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    • 3. 发明授权
    • Lipid-A analogs: monosaccharide and dissaccharide compounds for
inhibiting binding of lipid A receptors to lipid A receptors
    • 脂质-A类似物:用于抑制脂质A受体与脂质A受体结合的单糖和非糖化合物
    • US5593969A
    • 1997-01-14
    • US123590
    • 1993-09-17
    • Balreddy KamireddyMichael J. DarsleyDavid M. SimpsonRichard J. Massey
    • Balreddy KamireddyMichael J. DarsleyDavid M. SimpsonRichard J. Massey
    • A61K38/00C07H13/06C07H15/04C07K16/12A61K31/70C07H3/02C07H3/04
    • C07H13/06C07H15/04C07K16/1203A61K38/00
    • 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:A=NH.sub.2, X=P(OH), Y=Z=C, B=OCH.sub.3, orA=OH, X=P(OH), X=Z=C, B (if present)=OCH.sub.3, orA=OCO(CH.sub.2).sub.n NH.sub.2, X=P(OH), Y=Z=C, B=OCH.sub.3,wherein n=1-10, orA=OH, X=P(OH), Y=Z=C, B=O(CH.sub.2).sub.n CO.sub.2 H, wherein n=1-10, orA=OH, X=P(OH), Y=Z=C, B=(CH.sub.2).sub.n CO.sub.2 H, wherein n=1-10, orA=NH.sub.2, X=Z=C, Y=P(OH), B=OCH.sub.3, orA=OH, X=Z=C, Y=P(OH), B (if present)=OCH.sub.3, orA=OCO(CH.sub.2).sub.n NH.sub.2, X=Z=C, Y=P(OH), B=OCH.sub.3, wherein n=1-10, orA=OH, X=Z=C, Y=P(OH), B=O(CH.sub.2).sub.n CO.sub.2 H, wherein n=1-10, orA=OH, X=Z=C, Y=P(OH), B=(CH.sub.2).sub.n CO.sub.2 H, wherein n=1-11, orA=NH.sub.2, X=Y=C, Z=P(OH), B=OCH.sub.3, orA=OH, X=Y=C, Z=P(OH), B (if present)=OCH.sub.3, orA=OCO(CH.sub.2).sub.n NH.sub.2, X=Y=C, Z=P(OH), B=OCH.sub.3, wherein n=1-10, orA=OH, X=Y=C, Z=P(OH), B=O(CH.sub.2).sub.n CO.sub.2 H, wherein n=1-10, orA=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.
    • 下式的化合物:其中:R 1,R 1',R 2和R 2'彼此独立地为取代或未取代的支链或直链C 1-12烷基,烯烃或炔基,R 3为 OH,OCH 3,CH 2 COOH或者其中每个R 2“和R 21'彼此独立地是取代或未取代的支链或直链C 1-12烷基,烯烃或炔基,并且:A = NH 2,X = P (OH),Y = Z = C,B = OCH 3或A = OH,X = P(OH),X = Z = C,B(如果存在)= OCH 3或A = OCO(CH 2)n NH 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 2)n CO 2 H,其中 n = 1-10,或A = OH,X = P(OH),Y = Z = C,B =(CH2)nCO2H,其中n = 1-10,或A = NH2,X = Z = C,Y = P(OH),B = OCH3或A = OH,X = Z = C,Y = P(OH),B(如果存在)= OCH 3或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 2 H,其中n = 10或A = OH,X = Z = C,Y = P(OH),B =(CH2)nCO2H,其中n = 1-11或A = NH2,X = Y = C,Z = P ),B = OCH 3或A = OH,X = Y = C,Z = P(OH),B(如果存在)= OCH 3或A = OCO(CH 2)n NH 2,X = Y = C,Z = P (OH),B = OCH 3, 其中n = 1-10,或A = OH,X = Y = C,Z = P(OH),B = O(CH 2)n CO 2 H,其中n = 1-10,或A = OH,X = Y = C ,Z = P(OH),B =(CH2)nCO2H和n = 1-11。 该化合物可用于抑制脂质A与脂质A受体的结合。