SUBSTITUTED 2-THIO-3,5-DICYANO-4-PHENYL-6-AMINOPYRIDINES WITH ADENOSINE RECEPTOR-BINDING ACTIVITY AND THEIR USE AS CARDIOVASCULAR PREPARATIONS

摘要

6-Amino-4-(cyclic-substituted phenyl)-3,5-dicyano-2-thio-pyridine derivatives (I) are new. 6-Amino-4-(cyclic-substituted phenyl)-3,5-dicyano-2-thio-pyridine derivatives of formula (I) and their salts, hydrates, salt hydrates and solvates are new. [Image] R 1, R 2groups bonded to adjacent ring atoms, together completing a 5-7 membered saturated or partially unsaturated ring, optionally containing 1 or 2 N, O and/or S heteroatom(s) and optionally substituted by T (where itself can be optionally substituted by OH, T or Ph), CN, halo or =O; T : 1-4C alkyl; R 3alkyl (optionally substituted by 1-3 of OH, OT, cycloalkyl, 2-4C alkenyl, 2-4C alkynyl, halo or aryloxy), aryl (optionally substituted by 1-3 of halo, NO 2, OT, COOH, COOT, NHT or NT 2), alkoxy (optionally substituted by halo, OT, 3-6C cycloalkyl, 2-4C alkenyl, 2-4C aryl, Het, aryloxy, halo, CN, COOT, NH 2, NHT or NT 2), H, OH, halo, NO 2, CN or NHCOR 5; Het : 5-10 membered heteroaryl containing 1-3 N, O and/or S heteroatom(s); R 51-5C alkyl (optionally substituted by OH or OT), cycloalkyl or aryl (optionally substituted by 1-3 of halo, NO 2, OT, COOH, COOH, NHT or NT 2); R 42-4C alkenyl, cycloalkyl or alkyl (optionally substituted by 1-3 of halo, CF 3, SCF 3, cycloalkyl, OH, CONHR 6, OT, COOT, 2-4C alkenyl, aryl or Het (where aryl and Het are optionally substituted by 1-3 of halo, CF 3, alkyl (optionally substituted by COOH or COOT), OT, COOH, COOT, NH 2, NHT, NT 2, NO 2, CN or OH; and any ring N in Het is optionally in N-oxide form)); R 6H, alkyl, (optionally substituted by OH or OT), cycloalkyl or aryl (optionally substituted by 1-3 of halo, NO 2, OT, COOH, COOT, NHT or NT 2); and unless specified otherwise alkyl moieties have 1-8C, cycloalkyl moieties 3-7C and aryl moieties 6-10C. An independent claim is also included for the preparation of (I). ACTIVITY : Cardiant; Vasotropic; Uropathic; Cytostatic; Antiinflammatory; Neuroprotective; Analgesic; Hepatotropic; Antidiabetic; Hypotensive; Antiarteriosclerotic; Antiarrhythmic; Antianginal; Thrombolytic; Anticoagulant; Cerebroprotective; Antiasthmatic; Dermatological; Nootropic; Antiparkinsonian; Nephrotropic; Vulnerary. MECHANISM OF ACTION : Selective adenosine receptor ligand. (I) are selective ligands for one or more subtypes of the adenosine receptor, specifically the A1, A2a and/or A2b receptors, particularly the A1 and/or A2b receptors. In general (I; R 1+ R 2= OCH 2O, OCF 2O, OCH 2CH 2O or OCH 2CH(CH 2OH)O) are A1 receptor agonists and (I; R 1+ R 2= OCF 2O) are A1 receptor antagonists.