University of Tennessee Research Foundation

Gtx Corporation

The Ohio State University

Oncternal Therapeutics, Inc.

Molecular Design International, Inc.

Other

University of Mississippi

University of Memphis

Duane Douglas Miller

James T Dalton

Yali He

Ramesh Narayanan

Thamarai Ponnusamy

Dong-Jin Hwang

Wei Li

Charles B Duke

Karen A Veverka

Christopher C Coss

Donghua Yin

Mitchell S Steiner

Charles Ryan Yates

Sunjoo Ahn

Jianjun Chen

Jayaprakash Pagadala

Arnab Mukherjee

Leonid I Kirkovsky

Michael L Mohler

Chien-Ming Li

Gabor G Tigyi

Seoung-Soo Hong

Dennis R Feller

Amanda Jones

Yan Lu

Zhongzhi Wu

Igor Rakov

Renukadevi Patil

Jordan J Toutounchian

Wenqing Gao

Min Xiao

Zhao Wang

Tamas Virag

Bob M Moore, Ii

Suni Mustafa

Karl J Romstedt

Karin Emmons Thompson

Victor Nikulin

Oleg Kirichenko

Seoung Sung Hong

Gyong Suk Kang

Veeresa Gududuru

Eunju Hurh

Jeffrey D Kearbey

Eldon Geisert

Shivaputra Appanna Patil

Michael T Clark

Gamal Shams

Adeboye Adejare

Kui Zeng

Christina Barrett

Eldon E Geisert, Jr

Craig A Marhefka

Gangadhar G Durgam

Jena Steinle Smith

Souvik Banerjee

Michelle D Walker

Ryoko Tsukahara

Dong Jin Hwang

Jiyun Chen

Jin Wang

Hao Wu

David John Fischer

Charles G Brown

Daniel Lee Baker

Abby Louise Parrill-Baker

Jianjuan Chen

Christina Herring

Supriya A Bavadekar

Dick Gourley

Pengfei Song

Vineet M Sardar

Don B Elrod

Huiping Xu

Dean Wang

Terreia Jones

Karoly Liliom

Nora Nusser

Amira Ahmed

Weiping Zheng

Likeselam Asres

Ram Mahato

Devesh Srivastava

Lawrence M Pfeffer

Debolina Ganguly

James Fells

Satyanarayana Pochampally

Mostafa Waleed Gaber

Kinsie E Arnst

Renuka Gupte

Jeff Kearbey

Frank Park

Casey Bohl

Vanessa Morales-Tirado

Kiwon Chung

Bilal Abou Aleiwi

The invention encompasses novel dihydroquinoxalinone compounds with significantly improved water solubility and reduced toxicity to achieve higher therapeutic indexes and the treatment of cancer, virus infections, and inflammation using the same.

Metabolically stable pyrimidinyl dihydroquinoxalinones as tubulin polymerization inhibitors

Novel inhibitors of the bromodomain of Brahma-related gene 1 (BRG1) are described. Also described are methods of treating glioblastoma using inhibitors of the BRG1 bromodomain in combination with chemotherapeutics, such as DNA alkylating agents. As described herein, the inhibitors sensitize glioblastoma cells, including chemoresistant glioblastoma cells, to DNA alkylating agents, for example, temozolomide and carmustine.

Bromodomain inhibitors to target therapy-resistant cancer

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.

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

This invention is directed to selective androgen receptor degrader (SARD) compounds including heterocyclic rings 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, Kennedys 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 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

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.

This invention is directed to selective androgen receptor degrader (SARD) compounds pharmaceutical compositions and uses thereof in treating early prostate cancer, 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 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

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.

This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including cyclic and heterocyclic anilide rings and their synthetic precursors, and mono-, di-, or multi-substituted N-heterocyclic rings, R-isomers, non-hydroxylated and/or non-chiral propanamides in treating androgen receptor dependent diseases and conditions such as hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, 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 or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

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 propanamides, 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 or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

The present disclosure provides novel ATX inhibitors, and pharmaceutical compositions comprising said inhibitors, as well as methods of treatment comprising administration of said inhibitors.

Autotaxin inhibitors

Growing community of inventors

Germantown, TN, United States of America

Duane Douglas Miller