| 主权项 |
1. A dendrimer of the formula:
Core-(Repeating Unit)n-Terminating Group (I) wherein the core is linked to the repeating unit by removing one or more hydrogen atoms from the core and replacing the atom with the repeating unit and wherein:
the core has the formula: wherein:
X1 is amino or alkylamino(C≦12), dialkylamino(C≦12), heterocycloalkyl(C≦12), heteroaryl(C≦12), or a substituted version thereof;R1 is amino, hydroxy, or mercapto, or alkylamino(C≦12), dialkylamino(C≦12), or a substituted version of either of these groups; anda is 1, 2, 3, 4, 5, or 6; orthe core has the formula: wherein:
X2 is N(R5)y;
R5 is hydrogen, alkyl(C≦18), or substituted alkyl(C≦18); andy is 0, 1, or 2, provided that the sum of y and z is 3;R2 is amino, hydroxy, or mercapto, or alkylamino(C≦12), dialkylamino(C≦12), or a substituted version of either of these groups;b is 1, 2, 3, 4, 5, or 6; andz is 1, 2, 3; provided that the sum of z and y is 3; orthe core has the formula: wherein:
X3 is —NR6—, wherein R6 is hydrogen, alkyl(C≦8), or substituted alkyl(C≦8), —O—, or alkylaminodiyl(C≦8), alkoxydiyl(C≦8), arenediyl(C≦8), heteroarenediyl(C≦8), heterocycloalkanediyl(C≦8), or a substituted version of any of these groups;R3 and R4 are each independently amino, hydroxy, or mercapto, or alkylamino(C≦12), dialkylamino(C≦12), or a substituted version of either of these groups; or a group of the formula: —(CH2CH2N)e(Rc)Rd;wherein:
e is 1, 2, or 3;Rc and Rd are each independently hydrogen, alkyl(C≦6), or substituted alkyl(C≦6);c and d are each independently 1, 2, 3, 4, 5, or 6; orthe core is alkylamine(C≦18), dialkylamine(C≦36), heterocycloalkane(C≦12), or a substituted version of any of these groups;wherein the repeating unit comprises a degradable diacyl and a linker;
the degradable diacyl group has the formula: wherein:
A1 and A2 are each independently —O— or —NRa—, wherein: Ra is hydrogen, alkyl(C≦6), or substituted alkyl(C≦6);Y3 is alkanediyl(C≦12), alkenediyl(C≦12), arenediyl(C≦12), or a substituted version of any of these groups; or a group of the formula: wherein: X3 and X4 are alkanediyl(C≦12), alkenediyl(C≦12), arenediyl(C≦12), or a substituted version of any of these groups; Y5 is a covalent bond, alkanediyl(C≦12), alkenediyl(C≦12), arenediyl(C≦12), or a substituted version of any of these groups; andR9 is alkyl(C≦8) or substituted alkyl(C≦8);the linker group has the formula: wherein:
Y1 is alkanediyl(C≦12), alkenediyl(C≦12), arenediyl(C≦12), or a substituted version of any of these groups; andwherein when the repeating unit comprises a linker group, then the linker group is attached to a degradable diacyl group on both the nitrogen and the sulfur atoms of the linker group, wherein the first group in the repeating unit is a degradable diacyl group, wherein for each linker group, the next group comprises two degradable diacyl groups attached to the nitrogen atom of the linker group; and wherein n is the number of linker groups present in the repeating unit; andthe terminating group has the formula: wherein:
Y4 is alkanediyl(C≦18) or an alkanediyl(C≦18) wherein one or more of the hydrogen atoms on the alkanediyl(C≦18) has been replaced with —OH, —F, —Cl, —Br, —I, —SH, —OCH3, —OCH2CH3, —SCH3, or —OC(O)CH3;R10 is hydrogen, carboxy, hydroxy, oraryl(C≦12), alkylamino(C≦12), dialkylamino(C≦12), N-heterocycloalkyl(C≦12), —C(O)N(R11)-alkanediyl(C≦6)-heterocycloalkyl(C≦12), —C(O)-alkyl-amino(C≦12), —C(O)-dialkylamino(C≦12), —C(O)—N-heterocyclo-alkyl(C≦12), wherein:
R11 is hydrogen, alkyl(C≦6), or substituted alkyl(C≦6);wherein the final degradable diacyl in the chain is attached to a terminating group;n is 0, 1, 2, 3, 4, 5, or 6; or a pharmaceutically acceptable salt thereof. |
