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1. 发明授权

US07786131B2 Pyrimido[5,4-d]pyrimidines derivatives as irreversible inhibitors of tyrosine kinases 有权
标题翻译：嘧啶并[5,4-d]嘧啶衍生物作为酪氨酸激酶的不可逆抑制剂
公开(公告)号：US07786131B2
公开(公告)日：2010-08-31
申请号：US10441450
申请日：2003-05-20
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： C07D487/04 , A61K31/519 , A61P35/00 , A61P17/06 , C07D413/14 , C07D413/12 , C07D239/94 , C07D491/04
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 relates to pyrimido [5,4-d] pyrimidine compounds of Formula II or a pharmaceutically acceptable salt thereof, wherein Q is and X, E1, E2, E3, R6 and p are as defined herein. The compounds of this invention are irreversible inhibitors of tyrosine kinases and are useful in the treatment of cancer, atherosclerosis, restenosis, endometriosis and psoriasis.
摘要翻译：本发明涉及式II的嘧啶并[5,4-d]嘧啶化合物或其药学上可接受的盐，其中Q是且X，E1，E2，E3，R6和p如本文所定义。本发明的化合物是酪氨酸激酶的不可逆抑制剂，可用于治疗癌症，动脉粥样硬化，再狭窄，子宫内膜异位和银屑病。

2. 发明授权

US06602863B1 Irreversible inhibitors of tyrosine kinases 有权
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.

3. 发明授权

US06498163B1 Pyrido[2,3-D]pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation 失效
标题翻译：吡啶并[2,3-D]嘧啶和4-氨基嘧啶作为细胞增殖抑制剂
公开(公告)号：US06498163B1
公开(公告)日：2002-12-24
申请号：US09355681
申请日：1999-08-02
申请人： Diane Harris Boschelli , Annette Marian Doherty , Ali Fattaey , David William Fry , Susanne Andrea Trumpp-Kallmeyer , Zhipei Wu , Ellen Myra Dobrusin , Mark Robert Barvian
发明人： Diane Harris Boschelli , Annette Marian Doherty , Ali Fattaey , David William Fry , Susanne Andrea Trumpp-Kallmeyer , Zhipei Wu , Ellen Myra Dobrusin , Mark Robert Barvian
IPC分类号： A61K31519
CPC分类号： C07D239/47 , C07D239/48 , C07D471/04
摘要： This invention provides pyridopyrimidines and 4-aminopyrimidines that are useful for treating cell proliferative disorders, such as cancer and restenosis. We have now discovered a group of 7,8-dihydro-2-(amino and thio)pyrido[2,3-d]pyrimidines and 2,4-diaminopyrimidines that are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases. The compounds are readily synthesized and can be administered by a variety of routes, including orally, and have sufficient bioavailability. This invention provides compounds of Formula I: and Formula II: where W is NH, S, SO, or SO2, R1 includes phenyl and substituted phenyl, R2 includes alkyl and cycloalkyl, R3 includes alkyl and hydrogen, R8 and R9 include hydrogen and alkyl, and Z is carboxy. This invention also provides pharmaceutical formulations comprising a compound of Formula I or II together with a pharmaceutically acceptable carrier, diluent, or excipient therefor.
摘要翻译：本发明提供可用于治疗细胞增殖性疾病如癌症和再狭窄的吡啶并嘧啶和4-氨基嘧啶。我们现在已经发现了一组7,8-二氢-2-（氨基和硫代）吡啶并[2,3-d]嘧啶和2,4-二氨基嘧啶，其是细胞周期蛋白依赖性激酶（cdks）和生长因子的有效抑制剂介导的激酶。这些化合物很容易合成，并且可以通过多种途径施用，包括口服，并具有足够的生物利用度。本发明提供式I化合物和式II化合物：其中W是NH，S，SO或SO 2，R 1包括苯基和取代的苯基，R 2包括烷基和环烷基，R 3包括烷基和氢，R 8和R 9包括氢和烷基，并且Z是羧基。本发明还提供了包含式I或II化合物及其药学上可接受的载体，稀释剂或赋形剂的药物制剂。

4. 发明授权

US06344459B1 Irreversible inhibitors of tyrosine kinases 有权
标题翻译：不可逆的酪氨酸激酶抑制剂
公开(公告)号：US06344459B1
公开(公告)日：2002-02-05
申请号：US09155501
申请日：1999-06-08
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： A61K31517
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.
摘要翻译：本发明提供了酪氨酸激酶不可逆抑制剂的化合物。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。

5. 发明授权

US5721266A Substituted imidazolinyl-imidazolines as antagonists of SH-2 binding and therapeutic uses thereof 失效
标题翻译：取代的咪唑啉基 - 咪唑啉作为SH-2结合的拮抗剂及其治疗用途
公开(公告)号：US5721266A
公开(公告)日：1998-02-24
申请号：US312253
申请日：1994-09-26
申请人： Stuart James Decker , David William Fry , James Marino Hamby , Alan Robert Saltiel
发明人： Stuart James Decker , David William Fry , James Marino Hamby , Alan Robert Saltiel
IPC分类号： A61K31/4178 , A01N43/50
CPC分类号： A61K31/4178
摘要： Methods of treating proliferative diseases or viral, inflammatory, allergic and cardiovascular diseases, and restenosis are disclosed. The present invention demonstrates the use of N,N'-piperazinylbis-�2-amino-1-imidazolin-2-yl)-2-imidazolines!, 2-amino-1-(2-imidazolin-2-yl)-2-imidazolines, and N,N'-alkylene-bis�2-amino-1-(2-imidazolin-2-yl)-2-imidazolines!, their derivatives, and salts thereof, to antagonize the association of a protein tyrosine kinase with a substrate regulatory protein. The present invention also demonstrates the use of pharmaceutical compositions employing N,N'-piperazinylbis�2-amino-1-imidazolin-2-yl)-2-imidazolines!, 2-amino-1-(2-imidazolin-2-yl)-2-imidazolines, and N,N'-alkylenebis-�2-amino-1-(2-imidazolin-2-yl)-2-imidazolines!, their derivatives, and salts thereof, to antagonize the association of a protein tyrosine kinase with substrate regulatory protein. The present invention also relates to novel N,N'-piperazinylbis�2-amino-1-imidazolin-2-yl)-2-imidazolines!.
摘要翻译：公开了治疗增殖性疾病或病毒，炎性，过敏性和心血管疾病以及再狭窄的方法。本发明证明了使用N，N'-哌嗪基双[2-氨基-1-咪唑啉-2-基] -2-咪唑啉]，2-氨基-1-（2-咪唑啉-2-基）-2 - 咪唑啉和N，N'-亚烷基 - 双[2-氨基-1-（2-咪唑啉-2-基）-2-咪唑啉]及其衍生物及其盐，以拮抗蛋白酪氨酸激酶与底物调节蛋白。本发明还说明了使用N，N'-哌嗪基双[2-氨基-1-咪唑啉-2-基] -2-咪唑啉]，2-氨基-1-（2-咪唑啉-2-基））-2-咪唑啉和N，N'-亚烷基双 - [2-氨基-1-（2-咪唑啉-2-基）-2-咪唑啉]及其衍生物及其盐，以拮抗蛋白质酪氨酸激酶与底物调节蛋白。本发明还涉及新的N，N'-哌嗪基双[2-氨基-1-咪唑啉-2-基] -2-咪唑啉]。

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