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    • 31. 发明公开
    • NEW MONO-ACYLATED O-PHENYLENDIAMINES DERIVATIVES
    • 使用单苯乙烯邻苯二酚衍生物
    • EP1592667A2
    • 2005-11-09
    • EP04708323.3
    • 2004-02-05
    • F. HOFFMANN-LA ROCHE AG
    • FERTIG, GeorgHERTING, FrankKUBBIES, ManfredLIMBERG, AnjaREIFF, UlrikeWEIDNER, Michael
    • C07D213/90A61K31/381A61K31/44
    • C07D213/82C07C233/80C07C2601/02C07D333/38
    • Objects of the present invention are new mono-acylated o-phenylendiamines derivatives of formula (A) wherein Ar is thiophen-2,5-diyl, pyridine-2,5-diyl, pyridine-5,2-diyl, pyridine-2,6-diyl, pyridine-2,4-diyl or 1,4-phenylene, R1, R2 independently from each other represent hydrogen, C1-12-alkyl, C2-12-alkenyl, C2-12-alkynyl, C3-12-cycloalkyl, the alkyl, alkenyl, alkynyl and cycloalkyl groups being optionally mono or multiple substituted by hydroxy, halogen, C3-12-cycloalkyl, alkoxy, alkylsulfanyl, acyloxy, alkoxycarbonyl, acyl, C1-6-alkyl-NH-C(O)-, C1-6-alkyl-C(O)NH- or -NR3R4, or alternatively R1 is hydrogen, and R2 is hydroxyl, alkoxy, C2-C12-alkenyloxy or phenoxy, which phenoxy group is optionally substituted with methyl, methoxy, halogen, nitro, cyano, trifluoromethyl, ethenyl or -C(O)-O-CH3, provided that if R2 is hydroxy, Ar is not thiophen-2,5-diyl; and R3 and R4 independently from each other represent hydrogen or C1-6-alkyl, or wherein R3 and R4 together with the nitrogen-atom to which they are attached form a ring, which ring is monosubstituted by oxo and which ring may contain a further heteroatom, and pharmaceutically acceptable salts thereof, as well as processes for the manufacturing of these compounds, pharmaceutical compositions containing such compounds and their use in the manufacture of drugs for the treatment of diseases such as cancer.
    • 式A的单酰化邻苯二胺衍生物:其可用于治疗由组蛋白脱乙酰酶抑制如癌症介导的疾病。