Bifunctional compound, preparation method therefor, and use thereof
AssigneeSuzhou Kintor Pharmaceuticals, Inc.
InventorYouzhi Tong
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Abstract
The present invention relates to a bifunctional compound, a preparation method therefor, and a use thereof, wherein the bifunctional compound comprises an E3 ubiquitin ligase-binding moiety; a target protein-binding moiety that binds to an androgen receptor; and a linking moiety that links the E3 ubiquitin ligase-binding moiety and the target protein-binding moiety. The bifunctional compound of the present application allows the androgen receptor to be positioned adjacent to the ubiquitin ligase, so as to achieve the degradation or inhibition of the androgen receptor.
Claims13
Bifunctional compounds represented by formula (III) or pharmaceutically acceptable salts, stereoisomers thereof:
- ABM-L-VLM (III),
- wherein ABM is selected from the following structures, wherein represents the point of attachment of the linking moiety:
- L is the chemical linking moiety connecting ABM and VLM, and L is selected from —O—(CH2)m—O—(CH2)n—CO—, —O—(CH2)m—O—(CH2)n—O—(CH2)o—CO—, -(Cy)q-O—(CH2)m—O—(CH2)n—CO—, and -(Cy)q-O—(CH2)m—O—(CH2)n—O—(CH2)o—CO—,
- wherein Cy is selected from C6-10 aryl, C3-6 heteroaryl, C3-6 cycloalkyl and C3-6 heterocycloalkyl, and Cy is optionally substituted with 1, 2 or 3 RCy, and each RCy is independently selected from:
- hydrogen, halogen, cyano, C1-3 alkyl or C1-3 alkoxy optionally substituted with halogen;
- wherein m, n, o are each independently selected from:
- 1, 2, 3, 4;
- and
- VLM is
Dependencies are inferred from the claim text.