Delving into the Latest Updates on RC-45 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

HBV core protein

Action

modulators

Mechanism

HBV core protein modulators

Therapeutic Areas

Infectious DiseasesDigestive System Disorders

Active Indication

Hepatitis B

Inactive Indication-

Originator Organization

Roche China Holding Ltd.

Active Organization

Roche China Holding Ltd.

Inactive Organization-

License Organization-

Drug Highest PhaseDiscovery

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC18H19ClFN5O3

InChIKeyLUMWJWQVLZISQA-NSHDSACASA-N

CAS Registry1967002-25-0

Hepatitis B Virus (HBV) core protein allosteric modulators (CpAMs) are an attractive class of potential anti-HBV therapeutic agents. Here we describe the efforts toward the discovery of a series of 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine (THPP) compounds as HBV CpAMs that effectively inhibit a broad range of nucleos(t)ide-resistant HBV variants. The lead compound 45 demonstrated inhibition of HBV DNA viral load in a HBV AAV mouse model by oral administration.

JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 4,5,6,7-tetrahydropyrazolo[1.5-a]pyrizine (THPP) derivatives as capsid assembly modulators for the inhibition of heptitis B virus (HBV)

Author: Mayweg, Alexander ; Shen, Fang ; Hu, Taishan ; Tian, Xiaojun ; Ottaviani, Giorgio ; Zhou, Xue ; Zhu, Wei ; Shen, Hong C. ; Han, Xingchun ; Liu, Haixia ; Zhang, Zhisen ; Yang, Guang ; Qiu, Hongxia ; Zhou, Yuan ; Young, John A. T. ; Kou, Buyu ; Xu, Zhiheng ; Zhou, Zheng

Here the efforts toward the discovery of a series of 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine (THPP) compounds as HBV CpAMs that effectively inhibited a broad range of nucleos(t)ide-resistant HBV variants.The lead compound (chlorofluorophenyl)oxomorpholinyldihydropyrazolopyrazine carboxamide demonstrated inhibition of HBV DNA viral load in a HBV AAV mouse model by oral administration.

100 Deals associated with RC-45

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