Delving into the Latest Updates on BMS-354326 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

Tryptase

Mechanism

Tryptase inhibitors

Therapeutic Areas-

Active Indication-

Inactive Indication-

Originator Organization

Bristol Myers Squibb Co.

Active Organization

Bristol Myers Squibb Co.

Inactive Organization-

Drug Highest PhaseDiscovery

First Approval Date-

Regulation-

Structure

Molecular FormulaC28H40N4O5

InChIKeyXVYFBYVSZOCXRJ-OMQKAAQBSA-N

CAS Registry708258-16-6

Azetidinones such as BMS-363131 (2) and BMS-363130 (3), which contain a guanidine group in the C-3 side chain were previously shown to be very potent inhibitors of human tryptase with high selectivity versus other serine proteases, including trypsin. In this letter, we describe the discovery of a number of potent azetidinone tryptase inhibitors in which the guanidine moiety at the ring C-3 position is replaced with primary or secondary amine or aminopyridine functionality. In particular, BMS-354326 (4) is a highly potent tryptase inhibitor (IC(50)=1.8 nM), which has excellent selectivity against trypsin and most other related serine proteases.

100 Deals associated with BMS-354326

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