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1. 发明专利

IL235947D0 Solid state isonicotineamide derivatives and pharmaceutical compositions containing them 未知
公开(公告)号：IL235947D0
公开(公告)日：2015-02-01
申请号：IL23594714
申请日：2014-11-27
申请人： MERCK PATENT GMBH , BANKSTON DONALD , BECKER AXEL , SAAL CHRISTOPH , KUEHN CLEMENS , POMA MARCO
IPC分类号： C07D20060101
摘要： The invention relates to solid state forms of N—((S)-2,3-Dihydroxy-propyl)-3-(2-fluoro-4-iodo-phenylamino)-isonicotinamide, processes for their preparation, and medical uses thereof.

2. 发明专利

IL226233D0 Quinazoline carboxamide azetidines, their preparation and pharmaceutical compositions containing them 未知
公开(公告)号：IL226233D0
公开(公告)日：2013-07-31
申请号：IL22623313
申请日：2013-05-08
申请人： ANDREAS GOUTOPOULOS , XIAO YUFANG , HUCK BAYARD R , NEAGU CONSTANTIN , JONES REINALDO , MERCK PATENT GMBH , BANKSTON DONALD
IPC分类号： C07D20060101
摘要： The invention provides novel quinazoline carboxamide azetidine compounds according to Formula (I) and use for the treatment of hyperproliferative diseases, such as cancer.

3. 发明申请

WO2012170976A3 COMPOSITIONS AND METHODS FOR THE PRODUCTION OF PYRIMIDINE AND PYRIDINE COMPOUNDS WITH BTK INHIBITORY ACTIVITY 审中-公开
标题翻译：用BTK抑制活性生产吡嗪和吡啶化合物的组合物和方法
公开(公告)号：WO2012170976A3
公开(公告)日：2013-04-11
申请号：PCT/US2012041803
申请日：2012-06-10
申请人： MERCK PATENT GMBH , HODOUS BRIAN L , LIU-BUJALSKI LESLEY , JONES REINALDO , BANKSTON DONALD , JOHNSON THERESA L , MOCHALKIN IGOR , NGUYEN NGAN , QIU HUI , GOUTOPOULOS ANDREAS , BRUGGER NADIA
发明人： HODOUS BRIAN L , LIU-BUJALSKI LESLEY , JONES REINALDO , BANKSTON DONALD , JOHNSON THERESA L , MOCHALKIN IGOR , NGUYEN NGAN , QIU HUI , GOUTOPOULOS ANDREAS , BRUGGER NADIA
IPC分类号： C07D239/47 , A61K31/4418 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/5377 , A61P35/00 , A61P35/02 , C07D213/68 , C07D213/73 , C07D213/74 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D495/04
CPC分类号： A61K31/69 , A61K31/44 , A61K31/4545 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/55 , C07D213/68 , C07D213/73 , C07D213/74 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D451/02 , C07D471/10 , C07D495/04 , C07F5/022
摘要： The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.
摘要翻译：本发明提供了式（I），式（II），式（III），式（IV）和式（V））的新型嘧啶和吡啶化合物用于治疗过度增殖性疾病的制造和用途，包括但不限于癌症，狼疮，过敏性疾病，干燥病和类风湿性关节炎。在优选的实施方案中，本发明描述不可逆激酶抑制剂，包括但不限于Bruton酪氨酸激酶的抑制剂。

4. 发明申请

WO2012170976A2 COMPOSITIONS AND METHODS FOR THE PRODUCTION OF PYRIMIDINE AND PYRIDINE COMPOUNDS WITH BTK INHIBITORY ACTIVITY 审中-公开
标题翻译：用BTK抑制活性生产吡嗪和吡啶化合物的组合物和方法
公开(公告)号：WO2012170976A2
公开(公告)日：2012-12-13
申请号：PCT/US2012/041803
申请日：2012-06-10
申请人： MERCK PATENT GMBH , HODOUS, Brian L. , LIU-BUJALSKI, Lesley , JONES, Reinaldo , BANKSTON, Donald , JOHNSON, Theresa L. , MOCHALKIN, Igor , NGUYEN, Ngan , QIU, Hui , GOUTOPOULOS, Andreas , BRUGGER, Nadia
发明人： HODOUS, Brian L. , LIU-BUJALSKI, Lesley , JONES, Reinaldo , BANKSTON, Donald , JOHNSON, Theresa L. , MOCHALKIN, Igor , NGUYEN, Ngan , QIU, Hui , GOUTOPOULOS, Andreas , BRUGGER, Nadia
IPC分类号： C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D413/12 , C07D213/68 , C07D213/73 , C07D213/74 , C07D413/14 , C07D495/04 , A61K31/506 , A61K31/513 , A61K31/505 , A61K31/5377 , A61K31/4418 , A61P35/00 , A61P35/02
CPC分类号： A61K31/69 , A61K31/44 , A61K31/4545 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/55 , C07D213/68 , C07D213/73 , C07D213/74 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D451/02 , C07D471/10 , C07D495/04 , C07F5/022
摘要： The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.
摘要翻译：本发明提供了式（I），式（II），式（III），式（IV）和式（V））的新型嘧啶和吡啶化合物用于治疗过度增殖性疾病的制造和用途，包括但不限于癌症，狼疮，过敏性疾病，干燥病和类风湿性关节炎。在优选的实施方案中，本发明描述不可逆激酶抑制剂，包括但不限于Bruton酪氨酸激酶的抑制剂。

5. 发明申请

WO02076976A3 RHO-KINASE INHIBITORS 审中-公开
标题翻译： RHO-激酶抑制剂
公开(公告)号：WO02076976A3
公开(公告)日：2002-12-12
申请号：PCT/US0208659
申请日：2002-03-22
申请人： BAYER AG , NAGARATHNAM DHANAPALAN , ASGARI DAVOUD , SHAO JIANXING , LIU XIAO-GAO , KHIRE UDAY , WANG CHUNGUANG , HART BARRY , BOYER STEPHEN , WEBER OLAF , LYNCH MARK , BANKSTON DONALD
发明人： NAGARATHNAM DHANAPALAN , ASGARI DAVOUD , SHAO JIANXING , LIU XIAO-GAO , KHIRE UDAY , WANG CHUNGUANG , HART BARRY , BOYER STEPHEN , WEBER OLAF , LYNCH MARK , BANKSTON DONALD
IPC分类号： A61K31/517 , A61K31/5377 , A61P1/00 , A61P7/04 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/08 , A61P15/00 , A61P15/10 , A61P19/10 , A61P25/00 , A61P27/06 , A61P35/00 , A61P43/00 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
CPC分类号： C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.
摘要翻译：公开了化合物及其衍生物，它们的合成及其作为Rho激酶抑制剂的用途。本发明的这些化合物可用于抑制肿瘤生长，治疗勃起功能障碍以及治疗Rho激酶（例如冠心病）介导的其它适应症。

6. 发明申请

WO2002076976A2 RHO-KINASE INHIBITORS 审中-公开
标题翻译： RHO-激酶抑制剂
公开(公告)号：WO2002076976A2
公开(公告)日：2002-10-03
申请号：PCT/US2002/008659
申请日：2002-03-22
申请人： BAYER CORPORATION , NAGARATHNAM, Dhanapalan , ASGARI, Davoud , SHAO, Jianxing , LIU, Xiao-Gao , KHIRE, Uday , WANG, Chunguang , HART, Barry , BOYER, Stephen , WEBER, Olaf , LYNCH, Mark , BANKSTON, Donald
发明人： NAGARATHNAM, Dhanapalan , ASGARI, Davoud , SHAO, Jianxing , LIU, Xiao-Gao , KHIRE, Uday , WANG, Chunguang , HART, Barry , BOYER, Stephen , WEBER, Olaf , LYNCH, Mark , BANKSTON, Donald
IPC分类号： C07D403/04
CPC分类号： C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.
摘要翻译：公开了化合物及其衍生物，它们的合成，以及它们作为Rho激酶抑制剂的用途。本发明的这些化合物可用于抑制肿瘤生长，治疗勃起功能障碍和治疗由Rho激酶（例如冠心病）介导的其它适应症。

7. 发明申请

WO1995017408A1 SYNTHESIS OF DIARYL METHANES 审中-公开
标题翻译：二元甲烷的合成
公开(公告)号：WO1995017408A1
公开(公告)日：1995-06-29
申请号：PCT/US1994014327
申请日：1994-12-20
申请人： GLAXO WELLCOME INC. , BANKSTON, Donald, Dillard , FANG, Francis, Gerard , GEES, Thomas , SHARP, Matthew, Jude
发明人： GLAXO WELLCOME INC.
IPC分类号： C07D521/00
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D307/88
摘要： The present invention includes synthetic steps and intermediates involved in the reaction scheme a of converting compounds of formula (II) to the diarylmethanes of formula (I), wherein Y is oxygen or sulfur; A, B, C, D, and E are carbon or 1, 2 or 3 of A, B, C, D, and E are independently nitrogen, and the others are carbon; and wherein R through R are selected independently from the group consisting of: hydrogen, hydroxy, alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl alkyl, alkenyl, hydroxy alkyl, alkoxy alkyl, perhalo-alkyl, amino, nitro, nitrile, halo, oxo, carboxyl, sulfonyl, acyl, formyl, carbamoyl, trifluoromethyl, aminomethyl, azido, amido, hydrazino, aryl, aryloxy, heteroaryl, or aryl or heteroaryl, mono, di, or tri substituted with one or more hydrogen, hydroxy, alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl alkyl, alkenyl, hydroxy alkyl, alkoxy, alkyl, perhaloalkyl, amino, nitro, nitrile, halo, carboxyl, sulfonyl, acyl, formyl, carbamoyl, trifluoromethyl, aminomethyl, azido, amido, hydrazino, aryl, aryloxy, or heteroaryl groups and the pharmaceutically acceptable salts and solvates thereof.
摘要翻译：本发明包括将式（II）化合物转化成式（I）的二芳基甲烷的反应方案a的合成步骤和中间体，其中Y是氧或硫; A，B，C，D和E分别为碳或1,2或3个A，B，C，D和E独立为氮，其余为碳; 其中R 1至R 10独立地选自：氢，羟基，烷基，C 3 -C 8环烷基，C 3 -C 8环烷基烷基，烯基，羟基烷基，烷氧基烷基，全卤代烷基，氨基硝基，腈，卤素，氧代，羧基，磺酰基，酰基，甲酰基，氨基甲酰基，三氟甲基，氨基甲基，叠氮基，酰胺基，肼基，芳基，芳氧基，杂芳基或芳基或杂芳基，单，二或三取代有一个或更多的氢，羟基，烷基，C3-C8环烷基，C3-C8环烷基烷基，烯基，羟基烷基，烷氧基，烷基，全卤代烷基，氨基，硝基，腈，卤素，羧基，磺酰基，酰基，甲酰基，氨基甲酰基，三氟甲基，，叠氮基，酰胺基，肼基，芳基，芳氧基或杂芳基及其药学上可接受的盐和溶剂化物。

8. 发明申请

WO2013040059A1 NOVEL IMIDAZOLE AMINES AS MODULATORS OF KINASE ACTIVITY 审中-公开
标题翻译：新型咪唑胺作为激酶活性的调节剂
公开(公告)号：WO2013040059A1
公开(公告)日：2013-03-21
申请号：PCT/US2012/054900
申请日：2012-09-12
申请人： MERCK PATENT GMBH , LAN, Ruoxi , HUCK, Bayard R. , CHEN, Xiaoling , XIAO, Yufang , DESELM, Lizbeth Celeste , QIU, Hui , NEAGU, Constantin , BANKSTON, Donald , JONES, Christopher Charles Victor
发明人： LAN, Ruoxi , HUCK, Bayard R. , CHEN, Xiaoling , XIAO, Yufang , DESELM, Lizbeth Celeste , QIU, Hui , NEAGU, Constantin , BANKSTON, Donald , JONES, Christopher Charles Victor
IPC分类号： C07D401/14 , A61K31/506
CPC分类号： A61K31/506 , A61K31/4545 , A61K31/5377 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/107
摘要： The invention provides novel imidazole amine compounds according to Formula (I) and Formula (II) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
摘要翻译：本发明提供根据式（I）和式（II）的新型咪唑胺化合物，其用于治疗过度增殖性疾病如癌症的制造和用途。

9. 发明申请

WO2012069146A1 QUINAZOLINE CARBOXAMIDE AZETIDINES 审中-公开
标题翻译：喹唑啉羧酰胺亚胺
公开(公告)号：WO2012069146A1
公开(公告)日：2012-05-31
申请号：PCT/EP2011/005691
申请日：2011-11-11
申请人： MERCK PATENT GMBH , HUCK, Bayard, R. , JONES, Reinaldo , XIAO, Yufang , NEAGU, Constantin , BANKSTON, Donald , GOUTOPOULOS, Andreas
发明人： HUCK, Bayard, R. , JONES, Reinaldo , XIAO, Yufang , NEAGU, Constantin , BANKSTON, Donald , GOUTOPOULOS, Andreas
IPC分类号： C07D403/12
CPC分类号： C07D403/12 , A61K31/517 , A61K45/06
摘要： The invention provides novel quinazoline carboxamide azetidine compounds according to Formula (I) and use for the treatment of hyperproliferative diseases, such as cancer.
摘要翻译：本发明提供了根据式（I）的新型喹唑啉羧酰胺氮杂环丁烷化合物和用于治疗过度增殖性疾病如癌症的用途。

10. 发明申请

WO2004029045A3 PROCESS FOR PREPARING QUINAZOLINE RHO-KINASE INHIBITORS AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备喹唑啉RHO-激酶抑制剂及其中间体的方法
公开(公告)号：WO2004029045A3
公开(公告)日：2004-07-22
申请号：PCT/US0329538
申请日：2003-09-24
申请人： BAYER AG , BANKSTON DONALD , NAGARATHNAM DHANAPHALAN , ASGARI DAVOUD , SHAO JIANXING , LIU XIAO-GAO , KHIRE UDAY , WANG CHUNGUANG , HART BARRY , BOYER STEPHEN , WEBER OLAF , LYNCH MARK
发明人： BANKSTON DONALD , NAGARATHNAM DHANAPHALAN , ASGARI DAVOUD , SHAO JIANXING , LIU XIAO-GAO , KHIRE UDAY , WANG CHUNGUANG , HART BARRY , BOYER STEPHEN , WEBER OLAF , LYNCH MARK
IPC分类号： C07D239/86 , C07D239/91 , C07D239/93 , C07D307/79 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D215/22 , C07D401/04 , C07D401/14 , C07D403/04
CPC分类号： C07D307/79 , C07D239/86 , C07D239/91 , C07D239/93 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14
摘要： The present invention relates to methods of producing quinazoline compounds (I) and derivatives thereof which are useful as Rho-kinase Inhibitors or intermediates thereof (3). Rho-kinase inhibitors are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.
摘要翻译：本发明涉及可用作Rho激酶抑制剂或其中间体的喹唑啉化合物（I）及其衍生物的制备方法（3）。 Rho激酶抑制剂可用于抑制肿瘤生长，治疗勃起功能障碍，以及治疗由Rho激酶（例如冠心病）介导的其它适应症。

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