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31 条记录 (耗时 0.039 秒)

    Substituted benzoxazole compounds
    16.
    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。

    Pyrazine derivatives useful as adenosine receptor antagonists
    20.
    发明授权
    Pyrazine derivatives useful as adenosine receptor antagonists 失效
    用作腺苷受体拮抗剂的吡嗪衍生物

    公开(公告)号：US07790728B2

    公开(公告)日：2010-09-07

    申请号：US11997048

    申请日：2006-07-25

    申请人： Bernat Vidal Juan ,  Christina Esteve Trias ,  Lidia Soca Pueyo ,  Paul Robert Eastwood

    发明人： Bernat Vidal Juan ,  Christina Esteve Trias ,  Lidia Soca Pueyo ,  Paul Robert Eastwood

    IPC分类号： A61K31/4965

    CPC分类号： C07D487/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

    摘要： The present disclosure relates to a compound of formula (I) wherein: A is an optionally substituted monocyclic or polycyclic aryl or heteroaryl group; B is an optionally substituted monocyclic nitrogen-containing heteroaryl group; and either a) R1 and R2 are chosen from a hydrogen atom and specified substituents, or b) R2, R1 and the —NH— group to which R1 is attached, form a moiety chosen from the moiety of formulae (IIa) and (IIb): or a pharmaceutically acceptable salt thereof, or a N-oxide thereof. The present disclosure also relates to a method for treating a subject afflicted with a pathological condition or disease susceptible to amelioration by antagonism of the A2B adenosine receptor.

    摘要翻译： 本发明涉及式（I）化合物，其中：A为任选取代的单环或多环芳基或杂芳基; B是任选取代的单环含氮杂芳基; 和a）R 1和R 2选自氢原子和特定取代基，或b）R 2，R 1和R 1连接的-NH-基团，形成选自式（IIa）和（IIb）部分的部分 ）：或其药学上可接受的盐或其N-氧化物。 本公开还涉及用于治疗受到A2B腺苷受体拮抗作用而易于改善的病理状况或疾病的受试者的治疗方法。