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    • 1. 发明申请
    • MONO-ACYLATED O-PHENYLENDIAMINES DERIVATIVES AND THEIR USE AGAINST CANCER
    • 单酚O-邻苯二甲酸衍生物及其对癌症的使用
    • WO2004069803A3
    • 2004-11-18
    • PCT/EP2004001044
    • 2004-02-05
    • HOFFMANN LA ROCHE
    • FERTIG GEORGHERTING FRANKKUBBIES MANFREDLIMBERG ANJAREIFF ULRIKEWEIDNER MICHAEL
    • A61K31/381A61K31/44C07C233/80C07D213/82C07D213/90C07D333/38
    • 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, R , R 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 -NR R , or alternatively R is hydrogen, and R 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 R is hydroxy, Ar is not thiophen-2,5-diyl; and R and R independently from each other represent hydrogen or C1-6-alkyl, or wherein R and R 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.
    • 本发明的目的是式(A)的新的单酰化邻苯基苯胺衍生物,其中Ar是噻吩-2,5-二基,吡啶-2,5-二基,吡啶-5,2-二基,吡啶-2, 6-二基,吡啶-2,4-二基或1,4-亚苯基,R 1,R 2彼此独立地表示氢,C 1-12 - 烷基,C 2-12 - 烯基,C 2-12 - 炔基,C 3-12 - 环烷基,烷基,烯基,炔基和环烷基任选被羟基,卤素,C 3-12 - 环烷基,烷氧基,烷基硫烷基,酰氧基,烷氧基羰基,酰基,C 1-6 - NH-C(O) - ,C 1-6 - 烷基-C(O)NH-或-NR 3 R 4,或者R 1是氢,R 2是羟基,烷氧基, C 2 -C 12 - 烯氧基或苯氧基,该苯氧基任选被甲基,甲氧基,卤素,硝基,氰基,三氟甲基,乙烯基或-C(O)-O-CH 3取代,条件是如果R 2是羟基,则Ar 不是噻吩-2,5-二基; R 3和R 4彼此独立地表示氢或C 1-6 - 烷基,或其中R 3和R 4与它们所连接的氮原子一起形成环,其中 环被氧基单取代,并且该环可以含有另外的杂原子及其药学上可接受的盐,以及制备这些化合物的方法,含有这些化合物的药物组合物及其在制备用于治疗疾病的药物中的用途 作为癌症。