公开(公告)号：US20220096527A1

公开(公告)日：2022-03-31

申请号：US17542358

申请日：2021-12-03

Applicant: HOFFMANN-LA ROCHE INC.

Inventor： Xingchun HAN ,  Hassan JAVANBAKHT ,  Henrik MUELLER ,  Yongguang WANG ,  Song YANG

IPC: A61K31/7125 ,  C12Q1/6883 ,  C12N15/113 ,  C12Q1/70 ,  A61P31/14 ,  A61K31/4745 ,  A61K31/519 ,  C07K16/40 ,  A61P31/20

Abstract: The present invention relates to a method for identifying a compound that prevents, ameliorates and/or inhibits hepatitis B virus (HBV) infections. The compound (i) reduces the expression and/or activity of PAP associated domain containing 5 (PAPD5) and/or PAP associated domain containing 7 (PAPD7); and/or (ii) binds to PAPD5 and/or PAPD7 and inhibits 5 propagation of HBV; and is identified as a compound that prevents, ameliorates and/or inhibits HBV infections. An inhibitor of PAPD5 and/or PAPD7 for use in treating and/or preventing HBV infections; as well as a combined preparation comprising an inhibitor of PAPD5 and an inhibitor of PAPD7 for simultaneous or sequential use in the treatment or prevention of HBV infections is also provided. The present invention includes a 10-pharmaceutical composition for use in treatment and/or prevention of HBV infections, and a method for monitoring therapeutic success during treatment of HBV infections.

公开(公告)号：US20210061801A1

公开(公告)日：2021-03-04

申请号：US16958658

申请日：2018-12-21

Applicant: Hoffmann-La Roche Inc.

Inventor： Xingchun HAN ,  Min JIANG ,  Yongguang WANG ,  Song YANG

IPC: C07D471/04 ,  A61P31/20 ,  C07D455/06 ,  C07D519/00

Abstract: The present invention provides novel compounds having the general formula: wherein R1, R2, X, Y and A are as described herein, compositions including the compounds and methods of using the compounds.

公开(公告)号：US20190194768A1

公开(公告)日：2019-06-27

申请号：US16310765

申请日：2017-06-19

Applicant: HOFFMANN-LA ROCHE INC.

Inventor： Xingchun HAN ,  Hassan JAVANBAKHT ,  Henrik MUELLER ,  Yongguang WANG ,  Song YANG

IPC: C12Q1/70 ,  C07K16/40 ,  A61K31/4745 ,  A61K31/519 ,  C12N15/113 ,  A61P31/14 ,  C12Q1/6883

CPC classification number: C12Q1/706 ,  A61K31/4745 ,  A61K31/519 ,  A61P31/14 ,  C07K16/40 ,  C07K2317/732 ,  C12N15/113 ,  C12N15/1137 ,  C12N2310/14 ,  C12Q1/6883

Abstract: The present invention relates to a method for identifying a compound that prevents, ameliorates and/or inhibits a hepatitis B virus (HBV) infection, wherein a compound that (i) reduces the expression and/or activity of PAP associated domain containing 5 (PAPD5) and/or PAP associated domain containing 7 (PAPD7); and/or (ii) binds to PAPD5 and/or PAPD7 and inhibits 5 propagation of HBV; is identified as a compound that prevents, ameliorates and/or inhibits a HBV infection. The invention also provides for an inhibitor of PAPD5 and/or PAPD7 for use in treating and/or preventing a HBV infection; as well as a combined preparation comprising an inhibitor of PAPD5 and an inhibitor of PAPD7 for simultaneous or sequential use in the treatment or prevention of a HBV infection. Also comprised in the present invention is a 10 pharmaceutical composition for use in the treatment and/or prevention of a HBV infection, and a method for monitoring the therapeutic success during the treatment of a HBV infection.

公开(公告)号：US20240376073A1

公开(公告)日：2024-11-14

申请号：US18404194

申请日：2024-01-04

Applicant: Hoffmann-La Roche Inc.

Inventor： Sandra Marie Joseph GRALL-ULSEMER ,  Xingchun HAN ,  Joel Lukas KNECHT ,  Christian LERNER ,  Mingming LI ,  Yongqiang LIU ,  Patrizio MATTEI ,  Matthias NETTEKOVEN ,  Philippe PFLIEGER ,  Theodor STOLL ,  Jianhua WANG ,  Min WANG ,  Yongguang WANG ,  Song YANG ,  Chengang ZHOU

IPC: C07D401/12 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/427 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5355 ,  A61P31/04 ,  C07C53/06 ,  C07C53/10 ,  C07D233/90 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/14 ,  C07D487/04

Abstract: The invention provides novel heterocyclic compounds having the general formula (I), and pharmaceutically acceptable salts thereof, wherein R1 to R6 are as described herein: Frther provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.

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：US20180134705A1

公开(公告)日：2018-05-17

申请号：US15866954

申请日：2018-01-10

Applicant: Hoffmann-La Roche Inc.

Inventor： Zhanling CHENG ,  Xingchun HAN ,  Chungen LIANG ,  Song YANG

IPC: C07D471/04 ,  A61P31/20

CPC classification number: C07D471/04 ,  A61P31/20

Abstract: The invention provides novel compounds having the general formula: wherein R1 to R7 are as described herein, compositions including the compounds and methods of using the compounds.

公开(公告)号：US20230141403A1

公开(公告)日：2023-05-11

申请号：US18076383

申请日：2022-12-06

Applicant: Hoffmann-La Roche Inc.

Inventor： Zhanling CHENG ,  Xingchun HAN ,  Christian KRAMER ,  Holger KUEHNE ,  Christian LERNER ,  Mingming LI ,  Matthias NETTEKOVEN ,  Theodor STOLL ,  Min WANG ,  Song YANG

IPC: C07D487/04 ,  A61P31/04

CPC classification number: C07D487/04 ,  A61P31/04

Abstract: The invention provides novel imidazopyrazine derivatives having the general formula (I), or pharmaceutically acceptable salts thereof, wherein X, m, n, and R1 to R3 are as described herein:




Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.

公开(公告)号：US20230133845A1

公开(公告)日：2023-05-04

申请号：US17865192

申请日：2022-07-14

Applicant: Hoffmann-La Roche Inc.

Inventor： Mathis BRAENDLIN ,  Sandra Marie Joseph GRALL-ULSEMER ,  Xingchun HAN ,  Christian LERNER ,  Mingming LI ,  Yongqiang LIU ,  Sébastien SCHMITT ,  Jianhua WANG ,  Yongguang WANG ,  Min WANG ,  Song YANG ,  Chengang ZHOU

IPC: C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  A61P31/04

Abstract: The invention provides novel heterocyclic compounds having the general formula (I), and pharmaceutically acceptable salts thereof, wherein X, D, R1 to R4, and R6 to R10 are as described herein. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.

公开(公告)号：US20230012368A1

公开(公告)日：2023-01-12

申请号：US17349832

申请日：2021-06-16

Applicant: Hoffmann-La Roche Inc.

Inventor： Jean-Baptiste BLANC ,  Zhanling CHENG ,  Xingchun HAN ,  Nawaz KHAN ,  Christian KRAMER ,  Holger KUEHNE ,  Christian LERNER ,  Matthias NETTEKOVEN ,  Philippe PFLIEGER ,  Bernd PUELLMANN ,  Sebastien SCHMITT ,  Theodor STOLL ,  Jianhua WANG ,  Yongguang WANG ,  Song YANG

IPC: C07D487/04 ,  C07F9/6561 ,  C07D519/00 ,  C07H9/06 ,  A61P31/04

Abstract: Provided are novel imidazopyrazine derivatives having the general formula (I), wherein R1 to R11 are as described herein and pharmaceutically acceptable salts thereof.
Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and related diseases.

公开(公告)号：US20240140933A1

公开(公告)日：2024-05-02

申请号：US18514478

申请日：2023-11-20

Applicant: Hoffmann-La Roche Inc.

Inventor： Fabian DEY ,  Dong DING ,  Xingchun HAN ,  Chungen LIANG ,  Hongtao XU ,  Ge ZOU

IPC: C07D401/14 ,  C07D401/04

CPC classification number: C07D401/14 ,  C07D401/04

Abstract: The present invention relates to compounds of formula (I),






wherein R1 to R3, A1 to A3 and n are as described herein, and their pharmaceutically acceptable salt thereof, and compositions including the compounds and methods of using the compounds.