申请人:CIBA-GEIGY AG
公开号:EP0783887A2
公开(公告)日:1997-07-16
A composition suitable for topical administration in treatment of a hyperproliferative skin disease which is a gel comprising (A) a compound of formula
wherein A1 and A2 are each independently of the other hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl, acyl, lower alkylsulfonyl or arylsulfonyl; or wherein A1 and A2 together form unsubstituted or lower alkyl- or hydroxy-substituted lower alkylene; Ar1 and Ar2 are each independently of the other aryl, heteroaryl or unsubstituted or substituted cycloalkyl; the group -C(=X)- is -C(=O)-, -C(=S)-, -CH2- or -C(=CR1R2)- wherein R1 and R2 are each independently of the other hydrogen or lower alkyl; and R is hydrogen, lower alkyl, aryl-lower alkyl, aryl, amino, hydroxy or lower alkoxy; with the proviso that R is other than phenyl when A1 and A2 are hydrogen, Ar1 and Ar2 are phenyl and the group -C(=X)- is -C(=O)-; or a pharmaceutically acceptable salt thereof when a salt-forming group is present; (B)a C1-C4 alkyl monoether of diethyleneglycol, (C) a gelling agent and (D) a solvent which is miscible with (B).
一种适用于局部用药治疗过度增生性皮肤病的组合物,它是一种凝胶,包含 (A) 式中的化合物
其中A1和A2各自独立地为氢、低级烷基、低级烯基、低级炔基、芳基、酰基、低级烷基磺酰基或芳基磺酰基;或其中A1和A2共同形成未取代的或低级烷基或羟基取代的低级亚烷基;Ar1和Ar2各自独立地为芳基、杂芳基或未取代或取代的环烷基;基团-C(=X)-为-C(=O)-、-C(=S)-、-CH2-或-C(=CR1R2)-,其中R1和R2各自独立地为氢或低级烷基;和 R 是氢、低级烷基、芳基-低级烷基、芳基、氨基、羟基或低级烷氧基;但当 A1 和 A2 是氢、Ar1 和 Ar2 是苯基且基团-C(=X)-是-C(=O)-时,R 不是苯基;或当存在成盐基团时,是其药学上可接受的盐;(B)二乙二醇的 C1-C4 烷基单醚,(C)胶凝剂和(D)与(B)混溶的溶剂。