申请人:SMITH KLINE & FRENCH LABORATORIES
LIMITED
公开号:EP0403198A2
公开(公告)日:1990-12-19
Polymers of structure:
in which,
R¹ and R² are each C₁₋₄alkyl, or one is C₁₋₄alkyl and the other is -(CH₂)nR³;
n is 2 to 12;R3 is NR4R5 or
R6R7R8 X
R⁴ and R⁵ are the same or different and are each hydrogen, C₁₋₄alkyl, C(=NH)NH₂, or together with the nitrogen atom to which they are attached form a saturated or unsaturated ring optionally containing one or more further heteroatoms.
R⁶, R⁷ and R⁸ are the same or different and are each hydrogen, C₁₋₄alkyl or one of R⁶, R⁷ and R⁸ is C₁₋₄alkyl and the other two together with the nitrogen atom to which they are attached form a saturated or unsaturated ring optionally containing one or more further heteroatoms;
a, b and c are numbers which indicate the relative molar percentages of the units present in said polymer, (b) being from 1 to 10 molar percent, and (c) being from 30 to 98 molar percent; and
X⊖ is a counter ion,
processes for their preparation, pharmaceutical compositions containing them and their use in therapy as cholesterol lowering agents.
结构聚合物
其中
R¹ 和 R² 分别是 C₁₋₄烷基,或其中一个是 C₁₋₄烷基,另一个是-(CH₂)nR³;
n 是 2 至 12;R3 是 NR4R5 或
R6R7R8 X
R⁴ 和 R⁵ 可以相同或不同,各自为氢、C₁₋₄烷基、C(=NH)NH₂,或与所连接的氮原子一起形成饱和或不饱和环,可选地含有一个或多个杂原子。
R⁶、R⁷ 和 R⁸ 可以相同或不同,并且各自为氢、C₁₋₄烷基或 R⁶ 中的一个、R⁷ 和 R⁸ 是 C₁₋₄烷基,另外两个与它们所连接的氮原子一起形成一个饱和或不饱和环,可选择含有一个或多个杂原子;
a、b 和 c 是表示所述聚合物中存在的单元的相对摩尔百分比的数字,(b) 为 1 至 10 摩尔百分比,(c) 为 30 至 98 摩尔百分比;以及
X⊖ 是反离子、
它们的制备工艺、含有它们的药物组合物以及它们在治疗中作为降胆固醇剂的用途。