Macrolide derivatives having effect of potentiating antifungal activity

US7521428B2 · kind B2 · utility

Assignee

• The Kitasato Institute · JP

Inventors

• Satoshi Omura · Tokyo, JP
• Hiroshi Tomoda · Oshima, JP
• Toshiaki Sunazuka · Chiba, JP
• Masayoshi Arai · Paramythia, GR
• Tohru Nagamitsu · Yokohama, JP

Key dates

• Filing date: Oct 29, 2002
• Grant date: Apr 21, 2009
• Expiry date: Jun 29, 2025

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Macrolide derivatives having enhancing effect for activities of azole antifungal agents, acting at low concentration and within a short time against fungal infection and reducing the frequency of appearance of resistant microorganisms. One such substance is a compound represented by the formula [I]:wherein R1 is Ac, R2 and R3 are Ac, and R4 is Me; when R1 is H, R2 and R3 are Ac, and R4 is Me; when R1 is H, R2 and R3 are Ac, and R4 is H, when R1 Bzl, R2 and R3 are Bzl, and R4 is Me; when R1 is Ac, R2 and R3 are Pr, and R4 is Me; when R1 is Ac, R2 and R3 are Hex, and R4 is Me; when R1 is Ac, R2 and R3 are Bzl, and R4 is Me; when R1 is H, R2 and R3 are Pr, and R4 is Me; when R1 is H, R2 and R3 are Hex, and R4 is Me; when R1 is H, R2 and R3 are Bzl, and R4 is Me; when R1 is H, R2 is H, R3 is Bzl, and R4 is Me; when R1 is H, R2 and R3 are Hex, and R4 is H, or when R1 is H, R2 and R3 are Hex, and R4 is Et.