Alkoxy- and alkylamino-carbonylalkylphospholipids, a process for their preparation and their use as medicaments
申请人:HOECHST-ROUSSEL
PHARMACEUTICALS INCORPORATED
公开号:EP0332129A2
公开(公告)日:1989-09-13
The present invention relates to compounds of the formula
wherein A¹ is a bivalent radical of the formula -CmH2m- wherein m is an integer having a value from 0 to 20, inclusive; A² is a bivalent radical of the formula -CpH2p- wherein p is an integer having a value from 2 to 6, inclusive; X is a bivalent radical of the formula -O- or -N(R)- wherein R is selected from the group consisting of hydrogen, alkyl having 1 to 6 carbon atoms, inclusive, and phenyl radical of the formula:
wherein a is an integer having a value from 0 to 3, inclusive, and Z is selected from the group consisting of alkyl radicals having 1 to 6 carbon atoms, inclusive, alkoxy radicals having 1 to 6 carbon atoms, inclusive, halogen, hydroxy, and trifluromethyl radicals, wherein for each value of a, Z may be the same or different; Y is
wherein R¹ is alkyl having 1 to 6 carbon atoms, inclusive and R² and R³ are independently alkyl radicals having 1 to 6 carbon atoms, inclusive, or, taken together with R¹ and the nitrogen atom to which they are attached form a group of the formula
wherein r is 0 or 1, W is oxygen, CH₂, sulfur or N(R⁴) wherein R⁴ is an alkyl radical having 1 to 6 carbon atoms, inclusive or aryl; and n is an integer having a value of 3 or 4 and the geometrical isomers, or optical antipodes thereof, and a process for their preparation.
The compounds have anti-inflammatory activity and can, therefore, be used as medicaments.
本发明涉及如下式的化合物
其中 A¹ 是式 -CmH2m- 的二价基,其中 m 是值为 0 至 20(包括 20)的整数;A² 是式 -CpH2p- 的二价基,其中 p 是值为 2 至 6(包括 2)的整数;X 是式 -O- 或 -N(R)- 的二价基,其中 R 选自由氢、具有 1 至 6 个碳原子的烷基(包括 1 个碳原子)和式中的苯基组成的组:
其中 a 是数值为 0 至 3(包括 3)的整数,Z 选自具有 1 至 6 个碳原子的烷基(包括 1 至 6 个碳原子)、具有 1 至 6 个碳原子的烷氧基(包括 1 至 6 个碳原子)、卤素、羟基和三氟甲基基组成的组,对于每个 a 值,Z 可以相同或不同; Y 是
其中 R¹ 是具有 1 至 6 个碳原子(包括 6 个)的烷基,R² 和 R³ 独立地是具有 1 至 6 个碳原子(包括 6 个)的烷基,或与 R¹ 和它们所连接的氮原子一起形成一个式中的基团。
其中 r 为 0 或 1,W 为氧、CH₂、硫或 N(R⁴),其中 R⁴ 为具有 1 至 6 个碳原子的烷基或芳基;n 为数值为 3 或 4 的整数,以及它们的几何异构体或光学反义体,以及它们的制备方法。
这些化合物具有抗炎活性,因此可用作药物。