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

Invented by: Ramesh Narayanan
Cordova, TN

Duane D. Miller
Collierville, TN

Thamarai Ponnusamy
Memphis, TN

Dong-Jin Hwang
Arlington, TN

Jayaprakash Pagadala
Boca Raton, FL

Charles B. Duke
Memphis, TN

Christopher C. Coss
Upper Arlington, OH

James T. Dalton
Ann Arbor, MI

Yali He
Germantown, TN Applicant: Name City State Country Type GTx, Inc. University of Tennessee Research Foundation Memphis Knoxville TN TN US US

Originally Assigned to: GTX, INC.
Memphis, TN Family ID: 1000003438873
[Now assigned to . . .]

Issued:2018-07-31
Filed:2016-10-21
Application No:15331777
Examined by:Seaman; D Margaret M

This invention provides novel indole, indazole, benzimidazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

[pdf] U.S. Pat. No. 10,035,763

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