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    Novel compounds
    4.
    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

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

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

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

    CPC classification number: C07D207/14

    Abstract: 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.

    Piperazine derivatives which exhibit activity as serotonin and noradrenaline re-uptake inhibitors
    5.
    发明申请
    Piperazine derivatives which exhibit activity as serotonin and noradrenaline re-uptake inhibitors 审中-公开

    公开(公告)号：US20070105870A1

    公开(公告)日：2007-05-10

    申请号：US10586029

    申请日：2005-01-03

    Applicant: Gerwyn Bish ,  Alan Brown ,  Paul Fish ,  Michael Fray ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Whitlock

    Inventor： Gerwyn Bish ,  Alan Brown ,  Paul Fish ,  Michael Fray ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Whitlock

    IPC: A61K31/495 ,  C07D241/04

    CPC classification number: C07D295/205 ,  C07D249/18 ,  C07D295/073 ,  C07D295/096

    Abstract: A compound of formula (I), wherein R1 is H; R2 is aryl, het, C3-8cycloalkyl, C1-6alkyl, (CH2)2aryl or R4, wherein each of the cycloalkyl, aryl, het and R4 groups is optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, OH, halo, CF3, OCF3, OCHF2, O(CH2)yCF3, CN, CONH2, CON(H)C1-6alkyl, CON(C1-6alkyl)2, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl, C1-4alkoxy-C1-4alkoxy, SCF3, C1-6alkyISO2, C1-4alkyl-S-C1-4alkyl, C1-4alkyl-S—, C1-4alkyINR10R11 and NR10R11; or R1 and R2, together with the carbon atom to which they are bound, form a 5- or 6-membered carbocycle or a 5- or 6-membered heterocycle containing at least one N, O or S heteroatom; R3 is aryl, het or R4, each optionally substituted by at least one substituent independently selected from C1-6-alkyl, C1-6-alkoxy, het, OH, halo, CF3, OCF3, OCHF2, O(CH2)yCF3, CN, CONH2, CON(H)C1-6alkyl, CON(C1-6alkyl)2, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl, C1-4alkoxy-C1-4alkoxy, SCF3, C1-6alkyISO2, C1-4alkyl-S-C1-4alkyl, C1-4alkyl-S—, C1-4alkylNR10R11and NR10R11; R4 is a phenyl group fused to a 5- or 6 membered carbocycle, or a phenyl group fused to a 5- or 6-membered heterocycle containing at least one N, O or S heteroatom; R5 is H or C1-6alkyl; R10 and R11 are the same or different and are independently H or C1-4alkyl; A is a C1-3alkylene chain which is optionally substituted by OH, C1-4alkyl or C1-4alkoxy; x is an integer from 1 to 3; y is 1 or 2; z is an integer from 1 to 3; aryl is phenyl, naphthyl, anthracyl or phenanthryl; and het is 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 carbocycle or a second 4, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom.

    Novel compounds
    6.
    发明申请
    Novel compounds 失效
    新型化合物

    公开(公告)号：US20060111429A1

    公开(公告)日：2006-05-25

    申请号：US11280128

    申请日：2005-11-15

    Applicant: Paul Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Whitlock

    Inventor： Paul Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Whitlock

    IPC: A61K31/40 ,  C07D207/10

    CPC classification number: C07D207/14 ,  C07D405/12

    Abstract: 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.

    Abstract translation: 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。

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