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1. 发明申请

US20110071144A1 QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：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。

2. 发明授权

US06414148B1 Quinazoline derivatives and pharmaceutical compositions containing them 有权
标题翻译：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。

3. 再颁专利

USRE42353E1 Quinazoline derivatives and pharmaceutical compositions containing them 失效
标题翻译：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。

4. 发明授权

US06897210B2 Quinazoline derivatives and pharmaceutical compositions containing them 有权
公开(公告)号：US06897210B2
公开(公告)日：2005-05-24
申请号：US10698388
申请日：2003-11-03
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： A61F13/00 , A61F13/02 , A61F13/15 , A61K20060101 , A61K31/505 , A61K31/517 , A61K31/5377 , A61K31/541 , A61P3/10 , A61P9/00 , A61P9/10 , A61P13/12 , A61P17/06 , A61P19/02 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/02 , A61P43/00 , C07D20060101 , C07D207/00 , C07D211/00 , C07D239/72 , C07D239/93 , C07D239/94 , C07D309/02 , C07D317/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/02 , C07D417/12 , A61K31/33
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 compostions 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 VEGP, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

5. 发明授权

US06673803B2 Quinazoline derivatives and pharmaceutical compositions containing them 有权
标题翻译：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。

6. 发明授权

US06291455B1 4-anilinoquinazoline derivatives 失效
标题翻译： 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

7. 发明授权

US06184225B2 Quinazoline derivatives as VEGF inhibitors 有权
标题翻译：喹唑啉衍生物作为VEGF抑制剂
公开(公告)号：US06184225B2
公开(公告)日：2001-02-06
申请号：US09125271
申请日：1998-08-13
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： A01N4354
CPC分类号： C07D239/88 , C07D239/93 , C07D239/94
摘要： The invention relates to quinazoline derivatives of formula (I) wherein: Z represents —O—, —NH— or —S—; m is an integer from 1 to 5; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluorometlyl, 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—, —NR6—, NR8CO—, —CONR9—SO2NR10— or —NR11SO2—, (wherein R7, R8, R9, R10 and R11 each represents C1-3alkyl, C1-3alkoxyC2-3alkyl); R4 represents 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 5 or 6 membered saturated carbocylic 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 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：Z表示-O - ， - NH-或-S-; m为1〜5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; X1表示-O - ， - CH2-，-S-，-SO-，SO2-，-NR6-，NR8CO-，-CONR9-SO2NR10-或-NR11SO2-，（其中R7，R8，R9，R10和R11各自表示C1-3烷基，C1-3烷氧基C2-3烷基）; R 4表示可以含有杂原子连接基团的烯基，炔基或任选取代的烷基的基团，该烯基，炔基或烷基可以带有末端任选取代的5或6元饱和碳环或杂环基; 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式（I）化合物及其药学上可接受的盐的药物组合物抑制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。

8. 发明申请

US20050239777A1 Quinazoline derivatives and pharmaceutical compositions containing them 审中-公开
公开(公告)号：US20050239777A1
公开(公告)日：2005-10-27
申请号：US11024840
申请日：2004-12-30
申请人： Andrew Thomas , Craig Johnstone , Edward Clayton , Elaine Elizabeth Stokes , Jean-Jacques Lohmann , Laurent Andre Hennequin
发明人： Andrew Thomas , Craig Johnstone , Edward Clayton , Elaine Elizabeth Stokes , Jean-Jacques Lohmann , Laurent Andre Hennequin
IPC分类号： A61F13/00 , A61F13/02 , A61F13/15 , A61K20060101 , A61K31/505 , A61K31/517 , A61K31/5377 , A61K31/541 , A61P3/10 , A61P9/00 , A61P9/10 , A61P13/12 , A61P17/06 , A61P19/02 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/02 , A61P43/00 , C07D20060101 , C07D207/00 , C07D211/00 , C07D239/72 , C07D239/93 , C07D239/94 , C07D309/02 , C07D317/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/02 , C07D417/12 , C07D43/02
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.

9. 发明申请

US20100137397A1 Chemical Compounds 审中-公开
标题翻译：化学化合物
公开(公告)号：US20100137397A1
公开(公告)日：2010-06-03
申请号：US11815418
申请日：2006-02-02
申请人： Alan Martin Birch , Craig Johnstone , Alleyn Thomas Plowright , Iain Simpson , Paul Robert Owen Whittamore
发明人： Alan Martin Birch , Craig Johnstone , Alleyn Thomas Plowright , Iain Simpson , Paul Robert Owen Whittamore
IPC分类号： A61K31/407 , C07D495/04 , A61P3/10 , A61P9/00 , A61P3/04
CPC分类号： C07D495/04
摘要： A compound of the formula (1) or a pharmaceutically-acceptable salt: possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity such as 2 diabetes. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.
摘要翻译：式（1）的化合物或药学上可接受的盐：具有糖原磷酸化酶抑制活性，因此在治疗与糖原磷酸化酶活性增加相关的疾病状态如2型糖尿病中具有价值。描述了制备含有它们的化合物和药物组合物的方法。

10. 发明授权

US07572826B2 Thiophene-carboxamide derivatives and their use as inhibitors of the enzyme IKK-2 失效
标题翻译：噻吩 - 甲酰胺衍生物及其作为IKK-2酶抑制剂的用途
公开(公告)号：US07572826B2
公开(公告)日：2009-08-11
申请号：US10542326
申请日：2004-01-13
申请人： Alan Wellington Faull , Craig Johnstone , Andrew David Morley , Jeffrey Philip Poyser
发明人： Alan Wellington Faull , Craig Johnstone , Andrew David Morley , Jeffrey Philip Poyser
IPC分类号： A61K31/381 , C07D333/36
CPC分类号： C07D409/12 , C07D333/38 , C07D333/44 , C07D413/12
摘要： The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, R4, R5 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译：本发明涉及式（I）的噻吩甲酰胺，其中A，R 1，R 2，R 3，R 4，R 5和X如说明书中所定义，其制备中使用的方法和中间体，含有它们的药物组合物及其在治疗中的用途。

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