公开(公告)号：US20190321380A1

公开(公告)日：2019-10-24

申请号：US16471304

申请日：2017-12-19

申请人： Merck Sharp & Dohme Corp. ,  Idenix Pharmaceuticals LLC

发明人： Manuel de Lera Ruiz ,  Timothy J. Hartingh ,  Izzat Raheem ,  John Schreier ,  Jean-Laurent Paparin

IPC分类号： A61K31/675 ,  A61P31/18 ,  A61K31/536 ,  A61K31/496 ,  C07D473/34

摘要： Compounds of Formula I: and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.

公开(公告)号：US11123355B2

公开(公告)日：2021-09-21

申请号：US16471304

申请日：2017-12-19

申请人： Merck Sharp & Dohme Corp. ,  Idenix Pharmaceuticals LLC

发明人： Manuel de Lera Ruiz ,  Timothy J. Hartingh ,  Izzat Raheem ,  John Schreier ,  Jean-Laurent Paparin

IPC分类号： A61K31/675 ,  A61K31/522 ,  A61K31/505 ,  A61K31/34 ,  A61K31/44 ,  A61K31/4965 ,  A61P31/18 ,  A61K31/496 ,  A61K31/536 ,  C07D473/34

摘要： Compounds of Formula I: and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.

公开(公告)号：US20180037554A1

公开(公告)日：2018-02-08

申请号：US15549242

申请日：2016-02-01

申请人： Merck Sharp & Dohme Corp.

发明人： Amjad Ali ,  Rongze Kuang ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Pauline C. Ting ,  Purakkattle Biju ,  Manuel de Lera Ruiz ,  Sylvia J. Degrado ,  Alexander L. Tung ,  Timothy J. Henderson ,  Liwu Hong ,  Jae-Hun Kim ,  Dong Won-Shik Kim ,  Joe Lee ,  Jie Wu ,  Heping Wu ,  Yushi Xiao ,  Tao Yu ,  Gang Zhou ,  Xiaohong Zhu ,  Kevin D. McCormick ,  Jayaram R. Tagat ,  Dong Xiao ,  Tanweer Khan ,  Jianhua Cao ,  Michael Berlin ,  Yonglian Zhang

IPC分类号： C07D239/84 ,  C07D401/14 ,  C07D413/12 ,  C07D417/12 ,  C07D405/12 ,  C07D417/14 ,  C07D413/14 ,  C07D471/04 ,  C07D401/12 ,  C07D403/12

CPC分类号： C07D239/84 ,  A61K31/517 ,  A61P25/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： The present invention is directed to compounds of generic formula I: or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist.

公开(公告)号：US20160214997A1

公开(公告)日：2016-07-28

申请号：US14914843

申请日：2014-08-25

申请人： Amjad ALI ,  Gioconda V. GALLO ,  Timothy J. HENDERSON ,  Rongze KUANG ,  Yeon-Hee LIM ,  Michael Man-Chu LO ,  Edward METZGER ,  Manuel de Lera RUIZ ,  Andrew STAMFORD ,  Paul TEMPEST ,  Brent WHITEHEAD ,  Heping WU ,  MERCK SHARP & DOHME CORP.

发明人： Ali Amjad ,  Gioconda V. Gallo ,  Timothy J. Henderson ,  Rongze Kuang ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Edward Metzger ,  Manuel de Lera Ruiz ,  Andrew Stamford ,  Paul Tempest ,  Brent Whitehead ,  Heping Wu

IPC分类号： C07D519/00 ,  C07D491/147

CPC分类号： C07D519/00 ,  C07D491/147

摘要： The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.

摘要翻译： 本发明涉及作为A2A受体拮抗剂的2,2-二氟二氧代己基化合物。 本发明还涉及本文所述的2,2-二氟二氧代环戊基化合物在涉及A2A受体的神经障碍和疾病的潜在治疗或预防中的用途。 本发明还涉及包含这些化合物的药物组合物以及这些药物组合物用于预防或治疗其中涉及A2A受体的疾病的用途。

公开(公告)号：US20130225582A1

公开(公告)日：2013-08-29

申请号：US13857001

申请日：2013-04-04

申请人： Merck Sharp & Dohme Corp.

发明人： Kevin D. McCormick ,  Li Dong ,  Christopher W. Boyce ,  Manuel de Lera Ruiz ,  Salem Fevrier ,  Jie Wu ,  Junying Zheng ,  Younong Yu ,  Jianhua Chao ,  Walter S. Won ,  Ashwin U. Rao ,  Rongze Kuang ,  Pauline C. Ting ,  Xianhai Huang ,  Ning Shao ,  Anandan Palani ,  Micheal Y. Berlin ,  Robert G. Aslanian

IPC分类号： A61K31/5377 ,  A61K31/506 ,  A61K31/537 ,  A61K31/437 ,  A61K31/501 ,  C07D413/14 ,  C07D413/10 ,  C07D471/04

CPC分类号： A61K31/5377 ,  A61K31/437 ,  A61K31/501 ,  A61K31/506 ,  A61K31/537 ,  C07D235/02 ,  C07D263/52 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D498/10 ,  C07D519/00

摘要： In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.

摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的联芳基螺氨基恶唑啉类似物作为α2C肾上腺素能受体激动剂的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种此类化合物的药物制剂的方法 以及使用这些化合物或药物组合物治疗，预防，抑制或改善与α2C肾上腺素能受体相关的一种或多种病症的方法。

公开(公告)号：US20220331321A1

公开(公告)日：2022-10-20

申请号：US17633655

申请日：2020-07-21

申请人： Merck Sharp & Dohme Corp. ,  The Walter and Eliza Hall Institute of Medical Research ,  MSD R & D (China) Co. LTD.

发明人： 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分类号： A61K31/513 ,  C07D405/14 ,  C07D493/10 ,  C07D491/052 ,  C07D409/14 ,  C07D239/22 ,  C07D405/12 ,  C07D409/04 ,  A61P33/06 ,  A61K45/06

摘要： 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.

公开(公告)号：US20130045914A1

公开(公告)日：2013-02-21

申请号：US13655176

申请日：2012-10-18

申请人： Merck Sharp & Dohme Corp.

发明人： Kevin D. McCormick ,  Li Dong ,  Christopher W. Boyce ,  Manuel de Lera Ruiz ,  Salem Fevrier ,  Jie Wu ,  Junying Zheng ,  Younong Yu ,  Jianhua Chao ,  Walter S. Won ,  Ashwin U. Rao ,  Rongze Kuang ,  Pauline C. Ting ,  Xiahai Huang ,  Ning Shao ,  Adandan Palani ,  Michael Y. Berlin ,  Robert G. Aslanian

IPC分类号： A61K31/423 ,  A61K31/506 ,  A61K31/4439 ,  C07D498/04 ,  A61K31/497 ,  C07D417/10 ,  A61K31/427 ,  A61K31/4178 ,  C07D409/10 ,  C07D405/10 ,  A61K31/501 ,  A61K31/56 ,  A61K38/00 ,  A61P25/00 ,  A61P25/22 ,  A61P25/06 ,  A61P25/20 ,  A61P25/08 ,  A61P9/00 ,  A61P37/08 ,  A61P1/12 ,  A61P9/10 ,  A61P25/24 ,  A61P13/00 ,  A61P27/06 ,  A61P25/18 ,  A61P3/10 ,  A61P29/00 ,  A61P19/02 ,  C07D413/10

CPC分类号： A61K31/5377 ,  A61K31/437 ,  A61K31/501 ,  A61K31/506 ,  A61K31/537 ,  C07D235/02 ,  C07D263/52 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D498/10 ,  C07D519/00

摘要： In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.

摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的联芳基螺氨基恶唑啉类似物作为α2C肾上腺素能受体激动剂的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种这类化合物的药物制剂的方法 以及使用这些化合物或药物组合物治疗，预防，抑制或改善与α2C肾上腺素能受体相关的一种或多种病症的方法。

公开(公告)号：US11046714B2

公开(公告)日：2021-06-29

申请号：US14914843

申请日：2014-08-25

申请人： Merck Sharp & Dohme Corp. ,  Ali Amjad ,  Gioconda V. Gallo ,  Timothy J. Henderson ,  Rongze Kuang ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Edward Metzger ,  Manuel de Lera Ruiz ,  Andrew Stamford ,  Paul Tempest ,  Brent Whitehead ,  Heping Wu

发明人： Ali Amjad ,  Gioconda V. Gallo ,  Timothy J. Henderson ,  Rongze Kuang ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Edward Metzger ,  Manuel de Lera Ruiz ,  Andrew Stamford ,  Paul Tempest ,  Brent Whitehead ,  Heping Wu

IPC分类号： C07D519/00 ,  C07D491/147

摘要： The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.

公开(公告)号：US10138212B2

公开(公告)日：2018-11-27

申请号：US15549242

申请日：2016-02-01

申请人： Merck Sharp & Dohme Corp.

发明人： Amjad Ali ,  Rongze Kuang ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Pauline C. Ting ,  Purakkattle Biju ,  Manuel de Lera Ruiz ,  Sylvia J. Degrado ,  Alexander L. Tung ,  Timothy J. Henderson ,  Liwu Hong ,  Jae-Hun Kim ,  Dong Won-Shik Kim ,  Joe Lee ,  Jie Wu ,  Heping Wu ,  Yushi Xiao ,  Tao Yu ,  Gang Zhou ,  Xiaohong Zhu ,  Kevin D. McCormick ,  Jayaram R. Tagat ,  Dong Xiao ,  Tanweer Khan ,  Jianhua Cao ,  Michael Berlin ,  Yonglian Zhang

IPC分类号： C07D239/84 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  A61P25/14 ,  A61K31/517

摘要： The present invention is directed to compounds of generic formula I: or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist.

公开(公告)号：US08569312B2

公开(公告)日：2013-10-29

申请号：US13857001

申请日：2013-04-04

申请人： Merck Sharp & Dohme Corp.

发明人： Kevin D. McCormick ,  Li Dong ,  Christopher W. Boyce ,  Manuel de Lera Ruiz ,  Salem Fevrier ,  Jie Wu ,  Junying Zheng ,  Younong Yu ,  Jianhua Chao ,  Walter S. Won ,  Ashwin U. Rao ,  Rongze Kuang ,  Pauline C. Ting ,  Xianhai Huang ,  Ning Shao ,  Anandan Palani ,  Michael Y. Berlin ,  Robert G. Aslanian

IPC分类号： A61K31/506 ,  A61K31/501 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/4184 ,  C07D235/02 ,  C07D405/10 ,  C07D409/10 ,  C07D403/10

CPC分类号： A61K31/5377 ,  A61K31/437 ,  A61K31/501 ,  A61K31/506 ,  A61K31/537 ,  C07D235/02 ,  C07D263/52 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D498/10 ,  C07D519/00

摘要： In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.

摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的联芳基螺氨基恶唑啉类似物作为α2C肾上腺素能受体激动剂的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种此类化合物的药物制剂的方法 以及使用这些化合物或药物组合物治疗，预防，抑制或改善与α2C肾上腺素能受体相关的一种或多种病症的方法。