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1.发明授权公开(公告)号：US11149036B2
公开(公告)日：2021-10-19
申请号：US16621959
申请日：2018-06-22
申请人： John J. Acton, III , Merck Sharp & Dohme Corp. , MSD R&D (China) Co., Ltd. , Jianming Bao , Qiaolin Deng , Melissa Egbertson , Ronald Ferguson, II , Xiaolei Gao , Scott Timothy Harrison , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Zhaoyang Meng , Meng Na , Michael T. Rudd , Oleg Selyutin , David M. Tellers , Ling Tong , Fengqi Zhang
发明人： John J. Acton, III , Jianming Bao , Qiaolin Deng , Melissa Egbertson , Ronald Ferguson, II , Xiaolei Gao , Scott Timothy Harrison , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Zhaoyang Meng , Meng Na , Michael T. Rudd , Oleg Selyutin , David M. Tellers , Ling Tong , Fengqi Zhang
IPC分类号： C07D471/04 , C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D491/048 , C07D498/04
摘要： The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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公开(公告)号：US20170342076A1
公开(公告)日：2017-11-30
申请号：US15538910
申请日：2015-12-17
申请人： JIAN LIU , JOSEPH A. KOZLOWSKI , BRIAN M. ANDRESEN , SOBHANA BABU BOGA , XIAOLEI GAO , DEODIAL GUY GUIADEEN , JIAQIANG CAI , SHILAN LIU , DAHAI WANG , HAO WU , CHUNDAO YANG
发明人： JIAN LIU , JOSEPH A. KOZLOWSKI , BRIAN M. ANDRESEN , SOBHANA BABU BOGA , XIAOLEI GAO , DEODIAL GUY GUIADEEN , JIAQIANG CAI , SHILAN LIU , DAHAI WANG , HAO WU , CHUNDAO YANG
IPC分类号： C07D487/04 , A61K31/4985
CPC分类号： C07D487/04 , A61K31/4985 , A61K45/06
摘要： The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, Formula I or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.
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公开(公告)号：US20150353570A1
公开(公告)日：2015-12-10
申请号：US14762954
申请日：2014-01-22
申请人： Hao WU , Ronald M. KIM , Jian LIU , Xiaolei GAO , Sobhana Babu BOGA , Deodialsingh GUIADEEN , Joseph KOZLOWSKI , Wensheng YU , Rajan ANAND , Younong YU , Oleg B. Selyutin , Ying-Duo GAO , Shilan LIU , Chundao YANG , Hongjian WANG , MERCK SHARP & DOHME CORP.
发明人： RONALD M. KIM , JIAN LIU , XIAOLEI GAO , SOBHANA BABU BOGA , DEODIALSINGH GUIADEEN , JOSEPH A. KOZLOWSKI , WENSHENG WU , RAJAN ANAND , YOUNONG YU , OLEG B. SELYUTIN , YING-DUO GAO , HAO WU , SHILAN LIU , CHUNDAO YANG , HONGJIAN WANG
IPC分类号： C07D491/048 , C07D471/04 , A61K45/06 , A61K31/5383 , C07D455/02 , A61K31/5365 , A61K31/497 , C07D498/04
CPC分类号： C07D491/048 , A61K31/497 , A61K31/4985 , A61K31/506 , A61K31/519 , A61K31/5365 , A61K31/5383 , A61K45/06 , C07D455/02 , C07D471/04 , C07D487/04 , C07D498/04 , C07D519/00 , Y02A50/411 , Y02A50/463
摘要： The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.
摘要翻译： 本发明提供了根据式I的Bruton's酪氨酸激酶（Btk）抑制剂化合物或其药学上可接受的盐或包含这些化合物的药物组合物及其在治疗中的用途。 特别地，本发明涉及Btk抑制剂化合物在治疗Btk介导的病症中的用途。
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公开(公告)号：US20140221333A1
公开(公告)日：2014-08-07
申请号：US14233478
申请日：2012-07-19
申请人： Adrianus Petrus Antonius De Man , Jan-Gerard Sterrenburg , Han C.A. Raaijmakers , Allard Kaptein , Arthura A. Oubrie , Johannes Bernardus Maria Rewinkel , Christiaan Gerardus Johannes Maria Jans , Jacobus C.H.M. Wijkamans , Tjeerd A. Barf , Alan B. Cooper , Ronald M. Kim , Sobhana Babu Boga , Hugh Y. Zhu , Xiaolei Gao , Xin Yao , Rajan Anand , Hao Wu , Shilan Liu , Chundao Yang , Abdul-Basit Alhassan , James Wang , Younong Yu , Jian Liu , Henry M. Vaccaro
发明人： Adrianus Petrus Antonius De Man , Jan-Gerard Sterrenburg , Han C.A. Raaijmakers , Allard Kaptein , Arthura A. Oubrie , Johannes Bernardus Maria Rewinkel , Christiaan Gerardus Johannes Maria Jans , Jacobus C.H.M. Wijkamans , Tjeerd A. Barf , Alan B. Cooper , Ronald M. Kim , Sobhana Babu Boga , Hugh Y. Zhu , Xiaolei Gao , Xin Yao , Rajan Anand , Hao Wu , Shilan Liu , Chundao Yang , Abdul-Basit Alhassan , James Wang , Younong Yu , Jian Liu , Henry M. Vaccaro
IPC分类号： C07D487/04 , C07D513/04 , A61K31/55 , A61K31/5377 , A61K31/53 , A61K31/4985 , A61K31/541
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/06 , C07D471/04 , C07D513/04 , C07D519/00
摘要： Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
摘要翻译： 提供根据式（I）的6-5元稠合吡啶环化合物或其药学上可接受的盐，包含这些化合物的药物组合物及其在治疗中的用途。 特别地，提供了使用元稠合的吡啶环化合物来治疗布鲁丁的酪氨酸激酶（Btk）介导的病症。
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公开(公告)号：US20130096084A1
公开(公告)日：2013-04-18
申请号：US13703250
申请日：2011-06-22
申请人： Yongqi Deng , Liang Zhu , Gerald W. Shipps, JR. , Sie-Mun Lo , Binyuan Sun , Xiaohua Huang , Corey Bienstock , Alan B. Cooper , Xiaolei Gao , Xin Yao , Hugh Y. Zhu , Joseph M. Kelly , Sobhana Babu Boga , Abdul-Basit Alhassan , Jayaram R. Tagat , Umar Faruk Mansoor , Kevin J. Wilson , Brendan M. O'Boyle , Matthew Hersh Daniels , Adam Schell , Phieng Siliphaivanh , Christian Fischer
发明人： Yongqi Deng , Liang Zhu , Gerald W. Shipps, JR. , Sie-Mun Lo , Binyuan Sun , Xiaohua Huang , Corey Bienstock , Alan B. Cooper , Xiaolei Gao , Xin Yao , Hugh Y. Zhu , Joseph M. Kelly , Sobhana Babu Boga , Abdul-Basit Alhassan , Jayaram R. Tagat , Umar Faruk Mansoor , Kevin J. Wilson , Brendan M. O'Boyle , Matthew Hersh Daniels , Adam Schell , Phieng Siliphaivanh , Christian Fischer
IPC分类号： C07D401/14 , A61K45/06 , C07D405/14 , A61K31/454 , A61K31/55 , A61K31/551 , C07D401/12 , C07D409/14 , C07D417/14 , A61K31/506 , C07D471/04 , C07F7/18 , A61K31/695 , C07D413/14 , A61K31/5377 , A61K31/4545
CPC分类号： C07D401/14 , A61K31/454 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/1804
摘要： The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
摘要翻译： 本发明提供了式I化合物：（式I应在此插入）或其药学上可接受的盐，溶剂化物或酯，其中R，R 1，R 2和R 3如本文所定义。 这些化合物是ERK抑制剂。 还公开了包含上述化合物的药物组合物和使用其治疗癌症的方法。
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6.发明申请公开(公告)号：US20200207758A1
公开(公告)日：2020-07-02
申请号：US16621959
申请日：2018-06-22
申请人： John J. ACTON, III , Jianming BAO , Qiaolin DENG , Melissa EGBERTSON , Ronald FERGUSON, II , Xiaolei GAO , Scott Timothy HARRISON , Sandra L. KNOWLES , Chunsing LI , Michael Man-Chu LO , Robert D. MAZZOLA, Jr. , Zhaoyang MENG , Meng NA , Michael T. RUDD , Oleg SELYUTIN , David M. TELLERS , Ling TONG , Fengqi ZHANG
发明人： John J. ACTON, III , Jianming BAO , Qiaolin DENG , Melissa EGBERTSON , Ronald FERGUSON, II , Xiaolei GAO , Scott Timothy HARRISON , Sandra L. KNOWLES , Chunsing LI , Michael Man-Chu LO , Robert D. MAZZOLA, Jr. , Zhaoyang MENG , Meng NA , Michael T. RUDD , Oleg SELYUTIN , David M. TELLERS , Ling TONG , Fengqi ZHANG
IPC分类号： C07D471/04 , C07D401/14 , C07D401/04 , C07D413/14 , C07D405/14 , C07D491/048 , C07D498/04
摘要： The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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7.发明申请公开(公告)号：US20190315708A1
公开(公告)日：2019-10-17
申请号：US16471679
申请日：2017-12-18
申请人： Jianming BAO , Ronald FERGUSON , Xiaolei GAO , Scott HARRISON , Sandra L. KNOWLES , Michael Man-chu LO , Robert D. MAZZOLA, JR. , Jeffrey W. SCHUBERT , Merck Sharp & Dohme Corp. , MSD R&D (CHINA) CO., LTD.
发明人： Jianming BAO , Ronald FERGUSON , Xiaolei GAO , Scott HARRISON , Sandra L. KNOWLES , Michael Man-Chu LO , Robert D. Mazzola, Jr. , Jeffrey W. Shubert
IPC分类号： C07D401/04 , C07D401/14 , C07D417/14 , C07D513/04 , C07D405/14 , C07D413/14 , C07D498/08 , C07D491/107
摘要： The present invention is directed to heteroarylpiperidine ether compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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公开(公告)号：US20180009828A1
公开(公告)日：2018-01-11
申请号：US15538957
申请日：2015-12-17
申请人： JIAN LIU , JOSEPH A. KOZLOWSKI , XIAOLEI GAO , DEODIAL GUY GUIADEEN , SHILAN LIU , DAHAI WANG
发明人： JIAN LIU , JOSEPH A. KOZLOWSKI , XIAOLEI GAO , DEODIAL GUY GUIADEEN , SHILAN LIU , DAHAI WANG
IPC分类号： C07D519/00 , A61K31/4985
CPC分类号： C07D519/00 , A61K31/4985 , A61K45/06
摘要： The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, Formula (I) or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.
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![6,7-DIHYDRO-5H-PYRROLO[3,4-B]PYRIDIN-5-ONE ALLOSTERIC MODULATORS OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR](/abs-image/US/2017/06/29/US20170183342A1/abs.jpg.150x150.jpg)
9.发明申请公开(公告)号：US20170183342A1
公开(公告)日：2017-06-29
申请号：US15386009
申请日：2016-12-21
申请人： JIANMING BAO , XIAOLEI GAO , SANDRA L. KNOWLES , CHUNSING LI, I , MICHAEL MAN-CHU LO , ROBERT D. MAZZOLA, Jr. , DEBRA L. ONDEYKA , ANDREW W. STAMFORD , FENGQI ZHANG
发明人： JIANMING BAO , XIAOLEI GAO , SANDRA L. KNOWLES , CHUNSING LI, I , MICHAEL MAN-CHU LO , ROBERT D. MAZZOLA, Jr. , DEBRA L. ONDEYKA , ANDREW W. STAMFORD , FENGQI ZHANG
IPC分类号： C07D471/04 , C07D491/048 , C07D491/052 , C07D471/08
CPC分类号： C07D471/04 , C07D471/08 , C07D491/048 , C07D491/052 , C07D519/00 , C07F9/222 , C07F9/6561
摘要： The present invention is directed to 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine-5-one compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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公开(公告)号：US08999957B2
公开(公告)日：2015-04-07
申请号：US13703250
申请日：2011-06-22
申请人： Yongqi Deng , Liang Zhu , Gerald W. Shipps, Jr. , Sie-Mun Lo , Binyuan Sun , Xiaohua Huang , Corey Bienstock , Alan B. Cooper , Xiaolei Gao , Xin Yao , Hugh Y. Zhu , Joseph M. Kelly , Sobhana Babu Boga , Abdul-Basit Alhassan , Jayaram R. Tagat , Umar Faruk Mansoor , Kevin J. Wilson , Brendan M. O'Boyle , Matthew Hersh Daniels , Adam Schell , Phieng Siliphaivanh , Christian Fischer
发明人： Yongqi Deng , Liang Zhu , Gerald W. Shipps, Jr. , Sie-Mun Lo , Binyuan Sun , Xiaohua Huang , Corey Bienstock , Alan B. Cooper , Xiaolei Gao , Xin Yao , Hugh Y. Zhu , Joseph M. Kelly , Sobhana Babu Boga , Abdul-Basit Alhassan , Jayaram R. Tagat , Umar Faruk Mansoor , Kevin J. Wilson , Brendan M. O'Boyle , Matthew Hersh Daniels , Adam Schell , Phieng Siliphaivanh , Christian Fischer
IPC分类号： C07D401/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D401/14 , C07D405/14 , A61K31/454 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07F7/18
CPC分类号： C07D401/14 , A61K31/454 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/1804
摘要： The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
摘要翻译： 本发明提供了式I化合物：（式I应在此插入）或其药学上可接受的盐，溶剂化物或酯，其中R，R 1，R 2和R 3如本文所定义。 这些化合物是ERK抑制剂。 还公开了包含上述化合物的药物组合物和使用其治疗癌症的方法。
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