Aryloxy-, arylthio-, heteroaryloxy-, heteroarylthio-alkenylene derivatives of amines
申请人:FARMITALIA CARLO ERBA S.r.l.
公开号:EP0363782A1
公开(公告)日:1990-04-18
Aryloxy- and heteroaryloxy-alkylene derivatives of amines of formula
wherein each of A and B is a group of formula (i) to (iii):
wherein Y is -O-, -S- or -NR- in which R is hydrogen or C₁-C₆ alkyl; each of R₃, R₄, R₅ and R₆ is independently:
a) hydrogen, halogen, hydroxy, cyano or nitro;
b) C₁-C₆ alkyl unsubstituted or substituted by halogen,
c) C₁-C₆ alkoxy or C₁-C₆ alkylthio;
d) C₁-C₆ alkyl-sulfonyl;
e) a substituted amine group -NR₇R₈;
f) a -COR₁₂ group; or
g) two adjacent groups of R₃, R₄, R₅ and R₆, taken together, form a C₁-C₄ alkylenedioxy group;
each of R₁ and R₂ independently is hydrogen, C₃-C₆ alkynyl, C₃-C₆ alkenyl or C₁-C₆ alkyl unsubstituted or substituted by phenyl; or R₁ and R₂ taken together with the nitrogen atom to which they are linked, form a substituted or unsubstituted, saturated heterocyclic ring; and the pharmaceutically acceptable salts thereof; are active on the central nervous nervous system, in particular as antidepresssant, antiobesity antismoking and anti-alcoholabuse agents.
式胺的芳氧基和杂芳氧基烯烃衍生物
其中A和B各自为式(i)至(iii)的基团:
其中 Y 为-O-、-S-或-NR-,其中 R 为氢或 C₁-C₆ 烷基;R₃、R₄、R₅ 和 R₆ 各自独立:
a) 氢、卤素、羟基、氰基或硝基;
b) 未被卤素取代或取代的 C₁-C₆ 烷基、
c) C₁-C₆ 烷氧基或 C₁-C₆ 烷硫基;
d) C₁-C₆烷基磺酰基;
e) 取代的胺基团-NR₇R₈;
f) 一个-COR₁₂基团;或
g) 两个相邻的 R₃、R₄、R₅ 和 R₆ 基团共同形成 C₁-C₄ 烷二氧基;
R₁和R₂各自独立地为氢、C₃-C₆炔基、C₃-C₆烯基或未取代或被苯基取代的C₁-C₆烷基;或 R₁和R₂与它们相连的氮原子一起形成一个取代或未取代的饱和杂环;及其药学上可接受的盐;对中枢神经系统具有活性,特别是作为抗抑郁剂、抗肥胖剂、抗吸烟剂和抗酒精滥用剂。