申请人:American Home Products Corporation
公开号:US05366993A1
公开(公告)日:1994-11-22
There are disclosed compounds of the formula: ##STR1## wherein X is O, S or NR; R is hydrogen or lower alkyl; R.sup.1 and R.sup.2 are each, independently, hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.20 cycloalkyl, phenylloweralkyl, or substituted phenylloweralkyl substituted by halo, lower alkyl, lower alkoxy, halo lower alkyl, amino, monoloweralkylamino, diloweralkylamino or sulfonamido; A is O, S, NR, or a chemical bond; m is 0-15; n is 0-20; p is 0-15, where m+p.ltoreq.15; and the pharmacologically acceptable salts thereof, which by virtue of their ability to inhibit PLA.sub.2, are of use as antiinflammatory agents and there is also disclosed a method for the treatment of immunoinflammatory conditions, such as allergy, anaphylaxis, asthma and inflammation in mammals, as well as in the modulation of PAF-mediated biological processes, such as embryonic implantation, thus making the compounds useful as antifertility agents.
披露了具有以下公式的化合物:##STR1## 其中X是O,S或NR;R是氢或低级烷基;R.sup.1和R.sup.2各自独立地为氢,C.sub.1-C.sub.10烷基,C.sub.3-C.sub.20环烷基,苯基低级烷基,或被卤素,低级烷基,低级烷氧基,卤素低级烷基,氨基,单低级烷基氨基,二低级烷基氨基或磺酰氨基取代的取代苯基低级烷基;A是O,S,NR或化学键;m是0-15;n是0-20;p是0-15,其中m+p≤15;以及药理上可接受的盐,由于其能够抑制PLA.sub.2,因此可用作抗炎剂,并且还披露了用于治疗免疫炎性疾病的方法,例如过敏,过敏性反应,哮喘和哺乳动物的炎症,以及调节PAF介导的生物学过程,如胚胎植入,从而使化合物作为抗生育剂是有用的。