Dolastatin 15 derivatives with carbonyl and heterocyclic functionalities at the C-terminus

US5965537A · kind A · utility

Assignee

• BASF SE

Inventors

• Kurt Ritter · Heidelberg, DE
• Wilhelm Amberg · Ludwigshafen, DE
• Teresa Barlozzari · Wellesley, US
• Andreas Haupt · Ludwigshafen, DE
• Bernd Janssen · Ludwigshafen, DE
• Andreas Kling · Mannheim, DE

Key dates

• Filing date: Mar 10, 1997
• Grant date: Oct 12, 1999
• Expiry date: Mar 10, 2017

Classification

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

Abstract

The present invention relates to novel peptides useful as anti-cancer agents. The compounds of the invention are of Formula I, EQU A-B-D-E-F-G (I) A, B, D, and E are .alpha.-amino acid residues. In one embodiment, F is an azacycloalkanecarboxylic acid residue. In this embodiment, G is a monovalent radical, for example, a hydrogen atom, an alkyl group, an aryl group, or a heteroaryl group. In another embodiment, F is an azacycloalkyl group and G is a heteroaryl group connected to F by a carbon-carbon bond. In another embodiment, the invention includes a method for treating cancer in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound of Formula I in a pharmaceutically acceptable composition.