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.

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.

公开(公告)号：US09840478B2

公开(公告)日：2017-12-12

申请号：US14908421

申请日：2014-07-29

Applicant: MERCK SHARP & DOHME CORP. ,  MSD R&D (CHINA) CO., LTD.

Inventor： Peter D. Williams ,  John A. McCauley ,  David Jonathan Bennett ,  Christopher J. Bungard ,  Lehua Chang ,  Michael P. Dwyer ,  M. Katharine Holloway ,  Kartik M. Keertikar ,  H. Marie Loughran ,  Jessie J. Manikowski ,  Gregori J. Morriello ,  Dong-Ming Shen ,  Edward C. Sherer ,  Jurgen Schultz ,  Sherman T. Waddell ,  Catherine M. Wiscount ,  Nicolas Zorn ,  Xin-Jie Chu ,  Satyanarayana Tummanapalli ,  Vijayasaradhi Sivalenka ,  Bin Hu ,  Tao Ji ,  Bin Zhong

IPC: C07D241/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/14

CPC classification number: C07D241/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention is directed to piperazine derivatives, 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.

公开(公告)号：US20170073354A1

公开(公告)日：2017-03-16

申请号：US15124635

申请日：2015-03-06

Applicant: Jurgen SCHULZ ,  Peter D. WILLIAMS ,  John A. MCCAULEY ,  Christopher J. BUNGARD ,  David Jonathan BENNETT ,  Sherman T. WADDELL ,  Gregori J. MORRIELLO ,  Lehua CHANG ,  Michael P. DWYER ,  Katharine M. HOLLOWAY ,  Alejandro CRESPO ,  Xin-Jie CHU ,  Catherine WISCOUNT ,  Marie H. LOUGHRAN ,  Jesse J. MANIKOWSKI ,  Kartik M. KEERTIKAR ,  Bin HU ,  Bin ZHONG ,  Tao JI ,  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: C07D513/08 ,  A61K31/554 ,  A61K45/06

CPC classification number: C07D513/08 ,  A61K31/554 ,  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.

Abstract translation: 本发明涉及含有该化合物的式I药物组合物的化合物及其在抑制HIV蛋白酶，抑制HIV复制，预防HIV感染，HIV感染治疗和预防， 治疗和延迟艾滋病的发病或进展。

公开(公告)号：US20160159752A1

公开(公告)日：2016-06-09

申请号：US14908421

申请日：2014-07-29

Applicant: MERCK SHARP & DOHME CORP. ,  MSD R&D (CHINA) CO., LTD.

Inventor： Peter D. Williams ,  John A. McCauley ,  David Jonathan Bennett ,  Christopher J. Bungard ,  Lehua Chang ,  Michael P. Dwyer ,  M. Katharine Holloway ,  Kartik M. Keertikar ,  H. Marie Loughran ,  Jessie J. Manikowski ,  Gregori J. Morriello ,  Dong-Ming Shen ,  Edward C. Sherer ,  Jurgen Schultz ,  Sherman T. Waddell ,  Catherine M. Wiscount ,  Nicolas Zorn ,  Xin-Jie Chu ,  Satyanarayana Tummanapalli ,  Vijayasaradhi Sivalenka ,  Bin Hu ,  Tao Ji ,  Bin Zhong

IPC: C07D241/04 ,  C07D401/12 ,  C07D417/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/06 ,  C07D405/12

CPC classification number: C07D241/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention is directed to piperazine derivatives, 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.

Abstract translation: 本发明涉及哌嗪衍生物，包含它们的药物组合物及其在抑制HIV蛋白酶，HIV复制抑制，HIV预防感染，HIV感染治疗和预防治疗中的用途 ，并延迟艾滋病的发病或进展。

公开(公告)号：US20250066379A1

公开(公告)日：2025-02-27

申请号：US18716280

申请日：2022-12-05

Applicant: Merck Sharp & Dohme LLC ,  The Walter and Eliza Hall Institute of Medical Research ,  MSD R&D (China) Co., Ltd.

Inventor： John A. McCauley ,  Manuel De Lera Ruiz ,  Zhuyan Guo ,  Philippe Nantermet ,  Michael J. Kelly, III ,  Alvaro Gutierrez Bonet ,  Lianyun Zhao ,  Zhiyu Lei ,  Bin Hu ,  Dongmei Zhan ,  Anthony Hodder

IPC: C07D491/22 ,  A61K31/519 ,  A61K45/06 ,  C07D487/08 ,  C07D491/048 ,  C07D491/052 ,  C07D519/00

Abstract: Provided are 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. Also provided are 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：US20230139282A1

公开(公告)日：2023-05-04

申请号：US17795349

申请日：2021-02-02

Applicant: Manuel DE LERA RUIZ ,  Paola FAVUZZA ,  Zhuyan GUO ,  Bin HU ,  Michael J. KELLY, III ,  Zhiyu LEI ,  John A. MCCAULEY ,  David B. OLSEN ,  Brad SLEEBS ,  Tony TRIGLIA ,  Dongmei ZHAN ,  Lianyun ZHAO ,  Merck Sharp & Dohme LLC ,  The Walter and Eliza Hall Institute of Medical Research ,  MSD R&D (China) Co., Ltd.

Inventor： Manuel de Lera Ruiz ,  Paola Favuzza ,  Zhuyan Guo ,  Bin Hu ,  Michael J. Kelly, III ,  Zhiyu Lei ,  John A. McCauley ,  David B. Olsen ,  Brad Sleebs ,  Tony Triglia ,  Dongmei Zhan ,  Lianyun Zhao

IPC: A61K31/513 ,  A61K45/06 ,  C07D405/12 ,  C07D233/88 ,  C07D405/14 ,  C07D417/14 ,  C07D491/18 ,  A61P33/06 ,  A61K31/529 ,  A61K31/5377 ,  C07D401/06

Abstract: Provided are 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. Also provided are uses of the compounds of Formula (I), as defined herein, 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：US20230013692A1

公开(公告)日：2023-01-19

申请号：US17776040

申请日：2020-11-16

Applicant: Merck Sharp & Dohme LLC ,  MSD R&D (China) Co. Ltd. ,  The Walter and Eliza Hall Institute of Medical Research

Inventor： John A. McCauley ,  Manuel de Lera Ruiz ,  Zhuyan Guo ,  Bin Hu ,  Michael J. Kelly, III ,  Zhiyu Lei ,  David B. Olsen ,  Brad Sleebs ,  Dongmei Zhan ,  Lianyun Zhao

IPC: C07D239/22 ,  C07D401/06 ,  C07D405/14 ,  A61P33/06

Abstract: The present invention provides 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. The invention also provides uses of the compounds of Formula (I), as defined herein, for the possible inhibition of 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：US10787441B2

公开(公告)日：2020-09-29

申请号：US16094621

申请日：2017-04-17

Applicant: Merck Sharp & Dohme Corp.

Inventor： Joseph A. Kozlowski ,  Wensheng Yu ,  Bin Hu ,  Bin Zhong ,  Jinglai Hao ,  Dahai Wang ,  Zhixin Lei

IPC: A61K31/4178 ,  C07D405/14 ,  A61K38/21 ,  A61K38/19 ,  A61K45/06

Abstract: A compound of Formula (I) or (II), for treating or preventing an HCV infection in a subject.

公开(公告)号：US10738062B2

公开(公告)日：2020-08-11

申请号：US16326043

申请日：2017-08-14

Applicant: Merck Sharp & Dohme Corp.

Inventor： Wensheng Yu ,  Joseph A. Kozlowski ,  Ling Tong ,  Craig A. Coburn ,  Bin Hu ,  Bin Zhong ,  Jinglai Hao ,  Dahai Wang

IPC: C07D498/04 ,  A61K45/06 ,  A61K31/496 ,  A61K31/5365 ,  A61P31/14

Abstract: The present invention relates to novel Chromane-Substituted Tetracyclic Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, A′, R2 R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising a Chromane-Substituted Tetracyclic Compound, and methods of using the Chromane-Substituted Tetracyclic Compounds for treating or preventing HCV infection in a patient.