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US 10,865,202 B2Granted
Indole derivatives as estrogen receptor degraders
AssigneeArvinas Operations, Inc.
InventorsAndrew P. Crew, Yimin Qian, Hanqing Dong, Jing Wang
Life of this patent
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Abstract
The present disclosure relates to compounds and a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing the compounds, and processes for their preparation. The disclosure also relates to the use of the compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.
Claims20
A compound of formula (I):
- wherein:
- R1 is H, —OH, —OC1-3alkyl, or a halogen;
- R2 is —OH or —OC1-3alkyl;
- R3 is H or an optionally substituted lower alkyl,
- L is one or more covalently connected structural units of -(A)q-, wherein A is a chemical moiety, and q is an integer greater than or equal to 0;
- R4 is a straight chain or branched C1-6alkyl, or C3-6 cycloalkyl;
- R5 is H, or an optionally substituted lower alkyl,
- R6 is 4-methylthiazol-5-yl, oxazol-5-yl, optionally substituted imidazole, optionally substituted pyrazole, optionally substituted oxadiazole, optionally substituted triazole, halogen, or cyano group, or a pharmaceutically acceptable salt thereof.
5 more elements
Dependencies are inferred from the claim text.