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47 条记录 (耗时 0.055 秒)

    Quinazoline derivatives as VEGF inhibitors
    1.
    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：US08642608B2

    公开(公告)日：2014-02-04

    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： A01N43/54 ,  A61K31/517 ,  C07D239/72 ,  C07D401/00

    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。

    Cinnoline derivatives and use as medicine
    3.
    发明授权
    Cinnoline derivatives and use as medicine 失效

    公开(公告)号：US07087602B2

    公开(公告)日：2006-08-08

    申请号：US10310074

    申请日：2002-12-05

    申请人： Andrew Peter Thomas ,  Laurent Francois Andre Hennequin

    发明人： Andrew Peter Thomas ,  Laurent Francois Andre Hennequin

    IPC分类号： A01K31/502

    CPC分类号： C07D401/12 ,  A61K31/502 ,  A61K31/5377 ,  C07D237/28 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention relates to the use of cinnoline derivatives of formula (I) wherein Z represents —O—, —NH—, —S— or —CH2—; m is an integer from 1 to 5; R1 represents hydrogen, hydroxy, halogeno, nitro, cyano, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3alkylthio or NR6R7 (wherein R6 and R7, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, fluoro, chloro, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; R4 represents hydrogen, hydroxy, halogeno, cyano, nitro, amino, trifluoromethyl, C1-3alkyl or a group R5—X1 (wherein X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR8CO—, —CONR9−, —SO2NR10—, —NR11SO2— or —NR12— (wherein R8, R9, R10, R11 and R12 each independently represents hydrogen, C1-3alkyl or C1-3alkoxy C2-3alkyl) and R5is an optionally substituted alkyl, carbocylic or heterocylic group which may be saturated or unsaturated and may be directly linked to the cinnoline ring or be linked via a carbon chain which may have heteroatom linking groups within it and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human being, processes for the preparation of such derivatives, 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.

    Pyrimidine compounds
    6.
    发明授权
    Pyrimidine compounds 失效
    嘧啶化合物

    公开(公告)号：US07446105B2

    公开(公告)日：2008-11-04

    申请号：US10507163

    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

    摘要： Compounds of the formula (I) wherein R1, R2, R3, R4, R5, R6 and p are as defined within and 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： 其中R 1，R 2，R 3，R 4，R 4，R 4，R 4， 其中，R 6和R 6定义如上，其中药学上可接受的盐和体内可水解的酯被描述。 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
    8.
    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：US07173038B1

    公开(公告)日：2007-02-06

    申请号：US10129336

    申请日：2000-11-01

    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： A61K31/53 ,  A61K31/517 ,  A61K31/519 ,  C07D239/72

    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 piperidin-4-yl which may bear one or two substituents selected from hydroxy, halogeno, 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 a 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 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; R 1表示卤代或C 1-3烷基; X 1表示-O-; R 2选自以下三个基团之一：1）C 1-5烷基R 3（其中R 3，R 3，R 3， SUP>是可以具有一个或两个选自羟基，卤代，C 1-4 - 羟基烷基和C 1-4 - 烷氧基的取代基的哌啶-4-基; 2）C （其中R 3如上文所定义）;或其中R 3和R 3如上定义。 3）C 2-5炔基R 3（其中R 3如上定义）; 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，其在治疗包括癌症和类风湿性关节炎在内的疾病状态的数量方面具有价值。

    Cinnoline derivatives and use as medicine
    9.
    发明授权
    Cinnoline derivatives and use as medicine 失效
    噌啉衍生物用作药物

    公开(公告)号：US06514971B1

    公开(公告)日：2003-02-04

    申请号：US09142839

    申请日：1999-04-13

    申请人： Andrew Peter Thomas ,  Laurent Francois Andre Hennequin

    发明人： Andrew Peter Thomas ,  Laurent Francois Andre Hennequin

    IPC分类号： A61K31502

    CPC分类号： C07D401/12 ,  A61K31/502 ,  A61K31/5377 ,  C07D237/28 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention relates to the use of cinnoline derivatives of formula (I) wherein Z represents —O—, —NH—, —S— or —CH2—; m is a n integer from 1 to 5; R1 represents hydrogen, hydroxy, halogeno, nitro, cyano, trifluoromethyl, Cp1-3alkyl, C1-3alkoxy, C1-3alkylthio or NR6R7 (wherein R6 and R7, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, auoro, chioro, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; R4 represents hydrogen, hydroxy, halogeno, cyano, nitro, amino, trifluoromethyl, C1-3alkyl or a group R5—X1 (wherein X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR8CO—, —CONR9—, —SO2NR10—, —NR11SO2— or NR12— (wherein R8, R9, R10, R11 and R12 each independently represents hydrogen, C1-3alkyl or C1-3alkoxy C2-3alkyl) and R5 is an optionally substituted alkyl, carbocylic or heterocylic group which may be saturated or unsaturated and may be directly linked to the cinnoline ring or be linked via a carbon chain which may have heteroatom linking groups within it and salts thereof, in the manufacture of a medicament for use in the production of an anti angiogenic and/or vascular permeability reducing effect in a warmn-blooded animal such as a human being, processes for the preparation of such derivatives, pharmnaceutical compositions containing a compound of formula (I) or a pharmnaceutically 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.

    摘要翻译： 本发明涉及式（I）的噌啉衍生物，其中Z表示-O - ， - NH - ， - S-或-CH 2 - ; m是1至5的n整数; R 1表示氢，羟基，卤代，硝基，氰基，三氟甲基，C 1-3烷基，C 1-3烷氧基，C 1-3烷硫基或NR 6 R 7（其中R 6和R 7可以相同或不同，各自表示氢或C 1-3烷基）。 R2代表氢，羟基，酰基，氯，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; R 4表示氢，羟基，卤代，氰基，硝基，氨基，三氟甲基，C 1-3烷基或基团R 5 -X 1（其中X 1表示-O-，-CH 2 - ， - S - ， - SO-，-SO 2 - NR8CO-，-CONR9-，-SO2NR10-，-NR11SO2-或NR12-​​（其中R8，R9，R10，R11和R12各自独立地表示氢，C1-3烷基或C1-3烷氧基C2-3烷基），R5是任选取代的 烷基，碳环或杂环基团，其可以是饱和或不饱和的，并且可以直接连接到噌啉环，或者可以通过其中具有杂原子连接基团的碳链和其盐连接，制备用于 在温血动物例如人中产生抗血管生成和/或血管通透性降低作用，制备此类衍生物的方法，含有式（I）化合物或其药物上可接受的盐作为活性物质的药物组合物 成分和式（I）的化合物。式（I）的化合物 I）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。