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1. 发明申请

WO2016172330A1 SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：选择性受体降解剂（SARD）配体及其使用方法
公开(公告)号：WO2016172330A1
公开(公告)日：2016-10-27
申请号：PCT/US2016/028623
申请日：2016-04-21
申请人： GTX, INC. , UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
发明人： NARAYANAN, Ramesh , MILLER, Duane D. , PONNUSAMY, Thamarai , HWANG, Dong-Jin , DUKE, Charles B. , COSS, Christopher C. , JONES, Amanda , DALTON, James T.
IPC分类号： A61K31/277 , A61P35/00 , C07C13/47
CPC分类号： C07C255/58 , A61K9/0014 , A61K31/277 , C07B2200/07 , C07C255/60
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 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.
摘要翻译：本发明提供新颖的3-氨基丙酰胺选择性雄激素受体降解物（SARD）化合物，药物组合物及其在治疗前列腺癌，晚期前列腺癌，抗阉割前列腺癌，雄激素性脱发或其它高雄激素性皮肤疾病中的用途，肯尼迪氏症，肌萎缩性侧索硬化（ALS）和子宫肌瘤，以及用于降低包括致病性或抗性突变的雄激素受体全长（AR-FL）水平的AR-剪接变体（AR-SV）和致病性多聚谷氨酰胺（polyQ）多态性的方法 AR在一个主题。

2. 发明申请

WO2019222556A1 SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2019222556A1
公开(公告)日：2019-11-21
申请号：PCT/US2019/032751
申请日：2019-05-16
申请人： GTX, INC. , UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
发明人： NARAYANAN, Ramesh , MILLER, Duane, D. , PONNUSAMY, Thamarai , HWANG, Dong-Jin , HE, Yali
IPC分类号： A61K31/277 , A61K31/167 , A61K31/404 , A61P35/00 , A61P35/04
摘要： 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.

3. 发明申请

WO2016172358A1 SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：选择性受体降解剂（SARD）配体及其使用方法
公开(公告)号：WO2016172358A1
公开(公告)日：2016-10-27
申请号：PCT/US2016/028674
申请日：2016-04-21
申请人： GTX, INC. , UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
发明人： NARAYANAN, Ramesh , MILLER, Duane D. , PONNUSAMY, Thamarai , HWANG, Dong-Jin , HE, Yali , PAGADALA, Jayaprakash , DUKE, Charles B. , COSS, Christopher C. , DALTON, James T.
IPC分类号： C07C271/02 , A61K45/06 , A61K31/325
CPC分类号： A61K31/404 , A61K9/0014 , A61K31/403 , A61K31/405 , A61K31/416 , A61K31/4184 , A61K31/437 , A61K31/47 , A61K31/472 , A61K45/06 , C07C271/02 , C07D209/08 , C07D209/42 , C07D215/18 , C07D217/04 , C07D231/56 , C07D235/16 , C07D487/04
摘要： 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, androgenic alopecia or other hyper androgenic 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 and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
摘要翻译：本发明提供新型吲哚，吲唑，苯并咪唑，二氢吲哚，喹诺酮，异喹啉和咔唑选择性雄激素受体降解物（SARD）化合物，药物组合物及其在治疗前列腺癌，晚期前列腺癌，去势抗性前列腺癌，雄激素性脱发或其他高雄激素性皮肤疾病，肯尼迪氏病，肌萎缩性侧索硬化症（ALS）和子宫肌瘤，以及用于降低雄激素受体全长（AR-FL）水平的方法，包括致病和/或抗性突变，AR-剪接变体 AR-SV）和AR的病原性多聚谷氨酰胺（polyQ）多态性。

4. 发明申请

WO2021173721A1 SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2021173721A1
公开(公告)日：2021-09-02
申请号：PCT/US2021/019477
申请日：2021-02-24
申请人： UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
发明人： NARAYANAN, Ramesh , PONNUSAMY, Thamarai , MILLER, Duane D. , HE, Yali , HWANG, Dong-Jin
IPC分类号： A61K31/404 , C07D209/30 , A61P35/00
摘要： 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, 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.

5. 发明申请

WO2021173731A1 SELECTIVE ANDROGEN RECEPTOR COVALENT ANTAGONISTS (SARCAS) AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2021173731A1
公开(公告)日：2021-09-02
申请号：PCT/US2021/019490
申请日：2021-02-24
申请人： UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
发明人： NARAYANAN, Ramesh , PONNUSAMY, Thamarai , MILLER, Duane D. , HE, Yali , HWANG, Dong-Jin
IPC分类号： A61K31/325 , A61K45/06 , C07C271/02
摘要： This invention relates to selective androgen receptor covalent antagonists, synthetic intermediates and by-products, and related compounds, and compositions comprising the same, and uses thereof 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.

6. 发明申请

WO2021202936A1 PYRAZOLYLPROPANAMIDE COMPOUNDS AND USES THEREOF FOR TREATMENT OF PROSTATE CANCER 审中-公开
公开(公告)号：WO2021202936A1
公开(公告)日：2021-10-07
申请号：PCT/US2021/025468
申请日：2021-04-01
申请人： UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
发明人： NARAYANAN, Ramesh , MILLER, Duane D. , HE, Yali , PONNUSAMY, Thamarai , HWANG, Dong-Jin
IPC分类号： A61K31/167 , A61K31/415 , A61P35/00 , A61K31/4155 , A61K31/4192 , A61K31/422 , A61K31/4439 , A61K31/506 , A61K31/517 , A61K45/06
摘要： This invention relates to pyrazolylpropanamide compounds and uses thereof for treatment of prostate cancer, advanced prostate cancer, refractory prostate cancer, AR overexpressing prostate cancer, castration-resistant prostate cancer, castration-sensitive prostate cancer, AR-V7 expressing prostate cancer, or d567ES expressing prostate cancer, darolutamide resistant prostate cancer, enzalutamide resistant prostate cancer, apalutamide resistant prostate cancer, or abiraterone resistant prostate cancer.

7. 发明申请

WO2020243373A1 SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2020243373A1
公开(公告)日：2020-12-03
申请号：PCT/US2020/035015
申请日：2020-05-28
申请人： UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
发明人： NARAYANAN, Ramesh , MILLER, Duane D. , PONNUSAMY, Thamarai , HWANG, Dong-Jin , HE, Yali
IPC分类号： C07C237/20 , A61K31/167 , A61P5/28
摘要： 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.

8. 发明申请

WO2017214634A1 SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：选择性雄激素受体降解物（SARD）配体及其使用方法
公开(公告)号：WO2017214634A1
公开(公告)日：2017-12-14
申请号：PCT/US2017/037063
申请日：2017-06-12
申请人： UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
发明人： NARAYANAN, Ramesh , MILLER, Duane , PONNUSAMY, Thamarai , HWANG, Dong-Jin , HE, Yali
IPC分类号： A61K31/325 , C07C271/02
摘要： 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.
摘要翻译：本发明涉及吡咯，吡唑，咪唑，三唑和基于吗啉的选择性雄激素受体降解剂（SARD）化合物，包括杂环酰苯胺环及其合成前体，R- 异构体和非羟基化和/或非手性丙酰胺，以及其在治疗前列腺癌，晚期前列腺癌，去势抵抗性前列腺癌，三阴性乳腺癌，表达雄激素受体的其他癌症，雄激素性脱发或其他高雄激素性皮肤病，肯尼迪氏病，肌萎缩性侧索硬化症（ALS），腹主动脉瘤（AAA）和子宫肌瘤，以及降低包括致病性或抗性突变在内的雄激素受体全长（AR-FL）（AR-SV）和AR的致病性聚谷氨酰胺（polyQ）多态性。

9. 发明申请

WO2020051344A1 SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2020051344A1
公开(公告)日：2020-03-12
申请号：PCT/US2019/049769
申请日：2019-09-05
申请人： UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
发明人： NARAYANAN, Ramesh , MILLER, Duane D. , HE, Yali , HWANG, Dong-Jin , PONNUSAMY, Thamarai
IPC分类号： C07D231/16 , A61K31/415 , A61P5/00 , A61P5/26 , A61P9/00 , A61P15/08 , A61P17/00 , A61P17/10 , A61P21/00 , A61P35/00
摘要： 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.

10. 发明申请

WO2020051260A1 SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2020051260A1
公开(公告)日：2020-03-12
申请号：PCT/US2019/049618
申请日：2019-09-05
申请人： UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
发明人： NARAYANAN, Ramesh , MILLER, Duane D. , PONNUSAMY, Thamarai , HWANG, Dong-Jin , HE, Yali
IPC分类号： C07D209/08 , A61P5/26 , C07D401/12 , C07D235/06 , C07D471/04 , C07D231/56 , C07D249/18 , C07D215/06 , C07D217/04 , C07D209/88
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 pro static 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 poly glutamine (polyQ) polymorphisms of AR in a subject.

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