Di-fluoro azepane HBV capsid assembly modulators.


Journal

Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377

Informations de publication

Date de publication:
15 08 2023
Historique:
received: 25 04 2023
revised: 22 05 2023
accepted: 22 05 2023
medline: 2 8 2023
pubmed: 30 5 2023
entrez: 29 5 2023
Statut: ppublish

Résumé

The protein that forms the inner shell of the HBV virus, known as the capsid core protein, plays a crucial role in allowing chronic HBV infections to persist. Studies have shown that disrupting the assembly of the capsid can effectively combat the virus, and small molecule drugs that target the HBV capsid assembly modulator (CAM) process have been successful in clinical trials. Herein is described a distinct series of di-fluoro azepane CAMs with exceptional potency, pharmacokinetic, and solubility properties.

Identifiants

pubmed: 37247697
pii: S0960-894X(23)00228-7
doi: 10.1016/j.bmcl.2023.129350
pii:
doi:

Substances chimiques

Antiviral Agents 0
Capsid Proteins 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

129350

Informations de copyright

Copyright © 2023 Elsevier Ltd. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Auteurs

Lindsey G DeRatt (LG)

Janssen Research and Development, 1400 McKean Road, Spring House, PA 19477, United States. Electronic address: lderatt@its.jnj.com.

Bart Stoops (B)

Janssen Pharmaceutica, NV Turnhoutseweg 30, 2340 Beerse, Belgium.

Paul Shaffer (P)

Janssen Research and Development, 1400 McKean Road, Spring House, PA 19477, United States.

Angela M Lam (AM)

Janssen Research and Development, 1400 McKean Road, Spring House, PA 19477, United States.

Christine Espiritu (C)

Janssen Research and Development, 1400 McKean Road, Spring House, PA 19477, United States.

Robert Vogel (R)

Janssen Research and Development, 1400 McKean Road, Spring House, PA 19477, United States.

Vincent Lau (V)

Janssen Research and Development, 1400 McKean Road, Spring House, PA 19477, United States.

Osvaldo A Flores (OA)

Janssen Research and Development, 1400 McKean Road, Spring House, PA 19477, United States.

Scott D Kuduk (SD)

Janssen Research and Development, 1400 McKean Road, Spring House, PA 19477, United States. Electronic address: skuduk@its.jnj.com.

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Classifications MeSH