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    Amide compounds useful in therapy
    2.
    发明授权
    Amide compounds useful in therapy 失效
    酰胺化合物可用于治疗

    公开(公告)号：US08232269B2

    公开(公告)日：2012-07-31

    申请号：US12561398

    申请日：2009-09-17

    申请人： Karl Richard Gibson ,  Martin Peter Green ,  Toby James Underwood ,  Florian Wakenhut

    发明人： Karl Richard Gibson ,  Martin Peter Green ,  Toby James Underwood ,  Florian Wakenhut

    IPC分类号： A61K31/397 ,  A61K31/415 ,  A61K31/506 ,  A61K31/4184 ,  A61K31/454 ,  C07D231/20 ,  C07D205/04 ,  C07D403/12 ,  C07D235/02 ,  C07D401/12

    CPC分类号： C07D231/14 ,  C07D231/16 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12 ,  C07D487/04

    摘要： A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1 and R2 each independently represent H, halogen, CF3, C1-3 alkyl or C1-3 alkoxy; R3 represents C1-6 alkyl, C3-6 cycloalkyl, phenyl (optionally substituted by one or more substituents each independently selected from Ra) or Het (optionally substituted by one or more substituents each independently selected from OH, oxo, or C1-4 alkyl); R4 represents H or C1-3 alkyl; R5 represents C1-6 alkyl (optionally substituted by one or more substituents each independently selected from Rb), C3-6 cycloalkyl (optionally substituted by one or more substituents each independently selected from oxo or OH), or Het2 (optionally substituted by one or more substituents each independently selected from Rd); oxygen atom or 1 sulphur atom, or (c) 1 oxygen atom or 1 sulphur atom, (optionally substituted by one or more substituents each independently selected from OH, oxo or C1-4 alkyl); and R6 represents C1-3 alkyl (optionally substituted by one or more substituents each independently selected from Rf), C3-5 cycloalkyl (optionally substituted by one or more halogen), CN or halogen; where Rf represents halogen or phenyl: and compositions, processes for the preparation, and uses thereof, e.g. in the treatment of endometriosis or uterine fibroids.

    摘要翻译： 式（I）的化合物或其药学上可接受的盐或溶剂合物，其中R 1和R 2各自独立地表示H，卤素，CF 3，C 1-3烷基或C 1-3烷氧基; R 3表示C 1-6烷基，C 3-6环烷基，苯基（任选被一个或多个各自独立地选自Ra的取代基）或Het（任选被一个或多个各自独立地选自OH，氧代或C 1-4烷基的取代基取代） ）; R 4表示H或C 1-3烷基; R 5表示C 1-6烷基（任选被一个或多个独立地选自Rb的取代基取代），C 3-6环烷基（任选地被一个或多个独立地选自氧代或OH的取代基取代）或Het2（任选被一个或多个 更多取代基，各自独立地选自Rd）; 氧原子或1个硫原子，或（c）1个氧原子或1个硫原子（任选被一个或多个独立地选自OH，氧代或C 1-4烷基的取代基取代）; 和R 6表示C 1-3烷基（任选被一个或多个独立地选自Rf的取代基取代），C3-5环烷基（任选被一个或多个卤素取代），CN或卤素; 其中R f表示卤素或苯基;和组合物，制备方法及其用途，例如， 治疗子宫内膜异位症或子宫肌瘤。

    Amide Compounds Useful in Therapy
    3.
    发明申请
    Amide Compounds Useful in Therapy 失效
    酰胺化合物可用于治疗

    公开(公告)号：US20100249091A1

    公开(公告)日：2010-09-30

    申请号：US12561398

    申请日：2009-09-17

    申请人： Karl Richard Gibson ,  Martin Peter Green ,  Toby James Underwood ,  Florian Wakenhut

    发明人： Karl Richard Gibson ,  Martin Peter Green ,  Toby James Underwood ,  Florian Wakenhut

    IPC分类号： A61K31/397 ,  C07D231/20 ,  A61K31/415 ,  C07D205/04 ,  C07D403/12 ,  A61K31/506 ,  C07D235/02 ,  A61K31/4184 ,  C07D401/12 ,  A61K31/454 ,  A61P35/00 ,  A61P29/00

    CPC分类号： C07D231/14 ,  C07D231/16 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12 ,  C07D487/04

    摘要： A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1 and R2 each independently represent H, halogen, CF3, C1-3 alkyl or C1-3 alkoxy; R3 represents C1-6 alkyl, C3-6 cycloalkyl, phenyl (optionally substituted by one or more substituents each independently selected from Ra) or Het (optionally substituted by one or more substituents each independently selected from OH, oxo, or C1-4 alkyl); R4 represents H or C1-3 alkyl; R5 represents C1-6 alkyl (optionally substituted by one or more substituents each independently selected from Rb), C3-6 cycloalkyl (optionally substituted by one or more substituents each independently selected from oxo or OH), or Het2 (optionally substituted by one or more substituents each independently selected from Rd); oxygen atom or 1 sulphur atom, or (c) 1 oxygen atom or 1 sulphur atom, (optionally substituted by one or more substituents each independently selected from OH, oxo or C1-4 alkyl); and R6 represents C1-3 alkyl (optionally substituted by one or more substituents each independently selected from Rf), C3-5 cycloalkyl (optionally substituted by one or more halogen), CN or halogen; where Rf represents halogen or phenyl: and compositions, processes for the preparation, and uses thereof, e.g. in the treatment of endometriosis or uterine fibroids

    摘要翻译： 式（I）的化合物或其药学上可接受的盐或溶剂合物，其中R 1和R 2各自独立地表示H，卤素，CF 3，C 1-3烷基或C 1-3烷氧基; R 3表示C 1-6烷基，C 3-6环烷基，苯基（任选被一个或多个各自独立地选自Ra的取代基）或Het（任选被一个或多个各自独立地选自OH，氧代或C 1-4烷基的取代基取代） ）; R 4表示H或C 1-3烷基; R 5表示C 1-6烷基（任选被一个或多个独立地选自Rb的取代基取代），C 3-6环烷基（任选地被一个或多个独立地选自氧代或OH的取代基取代）或Het2（任选被一个或多个 更多取代基，各自独立地选自Rd）; 氧原子或1个硫原子，或（c）1个氧原子或1个硫原子（任选被一个或多个独立地选自OH，氧代或C 1-4烷基的取代基取代）; 和R 6表示C 1-3烷基（任选被一个或多个独立地选自Rf的取代基取代），C3-5环烷基（任选被一个或多个卤素取代），CN或卤素; 其中R f表示卤素或苯基;和组合物，制备方法及其用途，例如， 治疗子宫内膜异位症或子宫肌瘤

    Novel compounds
    5.
    发明申请
    Novel compounds 失效

    公开(公告)号：US20050137229A1

    公开(公告)日：2005-06-23

    申请号：US10872160

    申请日：2004-06-17

    申请人： Paul Fish ,  Michael Fray ,  Deborah Lovering ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Whitlock

    发明人： Paul Fish ,  Michael Fray ,  Deborah Lovering ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Whitlock

    IPC分类号： A61P13/00 ,  A61P25/24 ,  A61P29/00 ,  C07D207/14 ,  C07D211/06 ,  A61K31/445 ,  C07D211/56

    CPC分类号： C07D207/14

    摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R1 is H, C1-6alkyl, —C(X)Y, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R2 is aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R3 is C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy —C1-6alkyl and C1-4alkyl-S—C1-4alkyl; X is S or O; Y is H, C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl; and n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral center. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.

    N-Pyrrolidin-3YL-Amide Derivatives As Serotonin and Noradrenalin Re-Uptake Inhibitors
    6.
    发明申请
    N-Pyrrolidin-3YL-Amide Derivatives As Serotonin and Noradrenalin Re-Uptake Inhibitors 审中-公开

    公开(公告)号：US20090239928A1

    公开(公告)日：2009-09-24

    申请号：US11721352

    申请日：2005-12-02

    申请人： Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut

    发明人： Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut

    IPC分类号： A61K31/40 ,  C07D207/14 ,  A61P13/00

    CPC分类号： C07D207/14

    摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R1 is H, C1-6alkyl, —C(A)D, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-8allkyl, C1-8alkoxy, OH, halo, CF3, OCHF2, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; A is S or O; D is H, C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl; R2 represents aryl1 or het1, each of which is substituted by at least one substituent independently selected from B, provided that when R2 is substituted by halo then it is also substituted with at least one other substituent independently selected from B other than halo; B represents aryl2, het2, Oaryl2, Ohet2, Sarl2, Shet2, SC1-6alkyl, halogen, CHF2, OCHF2, CF2CF3, CH2CF3, CF2CH3, aryl2-C1-4alkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl, C3-6cycloalkylC1-4alkoxy, C3-6cycloalkyl-O—C1-4 alkyl, C3-6cycloalkyl-C1-4alkoxy-C1-4alkyl, OC3-6cycloalkyl, SC3-6cycloalkyl; wherein the aryl2 and het2 groups are optionally substituted by at least one group selected from C1-6alkyl, C3-6cycloalkyl, C1-6alkoxy, OC3-6cycloalkyl, halo, CN, OH, CF3, CHF2, OCF3, OCHF2, hydroxyC1$alkyl, C1-4alkoxy-C1-4alkyl, SC1-6alkyl and SCF3; n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral centre; R3 is H, C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-6alkyl, aryl3, het3, aryl3-C1-4alkyl or het3-C1-4alkyl, wherein the C3-8cycloalkyl, aryl3 or het3 groups are optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, CN, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; at each occurrence aryl, aryl1, aryl2 and aryl3 independently represent phenyl, naphthyl, anthracyl or phenanthryl; het1 represents an aromatic 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to an aryl group; at each occurrence het, het2, and het3 independently represents an aromatic or non-aromatic 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6-membered carbocyclic group or a second 4-, 5- or 6membered heterocycle which contains at least one N, O or S heteroatom.

    Amides useful as monoamine re-uptake inhibitors
    7.
    发明授权
    Amides useful as monoamine re-uptake inhibitors 失效
    用作单胺再吸收抑制剂的酰胺

    公开(公告)号：US07122683B2

    公开(公告)日：2006-10-17

    申请号：US11280128

    申请日：2005-11-15

    申请人： Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock

    发明人： Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock

    IPC分类号： C07D207/14

    CPC分类号： C07D207/14 ,  C07D405/12

    摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R1, R2, R3 and R20 are each independently H, Cl, Br, F, I, CF3, OCF3, Me or Et; R4 is het or C3-7 cycloalkyl optionally substituted by C1-4 alkyl, C1-4 alkoxy, alkoxyalkyl containing 2 to 4 carbon atoms or —S—(C1-4 alkyl); a is 0 or 1; and het is a non-aromatic 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6-membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, wherein the het group is optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; provided that at least one of R1, R2 and R3 are other than H. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.

    摘要翻译： 式（I）的化合物及其药学和/或兽医学上可接受的衍生物，其中：R 1，R 2，R 3和R 3 各自独立地为H，Cl，Br，F，I，CF 3，OCF 3，Me或Et; R 4是H或任选被C 1-4烷基取代的C 3-7环烷基，C 1-4 - 烷氧基，含有2至4个碳原子的烷氧基烷基或-S-（C 1-4烷基）; a是0或1; 并且它是非芳族的4-，5-或6-元杂环，其含有至少一个N，O或S杂原子，任选地与5或6元碳环基团或第二个4-，5-或 其含有至少一个N，O或S杂原子的6元杂环，其中所述基团任选地被至少一个独立地选自C 1-8烷基，C 1- 8个烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6 C 1-4烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-S SC 1 -4 烷基; 条件是R 1，R 2和R 3中的至少一个不是H.本发明的化合物表现出作为血清素的活性 和去甲肾上腺素再摄取抑制剂，因此可用于各种治疗领域，例如尿失禁。

    Compounds
    8.
    发明授权
    Compounds 失效

    公开(公告)号：US07378436B2

    公开(公告)日：2008-05-27

    申请号：US10872160

    申请日：2004-06-17

    申请人： Paul Vincent Fish ,  Michael Jonathan Fray ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock ,  Mark David Andrews ,  Alan Daniel Brown ,  Mark Ian Lansdell

    发明人： Paul Vincent Fish ,  Michael Jonathan Fray ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock ,  Mark David Andrews ,  Alan Daniel Brown ,  Mark Ian Lansdell

    IPC分类号： A61K31/40 ,  C07D295/10

    CPC分类号： C07D207/14

    摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R1 is H, C1-6alkyl, —C(X)Y, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R2 is aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R3 is C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy —C1-6alkyl and C1-4alkyl-S—C1-4alkyl; X is S or O; Y is H, C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl; and n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral center. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.

    N-Pyrrolidin-3-YL-Amide Derivatives As Serotonin and Noradrenalin Re-Uptake Inhibitors
    10.
    发明申请
    N-Pyrrolidin-3-YL-Amide Derivatives As Serotonin and Noradrenalin Re-Uptake Inhibitors 审中-公开

    公开(公告)号：US20090239929A1

    公开(公告)日：2009-09-24

    申请号：US11721359

    申请日：2005-12-02

    申请人： Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut

    发明人： Paul Vincent Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut

    IPC分类号： A61K31/40 ,  C07D207/14 ,  A61P13/00 ,  A61P25/24 ,  A61P25/00 ,  A61P15/12

    CPC分类号： C07D207/14

    摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R1 is H, C1-6alkyl, —C(A)D, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted; A is S or O; D is H, C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl; aryl represents phenyl, naphthyl, anthracyl or phenanthryl; het represents an aromatic or non-aromatic 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6-membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom; R2 is aryl1 or het1, each optionally substituted; n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral centre; R3 is (CH2)aE, wherein a is 0, 1 or 2 and E is a group selected from: Formula (i) wherein: X is O, S, NR12, (CH2)v or a bond; b is 1, 2, 3 or 4; c is 1, 2 or 3; v is 1 or 2; R10 and 11 are each independently H or C1-4 alkyl; and R12 is H, 1-6 alkyl, C(O)C1-6 alkyl, SO2—C1-6alkyl; and wherein one or more pairs of hydrogen atoms on adjacent carbon or nitrogen atoms may be replaced by a corresponding number of double bonds, provided the ring system is not aromatic; Formula (ii) a carbocyclic spiro group containing 6 to 12 carbon atoms; Formula (iii) wherein: d is 1, 2, 3 or 4; a is 1, 2 or 3; f is 1 or 2; and R30 is H or C1-4alkyl; and wherein one or more pairs of hydrogen atoms on adjacent carbon atoms may be replaced by a corresponding number of double bonds, provided the ring system is not aromatic; Formula (iv) wherein: g is 0, 1, 2 or 3; J is NR40; and R40 is C(O)C1-6 alkyl, S02-C1-6alkyl; Formula (v) wherein: h is 0, 1, 2 or 3; and R50 is H, C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; Formula (vi) —CH(cyclopropane)2; Formula (vii) C1-6alkyl, substituted by at least one substituent; and Formula (viii) C3-8cycloalkyl-C1-6alkyl; wherein the C1-6alkyl moiety is substituted at any point other than at the junction with the C3-8cycloalkyl moiety, by at least one substituent. The compounds exhibit activity as both serotonin and/or noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.