首页> 外国专利> Lipid-A analogs: monosaccharide and dissaccharide compounds for inhibiting binding of lipid A receptors to lipid A receptors

Lipid-A analogs: monosaccharide and dissaccharide compounds for inhibiting binding of lipid A receptors to lipid A receptors

机译:脂质A类似物:单糖和二糖化合物,可抑制脂质A受体与脂质A受体的结合

摘要

A compound of the formula: ##STR1## wherein: each of R.sub.1, R.sub.1 ', R.sub.2 and R.sub.2 ' independent of each other is a substituted or unsubstituted, branched or linear C.sub.1-12 alkyl, alkene or alkyne group, R.sub.3 is OH, OCH.sub.3, CH.sub.2 COOH or ##STR2## wherein each of R.sub.2" and R.sub.2 '41 independent of each other is a substituted or unsubstituted, branched or linear C.sub.1-12 alkyl, alkene or alkyne group and:PPA=NH.sub.2, X=P(OH), Y=Z=C, B=OCH. sub.3, orPPA=OH, X=P(OH), X=Z=C, B (if present)=OCH.sub.3, or PPA=OCO(CH.sub.2).sub.n NH.sub.2, X=P(OH), Y=Z=C, B=OCH.sub.3, PPwherein n=1-10, orPPA=OH, X=P(OH), Y=Z=C, B=O(CH.sub.2).sub.n CO.sub.2 H, wherein n=1-10, or P PA=OH, X=P(OH), Y=Z=C, B=(CH.sub.2).sub.n CO.sub.2 H, wherein n=1-10, orPPA=NH.sub.2, X=Z=C, Y=P(OH), B=OCH.sub. 3, orP PA=OH, X=Z=C, Y=P(OH), B (if present)=OCH.sub.3, orP PA=OCO(CH.sub.2).sub.n NH.sub.2, X=Z=C, Y=P(OH), B=OCH.sub.3, wherein n=1-10, orPPA=OH, X=Z=C, Y=P(OH), B=O(CH.sub.2).sub.n CO. sub.2 H, wherein n=1-10, orPPA=OH, X=Z=C, Y=P(OH), B=(CH. sub.2).sub.n CO.sub.2 H, wherein n=1-11, or PPA=NH.sub.2, X=Y=C, Z=P(OH), B=OCH.sub.3, orP PA=OH, X=Y=C, Z=P(OH), B (if present)=OCH.sub.3, orPP A=OCO(CH.sub.2).sub.n NH.sub. 2, X=Y=C, Z=P(OH), B=OCH.sub.3, wherein n=1- 10, orPPA=OH, X=Y=C, Z=P(OH), B=O(CH.sub.2).sub.n CO.sub. 2 H, wherein n=1-10, or PPA=OH, X=Y=C, Z=P (OH), B=(CH. sub.2).sub.n CO.sub.2 H and n=1-11 is disclosed. The compounds may be use to inhibit binding of Lipid A to Lipid A receptors.
机译:具有下式的化合物:其中R 1,R 1',R 2和R 2'各自独立地为取代或未取代的, R 3是支链或直链的C 1-12烷基,烯烃或炔基,R 3是OH,OCH 3,CH 2 COOH或## STR2 ##,其中每个彼此独立的“ 2”和R 2 '41是取代或未取代的,支链或直链的C 1-12烷基,烯基或炔基,并且:P = A = NH。 2,X = P(OH),Y = Z = C,B = OCH.sub.3,或

A = OH,X = P(OH),X = Z = C,B(如果存在)= OCH.sub.3或

A = OCO(CH.sub.2)n NH.sub.2,X = P(OH),Y = Z = C,B = OCH 3,

,其中n = 1-10,或

A = OH,X = P(OH),Y = Z = C,B = O(CH。 sub.2)sub.n CO.sub.2 H,其中n = 1-10,或

A = OH,X = P(OH),Y = Z = C,B =(CH 2)n CO 2 H,其中n = 1-10,或

A = NH 2,X = Z = C,Y = P(OH) ,B = OCH.sub.3或

A = OH,X = Z = C,Y = P(OH),B(如果存在)= OCH.sub.3或

< P> A = OCO(CH 2)n NH 2,X = Z = C,Y = P(OH),B = OCH 3,其中n = 1-10,或

A = OH,X = Z = C,Y = P(OH),B = O(CH 2)n CO.sub.2 H,其中n = 1-10,或P = A = OH,X = Z = C,Y = P(OH),B =(CH。 sub.2).sub.n CO.sub.2 H,其中n = 1-11,或P = A = NH.2,X = Y = C,Z = P(OH), B = OCH.3,或

A = OH,X = Y = C,Z = P(OH),B(如果存在)= OCH.sub.3,或

A = OCO(CH.sub.2)sub.n NH.sub。在图2中,X = Y = C,Z = P(OH),B = OCH 3,其中n = 1-10,或P = A = OH,X = Y = C,Z = P (OH),B = O(CH.sub.2).n。CO.sub。 2 H,其中n = 1-10,或P = A = OH,X = Y = C,Z = P(OH),B =(CH 2)n CO。公开了0.2 H和n = 1-11。所述化合物可用于抑制脂质A与脂质A受体的结合。

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