NOVEL ANTIGEN DERIVATIVE AND ITS MANUFACTURE

Japanese Patent JPS54141718

A

(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.

GERUHARUTO BAASHIYANKU
FUERIKUSU EMU DEIITORITSUHI
ROORANDO GISURA
ARUBERUTO HARUTOMAN
YAROSURAFU SUTANETSUKU
RAYOSU TARUKUSEI

JP2128179A

November 05, 1979

February 24, 1979

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CIBA GEIGY AG

A61K38/14; A61K39/00; A61K39/385; A61K39/39; C07H9/04; C07H15/04; G01N33/531; C07H23/00; C07K1/113; C07K9/00; C07K14/76; C07K16/00; C07K19/00; (IPC1-7): A61K39/00; C07H13/04; C07H13/08; C07H15/04; C07H15/18

JPS52139018A	1977-11-19
JPS52116416A	1977-09-29
JPS5273820A	1977-06-21

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