QUINOLINE DERIVATIVES FOR TREATING CANCER
    31.
    发明申请
    QUINOLINE DERIVATIVES FOR TREATING CANCER 审中-公开
    用于治疗癌症的喹诺酮衍生物

    公开(公告)号:US20090042910A1

    公开(公告)日:2009-02-12

    申请号:US12280854

    申请日:2007-03-01

    IPC分类号: A61K31/506 C07D401/12

    CPC分类号: C07D401/14

    摘要: The invention concerns quinoline derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has 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 in the treatment of cell proliferative disorders.

    摘要翻译: 本发明涉及式I的喹啉衍生物或其药学上可接受的盐,其中X 1,p,R 1,q,R 2,R 3,R 4,R 5,环A,r和R 6中的每一个在 描述; 其制备方法,含有它们的药物组合物及其在制备用于治疗细胞增殖性疾病的药物中的用途。

    Quinazoline derivatives
    32.
    发明授权
    Quinazoline derivatives 失效
    喹唑啉衍生物

    公开(公告)号:US07141577B2

    公开(公告)日:2006-11-28

    申请号:US10475016

    申请日:2002-04-15

    申请人: Patrick Ple

    发明人: Patrick Ple

    IPC分类号: A61K31/517 C07D47/02

    CPC分类号: C07D405/12

    摘要: The invention concerns quinazoline derivatives of Formula I (A Chemical Formula should be inserted here—please see paper copy enclosed) wherein each of Z, m, R1, n and R3 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 agent in the containment and/or treatment of solid tumor disease.

    摘要翻译: 本发明涉及式I的喹唑啉衍生物(A化学式应在此插入 - 请参见附有文件的复印件),其中Z,m,R 1,n和R 3 >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作在实体瘤疾病的遏制和/或治疗中作为抗侵入剂的药物的用途。

    Quinazoline derivatives as angiogenesis inhibitors

    公开(公告)号:US07074800B1

    公开(公告)日:2006-07-11

    申请号:US09913020

    申请日:2000-02-08

    IPC分类号: A61K31/517 C07D239/88

    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 R5X1— (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(C1-4alkylcarbamoyl, 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 angiogenesis inhibitors

    公开(公告)号:US20060004017A1

    公开(公告)日:2006-01-05

    申请号:US11169122

    申请日:2005-06-29

    IPC分类号: A61K31/517 C07D43/02

    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.

    Quinoline derivatives inhibiting the effect of growth factors such as VEGF
    37.
    发明授权
    Quinoline derivatives inhibiting the effect of growth factors such as VEGF 失效
    喹啉衍生物抑制生长因子如VEGF的作用

    公开(公告)号:US06809097B1

    公开(公告)日:2004-10-26

    申请号:US09254440

    申请日:1999-03-09

    IPC分类号: C07D21522

    摘要: Compounds of the formula (I): wherein: R2 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; n is an integer from 0 to 5; Z represents —O—, —NH—, —S— or —CH2—; G1 represents phenyl or a 5-10 membered heteroaromatic cyclic or bicyclic group; Y1, Y2, Y3 and Y4 each independently represents carbon or nitrogen; R1 represents fluoro or hydrogen; m is an integer from 1 to 3; R3 represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, —NR4R5 (wherein R4 and R5, can each be hydrogen or C1-3alkyl), or a group R6—X1— wherein X1 represents —CH2— or a heteroatom linker group and R6 is an alkyl, alkenyl or alkynyl chain optionally substituted by for example hydroxy, amino, nitro, alkyl, cycloalkyl, alkoxyalkyl, or an optionally substituted group selected from pyridone, phenyl and a heterocyclic ring, which alkyl, alkenyl or alkynyl chain may have a heteroatom linker group, or R6 is an optionally substituted group selected from pyridone, phenyl and a heterocyclic ring 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 such as humans, 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.

    摘要翻译: 式(I)的化合物:其中:R 2表示羟基,卤代,C 1-3烷基,C 1-3烷氧基,C 1-3烷酰氧基,三氟甲基,氰基,氨基或硝基; n为0〜5的整数, Z表示-O - , - NH - , - S-或-CH 2 - ; G 1表示苯基或5-10元杂芳族环状或双环基团; Y 1,Y 2,Y 3和Y 4各自独立地表示碳或氮; R 1表示氟或氢; m为1〜3的整数; R 3表示氢,羟基,卤代,氰基,硝基,三氟甲基,C 1-3烷基,-NR 4 R 5(其中R 4和R 5各自可以是氢或C 1-3烷基 )或基团R 6 -X 1 - ,其中X 1表示-CH 2 - 或杂原子连接基团,R 6是任选被例如羟基,氨基, ,硝基,烷基,环烷基,烷氧基烷基或选自吡啶酮,苯基和杂环的任选取代的基团,该烷基,烯基或炔基链可具有杂原子连接基团,或R 6为任选取代的基团, 吡啶酮,苯基和杂环及其盐在制备用于在温血动物如人类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,制备这些衍生物的方法,药物 含有式I化合物或其药学上可接受的盐的组合物具有活性 式I化合物和式I化合物及其药学上可接受的盐抑制VEGF在治疗许多疾病状态(包括癌症和类风湿性关节炎)中的价值的性质。