公开(公告)号：US20230248723A1

公开(公告)日：2023-08-10

申请号：US16769284

申请日：2018-12-04

申请人： Hoffmann-La Roche Inc.

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

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

CPC分类号： A61K31/4985 ,  A61P31/20 ,  G01N33/5067 ,  G01N33/5023

摘要： 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：US20220370447A1

公开(公告)日：2022-11-24

申请号：US17761521

申请日：2020-09-18

申请人： Hoffmann-La Roche Inc.

发明人： Qingyan BO ,  Valérie COSSON ,  Sheng FENG ,  Lu GAO ,  Yuyan JIN ,  Annabelle LEMENUEL ,  Miriam TRIYATNI ,  Xue ZHOU ,  Mingfen ZHU

IPC分类号： A61K31/506 ,  A61P31/20 ,  A61K31/522 ,  A61K31/675 ,  A61K31/7068 ,  A61K38/21 ,  A61K31/496

摘要： The present invention relates to method of treating HBV infection in a human patient, wherein the method comprises administration of a therapeutically effective amount of Compound (I), or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20210147850A1

公开(公告)日：2021-05-20

申请号：US17147797

申请日：2021-01-13

申请人： Hoffmann-La Roche Inc.

发明人： Marco BERRERA ,  Josephine FELBER ,  Jean-Christophe HOFLACK ,  Susanne KAMMLER ,  Tony KAM-THONG ,  Brian LEONARD ,  Lykke PEDERSEN ,  Philipp TROPBERGER ,  Miriam TRIYATNI ,  Daniel Jeremy TURLEY ,  Angelina WALLIER ,  Jitao David ZHANG

IPC分类号： C12N15/113 ,  A61P31/20

摘要： The present invention relates to a RTEL1 inhibitor for use in treatment of an HBV infection, in particular a chronic HBV infection. The invention in particular relates to the use of RTEL1 inhibitors for destabilizing cccDNA, such as HBV cccDNA. The invention also relates to antisense oligonucleotides which are complementary to RTEL1 and capable of reducing a RTEL1 mRNA. Also comprised in the present invention is a pharmaceutical composition and its use in the treatment and/or prevention of a HBV infection.