申请人:Adir et Compagnie
公开号:US05877190A1
公开(公告)日:1999-03-02
A compound of formula (I): ##STR1## wherein: R.sub.1 represents unsubstituted or substituted cycloalkyl, phenyl, naphthyl, heterocyclic, alkyl or alkenyl, A represents a bond, oxygen, sulphur, a group ##STR2## a group ##STR3## or a group ##STR4## wherein Rc represents hydrogen, alkyl or cycloalkyl, R.sub.2 represents halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, cycloalkyl, formyl, carboxy, alkylcarbonyl, cycloalkylcarbonyl, alkoxycarbonyl, cycloalkyloxycarbonyl, optionally substituted carbamoyl, optionally substituted amino, formylamino, cyano, optionally substituted amidino, hydroxyaminomethyl, amide oxime, hydrazono, or a group selected from: ##STR5## wherein R.sub.21, R.sub.22 and R.sub.23 are as defined in the description, R.sub.3 represents hydrogen or alkyl, cycloalkyl or acyl, or ##STR6## together form the ring ##STR7## X is oxygen, sulphur, or NR", B is phenyl, Ra and Rb, which may be identical or different, each represents hydrogen, halogen, or alkyl, hydroxy, alkoxy, carboxy, polyhalogenoalkyl, cyano, nitro, alkoxycarbonyl, cycloalkyloxycarbonyl, amino, carbamoyl, sulfo, alkylsulfonyl, cycloalkylsulfonyl or aminosulfonyl, their isomers, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful as PDE IV inhibitors.
化合物的化学式(I):##STR1## 其中:R.sub.1代表未取代或取代的环烷基,苯基,萘基,杂环基,烷基或烯基,A代表键,氧,硫,群组##STR2##,群组##STR3##或群组##STR4##其中Rc代表氢,烷基或环烷基,R.sub.2代表卤素,取代或未取代的烷基,取代或未取代的烯基,取代或未取代的炔基,环烷基,甲酰,羧基,烷基羰基,环烷基羰基,烷氧羰基,环烷氧羰基,可选取代的氨基甲酰胺,可选取代的氨基,甲酰氨基,氰基,可选取代的氨基甲酰胺基,羟基氨甲基,酰胺肟,肼酮或从以下选择的群组:##STR5##其中R.sub.21,R.sub.22和R.sub.23如说明书中所定义,R.sub.3代表氢或烷基,环烷基或酰基,或##STR6##一起形成环##STR7##X为氧,硫或NR",B为苯基,Ra和Rb,可以相同或不同,每个代表氢,卤素,或烷基,羟基,烷氧基,羧基,多卤代烷基,氰基,硝基,烷氧羰基,环烷氧羰基,氨基,氨基甲酰胺基,磺酰,烷基磺酰,环烷基磺酰或氨基磺酰,它们的异构体以及与药学上可接受的酸或碱形成的加合物,以及含有它们的药物制剂,用作PDE IV抑制剂。