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    Indole-amide derivatives and their use as glycogen phosphorylase inhibitors
    1.
    发明授权
    Indole-amide derivatives and their use as glycogen phosphorylase inhibitors 失效
    吲哚酰胺衍生物及其作为糖原磷酸化酶抑制剂的用途

    公开(公告)号：US07169927B2

    公开(公告)日：2007-01-30

    申请号：US10506748

    申请日：2003-03-04

    申请人： Alan Martin Birch ,  Andrew David Morley

    发明人： Alan Martin Birch ,  Andrew David Morley

    IPC分类号： C07D215/38 ,  C07D217/02

    CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D417/14

    摘要： Heterocyclic amides of formula (1) wherein: is a single or double bond; A is phenylene or heteroarylene; m is 0, 1 or 2; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R4 is independently selected from for example hydrogen, halo, nitro, cyano, hydroxy, C1-4alkyl, and C1-4alkanoyl; R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.

    摘要翻译： 式（1）的杂环酰胺其中：是单键或双键; A是亚苯基或亚杂芳基; m为0,1或2; n为0,1或2; R 1选自例如卤素，硝基，氰基，羟基，羧基; R 2是氢，羟基或羧基; R 3选自例如氢，羟基，芳基，杂环基和C 1-4烷基（任选被1或2个R 8取代） 组）; R 4独立地选自例如氢，卤素，硝基，氰基，羟基，C 1-4烷基和C 1-4烷基。 烷酰基; R 8选自例如羟基，-COCOOR 9，-C（O）N（R 9）（R 10） ），-NHC（O）R 9，（R 9）（R 10）N - 和-COOR 9 ; R 9和R 10选自例如氢，羟基，C 1-4烷基（任选被1或2个R SUP取代 > 13 ）; R 13选自羟基，卤素，三卤代甲基和C 1-4烷氧基; 或其药学上可接受的盐或前体药物; 具有糖原磷酸化酶抑制活性，因此具有与增加的糖原磷酸化酶活性相关的疾病状态的治疗价值。 描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。

    Heterocyclic amide derivatives as inhibitors of glycogen phosphorylase
    2.
    发明授权
    Heterocyclic amide derivatives as inhibitors of glycogen phosphorylase 失效
    杂环酰胺衍生物作为糖原磷酸化酶的抑制剂

    公开(公告)号：US07276517B2

    公开(公告)日：2007-10-02

    申请号：US11463144

    申请日：2006-08-08

    申请人： Alan Martin Birch ,  Andrew David Morley ,  Andrew Stocker ,  Paul Robert Owen Whittamore

    发明人： Alan Martin Birch ,  Andrew David Morley ,  Andrew Stocker ,  Paul Robert Owen Whittamore

    IPC分类号： A61K31/4375 ,  C07D471/04

    CPC分类号： C07D495/04

    摘要： Heterocyclic amides of formula (1) wherein: X is N or CH; R4 and R5 together are either —S—C(R6)═C(R7)— or —C(R7)═C(R6)—S—; R6 and R7 are independently selected from, for example hydrogen, halo and C1-4alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof, possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.

    摘要翻译： 式（1）的杂环酰胺其中：X是N或CH; R 4和R 5一起是-SC（R 6）-C（R 7） - 或 -C（R 7）C（R 6）-S-; R 6和R 7独立地选自，例如氢，卤素和C 1-4烷基; A是亚苯基或亚杂芳基; n为0,1或2; R 1选自例如卤素，硝基，氰基，羟基，羧基; R 2是氢，羟基或羧基; R 3选自例如氢，羟基，芳基，杂环基和C 1-4烷基（任选被1或2个R 8取代） 组）; R 8选自例如羟基，-COCOOR 9，-C（O）N（R 9）（R 10） ），-NHC（O）R 9，（R 9）（R 10）N - 和-COOR 9 ; R 9和R 10选自例如氢，羟基，C 1-4烷基（任选被1或2个R SUP取代 > 13 ）; R 13选自羟基，卤素，三卤代甲基和C 1-4烷氧基; 或其药学上可接受的盐或前药具有糖原磷酸化酶抑制活性，因此在治疗与增加的糖原磷酸化酶活性相关的疾病状态方面具有价值。 描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。

    Heterocyclic amide derivatives as inhibitors of glycogen phoshorylase
    3.
    发明授权
    Heterocyclic amide derivatives as inhibitors of glycogen phoshorylase 失效
    杂环酰胺衍生物作为糖原磷酸化酶的抑制剂

    公开(公告)号：US07129249B2

    公开(公告)日：2006-10-31

    申请号：US10506741

    申请日：2003-03-04

    申请人： Alan Martin Birch ,  Andrew David Morley ,  Andrew Stocker ,  Paul Robert Owen Whittamore

    发明人： Alan Martin Birch ,  Andrew David Morley ,  Andrew Stocker ,  Paul Robert Owen Whittamore

    IPC分类号： A61K31/4704 ,  A61K31/4375 ,  C07D215/38 ,  C07D471/04

    CPC分类号： C07D495/04

    摘要： Heterocyclic amides of formula (1) wherein: X is N or CH; R4 and R5 together are either —S—C(R6)═C(R7)— or —C(R7)═C(R6)—S—; R6 and R7 are independently selected from, for example hydrogen, halo and C1-4alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.

    摘要翻译： 式（1）的杂环酰胺其中：X是N或CH; R 4和R 5一起是-SC（R 6）-C（R 7） - 或 -C（R 7）C（R 6）-S-; R 6和R 7独立地选自，例如氢，卤素和C 1-4烷基; A是亚苯基或亚杂芳基; n为0,1或2; R 1选自例如卤素，硝基，氰基，羟基，羧基; R 2是氢，羟基或羧基; R 3选自例如氢，羟基，芳基，杂环基和C 1-4烷基（任选被1或2个R 8取代） 组）; R 8选自例如羟基，-COCOOR 9，-C（O）N（R 9）（R 10） ），-NHC（O）R 9，（R 9）（R 10）N - 和-COOR 9 ; R 9和R 10选自例如氢，羟基，C 1-4烷基（任选被1或2个R SUP取代 > 13 ）; R 13选自羟基，卤素，三卤代甲基和C 1-4烷氧基; 或其药学上可接受的盐或前体药物; 具有糖原磷酸化酶抑制活性，因此具有与增加的糖原磷酸化酶活性相关的疾病状态的治疗价值。 描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。

    Substituted benzoxazole compounds
    8.
    发明授权
    Substituted benzoxazole compounds 有权
    取代苯并恶唑化合物

    公开(公告)号：US06593354B2

    公开(公告)日：2003-07-15

    申请号：US09925110

    申请日：2001-08-09

    申请人： David Edward Clark ,  Paul Robert Eastwood ,  Neil Victor Harris ,  Clive McCarthy ,  Andrew David Morley ,  Stephen Dennis Pickett

    发明人： David Edward Clark ,  Paul Robert Eastwood ,  Neil Victor Harris ,  Clive McCarthy ,  Andrew David Morley ,  Stephen Dennis Pickett

    IPC分类号： A61K31423

    CPC分类号： C07D263/58 ,  C07D235/30

    摘要： The invention is directed to physiologically active compounds of formula (Ia): wherein R1 is optionally substituted aryl or optionally substituted heteroaryl; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R3 is alkylene, alkenylene or alkynylene; R5 is hydrogen or lower alkyl; L2 is optionally substituted alkylene or alkenylene; Y is carboxy; and Z1 is NR5; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates (e.g. hydrates) of such compounds and their N-oxides and prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (&agr;4&bgr;1).

    摘要翻译： 本发明涉及式（Ia）的生理活性化合物：其中R 1是任选取代的芳基或任选取代的杂芳基; R2是氢，卤素，低级烷基或低级烷氧基; R3是亚烷基，亚烯基或亚炔基; R5是氢或低级烷基; L2是任选取代的亚烷基或亚烯基; Y是羧基; Z1为NR5; 和相应的N-氧化物及其前药; 和这些化合物的药学上可接受的盐和溶剂合物（例如水合物）及其N-氧化物和前药。 这些化合物具有有价值的药物性质，特别是调节VCAM-1和纤连蛋白与整联蛋白VLA-4（α4β1）的相互作用的能力。