PYRIDOPYRIMIDINES FOR TREATING INFLAMMATORY AND OTHER DISEASES

摘要

The present invention relates to the use of pyridopyrimidine derivatives having the general formula (I) wherein X represents =NH, =N-Acyl, =O, or =S; R¹ represents -NR³R⁴, -SR³, -SO-R³, -SO₂-R³, -OR³; R², R³, and R⁴ are independently of each other hydrogen, -(CH₂)_nPh*, heteroaryl, C₃-C₇-cycloalkyl, C₁-C₆-alkyl, C₁-C₆-alkanoyl, C₂-C₆-alkenyl, C₂-C₆-alkynyl; wherein the cycloalkyl, alkyl, alkanoyl, alkenyl, alkynyl residues can optionally substituted by one or more of the following groups: -NR⁵R⁶, phenyl, substituted phenyl, thioalkyl, alkyloxy, hydroxy, carboxy, halogen, cycloalkyl; R⁵ and R⁶ are independently of each other hydrogen, (CH₂)_nPh*, heteroaryl, C₃-C₇-cycloalkyl, C₁-C₆-alkyl, C₁-C₆-alkanoyl, C₂-C₆-alkenyl, C₂-C₆-alkynyl; R⁵ and R⁶ can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ph* represents phenyl or substituted phenyl; n is 0, 1, 2, or 3; R⁴ can optionally be -CO-R³, -CO-OR³, -SO₂-R³, -SO₂-NR⁵R⁶, -CO-NR⁵R⁶, -CS-NR⁵R⁶, -C(=NH)-R³, -C(=NH)-NR⁵R⁶; R³ and R⁴ can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ar represents phenyl, substituted phenyl, or heteroaryl; and pharmaceutically acceptable salts thereof for prophylaxis and/or treatment of inflammatory diseases, neurodegenerative disorders, immunological diseases, neuroimmunological diseases, autoimmune diseases, diabetes, transplant rejection, infective diseases, prion diseases, cardiovascular diseases and disorders.