公开(公告)号：US08202873B2

公开(公告)日：2012-06-19

申请号：US12597255

申请日：2008-05-07

申请人： Valentina O. Badescu ,  Anne Marie Camp ,  Barry Peter Clark ,  Michael Philip Cohen ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Sarah Lynne Hellman ,  Michael Philip Mazanetz ,  Marta Maria Pineiro-Nunez ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  Maria Ann Whatton

发明人： Valentina O. Badescu ,  Anne Marie Camp ,  Barry Peter Clark ,  Michael Philip Cohen ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Sarah Lynne Hellman ,  Michael Philip Mazanetz ,  Marta Maria Pineiro-Nunez ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  Maria Ann Whatton

IPC分类号： A61K31/4965

CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine, persistent pain, and anxiety: where A and B are each independently —C(H)═ or —N═, provided that at least one of A and B is —N═, n is 1-3, m is 0-3, and R1-4 are as defined herein.

摘要翻译： 本发明提供式I的选择性5-HT7受体拮抗剂化合物及其在治疗偏头痛，持续性疼痛和焦虑中的用途：其中A和B各自独立地为-C（H）=或-N =，条件是在 A和B中的至少一个为-N =，n为1-3，m为0-3，R1-4如本文所定义。

公开(公告)号：US20100120785A1

公开(公告)日：2010-05-13

申请号：US12597255

申请日：2008-05-07

申请人： Valentina O. Badescu ,  Anne Marie Camp ,  Barry Peter Clark ,  Michael Philip Cohen ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Sarah Lynne Hellman ,  Michael Philip Mazanetz ,  Marta Maria Pineiro-Nunez ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  Maria Ann Whatton

发明人： Valentina O. Badescu ,  Anne Marie Camp ,  Barry Peter Clark ,  Michael Philip Cohen ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Sarah Lynne Hellman ,  Michael Philip Mazanetz ,  Marta Maria Pineiro-Nunez ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  Maria Ann Whatton

IPC分类号： A61K31/497 ,  C07D241/02 ,  A61P25/06

CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine, persistent pain, and anxiety: where A and B are each independently C(H)═ or N═, provided that at least one of A and B is —N═, n is 1-3, m is 0-3, and R14 are as defined herein.

摘要翻译： 本发明提供式I的选择性5-HT7受体拮抗剂化合物及其在治疗偏头痛，持续性疼痛和焦虑中的用途：其中A和B各自独立地为C（H）=或N =，条件是至少一种 A和B为-N =，n为1-3，m为0-3，R 14如本文所定义。

公开(公告)号：US08048884B2

公开(公告)日：2011-11-01

申请号：US12447546

申请日：2008-08-19

申请人： Michael Philip Cohen ,  Sarah Lynne Hellman ,  Sean Patrick Hollinshead ,  Sandra Ann Filla ,  Michael Wade Tidwell

发明人： Michael Philip Cohen ,  Sarah Lynne Hellman ,  Sean Patrick Hollinshead ,  Sandra Ann Filla ,  Michael Wade Tidwell

IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  A61K31/497

CPC分类号： C07D241/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12

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═; m is 0, 1 or 2; R1 is optionally substituted phenyl, optionally substituted pyrazol-4-yl; optionally substituted imidazolyl, optionally substituted pyridyl, or thienyl; R2 is hydrogen or methyl; and R3 and R4 are as defined herein.

摘要翻译： 本发明提供式I的选择性5-HT7受体拮抗剂化合物及其在治疗偏头痛中的用途：其中A为-C（H）=或-N =; m为0,1或2; R1是任选取代的苯基，任选取代的吡唑-4-基; 任选取代的咪唑基，任选取代的吡啶基或噻吩基; R2是氢或甲基; 并且R 3和R 4如本文所定义。

公开(公告)号：US20100075976A1

公开(公告)日：2010-03-25

申请号：US12447546

申请日：2008-08-19

申请人： Michael Philip Cohen ,  Sarah Lynne Hellman ,  Sean Patrick Hollinshead ,  Sandra Ann Filla ,  Michael Wade Tidwell

发明人： Michael Philip Cohen ,  Sarah Lynne Hellman ,  Sean Patrick Hollinshead ,  Sandra Ann Filla ,  Michael Wade Tidwell

IPC分类号： A61K31/496 ,  C07D403/04 ,  C07D403/14 ,  C07D401/14 ,  A61K31/497 ,  A61P25/06

CPC分类号： C07D241/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12

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═; m is 0, 1 or 2; R1 is optionally substituted phenyl, optionally substituted pyrazol-4-yl; optionally substituted imidazolyl, optionally substituted pyridyl, or thienyl; R2 is hydrogen or methyl; and R3 and R4 are as defined herein.

摘要翻译： 本发明提供式I的选择性5-HT7受体拮抗剂化合物及其在治疗偏头痛中的用途：其中A为-C（H）=或-N =; m为0,1或2; R1是任选取代的苯基，任选取代的吡唑-4-基; 任选取代的咪唑基，任选取代的吡啶基或噻吩基; R2是氢或甲基; 并且R 3和R 4如本文所定义。

公开(公告)号：US20120028961A1

公开(公告)日：2012-02-02

申请号：US13192707

申请日：2011-07-28

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 Rothhaar ,  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 Rothhaar ,  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 ,  A61P25/22 ,  A61P25/00 ,  A61P25/24 ,  C07D223/16 ,  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-HT2C receptor agonists for the treatment of 5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where: R6 is —S—R14; 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[d]吖庚因作为选择性5-HT 2C受体激动剂，用于治疗5-HT 2C相关病症，包括肥胖，强迫症/强迫症 ，抑郁症和焦虑症：其中：R6为-S-R14; 和其它取代基如说明书中所定义。

公开(公告)号：US08022062B2

公开(公告)日：2011-09-20

申请号：US10598302

申请日：2005-02-18

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 Rothhaar ,  Michael Wade Tidwell ,  Frantz Victor ,  Andrew Caerwyn Williams ,  Deyi Zhang ,  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 Rothhaar ,  Michael Wade Tidwell ,  Frantz Victor ,  Andrew Caerwyn Williams ,  Deyi Zhang ,  Michael Philip Mazanetz

IPC分类号： A61P3/04 ,  A61P25/22 ,  A61P25/24 ,  A61P25/30 ,  A61K31/55 ,  C07D223/16 ,  C07D401/12 ,  C07D417/12 ,  C07D413/12 ,  C07D403/12 ,  C07D409/12 ,  C07D405/12 ,  C07D413/14 ,  C07D417/06 ,  C07D403/06

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-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[d]吖庚因作为选择性5-HT 2C受体激动剂，用于治疗5-HT 2C相关病症，包括肥胖，强迫症/强迫症 ，抑郁症和焦虑症：其中：R6是-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：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。