Phthalidilidene derivatives of carnitine and alkanoylcarnitines and pharmaceutical compositions containing them
申请人:Sigma-Tau Industrie
Farmaceutiche Riunite S.p.A.
公开号:EP0488965A1
公开(公告)日:1992-06-03
(3-phtalidylidene) alkyl esters of carnitine and alkanoyl carnitines of general formula (I)
wherein
Y is a C₁-C₅ alkylene group, unsubstituted or substituted with one or more lower C₁-C₄ alkyl groups;
R is hydrogen or C₂-C₆ alkanoyl;
R₁, R₂,R₃, and R₄, identical or different, are hydrogen, halogen C₁-C₈ alkoxy, C₁-C₄ lower alkyl, halogen-substituted lower alkyl, amino, alkyl-substituted amino wherein the alkyl group has 1 to 4 carbon atoms, nitro, cyano, C₁-C₄ alkanoylamino, or R₁ and R₂ taken together, R₂ and R₃ taken together or R₃ and R₄ taken together form a C₁-C₄ alkylenedioxy group, and X⁻ is the anion of a pharmacologically acceptable salt are potent PAF (plateletactivating factor) and acetyl-cholinesterase antagonists.
Pharmaceutical compositions containing the compounds of formula (I) are useful for the therapeutical treatment of inflammatory and allergic conditions, particularly asthma, anaphylactic shock, as contraceptives and for the treatment of pre-senile and senile dementias (typically, Alzheimer's disease).
(3-phtalidylene) 烷基肉碱酯和通式 (I) 的烷酰基肉碱
其中
Y 是 C₁-C₅ 亚烷基,未被取代或被一个或多个低级 C₁-C₄ 烷基取代;
R 是氢或 C₂-C₆ 烷酰基;
R₁、R₂、R₃ 和 R₄,相同或不同,是氢、卤素 C₁-C₈烷氧基、C₁-C₄低级烷基、卤素取代的低级烷基、氨基、烷基取代的氨基(其中烷基有 1 至 4 个碳原子)、硝基、氰基、C₁-C₄烷酰氨基、或 R₁ 和 R₂ 合在一起、R₂ 和 R₃ 合在一起或 R₃ 和 R₄ 合在一起形成 C₁-C₄ 烷基二氧基,且 X- 是药理学上可接受的盐的阴离子,是强效的 PAF(血小板活化因子)和乙酰胆碱酯酶拮抗剂。
含有式 (I) 化合物的药物组合物可用于治疗炎症和过敏性疾病,尤其是哮喘、过敏性休克,也可用作避孕药和治疗老年前期痴呆症和老年性痴呆症(通常是阿尔茨海默氏症)。