Delving into the Latest Updates on TR-14531 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

TR 14531

Target

α4β1

Action

antagonists

Mechanism

α4β1 antagonists(Integrin alpha-4/beta-1 antagonists)

Therapeutic Areas

Other Diseases

Active Indication-

Inactive Indication

Inflammation

Originator Organization

Mitsubishi Tanabe Pharma Corp.

Active Organization-

Inactive Organization

Mitsubishi Tanabe Pharma Corp.

License Organization-

Drug Highest PhasePendingPhase 1

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC34H34N2O7S

InChIKeyYQQUBIXUFFJEJC-FGUUHEIUSA-N

CAS Registry676124-97-3

Author: Kinney, William A. ; Hornby, Pamela J. ; de Garavilla, Lawrence ; Prouty, Stephen M. ; Andrade-Gordon, Patricia ; Dyatkin, Alexey B. ; Fisher, M. Carolyn ; Santulli, Rosemary J. ; Abraham, William M. ; He, Wei ; Damiano, Bruce P. ; Kimball, Edward S. ; Kontoyianni, Maria ; Hoekstra, William J. ; Maryanoff, Bruce E. ; Hlasta, Dennis J.

Lawrence de Garavilla (Drug Discovery, Johnson & Johnson Pharmaceutical Research & Development, L.L.C., Spring House, Pennsylvania, USA) is added as the tenth author.

01 Feb 2004·Bioorganic & medicinal chemistry letters

Aza-bicyclic amino acid sulfonamides as α4β1/α4β7 integrin antagonists

Article

Author: Kinney, William A. ; Hornby, Pamela J. ; de Garavilla, Lawrence ; Prouty, Stephen M. ; Andrade-Gordon, Patricia ; Dyatkin, Alexey B. ; Fisher, M. Carolyn ; Abraham, William M. ; Santulli, Rosemary J. ; He, Wei ; Damiano, Bruce P. ; Kimball, Edward S. ; Kontoyianni, Maria ; Hoekstra, William J. ; Maryanoff, Bruce E. ; Hlasta, Dennis J.

The design, synthesis, and biological activity of novel alpha(4)beta(1) and alpha(4)beta(7) integrin antagonists, containing a bridged azabicyclic nucleus, are reported. Conformational analysis of targets containing an azabicyclo[2.2.2]octane carboxylic acid and known integrin antagonists indicated that this azabicycle would be a suitable molecular scaffold. Variation of substituents on the pendant arylsulfonamide and phenylalanine groups resulted in potent alpha(4)beta(1)-selective and dual alpha(4)beta(1)/alpha(4)beta(7) antagonists. Potent compounds 11i, 11h, and 14 were effective in the antigen-sensitized sheep model of asthma.

100 Deals associated with TR-14531

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