公开(公告)号：US20190183912A1

公开(公告)日：2019-06-20

申请号：US16327631

申请日：2017-08-22

Applicant: Merck Sharp & Dohme Corp. ,  IDENIX PHARMACEUTICALS LLC

Inventor： Daniel Da Costa ,  Cyril B. Dousson ,  David Dukhan ,  Jean-Laurent Paparin ,  Houcine Rahali ,  Izzat Raheem

IPC: A61K31/675 ,  A61P31/12

CPC classification number: A61K31/675 ,  A61K45/05 ,  A61K45/06 ,  A61P31/00 ,  A61P31/12 ,  C07F9/65616

Abstract: Compounds of Formula I: and pharmaceutically acceptable salts and co-crystals thereof 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：US20180362562A1

公开(公告)日：2018-12-20

申请号：US15781985

申请日：2016-12-05

Applicant: Merck Sharp & Dohme Corp. ,  Idenix Pharmaceuticals LLC

Inventor： Izzat Tiedje Raheem ,  Timothy J. Hartingh ,  John Schreier ,  Jean-Laurent Paparin

IPC: C07F9/6561 ,  A61K45/06 ,  A61P31/18 ,  A61K31/675

Abstract: Compounds of Formula I and pharmaceutically acceptable salts and co-crystals thereof 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：US20190321380A1

公开(公告)日：2019-10-24

申请号：US16471304

申请日：2017-12-19

Applicant: Merck Sharp & Dohme Corp. ,  Idenix Pharmaceuticals LLC

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

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

Abstract: 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：US20180179208A1

公开(公告)日：2018-06-28

申请号：US15847971

申请日：2017-12-20

Applicant: Merck Sharp & Dohme Corp. ,  Idenix Pharmaceuticals LLC

Inventor： Jean-Laurent Paparin ,  Izzat Raheem ,  Houcine Rahali ,  Daniel Da Costa ,  David Dukhan

IPC: C07D473/34 ,  A61K31/52 ,  A61P31/18 ,  A61K45/06

Abstract: 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：US20170198005A1

公开(公告)日：2017-07-13

申请号：US15038925

申请日：2014-11-26

Applicant: IDENIX PHARMACEUTICALS LLC

Inventor： Jean-Laurent Paparin ,  Eric Badaroux ,  Claire Pierra ,  Cyril B. Dousson

IPC: C07H19/16 ,  A61K31/7068 ,  A61K45/06 ,  C07H19/10 ,  A61K31/7076 ,  A61K31/708 ,  C07H19/06 ,  A61K31/7072

CPC classification number: C07H19/16 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/708 ,  A61K45/06 ,  C07D405/04 ,  C07D473/18 ,  C07D473/40 ,  C07F9/65586 ,  C07F9/65616 ,  C07F9/65744 ,  C07H19/06 ,  C07H19/10 ,  C07H19/11 ,  C07H19/20

Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2′-dichloro or 2′-fluoro-2′-chloro nucleoside analogue compounds which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human. In certain embodiments, the compounds are of Formula (I): or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof; wherein each of RA and RB is independently Cl or F, wherein at least one of RA and RB is Cl; and Base, PD and Z are as described herein.

公开(公告)号：US10745428B2

公开(公告)日：2020-08-18

申请号：US15781985

申请日：2016-12-05

Applicant: Merck Sharp & Dohme Corp. ,  Idenix Pharmaceuticals LLC

Inventor： Izzat Tiedje Raheem ,  Timothy J. Hartingh ,  John Schreier ,  Jean-Laurent Paparin

IPC: A61K31/675 ,  C07F9/6561 ,  A61P31/18 ,  A61K45/06

Abstract: Compounds of Formula I and pharmaceutically acceptable salts and co-crystals thereof 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：US10449208B2

公开(公告)日：2019-10-22

申请号：US16327631

申请日：2017-08-22

Applicant: Merck Sharp & Dohme Corp. ,  IDENIX PHARMACEUTICALS LLC

Inventor： Daniel Da Costa ,  Cyril B. Dousson ,  David Dukhan ,  Jean-Laurent Paparin ,  Houcine Rahali ,  Izzat Raheem

IPC: A61K31/675 ,  A61P31/12 ,  A61K45/00

Abstract: Compounds of Formula I: and pharmaceutically acceptable salts and co-crystals thereof 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：US10736908B2

公开(公告)日：2020-08-11

申请号：US16344233

申请日：2017-10-20

Applicant: Merck Sharp & Dohme Corp. ,  IDENIX Pharmaceuticals LLC

Inventor： Jean-Laurent Paparin ,  Houcine Rahali ,  Aurélien Salanson ,  Daniel Da Costa ,  David Dukhan ,  Timothy J. Hartingh ,  Izzat Raheem ,  John Schreier

IPC: C07D487/04 ,  A61K31/675 ,  A61P31/18 ,  C07F9/6561 ,  A61K31/427 ,  A61K31/536 ,  A61K31/4402 ,  A61K31/4725 ,  A61K31/52 ,  A61K31/496 ,  A61K45/06 ,  A61K31/513 ,  A61K31/665 ,  A61K31/5365 ,  A61K31/46 ,  A61K31/519

Abstract: Compounds of Formula (I): (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

Applicant: Merck Sharp & Dohme Corp. ,  Idenix Pharmaceuticals LLC

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

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

Abstract: 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：US10815264B2

公开(公告)日：2020-10-27

申请号：US15576607

申请日：2016-05-25

Applicant: IDENIX PHARMACEUTICALS LLC ,  SOUTHERN RESEARCH INSTITUTE ,  Cyril B. Dousson ,  David Dukhan ,  Jean-Laurent Paparin ,  Christophe C. Parsy

Inventor： Cyril B. Dousson ,  David Dukhan ,  Jean-Laurent Paparin ,  Christophe C. Parsy

IPC: C07D409/04 ,  C07H19/10 ,  C07H19/11 ,  A61P35/02

Abstract: The present application relates to novel nucleoside derivatives of formula (I) as claimed in claim 1, pharmaceutical compositions comprising the compounds, processes of preparation thereof, and methods of use thereof for treating cancer.