| 摘要 |
Aminotriazolone derivatives (I) their enantiomers, diastereoisomers, and salts with acids and bases are new. Aminotriazolone derivatives (I) their enantiomers, diastereoisomers, and salts with acids and bases: R1 and R2 = H, 1-6C alkyl, 1-6C alkenyl, 1-6C alkynyl, aryl, heteroaryl, 3-8C cycloalkyl or heterocycloalkyl (all optionally substituted by OH, cycloalkyl, aryl, heteroaryl, heterocycloalkyl or halo); aryl = phenyl, naphthyl, biphenyl, dihydronaphthyl or tetrahydronaphthyl; R3 = H, 1-6C alkyl, 1-6C alkenyl, 1-6C alkynyl, aryl, heteroaryl ( mono- or bicyclic with 0-4 heteroatoms), 3-8C cycloalkyl or heterocycloalkyl (mono- or bicyclic with 0-4 heteroatoms) (all optionally substituted by OH, cycloalkyl, aryl, heteroaryl, heterocycloalkyl or halo); R4 = a group of formula (II); W = a bond or 1-6C alkylene; B = 3-10 membered mono- or polycyclic group (may be aromatic (optionally substituted by alkyl, alkoxy, halogen, OH, perhaloalkyl, NO2, amino (optionally substituted, acyl, aminocarbonyl, acylamino, alkoxycarbonyl, formyl, carboxy, sulfo, sulfino, sulfamoyl, nitrile, aminoalkyl, thioalkyl, or hydroxyalkyl) and may contain 1-3 hetero atoms (O, N, S) and contains at least one oxo), -COR or hydroxy group (may contain one or more unsaturations and one or more substituents (alkyl, alkoxy, OH, aryl, aralkyl, halo)); R = H, 1-6C alkyl, alkoxy, amino, alkylamino or dialkylamino; R5 = H or 1-6C alkyl; A = -A2-, -A1-A2-, -A2-A1- or -A1-A2-A1-; A1 = 1-6C alkylene, 1-6C alkenylene or 1-6C alkynylene; A2 = phenylene, naphthylene, 3-8C cycloalkylene, heteroarylene or heterocyclalkylene (all of which may be substituted by OH, cycloalkyl, aryl, heteroaryl, heterocycloalkyl or halo); V = a bond, -CH2-, -CO-, -CS-, -CH2NH- or -CH=N-; or V+R3 with -A- + -NR4- = -A-CH=N-R4. Provided that only one of R1 and R2 may be H.
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