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    Oxindole derivatives
    2.
    发明授权
    Oxindole derivatives 失效
    羟吲哚衍生物

    公开(公告)号：US06265411B1

    公开(公告)日：2001-07-24

    申请号：US09180310

    申请日：1998-11-06

    申请人： Andrew Peter Thomas ,  Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin ,  Patrick Ple

    发明人： Andrew Peter Thomas ,  Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin ,  Patrick Ple

    IPC分类号： A61K31505

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

    摘要： The invention relates to compounds of formula (I), wherein: R2 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino, nitro, C2-4alkanoyl, C1-4alkanoylamino, C1-4alkoxycarbonyl, C1-4alkylthio, C1-4alkylsulphinyl, C1-4alkylsulphonyl, carbamoyl, {overscore (N)}—C1-4alkylcarbamoyl, {overscore (N)},{overscore (N)}-di(C1-4alkyl)carbamoyl, aminosulphonyl, {overscore (N)}—C1-4alkylaminosulphonyl, {overscore (N)},{overscore (N)}-di(C1-4alkyl)aminosulphonyl, C1-4alkylsulphonylamino, or a group R4X1 wherein X1 represents a direct bond, C2-4alkanoyl, —CONR5R6—, —SO2NR7R8— or —SO2R9— (wherein R5 and R7, each independently represents hydrogen or C1-2alkyl and R6, R8 and R9 each independently represents C1-4alkyl and wherein R4 is linked to R6, R8 or R9) and R4 represents an optionally substituted group selected from phenyl and a 5 or 6-membered heterocyclic group; n is an integer from 0 to 4, R1 represents hydrogen, C1-4alkyl, C1-4alkoxymethyl, di(C1-4alkoxy)methyl or C1-4alkanoyl; m is an integer from 0 to 4; and R3 represents hydroxy, halogeno, nitro, trifluoromethyl, C1-3alkyl, cyano, amino or R10X2 (wherein X2 represents a direct bond, —CH2—, or a single or double heteroatom linker group including —S—, —SO— and —NR15— (wherein R15 represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl), and R10 is an 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 R10 is an optionally substituted group selected from pyridone, phenyl and a heterocyclic ring. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF and FGF, properties 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）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，硝基，C 2-4烷酰基，C 1-4烷酰基氨基，C 1-4烷氧基羰基 ，C 1-4烷硫基，C 1-4烷基亚磺酰基，C 1-4烷基磺酰基，氨基甲酰基，（超核（N）） - C 1-4烷基氨基甲酰基，{过核（N）}，{过核（N） （超核（N）） - C 1-4烷基氨基磺酰基，（超核（N）}，（超核（N）） - 二（C 1-4烷基）氨基磺酰基，C 1-4烷基磺酰基氨基或其中X 1表示直接键的基团R 4 X 1， 烷酰基，-CONR 5 R 6 - ，-SO 2 NR 7 R 8 - 或-SO 2 R 9 - （其中R 5和R 7各自独立地表示氢或C 1-2烷基，R 6，R 8和R 9各自独立地表示C 1-4烷基，并且其中R 4连接至R 6，R 8或R 9 ）和R 4表示选自苯基和5或6元杂环基的任选取代的基团; n为0至4的整数，R 1表示氢，C 1-4烷基，C 1-4烷氧基甲基，二（C 1-4烷氧基）甲基或C 1-4烷酰基; m为0〜4的整数; 并且R 3表示羟基，卤代，硝基，三氟甲基，C 1-3烷基，氰基，氨基或R 10 X 2（其中X 2表示直接键，-CH 2 - 或包含-S-，-SO-和 - NR15-（其中R15表示氢，C1-3烷基或C1-3烷氧基C2-3烷基），R10是任选被例如羟基，氨基，硝基，烷基，环烷基，烷氧基烷基或任选取代的基团选择性取代的烯基或炔基链

    QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    3.
    发明申请
    QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
    喹诺酮衍生物和含有它们的药物组合物

    公开(公告)号：US20110071144A1

    公开(公告)日：2011-03-24

    申请号：US12766106

    申请日：2010-04-23

    申请人： Andrew Peter THOMAS ,  Craig Johnstone ,  Edward Clayton ,  Elaine Sophie Elizabeth Stokes ,  Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin

    发明人： Andrew Peter THOMAS ,  Craig Johnstone ,  Edward Clayton ,  Elaine Sophie Elizabeth Stokes ,  Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin

    IPC分类号： A61K31/517 ,  C07D239/94 ,  C07D405/12 ,  C07D403/12 ,  C07D413/12 ,  C07D401/12 ,  C07D417/12 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/496 ,  A61P35/00 ,  A61P9/00

    CPC分类号： C07D401/12 ,  A61F13/02 ,  A61F13/023 ,  A61F2013/00221 ,  A61F2013/8408 ,  A61K31/517 ,  A61K31/541 ,  C07D239/94 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention relates to quinazoline derivatives of formula (1) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected from alkyl and a 5 or 6 membered saturated carbocyclic or heterocyclic group, 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 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（1）的喹唑啉衍生物，其中m为1至2的整数; R 1表示氢，羟基，卤代，硝基，三氟甲基，氰基，C 1-3烷基，C 1-3烷氧基，C 1-3烷硫基或-NR 5 R 6（其中R 5和R 6可以相同或不同，各自表示氢或C 1-3烷基 ）; R2代表氢，羟基，卤代，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; X 1表示-O - ， - CH 2 - ， - S - ， - SO - ， - SO 2 - ， - NR 7 CO-，-CONR 8 - ， - SO 2 NR 9 - ， - NR 10 SO 2 - 或-NR 11 - （其中R 7，R 8，R 9，R 10 和R 11各自独立地表示氢，C 1-3烷基或C 1-3烷氧基C 2-3 - 烷基）; R 4表示任选取代的5或6元饱和碳环或杂环基团或为烯基，炔基或任选取代的烷基的基团，该烷基可含有杂原子连接基团，该烯基，炔基或烷基可带有末端任选取代的 选自烷基和5或6元饱和碳环或杂环基团的基团，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在治疗许多疾病状态（包括癌症和类风湿性关节炎）中具有价值的性质。

    Quinazoline derivatives and pharmaceutical compositions containing them
    4.
    发明授权
    Quinazoline derivatives and pharmaceutical compositions containing them 有权
    喹唑啉衍生物和含有它们的药物组合物

    公开(公告)号：US06414148B1

    公开(公告)日：2002-07-02

    申请号：US09269595

    申请日：1999-03-25

    申请人： Andrew Peter Thomas ,  Craig Johnstone ,  Edward Clayton ,  Elaine Sophie Elizabeth Stokes ,  Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin

    发明人： Andrew Peter Thomas ,  Craig Johnstone ,  Edward Clayton ,  Elaine Sophie Elizabeth Stokes ,  Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin

    IPC分类号： C07D23972

    CPC分类号： C07D401/12 ,  A61F13/02 ,  A61F13/023 ,  A61F2013/00221 ,  A61F2013/8408 ,  A61K31/517 ,  A61K31/541 ,  C07D239/94 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention relates to quinazoline derivatives of formula (1) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected from alkyl and a 5 or 6 membered saturated carbocyclic or heterocyclic group, 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 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（1）的喹唑啉衍生物，其中m为1至2的整数; R 1表示氢，羟基，卤代，硝基，三氟甲基，氰基，C 1-3烷基，C 1-3烷氧基，C 1-3烷硫基或-NR 5 R 6（其中R 5和R 6可以相同或不同，各自表示氢或C 1-3烷基 ）; R2代表氢，羟基，卤代，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; X 1表示-O - ， - CH 2 - ， - S - ， - SO - ， - SO 2 - ， - NR 7 CO-，-CONR 8 - ， - SO 2 NR 9 - ， - NR 10 SO 2 - 或-NR 11 - （其中R 7，R 8，R 9，R 10 和R 11各自独立地表示氢，C 1-3烷基或C 1-3烷氧基C 2-3 - 烷基）; R 4表示任选取代的5或6元饱和碳环或杂环基团或为烯基，炔基或任选取代的烷基的基团，该烷基可含有杂原子连接基团，该烯基，炔基或烷基可带有末端任选取代的 选自烷基和5或6元饱和碳环或杂环基团的基团，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在治疗许多疾病状态（包括癌症和类风湿性关节炎）中具有价值的性质。

    Chemical compounds
    6.
    发明授权
    Chemical compounds 有权
    化合物

    公开(公告)号：US6071921A

    公开(公告)日：2000-06-06

    申请号：US203764

    申请日：1998-12-02

    申请人： Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin ,  Andrew Peter Thomas

    发明人： Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin ,  Andrew Peter Thomas

    IPC分类号： A61K31/505 ,  A61K31/517 ,  A61P9/00 ,  A61P35/00 ,  A61P43/00 ,  C07D239/72 ,  C07D239/74 ,  C07D239/86 ,  C07D239/88 ,  C07D239/94 ,  C07D401/00 ,  C07D401/12 ,  C07D403/00 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    CPC分类号： C07D403/12 ,  C07D239/88 ,  C07D239/94 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention relates to quinazoline derivatives of the formula: ##STR1## [wherein: Y.sup.1 represents --O--, --S--, --CH.sub.2 --, --SO--, --SO.sub.2 --, --NR.sup.5 CO--, --CONR.sup.6 --, --SO.sub.2 NR.sup.7 --, --NR.sup.8 SO.sub.2 -- or --NR.sup.9 -- (wherein R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 each independently represents hydrogen, alkyl or alkoxyalkyl);R.sup.1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, alkyl, alkoxy, alkylthio, amino or alkylamino.R.sup.2 represents hydrogen, hydroxy, halogeno, alkyl, alkoxy, trifluoromethyl, cyano, amino or nitro;m is an integer from 1 to 5;R.sup.3 represents hydroxy, halogeno, alky, alkoxy, alkanoyloxy, trifluoromethyl, cyano, amino or nitro;R.sup.4 represents a group which is or which contains an optionally substituted pyridone, phenyl or aromatic heterocyclic group] and salts thereof; processes for their preparation and 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： 本发明涉及下式的喹唑啉衍生物：其中：Y1表示-O - ， - S - ， - CH2-，-SO-，-SO2-，-NR5CO-，-CONR6-，-SO2NR7-，-NR8SO2- 或-NR 9 - （其中R 5，R 6，R 7，R 8和R 9各自独立地表示氢，烷基或烷氧基烷基）。 R 1表示氢，羟基，卤代，硝基，三氟甲基，氰基，烷基，烷氧基，烷硫基，氨基或烷基氨基。 R2代表氢，羟基，卤代，烷基，烷氧基，三氟甲基，氰基，氨基或硝基; m为1〜5的整数; R3表示羟基，卤代，烷基，烷氧基，烷酰氧基，三氟甲基，氰基，氨基或硝基; R4表示含有任选取代的吡啶酮，苯基或芳族杂环基团的基团及其盐; 其制备方法和含有式I化合物或其药学上可接受的盐的药物组合物作为活性成分。 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。

    Substituted quinazolines
    7.
    发明授权
    Substituted quinazolines 失效
    取代喹唑啉

    公开(公告)号：US5962458A

    公开(公告)日：1999-10-05

    申请号：US768887

    申请日：1996-12-17

    申请人： Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin ,  Andrew Peter Thomas

    发明人： Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin ,  Andrew Peter Thomas

    IPC分类号： A61K31/505 ,  A61K31/517 ,  A61P9/00 ,  A61P35/00 ,  A61P43/00 ,  C07D239/72 ,  C07D239/74 ,  C07D239/86 ,  C07D239/88 ,  C07D239/94 ,  C07D401/00 ,  C07D401/12 ,  C07D403/00 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    CPC分类号： C07D403/12 ,  C07D239/88 ,  C07D239/94 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention relates to quinazoline derivatives of the formula: ##STR1## �wherein: Y.sup.1 represents --O--, --S--, --CH.sub.2 --, --SO--, --SO.sub.2 --, --NR.sup.5 CO--, --CONR.sup.6 -, --SO.sub.2 NR.sup.7 -, --NR.sup.8 SO.sub.2 -- or --NR.sup.9 - (wherein R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 each independently represents hydrogen, alkyl or alkoxyalkyl);R.sup.1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, alkyl, alkoxy, alkylthio, amino or alkylamino.R.sup.2 represents hydrogen, hydroxy, halogeno, alkyl, alkoxy, trifluoromethyl, cyano, amino or nitro;m is an integer from 1 to 5;R.sup.3 represents hydroxy, halogeno, alkyl, alkoxy, alkanoyloxy, trifluoromethyl, cyano, amino or nitro;R.sup.4 represents a group which is or which contains an optionally substituted pyridone, phenyl or aromatic heterocyclic group! and salts thereof; processes for their preparation and 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： 本发明涉及下式的喹唑啉衍生物：其中：Y1表示-O - ， - S - ， - CH2-，-SO-，-SO2-，-NR5CO-，-CONR6-，-SO2NR7-，-NR8SO2- 或-NR 9 - （其中R 5，R 6，R 7，R 8和R 9各自独立地表示氢，烷基或烷氧基烷基）。 R 1表示氢，羟基，卤代，硝基，三氟甲基，氰基，烷基，烷氧基，烷硫基，氨基或烷基氨基。 R2代表氢，羟基，卤代，烷基，烷氧基，三氟甲基，氰基，氨基或硝基; m为1〜5的整数; R3表示羟基，卤代，烷基，烷氧基，烷酰氧基，三氟甲基，氰基，氨基或硝基; R4表示含有任选取代的吡啶酮，苯基或芳族杂环基团的基团及其盐; 其制备方法和含有式I化合物或其药学上可接受的盐的药物组合物作为活性成分。 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 and pharmaceutical compositions containing them
    8.
    再颁专利
    Quinazoline derivatives and pharmaceutical compositions containing them 失效
    喹唑啉衍生物和含有它们的药物组合物

    公开(公告)号：USRE42353E1

    公开(公告)日：2011-05-10

    申请号：US12170027

    申请日：1997-09-23

    申请人： Andrew Peter Thomas ,  Craig Johnstone ,  Edward Clayton ,  Elaine Sophie Elizabeth Stokes ,  Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin

    发明人： Andrew Peter Thomas ,  Craig Johnstone ,  Edward Clayton ,  Elaine Sophie Elizabeth Stokes ,  Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin

    IPC分类号： C07D239/72 ,  C07D401/00 ,  C07D403/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00

    CPC分类号： C07D401/12 ,  A61F13/02 ,  A61F13/023 ,  A61F2013/00221 ,  A61F2013/8408 ,  A61K31/517 ,  A61K31/541 ,  C07D239/94 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention relates to quinazoline derivatives of formula (1) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected from alkyl and a 5 or 6 membered saturated carbocyclic or heterocyclic group, 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 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（1）的喹唑啉衍生物，其中m为1至2的整数; R 1表示氢，羟基，卤代，硝基，三氟甲基，氰基，C 1-3烷基，C 1-3烷氧基，C 1-3烷硫基或-NR 5 R 6（其中R 5和R 6可以相同或不同，各自表示氢或C 1-3烷基 ）; R2代表氢，羟基，卤代，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; X 1表示-O - ， - CH 2 - ， - S - ， - SO - ， - SO 2 - ， - NR 7 CO-，-CONR 8 - ， - SO 2 NR 9 - ， - NR 10 SO 2 - 或-NR 11 - （其中R 7，R 8，R 9，R 10 和R 11各自独立地表示氢，C 1-3烷基或C 1-3烷氧基C 2-3 - 烷基）; R 4表示任选取代的5或6元饱和碳环或杂环基团或为烯基，炔基或任选取代的烷基的基团，该烷基可含有杂原子连接基团，该烯基，炔基或烷基可带有末端任选取代的 选自烷基和5或6元饱和碳环或杂环基团的基团，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在治疗许多疾病状态（包括癌症和类风湿性关节炎）中具有价值的性质。

    Quinazoline derivatives and pharmaceutical compositions containing them
    10.
    发明授权
    Quinazoline derivatives and pharmaceutical compositions containing them 有权
    喹唑啉衍生物和含有它们的药物组合物

    公开(公告)号：US06673803B2

    公开(公告)日：2004-01-06

    申请号：US10080716

    申请日：2002-02-25

    申请人： Andrew Peter Thomas ,  Craig Johnstone ,  Elaine Sophie Elizabeth Stokes ,  Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin

    发明人： Andrew Peter Thomas ,  Craig Johnstone ,  Elaine Sophie Elizabeth Stokes ,  Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin

    IPC分类号： A61K31517

    CPC分类号： C07D401/12 ,  A61F13/02 ,  A61F13/023 ,  A61F2013/00221 ,  A61F2013/8408 ,  A61K31/517 ,  A61K31/541 ,  C07D239/94 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention relates to quinazoline derivatives of formula (I) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl);R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected from alkyl and a 5 or 6 membered saturated carbocyclic or heterocyclic group, 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 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2的整数; R 1表示氢，羟基，卤代，硝基，三氟甲基，氰基，C 1-3烷基，C 1-3烷氧基，C 1-3烷硫基或-NR 5 R 6（其中R 5和R 6） ，其可以相同或不同，各自表示氢或C 1-3烷基）; R 2表示氢，羟基，卤代，甲氧基，氨基或硝基; R 3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; X 1表示-O-，CH 2 - ， - S - ， - SO - ， - SO 2 - ， - NR 7 CO - ， - CONR 8 - ， - SO 2 NR 9 - SO 2 - 或-NR 11 - （其中R 7，R 8，R 9，R 10和R 11各自独立地表示氢，C 1-3烷基或C 1-3烷氧基C 2-3 - ）; R 4表示任选取代的5或6元饱和碳环或杂环基团或为烯基，炔基或任选取代的烷基的基团，该烷基可含有杂原子连接基团，该烯基，炔基或烷基可以 携带选自烷基和5或6元饱和碳环或杂环基的任选被取代的基团及其盐; 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在治疗许多疾病状态（包括癌症和类风湿性关节炎）中具有价值的性质。