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公开(公告)号：WO2016057500A1
公开(公告)日：2016-04-14
申请号：PCT/US2015/054221
申请日：2015-10-06
Applicant: MERCK PATENT GMBH , GAILLARD, Pascale , SEENISAMY, Jeyaprakashnarayanan , LIU-BUJALSKI, Lesley , POTNICK, Justin , CALDWELL, Richard D. , QIU, Hui , NEAGU, Constantin , JONES, Reinaldo , WON, Annie Cho , GOUTOPOULOS, Andreas , SHERER, Brian A. , JOHNSON, Theresa L. , GARDBERG, Anna
Inventor： GAILLARD, Pascale , SEENISAMY, Jeyaprakashnarayanan , LIU-BUJALSKI, Lesley , POTNICK, Justin , CALDWELL, Richard D. , QIU, Hui , NEAGU, Constantin , JONES, Reinaldo , WON, Annie Cho , GOUTOPOULOS, Andreas , SHERER, Brian A. , JOHNSON, Theresa L. , GARDBERG, Anna
IPC: C07D471/04 , C07D519/00 , A61K31/437 , A61K31/553 , A61P29/00 , A61P37/00
CPC classification number: C07D471/04 , C07D519/00
Abstract: The present invention relates to imidazopyridine compounds of formula I, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
Abstract translation: 本发明涉及式I的咪唑并吡啶化合物及其药学上可接受的组合物，其可用作BTK抑制剂。
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公开(公告)号：WO2015061247A2
公开(公告)日：2015-04-30
申请号：PCT/US2014061455
申请日：2014-10-21
Applicant: MERCK PATENT GMBH , QIU HUI , CALDWELL RICHARD D , NEAGU CONSTANTIN , MOCHALKIN IGOR , LIU-BUJALSKI LESLEY , JONES REINALDO , TATE DEVON , JOHNSON THERESA L , GARDBERG ANNA
Inventor： QIU HUI , CALDWELL RICHARD D , NEAGU CONSTANTIN , MOCHALKIN IGOR , LIU-BUJALSKI LESLEY , JONES REINALDO , TATE DEVON , JOHNSON THERESA L , GARDBERG ANNA
IPC: C07D213/81
CPC classification number: C07D401/04 , A61K9/0019 , A61K9/0043 , A61K9/0048 , A61K9/0078 , A61K9/02 , A61K9/06 , A61K9/08 , A61K9/1688 , A61K9/19 , A61K9/2018 , A61K9/2059 , A61K9/2826 , A61K9/286 , A61K47/06 , A61K47/186 , C07D213/81 , C07D213/82 , C07D239/47 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/14 , C07D407/04 , C07D409/04 , C07D413/04 , C07D413/06 , C07D413/14 , C07D451/02 , C07D471/08 , C07D487/04 , C07D487/08 , C07D487/10 , C07D495/04 , C07F5/022
Abstract: The present invention relates to pyridine, pyrimidine, pyrazine, and pyridazine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
Abstract translation: 本发明涉及用作BTK抑制剂的吡啶，嘧啶，吡嗪和哒嗪化合物及其药学上可接受的组合物。
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3.发明申请COMPOSITIONS AND METHODS FOR THE PRODUCTION OF PYRIMIDINE AND PYRIDINE COMPOUNDS WITH BTK INHIBITORY ACTIVITY 审中-公开用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
Applicant: 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
Inventor： HODOUS BRIAN L , LIU-BUJALSKI LESLEY , JONES REINALDO , BANKSTON DONALD , JOHNSON THERESA L , MOCHALKIN IGOR , NGUYEN NGAN , QIU HUI , GOUTOPOULOS ANDREAS , BRUGGER NADIA
IPC: 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 classification number: 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
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：WO2015061247A3
公开(公告)日：2015-04-30
申请号：PCT/US2014/061455
申请日：2014-10-21
Applicant: MERCK PATENT GMBH , QIU, Hui , CALDWELL, Richard D. , NEAGU, Constantin , MOCHALKIN, Igor , LIU-BUJALSKI, Lesley , JONES, Reinaldo , TATE, Devon , JOHNSON, Theresa L. , GARDBERG, Anna
Inventor： QIU, Hui , CALDWELL, Richard D. , NEAGU, Constantin , MOCHALKIN, Igor , LIU-BUJALSKI, Lesley , JONES, Reinaldo , TATE, Devon , JOHNSON, Theresa L. , GARDBERG, Anna
IPC: C07D403/12 , A61K31/4439 , A61K31/506 , C07D213/81 , C07D401/04 , C07D403/04 , C07D407/04 , C07D239/48 , C07D409/04 , C07D413/04 , C07D413/06 , C07D487/04 , C07D401/12
Abstract: The present invention relates to pyridine, pyrimidine, pyrazine, and pyridazine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
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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
Applicant: MERCK PATENT GMBH , HUCK, Bayard, R. , JONES, Reinaldo , XIAO, Yufang , NEAGU, Constantin , BANKSTON, Donald , GOUTOPOULOS, Andreas
Inventor： HUCK, Bayard, R. , JONES, Reinaldo , XIAO, Yufang , NEAGU, Constantin , BANKSTON, Donald , GOUTOPOULOS, Andreas
IPC: C07D403/12
CPC classification number: C07D403/12 , A61K31/517 , A61K45/06
Abstract: The invention provides novel quinazoline carboxamide azetidine compounds according to Formula (I) and use for the treatment of hyperproliferative diseases, such as cancer.
Abstract translation: 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。
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Patent Agency Ranking6.发明申请BICYCLIC AZAHETEROCYCLIC CARBOXAMIDES AS INHIBITORS OF THE KINASE P70S6K 审中-公开作为激酶P70S6K的抑制剂的双相类AZAHETEROCYCLIC CARBOXAMIDES
公开(公告)号：WO2012013282A1
公开(公告)日：2012-02-02
申请号：PCT/EP2011/003272
申请日：2011-07-01
Applicant: MERCK PATENT GMBH , HUCK, Bayard, R. , NEAGU, Constantin , JONES, Reinaldo C. , DESELM, Lizbeth, Celeste , XIAO, Yufang , KARRA, Srinivasa, R. , LAN, Ruoxi , MACHALKIN, Igor , SUTTON, Amanda, E. , RICHARDSON, Thomas, E.
Inventor： HUCK, Bayard, R. , NEAGU, Constantin , JONES, Reinaldo C. , DESELM, Lizbeth, Celeste , XIAO, Yufang , KARRA, Srinivasa, R. , LAN, Ruoxi , MACHALKIN, Igor , SUTTON, Amanda, E. , RICHARDSON, Thomas, E.
IPC: C07D239/74 , C07D403/12 , A61K31/517 , A61P35/00
CPC classification number: C07D239/94 , A61K31/517 , A61K45/06 , C07D239/74 , C07D403/12
Abstract: The invention provides novel bicyclic azaheterocyciic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Abstract translation: 本发明提供了根据式（I）的新型双环氮杂胞苷酰胺化合物，其用于治疗过度增殖性疾病如癌症的制备和用途。
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公开(公告)号：WO2010093419A1
公开(公告)日：2010-08-19
申请号：PCT/US2010/000313
申请日：2010-02-04
Applicant: MERCK PATENT GMBH , SUTTON, Amanda E. , RICHARDSON, Thomas E. , HUCK, Bayard R. , KARRA, Srinivasa R. , CHEN, Xiaoling , XIAO, Yufang , GOUTOPOULOS, Andreas , LAN, Ruoxi , PERREY, David , VANDEVEER, Harold, George , LIU-BUJALSKI, Lesley , STIEBER, Frank , HODOUS, Brian L. , QIU, Hui , JONES, Reinaldo C. , HEASLEY, Brian
Inventor： SUTTON, Amanda E. , RICHARDSON, Thomas E. , HUCK, Bayard R. , KARRA, Srinivasa R. , CHEN, Xiaoling , XIAO, Yufang , GOUTOPOULOS, Andreas , LAN, Ruoxi , PERREY, David , VANDEVEER, Harold, George , LIU-BUJALSKI, Lesley , STIEBER, Frank , HODOUS, Brian L. , QIU, Hui , JONES, Reinaldo C. , HEASLEY, Brian
IPC: C07D239/94 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , A61K31/517 , A61P35/00
CPC classification number: C07D215/04 , A61K31/47 , C07D239/94 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04
Abstract: The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Abstract translation: 本发明提供根据式（I）的新型取代的氨基氮杂环甲酰胺化合物，其用于治疗过度增殖性疾病如癌症的制备和用途。
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8.发明申请
公开(公告)号：WO2015106058A1
公开(公告)日：2015-07-16
申请号：PCT/US2015/010752
申请日：2015-01-09
Applicant: MERCK PATENT GMBH , JORAND-LEBRUN, Catherine , JONES, Reinaldo
Inventor： JORAND-LEBRUN, Catherine , JONES, Reinaldo
IPC: C07D401/14 , C07D405/14 , C07D413/14 , C07D403/14 , C07D451/04 , A61K31/506 , A61P35/00 , A61P17/00 , A61P19/00 , A61P1/00 , A61P37/00 , A61P29/00
CPC classification number: A61K31/506 , A61P19/02 , A61P29/00 , A61P37/00 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D451/04
Abstract: The present invention provides compounds of Formula (II) for the treatment of cancer, rheumatoid arthritis and other diseases.
Abstract translation: 本发明提供了用于治疗癌症，类风湿性关节炎和其它疾病的式（II）化合物。
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9.发明申请COMPOSITIONS AND METHODS FOR THE PRODUCTION OF PYRIMIDINE AND PYRIDINE COMPOUNDS WITH BTK INHIBITORY ACTIVITY 审中-公开用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
Applicant: 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
Inventor： HODOUS, Brian L. , LIU-BUJALSKI, Lesley , JONES, Reinaldo , BANKSTON, Donald , JOHNSON, Theresa L. , MOCHALKIN, Igor , NGUYEN, Ngan , QIU, Hui , GOUTOPOULOS, Andreas , BRUGGER, Nadia
IPC: 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 classification number: 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
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：WO2012016001A1
公开(公告)日：2012-02-02
申请号：PCT/US2011/045658
申请日：2011-07-28
Applicant: MERCK PATENT GMBH , HUCK, Bayard R. , CHEN, Xiaoling , NEAGU, Constantin , JONES, Reinaldo , XIAO, Yufang , MOCHALKIN, Igor
Inventor： HUCK, Bayard R. , CHEN, Xiaoling , NEAGU, Constantin , JONES, Reinaldo , XIAO, Yufang , MOCHALKIN, Igor
IPC: C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , A61K31/4706 , A61K31/517 , A61P35/00
CPC classification number: C07D403/12 , A61K31/4709 , A61K31/517 , A61K45/06 , C07D233/90 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/14 , C07D405/12 , C07D405/14
Abstract: The invention provides novel cyclic amine azaheterocyclic carboxamide according to Formula (I), Formula (II) and Formula (III) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Abstract translation: 本发明提供根据式（I），式（II）和式（III）的新型环胺氮杂环甲酰胺，其用于治疗过度增殖性疾病如癌症的制备和用途。
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