New 6-(4-carboxy-phenyl)-dihydropyridazinone esters or amides, having erythropoietin sensitizing and erythropoiesis stimulating activity, useful for treating anemia

摘要

6-(4-Carboxy-phenyl)-dihydropyridazinone ester or amide derivatives (I) and their tautomers or salts are new. Pyridazinone derivatives of formula (I) (including their tautomers and salts) are new. A, D, E, G = H, alkyl, OH, CF3, halo or alkoxy; R1, R2 = H or alkyl; R3 = OR4 or NR5R6; R4 = (i) 1-8C alkyl or cycloalkyl (both optionally substituted (os) by OH, alkoxy, cycloalkyl or aryl (itself os by 1 or 2 of halo, alkoxy, OH or CF3); (ii) 1-8C alkyl (os by NR7R8); or (iii) aryl (os by 1 or 2 of halo, alkyl, alkoxy or OH); R5 = H or 1-4C alkyl; R6 = (i) cycloalkyl or 4,5,6,7-tetrahydro-2-benzothienyl; (ii) aryl or Het, both os by 1-3 of halo, CF3, OH, alkoxy, COOH, alkoxycarbonyl, alkyl, SO2NR9R10 or -(CO)a-NR11R12; or (iii) 1-8C alkyl (os by 1 or 2 of halo, CF3, OH, alkoxy, COOH, alkoxycarbonyl, or aryl or Het (both os by 1-3 of alkyl, halo, alkoxy, alkoxycarbonyl, CF3 or CONH2)); or NR5R6 = 1,2,3,4-tetrahydroisoquinolin-2-yl, 1,2,3,4-tetrahydroquinolin-1-yl, morpholino, imidazol-1-yl or piperidino; R7, R8 = H, alkyl or benzyl; a = 0 or 1; R9 - R12 = H or alkyl; unless specified otherwise alkyl moieties have 1-6C, cycloalkyl moieties 3-8C and aryl moieties 6-10C. An Independent claim is also included for the preparation of (I).