公开(公告)号：US20190177326A1

公开(公告)日：2019-06-13

申请号：US16212121

申请日：2018-12-06

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

Inventor： Francois-Rene Alexandre ,  Rachid Rahali ,  Izzat Raheem ,  Christophe Parsy

IPC: C07D473/40 ,  A61K31/675 ,  A61K31/7072 ,  A61K31/522 ,  A61K31/52 ,  A61K31/513 ,  C07F9/6561 ,  C07D473/32 ,  C07D239/54 ,  C07D239/47

Abstract: The present invention is directed carbocyclic nucleoside reverse transcriptase inhibitors compounds of Formula I and their use in the inhibition of HIV reverse transcriptase, 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 and/or ARC.

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：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：US20180155385A1

公开(公告)日：2018-06-07

申请号：US15576948

申请日：2016-05-23

Applicant: IDENIX PHARMACEUTICALS LLC

Inventor： Cyril B. DOUSSON ,  David DUKHAN ,  Christophe Claude PARSY

IPC: C07H19/11 ,  A61P35/00

Abstract: The present invention relates to novel nucleoside derivatives, pharmaceutical compositions comprising the compounds, processes of preparation thereof, and methods of use thereof for treating cancer.

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：US20170066795A1

公开(公告)日：2017-03-09

申请号：US15123124

申请日：2015-03-05

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

Inventor： John Zoltan Sulliva-Bolyai ,  Benjamin Alexander Mayes ,  Douglas Lytle Mayers ,  Xiao-Jian Zhou ,  Adel M. Moussa ,  Alistair James Stewart ,  Sindhura Ganga ,  Clinton Scott Shultz ,  Alfred Lee

IPC: C07H19/10 ,  A61K9/48 ,  A61K31/7072 ,  A61K9/20

CPC classification number: C07H19/10 ,  A61K9/20 ,  A61K9/2018 ,  A61K9/2077 ,  A61K9/48 ,  A61K9/4858 ,  A61K31/7072 ,  C07B2200/13

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 solid forms of Compound I: (Compound I)

Abstract translation: 本文提供了用于治疗黄病毒科感染（包括HCV感染）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病毒剂组合施用。 在某些实施方案中，化合物是化合物I的固体形式：（化合物I）

公开(公告)号：US09192621B2

公开(公告)日：2015-11-24

申请号：US14038617

申请日：2013-09-26

Applicant: IDENIX PHARMACEUTICALS LLC

Inventor： Benjamin Alexander Mayes ,  Adel M. Moussa

IPC: C07H19/10 ,  C07H19/20 ,  A61K31/7076 ,  C07H17/02 ,  A61K45/06 ,  C07H19/16 ,  A61K31/403 ,  A61K31/497 ,  A61K31/7056 ,  A61K31/708 ,  A61K38/21

CPC classification number: A61K31/7076 ,  A61K31/403 ,  A61K31/497 ,  A61K31/7056 ,  A61K31/708 ,  A61K38/212 ,  A61K45/06 ,  C07H17/02 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20 ,  A61K2300/00

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, provided herein are compounds according to Formula 1001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein Base, Y, Z, A, RC and RD are as described herein.

Abstract translation: 本文提供了用于治疗黄病毒科感染（包括HCV感染）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病毒剂组合施用。 在某些实施方案中，本文提供了根据式1001的化合物：或其药学上可接受的盐，溶剂化物，立体异构体形式，互变异构形式或其多晶型物，其中碱，Y，Z，A，RC和RD如本文所述。

公开(公告)号：US11040975B2

公开(公告)日：2021-06-22

申请号：US16212121

申请日：2018-12-06

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

Inventor： Francois-Rene Alexandre ,  Rachid Rahali ,  Izzat Raheem ,  Christophe Parsy

IPC: C07D473/40 ,  C07D473/32 ,  C07D239/47 ,  C07D239/54 ,  A61K31/675 ,  A61K31/7072 ,  A61K31/522 ,  A61K31/513 ,  C07F9/6561 ,  A61K31/52 ,  C07F9/6512

Abstract: The present invention is directed carbocyclic nucleoside reverse transcriptase inhibitors compounds of Formula I and their use in the inhibition of HIV reverse transcriptase, 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 and/or ARC.

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：US10525072B2

公开(公告)日：2020-01-07

申请号：US14972009

申请日：2015-12-16

Applicant: Idenix Pharmaceuticals LLC ,  Universita Degli Studi Di Cagliari

Inventor： Jean-Pierre Sommadossi ,  Paolo La Colla ,  David N. Standring ,  Vadim Bichko ,  Lin Qu

IPC: C12Q1/70 ,  A61K31/7072 ,  A61K31/7052 ,  A61K38/21 ,  A61K45/06 ,  C07H19/06 ,  C07H19/16 ,  C07K14/005 ,  C12Q1/04 ,  C12Q1/18

Abstract: The present invention discloses a method for the treatment of Flaviviridae infection that includes the administration of a 2′-branched nucleoside, or a pharmaceutically acceptable prodrug and/or salt thereof, to a human in need of therapy in combination or alternation with a drug that directly or indirectly induces a mutation in the viral genome at a location other than a mutation of a nucleotide that results in a change from serine to a different amino acid in the highly conserved consensus sequence, XRXSGXXXT (SEQ ID NO: 63), of domain B of the RNA polymerase region, or is associated with such a mutation. The invention also includes a method to detect a mutant strain of Flaviviridae and a method for its treatment.