发明名称 MACROPHAGE-ACTIVE MURAMYLPEPTIDE LIPOPHILIC DERIVATIVES, COMPOSITIONS AND MANUFACTURE
摘要 1. Muramylpeptide derivatives, characterised by the following formula see diagramm : EP0165123,P28,F1 in which the substituents R1 , R2 , R11 , R14 , W, X, Y, A and B have the following meanings : R1 is H or CH3 R2 is a -NH2 , -OH group, or a -OV group, with V being a hydrocarbon comprising from 1 to 10 carbon atoms, R11 is a hydrogen atom or a phenylamino group, R14 is a hydrogen atom or an acyl group comprising 1 to 4 carbon atoms, X is an aminoacyl residue of the group comprising : alanyl, valyl, isoleucyl, norleucyl, leucyl, seryl, threonyl, prolyl, glutaminyl, asparaginyl, methionyl, tryptophanyl, phenylalanyl, tyrosyl, glycyl, it being understood that said amino acyl group may be N-substituted by a lower alkyl group, more particularly methyl, Y has the same meaning as R2 or is a lipophile group -OCH2 -CHO(R3 )CH2 O(R4 ) with R3 and R4 , respectively identical or different, being acyl or alkyl groups comprising from 8 to 100 carbon atoms ; Z has the same meaning as R2 or is a lipophile group -CO-CHO(R3 )CH2 O(R4 ) with R3 and R4 , respectively identical or different, being acyl or alkyl groups comprising from 8 to 100 carbon atoms ; the methylene groups contained in the glyceryl groups, R3 and R4 , possibly being substituted by a lower alkyl group, more particularly methyl ; it being however understood that at least one of the two groups Y and Z always consist of the corresponding lipophile group ; W is an oxygen atom or, when Z is the above mentioned lipophile group, a NH group ; A and B are either direct linkage or bridging arms, more particularly groups, respectively identical or different, comprising respectively one to three aminoacyl residue, themselves identical or different from one another, or further a -NH-(CH2 )p -CO- group with value of p comprised between 2 and 10, or -NH-CH2 -H2 -O-, and finally, one of the methylene groups of the glutamyl residue possibly being substituted by a lower alkyl, more particularly methyl.
申请公布号 JPS60252497(A) 申请公布日期 1985.12.13
申请号 JP19850099454 申请日期 1985.05.10
申请人 AGENCE NATIONALE DE VALOR DE LA RECH ANVAR 发明人 NIJIERU FUIRITSUPISU;FURANSOWAAZU OODEIBEERU;JIYAN MARI BERUNAARU;RUI SHIEDEIDO;PIEERU RUFURANSHIE;MISHIERU RUBUERU;MONITSUKU PARAN
分类号 A61K9/00;A61K9/127;A61K38/00;A61P35/00;A61P37/00;C07K9/00;C07K14/52;C07K14/53;C07K14/535 主分类号 A61K9/00
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