Delving into the Latest Updates on RO-0506997 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

A4I antagonist

Target

CD49d

Action

antagonists

Mechanism

CD49d antagonists(Integrin alpha-4 antagonists)

Therapeutic Areas

Immune System DiseasesNervous System DiseasesOther Diseases

Active Indication-

Inactive Indication

Multiple Sclerosis

Originator Organization

F. Hoffmann-La Roche Ltd.

Active Organization-

Inactive Organization

F. Hoffmann-La Roche Ltd.

License Organization-

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC25H25F2N3O5

InChIKeyWUWFMJLSHFBJBN-IBGZPJMESA-N

CAS Registry343851-28-5

N-Acyl 4-(5-pyrimidine-2,4-dionyl)phenylalanine derivatives of type 4 were designed to replace the 2,6-dichlorobenzoylamine portion of compound 1 in order to identify novel compounds with improved potency against α4-integrins. Several derivatives were identified as very potent dual-acting α4-integrin, α4β1 and α4β7 antagonists. Investigation of a limited number of prodrug esters led to the discovery of the ethyl ester prodrug 42, which demonstrated good intestinal fluid stability and good permeability. Despite low solubility, 42 gave acceptable blood levels of 30 when dosed orally in non-human primates. Additionally, 42 had an overall excellent profile and was selected for clinical trials. Investigation of N-acyl 4-(5-pyrimidine-2,4-dionyl)phenylalanine derivatives led to the discovery of several very potent dual-acting α4-integrin antagonists. Ethyl ester prodrug 42 advanced to human clinical trials based on the excellent intestinal fluid stability, good permeability and superior efficacy in non-human primates.

100 Deals associated with RO-0506997

Login to view more data

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Multiple Sclerosis	Phase 2	United Kingdom	F. Hoffmann-La Roche Ltd.	12 Jan 2005
Multiple Sclerosis	Phase 2	Spain	F. Hoffmann-La Roche Ltd.	12 Jan 2005
Multiple Sclerosis	Phase 2	Czechia	F. Hoffmann-La Roche Ltd.	12 Jan 2005
Multiple Sclerosis	Phase 2	Germany	F. Hoffmann-La Roche Ltd.	12 Jan 2005