公开(公告)号：US20080004330A1

公开(公告)日：2008-01-03

申请号：US11568641

申请日：2005-05-19

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

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

IPC分类号： A61K31/4025 ,  A61K31/40 ,  A61P25/00 ,  A61P25/24 ,  C07D207/06 ,  C07D405/12

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： 本发明提供其中A为（1），（2），（3），（4），（5），（6）或（7）的式（I）化合物，其中R 1，R 7， SUB> 1 在本文中定义。 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：US20060270713A1

公开(公告)日：2006-11-30

申请号：US10558626

申请日：2004-05-11

申请人： Christopher Beadle ,  Manuel Casesthomas ,  Barry Clark ,  Peter Gallagher ,  John Masters ,  Graham Timms ,  Magnus Walter ,  Maria Whatton ,  Virginia Wood ,  Jeremy Gilmore

发明人： Christopher Beadle ,  Manuel Casesthomas ,  Barry Clark ,  Peter Gallagher ,  John Masters ,  Graham Timms ,  Magnus Walter ,  Maria Whatton ,  Virginia Wood ,  Jeremy Gilmore

IPC分类号： A61K31/4439 ,  A61K31/416 ,  A61K31/40 ,  C07D403/02

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).

公开(公告)号：US20070066663A1

公开(公告)日：2007-03-22

申请号：US10558588

申请日：2004-05-25

申请人： Christopher Beadle ,  Manuel Cases-Thomas ,  Barry Clark ,  Peter Gallagher ,  John Masters ,  Graham Timms ,  Magnus Walter ,  Maria Whatton ,  Virginia Wood ,  Jeremy Gilmore

发明人： Christopher Beadle ,  Manuel Cases-Thomas ,  Barry Clark ,  Peter Gallagher ,  John Masters ,  Graham Timms ,  Magnus Walter ,  Maria Whatton ,  Virginia Wood ,  Jeremy Gilmore

IPC分类号： A61K31/41

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：US20070093526A1

公开(公告)日：2007-04-26

申请号：US10597795

申请日：2005-02-11

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

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

IPC分类号： A61K31/4545 ,  A61K31/454 ,  C07D403/02 ,  C07D401/02

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：US20060058360A1

公开(公告)日：2006-03-16

申请号：US10532765

申请日：2003-10-24

申请人： Serge Boulet ,  Sandra Filla ,  Peter Gallagher ,  Kevin Hudziak ,  Anette Johansson ,  Rushad Karanjawala ,  John Masters ,  Brian Mathes ,  Richard Rathmell ,  Maria Whatton ,  Victor Matassa ,  Chad Wolfe

发明人： Serge Boulet ,  Sandra Filla ,  Peter Gallagher ,  Kevin Hudziak ,  Anette Johansson ,  Rushad Karanjawala ,  John Masters ,  Brian Mathes ,  Richard Rathmell ,  Maria Whatton ,  Victor Matassa ,  Chad Wolfe

IPC分类号： A61K31/428 ,  A61K31/425 ,  C07D277/62 ,  C07D275/06

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 —)— 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：US20060014779A1

公开(公告)日：2006-01-19

申请号：US10532657

申请日：2003-10-24

申请人： Serge Boulet ,  Ann Filla ,  Peter Gallagher ,  Kevin Hudziak ,  Anette Johansson ,  Rushad Karanjawla ,  John Masters ,  Victor Matassa ,  Brian Mathes ,  Richard Rathmell ,  Maria Whatton ,  Chad Wolfe

发明人： Serge Boulet ,  Ann Filla ,  Peter Gallagher ,  Kevin Hudziak ,  Anette Johansson ,  Rushad Karanjawla ,  John Masters ,  Victor Matassa ,  Brian Mathes ,  Richard Rathmell ,  Maria Whatton ,  Chad Wolfe

IPC分类号： A61K31/4745 ,  A61K31/4743 ,  A61K31/4704 ,  A61K31/428 ,  A61K31/423

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：US20060079554A1

公开(公告)日：2006-04-13

申请号：US10536295

申请日：2003-11-25

申请人： Peter Barry ,  Manuel Cases-Thomas ,  Peter Gallagher ,  Jeremy Gilmore ,  John Masters ,  Graham Timms ,  Maria Whatton ,  Virginia Wood

发明人： Peter Barry ,  Manuel Cases-Thomas ,  Peter Gallagher ,  Jeremy Gilmore ,  John Masters ,  Graham Timms ,  Maria Whatton ,  Virginia Wood

IPC分类号： A61K31/445 ,  C07D211/56

CPC分类号： C07D405/12 ,  C07D211/58

摘要： N,N-disubstituted 4-amino-piperidines of the general Formula (I) are inhibitors of the uptake of serotonin and/or norepinephrine and/or dopamine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system.

摘要翻译： 通式（I）的N，N-二取代的4-氨基 - 哌啶是5-羟色胺和/或去甲肾上腺素和/或多巴胺摄取的抑制剂。 因此，它们可用于治疗中枢和/或周围神经系统的病症。

公开(公告)号：US20060258654A1

公开(公告)日：2006-11-16

申请号：US10567639

申请日：2004-08-09

申请人： Barry Clark ,  Peter Gallagher

发明人： Barry Clark ,  Peter Gallagher

IPC分类号： A61K31/5377 ,  C07D413/02

CPC分类号： C07D413/12

摘要： The invention relates to compounds of formula (I): wherein R, R1, R2 and X are defined herein, their preparation, and their use as pharmaceuticals.

摘要翻译： 本发明涉及式（I）化合物：其中R，R 1，R 2和X在本文中定义，其制备及其作为药物的用途。

公开(公告)号：US20060035894A1

公开(公告)日：2006-02-16

申请号：US10524650

申请日：2003-08-18

申请人： Magnus Walter ,  Barry Clark ,  Peter Gallagher ,  Helen Haughton ,  Helene Rudyk

发明人： Magnus Walter ,  Barry Clark ,  Peter Gallagher ,  Helen Haughton ,  Helene Rudyk

IPC分类号： A61K31/5377 ,  C07D413/02 ,  A61K31/535

CPC分类号： C07D265/30

摘要： Compounds of formula (I): wherein A is S or O; R is H; Ar is an optionally substituted phenyl group; X is an optionally substituted phenyl group, a C1-C4 alkyl, a C3-C6 cycloalkyl group or a CH2(C3-C6 cycloalkyl) group; R′ is H or C1-C4 alkyl; and each R1 is independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof are selective inhibitors of norepinephrine reuptake.

摘要翻译： 式（I）的化合物：其中A是S或O; R为H; Ar是任选取代的苯基; X是任选取代的苯基，C 1 -C 4烷基，C 3 -C 6亚烷基， 环烷基或CH 2（C 3 -C 6环烷基）基团; R'是H或C 1 -C 4烷基; 且每个R 1独立地为H或C 1 -C 4烷基; 和其药学上可接受的盐是去甲肾上腺素再摄取的选择性抑制剂。

公开(公告)号：US20070060585A1

公开(公告)日：2007-03-15

申请号：US10575469

申请日：2004-12-10

申请人： Peter Gallagher ,  Carlos Lamas-Peteira ,  Francisco Agejas-Chicharro

发明人： Peter Gallagher ,  Carlos Lamas-Peteira ,  Francisco Agejas-Chicharro

IPC分类号： A61K31/5377 ,  A61K31/5375 ,  C07D413/02

CPC分类号： C07D265/30 ,  C07D295/027 ,  C07D295/192 ,  C07D401/10

摘要： Compounds of the general formula (I) are inhibitors of the reuptake of norepinephrine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system.

摘要翻译： 通式（I）的化合物是去甲肾上腺素再摄取的抑制剂。 因此，它们可用于治疗中枢和/或周围神经系统的病症。