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39 条记录 (耗时 0.075 秒)

    Chemical compounds
    36.
    发明申请
    Chemical compounds 审中-公开
    化合物

    公开(公告)号：US20090018157A1

    公开(公告)日：2009-01-15

    申请号：US10579552

    申请日：2004-11-25

    申请人： Craig Johnstone ,  Darren McKerrecher ,  Kurt Gordon Pike

    发明人： Craig Johnstone ,  Darren McKerrecher ,  Kurt Gordon Pike

    IPC分类号： A61K31/443 ,  A61P3/04 ,  A61P3/10 ,  C07D405/12 ,  A61K31/4433

    CPC分类号： C07D405/12

    摘要： Compounds of Formula (I) wherein: R1—X— is selected from: methyl, methoxymethyl and Formula (X); R2 is selected from hydrogen, methyl, chloro and fluoro; n is 1 or 2; or a salt, pro-drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.

    摘要翻译： 式（I）的化合物，其中：R 1 -X-选自：甲基，甲氧基甲基和式（X）; R2选自氢，甲基，氯和氟; n为1或2; 或其盐，前药或溶剂化物。 还描述了它们用作GLK活化剂，含有它们的药物组合物及其制备方法。

    Quinazoline derivatives as angiogenesis inhibitors
    37.
    发明申请
    Quinazoline derivatives as angiogenesis inhibitors 审中-公开

    公开(公告)号：US20060004017A1

    公开(公告)日：2006-01-05

    申请号：US11169122

    申请日：2005-06-29

    申请人： Elaine Stokes ,  Darren McKerrecher ,  Laurent Hennequin ,  Patrick Ple

    发明人： Elaine Stokes ,  Darren McKerrecher ,  Laurent Hennequin ,  Patrick Ple

    IPC分类号： A61K31/517 ,  C07D43/02

    CPC分类号： A61K31/505 ,  A61K31/517 ,  C07D231/12 ,  C07D233/56 ,  C07D239/88 ,  C07D239/94 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

    摘要： The invention relates to the use of compounds of formula (I), wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1-3 heteroatoms selected independently from O, N and S; Z is —O—, —NH—, —S—, —CH2— or a direct bond; n is 0-5; m is 0-3; R2 represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3alkylsulphanyl, —NR3R4 (wherein R3 and R4, which may be the same or different, each represents hydrogen or C1-3alkyl), or R5Xt— (wherein X1 and R5 are as defined herein; R1 represents hydrogen, oxo, halogeno, hydroxy, C1-4alkoxy, C1-4alkyl, C1-4alkoxymethyl, C1-4alkanoyl, C1-4haloalkyl, cyano, amino, C2-5alkenyl, C2-5alkynyl, C1-3alkanoyloxy, nitro, C1-4alkanoylamino, C1-4alkoxycarbonyl, C1-4alkylsulphanyl, C1-4alkylsulphinyl, C1-4alkylsulphonyl, carbamoyl, N—C1-4alkylcarbamoyl, N,N-di(C1-4alkyl)carbamoyl, aminosulphonyl, N—C1-4alkylaminosulphonyl, N,N-di(C1-4alkyl)aminosulphonyl, N-(C1-4alkylsulphonyl)amino, N—(C1-4alkylsulphonyl)—N—(C1-4alkyl)amino, N,N-di(C1-4alkylsulphonyl)amino, a C3-7alkylene chain joined to two ring C carbon atoms, C1-4alkanoylaminoC1-4alkyl, carboxy or a group R56X10 (wherein X10 and R56 are as defined herein); and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient and compounds of formula (I). The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

    Quinazoline derivatives
    39.
    发明授权
    Quinazoline derivatives 失效
    喹唑啉衍生物

    公开(公告)号：US06806274B1

    公开(公告)日：2004-10-19

    申请号：US10019945

    申请日：2002-01-07

    申请人： Graham C Crawley ,  Laurent F A Hennequin ,  Darren McKerrecher ,  Patrick Ple ,  Jeffrey Philip Poyser ,  Christine M P Lambert

    发明人： Graham C Crawley ,  Laurent F A Hennequin ,  Darren McKerrecher ,  Patrick Ple ,  Jeffrey Philip Poyser ,  Christine M P Lambert

    IPC分类号： A61K31517

    CPC分类号： C07D231/12 ,  C07D215/54 ,  C07D233/56 ,  C07D239/94 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D487/04

    摘要： The invention concerns quinazoline derivatives of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3 includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2 and R3 is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal.

    摘要翻译： 本发明涉及式（I）的喹唑啉衍生物，其中Q 1包括任选被诸如卤代，三氟甲基和氰基的基团取代的喹唑啉环，或下式：Q 3 -X 1 - 的基团，其中 X 1包括直接键，O和Q 3包括芳基，芳基 - （1-6C）烷基，杂环基和杂环基 - （1-6C）烷基; R 2和R 3各自为氢或（1-6C）烷基; Z包括O，S和NH; 和Q 2包括芳基和芳基 - （1-3C）烷基或其药学上可接受的盐; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗温血动物中的T细胞介导的疾病或医学病症的药物中的用途。