Dendrimer scaffolds for pharmaceutical use

摘要

This invention relates to certain dendrimer compounds. In particular, this invention relates to novel dendrimer compounds that can be elaborated to give increasingly large and complex compounds. These elaborated compounds can be attached to, or can encapsulate within, active agent(s) so as to beneficially modify the characteristics of that active agent. Alternatively, the elaborated compounds can themselves be beneficially modified into therapeutic agents by the attachment of inactive agents.

主权项

1. A compound of formula (I): or salts thereof, wherein: Y1, Y2, Y3, Y4 or Y5 are m=n=p=q=2; or m=0 and n=p=q=2; or m=n=0 and p=q=2; or m=n=p=0 and q=2; or m=n=p=q=0,
wherein:when q=2, C1 is when q=0, C1 is NHP2 or N(CH2CO2P4)2 or NHCOCH3 or when p=2, C2 is when p=0, C2 is NHP2 or N(CH2CO2P4)2 or NHCOCH3 or when n=2, C3 is when n=0, C3 is NHP2 or N(CH2CO2P4)2 or NHCOCH3 or when m=2, C5 is NHP2 or N(CH2CO2P4)2 or NHCOCH3 or  and C4 is when m=0, C4 is NHP2 or N(CH2CO2P4)2 or NHCOCH3 or R, R0, R1, R2, R3 and R4 are H or the side chain of a natural amino acid (except proline); P1 is H or a hydroxy protecting group; P2 is H or an amino protecting group; P4 is H or a carboxylic acid protecting group; X is a leaving group or OP3 or wherein P3 is H or a carboxylic acid protecting group; wherein:
each of Y1, Y2, Y3, Y4, Y5, C1, C2, C3, C4, C5 are as previously defined and can be the same or different;m, n, p and q are as previously defined and can be the same or different;R, R0, R1, R2, R3 and R4 are as previously defined and can be the same or different;r is 1, 2, or 3; andD′ is an aryl; or a straight-, branched- or cyclo-alkyl moiety, or wherein when D′ isr is 3.