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    Thiazole Compounds and Their Use as PGD2 Antagonists
    2.
    发明申请
    Thiazole Compounds and Their Use as PGD2 Antagonists 审中-公开
    噻唑化合物及其用作PGD2拮抗剂

    公开(公告)号：US20090221604A1

    公开(公告)日：2009-09-03

    申请号：US12065756

    申请日：2006-09-08

    申请人： Neil Victor Harris ,  George Hynd ,  Sophie Gardan

    发明人： Neil Victor Harris ,  George Hynd ,  Sophie Gardan

    IPC分类号： A61K31/496 ,  C07D417/04 ,  A61P35/00 ,  A61P17/00 ,  A61P11/06

    CPC分类号： C07D277/42 ,  C07D277/56 ,  C07D417/04

    摘要： A compound for use as a PGD2 antagonist is of structural formula [1] in which: A represents a fully saturated or partially unsaturated monocyclic 5-7 membered ring containing one or two nitrogen atoms; B represents a direct bond, an optionally substituted methylene group, an optionally substituted nitrogen atom, oxygen, or S(O)n, where n=0, 1, or 2; L represents a direct bond, or an optionally substituted alkylene or alkenylene group; R1 represents an optionally substituted aryl or heteroaryl group, or an optionally substituted aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group; R2 represents an optionally substituted aryl or heteroaryl group, or an optionally substituted aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group; X represents a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, sulfonic acid or a group of formula C(═O)NHSO2Y or SO2NHC(═O)Y; and Y represents an optionally substituted aryl or heteroaryl group or an optionally substituted alkyl or cycloalkyl group; or a N-oxide, pharmaceutically acceptable salt, solvate or prodrug thereof.

    摘要翻译： 用作PGD 2拮抗剂的化合物是结构式[1]，其中：A表示含有一个或两个氮原子的完全饱和或部分不饱和的单环5-7元环; B表示直接键，任选取代的亚甲基，任选取代的氮原子，氧或S（O）n，其中n = 0,1或2; L表示直接键或任选取代的亚烷基或亚烯基; R 1表示任选取代的芳基或杂芳基，或任选取代的芳基稠合 - 杂环烷基，杂芳基 - 稠合 - 环烷基，杂芳基 - 稠合 - 杂环烷基或芳基 - 稠合环烷基; R 2表示任选取代的芳基或杂芳基，或任选取代的芳基稠合 - 杂环烷基，杂芳基 - 稠合 - 环烷基，杂芳基 - 稠合 - 杂环烷基或芳基 - 稠合环烷基; X表示羧酸，四唑，3-羟基异恶唑，异羟肟酸，次膦酸盐，膦酸盐，膦酰胺，磺酸或式C（-O）NHSO 2 Y或SO 2 NHC（-O）Y的基团; 并且Y表示任选取代的芳基或杂芳基或任选取代的烷基或环烷基; 或其N-氧化物，药学上可接受的盐，溶剂合物或前药。

    Substituted tetrahydroisoquinolines
    6.
    发明授权
    Substituted tetrahydroisoquinolines 失效
    取代的四氢异喹啉

    公开(公告)号：US07211586B2

    公开(公告)日：2007-05-01

    申请号：US10715662

    申请日：2003-11-18

    申请人： Garry Fenton ,  Neil Victor Harris

    发明人： Garry Fenton ,  Neil Victor Harris

    IPC分类号： A61K31/4709 ,  A61K31/47 ,  C07D217/12

    CPC分类号： C07D413/06 ,  C07D217/06 ,  C07D217/16 ,  C07D413/14

    摘要： The invention is directed to physiologically active compounds of formula (I): wherein: R1 represents optionally substituted aryl, optionally substituted heteroaryl, R3NH—Ar1—L2— or R3—NH—C(═O)—NH—Ar2—L2—; R3 represents aryl or heteroaryl; Ar1 represents a saturated, partially saturated or fully unsaturated 8- to 10-membered bicyclic ring system containing at least one heteroatom selected from O, S or N; Ar2 represents aryldiyl or heteroaryldiyl; L1 represents a linkage, such as an alkylene linkage; L2 represents an alkylene chain linkage; R2 represents hydrogen, halogen, C1-4alkyl or C1-4alkoxy; and Y is carboxy or an acid bioisostere; but excluding compounds where an oxygen, nitrogen or sulfur atom is attached directly to a carbon carbon multiple bond of an alkenylene or alkynylene residue; and the corresponding N-oxides and ester prodrugs thereof, and the pharmaceutically acceptable salts and solvates of such compounds, and the N-oxides and ester prodrugs thereof. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (α4β1).

    摘要翻译： 本发明涉及式（I）的生理活性化合物：其中：R 1表示任选取代的芳基，任选取代的杂芳基，R 3 NH-Ar 1 - 或 - R 3 -NH-C（ - ） - -NH-Ar 2 -L 2 - ; R 3表示芳基或杂芳基; Ar 1表示含有至少一个选自O，S或N的杂原子的饱和的，部分饱和的或完全不饱和的8至10元双环体系; Ar 2代表芳基二基或杂芳基二基; L 1表示连接，例如亚烷基键; L 2代表亚烷基链键; R 2表示氢，卤素，C 1-4烷基或C 1-4烷氧基; Y为羧基或酸式生物电子等排体; 但不包括其中氧，氮或硫原子直接连接到亚烯基或亚炔基残基的碳碳多重键上的化合物; 和其相应的N-氧化物和酯前体药物，以及这些化合物的药学上可接受的盐和溶剂化物，及其N-氧化物和酯前体药物。 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 alkanoic acids
    7.
    发明授权
    Substituted alkanoic acids 失效
    取代的链烷酸

    公开(公告)号：US07166616B2

    公开(公告)日：2007-01-23

    申请号：US10427598

    申请日：2003-05-01

    申请人： Neil Victor Harris ,  Garry Fenton

    发明人： Neil Victor Harris ,  Garry Fenton

    IPC分类号： C07D263/58 ,  C07D261/02 ,  A61K31/423 ,  A61K31/445

    CPC分类号： C07D263/58 ,  A61K31/423 ,  C07C275/42 ,  C07C2601/08 ,  C07C2602/08 ,  C07D413/12

    摘要： The invention is directed to physiologically active compounds of general formula (I): wherein: represents (i) a saturated 3 to 6 membered carbocycle, optionally substituted by one or more alkyl groups, (ii) indanyl or (iii) a saturated 4 to 6 membered heterocyclic ring; R1 represents R3Z1-Het- or R4N(R5)—C(═O)—NH—Ar1—; L1 represents an —R6—R7— linkage; R2 represents hydrogen, halogen, lower alkyl or lower alkoxy; L2 represents an alkylene linkage; Y is carboxy or an acid bioisostere; and their corresponding N-oxides or prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their corresponding N-oxides or 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 (α4β1).

    摘要翻译： 本发明涉及通式（I）的生理活性化合物：其中：（i）饱和的3至6元碳环，任选被一个或多个烷基取代，（ii）茚满基或（iii）饱和的4至 6元杂环; R 1表示R 3 Z 1或H 4 - 或R 4 N（R 5） （O）-NH-Ar 1 - ; L 1表示-R 6-6R 7 - 键; R 2表示氢，卤素，低级烷基或低级烷氧基; L 2表示亚烷基键; Y是羧基或酸生物电子等排体; 及其相应的N-氧化物或前体药物，以及这些化合物的药学上可接受的盐和溶剂合物及其相应的N-氧化物或前体药物。 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 bicyclic heteroaryl compounds and their use as integrin antagonists
    8.
    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
    9.
    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。

    Substituted &bgr;-alanines
    10.
    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。