Selective androgen receptor degrader (SARD) ligands and methods of use thereof

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United States of America

PATENT NO 12215086
APP PUB NO 20230002326A1
SERIAL NO

17582851

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Abstract

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This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors. R-isomers, and non-hydroxylated and/or non-chiral propenamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic to or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

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Patent Owner(s)

  • UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
He, Yali Germantown, US 44 1310
Hwang, Dong-Jin Arlington, US 30 254
Miller, Duane D Collierville, US 179 4313
Narayanan, Ramesh Cordova, US 56 684
Ponnusamy, Thamarai Memphis, US 34 267

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