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    Compounds
    3.
    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.

    Amides useful as monoamine re-uptake inhibitors
    4.
    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。

    Hydroxamic acid derivatives as matrix metalloprotease (MMP) inhibitors
    7.
    发明授权
    Hydroxamic acid derivatives as matrix metalloprotease (MMP) inhibitors 有权
    羟肟酸衍生物作为基质金属蛋白酶（MMP）抑制剂

    公开(公告)号：US06387931B1

    公开(公告)日：2002-05-14

    申请号：US09423359

    申请日：2001-10-12

    申请人： Kevin Neil Dack ,  Gavin Alistair Whitlock

    发明人： Kevin Neil Dack ,  Gavin Alistair Whitlock

    IPC分类号： A61K31445

    CPC分类号： C07D401/10 ,  C07D211/16 ,  C07D211/22 ,  C07D211/70 ,  C07D405/10 ,  C07D405/12 ,  Y02P20/55

    摘要： Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diseases.

    摘要翻译： 式（I）化合物或其药学或兽医学上可接受的盐，或任一实体的药学上或兽医学上可接受的溶剂合物，其中虚线代表任选的键; A是C或CH; B是CH 2，O或不存在; R 1和R 2各自独立地选自氢，任选被C 1至C 4烷氧基或苯基取代的C 1 -C 6烷基和C 1至C 6烯基; 或者与它们所连接的碳原子一起形成C3-C6环烷基，其任选地并入选自O，SO，SO 2和NR 6的杂原子，或任选地苯并稠合; R3是氢，卤素，R7或OR7; R4是氢，C1-C4烷基，C1-C4烷氧基，三氟甲基或卤素; R6是氢或C1-C4烷基; R7是任选取代的单环或双环环系; m为1或2; 且n为0,1或2; 条件是当A为C时B不为O; 是用于治疗组织溃疡，伤口修复和皮肤疾病的MMP抑制剂。

    Hydroxamic acid derivatives as matrix metalloprotease (MMP) inhibitors
    10.
    发明授权
    Hydroxamic acid derivatives as matrix metalloprotease (MMP) inhibitors 失效

    公开(公告)号：US06495568B1

    公开(公告)日：2002-12-17

    申请号：US09423359

    申请日：2001-10-12

    申请人： Kevin Neil Dack ,  Gavin Alistair Whitlock

    发明人： Kevin Neil Dack ,  Gavin Alistair Whitlock

    IPC分类号： A61K31445

    CPC分类号： C07D401/10 ,  C07D211/16 ,  C07D211/22 ,  C07D211/70 ,  C07D405/10 ,  C07D405/12 ,  Y02P20/55

    摘要： Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diseases.