申请人:FARMITALIA CARLO ERBA S.r.l.
公开号:EP0278603A1
公开(公告)日:1988-08-17
The invention relates to compounds having the general formula (I)
wherein
Z represents a C2-C6 alkylene chain or a -CH = CH-CH = group or an -E-CHR4-(CH2)p-group, in which p is zero, 1 or 2;
E represents an oxygen atom or a
group, wherein q is zero, 1 or 2; and R4 is hydrogen or C1-C3 alkyl;
R, represents C,-C6 alkyl, benzyl, pyridyl or phenyl, the phenyl being unsubstituted or substituted by one or two substituents chosen independently from halogen, trifluoromethyl, C1-C6 alkyl, C1-C6 alkoxy, nitro, amino, formylamino and C2-C8 alkanoylamino;
each of R2 and R3 is independently:
a) hydrogen, halogen or C,-C6 alkyl;
b) hydroxy, C,-C6 alkoxy or C3-C4 alkenyloxy; or
c) nitro, amino, formylamino or C2-C8 alkanoylamino;
and
W represents:
a') a
group,
wherein n is 1 or 2 and R represents hydrogen or C1-C6 alkyl;
or b') a
group, wherein Q represents hydrogen, carboxy, CONH2, C2-C7 alkoxycarbonyl or a
or a
group, wherein Ra represents hydrogen or C,-C2o alkyl and Rb represents C1-C20 alkyl or a -(CH2)m-R5 group, wherein m is zero, 1 or 2 and Rs is:
a") C5-C8 cycloalkyl;
b") pyridyl unsubstituted or substituted by one or two substituents chosen independently from halogen, C,-C6 alkyl and C1-C6 alkoxy; or
c") phenyl unsubstituted or substituted by one or two substituents independently chosen from halogen, CF3, C1-C6 alkyl, C1-C6 alkoxy, amino, nitro, formylamino, C2-C8 alkanoylamino, di(C1-C6 alkyl)amino, hydroxy, formyloxy and C2-C8 alkanoyloxy, and the pharmaceutically acceptable salts thereof, which possess immunomodulating activity and are useful e.g. in the treatment of neoplastic diseases and acute and chronic infections of both bacterial and viral origin in mammals.
本发明涉及具有通式(I)的化合物
其中
Z 代表 C2-C6 烯链或 -CH = CH-CH = 基团或 -E-CHR4-(CH2)p 基团,其中 p 为 0、1 或 2;
E 代表氧原子或
基团,其中 q 为 0、1 或 2;R4 为氢或 C1-C3 烷基;
R,代表 C,-C6 烷基、苄基、吡啶基或苯基,苯基未被取代或被一个或两个独立选自卤素、三氟甲基、C1-C6 烷基、C1-C6 烷氧基、硝基、氨基、甲酰氨基和 C2-C8 烷酰氨基的取代基取代;
R2 和 R3 各自独立:
a) 氢、卤素或 C,-C6烷基;
b) 羟基、C,-C6 烷氧基或 C3-C4 烯氧基;或
c) 硝基、氨基、甲酰氨基或 C2-C8 烷酰氨基;
和
W 代表
a')
基团、
其中 n 为 1 或 2,R 代表氢或 C1-C6 烷基;
或
其中 Q 代表氢、羧基、CONH2、C2-C7 烷氧羰基或 a
或
基团,其中 Ra 代表氢或 C,-C2o烷基,Rb 代表 C1-C20 烷基或-(CH2)m-R5 基团,其中 m 为零、1 或 2,Rs 为:
a") C5-C8 环烷基;
b") 未取代的吡啶基,或被一个或两个独立选自卤素、C,-C6 烷基和 C1-C6 烷氧基的取代基取代的吡啶基;或
c")未被取代或被一个或两个取代基取代的苯基,这些取代基独立地选自卤素、CF3、C1-C6 烷基、C1-C6 烷氧基、氨基、硝基、甲酰氨基、C2-C8 烷酰氨基、二(C1-C6 烷基)氨基、羟基、甲酰氧基和 C2-C8 烷酰氧基,以及它们的药学上可接受的盐,它们具有免疫调节活性,可用于治疗哺乳动物的肿瘤性疾病以及细菌和病毒引起的急性和慢性感染。