SUBSTITUTED 2-THIO-3,5-DICYANO-4-PHENYL-6-AMINOPYR

专利名称：SUBSTITUTED 2-THIO-3,5-DICYANO-4-PHENYL-6-AMINOPYRIDINES WITHADENOSINE RECEPTOR-BINDING ACTIVITYAND THEIR USE AS CARDIOVASCULARPREPARATIONS

发明人：ROSENTRETER, ULRICH, DR.,KRAEMER,

THOMAS, DR.,VAUPEL, ANDREA,DR.,HUEBSCH, WALTER, DR.,DIEDRICHS,NICOLE, DR.,KRAHN, THOMAS,DR.,DEMBOWSKY, KLAUS, DR.,STASCH,JOHANNES-PETER, DR.,SHIMADA,MITSUYUKI

申请号：EP05011426.3申请日：20020319公开号：EP15013A3公开日：20051109

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 offormula (I) and their salts, hydrates, salt hydrates and solvates are new. [Image] R 1, R2groups bonded to adjacent ring atoms, together completing a 5-7 membered saturatedor 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 orPh), 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 1-3of 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, Oand/or S heteroatom(s); R 51-5C alkyl (optionally substituted by OH or OT), cycloalkyl oraryl (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 areoptionally substituted by 1-3 of halo, CF 3, alkyl (optionally substituted by COOH orCOOT), OT, COOH, COOT, NH 2, NHT, NT 2, NO 2, CN or OH; and any ring N in Het isoptionally in N-oxide form)); R 6H, alkyl, (optionally substituted by OH or OT), cycloalkylor aryl (optionally substituted by 1-3 of halo, NO 2, OT, COOH, COOT, NHT or NT 2); andunless specified otherwise alkyl moieties have 1-8C, cycloalkyl moieties 3-7C and arylmoieties 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 OFACTION : Selective adenosine receptor ligand. (I) are selective ligands for one or moresubtypes 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, OCH2CH 2O or OCH 2CH(CH 2OH)O) are A1 receptor agonists and (I; R 1+ R 2= OCF 2O) areA1 receptor antagonists.

申请人：BAYER HEALTH CARE AKTIENGESELLSCHAFT

地址：51368 Leverkusen DE

国籍：DE

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