Macrolides

US6124453A · kind A · utility

Assignee

• Novartis AG · CH

Inventors

• Theodor Fehr · Dornach, CH
• Lukas Oberer · Tenniken, CH
• Valérie Quesniaux Ryffel · Saint-Denis-en-Val, FR
• Jean-Jacques Sanglier · Oberwil, CH
• Walter Schuler · Weil am Rhein, DE

Key dates

• Filing date: Dec 24, 1996
• Grant date: Sep 26, 2000
• Expiry date: Dec 24, 2016

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A novel class of macrolides in which PA1 i) positions 2 to 6 inclusive of the macrocyclic ring are provided by a piperidazinyl carboxylic acid residue; and/or PA1 ii) positions 7 to 9 inclusive of the macrocyclic ring are provided by an aromatic .alpha.-amino acid residue; and/or PA1 iii) positions 10 to 12 inclusive of the macrocyclic ring are provided by an aliphatic .alpha.-amino acid residue, preferably comprising two, or especially all three of the characteristic structural features i), ii) and iii), more especially a compound of formula IX ##STR1## is provided having immunosuppressant and antinflammatory properties and protected and ring-open forms thereof.