申请人:SMITH KLINE & FRENCH LABORATORIES
LIMITED
公开号:EP0403198A3
公开(公告)日:1992-02-12
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各自是C₁₋₄烷基,或者一个是C₁₋₄烷基,另一个是-(CH₂)nR³;n为2到12;R³为NR4R5或R6R7R8中的一种;R⁴和R⁵相同或不同,分别为氢、C₁₋₄烷基、C(=NH)NH₂,或者与它们连接的氮原子一起形成一个饱和或不饱和的环,可选地含有一个或多个进一步的杂原子;R⁶、R⁷和R⁸相同或不同,分别为氢、C₁₋₄烷基,或者R⁶、R⁷和R⁸中的一个是C₁₋₄烷基,另外两个与它们连接的氮原子一起形成一个饱和或不饱和的环,可选地含有一个或多个进一步的杂原子;a、b和c是相对摩尔百分比指示所述聚合物中存在的单元,其中(b)为1到10摩尔百分比,(c)为30到98摩尔百分比;X⊖是一个计数离子,它们的制备方法,含有它们的制药组合物及其作为降低胆固醇药物的用途。