Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
View Patent ↗Antiproliferative compounds having a structure represented by formula (II), where n, R 1 , R 2 , R 3 , R 4 , and R 5 are as defined herein, can be used to treat tumors, optionally when conjugated to a ligand such as an antibody:
1. A compound having a structure according to formula (VIII-b)
wherein R 9 and R 10 are independently H or an amine protecting group and R 11 is H, C 1 -C 10 alkyl, C 2 -C 10 alkenyl, C 2 -C 10 alkynyl, aryl, cycloaliphatic, alkylcycloaliphatic, arylalkyl, or alkylaryl.
2. A compound according to claim 1 , wherein R 9 and R 10 are independently selected from H, Boc (t-butoxycarbonyl), Troc (2,2,2-trichloroethoxy carbonyl), Bpoc (1-methyl-1-(4-biphenyl)ethoxycarbonyl), Cbz (benzyloxy carbonyl), Aloc (allyloxycarbonyl), methylamine, and Fmoc (9-flurenylmethoxycarbonyl).
3. A compound according to claim 2 , wherein R 11 is H or C 1 -C 5 alkyl.
4. A compound according to claim 3 , wherein R 11 is Me.
5. A compound according to claim 1 , wherein R 11 is H or C 1 -C 5 alkyl.
6. A compound according to claim 5 , wherein R 11 is Me.
7. A compound according to claim 1 , wherein R 9 and R 10 are different amine protecting groups.
8. A compound according to claim 7 , wherein R 11 is H or C 1 -C 5 alkyl.
9. A compound according to claim 8 , wherein R 11 is Me.
10. A compound according to claim 1 , having a structure represented by the formula:
11. A compound according to claim 1 , having a structure represented by the formula
12. A compound according to claim 1 , having a structure represented by the formula
13. A compound according to claim 1 , having a structure represented by the formula
14. A compound according to claim 1 , having a structure represented by the formula
15. A compound according to claim 1 , having a structure represented by the formula