖核酸病毒，例如鼻病毒，肠病毒，脊髓灰质炎病毒，A组和B组的柯萨奇病毒，回波病毒和孟戈病毒以及黄病毒如丙型肝炎和牛腹泻病毒的生长。

公开(公告)号：US5545653A

公开(公告)日：1996-08-13

申请号：US482041

申请日：1995-06-07

申请人： Shawn C. Miller ,  Frantz Victor ,  Wayne A. Spitzer ,  Thomas R. Sattelberg, Sr. ,  Mark J. Tebbe

发明人： Shawn C. Miller ,  Frantz Victor ,  Wayne A. Spitzer ,  Thomas R. Sattelberg, Sr. ,  Mark J. Tebbe

IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61K31/535 ,  A61K31/5355 ,  A61P11/00 ,  A61P31/12 ,  C07D235/30 ,  C07D417/04 ,  A61K31/425

CPC分类号： C07D235/30

摘要： The present application provides a series of benzimidazole compounds which inhibit the growth of picornaviruses, such as rhinoviruses, enteroviruses, cardioviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus. Such compounds are also useful as intermediates for preparing additional benzimidazole antiviral compounds.

摘要翻译： 本申请提供了一系列抑制小核糖核酸病毒（例如鼻病毒，肠病毒，心脏病毒，脊髓灰质炎病毒，A组和B组柯萨克病毒，回波病毒和Mengo病毒）生长的苯并咪唑化合物。 这样的化合物也可用作制备另外的苯并咪唑抗病毒化合物的中间体。

公开(公告)号：US08748459B2

公开(公告)日：2014-06-10

申请号：US13363895

申请日：2012-02-01

申请人： Michael Philip Cohen ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  DeAnna Piatt Zacherl ,  Deyi Zhang

发明人： Michael Philip Cohen ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  DeAnna Piatt Zacherl ,  Deyi Zhang

IPC分类号： A61K31/445 ,  C07D401/06

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-HTlF 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，以及用于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。

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。

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.