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    Quinazoline derivatives as angiogenesis inhibitors
    1.
    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 as VEGF inhibitors
    3.
    发明申请
    Quinazoline derivatives as VEGF inhibitors 审中-公开
    喹唑啉衍生物作为VEGF抑制剂

    公开(公告)号：US20070265286A1

    公开(公告)日：2007-11-15

    申请号：US11642979

    申请日：2006-12-21

    申请人： Andrew Thomas ,  Elaine Stokes ,  Laurent Hennequin

    发明人： Andrew Thomas ,  Elaine Stokes ,  Laurent Hennequin

    IPC分类号： A61K31/517 ,  A61P19/02 ,  A61P3/00 ,  A61P35/00 ,  A61P37/00 ,  C07D239/94

    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; 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>是可以带有一个或两个选自羟基，卤代，C 1-4 - 烷基，C 1-4 - 羟基烷基和C 1-4烷氧基; 2）C 2-5烯基R 3（其中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，其在治疗许多疾病状态（包括癌症和类风湿性关节炎）中是有价值的。

    Quinazoline derivatives
    6.
    发明申请
    Quinazoline derivatives 审中-公开
    喹唑啉衍生物

    公开(公告)号：US20070032513A1

    公开(公告)日：2007-02-08

    申请号：US10572261

    申请日：2004-09-13

    申请人： Laurent Hennequin ,  Christopher Halsall

    发明人： Laurent Hennequin ,  Christopher Halsall

    IPC分类号： A61K31/517 ,  C07D403/02

    CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D403/14

    摘要： The invention concerns quinazoline derivatives of the Formula I: (A chemical formula should be inserted here—please see paper copy enclosed herewith) wherein each of R1, R2, W, X1, X2, Z, a and b are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula I are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, particularly EGFR tyrosine kinase.

    摘要翻译： 本发明涉及式I的喹唑啉衍生物：（化学式应在此插入，请参见随附的纸质复制品），其中R 1，R 2，W，X 1，X 2，Z，a和b各自如说明书中所定义 ; 其准备过程; 含有它们的药物组合物及其在制备用于提供抗增殖作用的药物中的用途。 预期式I的喹唑啉衍生物可用于治疗疾病，例如由erbB受体酪氨酸激酶，特别是EGFR酪氨酸激酶介导的某些癌症。

    3-Cyano-quinoline derivatives
    7.
    发明申请
    3-Cyano-quinoline derivatives 失效
    3-氰基 - 喹啉衍生物

    公开(公告)号：US20050282856A1

    公开(公告)日：2005-12-22

    申请号：US10532958

    申请日：2003-10-28

    申请人： Laurent Hennequin

    发明人： Laurent Hennequin

    IPC分类号： A61P35/00 ,  C07D405/12 ,  A61K31/4709 ,  C07D45/02

    CPC分类号： C07D405/12

    摘要： The invention concerns quinoline derivatives of Formula (I) wherein each of Z1, m, R1, n, R3, Z2 and R14 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive or anti-proliferative agent in the containment and/or treatment of solid tumour disease.

    摘要翻译： 本发明涉及式（I）的喹啉衍生物，其中Z 1，m，R 1，n，R 3，Z， > 2 和R 14具有上文在描述中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于在实体瘤疾病的遏制和/或治疗中作为抗侵袭性或抗增殖剂的药物的用途。

    Quinazoline compounds
    8.
    发明申请
    Quinazoline compounds 失效

    公开(公告)号：US20050085465A1

    公开(公告)日：2005-04-21

    申请号：US10502538

    申请日：2003-01-28

    申请人： Laurent Hennequin

    发明人： Laurent Hennequin

    IPC分类号： C07D491/113 ,  A61K31/517 ,  A61K31/519 ,  A61P9/00 ,  A61P35/00 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D471/04 ,  C07D491/04 ,  C07D519/00 ,  A61K31/541 ,  A61K31/5377

    CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D491/04

    摘要： The invention relates to compounds of the formula (I): wherein ring C is as defined herein, for example indolyl, indazolyl or azaindolyl; Z is —O—, —NH— or —S—; n is 0-5; m is 0-3; R1 and R2 are defined herein including groups: (i) Q1X1 wherein Q1 and X1 are as defined herein; (ii) Q15W3 wherein Q15 and W3 are as defined herein, (iii) Q21W4C1-5alkylX1- wherein Q21, W4 and X1 are as defined herein, (iv) Q28C1-5alkylX1-, Q28C2-5alkenylX1- or Q28C2-5alkynylX1- wherein Q29 and X1 are as defined herein and (v) Q29C1-5alkylX1-, Q29C2-5alkenylX1- or Q29C2-5alkynylX1- wherein Q29 and X1 are as defined herein; R2 can also be 6,7-methylenedioxy or 6,7-ethylenedioxy; and salts thereof; their use 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; intermediates used in such processes; processes for making such intermediates; pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof and methods of treating disease states involving angiogenesis by administering a compound of formula I or a pharmaceutically acceptable salt thereof. The compounds of formula I inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

    Quinazoline compounds
    9.
    发明申请
    Quinazoline compounds 失效

    公开(公告)号：US20080027069A1

    公开(公告)日：2008-01-31

    申请号：US11705035

    申请日：2007-02-12

    申请人： Laurent Hennequin

    发明人： Laurent Hennequin

    IPC分类号： A61K31/517 ,  A61P35/00 ,  C07D401/14 ,  C07D471/04

    CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D491/04

    摘要： The invention relates to compounds of the formula (I): wherein ring C is as defined herein, for example indolyl, indazolyl or azaindolyl; Z is —O—, —NH— or —S—; n is 0-5; m is 0-3; R1 and R2 are defined herein including groups: (i) Q1X1 wherein Q1 and X1 are as defined herein; (ii) Q15W3 wherein Q15 and W3 are as defined herein, (iii) Q21W4C1-5alkylX1— wherein Q21, W4 and X1 are as defined herein, (iv) Q28C1-5alkylX1—, Q28C2-5alkenylX1— or Q28C2-5alkynylX1— wherein Q28 and X1 are as defined herein and (v) Q29C1-5alkylX1—, Q29C2-5alkenylX1— or Q29C2-5alkynylX1— wherein Q29 and X1 are as defined herein; R2 can also be 6,7-methylenedioxy or 6,7-ethylenedioxy; and salts thereof; their use 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; intermediates used in such processes; processes for making such intermediates; pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof and methods of treating disease states involving angiogenesis by administering a compound of formula I or a pharmaceutically acceptable salt thereof. The compounds of formula I inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.