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    Quinazoline derivatives
    1.
    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。

    Quinazoline derivatives as angiogenesis inhibitors
    3.
    发明授权
    Quinazoline derivatives as angiogenesis inhibitors 有权

    公开(公告)号：US07074800B1

    公开(公告)日：2006-07-11

    申请号：US09913020

    申请日：2000-02-08

    申请人： Elaine S E Stokes ,  Darren Mckerrecher ,  Laurent F A Hennequin ,  Patrick Ple

    发明人： Elaine S E Stokes ,  Darren Mckerrecher ,  Laurent F A Hennequin ,  Patrick Ple

    IPC分类号： A61K31/517 ,  C07D239/88

    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 R5X1— (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(C1-4alkylcarbamoyl, 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
    4.
    发明授权
    Quinazoline derivatives 失效

    公开(公告)号：US07262201B1

    公开(公告)日：2007-08-28

    申请号：US09806836

    申请日：1999-10-05

    申请人： Laurent F A Hennequin ,  Georges Pasquet

    发明人： Laurent F A Hennequin ,  Georges Pasquet

    IPC分类号： A61K31/5377 ,  A61K31/517 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14

    摘要： The invention relates to the use of compounds of the formula I: wherein: ring C is a 5-6 membered heterocyclic moiety; Z is —O—, —S—, or —CH2—; R1 is hydrogen, C1-4alkyl, C1-4alkoxymethyl, di(C1-4)alkoxy)methyl, C1-4alkanoyl, trifluoromethyl, cyano, amino, C2-5alkenyl, C2-5alkynyl, carboxy, C3-7cycloalkyl, C3-7-cycloalkylC1-3alkyl, or an optionally substituted group selected from phenyl, benzyl, phenylC2-4alkyl and a 5-6 membered heterocyclic group; n is an integer from 0 to 5; m is an integer from 0 to 3; R2 represents hydrogen, hydroxy, halgeno, 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 R5X1— (wherein X1 represents a direct bond, —CH2—, or a heteroatom linker group and R5 is an alkyl, alkenyl or alkynyl chain optionally substituted by for example hydroxy, amino, nitro, alkyl, cycloalkyl, alkoxyalkyl, or an optionally substituted group selected from pyridone, phenyl and a heterocyclic ring, which alkyl, alkenyl or alkynyl chain may have a heteroatom linker group, or R5 is an optionally substituted group selected from pyridone, phenyl and a heterocyclic ring, 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.