DIHYDROCERAMIDE DESATURASE INHIBITORS.
申请人:CONSEJO SUPERIOR DE INVESTIGACIONES CIENTIFICAS
公开号:EP1354870A1
公开(公告)日:2003-10-22
Cyclopropenylceramide derivatives as inhibitors of desaturases characterized by the general formula I in which R1 can be an alkyl, alkenyl, alkynyl, aryl or any heterocyclic group, n can have any value and it can be branched or straight chained and can contain unsaturated carbons and R2 and R3 can have the same or different values, and it can represent aryl, heteroaryl, alkyl or acyl groups with one or more unsaturated carbons on the chain, that can be branched or straight and substituted with OH groups. Members of this new class of compounds have shown an extraordinary activity as inhibitors of the dihydroceramide desaturase and of ceramide biosynthesis and are useful for the treatment of clinical conditions associated with increased intracellular ceramide.
环丙烯基鞘氨醇衍生物作为脱饱和酶抑制剂,其一般式为I,其中R1可以是烷基,烯基,炔基,芳基或任何杂环基团,n可以有任何值,可以是支链或直链,可以含有不饱和碳,并且R2和R3可以具有相同或不同的值,并且可以表示带有一个或多个链上不饱和碳的芳基,杂环芳基,烷基或酰基基团,可以是支链或直链,并且可以用OH基团取代。这种新类化合物的成员已经表现出极高的脱氢鞘氨醇酰酶和鞘氨醇生物合成抑制活性,并且对于治疗与细胞内鞘氨醇增加有关的临床病症非常有用。