公开(公告)号：US20230041951A1

公开(公告)日：2023-02-09

申请号：US17694183

申请日：2022-03-14

申请人： University of Tennessee Research Foundation ,  Oncternal Therapeutics, Inc.

发明人： Ramesh Narayanan ,  Duane D. Miller ,  Thamarai Ponnusamy ,  Dong-Jin Hwang ,  Yali He ,  Jayaprakash Pagadala ,  Christopher C. Coss ,  James T. Dalton ,  Charles B. Duke

IPC分类号： A61K31/404 ,  A61K31/437 ,  A61K31/4184 ,  A61K31/47 ,  A61P35/00 ,  A61K31/403 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/472

摘要： 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.

公开(公告)号：US20200222365A1

公开(公告)日：2020-07-16

申请号：US16556828

申请日：2019-08-30

申请人： University of Tennessee Research Foundation

发明人： Ramesh NARAYANAN ,  Duane D. Miller ,  Thamarai Ponnusamy ,  Dong-Jin Hwang ,  Yali He ,  Jayaprakash Pagadala ,  Christopher C. Coss ,  James T. Dalton ,  Charles B. Duke

IPC分类号： A61K31/404 ,  A61K31/437 ,  A61K31/4184 ,  A61K31/47 ,  A61P35/00 ,  A61K31/403 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/472

摘要： 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.

公开(公告)号：US12128026B2

公开(公告)日：2024-10-29

申请号：US17694183

申请日：2022-03-14

申请人： University of Tennessee Research Foundation ,  Oncternal Therapeutics, Inc.

发明人： Ramesh Narayanan ,  Duane D. Miller ,  Thamarai Ponnusamy ,  Dong-Jin Hwang ,  Yali He ,  Jayaprakash Pagadala ,  Christopher C. Coss ,  James T. Dalton ,  Charles B. Duke

IPC分类号： A61K31/404 ,  A61K31/403 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/47 ,  A61K31/472 ,  A61P35/00

CPC分类号： A61K31/404 ,  A61K31/403 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/47 ,  A61K31/472 ,  A61P35/00

摘要： 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.

公开(公告)号：US11591290B2

公开(公告)日：2023-02-28

申请号：US16776395

申请日：2020-01-29

申请人： ONCTERNAL THERAPEUTICS, INC ,  University of Tennessee Research Foundation

发明人： Ramesh Narayanan ,  Duane D. Miller ,  Thamarai Ponnusamy ,  Dong-Jin Hwang ,  Charles B. Duke ,  Christopher C. Coss ,  Amanda Jones ,  James T. Dalton

IPC分类号： C07C237/00 ,  C07C237/20 ,  A61P35/00 ,  A61P25/00 ,  A61P5/28

摘要： 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.