NOUVEAUX DERIVES DE L'INDOLE, LEUR PREPARATION A TITRE DE MEDICAMENTS, COMPOSITIONS PHARMACEUTIQUES ET NOTAMMENT COMME INHIBITEURS DE KDR
2-(Pyrazolyl or indazolyl)-indole derivatives (I), in all possible racemic, enantiomeric or diasteroisomeric forms, their addition salts with (in)organic acids or inorganic bases are new. 2-(pyrazolyl or indazolyl)-indole derivatives of formula (I), in all possible racemic, enantiomeric or diasteroi...
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Zusammenfassung: | 2-(Pyrazolyl or indazolyl)-indole derivatives (I), in all possible racemic, enantiomeric or diasteroisomeric forms, their addition salts with (in)organic acids or inorganic bases are new. 2-(pyrazolyl or indazolyl)-indole derivatives of formula (I), in all possible racemic, enantiomeric or diasteroisomeric forms, their addition salts with (in)organic acids or inorganic bases are new. [Image] R 1>pyrazolyl or indazolyl, optionally substituted by one or more of halo, hydroxy, nitro, cyano, R 4>, OR4, SR 4>, COR 4>, OCOR 4>, COOR 4>, COOH (optionally as salt), NR 5>COR 4>, NR 5>COOR 4>, S(O) nR 4>, S(O) nOR 4>, NR5-SO 2R 4>, OS(O) nR 4>, NY 1>Y 2>, CONY 1>Y 2>, OCONY 1>Y 2>, NR5CONY 1>Y 2>, S(O) nNY 1>Y 2>or optionally substituted thienyl; R 2>, R 3>hydrogen, halo, hydroxy, nitro, cyano, R 4>, OR 4>, COR 4>, OCOR 4>, COOR 4>, COOH, NR 5>COR 4>, NR5COOR 4>, S(O) nR 4>, S(O) nOR 4>, NR 5>-SO 2R 4>, NY 1>Y 2>, CONY 1>Y 2>, NR 5>CONY 1>Y 2>, S(O) nNY 1>Y 2>or OCONY 1>Y 2>; or R 2>+ R 3>optionally substituted 4-6 membered ring optionally containing one or more heteroatoms O,N or S; n : 0-2; R 4>alkyl, alk-NY 1>Y 2>, alk-CONY 1>Y 2>, alkenyl, alkynyl, cycloalkyl, (hetero)aryl, (hetero)cycloalkylalkyl, heteroarylalkyl or aralkyl, all optionally substituted; R 5>hydrogen, alkyl, alkenyl, (hetero)cycloalkyl, (hetero)aryl, aralkyl, (hetero)cycloalkylalkyl, or heteroarylalkyl, all optionally substituted; Y 1>, Y 2>hydrogen, alkyl, alkenyl, (hetero)cycloalkyl, heterocycloalkylalkyl, (hetero)aryl, (hetero)aralkyl or (hetero)arylcarboxy, (all optionally substituted by one or more of halo, hydroxy, alkoxy, alkyl (optionally substituted by hydroxy or carboxy), cyano, nitro, trifluoromethyl, trifluoromethoxy, carboxy (optionally as salt or optionally substituted alkyl ester), Nalk-CO-alk, NHCO-alk, S(O) n-alk, NHS(O) n-alkyl, NHCO-NY 3>Y 4>, CONY 3>Y 4>, S(O) nNY 3>Y 4>, aryl, arylalkoxy, aryloxy, aryloxyalkyl, heteroaryl or heterocycloalkyl (both optionally substituted by one or more T 1>)); or NY 1>Y 2>optionally substituted ring; Y 3>, Y 4>hydrogen, aryl or alkyl (optionally substituted by one or more T 1>); T 1>halo, alkyl, carboxy (optionally as salt or ester) or amino (optionally substituted by 1 or 2 alkyl or by one phenyl (optionally substituted by a dioxol residue)); and alk : 1-6C alkyl. ACTIVITY : Cytostatic; Antiallergic; Antiasthmatic; Anticoagulant; Thrombolytic; Ophthalmological; Antipsoriatic; Antiasthmatic; Antirheumatic; Antidiabetic; Antiarteriosclerotic; A |
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