Lipid A analogues having immunoactivating and anti-tumour activity

摘要

Compounds of formula (I): [in which: R<1> is hydroxy, protected hydroxy, fluorine, or -OP(O)(OH)2; R<2> and R<3> are independently optionally substituted C6 - C20 aliphatic acyl; R<4> is hydroxy, protected hydroxy, or -OP(O)(OH)2, where at least one of R<1> and R<4> is -OP(O)(OH)2; and R<5> is hydroxy, protected hydroxy, or fluorine; provided that, except where at least one of R<1> and R<5> is fluorine, then at least one of R<2> and R<3> is a substituted C6 - C20 aliphatic acyl having (i) at least one halogen substituent and (ii) at least one of halogen, hydroxy and C6 - C20 aliphatic acyloxy or at least one of R<2> and R<3> is a substituted C6 - C20 aliphatic acyl which is substituted by at least one halogen-substituted C6 - C20 aliphatic carboxylic acyloxy]; have Lipid A-like activity and may be used for the treatment, prophylaxis, diagnosis and support of an animal suffering a disease or disorder arising from a deficiency in the immune system or from a tumor. They may be prepared by phosphorylation of corresponding compounds lacking a phosphoryl group.