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：US20080255092A1

公开(公告)日：2008-10-16

申请号：US11996457

申请日：2006-09-01

申请人： John Gordon Allen ,  Karin Briner ,  Christopher Stanley Galka ,  Richard Charles Hoying ,  Maria Angeles Martinez-Grau ,  Julie Miyashiro ,  Natalia Pokrovskaia ,  Matthew Robert Reinhard

发明人： John Gordon Allen ,  Karin Briner ,  Christopher Stanley Galka ,  Richard Charles Hoying ,  Maria Angeles Martinez-Grau ,  Julie Miyashiro ,  Natalia Pokrovskaia ,  Matthew Robert Reinhard

IPC分类号： A61K31/55 ,  C07D223/16

CPC分类号： C07D223/16 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  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: R6 D R?N—R″R* where R6 is —(CrC3)alkyl-S—(C0-C3)alkyl-R10, —(C1-C3)alkyl-NR11R12, —(CrC3)alkyl-O—R13. 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]吖庚因作为选择性的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，抑郁症和焦虑症：R6 DR？N-R''R *其中R6是 - （CrC3）烷基-S-（C0-C3）烷基-R10， - （C1-C3）烷基-NR11R12 - （ C 1 -C 3烷基-O-R 13。 和其它取代基如说明书中所定义。

公开(公告)号：US08580780B2

公开(公告)日：2013-11-12

申请号：US13192707

申请日：2011-07-28

申请人： John Gordon Allen ,  Karin Briner ,  Christopher Stanley Galka ,  Maria Angeles Martinez-Grau ,  Matthew Robert Reinhard ,  Michael John Rodriguez ,  Roger Ryan Rothhaar ,  Michael Wade Tidwell ,  Frantz Victor ,  Deyi Zhang ,  Steven Armen Boyd ,  Arundhati S. Deo ,  Wai-Man Lee ,  Christopher Stephen Siedem ,  Ajay Singh

发明人： John Gordon Allen ,  Karin Briner ,  Christopher Stanley Galka ,  Maria Angeles Martinez-Grau ,  Matthew Robert Reinhard ,  Michael John Rodriguez ,  Roger Ryan Rothhaar ,  Michael Wade Tidwell ,  Frantz Victor ,  Deyi Zhang ,  Steven Armen Boyd ,  Arundhati S. Deo ,  Wai-Man Lee ,  Christopher Stephen Siedem ,  Ajay Singh

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 —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：US08680091B2

公开(公告)日：2014-03-25

申请号：US13156575

申请日：2011-06-09

申请人： Karen Briner ,  Manuel Javier Cases-Thomas ,  Marta Adeva Bartolome ,  Christopher Stanley Galka ,  Alicia Marcos Llorente ,  Maria Angeles Martinez-Grau ,  Michael Philip Mazanetz ,  John Cunningham O'Toole ,  Richard Edmund Rathmell ,  Matthew Robert Reinhard ,  Selma Sapmaz ,  Andrew Caerwyn Williams

发明人： Karen Briner ,  Manuel Javier Cases-Thomas ,  Marta Adeva Bartolome ,  Christopher Stanley Galka ,  Alicia Marcos Llorente ,  Maria Angeles Martinez-Grau ,  Michael Philip Mazanetz ,  John Cunningham O'Toole ,  Richard Edmund Rathmell ,  Matthew Robert Reinhard ,  Selma Sapmaz ,  Andrew Caerwyn Williams

IPC分类号： A61K31/55 ,  C07D223/16 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12

CPC分类号： C07D223/16 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

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, where, R6 is —NR10R11, where R10 is substituted phenylalkyl or substituted pyridylalkyl 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-HT2c相关疾病，包括肥胖，强迫症/ 强迫症，抑郁症和焦虑症，其中R6是-NR10R11，其中R10是取代的苯基烷基或取代的吡啶基烷基和其它取代基如说明书中所定义。

公开(公告)号：US20110269745A1

公开(公告)日：2011-11-03

申请号：US13156575

申请日：2011-06-09

申请人： Karin BRINER ,  Marta ADEVA BARTOLOME ,  Manuel Javier CASES-THOMAS ,  Christopher Stanley GALKA ,  Alicia MARCOS LLORENTE ,  Maria Angeles MARTINEZ-GRAU ,  Michael Philip MAZANETZ ,  John Cunningham O'Toole ,  Richard Edmund RATHMELL ,  Matthew Robert REINHARD ,  Selma SAPMAZ ,  Andrew Caerwyn WILLIAMS

发明人： Karin BRINER ,  Marta ADEVA BARTOLOME ,  Manuel Javier CASES-THOMAS ,  Christopher Stanley GALKA ,  Alicia MARCOS LLORENTE ,  Maria Angeles MARTINEZ-GRAU ,  Michael Philip MAZANETZ ,  John Cunningham O'Toole ,  Richard Edmund RATHMELL ,  Matthew Robert REINHARD ,  Selma SAPMAZ ,  Andrew Caerwyn WILLIAMS

IPC分类号： A61K31/55 ,  C07D417/12 ,  C07D413/12 ,  C07D401/12 ,  C07D403/12 ,  A61P25/22 ,  C07D417/14 ,  C07D409/12 ,  A61P3/04 ,  A61P25/00 ,  A61P25/24 ,  C07D223/16 ,  C07D401/14

CPC分类号： C07D223/16 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

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, where, R6 is —NR10R11, where R10 is substituted phenylalkyl or substituted pyridylalkyl 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-HT2c相关疾病，包括肥胖，强迫症/ 强迫症，抑郁症和焦虑症，其中R6是-NR10R11，其中R10是取代的苯基烷基或取代的吡啶基烷基和其它取代基如说明书中所定义。

公开(公告)号：US07994163B2

公开(公告)日：2011-08-09

申请号：US11996457

申请日：2006-09-01

申请人： John Gordon Allen ,  Karin Briner ,  Christopher Stanley Galka ,  Richard Charles Hoying ,  Maria Angeles Martinez-Grau ,  Julie Miyashiro ,  Natalia Pokrovskaia ,  Matthew Robert Reinhard

发明人： John Gordon Allen ,  Karin Briner ,  Christopher Stanley Galka ,  Richard Charles Hoying ,  Maria Angeles Martinez-Grau ,  Julie Miyashiro ,  Natalia Pokrovskaia ,  Matthew Robert Reinhard

IPC分类号： A61P3/04 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  A61K31/55 ,  C07D223/16 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12

CPC分类号： C07D223/16 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  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: R6 D R?N—R″R* where R6 is —(CrC3)alkyl-S—(C0-C3)alkyl-R10, —(C1-C3)alkyl-NR11R12, —(CrC3)alkyl-O—R13. 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]吖庚因作为选择性的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，抑郁症和焦虑症：R6 DR？N-R“R *其中R6是 - （CrC3）烷基-S-（C0-C3）烷基-R10， - （C1-C3）烷基-NR11R12 - （CrC3 ）烷基-O-R13。 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。

公开(公告)号：US20080269196A1

公开(公告)日：2008-10-30

申请号：US11996751

申请日：2006-09-01

申请人： Karin Briner ,  Maria Adeva Bartolome ,  Manuel Javier Cases-Thomas ,  Christopher Stanley Galka ,  Alicia Marcos Llorente ,  Maria Angeles Martinez-Grau ,  Michael Philip Mazanetz ,  John Cunningham O' Toole ,  Richard Edmund Rathmell ,  Matthew Robert Reinhard ,  Selma Sapmaz ,  Andrew Caerwyn Williams

发明人： Karin Briner ,  Maria Adeva Bartolome ,  Manuel Javier Cases-Thomas ,  Christopher Stanley Galka ,  Alicia Marcos Llorente ,  Maria Angeles Martinez-Grau ,  Michael Philip Mazanetz ,  John Cunningham O' Toole ,  Richard Edmund Rathmell ,  Matthew Robert Reinhard ,  Selma Sapmaz ,  Andrew Caerwyn Williams

IPC分类号： A61K31/55 ,  C07D223/16

CPC分类号： C07D223/16 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

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, where, R6 is —NR10R11, where R10 is substituted phenylalkyl or substituted pyridylalkyl 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-HT2c相关疾病，包括肥胖，强迫症/ 强迫症，抑郁症和焦虑症，其中R6是-NR10R11，其中R10是取代的苯基烷基或取代的吡啶基烷基和其它取代基如说明书中所定义。