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公开(公告)号:US07674907B2
公开(公告)日:2010-03-09
申请号:US11184237
申请日:2005-07-18
申请人: Joseph J. Nunes , Matthew W. Martin , Ryan White , David McGowan , Jean E. Bemis , Frank Kayser , Jiasheng Fu , Jinqian Liu , XianYun Jiao
发明人: Joseph J. Nunes , Matthew W. Martin , Ryan White , David McGowan , Jean E. Bemis , Frank Kayser , Jiasheng Fu , Jinqian Liu , XianYun Jiao
IPC分类号: C07D491/048 , A61K31/4355
CPC分类号: C07D491/04 , C07D491/14
摘要: The present invention relates to furanopyridine compounds having the general Formula I: and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula I, methods of modulating Lck and ACK-1 enzymes and of treating various related diseases and conditions, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma, thymoma, just to name a few, in a mammal, comprising administering to the mammal a therapeutically effective amount a compound of Formula I, as described above, and methods of manufacturing medicaments comprising the compound of Formula I.
摘要翻译: 本发明涉及具有通式I的呋喃并吡啶化合物及其立体异构体,互变异构体,溶剂合物,药用盐和衍生物及其前药。 本发明还包括药物组合物,其包含式I化合物,调节Lck和ACK-1酶的方法以及治疗各种相关疾病和病症,包括炎症,T细胞活化抑制,增殖,关节炎,器官移植,缺血或再灌注 损伤,心肌梗塞,中风,多发性硬化,炎性肠病,克罗恩病,狼疮,超敏反应,1型糖尿病,牛皮癣,皮炎,桥本氏甲状腺炎,干燥综合征,自身免疫性甲状腺功能亢进,艾迪生病,自身免疫性疾病,肾小球肾炎,过敏性疾病,哮喘 ,干草组织,湿疹,癌症,结肠癌,胸腺瘤,仅举几个例子,在哺乳动物中,包括向哺乳动物施用治疗有效量的如上所述的式I化合物和制备包含以下化合物的药物的方法: 一级方程式
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公开(公告)号:US20100234373A1
公开(公告)日:2010-09-16
申请号:US12788201
申请日:2010-05-26
申请人: Erin F. Dimauro , Jean E. Bemis , Stuart C. Chaffee , Ning Chen , Essa Hu , Roxanne Kunz , Matthew W. Martin , David C. McGowan , Shannon Rumfelt
发明人: Erin F. Dimauro , Jean E. Bemis , Stuart C. Chaffee , Ning Chen , Essa Hu , Roxanne Kunz , Matthew W. Martin , David C. McGowan , Shannon Rumfelt
IPC分类号: A61K31/5377 , A61K31/506 , A61K31/505 , A61K31/4709 , A61K31/44 , C07D413/12 , C07D413/14 , C07D417/14 , C07D239/48 , C07D215/38 , C07D213/74 , A61P19/02 , A61P29/00 , A61P17/06 , A61P1/04 , A61P3/10 , A61P37/06
CPC分类号: C07D213/75 , C07D215/38 , C07D239/42 , C07D239/48 , C07D239/50 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04
摘要: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including autoimmune disease and inflammation. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, L, R1, R2 and R3 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of the present invention, methods of use such as treatment of Lck and/or c-Kit kinase mediated diseases by administering the compounds of the invention, or compositions including one or more compounds of the invention, and intermediates and processes useful for the preparation of compounds of the present invention.
摘要翻译: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病,包括自身免疫疾病和炎症的化合物。 在一个实施方案中,化合物具有通式I,其中A1,A2,A3,A4,L,R1,R2和R3如本文所定义。 本发明还包括药物组合物,其包含一种或多种本发明化合物,通过施用本发明化合物来治疗Lck和/或c-Kit激酶介导的疾病的使用方法,或包含一种或多种本发明化合物的组合物 发明,以及可用于制备本发明化合物的中间体和方法。
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公开(公告)号:US07754717B2
公开(公告)日:2010-07-13
申请号:US11503551
申请日:2006-08-11
申请人: Erin F. Dimauro , Jean E. Bemis , Stuart C. Chaffee , Ning Chen , Essa Hu , Roxanne Kunz , Matthew W. Martin , David C. McGowan , Shannon Rumfelt
发明人: Erin F. Dimauro , Jean E. Bemis , Stuart C. Chaffee , Ning Chen , Essa Hu , Roxanne Kunz , Matthew W. Martin , David C. McGowan , Shannon Rumfelt
IPC分类号: A01N43/60 , A01N43/54 , A01N43/42 , A61K31/495 , A61K31/50 , A61K31/501 , A61K31/4965 , A61K31/51 , A61K31/47 , C07D239/42 , C07D401/04 , C07D237/30 , C07D401/00
CPC分类号: C07D213/75 , C07D215/38 , C07D239/42 , C07D239/48 , C07D239/50 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04
摘要: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including autoimmune disease and inflammation. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, L, R1, R2 and R3 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of the present invention, methods of use such as treatment of Lck and/or c-Kit kinase mediated diseases by administering the compounds of the invention, or compositions including one or more compounds of the invention, and intermediates and processes useful for the preparation of compounds of the present invention.
摘要翻译: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病,包括自身免疫疾病和炎症的化合物。 在一个实施方案中,化合物具有通式I,其中A1,A2,A3,A4,L,R1,R2和R3如本文所定义。 本发明还包括药物组合物,其包含一种或多种本发明化合物,通过施用本发明化合物来治疗Lck和/或c-Kit激酶介导的疾病的使用方法,或包含一种或多种本发明化合物的组合物 发明,以及可用于制备本发明化合物的中间体和方法。
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公开(公告)号:US07442698B2
公开(公告)日:2008-10-28
申请号:US10891636
申请日:2004-07-13
申请人: John L. Buchanan , Daniel Elbaum , Matthew W. Martin , David C. McGowan , Perry M. Novak , Joseph J. Nunes
发明人: John L. Buchanan , Daniel Elbaum , Matthew W. Martin , David C. McGowan , Perry M. Novak , Joseph J. Nunes
IPC分类号: C07D239/48 , C07D403/12 , A61K31/505
CPC分类号: C04B35/632 , C07D213/75 , C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要: The present invention relates to pyrimidine or pyridine carbamate compounds having the general Formula I: and pharmaceutically acceptable salts or derivatives thereof. Also included are methods of treatment of various diseases and conditions, including inflammation, inhibition of T cell activation and proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma, thymoma, just to name a few, in a mammal, the methods comprising administering a therapeutically-effective amount a compound of Formula I, or a salt or derivative form thereof, as described above.
摘要翻译: 本发明涉及具有通式I的嘧啶或吡啶氨基甲酸酯化合物及其药学上可接受的盐或衍生物。 还包括治疗各种疾病和病症的方法,包括炎症,T细胞活化和增殖的抑制,关节炎,器官移植,缺血或再灌注损伤,心肌梗塞,中风,多发性硬化,炎性肠病,克罗恩病,狼疮, 超敏反应,1型糖尿病,牛皮癣,皮炎,桥本甲状腺炎,干燥综合征,自身免疫性甲状腺功能亢进,艾迪生病,自身免疫性疾病,肾小球性肾炎,过敏性疾病,哮喘,干草病,湿疹,癌症,结肠癌,胸腺瘤,仅举几例 哺乳动物,所述方法包括给予治疗有效量的如上所述的式I化合物或其盐或衍生物形式。
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公开(公告)号:US20090176774A1
公开(公告)日:2009-07-09
申请号:US12157303
申请日:2008-06-09
申请人: Michele Potashman , Tae-Seong Kim , Steven Bellon , Shon Booker , Yuan Cheng , Joseph L. Kim , Andrew Tasker , Ning Xi , Shimin Xu , Jean-Christophe Harmange , George Borg , Matthew Weiss , Brian L. Hodous , Russell Graceffa , William H. Buckner , Craig E. Masse , Deborah Choquette , Matthew W. Martin , Julie Germain , Lucian V. DiPietro , Stuart C. Chaffee , Joseph J. Nunes , John L. Buchanan , David C. McGowan , Douglas A. Whittington , Gregory J. Habgood , Vinod F. Patel , Daniel La
发明人: Michele Potashman , Tae-Seong Kim , Steven Bellon , Shon Booker , Yuan Cheng , Joseph L. Kim , Andrew Tasker , Ning Xi , Shimin Xu , Jean-Christophe Harmange , George Borg , Matthew Weiss , Brian L. Hodous , Russell Graceffa , William H. Buckner , Craig E. Masse , Deborah Choquette , Matthew W. Martin , Julie Germain , Lucian V. DiPietro , Stuart C. Chaffee , Joseph J. Nunes , John L. Buchanan , David C. McGowan , Douglas A. Whittington , Gregory J. Habgood , Vinod F. Patel , Daniel La
IPC分类号: A61K31/536 , A61K31/517 , A61K31/502 , A61K31/498 , A61K31/4709
CPC分类号: C07D213/64 , C07D213/81 , C07D215/233 , C07D215/38 , C07D215/48 , C07D215/54 , C07D237/34 , C07D239/34 , C07D239/47 , C07D239/84 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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公开(公告)号:US08178557B2
公开(公告)日:2012-05-15
申请号:US12157303
申请日:2008-06-09
申请人: Michele Potashman , Tae-Seong Kim , Steven Bellon , Shon Booker , Yuan Cheng , Joseph L. Kim , Andrew Tasker , Ning Xi , Shimin Xu , Jean-Christophe Harmange , George Borg , Matthew Weiss , Brian L. Hodous , Russell Graceffa , William H. Buckner , Craig E. Masse , Deborah Choquette , Matthew W. Martin , Julie Germain , Lucian V. DiPietro , Stuart C. Chaffee , Joseph J. Nunes , John L. Buchanan , David C. McGowan , Douglas A. Whittington , Gregory J. Habgood , Vinod F. Patel , Daniel La
发明人: Michele Potashman , Tae-Seong Kim , Steven Bellon , Shon Booker , Yuan Cheng , Joseph L. Kim , Andrew Tasker , Ning Xi , Shimin Xu , Jean-Christophe Harmange , George Borg , Matthew Weiss , Brian L. Hodous , Russell Graceffa , William H. Buckner , Craig E. Masse , Deborah Choquette , Matthew W. Martin , Julie Germain , Lucian V. DiPietro , Stuart C. Chaffee , Joseph J. Nunes , John L. Buchanan , David C. McGowan , Douglas A. Whittington , Gregory J. Habgood , Vinod F. Patel , Daniel La
IPC分类号: A61K31/04
CPC分类号: C07D213/64 , C07D213/81 , C07D215/233 , C07D215/38 , C07D215/48 , C07D215/54 , C07D237/34 , C07D239/34 , C07D239/47 , C07D239/84 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译: 所选化合物对于预防和治疗诸如HGF介导的疾病等疾病是有效的。 本发明包括新颖的化合物,类似物,前药和药学上可接受的盐,用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。
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公开(公告)号:US07435823B2
公开(公告)日:2008-10-14
申请号:US11042634
申请日:2005-01-24
申请人: Michele Potashman , Tae-Seong Kim , Steven Bellon , Shon Booker , Yuan Cheng , Joseph L. Kim , Andrew Tasker , Ning Xi , Shimin Xu , Jean-Christophe Harmange , George Borg , Matthew Weiss , Brian L. Hodous , Russell Graceffa , William H. Buckner , Craig E. Masse , Deborah Choquette , Matthew W. Martin , Julie Germain , Lucian V. DiPietro , Stuart C. Chaffee , Joseph J. Nunes , John L. Buchanan , Gregory J. Habgood , David C. McGowan , Douglas A. Whittington , Daniel La , Vinod F. Patel
发明人: Michele Potashman , Tae-Seong Kim , Steven Bellon , Shon Booker , Yuan Cheng , Joseph L. Kim , Andrew Tasker , Ning Xi , Shimin Xu , Jean-Christophe Harmange , George Borg , Matthew Weiss , Brian L. Hodous , Russell Graceffa , William H. Buckner , Craig E. Masse , Deborah Choquette , Matthew W. Martin , Julie Germain , Lucian V. DiPietro , Stuart C. Chaffee , Joseph J. Nunes , John L. Buchanan , Gregory J. Habgood , David C. McGowan , Douglas A. Whittington , Daniel La , Vinod F. Patel
IPC分类号: C07D215/38 , C07D265/34
CPC分类号: C07D213/64 , C07D213/81 , C07D215/233 , C07D215/38 , C07D215/48 , C07D215/54 , C07D237/34 , C07D239/34 , C07D239/47 , C07D239/84 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译: 所选化合物对于预防和治疗诸如HGF介导的疾病等疾病是有效的。 本发明包括新颖的化合物,类似物,前药和药学上可接受的盐,用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。
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公开(公告)号:US07795254B2
公开(公告)日:2010-09-14
申请号:US12290223
申请日:2008-10-28
申请人: Jean-Christophe Harmange , Matthew W. Martin , Yohannes Teffera , Raju Subramanian , Ryan White , Roger Zanon , Jay Larrow , Joseph F. Payack , Mina Dilmeghani Seran
发明人: Jean-Christophe Harmange , Matthew W. Martin , Yohannes Teffera , Raju Subramanian , Ryan White , Roger Zanon , Jay Larrow , Joseph F. Payack , Mina Dilmeghani Seran
IPC分类号: C07D413/12 , A61K31/538
CPC分类号: C07D413/14
摘要: Selected benzomorpholine compounds, including 7-((6,7-bis(methyloxy)-4-quinolinyl)oxy)-N-(5 -methyl-3-isoxazolyl)-2,3-dihydro-4H-1,4-benzoxazine-4-carboxamide, are effective for prophylaxis and treatment of diseases, such as VEGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译: 选择的苯并吗啉化合物,包括7 - ((6,7-双(甲氧基)-4-喹啉基)氧)-N-(5-甲基-3-异恶唑基)-2,3-二氢-4H-1,4-苯并恶嗪 -4-甲酰胺对于预防和治疗诸如VEGF介导的疾病的疾病是有效的。 本发明包括新颖的化合物,类似物,前药和药学上可接受的盐,用于预防和治疗涉及癌症等的疾病和其它疾病或病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。
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公开(公告)号:US20090149454A1
公开(公告)日:2009-06-11
申请号:US12290223
申请日:2008-10-28
申请人: Jean-Christophe Harmange , Matthew W. Martin , Yohannes Teffera , Raju Subramanian , Ryan White , Roger Zanon , Jay Larrow , Joseph F. Payack , Mina Dilmeghani Seran
发明人: Jean-Christophe Harmange , Matthew W. Martin , Yohannes Teffera , Raju Subramanian , Ryan White , Roger Zanon , Jay Larrow , Joseph F. Payack , Mina Dilmeghani Seran
IPC分类号: A61K31/538 , C07D413/14 , A61P35/00
CPC分类号: C07D413/14
摘要: Selected benzomorpholine compounds are effective for prophylaxis and treatment of diseases, such as VEGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译: 选择的苯并吗啉化合物对于预防和治疗诸如VEGF介导的疾病的疾病是有效的。 本发明包括新颖的化合物,类似物,前药和药学上可接受的盐,用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。
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公开(公告)号:US08492404B2
公开(公告)日:2013-07-23
申请号:US12788201
申请日:2010-05-26
IPC分类号: A01N43/42 , A61K31/47 , C07D215/46
CPC分类号: C07D213/75 , C07D215/38 , C07D239/42 , C07D239/48 , C07D239/50 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04
摘要: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including autoimmune disease and inflammation. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, L, R1, R2 and R3 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of the present invention, methods of use such as treatment of Lck and/or c-Kit kinase mediated diseases by administering the compounds of the invention, or compositions including one or more compounds of the invention, and intermediates and processes useful for the preparation of compounds of the present invention.
摘要翻译: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病,包括自身免疫疾病和炎症的化合物。 在一个实施方案中,化合物具有通式I,其中A1,A2,A3,A4,L,R1,R2和R3如本文所定义。 本发明还包括药物组合物,其包含一种或多种本发明化合物,通过施用本发明化合物来治疗Lck和/或c-Kit激酶介导的疾病的使用方法,或包含一种或多种本发明化合物的组合物 发明,以及可用于制备本发明化合物的中间体和方法。
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