Diazepinone HBV capsid assembly modulators

Scott D Kuduk; Lindsey G DeRatt; Bart Stoops; Paul Shaffer; Angela M Lam; Christine Espiritu; Robert Vogel; Vincent Lau; Osvaldo A Flores; George D Hartman

doi:10.1016/j.bmcl.2022.128823

Diazepinone HBV capsid assembly modulators

Bioorg Med Chem Lett. 2022 Sep 15:72:128823. doi: 10.1016/j.bmcl.2022.128823. Epub 2022 May 27.

Authors

Affiliations

¹ Janssen Research and Development, 1400 McKean Road, Spring House, PA 19477, United States. Electronic address: skuduk@its.jnj.com.
² Janssen Research and Development, 1400 McKean Road, Spring House, PA 19477, United States.
³ Janssen Pharmaceutica, NV Turnhoutseweg 30, 2340 Beerse, Belgium.

PMID: 35644301
DOI: 10.1016/j.bmcl.2022.128823

Abstract

The HBV capsid core protein serves a number of important functions in the viral life cycle enabling chronic HBV infection to persist, and therefore is a promising drug target. Interfering with capsid assembly has shown efficacy in clinical trials with small molecule capsid assembly modulators (CAMs). Herein is described the further optimization of a progressive series of diazepinone HBV CAMs.

Keywords: Capsid; Diazepinone; HBV.

MeSH terms

Antiviral Agents / metabolism
Capsid Proteins / metabolism
Capsid* / metabolism
Hepatitis B virus* / metabolism
Virus Assembly

Substances

Antiviral Agents
Capsid Proteins