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    • 4. 发明授权
    • Adjuvants for use in vaccination
    • 用于疫苗接种的佐剂
    • US08728515B2
    • 2014-05-20
    • US12988587
    • 2009-04-22
    • Mark Stephen BairdJuma' a Raheem Najeem Al-DulayymiCornelia TheunissenGani KozaSeppe Vander BekenJohan Adriaan Marc Grooten
    • Mark Stephen BairdJuma' a Raheem Najeem Al-DulayymiCornelia TheunissenGani KozaSeppe Vander BekenJohan Adriaan Marc Grooten
    • A61K9/127A61K39/00C07C61/00C07D303/12
    • A61K39/39A61K2039/55555
    • A compound of formula (I) for use as an adjuvant in vaccination; wherein R is an optionally-substituted alkyl, alkenyl, alkynyl, aryl, arylalkyl or alkylaryl moiety having from 1 to 50 carbon atoms; R1 is an optionally-substituted alkyl, alkenyl, alkynyl, aryl, arylalkyl or alkylaryl moiety having from 1 to 40 carbon atoms; each of R2, R3 and R4 is independently selected from an optionally-substituted alkylene, alkenylene, alkynylene, arylene, arylalkylene or alkylarylene moiety having from 1 to 40 carbon atoms; each of X, Y and Z is independently selected from an optionally-substituted alkylene, alkenylene, alkynylene, arylene, alkylarylene or cycloalkylene, ketone, ester, amide, imide, imine, thioether, ether, thioester, thioketone; and P is selected from hydrogen, an alkyl group, a sugar residue, or a metal, phosphonium or ammonium species; wherein at least one of X, Y and Z includes a moiety selected from cyclopropyl, C=A, C-AH and C—OR5; wherein R5 is alkyl or haloalkyl, and A is S, O or NR6, wherein R6 maybe H or 20 alkyl.
    • 用作疫苗接种佐剂的式(I)化合物; 其中R是具有1至50个碳原子的任选取代的烷基,烯基,炔基,芳基,芳基烷基或烷芳基部分; R1是具有1至40个碳原子的任选取代的烷基,烯基,炔基,芳基,芳基烷基或烷芳基部分; R 2,R 3和R 4各自独立地选自具有1至40个碳原子的任选取代的亚烷基,亚烯基,亚炔基,亚芳基,芳基亚烷基或烷基亚芳基; X,Y和Z各自独立地选自任选取代的亚烷基,亚烯基,亚炔基,亚芳基,亚烷基亚芳基或亚环烷基,酮,酯,酰胺,酰亚胺,亚胺,硫醚,醚,硫酯,硫酮; 并且P选自氢,烷基,糖残基或金属,鏻或铵物质; 其中X,Y和Z中的至少一个包括选自环丙基,C = A,C-AH和C-OR 5的部分; 其中R 5是烷基或卤代烷基,A是S,O或NR 6,其中R 6可以是H或20烷基。