Quinazoline derivatives and their use in the treatment of cancer
    31.
    发明授权
    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:US07659279B2

    公开(公告)日:2010-02-09

    申请号:US10555085

    申请日:2004-04-27

    IPC分类号: A61K31/517 C07D239/88

    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X1,Q1,Z,R1,R2,Y,a和m如描述中所定义,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。

    4-ANILINO QUINAZOLINE DERIVATIVES AS ANTIPROLIFERATIVE AGENTS
    35.
    发明申请
    4-ANILINO QUINAZOLINE DERIVATIVES AS ANTIPROLIFERATIVE AGENTS 审中-公开
    4-苯胺喹诺酮衍生物作为抗增生剂

    公开(公告)号:US20080269487A1

    公开(公告)日:2008-10-30

    申请号:US12147250

    申请日:2008-06-26

    IPC分类号: C07D401/02

    CPC分类号: C07D401/12 C07D403/12

    摘要: The invention concerns quinazoline derivatives of Formula (I) wherein each of Q1, Z, R1 and Q2 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 receptor tyrosine kinases.

    摘要翻译: 本发明涉及式(I)的喹唑啉衍生物,其中Q 1,Z,R 1和Q 2 2中的每一个具有定义的任何含义 在说明中; 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受体酪氨酸激酶抑制敏感的肿瘤中的抗增殖剂的药物中的用途。

    Quinazoline Derivatives
    36.
    发明申请
    Quinazoline Derivatives 审中-公开
    喹唑啉衍生物

    公开(公告)号:US20080234263A1

    公开(公告)日:2008-09-25

    申请号:US10572303

    申请日:2004-09-13

    摘要: The invention concerns quinazoline derivatives of Formula (I) wherein each of R1, R3, R20, X1, X2, Z, W, (a) and (q) 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 turnours which are sensitive to inhibition of 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,其中R 1,R 3,R 20,X 1, Z,W,(a)和(q)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抑制erbB受体酪氨酸激酶,特别是EGFR酪氨酸激酶敏感的转导酶的抗增生剂中的用途。

    Quinazoline Derivatives As Angiogenesis Inhibitors
    37.
    发明申请
    Quinazoline Derivatives As Angiogenesis Inhibitors 失效
    喹唑啉衍生物作为血管生成抑制剂

    公开(公告)号:US20080058342A1

    公开(公告)日:2008-03-06

    申请号:US10566842

    申请日:2004-08-05

    摘要: The present invention relates to compounds of the Formula (I): wherein: ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which moiety may be saturated or unsaturated, which may be aromatic or non-aromatic, and which optionally may contain 1-3 heteroatoms selected independently from O, N and S; is —O— —NH— or —S—; is 0, 1, 2, 3, 4 or 5; is 0, 1, 2 or 3; and R2 and R1 are as defined herein; 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; 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.

    摘要翻译: 本发明涉及式(I)的化合物:其中:环C是8,9,10,12或13元双环或三环部分,该部分可以是饱和或不饱和的,其可以是芳族或非芳族的 ,并且其任选地可以含有1-3个独立地选自O,N和S的杂原子; 是-O-NH-或-S-; 是0,1,2,3,4或5; 是0,1,2或3; 且R 2和R 1如本文所定义; 及其盐; 它们在制备用于在温血动物中产生抗血管生成和/或血管通透性降低作用的药物中的用途; 制备这些化合物的方法; 含有式(I)化合物或其药学上可接受的盐的药物组合物和通过给予式I化合物或其药学上可接受的盐治疗涉及血管发生的疾病状态的方法。 式(I)的化合物抑制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 compounds
    39.
    发明授权

    公开(公告)号:US07268230B2

    公开(公告)日:2007-09-11

    申请号:US10502538

    申请日:2003-01-28

    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.

    3-Cyano-quinoline derivatives
    40.
    发明申请
    3-Cyano-quinoline derivatives 审中-公开
    3-氰基 - 喹啉衍生物

    公开(公告)号:US20070191346A1

    公开(公告)日:2007-08-16

    申请号:US11642978

    申请日:2006-12-21

    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。