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25 条记录 (耗时 0.032 秒)

    Substituted &bgr;-alanines
    1.
    发明授权
    Substituted &bgr;-alanines 有权
    取代的β-丙氨酸

    公开(公告)号：US06352977B1

    公开(公告)日：2002-03-05

    申请号：US09589825

    申请日：2000-06-08

    申请人： Peter Charles Astles ,  Neil Victor Harris ,  Andrew David Morley

    发明人： Peter Charles Astles ,  Neil Victor Harris ,  Andrew David Morley

    IPC分类号： C07C27542

    CPC分类号： C07D207/27 ,  C07C275/42

    摘要： The invention is directed to physiologically active compounds of general formula (I): wherein R1 is hydrogen, halogen, lower alkyl or lower alkoxy; X1, X2 and X6 independently represent N or CR2; and one of X3, X4 and X5 represents CR3 and the others independently represents N or CR2 where R2 is hydrogen, halogen, lower alkyl or lower alkoxy; and R3 represents a group —L1—(CH2)n—C(═O)—N(R4)—CH2—CH2—Y; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their 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： 本发明涉及通式（I）的生理活性化合物：其中R 1是氢，卤素，低级烷基或低级烷氧基; X1，X2和X6独立地表示N或CR2; X 3，X 4和X 5中的一个表示CR 3，其余的独立地表示N或CR 2，其中R 2为氢，卤素，低级烷基或低级烷氧基; 并且R 3表示基团-L 1 - （CH 2）n -C（= O）-N（R 4）-CH 2 -CH 2 -Y; 及其前药，以及这些化合物及其前药的药学上可接受的盐和溶剂合物。 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。

    Substituted benzoxazole compounds
    4.
    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。

    Substituted bicyclic heteroaryl compounds and their use as integrin antagonists
    5.
    发明授权
    Substituted bicyclic heteroaryl compounds and their use as integrin antagonists 有权
    取代的双环杂芳基化合物及其作为整联蛋白拮抗剂的用途

    公开(公告)号：US06706738B2

    公开(公告)日：2004-03-16

    申请号：US09975721

    申请日：2001-10-11

    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： A61K31443

    CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14

    摘要： The invention is directed to physiologically active compounds of general formula (I): R1Z1—Het—L1—Ar1—L2—Y  (I) wherein Het is an optionally substituted, saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring containing at least one heteroatom selected from O, S or N; R1 is optionally substituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl or heterocycloalkyl; Z1 represents a direct bond, an alkylene chain, NR4, O or S(O)n; L1 is an a —R5—R6— linkage where R5 is alkylene, alkenylene or alkynylene and R6 is a direct bond, cycloalkylene, heterocycloalkylene, arylene, heteroaryldiyl, —C(═Z3)—NR4—, —NR4—C(═Z3)—, —Z3—, —C(═O)—, —C(═NOR4)—, —NR4—, —NR4—C(═Z3)—NR4—, —SO2—NR4—, —NR4—SO2—, —O—C(═O)—, —C(═O)—O—, —NR4—C(═O)—O— or —O—C(═O)—NR4—; L2 is a direct bond; an optionally substituted alkylene, alkenylene, alkynylene, cycloalkenylene, cycloalkylene, heteroaryldiyl, heterocycloalkylene or arylene linkage; a —[C(═O)—N(R9)—C(R4)(R10)]p— linkage; a —Z4—R11— linkage; a —C(═O)—CH2—C(═O)— linkage; a —R11—Z4—R11— linkage; or a —L3—L4—L5— linkage; and Y is carboxy or an acid bioisostere; 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： 本发明涉及通式（I）的生理活性化合物：其中Het是任选取代的，饱和的，部分饱和的或完全不饱和的8至10元双环，其含有至少一个选自O，S或N的杂原子; R 1是任选取代的芳基，杂芳基，烷基，烯基，炔基，环烷基或杂环烷基; Z 1表示直接键，亚烷基链，NR 4，O或S（O）n; L 1是-R 5 -R 6 - 键，其中R 5是亚烷基，亚烯基或亚炔基，R 6是直接键，亚环烷基，亚杂环亚烷基，亚芳基，杂芳基二基，-C （= Z 3）-NR 4 - ， - NR 4 -C（= Z 3） - ， - Z 3 - ， - C（= O） - ， - -NR 4 - ， - NR 4 -C（= Z 3）-NR 4 - ， - SO 2 -NR 4 - ， - NR 4 -SO 2 - ， - OC（= O） - ， - C（= O）-O-，-NR 4 -C（= O）-O-或-OC（= O）-NR 4 - L 2是直接键; 亚烯基，亚炔基，亚环烯基，亚环烷基，杂芳基二基，杂环亚烷基或亚芳基键; a - [C（= O）-N（R 9）-C（R 4）（R 10）] p - 键; a -Z 4 -R 11 - 键; -C（= O）-CH 2 -C（= O） - 键; -R 11 -Z 4 -R 11 - 键; 或-L 3 -L 4 -L 5 - 键; Y为羧基或酸式生物电子等排体; 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。

    Substituted bicyclic compounds
    6.
    发明授权
    Substituted bicyclic compounds 有权
    取代的双环化合物

    公开(公告)号：US06562851B2

    公开(公告)日：2003-05-13

    申请号：US10002041

    申请日：2001-11-02

    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 ,  C07D413/12 ,  C07D413/14

    摘要： The invention is directed to physiologically active compounds of general formula (I): wherein Het is an optionally substituted, saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring system containing at least one heteroatom selected from O, S or N; R1 is optionally substituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl or heterocycloalkyl; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; Z1 is NR5; L1 is a —R6—R7— linkage (where R6 is alkylene, alkenylene or alkynylene and R7 is a direct bond, cycloalkylene, heterocycloalkylene, aryldiyl, heteroaryldiyl, —C(═Z3)—NR5—, —NR5—C(═Z3)—, —Z3—, —C(═O)—, —C(═NOR5)—, —NR5—, —NR5—C(═Z3)—NR5—, —SO2—NR5—, —NR5—SO2—, —O—C(═O)—, —C(═O)—O—, —NR5—C(═O)—O— or —O—C(═O)—NR5—); L2 is an alkylene chain substituted by hydroxy, oxo, —OR4, —O—C(═O)—R4, —N(R8)—C(═O)—R9, —N(R8)—C(═O)—OR9, —N(R8)—SO2—R9, or —NY3Y4; and Y is carboxy or an acid bioisostere; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates 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： 本发明涉及通式（I）的生理活性化合物：其中Het是含有至少一个选自O，S或N的杂原子的任选取代的，饱和的，部分饱和的或完全不饱和的8至10元双环体系; R 1是任选取代的芳基，杂芳基，烷基，烯基，炔基，环烷基或杂环烷基; R2是氢，卤素，低级烷基或低级烷氧基; Z1是NR5; L1是-R6-R7-键（其中R6是亚烷基，亚烯基或亚炔基，R7是直接键，亚环烷基，亚杂烷基亚烷基，芳基二基，杂芳基二基，-C（= Z3）-NR5-，-NR5-C（= Z3 ） - ， - Z3 - ， - （= O） - ， - （= NOR5） - ， - NR5-，-NR5-C（= Z3）-NR5-，-SO2-NR5-，-NR5-SO2- ，-OC（= O） - ， - C（= O）-O-，-NR 5 -C（= O）-O-或-OC（= O）-NR 5 - ）; L2是被羟基，氧代，-OR4，-OC（= O）-R4，-N（R8）-C（= O）-R9，-N（R8）-C（= O）-OR9取代的亚烷基链 ，-N（R 8）-SO 2 -R 9或-NY 3 Y 4; Y为羧基或酸式生物电子等排体; 和相应的N-氧化物及其前药; 和这些化合物及其N-氧化物和前药的药学上可接受的盐和溶剂化物。 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。