| 摘要 |
(A) Novel antigen derivs. (I) consist of an antigen to which at least one muramyl peptide is covalently bonded, opt. via a bridging gp. Prefd. cpds. are of formula (Ia): A-[(Z)m-MP]n (Ia) (A is an antigen residue; Z is a bridging gp.; MP is a muramyl peptide residue; m = 0 or 1; n /-1). The muramyl peptides are pref. of formula (III) (or the corresp. oligomers). (X is CO, COO or SO2; R1 is H, alkyl, opt. substd. benzyl or acyl; R2 is opt. substd. alkyl or carbocyclic aryl; R4 and R6 are each H, alkyl, opt. substd. benzyl or acyl; R3 is H or alkyl; R7, R9 and R13 are each H or lower alkyl; R8 is H, lower alkyl, opt. etherified or esterified lower hydroxyalkyl or mercaptoalkyl, opt. acylated aminoalkyl, 5 or 6C cycloalkyl, (5 or 6C cycloalkyl)-lower alkyl, opt. substd. aryl or aralkyl, or N-contg. heterocyclyl or heterocyclyl-lower alkyl; R7 and R8 can also together form 3 or 4C alkylene; R10, R11 and R12 are each opt. esterified or amidated carboxy, and R11 can also be H; or R1, R4 and R6 are tri-(lower alkyl)-silyl, pref. SiMe3). (B) Cpds. (II) are new provided that (i) X is CO and (ii) at least one of R7, R9 and R13 is lower alkyl unless R1, R4 and R6 are trialkylsilyl or R7 and R8 form a ring. (I) are used in a wide variety of vaccines against bacteria, viruses, tumour cells, parasites, allergens etc. |
