Substituted 2-furanyl or 5-oxo-2-furanyl-alkoxy phosphoryl alkyl cyclimmonium salts
申请人:SANDOZ AG
公开号:EP0178261A2
公开(公告)日:1986-04-16
Compounds of formula I
wherein R is n-C12-20alkyl, alkenyl or alkynyl, C12-24alkoxyalkyl, phenyl or C7-9phenylalkyl,
Y is CH2; O;
Tis
wherein Ro is hydrogen or methyl; and X is
represents a 5- or 6-membered mono-cyclic ring optionally containing one further heteroatom selected from nitrogen or sulphur; or a 10-membered bicyclic ring optionally containing one further nitrogen atom; each of which rings may be unsubstituted or either mono, di-, or tri-substituted by C1-4alkyl or mono- ⊖ substituted by CF3, halo, COOH or COOCH3
Z is a pharmaceutically acceptable anion,
m is 1 or 2;
n is 1 or 2;
p is 2 to 8; and
y is ⊖ and q is 0 ; or
y is H and q is 1,
which are indicated for use as pharmaceuticals particularly for the use in inhibiting PAF induced blood platelet aggregation or treating PAF mediated bronchoconstriction and extravasation and PAF induced hypotension and ischemic bowel disease.
式 I 的化合物
其中 R 是 n-C12-20烷基、烯基或炔基、C12-24烷氧基烷基、苯基或 C7-9 苯基烷基、
Y 是 CH2;O
Tis
其中 Ro 是氢或甲基;X 是
代表一个 5 或 6 元单环,可选择再含有一个选自氮或硫的杂原子;或代表一个 10 元双环,可选择再含有一个氮原子;其中每个环可以是未取代的,或被 C1-4 烷基单取代、二取代或三取代,或被 CF3、卤素、COOH 或 COOCH3 单取代⊖。
Z 是药学上可接受的阴离子、
m 是 1 或 2
n 是 1 或 2
p 是 2 至 8;以及
y 是⊖,q 是 0;或
y 是 H,q 是 1、
这些化合物可用作药物,特别是用于抑制 PAF 诱导的血小板聚集或治疗 PAF 介导的支气管收缩和外渗以及 PAF 诱导的低血压和缺血性肠病。