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公开(公告)号：US09440952B2
公开(公告)日：2016-09-13
申请号：US14772589
申请日：2014-02-27
Applicant: Merck Sharp & Dohme Corp.
Inventor： Michael Miller , Kallol Basu , Duane DeMong , Jack Scott , Hong Liu , Xing Dai , Joel M. Harris , Bernard Neustadt , Andrew Stamford , Marc Poirier , John A. McCauley , Thomas Greshock , Heather Stevenson , John Sanders , Jonathan Kern
IPC: C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/10 , C07D451/02 , C07D487/10 , C07D491/04 , C07D491/08 , C07D491/056 , C07D498/04 , C07D498/08 , C07D403/04 , C07D491/10 , C07D487/04 , C07D491/107 , C07D491/113
CPC classification number: C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D451/02 , C07D471/10 , C07D487/04 , C07D487/10 , C07D491/04 , C07D491/056 , C07D491/08 , C07D491/10 , C07D491/107 , C07D491/113 , C07D498/04 , C07D498/08
Abstract: The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
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公开(公告)号：US20140371138A1
公开(公告)日：2014-12-18
申请号：US14473117
申请日：2014-08-29
Applicant: Merck Sharp & Dohme Corp.
Inventor： Craig A. Coburn , John A. McCauley , Steven W. Ludmerer , Kun Liu , Joseph P. Vacca , Hao Wu , Bin Hu , Richard Soll , Fei Sun , Xinghai Wang , Man Yan , Chengren Zhang , Mingwei Zheng , Bin Zhong , Jian Zhu
IPC: C07K5/08 , A61K38/05 , A61K38/06 , C07D471/04 , A61K31/437 , C07K5/06 , A61K45/06
CPC classification number: C07D498/04 , A61K31/4025 , A61K31/404 , A61K31/4178 , A61K31/4184 , A61K31/423 , A61K31/437 , A61K31/4439 , A61K31/4985 , A61K31/506 , A61K31/5365 , A61K31/5377 , A61K31/5383 , A61K31/553 , A61K38/05 , A61K38/06 , A61K45/06 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D498/10 , C07K5/06 , C07K5/08
Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
Abstract translation: 本发明涉及可用作丙型肝炎病毒（HCV）NS5A抑制剂，这种化合物的合成以及这些化合物用于抑制HCV NS5A活性用于治疗或预防HCV感染的用途的式（I）化合物和 抑制基于细胞的系统中的HCV病毒复制和/或病毒生产。
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公开(公告)号：US20220331321A1
公开(公告)日：2022-10-20
申请号：US17633655
申请日：2020-07-21
Applicant: Merck Sharp & Dohme Corp. , The Walter and Eliza Hall Institute of Medical Research , MSD R & D (China) Co. LTD.
Inventor： John A. McCauley , Alan F. Cowman , Manuel de Lera Ruiz , Paola Favuzza , Zhuyan Guo , Bin Hu , Michael J. Kelly, III , Zhiyu Lei , David B. Olsen , Brad Sleebs , Jennifer K. Thompson , Tony Triglia , Dongmei Zhan , Cailing Zhang , Lianyun Zhao
IPC: A61K31/513 , C07D405/14 , C07D493/10 , C07D491/052 , C07D409/14 , C07D239/22 , C07D405/12 , C07D409/04 , A61P33/06 , A61K45/06
Abstract: Methods of treating malaria comprising administration of compounds of Formula (I′) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. It also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin X, plasmepsin IX or plasmepsin X and IX activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.
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公开(公告)号：US20220259227A1
公开(公告)日：2022-08-18
申请号：US17670689
申请日：2022-02-14
Applicant: Merck Sharp & Dohme Corp.
Inventor： Timothy John Hartingh , John A. McCauley , Tao Yu , Yonglian Zhang
IPC: C07D498/22 , A61K45/06
Abstract: The present invention relates to Tetracyclic Heterocycle Compounds of Formula and pharmaceutically acceptable salts or prodrug thereof, wherein R1 is as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Heterocycle Compound, and methods of using the Tetracyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
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公开(公告)号：US20190322666A1
公开(公告)日：2019-10-24
申请号：US16454857
申请日：2019-06-27
Applicant: MERCK SHARP & DOHME CORP.
Inventor： Tao Yu , Sherman T. Waddell , Thomas H. Graham , Yonglian Zhang , John A. McCauley , Andrew W. Stamford , Jiaqiang Cai , Zhiqi Qi
IPC: C07D471/16 , A61K31/635 , A61K31/427 , A61K31/513 , A61K31/5365 , A61K31/4402 , A61K31/4985 , A61K31/505 , A61K31/52 , A61K31/683
Abstract: The present invention relates to Fused Tricyclic Heterocyclic Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocyclic Compound, and methods of using the Fused Tricyclic Heterocyclic Compounds for treating or preventing HIV infection in a subject.
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Patent Agency Ranking
公开(公告)号：US10138255B2
公开(公告)日：2018-11-27
申请号：US15124635
申请日：2015-03-06
Applicant: Merck Sharp & Dohme Corp. , MSD R&D (China) Co., Ltd.
Inventor： Peter D. Williams , John A. McCauley , Christopher J. Bungard , David Jonathan Bennett , Sherman T. Waddell , Gregori J. Morriello , Lehua Chang , Michael P. Dwyer , M. Katharine Holloway , Alejandro Crespo , Xin-Jie Chu , Catherine Wiscount , H. Marie Loughran , Jesse J. Manikowski , Jurgen Schulz , Kartik M. Keertikar , Bin Hu , Bin Zhong , Tao Ji
IPC: A61K31/554 , C07D513/08 , A61K45/06
Abstract: The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
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公开(公告)号：US20180099967A1
公开(公告)日：2018-04-12
申请号：US15840017
申请日：2017-12-13
Applicant: MERCK SHARP & DOHME CORP.
Inventor： Tao Yu , Sherman T. Waddell , Thomas H. Graham , Yonglian Zhang , John A. McCauley , Andrew W. Stamford , Jiaqiang Cai , Zhiqi Qi
IPC: C07D471/16 , A61K31/52 , A61K31/4402 , A61K31/4985 , A61K31/505 , A61K31/427 , A61K31/5365 , A61K31/635 , A61K31/683 , A61K31/513
CPC classification number: C07D471/16 , A61K31/427 , A61K31/4402 , A61K31/4985 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/5365 , A61K31/635 , A61K31/683
Abstract: The present invention relates to Fused Tricyclic Heterocyclic Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocyclic Compound, and methods of using the Fused Tricyclic Heterocyclic Compounds for treating or preventing HIV infection in a subject.
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公开(公告)号：US20180051043A1
公开(公告)日：2018-02-22
申请号：US15560896
申请日：2016-03-25
Applicant: Merck Sharp & Dohme Corp.
Inventor： Tao Yu , Sherman T. Waddell , John A. McCauley , Thomas H. Graham , Hong Li , Izzat Raheem , Jay A. Grobler
IPC: C07F9/6561 , A61K31/683 , A61K31/675
CPC classification number: C07F9/6561 , A61K31/427 , A61K31/4402 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/635 , A61K31/675 , A61K31/683 , A61K2300/00
Abstract: The present invention relates to Phosphate Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R1, R2, R3, R4, R5, R9 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Phosphate Substituted Quinolizine Derivative, and methods of using the Phosphate Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
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公开(公告)号：US09718818B2
公开(公告)日：2017-08-01
申请号：US14912761
申请日：2014-08-18
Applicant: MERCK SHARP & DOHME CORP. , Duane DeMong , Thomas J. Greshock , Ronald K. Chang , Xing Dai , Hong Liu , John A. McCauley , Wei Li , Kallol Basu , Jack D. Scott , Michael Miller
Inventor： Duane DeMong , Thomas J. Greshock , Ronald K. Chang , Xing Dai , Hong Liu , John A. McCauley , Wei Li , Kallol Basu , Jack D. Scott , Michael Miller
IPC: A61K31/44 , C07D471/04 , C07D498/04 , C07D519/00 , C07D487/04
CPC classification number: C07D471/04 , C07D487/04 , C07D498/04 , C07D519/00
Abstract: The present invention is directed to azaindazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
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公开(公告)号：US20160200722A1
公开(公告)日：2016-07-14
申请号：US14912761
申请日：2014-08-18
Applicant: Duane DEMONG , Thomas J. GRESHOCK , Ronald K. CHANG , Xing DAI , Hong LIU , John A. MCCAULEY , Wei LI , Kallol BASU , Jack D. SCOTT , Michael MILLER , MERCK SHARP & DOHME CORP.
Inventor： Duane DeMong , Thomas J. Greshock , Ronald K. Chang , Xing Dai , Hong Liu , John A. McCauley , Wei Li , Kallol Basu , Jack D. Scott , Michael Miller
IPC: C07D471/04 , C07D498/04 , C07D519/00
CPC classification number: C07D471/04 , C07D487/04 , C07D498/04 , C07D519/00
Abstract: The present invention is directed to azaindazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
Abstract translation: 本发明涉及作为LRRK2激酶的有效抑制剂并且可用于治疗或预防涉及LRRK2激酶的疾病（例如帕金森病）的唑烷化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及LRRK-2激酶的疾病中的用途。
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