Acyl derivatives of azolones

US5637592A · kind A · utility

Assignee

• Janssen Pharmaceutica NA · BE

Inventors

• Jan Heeres · Vosselaar, BE
• Raymond A. Stokbroekx · Beerse, BE
• Joseph H. Mostmans · Ekeren, BE
• Louis Jozef Elisabeth Van Der Veken · Vosselaar, BE

Key dates

• Filing date: May 23, 1995
• Grant date: Jun 10, 1997
• Expiry date: May 23, 2015

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D409/12
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The invention is concerned with the compounds having the formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y is CH or N; R.sup.1, R.sup.2 and R.sup.3 each independently are hydrogen or C.sub.1-4 alkyl; R.sup.4 and R.sup.5 each independently are hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, hydroxy, trifiuoromethyl, trifiuoromethyloxy or difluoromethyloxy; R.sup.6 is hydrogen; or R.sup.6 is phenyl optionally substituted with halo; pyridinyl; furanyl; thienyl; 3-chloro-benzo[b]thien-2-yl; trifiuoromethyl; C.sub.1-4 alkyloxycarbonyl; dihalophenylcyclopropanyl; C.sub.3-6 cycloalkyl; adamantyl; C.sub.2-6 alkenyl optionally substituted with halophenyl; or C.sub.1-4 alkyl optionally substituted with halo, phenyl, halophenyl, dihalophenyl, phenyloxy, piperidinyl, pyrrolidinyl, piperazinyl, C.sub.1-4 alkylpiperazinyl, C.sub.1-4 alkylcarbonylpiperazinyl, C.sub.1-4 alkyloxycarbonylpiperazinyl, phthalimino, amino, mono- or di(C.sub.1-20)alkylamino or C.sub.3-6 cycloalkylamino; Z is C.dbd.O or CHOH; and ##STR2## is a radical of formula ##STR3## Compositions comprising said compounds, processes for preparing the same a…