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1.发明申请3,3'-DISUBSTITUTED INDOLINES AS INHIBITORS OF CHOLESTEROL ESTER TRANSFER PROTEIN 有权作为胆固醇转运蛋白的抑制剂的3,3'-取代的吲哚公开(公告)号：US20160355474A1
公开(公告)日：2016-12-08
申请号：US15028306
申请日：2014-10-06
Applicant: MERCK SHARP & DOHME CORP.
Inventor： JONATHAN E. WILSON , Petr Vachal , Ravi Kurukulasuriya
IPC: C07D209/12 , A61K31/404 , C07D401/06 , A61K31/4439 , C07D417/06 , A61K31/427 , C07D401/04 , A61K31/5377 , C07D209/14 , C07D209/18 , C07D405/12 , C07D403/10 , C07D401/10 , A61K31/454 , C07D413/10 , C07D491/107 , A61K45/06
CPC classification number: C07D209/12 , A61K31/404 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K45/06 , C07D209/10 , C07D209/14 , C07D209/18 , C07D209/24 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/10 , C07D405/12 , C07D413/10 , C07D417/06 , C07D491/107
Abstract: 3,3′-Disubstituted indoline compounds, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
Abstract translation: 包括化合物的药学上可接受的盐的3,3'-二取代二氢吲哚化合物是CETP抑制剂，可用于提高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。
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公开(公告)号：US09957265B2
公开(公告)日：2018-05-01
申请号：US14778052
申请日：2014-03-19
Applicant: Merck Sharp & Dohme Corp.
Inventor： Christopher Dinsmore , Peter Fuller , David Guerin , Christopher F. Thompson , Qinglin Pu , Mark E. Scott , Jason David Katz , Ravi Kurukulasuriya , Joshua T. Close , Danielle Falcone , Jason Brubaker , Hongbo Zeng , Yunfeng Bai , Jianmin Fu , Norman Kong , Yumei Liu , Zhixiang Zheng
IPC: C07D471/04 , C07D519/00
CPC classification number: C07D471/04 , C07D519/00
Abstract: Provided are compounds of Formula I, a JAK inhibitor, and use thereof for the treatment of JAK-mediated diseases by the application.
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公开(公告)号：US10538497B2
公开(公告)日：2020-01-21
申请号：US16061597
申请日：2016-12-12
Applicant: Merck Sharp & Dohme Corp.
Inventor： Yongxin Han , Abdelghani Achab , Purakkattle Biju , Yongqi Deng , Xavier Fradera , Liangqin Guo , Shuwen He , Joseph Kozlowski , Ravi Kurukulasuriya , Kun Liu , Meredeth Ann McGowan , Qinglin Pu , Nunzio Sciammetta , Hongjun Zhang , Hua Zhou
IPC: A61K31/4245 , A61K31/433 , C07D271/08 , C07D285/10 , C07D413/12 , C07D417/12 , A61P35/00 , A61P31/12 , A61P25/24 , A61P25/28 , A61P37/06 , A61P27/12 , A61P31/14 , A61P35/02
Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
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4.发明申请GEMINALLY SUBSTITUTED CYANOETHYLPYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS 有权作为JANUS KINASE抑制剂的GEMYALLY取代的氰基乙基吡唑啉吡啶公开(公告)号：US20160272632A1
公开(公告)日：2016-09-22
申请号：US14778046
申请日：2014-03-19
Applicant: Matthew Lloyd CHILDERS , Peter FULLER , David GUERIN , Jason David KATZ , Qinglin PU , Mark E. SCOTT , Christopher E. THOMPSON , Michelle MARTINEZ , Danielle FALCONE , Luis TORRES , Yongqi DENG , Ravi KURUKULASURIYA , Hongbo ZENG , Yunfeng BAI , Norman KONG , Yumei LIU , MERCK SHARP & DOHME CORP.
Inventor： Matthew Lloyd Childers , Peter Fuller , David Guerin , Jason David Katz , Qinglin Pu , Mark E. Scott , Christopher F. Thompson , Michelle Martinez , Danielle Falcone , Luis Torres , Yongqi Deng , Ravi Kurukulasuriya , Hongbo Zeng , Yunfeng Bai , Norman Kong , Yumei Liu , Zhixiang Zheng
IPC: C07D471/04 , C07D519/00
CPC classification number: C07D471/04 , C07D519/00
Abstract: The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
Abstract translation: 本发明提供了作为JAK抑制剂的式（I）化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。
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公开(公告)号：US09226922B2
公开(公告)日：2016-01-05
申请号：US14431485
申请日：2013-09-26
Applicant: Merck Sharp & Dohme Corp.
Inventor： Kevin J. Wilson , David J. Witter , Matthew H. Daniels , Angie R. Angeles , Phieng Siliphaivanh , David Sloman , Brendan O'Boyle , Danielle Falcone , Catherine White , Ron Ferguson , Wei Zhou , Kathryn Lipford , Umar Faruk Mansoor , Salem Fevrier , Xianhai Huang , Ravi Kurukulasuriya , Judson E. Richard , Shuyi Tang , Christopher Boyce , Joseph Kozlowski , Raman Kumar Bakshi , Ganesh Babu Karunakaran
IPC: C07D401/14 , A61K31/437 , C07D471/04 , A61K45/06 , A61K31/4545
CPC classification number: A61K31/437 , A61K31/4545 , A61K45/06 , C07D471/04
Abstract: Disclosed are the ERK inhibitors of formula (1.0), having a pyrazolopyridine base structure, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0).
Abstract translation: 公开了具有吡唑并吡啶基结构的式（1.0）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（1.0）化合物治疗癌症的方法。
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Patent Agency Ranking
公开(公告)号：US20180362482A1
公开(公告)日：2018-12-20
申请号：US16061597
申请日：2016-12-12
Applicant: Merck Sharp & Dohme Corp.
Inventor： Yongxin Han , Abdelghani Achab , Purakkattle Biju , Yongqi Deng , Xavier Fradera , Liangqin Guo , Shuwen He , Joseph Kozlowski , Ravi Kurukulasuriya , Kun Liu , Meredeth Ann McGowan , Qinglin Pu , Nunzio Sciammetta , Hongjun Zhang , Hua Zhou
IPC: C07D271/08 , C07D285/10 , C07D413/12 , A61P25/24 , A61P25/28 , A61P35/02 , A61P31/14 , A61P27/12 , A61P37/06
CPC classification number: C07D271/08 , A61P25/24 , A61P25/28 , A61P27/12 , A61P31/14 , A61P35/02 , A61P37/06 , C07D285/10 , C07D413/12 , C07D417/12 , C07F9/65318
Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
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公开(公告)号：US09957264B2
公开(公告)日：2018-05-01
申请号：US14778046
申请日：2014-03-19
Applicant: Merck Sharp & Dohme Corp.
Inventor： Matthew Lloyd Childers , Peter Fuller , David Guerin , Jason David Katz , Qinglin Pu , Mark E. Scott , Christopher F. Thompson , Michelle Martinez , Danielle Falcone , Luis Torres , Yongqi Deng , Ravi Kurukulasuriya , Hongbo Zeng , Yunfeng Bai , Norman Kong , Yumei Liu , Zhixiang Zheng
IPC: C07D471/04 , C07D519/00
CPC classification number: C07D471/04 , C07D519/00
Abstract: The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
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公开(公告)号：US09688630B2
公开(公告)日：2017-06-27
申请号：US15028306
申请日：2014-10-06
Applicant: Merck Sharp & Dohme Corp.
Inventor： Jonathan E. Wilson , Petr Vachal , Ravi Kurukulasuriya
IPC: C07D491/107 , C07D417/06 , C07D413/10 , C07D405/12 , C07D403/10 , C07D401/04 , C07D401/06 , C07D401/10 , A61K31/5377 , A61K31/4439 , A61K31/454 , A61K31/427 , A61K31/404 , C07D209/12 , A61K45/06 , C07D209/10 , C07D209/24 , C07D209/14 , C07D209/18
CPC classification number: C07D209/12 , A61K31/404 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K45/06 , C07D209/10 , C07D209/14 , C07D209/18 , C07D209/24 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/10 , C07D405/12 , C07D413/10 , C07D417/06 , C07D491/107
Abstract: 3,3′-Disubstituted indoline compounds, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
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公开(公告)号：US09233979B2
公开(公告)日：2016-01-12
申请号：US14431462
申请日：2013-09-26
Applicant: Merck Sharp & Dohme Corp.
Inventor： Kevin J. Wilson , David J. Witter , Phieng Siliphaivanh , Kathryn Lipford , David Sloman , Danielle Falcone , Brendan O'Boyle , Umar Faruk Mansoor , Jongwon Lim , Joey L. Methot , Christopher Boyce , Lei Chen , Matthew H. Daniels , Salem Fevrier , Xianhai Huang , Ravi Kurukulasuriya , Ling Tong , Wei Zhou , Joseph Kozlowski , Milana M. Maletic , Bidhan A. Shinkre , Jayanth Thiruvellore Thatai , Raman Kumar Bakshi , Ganesh Babu Karunakaran
IPC: C07D401/14 , A61K31/437 , C07D498/18 , C07D471/04 , A61K31/5377 , A61K31/496 , C07D471/14 , A61K31/4375 , C07D498/14 , A61K31/553 , C07D519/00 , A61K45/06
CPC classification number: C07D498/18 , A61K31/437 , A61K31/4375 , A61K31/496 , A61K31/5377 , A61K31/553 , A61K45/06 , C07D471/04 , C07D471/14 , C07D471/16 , C07D498/14 , C07D498/16 , C07D519/00 , A61K2300/00
Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).
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公开(公告)号：US20150258074A1
公开(公告)日：2015-09-17
申请号：US14431485
申请日：2013-09-26
Applicant: Kevin J. WILSON , David J. WITTER , Matthew H. DANIELS , Angie R. ANGELES , Phieng SILIPHAIVANH , David L. SLOMAN , Brendan O'BOYLE , Danielle FALCONE , Catherine WHITE , Ron FERGUSON , Wei ZHOU , Kathryn LIPFORD , Umar Faruk MANSOOR , Salem FEVRIRE , Xianhai HUANG , Ravi KURUKULASURIYA , Judson E. RICHARD , Shuyi TANG , Christopher BOYCE , Joseph KOZLOWSKI , Raman Kumar BAKSHI , Ganesh Babu UNAKARAN , Merck Sharp & Dohme Corp.
Inventor： Kevin J. Wilson , David J. Witter , Matthew H. Daniels , Angie R. Angeles , Phieng Siliphaivanh , David Sloman , Brendan O'Boyle , Danielle Falcone , Catherine White , Ron Ferguson , Wei Zhou , Kathryn Lipford , Umar Faruk Mansoor , Salem Fevrier , Xianhai Huang , Ravi Kurukulasuriya , Judson E. Richard , Shuyi Tang , Christopher Boyce , Joseph Kozlowski , Raman Kumar Bakshi , Ganesh Babu Karunakaran
IPC: A61K31/437 , A61K45/06 , A61K31/4545 , C07D471/04
CPC classification number: A61K31/437 , A61K31/4545 , A61K45/06 , C07D471/04
Abstract: Disclosed are the ERK inhibitors of formula (1.0), having a pyrazolopyridine base structure, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0).
Abstract translation: 公开了具有吡唑并吡啶基结构的式（1.0）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（1.0）化合物治疗癌症的方法。
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