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US 2023/0405157 A1Published application
Melanocortin type 2 receptor (mc2r) targeted therapeutics and uses thereof
AssigneeRadionetics Oncology, Inc.
InventorsJian ZHAO, Mi CHEN, Yunfei ZHU, Sun Hee KIM
Life of this patent
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Abstract
Described herein are radiotherapeutics that target tumor cells expressing the melanocortin type 2 receptor (MC2R) and their use in the treatment and/or diagnosis of cancer.
Claims32
1-78. (canceled)
A compound of Formula (I), or a pharmaceutically acceptable salt thereof:
- wherein:
- R1 is Ra;
- and Y is N;
- or R1 is R4;
- and Y is C—Ra;
- Ra is —CH2NRs-L2-Rb, or —C(═O)NR8-L2-Rb;
- L2 is absent, -(unsubstituted or substituted C1-C6 alkylene)-, -(unsubstituted or substituted C1-C6 alkylene)-N(R9)—, -(unsubstituted or substituted C1-C6 alkylene)q-(unsubstituted or substituted C3-C6cycloalkyl), -(unsubstituted or substituted C1-C6 alkylene)q-(unsubstituted or substituted aryl), -(unsubstituted or substituted C1-C6 alkylene)q-(unsubstituted or substituted C2-C6heterocycloalkyl), or -(unsubstituted or substituted C1-C6 alkylene)q-(unsubstituted or substituted heteroaryl);
- q is 0 or 1;
- Rb is -L3-Q;
- L3 is a linker;
- Q is a chelating moiety or a radionuclide complex thereof;
- L1 is absent or —C(═O)—;
- R2 is ring that is selected from the group consisting of:
- C3-C8cycloalkyl, C2-C8heterocycloalkyl, aryl, or heteroaryl, wherein R2 is unsubstituted or is substituted with R3a, R3b, or R3c, or combinations thereof,
- each R3a, R3b, R3c, R4, and R5 is independently hydrogen, halogen, substituted or unsubstituted C1-C4alkyl, substituted or unsubstituted C1-C4alkenyl, substituted or unsubstituted C1-C4alkynyl, substituted or unsubstituted C1-C4fluoroalkyl, substituted or unsubstituted C1-C4heteroalkyl, —CN, —N(R9)2, or —OR9;
- R6 is C1-C4alkyl;
- R7 is hydrogen or C1-C4alkyl;
- R8 is hydrogen or C1-C4alkyl;
- each R9 is independently hydrogen, C1-C4alkyl, C1-C4fluoroalkyl, substituted or unsubstituted C1-C4heteroalkyl;
- X1 is CR5 or N;
- X2 is CR4 or N;
- m is 0, 1, or 2;
- and n is 0, 1, 2, or 3.
20 more elements
Dependencies are inferred from the claim text.