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1. 发明申请

US20070054916A1 Aryl nitrogen-containing bicyclic compounds and methods of use 审中-公开
标题翻译：芳基含氮双环化合物及其使用方法
公开(公告)号：US20070054916A1
公开(公告)日：2007-03-08
申请号：US11240590
申请日：2005-09-30
申请人： Vinod Patel , Joseph Kim , Stephanie Geuns-Meyer , Stuart Chaffee , Victor Cee , Brian Hodous , Steven Bellon , Jean-Christophe Harmange , Philip Olivieri , Maya Thaman , Erin DiMauro , John Buchanan , David McGowan , Brian Albrecht , Holly Deak , Jean Bemis , Ryan White , Matthew Martin , Gregory Habgood , Paul Tempest , Craig Masse , William Buckner , Bradley Herberich , Russell Graceffa , Dawei Zhang , Shimin Xu , Kelvin Sham , Robert Rzasa , James Falsey , Partha Chakrabarti , Guo-Qiang Cao , Susan Tomlinson , Liping Pettus , Adrian Smith , Nick Paras , Gang Liu , Frenel DeMorin , Andrew Tasker , Anthony Reed
发明人： Vinod Patel , Joseph Kim , Stephanie Geuns-Meyer , Stuart Chaffee , Victor Cee , Brian Hodous , Steven Bellon , Jean-Christophe Harmange , Philip Olivieri , Maya Thaman , Erin DiMauro , John Buchanan , David McGowan , Brian Albrecht , Holly Deak , Jean Bemis , Ryan White , Matthew Martin , Gregory Habgood , Paul Tempest , Craig Masse , William Buckner , Bradley Herberich , Russell Graceffa , Dawei Zhang , Shimin Xu , Kelvin Sham , Robert Rzasa , James Falsey , Partha Chakrabarti , Guo-Qiang Cao , Susan Tomlinson , Liping Pettus , Adrian Smith , Nick Paras , Gang Liu , Frenel DeMorin , Andrew Tasker , Anthony Reed
IPC分类号： A61K31/525 , A61K31/519 , A61K31/517
CPC分类号： C07D215/38 , C07C205/37 , C07D215/12 , C07D217/12 , C07D217/22 , C07D217/26 , C07D239/26 , C07D239/84 , C07D239/94 , C07D239/95 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , 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 inflammation, cancer and related conditions. The compounds have a general Formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the 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，包括炎症，癌症和相关病症的化合物。化合物具有通式I，其中A 1，A 2，A 3，B，R 1， R 2，R 3和R 4在本文中定义。因此，本发明还包括含有本发明化合物的药物组合物，使用本发明化合物和组合物预防和治疗激酶介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。

2. 发明申请

US20060241115A1 Compounds and methods of use 有权
公开(公告)号：US20060241115A1
公开(公告)日：2006-10-26
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 Kim , Andrew Tasker , Ning Xi , Shimin Xu , Jean-Christophe Harmange , George Borg , Matthew Weiss , Brian Hodous , Russell Graceffa , William Buckner , Craig Masse , Deborah Choquette , Matthew Martin , Julie Germain , Lucian DiPietro , Stuart Chaffee , Joseph Nunes , John Buchanan , Gregory Habgood , David McGowan , Douglas Whittington
发明人： Michele Potashman , Tae-Seong Kim , Steven Bellon , Shon Booker , Yuan Cheng , Joseph Kim , Andrew Tasker , Ning Xi , Shimin Xu , Jean-Christophe Harmange , George Borg , Matthew Weiss , Brian Hodous , Russell Graceffa , William Buckner , Craig Masse , Deborah Choquette , Matthew Martin , Julie Germain , Lucian DiPietro , Stuart Chaffee , Joseph Nunes , John Buchanan , Gregory Habgood , David McGowan , Douglas Whittington
IPC分类号： A61K31/517 , A61K31/502 , A61K31/498 , A61K31/4709 , C07D43/02
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.

3. 发明申请

US20060217380A1 Heteroaryl-substituted alkyne compounds and method of use 有权
标题翻译：杂芳基取代的炔化合物及其使用方法
公开(公告)号：US20060217380A1
公开(公告)日：2006-09-28
申请号：US11251490
申请日：2005-10-14
申请人： Stuart Chaffee , Brian Albrecht , Brian Hodous , Matthew Martin , David McGowan , Erin DiMauro , Gade Reddy , Victor Cee , Philip Olivieri , Anthony Reed , Karina Romero
发明人： Stuart Chaffee , Brian Albrecht , Brian Hodous , Matthew Martin , David McGowan , Erin DiMauro , Gade Reddy , Victor Cee , Philip Olivieri , Anthony Reed , Karina Romero
IPC分类号： A61K31/517 , A61K31/5377 , A61K31/503
CPC分类号： C07D213/74 , C07D213/81 , C07D215/14 , C07D239/42 , C07D241/42 , C07D401/06 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/06 , C07D409/06 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, R1 and R2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the 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，包括炎症，癌症和相关病症的化合物。化合物具有通式I，其中A 1，A 2，A 3，A 4，R 4，本文定义了SUP> 1和R 2。因此，本发明还包括含有本发明化合物的药物组合物，使用本发明化合物和组合物预防和治疗激酶介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。

4. 发明申请

US20070072862A1 Bis-aryl amide compounds and methods of use 失效
标题翻译：双芳基酰胺化合物及其使用方法
公开(公告)号：US20070072862A1
公开(公告)日：2007-03-29
申请号：US11503551
申请日：2006-08-11
申请人： Erin Dimauro , Jean Bemis , Stuart Chaffee , Ning Chen , Essu Hu , Roxanne Kunz , Matthew Martin , David McGowan , Shannon Rumfelt
发明人： Erin Dimauro , Jean Bemis , Stuart Chaffee , Ning Chen , Essu Hu , Roxanne Kunz , Matthew Martin , David McGowan , Shannon Rumfelt
IPC分类号： A61K31/506 , A61K31/502 , A61K31/501 , A61K31/497 , A61K31/498 , A61K31/4745 , A61K31/4709
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A 1，A 2，A 3，A 4， >，L，R 1，R 2和R 3在本文中定义。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。

5. 发明申请

US20060040961A1 Furanopyrimidines 有权
标题翻译：呋喃并嘧啶
公开(公告)号：US20060040961A1
公开(公告)日：2006-02-23
申请号：US11169312
申请日：2005-06-29
申请人： John Buchanan , William Buckner , Simon Burkitt , Erin DiMauro , Christopher Farthing , Alexander Frenkel , Martin Harrison , Frank Kayser , Jinqian Liu , Sarah Lively , Teresa Marshall , David McGowan , Rajiv Sharma , Stephen Shuttleworth , Xiaotian Zhu
发明人： John Buchanan , William Buckner , Simon Burkitt , Erin DiMauro , Christopher Farthing , Alexander Frenkel , Martin Harrison , Frank Kayser , Jinqian Liu , Sarah Lively , Teresa Marshall , David McGowan , Rajiv Sharma , Stephen Shuttleworth , Xiaotian Zhu
IPC分类号： A61K31/519 , C07D491/02
CPC分类号： C07D491/04 , C07D495/04
摘要： The present invention relates to furanopyrimidine 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 treating various diseases and conditions in a mammal, 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 and thymoma, comprising administering to the mammal a therapeutically effective amount of a compound of Formula I. The invention also relates to methods of manufacturing medicaments, which comprise one or more compounds of Formula I.
摘要翻译：本发明涉及具有通式I的呋喃并嘧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，治疗哺乳动物各种疾病和病症的方法，包括炎症，抑制T细胞活化，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，肾小球性肾炎，过敏性疾病，哮喘，干草病，湿疹，结肠癌和胸腺瘤，包括向哺乳动物施用治疗有效量的式I化合物。本发明还涉及制备药物的方法，其包含一种或多种式I化合物。

6. 发明申请

US20060046977A1 Furanopyridine derivatives and methods of use 有权
标题翻译：呋喃并吡啶衍生物和使用方法
公开(公告)号：US20060046977A1
公开(公告)日：2006-03-02
申请号：US11184237
申请日：2005-07-18
申请人： Joseph Nunes , Matthew Martin , Ryan White , David McGowan , Jean Bemis , Frank Kayser , Jiasheng Fu , Jinqian Liu , Xian Jiao
发明人： Joseph Nunes , Matthew Martin , Ryan White , David McGowan , Jean Bemis , Frank Kayser , Jiasheng Fu , Jinqian Liu , Xian Jiao
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/4741 , C07F7/02 , C07D491/02 , A61K31/695
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

7. 发明申请

US20050026914A1 Substituted heterocyclic compounds and methods of use 失效
标题翻译：取代的杂环化合物及其使用方法
公开(公告)号：US20050026914A1
公开(公告)日：2005-02-03
申请号：US10891636
申请日：2004-07-13
申请人： John Buchanan , Daniel Elbaum , Matthew Martin , David McGowan , Perry Novak , Joseph Nunes
发明人： John Buchanan , Daniel Elbaum , Matthew Martin , David McGowan , Perry Novak , Joseph Nunes
IPC分类号： A61P37/00 , C07D213/75 , C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , A61K31/541 , A61K31/506 , A61K31/5377 , C07D413/02 , C07D417/02 , C07
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。

8. 发明授权

US07674907B2 Furanopyridine derivatives and methods of use 有权
标题翻译：呋喃并吡啶衍生物和使用方法
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

9. 发明申请

US20140073642A1 QUINAZOLINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS AND FURTHER DISEASES 有权
标题翻译：用于治疗病毒感染和进一步疾病的喹唑啉衍生物
公开(公告)号：US20140073642A1
公开(公告)日：2014-03-13
申请号：US14118527
申请日：2012-05-18
申请人： David McGowan , Pierre Jean-Marie Bernard Raboisson , Tim Hugo Maria Jonckers , Stefaan Julien Last , Werner Embrechts , Serge Maria Aloysius Pieters
发明人： David McGowan , Pierre Jean-Marie Bernard Raboisson , Tim Hugo Maria Jonckers , Stefaan Julien Last , Werner Embrechts , Serge Maria Aloysius Pieters
IPC分类号： C07D491/056 , C07D295/192 , C07D403/04 , C07D239/95 , C07D401/06
CPC分类号： C07D491/056 , C07D239/95 , C07D295/192 , C07D401/06 , C07D403/04
摘要： This invention relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy of disorders in which the modulation of toll-like-receptors is involved.
摘要翻译：本发明涉及喹唑啉衍生物，其制备方法，药物组合物及其在治疗涉及toll样受体调节的病症中的用途。

10. 发明授权

US08623899B2 Bis-benzimidazole derivatives as hepatitis C virus inhibitors 有权
标题翻译：双苯并咪唑衍生物作为丙型肝炎病毒抑制剂
公开(公告)号：US08623899B2
公开(公告)日：2014-01-07
申请号：US13389277
申请日：2010-08-06
申请人： David McGowan , Samuel Dominique Demin , Stefaan Julien Last , Koen Vandyck , Pierre Jean-Marie Bernard Raboisson
发明人： David McGowan , Samuel Dominique Demin , Stefaan Julien Last , Koen Vandyck , Pierre Jean-Marie Bernard Raboisson
IPC分类号： A61K31/4184 , C07D403/10
CPC分类号： C07D403/04 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/14
摘要： Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R′ have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
摘要翻译：式I的HCV复制抑制剂包括立体化学异构形式，以及其盐，水合物，溶剂化物，其中R和R'具有如本文所定义的含义。本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在HCV治疗中单独或与其它HCV抑制剂组合的用途。

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