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31. 发明授权

US06441012B1 Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US06441012B1
公开(公告)日：2002-08-27
申请号：US09744331
申请日：2001-01-23
申请人： David R Brittain , Craig Johnstone , Michael S Large , Gareth M Davies
发明人： David R Brittain , Craig Johnstone , Michael S Large , Gareth M Davies
IPC分类号： C07D26358
CPC分类号： C07D263/58 , C07D413/04
摘要： Compound of formula (I) wherein: A is a bicyclic heteroaryl, optionally substituted with one or more substituents; B is linker group connecting group A to group D and comprising a 3 or 4 atom linker where each atom is independently selected from carbon, oxygen, nitrogen and sulphur and is optionally subsituted with one or more C1-6 alkyl groups or two of such adjacent alkyl substituents may form a ring; C is aryl or a mono or bicyclic heteroaryl, each of which can be optionally substituted; D is an aryl or heteroaryl, both of which are optionally substituted R1 is hydrogen, C1-5 alkyl, C1-3 alkanoyl or C1-3 alkoxycarbonyl; R2 to R5 are each independently selected from hydrogen, C1-6 alkyl, aryl and heteroaryl containing up to 2 heteroatoms chosen from oxygen, sulphur and nitrogen, the aryl and heteroaryl optionally substituted with C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-4 alkoxy, C1-4 alkanoyl, C1-6 alkylamino, C1-4alkylC1-6alkyoxyl, C1-6alkylaminoC1-6alkyl, nitro, cyano, halogeno, trifluoromethyl, hydroxy, (CH2)pOH where p is 1 or 2, —CO2Ra, and —CONRaRb, where Ra and Rb are independently selected from hydrogen and C1-6 alkyl or two of R2 to R5 can be taken together to form a 3 to 7 membered ring; R6 is an acidic functional group; r and s are each independently 0 or 1 with the proviso that r and s cannot both be 0; or a pharmaceutically acceptable salt or in vivo hydrolysable derivative thereof.
摘要翻译：式（I）的化合物，其中：A是任选被一个或多个取代基取代的二环杂芳基; B是连接基团A与D组并且包含3或4个原子连接体的连接基团，其中每个原子独立地选自碳，氧，氮和硫，并且任选被一个或多个C 1-6烷基取代或两个相邻的烷基取代基可以形成环; C是芳基或单或双环杂芳基，其各自可任选被取代; D是芳基或杂芳基，它们都是任选取代的R 1是氢，C 1-5烷基，C 1-3烷酰基或C 1-3烷氧基羰基; R 2至R 5各自独立地选自氢，C 1-6烷基，芳基和含有至多2个选自氧，硫和氮的杂原子的杂芳基，芳基和杂芳基任选被C 1-6烷基，C 2-6烯基， 6-炔基，C 1-4烷氧基，C 1-4烷酰基，C 1-6烷基氨基，C 1-4烷基C 1-6烷氧基，C 1-6烷基氨基C 1-6烷基，硝基，氰基，卤代，三氟甲基，羟基，（CH 2）p OH其中p为1或2 ，-CO 2 R a和-CONR a R b，其中R a和R b独立地选自氢和C 1-6烷基，或者R 2至R 5中的两个可以一起形成3至7元环; R6是酸性官能团; r和s各自独立地为0或1，条件是r和s不能都是0; 或其药学上可接受的盐或体内可水解的衍生物。

32. 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

33. 发明授权

US5866572A Quinazoline derivatives 失效
标题翻译：喹唑啉衍生物
公开(公告)号：US5866572A
公开(公告)日：1999-02-02
申请号：US796483
申请日：1997-02-13
申请人： Andrew John Barker , Craig Johnstone
发明人： Andrew John Barker , Craig Johnstone
IPC分类号： A61P35/00 , C07D239/94 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D521/00 , A61K31/505 , A61K31/535
CPC分类号： C07D231/12 , C07D233/56 , C07D239/94 , C07D249/08 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14
摘要： The invention concerns quinazoline derivatives of the formula I ##STR1## wherein X.sup.1 is a direct link or a group such as CO, C(R.sup.2).sub.2 and CH(OR.sup.2);wherein Q.sup.1 is phenyl, naphthyl or a 5- or 6-membered heteroaryl moiety and Q.sup.1 optionally bears up to 3 substituents;wherein m is 1 or 2 and each R.sup.1 may be a group such as hydrogen, halogeno and trifluoromethyl; andwherein Q.sup.2 may be phenyl or a 9- or 10-membered bicyclic heterocyclic moiety and Q.sup.2 optionally bears up to 3 substituents;or a pharmaceutically-acceptable salt thereof;processes for their preparation, pharmaceutical compositions containing them and the use of their receptor tyrosine kinase inhibitory properties in the treatment of proliferative disease such as cancer.
摘要翻译：本发明涉及式I的喹唑啉衍生物，其中X1是直接键或诸如CO，C（R 2）2和CH（OR 2）的基团; 其中Q1是苯基，萘基或5-或6-元杂芳基部分，并且Q1任选地带有至多3个取代基; 其中m为1或2，并且每个R 1可以为诸如氢，卤代和三氟甲基的基团; 并且其中Q2可以是苯基或9-或10-元双环杂环部分，Q2任选地带有多达3个取代基; 或其药学上可接受的盐; 其制备方法，含有它们的药物组合物及其受体酪氨酸激酶抑制性质在治疗增殖性疾病如癌症中的用途。

34. 发明申请

US20100029754A1 THIOPHENE-CARBOXAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF THE ENZYME IKK-2 审中-公开
标题翻译：三苯甲酰胺衍生物及其作为酶的抑制剂IKK-2
公开(公告)号：US20100029754A1
公开(公告)日：2010-02-04
申请号：US12537532
申请日：2009-08-07
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 , C07D333/38 , A61P29/00 , A61P11/00
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。

35. 发明申请

US20090124682A1 Indan-Amide Derivatives with Glycogen Phosphorylase Inhibitory Activity 审中-公开
标题翻译：具有糖原磷酸化酶抑制活性的茚满酰胺衍生物
公开(公告)号：US20090124682A1
公开(公告)日：2009-05-14
申请号：US11883770
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： A61K31/40 , C07D209/42 , A61P3/10 , A61P3/04 , A61P9/10
CPC分类号： C07D209/42
摘要： A compound of the formula (1) or a pharmaceutically-acceptable salt: (A chemical formula should be inserted here—please see paper copy enclosed herewith) (1) possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.
摘要翻译：式（1）化合物或其药学上可接受的盐：（化学式应插入此处，请参见随附的纸质复制品）（1）具有糖原磷酸化酶抑制活性，因此具有治疗疾病相关的价值具有增加的糖原磷酸化酶活性。描述了制备含有它们的化合物和药物组合物的方法。

36. 发明授权

US07098240B2 Compounds 失效
标题翻译：化合物
公开(公告)号：US07098240B2
公开(公告)日：2006-08-29
申请号：US10484645
申请日：2002-07-19
申请人： David Griffiths , Craig Johnstone
发明人： David Griffiths , Craig Johnstone
IPC分类号： A61K31/38 , C07D409/00 , C07D333/36
CPC分类号： C07D409/04
摘要： The invention relates to thiophene carboxamides of formula (I), wherein R1, R2, R3, A, n 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R 1，R 2，R 3，A，n和X分别为在其制备中使用的说明书，方法和中间体中定义，含有它们的药物组合物及其在治疗中的用途

37. 发明申请

US20060058522A1 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酶ikk-2的抑制剂的用途
公开(公告)号：US20060058522A1
公开(公告)日：2006-03-16
申请号：US10542326
申请日：2004-01-13
申请人： Alan Faull , Craig Johnstone , Andrew Morley , Jeffrey Poyser
发明人： Alan Faull , Craig Johnstone , Andrew Morley , Jeffrey Poyser
IPC分类号： C07D417/02 , C07D413/02 , C07D409/02
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

38. 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.

39. 发明授权

US06897214B2 Quinazoline derivatives 失效
标题翻译：喹唑啉衍生物
公开(公告)号：US06897214B2
公开(公告)日：2005-05-24
申请号：US10136276
申请日：2002-05-02
申请人： Andrew John Barker , Craig Johnstone
发明人： Andrew John Barker , Craig Johnstone
IPC分类号： A61P35/00 , C07D239/94 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D521/00 , C07D40/00 , A61K31/535 , C07D239/72
CPC分类号： C07D231/12 , C07D233/56 , C07D239/94 , C07D249/08 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14
摘要： The invention concerns quinazoline derivatives of the formula I wherein X1 is a direct link or a group such as CO, C(R2)2 and CH(OR2); wherein Q1 is phenyl, naphthyl or a 5- or 6-membered heteroaryl moiety and Q1 optionally bears up to 3 substituents; wherein m is 1 or 2 and each R1 may be a group such as hydrogen, halogeno and trifluoromethyl; and wherein Q2 may be phenyl or a 9- or 10-membered bicyclic heterocyclic moiety and Q2 optionally bears up to 3 substituents; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and the use of their receptor tyrosine kinase inhibitory properties in the treatment of proliferative disease such as cancer.
摘要翻译：本发明涉及式I的喹唑啉衍生物，其中X 1是直链，或基团如CO，C（R 2）2，和CH（OR 2）; 其中Q 1是苯基，萘基或5或6元杂芳基部分和Q 1至多3个取代基; 其中m为1或2，并且每个R 1可以为诸如氢，卤代和三氟甲基的基团; 并且其中Q 2可以是苯基或9或10元双环杂环部分，Q 2任选地带有至多3个取代基; 或其药学上可接受的盐; 其制备方法，含有它们的药物组合物及其受体酪氨酸激酶抑制性质在治疗增殖性疾病如癌症中的用途。

40. 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。

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