公开(公告)号：US20230248723A1

公开(公告)日：2023-08-10

申请号：US16769284

申请日：2018-12-04

Applicant: Hoffmann-La Roche Inc.

Inventor： Jitao David ZHANG ,  Xingchun HAN ,  Song YANG ,  Miriam TRIYATNI ,  Brian LEONARD ,  Angelina WALLIER ,  Josephine SCHMALER ,  Daniel TURLEY ,  Philipp TROPBERGER ,  Samuel CROSET

IPC: A61K31/4985 ,  A61P31/20 ,  G01N33/50

CPC classification number: A61K31/4985 ,  A61P31/20 ,  G01N33/5067 ,  G01N33/5023

Abstract: The present invention relates to novel therapeutic agents against hepatitis B virus (HBV) infection, particularly inhibitors of viral covalently closed circular DNA (cccDNA) which is the key barrier for HBV cure. Accordingly, the invention provides the pyrrolo[2,3-b]pyrazine compounds of formula (I), as described and defined herein, for use in the treatment of HBV infection. The compounds provided herein are highly potent against HBV infection and enable an improved therapy, particularly of chronic HBV infection and HBV rebound. The present invention further relates to a novel screening assay for the identification of therapeutic agents against HBV infection, particularly cccDNA inhibitors, which is performed in hepatocyte-like cells that recapitulate the complete HBV life cycle following infection with patient-derived HBV.

公开(公告)号：US20220251556A1

公开(公告)日：2022-08-11

申请号：US17590754

申请日：2022-02-01

Applicant: HOFFMANN-LA ROCHE INC.

Inventor： Erik FUNDER ,  Natascha HRUSCHKA ,  Susanne KAMMLER ,  Erich KOLLER ,  Brian LEONARD ,  Souphalone LUANGSAY ,  Susanne MOHR ,  Tobias NILSSON ,  Søren OTTOSEN ,  Lykke PEDERSEN ,  Søren V. RASMUSSEN ,  Steffen SCHMIDT ,  Sabine SEWING ,  Daniel TURLEY ,  Johanna Marie WALTHER

IPC: C12N15/113 ,  A61K31/7088 ,  A61P31/20

Abstract: Enhanced antisense oligonucleotides targeting Regulator of telomere elongation helicase 1 (RTEL1), leading to modulation of the expression of RTEL1 or modulation of RTEL1 activity are provided. This disclosure relates to the use of enhanced antisense oligonucleotides targeting RTEL1 for use in treating and/or preventing a hepatitis B virus (HBV) infection, in particular a chronic HBV infection. This disclosure further relates to the use of the enhanced antisense oligonucleotides targeting RTEL1 for destabilizing cccDNA, such as HBV cccDNA. A pharmaceutical composition and its use in the treatment and/or prevention of a HBV infection is also described.