申请人:OTSUKA PHARMACEUTICAL FACTORY, INC.
公开号:EP0275312A1
公开(公告)日:1988-07-27
Thiazole derivatives represented by general formula (I) and salts thereof, wherein R' and R2 may be the same or different and each represents C1-C6 alkyl group, R3 represents a hydrogen atom or a C1-C6 alkyl group, or R2 and R3 may be bound to each other to form -(CH2)4-, R4 and R6 may be the same or different and each represents a hydrogen atom, a C1-C20 alkyl group, a phenyl group, a phenyithio group, a C1-C6 alkylthio group, a C1-C6 alkylthio-C1-C6 alkyl group, a halogen atom, a nitro group, a C1-C6 alkoxycarbonyl-C2-C6 alkenyl group, a carboxy-C2-C6 alkenyl group, a carbazoyl group, a carboxyl group, a carboxy-C1-C6 alkyl group, a C1-C6 alkoxy- carbonyl-C1-C6 alkyl group, a C1-C6 alkoxycarbonyl group, a piperidinocarbonyl group, an N.N-di(C1-C6 alkyl)aminocarbonyl group, an N-phenylaminocarbonyl group or a hydroxy-C1-C6 alkyl group, and A represents an imino group, an oxygen atom, a sulfur atom, a sulfinyl group, a sulfonyl group or a C1-Ce alkylene group, provided that the case wherein R3 represents a hydrogen atom, R4 represents a C1-C6 alkyl group or a phenyl group. R5 represents a hydrogen atom, and A represents an imino group is excluded. These compounds have a particularly excellent effect of inhibiting neoplasia of blood vessel, and are useful for treating malignant tumors, retinitis, psoriasis, etc.
通式(I)代表的噻唑衍生物及其盐,其中R'和R2可以相同或不同,各自代表C1-C6烷基,R3代表氢原子或C1-C6烷基,或R2和R3可以相互结合形成-(CH2)4-,R4和R6可以相同或不同,各自代表氢原子、C1-C20烷基、苯基、苯硫基、C1-C6烷硫基、C1-C6烷硫基-C1-C6烷基、卤素原子、硝基、噻唑衍生物及其盐、C1-C6烷硫基、C1-C6烷硫基-C1-C6烷基、卤素原子、硝基、C1-C6烷氧基羰基-C2-C6烯基、羧基-C2-C6烯基、咔唑基、羧基、C1-C6烷氧基羰基-C1-C6烷基、C1-C6烷氧基羰基、哌啶羰基、N.N-二(C1-C6 烷基)氨基羰基、N-苯氨基羰基或羟基-C1-C6 烷基,且 A 代表亚氨基、氧原子、硫原子、亚砜基、磺酰基或 C1-Ce 亚烷基,条件是 R3 代表氢原子,R4 代表 C1-C6 烷基或苯基。R5代表氢原子,A代表亚氨基的情况除外。这些化合物在抑制血管瘤化方面具有特别出色的效果,可用于治疗恶性肿瘤、视网膜炎、牛皮癣等。