利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

26 条记录 (耗时 0.036 秒)

    Quinazoline derivatives as VEGF inhibitors
    11.
    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
    12.
    发明申请
    Quinazoline derivatives 失效
    喹唑啉衍生物

    公开(公告)号：US20050165035A1

    公开(公告)日：2005-07-28

    申请号：US10857342

    申请日：2004-06-01

    申请人： Robert Bradbury ,  Jason Kettle ,  James McCabe ,  Andrew Turner ,  Laurent Hennequin

    发明人： Robert Bradbury ,  Jason Kettle ,  James McCabe ,  Andrew Turner ,  Laurent Hennequin

    IPC分类号： C07D401/12 ,  A61K31/517 ,  C07D43/02

    CPC分类号： C07D401/12

    摘要： The invention concerns quinazoline derivatives of Formula I wherein R1 and R2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB, particularly EGF, receptor tyrosine kinases.

    摘要翻译： 本发明涉及式I的喹唑啉衍生物，其中R 1和R 2具有本说明书中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗对erbB特别是EGF受体酪氨酸激酶的抑制敏感的肿瘤中的抗增殖剂的药物中的用途。

    Quinazoline derivatives
    14.
    发明申请
    Quinazoline derivatives 审中-公开
    喹唑啉衍生物

    公开(公告)号：US20070099943A1

    公开(公告)日：2007-05-03

    申请号：US11636549

    申请日：2006-12-11

    申请人： Robert Bradbury ,  Jason Kettle ,  James McCabe ,  Andrew Turner ,  Laurent Hennequin

    发明人： Robert Bradbury ,  Jason Kettle ,  James McCabe ,  Andrew Turner ,  Laurent Hennequin

    IPC分类号： A61K31/517 ,  C07D403/02

    CPC分类号： C04B35/632 ,  C07D401/12

    摘要： The invention concerns quinazoline derivatives of Formula I wherein R1 and R2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB, particularly EGF, receptor tyrosine kinases.

    摘要翻译： 本发明涉及式I的喹唑啉衍生物，其中R 1和R 2具有本说明书中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗对erbB特别是EGF受体酪氨酸激酶的抑制敏感的肿瘤中的抗增殖剂的药物中的用途。

    Quinazoline derivatives and their use in the treatment of cancer
    16.
    发明申请
    Quinazoline derivatives and their use in the treatment of cancer 失效
    喹唑啉衍生物及其在治疗癌症中的应用

    公开(公告)号：US20060211714A1

    公开(公告)日：2006-09-21

    申请号：US10555085

    申请日：2004-04-27

    申请人： Laurent Hennequin ,  Alleyn Plowright

    发明人： Laurent Hennequin ,  Alleyn Plowright

    IPC分类号： A61K31/517 ,  C07D403/02

    CPC分类号： C07D403/12 ,  C07D403/14

    摘要： The invention concerns quinazoline derivatives of the formula: (I); wherein X1, Q1, Z, R1, R2, Y, a and m are as defined in the description, which are erbB tyrosine kinase inhibitors, particularly EGFR tyrosine kinase inhibitors. Also claimed are processes for their preparation; pharmaceutical compositions containing them; and their use as therapeutic agents in the treatment of erbB tyrosine kinase mediated diseases such as cancer.

    摘要翻译： 本发明涉及式（I）的喹唑啉衍生物： 其中X 1，Q 1，Z，R 1，R 2，Y，a和m分别为 在描述中定义，其是erbB酪氨酸激酶抑制剂，特别是EGFR酪氨酸激酶抑制剂。 还要求他们的准备过程; 含有它们的药物组合物; 以及它们在治疗erbB酪氨酸激酶介导的疾病如癌症中的用途。

    Chemical compounds
    17.
    发明申请
    Chemical compounds 审中-公开

    公开(公告)号：US20060148819A1

    公开(公告)日：2006-07-06

    申请号：US11355006

    申请日：2006-02-16

    申请人： Laurent Hennequin

    发明人： Laurent Hennequin

    IPC分类号： A61K31/496 ,  C07D403/02

    CPC分类号： C07D401/14 ,  A61K31/502 ,  A61K31/5025 ,  C07D495/04

    摘要： The invention relates to compounds of the formula (I): wherein: ring C is 9 or 10-membered bicyclic heteroaromatic group containing at least one nitrogen atom in the ring attached to Z and optionally containing a further 1-3 heteroatoms, selected independenly from 0, S, and N, with the proviso that ring C is not a quinazoline, quinoline or cinnoline group; either any one of G1, G2, G3, G4 and G5 is nitrogen and the other four are —CH—, or G1, G2, G3, G4 and G5 are all —CH—; Z is —O—, NH—, —S—, CH2— or a direct substituents R1 may be attached at any free carbon atom of the indole, azaindole or indazole group; m is an integer from 0 to 2; Rb represents hydrogen or another value as defined herein; R1 represents hydrogen, hydroxy, halogeno, C1-4alkyl, or any other value as defined herein; 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 R5 and X1 are as defined herein) and salts thereof, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient ans the use of a compound of formula (I) in the manufacture of a medicament for the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals. 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 state including cancer ad rheumatoid arthritis.

    Substituted 3-cyanoquinolines as mek inhibitors
    18.
    发明申请
    Substituted 3-cyanoquinolines as mek inhibitors 失效
    取代的3-氰基喹啉作为mek抑制剂

    公开(公告)号：US20060089382A1

    公开(公告)日：2006-04-27

    申请号：US10520468

    申请日：2003-07-04

    申请人： Laurent Hennequin ,  Keith Gibson ,  Kevin Foote

    发明人： Laurent Hennequin ,  Keith Gibson ,  Kevin Foote

    IPC分类号： A61K31/4709 ,  C07D405/02

    CPC分类号： C07D405/12 ,  C07D405/14 ,  C07D417/14

    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作为固体肿瘤疾病的遏制和/或治疗中的抗侵袭性或抗增殖剂的药物中的用途。

    Quinzoline derivatives for use in the treatment of cancer
    19.
    发明申请
    Quinzoline derivatives for use in the treatment of cancer 失效
    喹唑啉衍生物用于治疗癌症

    公开(公告)号：US20050250797A1

    公开(公告)日：2005-11-10

    申请号：US10520266

    申请日：2003-07-04

    申请人： Laurent Hennequin ,  Keith Gibson ,  Kevin Foote

    发明人： Laurent Hennequin ,  Keith Gibson ,  Kevin Foote

    IPC分类号： A61K31/517 ,  A61K31/5377 ,  A61P35/00 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D45/02

    CPC分类号： C07D405/12 ,  C07D405/14

    摘要： The invention concerns quinazoline derivatives of Formula (I) wherein each of Z, 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）的喹唑啉衍生物，其中Z，m，R 1，n，R 3，Z 2和R 2中的每一个 在说明书中具有上文定义的任何含义; 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。