Bioorthogonal compositions
AssigneesTambo, Inc., The Research Foundation for The State University of New York
InventorsJose Manuel Mejia Oneto, Nathan Yee, Maksim Royzen, Sangeetha Srinivasan, Ethan Miller
Life of this patent
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Abstract
Cyclooctene conjugates of therapeutic or diagnostic agents have improved aqueous solubility and can release the agents upon contact with a tetrazine-containing biomaterial. The cyclooctene conjugates provide site-selective delivery of agents at the location of the tetrazine-containing biomaterial in a subject. The compositions and methods have applications in the treatment of various diseases or conditions including cancer, tumor growths, and bacterial infections.
Claims26
A compound of formula (I-A), or a pharmaceutically acceptable salt thereof
- wherein
- R1a is selected from the group consisting of C1-4alkyl, C1-4haloalkyl, and C1-4alkoxy;
- R1b is selected from the group consisting of G1, OH, —NR1c—C1-4alkylene-G1, —NR1c—C1-4alkylene-N(R1d)2, —N(R1c)CHR1eCO2H, —N(R1c)—C1-6alkylene-CO2H, —N(R1f)—C2-4alkylene-(N(C1-4alkylene-CO2H)—C2-4alkylene)n-N(C1-4alkylene-CO2H)2, —N(R1c)CHR1cC(O)OC1-6alkyl, —N(R1c)—C1-6alkylene-C(O)OC1-6alkyl, and —N(R1f)—C2-4alkylene-(N(C1-4alkylene-C(O)OC1-6alkyl)-C2-4alkylene)n-N(C1-4alkylene-C(O)OC1-6alkyl)2;
- R1c and R1d, at each occurrence, are independently hydrogen or C1-4alkyl;
- R1e is —C1-4alkylene-CO2H, —C1-4alkylene-CONH2, or —C1-4alkylene-OH;
- R1f is hydrogen, C1-6alkyl, or C1-4alkylene-CO2H;
- D, at each occurrence, is independently a payload selected from the group consisting of auristatin and monomethyl auristatin E;
- -L1- is a linker;
- -L2- is selected from the group consisting of —C(O)— and C1-3alkylene;
- G1 is an optionally substituted heterocyclyl;
- m is 1, 2, or 3;
- n is 0, 1, 2, or 3;
- and
- p is 0, 1, or 2.
Dependencies are inferred from the claim text.