Delving into the Latest Updates on IRL-3461 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

endothelin receptor

Mechanism

endothelin receptor antagonists(Endothelin receptor antagonists)

Therapeutic Areas

Cardiovascular Diseases

Active Indication-

Inactive Indication

Cardiovascular Diseases

Originator Organization

Novartis Pharma AG

Active Organization-

Inactive Organization

Novartis Pharma AG

Drug Highest PhasePendingDiscovery

First Approval Date-

Regulation-

Structure

Molecular FormulaC31H40N4O6S

InChIKeyIFLIQLQVUMXNFU-IAPPQJPRSA-N

CAS Registry173189-01-0

IRL 3461, N-butanesulfonyl-[N-(3,5-dimethylbenzoyl)-N-methyl-3-[4-(5-+ ++isoxazolyl) -phenyl]-alanyl]-(L)-valineamide, a potent and bifunctional (ETA + ETB) [Ki(ETA) = 1.8 nM, Ki(ETB) = 1.2 nM] antagonist was discovered by structural modification of IRL 2500, an ETB selective antagonist. IRL 3461 was found to be stable on incubation with human, rat, mouse, and guinea pig plasmas.

01 Aug 1998·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

Stereoselective synthesis of a novel and bifunctional endothelin antagonist, IRL 3630

Q4 · MEDICINE

Article

Author: Kenji Hayakawa ; Toshiki Murata ; Yoko Yuumoto ; Ikushi Nakamura ; Junichi Sakaki

IRL 3630 (3), a single enantiomer of IRL 3461 with more potency was identified. Coupling reaction of the racemic fragment (1) with the chiral (L)-valinesulfonamide (2) under a biphasic solvent system (CH2Cl2-H2O) successfully led to the predominant formation of the desired isomer (3) with concomitant isomerization of 1. IRL 3630, N-butanesulfonyl-[N-(3,5-dimethylbenzoyl)-N-methyl-3-[4-(5-+ ++isoxazolyl) -phenyl]-(D)-alanyl]-(L)-valineamide, is a highly potent and bifunctional (ETA + ETB) antagonist [Ki(ETA) = 1.5 nM, Ki(ETB) = 1.2 nM].

100 Deals associated with IRL-3461

Login to view more data