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47 条记录 (耗时 0.071 秒)

    Pyrimidine derivatives possessing cell-cycle inhibitors activity
    31.
    发明授权
    Pyrimidine derivatives possessing cell-cycle inhibitors activity 失效
    具有细胞周期抑制剂活性的嘧啶衍生物

    公开(公告)号：US07579344B2

    公开(公告)日：2009-08-25

    申请号：US10556607

    申请日：2004-05-12

    申请人： David William Heaton ,  Andrew Peter Thomas

    发明人： David William Heaton ,  Andrew Peter Thomas

    IPC分类号： C07D471/04 ,  A61K31/415 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Compounds of the formula (I), and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti cell proliferation) effect in a warm blooded animal, such as man.

    摘要翻译： 描述了式（I）化合物及其药学上可接受的盐和体内可水解的酯。 还描述了其制备方法及其作为药物的用途，特别是用于在温血动物如人中产生细胞周期抑制（抗细胞增殖）作用的药物。

    Pyrimidines as Igf-I Inhibitors
    35.
    发明申请
    Pyrimidines as Igf-I Inhibitors 审中-公开
    嘧啶类作为Igf-I抑制剂

    公开(公告)号：US20080161330A1

    公开(公告)日：2008-07-03

    申请号：US11909943

    申请日：2006-03-31

    申请人： Andrew Peter Thomas

    发明人： Andrew Peter Thomas

    IPC分类号： A61K31/506 ,  C07D413/14 ,  A61P35/00

    CPC分类号： C07D413/04

    摘要： A compound of formula (I) wherein the substituents are as defined in the text for use in inhibiting insulin-like growth factor 1 receptor activity in a warm blooded animal such as man.

    摘要翻译： 式（I）的化合物，其中取代基如文中所定义，用于在温血动物如人中抑制胰岛素样生长因子1受体活性。

    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

    申请人： Andrew Peter Thomas ,  Laurent Francois Andre Hennequin ,  Patrick Ple

    发明人： Andrew Peter Thomas ,  Laurent Francois Andre Hennequin ,  Patrick Ple

    IPC分类号： C07D21522

    CPC分类号： C07D215/233 ,  C07D215/44 ,  C07D215/48 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D417/12 ,  C07D471/04

    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。

    Quinazoline derivatives and pharmaceutical compositions containing them
    38.
    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。

    Chemical compounds
    39.
    发明授权
    Chemical compounds 有权
    化合物

    公开(公告)号：US06362336B1

    公开(公告)日：2002-03-26

    申请号：US09877005

    申请日：2001-06-11

    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： C07D29372

    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: [wherein: Y1 represents —O—, —S—, —CH2—, —SO—, —SO2—, —NR5CO—, —CONR6—, —SO2NR7—, —NR8SO2— or —NR9— (wherein R5, R6, R8 and R9 each independently represents hydrogen, alkyl or alkoxyalkyl); R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, alkyl, alkoxy, alkylthio, amino or alkylamino. R2 represents hydrogen, hydroxy, halogeno, alkyl, alkoxy, trifluoromethyl, cyano, amino or nitro; m is an integer from 1 to 5; R3 represents hydroxy, halogeno, alkyl, alkoxy, alkanoyloxy, trifluoromethyl, cyano, amino or nitro; R4 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 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。 ，羟基，卤代，烷基，烷氧基，三氟甲基，氰基，氨基或硝基; m为1至5的整数; R 3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; 其为或含有任选取代的吡啶酮，苯基或芳族杂环基]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，其在治疗数目中具有价值 的疾病状态，包括癌症和类风湿性关节炎。

    4-anilinoquinazoline derivatives
    40.
    发明授权
    4-anilinoquinazoline derivatives 失效
    4-苯胺基喹唑啉衍生物

    公开(公告)号：US06291455B1

    公开(公告)日：2001-09-18

    申请号：US09142339

    申请日：1998-09-08

    申请人： Andrew Peter Thomas ,  Craig Johnstone ,  Laurent Francois Andre Hennequin

    发明人： Andrew Peter Thomas ,  Craig Johnstone ,  Laurent Francois Andre Hennequin

    IPC分类号： A61K31517

    CPC分类号： C07D239/94

    摘要： The invention relates to quinazoline derivatives of formula (I) (wherein: R1 represents hydrogen or methoxy; R2 represents methoxy, ethoxy, 2-methoxyethoxy, 3-methoxypropoxy, 2-ethoxyethoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, 2-hydroxyethoxy, 3-hydroxypropoxy, 2-(N,N-dimethylamino)ethoxy, 3-(N,N-dimethylamino)propoxy, 2-morpholinoethoxy, 3-morpholinopropoxy, 4-morpholinobutoxy, 2-piperidinoethoxy, 3-piperidinopropoxy, 4-piperidinobutoxy, 2-(piperazin-1-yl)ethoxy, 3-(piperazin-1-yl)propoxy, 4-(piperazin-1-yl)butoxy, 2-(4-methylpiperazin-1-yl)ethoxy, 3-(4methylpiperazin-1-yl)propoxy or 4-(4-methylpiperazin-1-yl)butoxy; the phenyl group bearing (R3)2 is selected from: 2-fluoro-5-hydroxyphenyl, 4-bromo-2-fluorophenyl, 2,4-difluorophenyl, 4-chloro-2-fluorophenyl, 2-fluoro-4-methylphenyl, 2-fluoro-4-methoxyphenyl, 4-bromo-3-hydroxyphenyl, 4-fluoro-3-hydroxyphenyl, 4-chloro-3-hydroxyphenyl, 3-hydroxy-4-methylphenyl, 3-hydroxy-4-methoxyphenyl and 4-cyano-2-fluorophenyl); 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： 本发明涉及式（I）的喹唑啉衍生物（其中：R1代表氢或甲氧基; R2代表甲氧基，乙氧基，2-甲氧基乙氧基，3-甲氧基丙氧基，2-乙氧基乙氧基，三氟甲氧基，2,2,2-三氟乙氧基， 3-（N，N-二甲基氨基）乙氧基，3-（N，N-二甲基氨基）丙氧基，2-吗啉代乙氧基，3-吗啉代丙氧基，4-吗啉代丁氧基，2-哌啶子基乙氧基，3-哌啶基丙氧基， 哌啶基丁氧基，2-（哌嗪-1-基）乙氧基，3-（哌嗪-1-基）丙氧基，4-（哌嗪-1-基）丁氧基，2-（4-甲基哌嗪-1-基） （4-甲基哌嗪-1-基）丙氧基或4-（4-甲基哌嗪-1-基）丁氧基;带有（R3）2的苯基选自：2-氟-5-羟基苯基，4-溴-2-氟苯基， 2,4-二氟苯基，4-氯-2-氟苯基，2-氟-4-甲基苯基，2-氟-4-甲氧基苯基，4-溴-3-羟基苯基，4-氟-3-羟基苯基， 3-羟基-4-甲基苯基，3-羟基-4-甲氧基苯基和4-氰基-2-氟苯基）; 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， 治疗许多疾病状态（包括癌症和类风湿性关节炎）的价值