Pharmaceutically active compounds and liposomes, and methods...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/09 (2006.01) A61K 9/127 (2006.01) A61K 31/695 (2006.01) C07C 233/20 (2006.01) C07C 233/31 (2006.01) C07F 7/18 (2006.01) C07F 9/02 (2006.01)

Patent

CA 2182485

This invention provides a compound having the formula R1-Y1-CHZ1-CH(NY2Y3)-CH2- Z2, wherein: R1 is a straight-chained alkyl, alkenyl or alkynyl group having from 8 to 19 carbon atoms in the aliphatic chain; Y1 is -CH=CH-, -C||C- or - CH(OH)CH(OH)-; Z1 is OH or a conversion-inhibiting group; Z2 is a conversion- inhibiting group; Y2 is H, a phenyl group, an alkyl-substituted phenyl group having from 1 to about 6 carbons in the alkyl chain, or an alkyl chain having from 1 to 6 carbons; Y3 is H or a group having the formula -C(O)R2 or - S(O)2R2; R2 is a straight-chained alkyl, alkenyl or alkynyl group having from 1 to 23 carbon atoms in the chain; and when Z2 is an amino, R2 is an aliphatic chain having from 1 to 9 or from 19 to 23 carbon atoms in the aliphatic chain.

L'invention concerne un composé de formule R?1¿-Y?1¿-CHZ?1¿-CH(NY?2¿Y?3¿)-CH¿2?-Z?2¿, dans laquelle R?1¿ est un groupe alkyle, alcényle, ou alcynyle à chaîne droite, présentant de 8 à 10 atomes de carbone dans la chaîne aliphatique; Y?1¿ est -CH=CH-, -C||C- ou bien -CH(OH)CH(OH)-; Z?1¿ est OH ou bien un groupe inhibiteur de conversion; Z?2¿ est un groupe inhibiteur de conversion; Y?2¿ est H, un groupe phényle, un groupe phényle à substitution alkyle ayant de 1 à environ 6 carbones dans la chaîne alkyle, ou bien une chaîne alkyle ayant de 1 à 6 carbones; Y?3¿ est H, ou bien un groupe ayant la formule -C(O)R?2¿ ou -S(O)¿2?R?2¿; R?2¿ est un groupe alkyle, alcényle ou alcynyle à chaîne droite possédant de 1 à 23 atomes de carbone; et lorsque Z?2¿ est un amino, R?2¿ est une chaîne aliphatique ayant de 1 à 9 ou de 19 à 23 atomes de carbone.

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