Water soluble azoles as broad-spectrum antifungals

US6384030B1 · kind B1 · utility

Inventors

• Lieven Meerpoel · Beerse, BE
• Leo Jacobus Jozef Backx · Arendonk, BE
• Louis Jozef Elisabeth Van Der Veken · Vosselaar, BE
• Jan Heeres · Vosselaar, BE
• Frank Christopher Odds · Schilde, BE

Key dates

• Filing date: Nov 9, 2000
• Grant date: May 7, 2002
• Expiry date: Nov 9, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D249/12
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention concerns novel compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein L represent a radical of formula wherein each Alk independently represents an optionally substituted C1-6alkanediyl; is 1, 2 or 3; Y is O, S or NR2; R1 represents hydrogen, aryl, Het1, or an optionally substituted C1-6alkyl; each R2 independently represents hydrogen or C1-6alkyl; or in case R1 and R2 are attached to the same nitrogen atom, they may be taken together to form a heterocyclic radical; or they may be taken together to form an azido radical; each R3 independently represents hydrogen, hydroxy or C1-4alkyloxy; aryl represents phenyl, naphthalenyl, 1,2,3,4-tetrahydro-naphthalenyl, indenyl or indanyl; each of said aryl groups may optionally be substituted; Het1 represents an optionally substituted monocyclic or bicyclic heterocyclic radical; Het2 is the same as Het1 and may also be piperazinyl, homopiperazinyl, 1,4-dioxanyl, morpholinyl, thiomorpholinyl; R6 represents hydrogen or C1-4alkyl; R7 represents hydrogen or C1-4alkyl; or R6 and R7 taken together form a bivalent radical of formula —N&box…