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：US20100197700A1

公开(公告)日：2010-08-05

申请号：US12678345

申请日：2008-09-30

申请人： Valentina O Badescu ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Maria Ann Whatton

发明人： Valentina O Badescu ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Maria Ann Whatton

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

CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14

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═ and R1-7 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 =且R1-7如本文所定义。

公开(公告)号：US07910588B2

公开(公告)日：2011-03-22

申请号：US12678345

申请日：2008-09-30

申请人： Valentina O Badescu ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Maria Ann Whatton

发明人： Valentina O Badescu ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Maria Ann Whatton

IPC分类号： A61K31/444 ,  A61K31/497 ,  C07D401/14 ,  C07D403/14

CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14

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═ and R1-7 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 =且R1-7如本文所定义。

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—.

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：US07615648B2

公开(公告)日：2009-11-10

申请号：US11568641

申请日：2005-05-19

申请人： John Richard Harris ,  Barry Peter Clark ,  Peter Thaddeus Gallagher ,  Maria Ann Whatton

发明人： John Richard Harris ,  Barry Peter Clark ,  Peter Thaddeus Gallagher ,  Maria Ann Whatton

IPC分类号： C07D207/00 ,  A01N43/36

CPC分类号： C07D207/09 ,  C07D405/12 ,  C07D493/08

摘要： The present invention provides compounds of formula (I) wherein A is (1), (2), (3), (4), (5), (6) or (7) and wherein R1, R7, y and Ar1 are defined herein. The compounds are inhibitors of the uptake of one or more monoamines selected from serotonin, norepinephrine and dopamine and, as such, may be useful in the treatment of disorders of the central and/or peripheral nervous system.

摘要翻译： 本发明提供式（I）化合物，其中A是（1），（2），（3），（4），（5），（6）或（7），其中R 1，R 7，Y和Ar 1是 本文定义。 这些化合物是一种或多种选自5-羟色胺，去甲肾上腺素和多巴胺的单胺摄取的抑制剂，因此可用于治疗中枢和/或周围神经系统疾病。

公开(公告)号：US07521462B2

公开(公告)日：2009-04-21

申请号：US10597795

申请日：2005-02-11

申请人： Serge Louis Boulet ,  Barry Peter Clark ,  John Fairhurst ,  Peter Thaddeus Gallagher ,  Anette Margareta Johansson ,  Maria Ann Whatton ,  Virginia Ann Wood

发明人： Serge Louis Boulet ,  Barry Peter Clark ,  John Fairhurst ,  Peter Thaddeus Gallagher ,  Anette Margareta Johansson ,  Maria Ann Whatton ,  Virginia Ann Wood

IPC分类号： A61K31/4468 ,  A61K31/4535

CPC分类号： C07D513/04 ,  A61K31/454 ,  A61K31/4545 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： The present invention provides compounds of formula (I) where n, R1, R2, R3, R4, R5 and Heteroaryl are defined herein. The compounds are inhibitors of the uptake of one or more monoamines selected from serotonin, norepinephrine and dopamine and, as such, may be useful in the treatment of disorders of the central and/or peripheral nervous system.

摘要翻译： 本发明提供式（I）化合物，其中n，R 1，R 2，R 3，R 4，R 5和杂芳基如本文所定义。 这些化合物是一种或多种选自5-羟色胺，去甲肾上腺素和多巴胺的单胺摄取的抑制剂，因此可用于治疗中枢和/或周围神经系统疾病。

公开(公告)号：US07432280B2

公开(公告)日：2008-10-07

申请号：US10558588

申请日：2004-05-25

申请人： Christopher David Beadle ,  Manuel Javier Cases-Thomas ,  Barry Peter Clark ,  Peter Thaddeus Gallagher ,  John Joseph Masters ,  Graham Henry Timms ,  Magnus Wilhelm Walter ,  Maria Ann Whatton ,  Virginia Ann Wood ,  Jeremy Gilmore

发明人： Christopher David Beadle ,  Manuel Javier Cases-Thomas ,  Barry Peter Clark ,  Peter Thaddeus Gallagher ,  John Joseph Masters ,  Graham Henry Timms ,  Magnus Wilhelm Walter ,  Maria Ann Whatton ,  Virginia Ann Wood ,  Jeremy Gilmore

IPC分类号： A01N43/90 ,  A01N43/40 ,  A61K31/44 ,  A61K31/445 ,  C07D453/02 ,  C07D211/56 ,  C07D211/98

CPC分类号： C07D405/12 ,  C07D211/56 ,  C07D453/02

摘要： The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, which are useful for the inhibition of the uptake of one or more physiologically active monoamines (serotonin, norepinephrine, and dopamine).

摘要翻译： 本发明提供式（I）化合物及其药学上可接受的盐，其可用于抑制一种或多种生理活性单胺（5-羟色胺，去甲肾上腺素和多巴胺）摄取。

公开(公告)号：US07619096B2

公开(公告)日：2009-11-17

申请号：US10558626

申请日：2004-05-11

申请人： Christopher David Beadle ,  Manuel Javier Cases-Thomas ,  Barry Peter Clark ,  Peter Thaddeus Gallagher ,  John Joseph Masters ,  Graham Henry Timms ,  Magnus Wilhelm Walter ,  Maria Ann Whatton ,  Virginia Ann Wood ,  Jeremy Gilmore

发明人： Christopher David Beadle ,  Manuel Javier Cases-Thomas ,  Barry Peter Clark ,  Peter Thaddeus Gallagher ,  John Joseph Masters ,  Graham Henry Timms ,  Magnus Wilhelm Walter ,  Maria Ann Whatton ,  Virginia Ann Wood ,  Jeremy Gilmore

IPC分类号： C07D207/00 ,  A61K31/40 ,  C07D295/00 ,  A01N43/36

CPC分类号： C07D207/14 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

摘要： The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, which are useful for the inhibition of the uptake of one or more physiologically active monoamines (serotonin, norepinephrine, and dopamine).

摘要翻译： 本发明提供式（I）化合物及其药学上可接受的盐，其可用于抑制一种或多种生理活性单胺（5-羟色胺，去甲肾上腺素和多巴胺）摄取。