ΠΑΡΑΓΩΓΑ ΑΜΙΝΟΚΙΝΟΛΙΝΗΣ ΚΑΙ Η ΧΡΗΣΗ ΤΟΥΣ ΩΣ ΣΥΝΔΕΤΕΣ ΤΩΝ Α3 ΑΔΕΝΟΣΙΝΗΣ

• Main Authors: BOER KINGA, VARGANE SZEREDI JUDIT, FINET MICHEL, TIMARI GEZA, GERBER KATALIN, KAPUI ZOLTAN, ARANYI PETER, BATORI SANDOR, MIKUS ENDRE, URBAN-SZABO KATALIN
• Format: Patent
• Language: Greek
• Published: 19.06.2013
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Οι χημικές ενώσεις του γενικού χημικού τύπου (I), και τα άλατα τους, τα διαλύματα τους, τα ισομερή τους (ταυτομερή, δεσμότροπα, οπτικώς ενεργά ισομερή) καθώς επίσης και τα άλατα και τα διαλύματα, είναι ισχυροί συνδέτες του Α3 υποδοχέα αδενοσίνης, κατά προτίμηση ανταγωνιστές. 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 inhibitory constant value of (I) was 0.5-15 nM.