| 摘要 |
<p>This invention relates generally to the field of medicinal chemistry, and more specifically to derivatives of a subclass of triterpenoid acids that have multi-medicament properties, that is derivatives of the lupane, betulinic acid, formulations containing such, and their use to prevent or treat certain diseases, and preferably to derivatives or analogues of betulinic acid, that have structural formula (1), wherein: Y is OR1, NR12, O-M1; R1 is H, lower alkyl; M?1 is Na+, K+, Mg++, Ca++¿ ions; each R2 is independently CH¿2?OR1 or CH3; each R?3¿ is independently H, CH¿3?, lower alkyl, COY, CH2OH, CH2OCH2CH=CH2, CH2OSO3-M?1¿; each Z is independently NHR12, NR?1Ac, NR1¿Bz, H, OCH¿3?, lower alkyl, OH, OSO3?-M1, OCH¿2CH=CH2, OCH2CO2H or O-glucoside; each X is independently O, S, NR1 or NR¿2?1; each W is independently C=O, C=CR12, CR1CR13, CR1-CR12OR?1, COR1-CR1OR1, COR1CR1¿2OR?1, CR1CR1¿2NR12, CR1CR12OCR1COY, CHR4; R4 is H, OH, OSO¿3?-M1, or NH(CH¿2?)nNH2, where n=1-8, or NH-Ph-NH2 where Ph=an phenyl or naphtyl rings substituted with up to 3 amine functionalities and the remaining substitutions can be H, R?1, R2¿ or COY; R?5 and R6¿ are independently H, CH¿3?, or taken together form a 5- or 6- membered carbocyclic ring.</p> |
