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    QUINAZOLINE DERIVATIVES AS VEGF INHIBITORS
    41.
    发明申请
    QUINAZOLINE DERIVATIVES AS VEGF INHIBITORS 有权
    喹诺酮衍生物作为VEGF抑制剂

    公开(公告)号：US20110065736A1

    公开(公告)日：2011-03-17

    申请号：US12761105

    申请日：2010-04-15

    申请人： Andrew Peter Thomas ,  Elaine Sophie Elizabeth Stokes ,  Laurent Francois Andre Hennequin

    发明人： Andrew Peter Thomas ,  Elaine Sophie Elizabeth Stokes ,  Laurent Francois Andre Hennequin

    IPC分类号： A61K31/517 ,  A61P35/00 ,  A61P3/10 ,  A61P17/06 ,  A61P19/02 ,  A61P29/00 ,  A61P37/00 ,  A61P15/00 ,  A61P27/02

    CPC分类号： C07D401/12

    摘要： The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3 (wherein R3 is piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4alkyl, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3 (wherein R3 is as defined hereinbefore); 3) C2-5alkynylR3 (wherein R3 is as defined hereinbefore); and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. 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.

    摘要翻译： 本发明涉及式（I）的喹唑啉衍生物，其中m为1至3的整数; R1代表卤代或C1-3烷基; X1表示-O-; R2选自以下三个基团之一：1）C 1-5烷基R 3（其中R 3是可以带有一个或两个选自羟基，卤代C 1-4烷基，C 1-4羟烷基和C 1-4烷氧基的取代基的哌啶-4-基; 2）C 2-5烯基R 3（其中R 3如上所定义）; 3）C 2-5炔基R 3（其中R 3如上文所定义）; 并且其中任何烷基，烯基或炔基可以具有一个或多个选自羟基，卤代和氨基的取代基; 及其盐; 其制备方法，含有式（I）化合物或其药学上可接受的盐作为活性成分的药物组合物。 式（I）化合物及其药学上可接受的盐抑制VEGF的作用，其在治疗许多疾病状态（包括癌症和类风湿性关节炎）中是有价值的。

    Pyrimidine compounds
    42.
    发明授权
    Pyrimidine compounds 失效
    嘧啶化合物

    公开(公告)号：US07485638B2

    公开(公告)日：2009-02-03

    申请号：US10507162

    申请日：2003-03-06

    申请人： Nicholas John Newcombe ,  Andrew Peter Thomas

    发明人： Nicholas John Newcombe ,  Andrew Peter Thomas

    IPC分类号： C07D403/04 ,  A61K31/506

    CPC分类号： C07D403/04 ,  C07D405/14

    摘要： Compounds of the formula (I), wherein R1, R2, R3, R4, R5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.

    摘要翻译： 描述式（I）的化合物，其中R 1，R 2，R 3，R 4，R 5和p如本文所定义，以及其药学上可接受的盐和体内可水解的酯。 还描述了它们的制备方法及其作为药物的用途，特别是用于在温血动物如人中产生细胞周期抑制（抗细胞增殖）作用的药物。

    Quinazoline derivatives as VEGF inhibitors
    46.
    发明授权
    Quinazoline derivatives as VEGF inhibitors 有权
    喹唑啉衍生物作为VEGF抑制剂

    公开(公告)号：US06184225B2

    公开(公告)日：2001-02-06

    申请号：US09125271

    申请日：1998-08-13

    申请人： Andrew Peter Thomas ,  Craig Johnstone ,  Laurent Francois Andre Hennequin

    发明人： Andrew Peter Thomas ,  Craig Johnstone ,  Laurent Francois Andre Hennequin

    IPC分类号： A01N4354

    CPC分类号： C07D239/88 ,  C07D239/93 ,  C07D239/94

    摘要： The invention relates to quinazoline derivatives of formula (I) wherein: Z represents —O—, —NH— or —S—; m is an integer from 1 to 5; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluorometlyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio or NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino, or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, SO2—, —NR6—, NR8CO—, —CONR9—SO2NR10— or —NR11SO2—, (wherein R7, R8, R9, R10 and R11 each represents C1-3alkyl, C1-3alkoxyC2-3alkyl); R4 represents a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted 5 or 6 membered saturated carbocylic or heterocyclic group; and salts thereof, processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient 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.

    摘要翻译： 本发明涉及式（I）的喹唑啉衍生物，其中：Z表示-O - ， - NH-或-S-; m为1〜5的整数; R 1表示氢，羟基，卤代，硝基，三氟甲基，氰基，C 1-3烷基，C 1-3烷氧基，C 1-3烷硫基或NR 5 R 6（其中R 5和R 6可以相同或不同，各自表示氢或C 1-3烷基）。 R2代表氢，羟基，卤代，甲氧基，氨基或硝基; R3表示羟基，卤代，C1-3烷基，C1-3烷氧基，C1-3烷酰氧基，三氟甲基，氰基，氨基或硝基; X1表示-O - ， - CH2-，-S-，-SO-，SO2-，-NR6-，NR8CO-，-CONR9-SO2NR10-或-NR11SO2-，（其中R7，R8，R9，R10和R11各自 表示C1-3烷基，C1-3烷氧基C2-3烷基）; R 4表示可以含有杂原子连接基团的烯基，炔基或任选取代的烷基的基团，该烯基，炔基或烷基可以带有末端任选取代的5或6元饱和碳环或杂环基; 及其盐，其制备方法，含有式（I）化合物或其药学上可接受的盐作为活性成分的式（I）化合物及其药学上可接受的盐的药物组合物抑制VEGF的作用， 治疗许多疾病状态（包括癌症和类风湿性关节炎）的价值。