申请人:Ohmeda Pharmaceutical Products Division Inc.
公开号:EP0328830A1
公开(公告)日:1989-08-23
A compound of the formula
and/or a pharmaceutically acceptable acid addition salt thereof, in which formula:
R1 is an unsaturated heterocyclic ring of 5 cyclic member atoms, including 1 to 4 nitrogen atoms, and 0 to 1 sulphur or oxygen atoms, said heterocyclic ring being unsubstituted or substituted wherein the or each substituent is selected from lower alkyl, lower alkoxy and lower alkoxy lower alkyl groups;
R2 is a substituted or unsustituted phenyl group in which the or each substituent is a halogen atom;
R3 is a lower alkyl or a lower alkoxy lower alkyl group; and
L is a lower alkyl group; a lower alkoxy group; a thienyl lower alkyl group; a lower alkoxy lower alkyl group; a thiazolyl lower alkyl group, unsubstituted, or substituted in the 4-position (of the thiazolylmoiety) with a lower alkyl group; a (4,5-di-hydro-5-oxo-1 H-tetrazol-1-yl) lower alkyl group, unsubstituted, or substituted in the 4-position (of the tetrazolyl moiety) with a lower alkyl group; a pyrazolyl lower alkyl group; a pyridinyl lower alkyl group; an oxophenyl lower alkyl group; a 2,4-(1 H,3H)-pyridinedionyl group, disusbstituted in the
3-position with lower alkyl groups; or a phenyl lower alkyl group, unsubstituted or substituted (in the phenyl moiety) with at least one substituent selected from lower alkyl groups; lower alkoxy groups, halgenated lower alkyl groups, and halogen atoms, has analgesic and anaesthetic properties and may be used in analagesic and anaesthetic compositions.
式化合物
和/或其药学上可接受的酸加成盐,其中式
R1 是由 5 个环状成员原子组成的不饱和杂环,包括 1 至 4 个氮原子和 0 至 1 个硫或氧原子,所述杂环是未取代或取代的,其中或每个取代基选自低级烷基、低级烷氧基和低级烷氧基低级烷基;
R2 是取代或未取代的苯基,其中或每个取代基是卤素原子;
R3 是低级烷基或低级烷氧基低级烷基;以及
L 是低级烷基;低级烷氧基;噻吩基低级烷基;低级烷氧基低级烷基;未取代的噻唑基低级烷基,或在(噻唑基)4 位被低级烷基取代的噻唑基低级烷基;未被取代的(4,5-二氢-5-氧代-1 H-四唑-1-基)低级烷基,或在(四唑基)的 4 位被低级烷基取代的(4,5-二氢-5-氧代-1 H-四唑-1-基)
或苯基低级烷基,未被取代或(在苯基中)被至少一个选自低级烷基、低级烷氧基、卤代低级烷基和卤素原子的取代基取代,具有镇痛和麻醉特性,可用于镇痛和麻醉组合物中。