公开(公告)号：US10513534B2

公开(公告)日：2019-12-24

申请号：US14047862

申请日：2013-10-07

Applicant: IDENIX PHARMACEUTICALS LLC ,  Centre National De La Recherche Scientifique ,  UNIVERSITE DE MONTPELLIER

Inventor： Gilles Gosselin ,  Christophe Claude Parsy ,  Francois-Rene Alexandre ,  Houcine Rahali ,  Jean-Francois Griffon ,  Dominique Surleraux ,  Cyril B. Dousson ,  Claire Pierra ,  Adel M. Moussa ,  Benjamin Alexander Mayes ,  Alistair James Stewart

IPC: C07H19/06 ,  C07H19/073 ,  C07H19/10 ,  C07H19/11 ,  C07H19/16 ,  C07H19/173 ,  C07H19/20 ,  C07H19/213 ,  A61K31/7072 ,  A61K45/06 ,  A61K38/21 ,  A61K31/7076 ,  C07H19/14 ,  A61K31/7064 ,  C07H19/12 ,  A61K31/706 ,  A61K31/7068 ,  A61K31/708 ,  A61K31/403 ,  A61K31/497 ,  A61K31/7105 ,  C07H19/23

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′-chloro nucleosides according to Formula 2001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, Z and PD are as described herein.

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：US20170029456A1

公开(公告)日：2017-02-02

申请号：US15039176

申请日：2014-11-25

Applicant: IDENIX PHARMACEUTICALS LLC

Inventor： Cyril B. Dousson ,  David Dukhan ,  Christophe Claude Parsy

IPC: C07H19/207 ,  C07H19/10

CPC classification number: C07H19/207 ,  A61K31/7052 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/708 ,  C07H19/06 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20

Abstract: Provided herein are compounds, compositions and methods for the treatment of liver cancer such as hepatocellular carcinoma, cholangiocarcinoma, or biliary tract cancer. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-cancer agents. In certain embodiments, the compounds are nucleoside analogs of Formula I: (I); or a pharmaceutically acceptable salt thereof, wherein Base, Z1, Z2, Z3, Z4, V, W, X, Ar, R1 and R2 are as described herein.

Abstract translation: 本文提供了用于治疗肝癌如肝细胞癌，胆管癌或胆道癌的化合物，组合物和方法。 在某些实施方案中，公开了核苷衍生物的化合物和组合物，其可以单独施用或与其它抗癌剂组合施用。 在某些实施方案中，化合物是式I的核苷类似物：（I）; 或其药学上可接受的盐，其中基团，Z 1，Z 2，Z 3，Z 4，V，W，X，Ar，R 1和R 2如本文所述。

公开(公告)号：US10238680B2

公开(公告)日：2019-03-26

申请号：US14954815

申请日：2015-11-30

Applicant: IDENIX PHARMACEUTICALS LLC ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE ,  UNIVERSITE DE MONTPELLIER

Inventor： Benjamin Alexander Mayes ,  Adel M. Moussa ,  Cyril B. Dousson ,  Gilles Gosselin ,  Claire Pierra ,  David Dukhan

IPC: C07H19/10 ,  A61K31/7068 ,  A61K31/7072 ,  A61K45/06 ,  A61K9/00

Abstract: Provided herein are compounds, compositions, and methods for the treatment of viral infections, for example, 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 D-amino acid phosphoramidate halogeno pyrimidine nucleoside analog 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: PD, X, R1, R2, RA, and RB are as described herein.

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：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.

公开(公告)号：US10683321B2

公开(公告)日：2020-06-16

申请号：US15104706

申请日：2014-12-17

Applicant: IDENIX PHARMACEUTICALS LLC

Inventor： David Dukhan ,  Cyril B. Dousson ,  Adel M. Moussa ,  Benjamin Alexander Mayes ,  Alistair James Stewart

IPC: C07H19/207 ,  C07H19/10 ,  C07H19/16 ,  C07H19/06 ,  C07H19/20 ,  A61P31/14

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 4′-OR nucleosides of Formula I: or a pharmaceutically acceptable salt thereof, wherein Base, PD, R, Z1, Z2, Z3, and Z4 are as defined herein.

公开(公告)号：US10231986B2

公开(公告)日：2019-03-19

申请号：US14866759

申请日：2015-09-25

Applicant: Centre National De La Recherche Scientifique ,  Universite Montpellier 2 Sciences Et Techniques ,  Idenix Pharmaceuticals LLC

Inventor： David Dukhan ,  Christophe Claude Parsy ,  Gilles Gosselin ,  Jean-François Griffon ,  Guillaume Brandt ,  Cyril B. Dousson ,  Adel M. Moussa ,  Benjamin Alexander Mayes ,  Alistar James Stewart

IPC: C07H19/073 ,  C07H19/10 ,  C07H19/173 ,  C07H19/20 ,  A61K31/7072 ,  C07H17/02 ,  A61K31/7068 ,  A61K45/06 ,  A61K9/00 ,  A61K31/7076

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′-cyano, azido or amino nucleosides according to Formula 1001 or 2001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof, wherein Base, W, R1 and R2 are as described herein.

公开(公告)号：US10202411B2

公开(公告)日：2019-02-12

申请号：US15304506

申请日：2015-04-16

Applicant: IDENIX PHARMACEUTICALS LLC

Inventor： David Dukhan ,  Cyril B. Dousson ,  Gilles Gosselin ,  Jean-Laurent Paparin ,  Guillaume Brandt ,  Rachid Rahali ,  Aurelien Salanson ,  François-René Alexandre

IPC: A01N43/04 ,  A61K31/70 ,  C07H19/20 ,  C07H19/10 ,  C07H19/11 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K45/06 ,  A61K31/7064 ,  A61K31/708 ,  A61K31/7052 ,  A61K31/706

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 3′-substituted methyl or alkynyl nucleosides of Formula I: (I); or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein Base, PD, RA, RB1, RB2, RC and Z are as defined herein.

公开(公告)号：US10005779B2

公开(公告)日：2018-06-26

申请号：US14296122

申请日：2014-06-04

Applicant: Idenix Pharmaceuticals LLC

Inventor： David Dukhan ,  Gilles Gosselin ,  Cyril B. Dousson

IPC: C07D409/04 ,  C07D473/18 ,  A61K31/506 ,  A61K31/522 ,  A61K45/06 ,  C07H19/067

CPC classification number: C07D473/18 ,  A61K31/506 ,  A61K31/522 ,  A61K45/06 ,  C07D409/04 ,  C07H19/067

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 1′,4′-thio nucleoside 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 3001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof; wherein Base, RA, RB, W, X, Y, and Z are as described herein.