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。

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：US08420631B2

公开(公告)日：2013-04-16

申请号：US11995344

申请日：2006-09-01

申请人： John Gordon Allen ,  Karin Briner ,  Anne Marie Camp ,  Manuel Javier Cases-Thomas ,  Richard Charles Hoying ,  Maria Angeles Martinez-Grau ,  Michael Philip Mazanetz ,  Natalia Pokrovskaia ,  Richard Edmund Rathmell ,  Roger Ryan Rothhaar ,  Selma Sapmaz ,  Andrew Caerwyn Williams

发明人： John Gordon Allen ,  Karin Briner ,  Anne Marie Camp ,  Manuel Javier Cases-Thomas ,  Richard Charles Hoying ,  Maria Angeles Martinez-Grau ,  Michael Philip Mazanetz ,  Natalia Pokrovskaia ,  Richard Edmund Rathmell ,  Roger Ryan Rothhaar ,  Selma Sapmaz ,  Andrew Caerwyn Williams

IPC分类号： A61P3/04 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  A61K31/55 ,  C07D223/16 ,  C07D401/06 ,  C07D403/04 ,  C07D409/04 ,  C07D417/06

CPC分类号： C07D223/16 ,  C07D401/06 ,  C07D403/04 ,  C07D409/04 ,  C07D417/06

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, —CH═CR11R11′, or —(C0-C8)alkyl-Ar2 optionally substituted on the alkyl moiety with 1 to 6 fluoro substituents 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-C≡C-R10，-CH = CR11R11'或 - 任选在具有1至6个氟取代基的烷基部分上取代的 - （C 0 -C 8）烷基-Ar 2和其它取代基 如说明书中所定义。

公开(公告)号：US20080207897A1

公开(公告)日：2008-08-28

申请号：US11995344

申请日：2006-09-01

申请人： John Gordon Allen ,  Karin Briner ,  Anne Marie Camp ,  Manuel Javier Cases-Thomas ,  Richard Charles Hoying ,  Maria Angeles Martinez-Grau ,  Michael Philip Mazanetz ,  Natalia Pokrovskaia ,  Richard Edmund Rathmell ,  Roger Ryan Rothhaar ,  Selma Sapmaz ,  Andrew Caerwyn Williams

发明人： John Gordon Allen ,  Karin Briner ,  Anne Marie Camp ,  Manuel Javier Cases-Thomas ,  Richard Charles Hoying ,  Maria Angeles Martinez-Grau ,  Michael Philip Mazanetz ,  Natalia Pokrovskaia ,  Richard Edmund Rathmell ,  Roger Ryan Rothhaar ,  Selma Sapmaz ,  Andrew Caerwyn Williams

IPC分类号： C07D223/16

CPC分类号： C07D223/16 ,  C07D401/06 ,  C07D403/04 ,  C07D409/04 ,  C07D417/06

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, —CH═CR11R11′, or —(C0-C8)alkyl-Ar2 optionally substituted on the alkyl moiety with 1 to 6 fluoro substituents 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-HT 2C相关疾病，包括肥胖症，强迫症/强迫症，抑郁症和焦虑症：其中R 6是-C≡CR10， 或者 - （C 0 -C 8 -C 8）烷基-C 1 -C 10烷基， 在具有1至6个氟取代基和其它取代基的烷基部分上任选取代的O 2'如本说明书中所定义。

公开(公告)号：US07410982B2

公开(公告)日：2008-08-12

申请号：US10532765

申请日：2003-10-24

申请人： Serge Louis Boulet ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Kevin John Hudziak ,  Anette Margareta Johansson ,  Rushad E. Karanjawala ,  John Joseph Masters ,  Brian Michael Mathes ,  Richard Edmund Rathmell ,  Maria Ann (nee Fagan) Whatton ,  Victor Matassa ,  Chad Nolan Wolfe

发明人： Serge Louis Boulet ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Kevin John Hudziak ,  Anette Margareta Johansson ,  Rushad E. Karanjawala ,  John Joseph Masters ,  Brian Michael Mathes ,  Richard Edmund Rathmell ,  Maria Ann (nee Fagan) Whatton ,  Victor Matassa ,  Chad Nolan Wolfe

IPC分类号： A61K31/4365 ,  C07D409/02

CPC分类号： C07D275/04 ,  C07D215/20 ,  C07D217/02 ,  C07D217/04 ,  C07D217/24 ,  C07D277/62 ,  C07D333/54 ,  C07D471/04 ,  C07D495/04

摘要： There is provided a heretoaryloxy/thio 3-substituted propanamine compound of formula (I) wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl —S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, and thienopyridyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro acetyl, —CF3, —SCF3 and cyano; Z is selected from H, OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof.

公开(公告)号：US07417064B2

公开(公告)日：2008-08-26

申请号：US10532657

申请日：2003-10-24

申请人： Serge Louis Boulet ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Kevin John Hudziak ,  Anette Margareta Johansson ,  Rushad E. Karanjawala ,  John Joseph Masters ,  Victor Giulio Matassa ,  Brian Michael Mathes ,  Richard Edmund Rathmell ,  Maria Ann Whatton ,  Chad Nolan Wolfe

发明人： Serge Louis Boulet ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Kevin John Hudziak ,  Anette Margareta Johansson ,  Rushad E. Karanjawala ,  John Joseph Masters ,  Victor Giulio Matassa ,  Brian Michael Mathes ,  Richard Edmund Rathmell ,  Maria Ann Whatton ,  Chad Nolan Wolfe

IPC分类号： A61K31/381 ,  C07D333/64

CPC分类号： C07C217/20 ,  C07C217/34 ,  C07D333/54

摘要： There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from H, OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1-C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; with the proviso that, when Z is H, then Y may not be optionally substituted phenyl or optionally substituted naphthyl.

公开(公告)号：US07037932B2

公开(公告)日：2006-05-02

申请号：US10476137

申请日：2002-05-06

申请人： Peter Gallagher ,  Richard Edmund Rathmell ,  Maria Ann Fagan

发明人： Peter Gallagher ,  Richard Edmund Rathmell ,  Maria Ann Fagan

IPC分类号： A61K31/343 ,  A61K31/381 ,  A61K31/404 ,  C07D209/04 ,  C07D333/52

CPC分类号： C07D333/54 ,  C07D209/08 ,  C07D307/79 ,  C07D333/62 ,  C07D333/68

摘要： There is provided a heretoaryloxy 3-substituted propanamine compound of formula (I): wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents selected from halo, C1–C4 alkyl and C1–C4 alkoxy, and thienyl optionally substituted with up to 3 substituents selected from halo and C1–C4 alkyl; Y is selected from benzothienyl, indolyl and benzofuranyl, optionally substituted with up to 5 substituents selected from halo, C1–C4 alkyl, C1–C4 alkoxy, nitro, acetyl and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1–C4 alkyl; R1 and R2 are each independently H or C1–C4 alkyl; and pharmaceutically acceptable salts thereof.

摘要翻译： 提供式（I）的异烟酰基-3-取代的丙胺化合物：其中A选自-O-和-S-; X选自任选被至多5个选自卤素，C 1 -C 4烷基和C 1 -C 4烷基的取代基取代的苯基 > 4个烷氧基，任选被至多3个选自卤素和C 1 -C 4烷基的取代基取代的噻吩基; Y选自苯并噻吩基，吲哚基和苯并呋喃基，任选被至多5个选自卤素，C 1 -C 4烷基，C 1〜 -C≡4烷氧基，硝基，乙酰基和氰基; 当Y是吲哚基时，它可以被选自C 1 -C 4烷基的N-取代基取代或进一步取代; R 1和R 2各自独立地为H或C 1 -C 4烷基; 及其药学上可接受的盐。

公开(公告)号：US07410996B2

公开(公告)日：2008-08-12

申请号：US10533328

申请日：2003-10-24

申请人： Serge Louis Boulet ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Kevin John Hudziak ,  Anette Margareta Johansson ,  Rushad E. Karanjawala ,  John Joseph Masters ,  Victor Giulio Matassa ,  Brian Michael Mathes ,  Richard Edmund Rathmell ,  Maria Ann Whatton ,  Chad Nolan Wolfe

发明人： Serge Louis Boulet ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Kevin John Hudziak ,  Anette Margareta Johansson ,  Rushad E. Karanjawala ,  John Joseph Masters ,  Victor Giulio Matassa ,  Brian Michael Mathes ,  Richard Edmund Rathmell ,  Maria Ann Whatton ,  Chad Nolan Wolfe

IPC分类号： A61K31/381 ,  C07D333/64

CPC分类号： C07D275/04 ,  C07C217/16 ,  C07C217/30 ,  C07C217/48 ,  C07C323/32 ,  C07D307/86 ,  C07D333/54 ,  C07D333/62 ,  C07D475/04

摘要： There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1-C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof with the proviso that when Y is optionally substituted phenyl or optionally substituted 1,3-benzodioxolyl and Z is OR3 and X is optionally substituted phenyl then A is —S—.