Drug intelligence / Profile preview

1-[1'-(3-phenylacryloyl)spiro[1-benzofuran-3,4'-piperidin]-5-yl]methanamine

Development stage
Preclinical
Lead developer
Johnson & Johnson
Modality
Small Molecules
Administration
Oral
01

Overview

This compound is a synthetic small molecule belonging to the class of cinnamic acid derivatives. It was developed as part of a series of spirocyclic piperidine amide derivatives and has been studied as a potent and selective inhibitor of human mast cell tryptase. Tryptase is an enzyme implicated in allergic and inflammatory responses. The compound demonstrated oral efficacy in animal models of airway inflammation (asthma models in sheep and guinea pig). Its mechanism involves binding to the active site of tryptase, exploiting a hydrophobic pocket within the enzyme structure[7]. The research and early development were conducted by Johnson & Johnson Pharmaceutical Research & Development.

Other names
(2E)-1-[5-(aminomethyl)-2H-spiro[1-benzofuran-3,4'-piperidine]-1'-yl]-3-phenylprop-2-en-1-one1-(1'-(3-phenylacryloyl)spiro(1-benzofuran-3,4'-piperidin)-5-yl)methanamine(2E)-1-(5-(aminomethyl)-2H-spiro(1-benzofuran-3,4'-piperidine)-1'-yl)-3-phenylprop-2-en-1-one
02

Targets

TPSB2 (Mast Cell Tryptase)

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