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US 2024/0285628 A1Published application
Non-peptide targeted therapeutics and uses thereof
AssigneeCrinetics Pharmaceuticals, Inc.
InventorsR. Scott STRUTHERS, Jian ZHAO, Yunfei ZHU
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Abstract
Described herein are non-peptide drug conjugates (NPDCs) that target tumor cells expressing cell surface peptide and protein G protein-coupled receptors and their use in the treatment and/or diagnosis of cancer.
Claims22
A compound of Formula (I), or a pharmaceutically acceptable salt thereof:
- wherein:
- (a) NP is a non-peptide ligand that binds to a gonadotropin-releasing hormone receptor (GnRHR) expressed in tumor cells;
- (b) a payload moiety (Q) comprising a chemotherapeutic;
- and
- (c) a linker (L) that covalently connects the non-peptide ligand NP and the payload moiety Q;
- wherein NP has a structure of Formula (X), or a pharmaceutically acceptable salt thereof:
- wherein:
- V is CH or N;
- and W is CH or N;
- T is absent, —CH2—, —CH(CH3)—, or —C(CH3)2—:
- X2 is absent, —O—, or —N(R7)—;
- and
- R7 is hydrogen or substituted or unsubstituted C1-C6alkyl:
- wherein upon administration to a mammal, the compound of Formula (I), or a pharmaceutically acceptable salt thereof, is targeted to tumor cells expressing the GnRHR.
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Dependencies are inferred from the claim text.