Watersoluble azole antifungals

US5707977A · kind A · utility

Assignee

• Janssen Pharmaceutica NA · BE

Inventors

• Jan Heeres · Vosselaar, BE
• Leo Jacobus Jozef Backx · Arendonk, BE
• Luc Alfons Leo Van der Eycken · Vosselaar, BE
• Frank Christopher Odds · Schilde, BE
• Jean Mesens · Wechelderzande, BE

Key dates

• Filing date: Jun 20, 1996
• Grant date: Jan 13, 1998
• Expiry date: Jun 20, 2016

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07F9/65586
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

A compound of formula (I), ##STR1## an acid or base addition salt thereof or a stereochemically isomeric form thereof, wherein A and B taken together form --N.dbd.CH--, --CH.dbd.N--, --CH.sub.2 --CH.sub.2, CH.dbd.CH--, --C(.dbd.O)--CH.sub.2 --, --CH.sub.2 --C(.dbd.O); D is a radical of formula ##STR2## L is a radical of formula ##STR3## Alk is a C.sub.1-4 alkanediyl radical; R.sup.1 is halo; R.sup.2 is hydrogen or halo; R.sup.3 is hydrogen, C.sub.1-6 alkyl, phenyl or halophenyl; R.sup.4 is hydrogen, C.sub.1-6 alkyl, phenyl or halophenyl; R.sup.5 is hydrogen or C.sub.1-6 alkyl; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxycarbonyl, or R.sup.5 and R.sup.6 taken together with the nitrogen atom to which they are attached form a heterocyclic ring. Active intermediates, compositions and methods of preparing compounds, compositions are described.