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1. 发明申请

WO2005040159A1 4-(PYRAZOL-3-YLAMINO) PYRIMIDINE DERIVATIVES FOR USE IN THE TREATMENT OF CANCER 审中-公开
标题翻译： 4-（PYRAZOL-3-YLAMINO）吡嗪衍生物用于治疗癌症
公开(公告)号：WO2005040159A1
公开(公告)日：2005-05-06
申请号：PCT/GB2004/004307
申请日：2004-10-11
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , NOWAK, Thorsten , THOMAS, Andrew, Peter
发明人： NOWAK, Thorsten , THOMAS, Andrew, Peter
IPC分类号： C07D413/14
CPC分类号： C07D413/14 , C07D417/14 , C07D471/10
摘要： A compound of Formula (I); wherein the substituents are as defined in the text for use in modulating 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调节胰岛素样生长因子1受体活性。

2. 发明申请

WO2004101549A1 2-ANILINO-4-(IMIDAZOL-5-YL)-PYRIMIDINE DERIVATIVES AND THEIR USE AS CDK (CDK2) INHIBITORS 审中-公开
标题翻译： 2-苯胺基-4-（咪唑-5-基） - 吡啶衍生物及其作为CDK（CDK2）抑制剂的用途
公开(公告)号：WO2004101549A1
公开(公告)日：2004-11-25
申请号：PCT/GB2004/002025
申请日：2004-05-12
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , THOMAS, Andrew, Peter
发明人： THOMAS, Andrew, Peter
IPC分类号： C07D403/04
CPC分类号： C07D401/14 , C07D403/04 , C07D409/14
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。

3. 发明申请

WO2002096887A1 2-ANILINO-PYRIMIDINE DERIVATIVES AS CYCLIN DEPENDENT KINASE INHIBITORS 审中-公开
标题翻译：作为CYCLIN依赖性激酶抑制剂的2-苯胺基吡啶衍生物
公开(公告)号：WO2002096887A1
公开(公告)日：2002-12-05
申请号：PCT/GB2002/002428
申请日：2002-05-24
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , NEWCOMBE, Nicholas, John , THOMAS, Andrew, Peter
发明人： NEWCOMBE, Nicholas, John , THOMAS, Andrew, Peter
IPC分类号： C07D239/47
CPC分类号： C07D239/47 , A61K31/505 , C07D405/12
摘要： Compounds of the formula (I): wherein R 1 , R 2 , R 3 , p, q, and X are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters 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：式（I）的化合物：其中R 1，R 2，R 3，p，q和X如上所定义，并且描述了药学上可接受的盐和体内可水解的酯。还描述了它们的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。

4. 发明申请

WO2002066481A1 PYRIMIDINE DERIVATIVES FOR INHIBITION OF CELL-PROLIFERATION 审中-公开
标题翻译：用于抑制细胞增殖的吡嗪衍生物
公开(公告)号：WO2002066481A1
公开(公告)日：2002-08-29
申请号：PCT/GB2002/000603
申请日：2002-02-12
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , THOMAS, Andrew, Peter
发明人： THOMAS, Andrew, Peter
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Compounds of the formula (I): wherein Ring A, R 1 , R 3 , R 4 , p, q, and n are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters 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-quest-blooded animal, such as man.
摘要翻译：式（I）的化合物：其中环A，R 1，R 3，R 4，p，q和n如上所定义，并且描述了药学上可接受的盐和体内可水解的酯。还描述了它们的制备方法及其作为药物的用途，特别是用于在热血追寻血液动物如人中产生细胞周期抑制（抗细胞增殖）作用的药物。

5. 发明申请

WO2008075068A3 ACYLAMINOPYRAZOLES AS FGFR INHIBITORS 审中-公开
标题翻译：作为FGFR抑制剂的亚氨基酰胺
公开(公告)号：WO2008075068A3
公开(公告)日：2008-10-02
申请号：PCT/GB2007004917
申请日：2007-12-20
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , FOOTE KEVIN MICHAEL , THEOCLITOU MARIA-ELENA , THOMAS ANDREW PETER , BUTTAR DAVID
发明人： FOOTE KEVIN MICHAEL , THEOCLITOU MARIA-ELENA , THOMAS ANDREW PETER , BUTTAR DAVID
IPC分类号： C07D231/40 , A61K31/415 , A61P35/00 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/04
CPC分类号： C07D231/40 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D471/04 , C07D487/04
摘要： There is provided a compound of formula (I); or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
摘要翻译：提供式（I）化合物; 或其药学上可接受的盐。还提供了制备式1化合物的方法和式1化合物作为药物和用于治疗癌症的用途。

6. 发明申请

WO2008075068A2 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2008075068A2
公开(公告)日：2008-06-26
申请号：PCT/GB2007/004917
申请日：2007-12-20
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , FOOTE, Kevin, Michael , THEOCLITOU, Maria-Elena , THOMAS, Andrew, Peter , BUTTAR, David
发明人： FOOTE, Kevin, Michael , THEOCLITOU, Maria-Elena , THOMAS, Andrew, Peter , BUTTAR, David
CPC分类号： C07D231/40 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D471/04 , C07D487/04
摘要： There is provided a compound of formula (I); or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
摘要翻译：提供式（I）化合物; 或其药学上可接受的盐。还提供了制备式1化合物的方法和式1化合物作为药物和用于治疗癌症的用途。

7. 发明申请

WO2008001070A1 PYRIMIDINE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER 审中-公开
标题翻译：吡嗪衍生物可用于治疗癌症
公开(公告)号：WO2008001070A1
公开(公告)日：2008-01-03
申请号：PCT/GB2007/002381
申请日：2007-06-27
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BUTTAR, David , FOOTE, Kevin, Michael , NOWAK, Thorsten , RUDGE, David, Alan , THEOCLITOU, Maria-Elena , THOMAS, Andrew, Peter
发明人： BUTTAR, David , FOOTE, Kevin, Michael , NOWAK, Thorsten , RUDGE, David, Alan , THEOCLITOU, Maria-Elena , THOMAS, Andrew, Peter
IPC分类号： C07D413/14 , A61K31/506 , A61P35/00
CPC分类号： C07D413/14
摘要： There is provided a compound of formula (I): processes for the manufacture thereof, pharmaceutical compositions thereof and uses in therapy.
摘要翻译：提供式（I）的化合物：其制备方法，其药物组合物和治疗用途。

8. 发明申请

WO2003076435A1 PYRIMIDINE COMPOUNDS 审中-公开
标题翻译：吡嗪化合物
公开(公告)号：WO2003076435A1
公开(公告)日：2003-09-18
申请号：PCT/GB2003/000957
申请日：2003-03-06
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , NEWCOMBE, Nicholas, John , THOMAS, Andrew, Peter
发明人： NEWCOMBE, Nicholas, John , THOMAS, Andrew, Peter
IPC分类号： C07D403/04
CPC分类号： C07D403/04 , C07D405/14
摘要： Compounds of the formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters 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：描述式（I）的化合物，其中R 1，R 2，R 3，R 4，R 5和p如本文所定义，并且其药学上可接受的盐和体内可水解的酯。还描述了它们的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。

9. 发明申请

WO2003076433A1 PYRIMIDINE COMPOUNDS 审中-公开
标题翻译：吡嗪化合物
公开(公告)号：WO2003076433A1
公开(公告)日：2003-09-18
申请号：PCT/GB2003/000904
申请日：2003-03-06
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , NEWCOMBE, Nicholas, John , THOMAS, Andrew, Peter
发明人： NEWCOMBE, Nicholas, John , THOMAS, Andrew, Peter
IPC分类号： C07D403/04
CPC分类号： C07D403/04
摘要： Compounds of the formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and p are as defined within and a pharmaceutically acceptable salts and ( in vivo hydrolysable esters 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：其中R 1，R 2，R 3，R 4，R 5，R 6和p的式（I）化合物和其药学上可接受的盐和（还描述了它们的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。

10. 发明申请

WO1997032856A1 4-ANILINOQUINAZOLINE DERIVATIVES 审中-公开
标题翻译： 4-苯胺氮杂环丁烷衍生物
公开(公告)号：WO1997032856A1
公开(公告)日：1997-09-12
申请号：PCT/GB1997000550
申请日：1997-02-28
申请人： ZENECA LIMITED , ZENECA PHARMA S.A. , THOMAS, Andrew, Peter , HENNEQUIN, Laurent, François, André , JOHNSTONE, Craig
发明人： ZENECA LIMITED , ZENECA PHARMA S.A.
IPC分类号： C07D239/94
CPC分类号： C07D239/94
摘要： The invention relates to quinazoline derivatives of formula (I) (wherein: R represents hydrogen or methoxy; R 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-(4-methylpiperazin-1-yl)propoxy or 4-(4-methylpiperazin-1-yl)butoxy; the phenyl group bearing (R )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：R 1表示氢或甲氧基; R 2表示甲氧基，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-（N，N-二甲基氨基）乙氧基，3-（N，N-二甲氨基）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）乙氧基，3-（4-甲基哌嗪-1-基）丙氧基或4-（4-甲基哌嗪-1-基）丁氧基;带有（R 3）2的苯基选自：2-氟-5 4-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 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）。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。

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