Immunosuppressive effects of pteridine derivatives

US7276506B2 · kind B2 · utility

Assignee

• 4 AZA Bioscience NV · BE

Inventors

• Mark Waer · Heverlee, BE
• Piet Herdewijn · Heverlee, BE
• Wolfgang Pfleiderer · Konstanz, DE

Key dates

• Filing date: Aug 29, 2003
• Grant date: Oct 2, 2007
• Expiry date: Nov 30, 2023

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D475/08
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention relates to a group of trisubstituted and tetrasubstituted pteridine derivatives, having the formula:wherein X represents an oxygen atom or a group with the formula NZ and wherein: R1 C1-7 alkyl or arylalkyl; Z is a group independently defined as R1 or the group NZ together with R1 is an optionally substituted heterocyclic group containing at least one nitrogen atom; R2 is amino or acylamino; R4 is an atom or a group selected from the group consisting of hydrogen; C1-7 alkyl; and C1-7 alkoxy; and R3 is an atom or a group selected from the group consisting of aryl optionally substituted with one or more substituents selected from the group consisting of halogen, C1-7 alkyl, and C1-7 alkoxy, their pharmaceutically acceptable salts, and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and being useful in the treatment in transplant rejection, certain inflammatory diseases, cardiovascular disorders, allergic conditions, disorders of the central nervous system and cell proliferative disorders.