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公开(公告)号：US06602863B1
公开(公告)日：2003-08-05
申请号：US09671559
申请日：2000-09-27
申请人： Alexander James Bridges , William Alexander Denny , Ellen Myra Dobrusin , Annette Marian Doherty , David William Fry , Dennis Joseph McNamara , Howard Daniel Hollis Showalter , Jeffrey B. Smaill , Hairong Zhou
发明人： Alexander James Bridges , William Alexander Denny , Ellen Myra Dobrusin , Annette Marian Doherty , David William Fry , Dennis Joseph McNamara , Howard Daniel Hollis Showalter , Jeffrey B. Smaill , Hairong Zhou
IPC分类号： A61K31333
CPC分类号： C07D231/12 , C07D233/56 , C07D239/94 , C07D249/08 , C07D403/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07F9/6561
摘要： The present invention provides compounds that are irreversible inhibitors of tyrosine kinases. Also provided is a method of treating cancer, restenosis, atherosclerosis, endometriosis, and psoriasis and a pharmaceutical composition that comprises a compound that is an irreversible inhibitor of tyrosine kinases.
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12.发明授权Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family 失效能够抑制表皮生长因子受体家族酪氨酸激酶的双环化合物公开(公告)号：US06713484B2
公开(公告)日：2004-03-30
申请号：US10201808
申请日：2002-07-24
IPC分类号： A61K31519
CPC分类号： C07D471/04 , A61K31/4985 , A61K31/519 , C07D473/34 , C07D495/04
摘要： Described are heterocyclic pyrimidine derivatives and a method of inhibiting epidermal growth factor by treating, with an effective inhibiting amount, a mammal, in need thereof, a compound of the formula: where: at least two of A-E are nitrogen, with the remaining atom(s) carbon; X=NH or NR7, such that R7=lower alkyl (1-4 carbon atoms), OH, NH2, lower alkoxy (1-4 carbon atoms) or lower monoalkylamino (1-4 carbon atoms); n=0, 1, 2. The remaining substituents are described in detail in the specification.
摘要翻译： 描述的是杂环嘧啶衍生物和抑制表皮生长因子的方法，其中：有效抑制量的哺乳动物，有需要的下列化合物：其中：至少两个AE是氮，剩余的原子（ s）碳; X = NH或NR 7，使得R 7 =低级烷基（1-4个碳原子），OH，NH 2，低级烷氧基（1-4个碳原子）或低级单烷基氨基（1-4 碳原子）; n = 0,1,2。其余取代基在说明书中详细描述。
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13.发明授权Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family 失效能够抑制表皮生长因子受体家族酪氨酸激酶的双环化合物公开(公告)号：US06521620B1
公开(公告)日：2003-02-18
申请号：US09183190
申请日：1998-10-30
IPC分类号： A61K314985
CPC分类号： C07D471/04 , A61K31/4985 , A61K31/519 , C07D473/34 , C07D495/04
摘要： Described are heterocyclic pyrimidine derivatives and a method of inhibiting epidermal growth factor by treating, with an effective inhibiting amount, a mammal, in need thereof, a compound of the formula: where: at least two of A-E are nitrogen, with the remaining atom(s) carbon; X=NH or NR7, such that R7=lower alkyl (1-4 carbon atoms), OH, NH2, lower alkoxy (1-4 carbon atoms) or lower monoalkylamino (1-4 carbon atoms); n=0, 1, 2. The remaining substituents are described in detail in the specification.
摘要翻译： 描述的是杂环嘧啶衍生物和抑制表皮生长因子的方法，其中：有效抑制量的哺乳动物，有需要的下列化合物：其中：至少两个AE是氮，剩余的原子（ X = NH或NR7，使得R7 =低级烷基（1-4个碳原子），OH，NH2，低级烷氧基（1-4个碳原子）或低级单烷基氨基（1-4个碳原子）; n = 剩余的取代基在说明书中详细描述。
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公开(公告)号：US6153617A
公开(公告)日：2000-11-28
申请号：US269647
申请日：1999-03-25
IPC分类号： C07D401/04 , C07D403/04 , C07D471/04 , C07D487/04 , C07D495/04 , A61K31/489 , C07D239/72
CPC分类号： C07D401/04 , C07D403/04 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The invention provides compounds of Formula I ##STR1## that are irreversible inhibitors of tyrosine kinases. Also provided is a method of treating cancer, restenosis, atherosclerosis, endometriosis, and psoriasis and a pharmaceutical composition that comprises a compound that is an irreversible inhibitor of tyrosine kinases.
摘要翻译： PCT No.PCT / US98 / 15592 Sec。 371日期1999年3月25日 102（e）1999年3月25日PCT提交1998年7月29日PCT公布。 出版物WO99 / 06396 日期1999年2月11日本发明提供了作为酪氨酸激酶不可逆抑制剂的式I化合物。 还提供了治疗癌症，再狭窄，动脉粥样硬化，子宫内膜异位症和牛皮癣的方法以及包含作为酪氨酸激酶不可逆抑制剂的化合物的药物组合物。
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公开(公告)号：US6127374A
公开(公告)日：2000-10-03
申请号：US269545
申请日：1999-03-25
IPC分类号： C07D239/74 , C07D239/88 , C07D239/93 , C07D239/94 , C07D401/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D495/04 , A61K31/517
CPC分类号： C07D401/12 , C07D239/74 , C07D239/88 , C07D239/93 , C07D239/94 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： This invention provides irreversible inhibitors of tyrosine kinases having for formula ##STR1## which compounds are useful for treating cancer, restenosis, atherosclerosis, endometriosis and psoriasis.
摘要翻译： PCT No.PCT / US98 / 15784 Sec。 371日期1999年3月25日 102（e）1999年3月25日PCT提交1998年7月29日PCT公布。 公开号WO99 / 06378 日期1999年2月11日本发明提供具有下式的酪氨酸激酶的不可逆抑制剂，其化合物可用于治疗癌症，再狭窄，动脉粥样硬化，子宫内膜异位症和牛皮癣。
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16.发明授权4-bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors 失效4-溴或4-碘苯基氨基苯并肟酸衍生物及其作为MEK抑制剂的用途公开(公告)号：US07169816B2
公开(公告)日：2007-01-30
申请号：US11249543
申请日：2005-10-12
申请人： Stephen Douglas Barrett , Alexander James Bridges , Annette Marian Doherty , David Thomas Dudley , Alan Robert Saltiel , Haile Tecle
发明人： Stephen Douglas Barrett , Alexander James Bridges , Annette Marian Doherty , David Thomas Dudley , Alan Robert Saltiel , Haile Tecle
IPC分类号： A61K31/166 , C07D233/64
CPC分类号： C07D295/088 , C07C259/10 , C07D211/22 , C07D213/30 , C07D307/42 , C07D309/06 , C07D333/16
摘要： Phenylamino benzhydroxamic acid derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.
摘要翻译： 下式的苯基氨基苯并肟酸衍生物其中R 1，R 2，R 3，R 4，R 4， R 5和R 6是氢或取代基如烷基，并且其中R 7是氢或有机基团是MEK的有效抑制剂 因此，在治疗癌症和其它增殖性疾病如牛皮癣和再狭窄方面是有效的。
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17.发明授权Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family 失效能抑制表皮生长因子受体家族酪氨酸激酶的三环化合物公开(公告)号：US06596726B1
公开(公告)日：2003-07-22
申请号：US08811803
申请日：1997-03-06
申请人： Alexander James Bridges , William Alexander Denny , David Fry , Alan Kraker , Robert Frederick Meyer , Gordon William Rewcastle , Andrew Mark Thompson , Howard Daniel Hollis Showalter
发明人： Alexander James Bridges , William Alexander Denny , David Fry , Alan Kraker , Robert Frederick Meyer , Gordon William Rewcastle , Andrew Mark Thompson , Howard Daniel Hollis Showalter
IPC分类号： A61K31505
CPC分类号： C07D471/04 , C07D239/70 , C07D471/14 , C07D473/34 , C07D487/04 , C07D491/04 , C07D491/14 , C07D495/04 , C07D513/04 , C07D513/14
摘要： Described are compounds of the following formula and a method of inhibiting epidermal growth factor by treating, with an effective inhibiting amount, a mammal, in need thereof, a compound of the formula: wherein the formula terms are described in the specification and wherein the members in the aforementioned structure are defined in the specification.
摘要翻译： 描述了下式的化合物和抑制表皮生长因子的方法：通过以有效抑制量治疗有需要的哺乳动物，下式的化合物：其中式术语在说明书中描述，其中成员 上述结构在说明书中定义。
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公开(公告)号：US06545030B1
公开(公告)日：2003-04-08
申请号：US09889104
申请日：2002-01-17
IPC分类号： A61K3141
CPC分类号： C07D291/04 , A61K45/06 , C07D231/20 , C07D231/46 , C07D249/06 , C07D249/12 , C07D249/14 , C07D257/04 , C07D263/10 , C07D271/07 , C07D275/03 , C07D285/08
摘要： 1-Heterocycle substituted diarylamines, methods of making and using them, and compositions containing them.
摘要翻译： 1-杂环取代的二芳基胺，其制备和使用方法，以及含有它们的组合物。
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![N-[4-(3-chloro-4-fluoro-phenylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6-yl]-acrylamide, and irreversible inhibitor of tyrosine kinases](/abs-image/US/2002/02/05/US06344455B1/abs.jpg.150x150.jpg)
19.发明授权N-[4-(3-chloro-4-fluoro-phenylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6-yl]-acrylamide, and irreversible inhibitor of tyrosine kinases 失效N- [4-（3-氯-4-氟 - 苯基氨基）-7-（3-吗啉-4-基 - 丙氧基） - 喹唑啉-6-基] - 丙烯酰胺和酪氨酸激酶的不可逆抑制剂公开(公告)号：US06344455B1
公开(公告)日：2002-02-05
申请号：US09831991
申请日：2001-05-16
IPC分类号： A61K315377
CPC分类号： C07D239/94
摘要： This invention relates to the compound N-[4-(3-chloro4-fluoro-phenylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6-yl]-acrylamide that is an irreversible inhibitor of tyrosine kinases. This invention also relates to a method of treating cancer, atherosclerosis, restenosis, endometriosis, and psoriasis using the compound N-[4-(3-chloro4-fluoro-phenylamino)-7-(3-morpholin4-yl-propoxy)-quinazolin-6-yl]-acrylamide, and to a pharmaceutical composition that comprises the compound N-[4-(3-chloro4-fluoro-phenylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6-yl]-acrylamide.
摘要翻译： 本发明涉及作为酪氨酸不可逆抑制剂的化合物N- [4-（3-氯-4-氟 - 苯基氨基）-7-（3-吗啉-4-基 - 丙氧基） - 喹唑啉-6-基] - 丙烯酰胺 激酶。 本发明还涉及使用化合物N- [4-（3-氯-4-氟 - 苯基氨基）-7-（3-吗啉-4-基 - 丙氧基） - 喹唑啉的方法治疗癌症，动脉粥样硬化，再狭窄，子宫内膜异位症和牛皮癣 -6-基] - 丙烯酰胺，以及包含化合物N- [4-（3-氯-4-氟 - 苯基氨基）-7-（3-吗啉-4-基 - 丙氧基） - 喹唑啉-6-基] 吡啶-3-基] - 丙烯酰胺。
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20.发明授权2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors 失效2-（4-溴或4-碘苯基氨基）苯甲酸衍生物及其作为MEK抑制剂的用途公开(公告)号：US06310060B1
公开(公告)日：2001-10-30
申请号：US09462319
申请日：2000-01-05
申请人： Stephen Douglas Barrett , Alexander James Bridges , Donna Reynolds Cody , Annette Marian Doherty , David Thomas Dudley , Alan Robert Saltiel , Mel Conrad Schroeder , Haile Tecle
发明人： Stephen Douglas Barrett , Alexander James Bridges , Donna Reynolds Cody , Annette Marian Doherty , David Thomas Dudley , Alan Robert Saltiel , Mel Conrad Schroeder , Haile Tecle
IPC分类号： A61K31535
CPC分类号： C07D213/40 , C07C215/68 , C07C229/58 , C07C237/08 , C07C237/16 , C07C237/20 , C07C237/30 , C07C237/32 , C07C237/36 , C07C237/38 , C07C239/22 , C07C243/38 , C07C311/44 , C07C2601/02 , C07C2601/14 , C07D257/04 , C07D257/06 , C07D295/13 , C07D295/155 , C07D295/32 , C07D333/20
摘要： Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, and Z is COOR7, tetrazolyl, CONR6R7, or CH2OR7, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as inflammation, psoriasis and restenosis, as well as stroke, heart failure, and immunodeficiency disorders.
摘要翻译： 式R 1，R 2，R 3，R 4，R 5和R 6的苯基氨基苯甲酸，苯甲酰胺和苄醇衍生物是氢或取代基如烷基，其中R 7是氢或有机基团，Z是COOR 7，四唑基 ，CONR6R7或CH2OR7是MEK的有效抑制剂，因此在治疗癌症和其它增殖性疾病如炎症，牛皮癣和再狭窄以及中风，心力衰竭和免疫缺陷障碍中是有效的。
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