University of Tennessee Research Foundation

Gtx Corporation

Oncternal Therapeutics, Inc.

The Ohio State University

The United States Government As Represented by the Department of Veterans Affairs

James T Dalton

Duane Douglas Miller

Ramesh Narayanan

Mitchell S Steiner

Yali He

Thamarai Ponnusamy

Sunjoo Ahn

Charles B Duke

Christopher C Coss

Dong-Jin Hwang

Wei Li

Karen A Veverka

Donghua Yin

Seoung-Soo Hong

Arnab Mukherjee

Leonid I Kirkovsky

Jianjun Chen

Jayaprakash Pagadala

Chien-Ming Li

David A Dickason

Tai Ahn

Thomas G Bird

Michael L Mohler

Yan Lu

Amanda Jones

Zhongzhi Wu

Wenqing Gao

Jin Wang

Zhao Wang

Jeetendra Eswaraka

Min Xiao

Igor Rakov

Jeffrey D Kearbey

Craig A Marhefka

Christina Barrett

Jiyun Chen

Dong Jin Hwang

Veeresa Gududuru

Eunju Hurh

Ching-Shih Chen

David John Fischer

John C Byrd

Natarajan Muthusamy

Daniel Lee Baker

Gabor G Tigyi

Danilo Perrotti

Tamas Virag

Frank Frissora

Nora Nusser

Vineet M Sardar

Don B Elrod

Karoly Liliom

Huiping Xu

Dean Wang

David Hong

Kiwon Chung

Muralimohan Yepuru

Robert H Getzenberg

Ellis Levin

Jianjuan Chen

Ronald A Morton

Christina Herring

Devesh Srivastava

Xiaobin Zhao

Qing Liu

Jeff Kearbey

Casey Bohl

Dave Dickason

Li Wei

Juhyun Kim

This invention provides novel indole, indazole, benzimidazole, benzotriazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, 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.

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

This invention relates to the treatment of breast cancer in a subject, for example a female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer; advanced breast cancer; breast cancer that has failed selective estrogen receptor modulator (SERM) (tamoxifen, toremifene, raloxifene), gonadotropin-releasing hormone (GnRH) agonist (goserelin), aromatase inhibitor (AI) (letrozole, anastrozole, exemestane), cyclin-dependent kinase 4/6 (CDK 4/6) inhibitor (palbociclib (Ibrance), ribociclib (Kisqali), abemaciclib (Vorzenio)), mTOR inhibitor (everolimus), trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, neratinib (Nerlynx), olaparib (Lynparza) (an inhibitor of the enzyme poly ADP ribose polymerase (PARP)), bevacizumab (Avastin), and/or fulvestrant treatments; metastasis in a subject suffering from breast cancer; HER2-positive; treating a subject suffering from ER mutant expressing breast cancer and/or treating breast cancer in a subject, by first determining theF-16β-fluoro-5α-dihydrotestosterone (F-DHT) tumor uptake and identifying said subject as having AR-positive breast cancer based onF-DHT tumor uptake, comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.

Treatment of skeletal-related events for breast cancer patients

The present invention relates to solid forms of (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide and process for producing the same.

Solid forms of selective androgen receptor modulators

This invention provides novel 3-amino propanamide selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, androgenic alopecia or other 5 hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.

Compounds for treatment of cancer

The present invention relates to solid forms of (S)&#x2014;N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide and process for producing the same.

The present invention relates to a compound of formula XXII and a compound of formula 17ya, which are defined as anywhere in the specification, to a composition comprising the same, and to a method of using thereof in the treatment of various forms of cancer.

This invention relates to the treatment of breast cancer in a subject, for example a female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer; advanced breast cancer; breast cancer that has failed selective estrogen receptor modulator (SERM) (tamoxifen, toremifene, raloxifene), gonadotropin-releasing hormone (GnRH) agonist (goserelin), aromatase inhibitor (AI) (letrozole, anastrozole, exemestane), cyclin-dependent kinase 4/6 (CDK 4/6) inhibitor (palbociclib (Ibrance), ribociclib (Kisqali), abemaciclib (Vorzenio)), mTOR inhibitor (everolimus), trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, neratinib (Nerlynx), olaparib (Lynparza) (an inhibitor of the enzyme poly ADP ribose polymerase (PARP)), bevacizumab (Avastin), and/or fulvestrant treatments; metastasis in a subject suffering from breast cancer; HER2-positive; treating a subject suffering from ER mutant expressing breast cancer and/or treating breast cancer in a subject, by first determining theF-16&#x3b2;-fluoro-5&#x3b1;-dihydrotestosterone (F-DHT) tumor uptake and identifying said subject as having AR-positive breast cancer based onF-DHT tumor uptake, comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.

Non-invasive method of evaluating breast cancers for selective androgen receptor modulator (SARM) therapy

This invention provides substituted acylanilide compounds and uses thereof in treating a variety of diseases or conditions in a subject including, inter alia, a muscle wasting disease and/or disorder such as Duchenne muscular dystrophy or Becker muscular dystrophy.

Selective androgen receptor modulator and methods of use thereof

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

This invention relates to the treatment of breast cancer in a subject, for example a female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer; advanced breast cancer; breast cancer that has failed SERM (tamoxifen, toremifene), aromatase inhibitor, palbociclib (Ibrance), trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and/or fulvestrant treatments; metastasis in a subject suffering from breast cancer; and/or HER2-positive; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.

Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS)

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Lakeland, TN, United States of America

James T Dalton