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Details

Stereochemistry ACHIRAL
Molecular Formula C25H18N4O3
Molecular Weight 422.4354
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of MK-0873

SMILES

[O-][N+]1=CC=CC(=C1)C#CC2=CC(=CC=C2)N3C=C(C(=O)NC4CC4)C(=O)C5=C3N=CC=C5

InChI

InChIKey=JJWKQXNHYDJXKF-UHFFFAOYSA-N
InChI=1S/C25H18N4O3/c30-23-21-7-2-12-26-24(21)29(16-22(23)25(31)27-19-10-11-19)20-6-1-4-17(14-20)8-9-18-5-3-13-28(32)15-18/h1-7,12-16,19H,10-11H2,(H,27,31)

HIDE SMILES / InChI

Description

MK-0873 is a novel selective phosphodiesterase-4 inhibitor, which has been in development for the treatment of chronic obstructive pulmonary disease (COPD). In preclinical studies, intravenous administration of MK-0873 produced potent, dose-dependent inhibition of antigen-induced bronchoconstriction in sensitized guinea pigs. MK-0873 protected against both the early- and late-phase bronchoconstrictor response to antigen challenge in Ascaris-sensitive sheep. In healthy volunteers, MK-0873 has been shown to be safe and generally well tolerated in single oral doses up to 6 mg and in multiple oral doses up to 4 mg for 28 days. The most commonly reported adverse events were similar to those reported in other studies with drugs in its class: i.e. headaches and gastrointestinal complaints.

Originator

Approval Year

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
MK-0873 2.5 mg tablets once daily for 12 weeks
Route of Administration: Oral