2-Substituted-6-trifluoromethyl purine derivatives with adenosine-A3 antagonistic activity
AssigneeSolvay Pharmaceuticals GmbH
InventorsMelle Koch, Jacobus den Hartog, Gerrit-Jan Koomen, Martinus Wanner, Roelof Feenstra
Life of this patent
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Abstract
The present invention relates to 2-substituted-6-trifluoromethyl purine derivatives as selective adenosine antagonists, in particular adenosine-A3 receptor antagonists, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said purine derivatives. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.
Claims12
Compounds of the general formula (1):
- wherein:
- R1 represents —[X—(CH2)n]m-Y, in which formula X is either NH or oxygen, n is 0, 1, 2 or 3, m is 0 or 1, and Y is an optionally substituted 5- or 6-membered aromatic or non-aromatic ring, containing 0, 1 or 2 hetero-atoms selected from N, O and S, or R1 represents a nitro goup,
- R2 is hydrogen, C1-3-alkyl, ribose, —CH2—O—CO-O-t-butyl or aryl-(C1-3)alkyl,
- R3 represents hydrogen, halogen, NH2, —NH—(C1-6)alkyl, —N-di(C1-6)alkyl, —NH-cyclo(C3-8)alkyl, C2-4-alkenyl(hetero)aryl or C2-4-alkynyl(hetero)aryl, of which the hetero-atoms are selected from N, O, and S, and which (hetero)aryl groups may be optionally substituted, or R3 represents an optionally substituted 5- or 6-membered aromatic or non-aromatic ring, containing 0, 1 or 2 hetero-atoms selected from nitrogen, oxygen and sulphur,
- and tautomers, stereoisomers and salts thereof
A pharmaceutical composition comprising, in addition to a pharmaceutically acceptable carrier and/or at least one pharmaceutically acceptable auxiliary substance, a pharmacologically active amount of at least one compound of one of the claims, or a salt thereof, as an active ingredient.
The compound with formula (2a):
- being useful in the synthesis of compounds of the general formula (1).
Dependencies are inferred from the claim text.