Aminoquinoline derivatives and their use as adenosine A3 ligands

Aminoquinoline derivatives (I) and their salts, solvates, isomers (tautomers, desmotrops, optically active isomers) and their salts or solvates are new. Aminoquinoline derivatives of formula (I) and their salts, solvates, isomers (tautomers, desmotrops, optically active isomers) and their salts or solvates are new. [Image] R 1>H or 1-4C alkyl; R 2>H or 1-4C alkyl; R 3>H, 1-4C alkyl, 3-6C cycloalkyl, phenyl, thienyl or furyl (optionally substituted by 1-4C alkyl, 1-4C alkoxy or halo), 5-6 membered heteroaromatic ring containing 1-3N, 5 membered heteroaromatic ring containing O, N or S (optionally substituted with 1-4C alkyl, 1-4C alkoxy or halo); R 4>, R 5>H, 3-6C cycloalkyl or 1-4C alkyl (optionally containing amino group substituted by 1-2 1-4C alkyl, OH, carboxy or alkyl group substituted with 1-4C alkyl), benzyl, -SO 2OH or 1-4C acyl; NR 4>R 5>a group of formula (a); R 7>, R 8>H, 1-4C alkyl or 3-6C cycloalkyl; R 6>H, 1-4C alkyl, phenyl, benzyl, thienyl or furyl (optionally substituted by methylenedioxy or 1 or more 1-4C alkyl, 1-4C alkoxy, hydroxy, trifluoromethyl, cyano or halo), or 5 or 6 membered heteroaromatic ring (containing either 1-3 N, 1 N and 1 O or 1 N and 1 S, and optionally substituted by 1 or more 1-4C alkyl, 1-4C alkoxy or halo); X : CH 2, NH, NR 9>, S, O, sulfo or sulfoxy; R 9>1-4C alkyl or 3-6C cycloalkyl; Z : O, S, CHR 1> 0> or NR 1>; R 1> 0>H, 1-4C alkyl or 3-6C cycloalkyl; R 1> 1>H, 1-4C alkyl, 3-6C cycloalkyl, SO 2OH or 1-4C acyl; n : 0-2; m, o : 1-3; and p, r : 0-1. Provided that either: (1) R 4> and R 5> are H, 3-6C cycloalkyl or 1-4C alkyl optionally contains amino group substituted 1-2 1-4C alkyl, OH, carboxy or alkyl group substituted with 1-4C alkyl; (2) R 4> is H, 1-4C alkyl or benzyl and R 5> is H, -SO 2OH or 1-4C acyl; or (3) NR 4>R 5> is (a). [Image] Independent claims are also included for the following: (1) preparation of (I); and (2) new compounds of formulae (II''), (III''), (IV''), (V''), (VI''), (VII''), (VIII'') and (XIII''). [Image] ACTIVITY : Cardiant; Nephrotropic; Respiratory-Gen.; CNS-Gen.; Cytostatic; Ophthalmological; Antiinflammatory; Antiasthmatic; Vasotropic; Antidepressant; Antiarrhythmic; Antiparkinsonian; Nootropic; Antiallergic; Dermatological; Antiarthritic; Immunosuppressive; Gastrointestinal-Gen.; Anabolic; Hypertensive; Antipsoriatic; Antirheumatic; Neuroprotective; Antidiabetic. MECHANISM OF ACTION : Adenosine A3 ligands. (I) were tested for adenosine A3 ligand activity in HEK-293 cells. The inhib