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：US20150246917A1

公开(公告)日：2015-09-03

申请号：US14711345

申请日：2015-05-13

Applicant: Merck Sharp & Dohme Corp.

Inventor： Craig A. Coburn ,  Steven W. Ludmerer ,  Kun Liu ,  Hao Wu ,  Richard Soll ,  Bin Zhong ,  Jian Zhu

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/4985 ,  C07D401/14 ,  A61K31/4439 ,  C07D403/14 ,  A61K31/4184 ,  C07D403/12 ,  C07D413/14 ,  A61K31/423 ,  C07D405/14 ,  A61K31/4025 ,  C07D405/12 ,  A61K31/404 ,  A61K31/506 ,  A61K31/5377 ,  C07D498/04 ,  A61K31/5383 ,  A61K31/553 ,  A61K45/06 ,  A61K31/437

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。

公开(公告)号：US20220356182A1

公开(公告)日：2022-11-10

申请号：US17324799

申请日：2021-05-19

Applicant: Merck Sharp & Dohme Corp.

Inventor： Craig A. Coburn ,  Steven W. Ludmerer ,  Kun Liu ,  Hao Wu ,  Richard Soll ,  Bin Zhong ,  Jian Zhu

IPC: C07D471/04 ,  C07D407/14 ,  A61K31/4985 ,  A61K31/4439 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/4025 ,  A61K31/519 ,  A61K31/404 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/427 ,  A61K31/4245 ,  A61K31/475 ,  A61K31/536 ,  A61K31/4178 ,  A61K31/517 ,  A61K31/5386 ,  A61K31/553 ,  C07D487/04 ,  C07D401/14 ,  C07D403/14 ,  C07D403/12 ,  C07D413/14 ,  C07D405/14 ,  C07D405/12 ,  C07D417/14 ,  C07D409/14 ,  A61K31/437

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.

公开(公告)号：US20200262836A1

公开(公告)日：2020-08-20

申请号：US16829878

申请日：2020-03-25

Applicant: Merck Sharp & Dohme Corp.

Inventor： CRAIG A. COBURN ,  STEVEN W. LUDMERER ,  KUN LIU ,  Hao Wu ,  Richard Soll ,  Bin Zhong ,  Jian Zhu

IPC: C07D471/04 ,  A61K31/437 ,  C07D409/14 ,  C07D417/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D403/12 ,  C07D403/14 ,  C07D401/14 ,  C07D487/04 ,  A61K31/553 ,  A61K31/5386 ,  A61K31/517 ,  A61K31/4178 ,  A61K31/536 ,  A61K31/475 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/404 ,  A61K31/519 ,  A61K31/4025 ,  A61K31/423 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/4985 ,  C07D407/14

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.

公开(公告)号：US20160257697A1

公开(公告)日：2016-09-08

申请号：US14761259

申请日：2013-12-31

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Ling Tong ,  Wensheng Yu ,  Joseph A. Kozlowski ,  Lei Chen ,  Oleg Selyutin ,  Seong Heon Kim ,  Michael Dwyer ,  Bin Hu ,  Bin Zhong ,  Dahai Wang ,  Jinglai Hao ,  Changmao Shen ,  Zhixin Lei ,  Weijun Wang

IPC: C07D498/04 ,  C07D519/00 ,  A61K45/06 ,  A61K31/7056 ,  A61K31/7072 ,  A61K38/00 ,  A61K31/5365 ,  A61K38/21

CPC classification number: C07D498/04 ,  A61K31/4985 ,  A61K31/5365 ,  A61K31/7056 ,  A61K31/7072 ,  A61K38/005 ,  A61K38/212 ,  A61K45/06 ,  C07D519/00 ,  Y02A50/385 ,  Y02A50/387 ,  Y02A50/389 ,  Y02A50/395 ,  A61K2300/00

Abstract: Thiophene-substituted tetracyclic compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein A, A′, R2, R3, R4 and R5 are as defined herein. The compositions comprising at least one thiophene-substituted tetracyclic compound, and methods of using the thiophene-substituted tetracyclic compounds for treating or preventing HCV infection in a patient are also provided.

Abstract translation: 式（I）的噻吩取代的四环化合物及其药学上可接受的盐，其中A，A'，R 2，R 3，R 4和R 5如本文所定义。 还提供了包含至少一种噻吩取代的四环化合物的组合物，以及使用噻吩取代的四环化合物治疗或预防患者HCV感染的方法。

公开(公告)号：US09090661B2

公开(公告)日：2015-07-28

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: A61K31/4178 ,  C07D405/14 ,  C07K5/08 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D498/10 ,  A61K31/437 ,  A61K38/05 ,  A61K38/06 ,  A61K45/06 ,  C07K5/06

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。

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.