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公开(公告)号：US10093613B2
公开(公告)日：2018-10-09
申请号：US15830688
申请日：2017-12-04
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： C07C237/20 , 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 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.
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公开(公告)号：US09814698B2
公开(公告)日：2017-11-14
申请号：US15135334
申请日：2016-04-21
发明人： Ramesh Narayanan , Duane D. Miller , Thamarai Ponnusamy , Dong-Jin Hwang , Jayaprakash Pagadala , Charles B. Duke , Christopher C. Coss , James T. Dalton , Yali He
IPC分类号： A61K31/404 , A61K9/00 , A61K31/437 , A61K31/4184 , A61K31/47 , A61K31/472 , A61K31/403 , A61K31/416
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.
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公开(公告)号：US20170166526A1
公开(公告)日：2017-06-15
申请号：US15331777
申请日：2016-10-21
发明人： Ramesh Narayanan , Duane D. Miller , Thamarai Ponnusamy , Dong-Jin Hwang , Jayaprakash Pagadala , Charles B. Duke , Christopher C. Coss , James T. Dalton , Yali He
IPC分类号： C07D209/08 , C07D209/42 , C07D215/00 , C07D471/04 , C07D231/56 , C07D217/04 , A61K9/00 , C07D235/04
CPC分类号： C07D209/08 , A61K9/0014 , C07D209/42 , C07D209/86 , C07D209/88 , C07D215/00 , C07D215/06 , C07D217/04 , C07D231/56 , C07D235/04 , C07D235/06 , C07D471/04
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, 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.
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公开(公告)号：US10441570B2
公开(公告)日：2019-10-15
申请号：US15981636
申请日：2018-05-16
发明人： Ramesh Narayanan , Duane D. Miller , Thamarai Ponnusamy , Dong-Jin Hwang , Yali He , Jayaprakash Pagadala , Charles B. Duke , Christopher C. Coss , James T. Dalton
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.
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公开(公告)号：US10035763B2
公开(公告)日：2018-07-31
申请号：US15331777
申请日：2016-10-21
发明人： Ramesh Narayanan , Duane D. Miller , Thamarai Ponnusamy , Dong-Jin Hwang , Jayaprakash Pagadala , Charles B. Duke , Christopher C. Coss , James T. Dalton , Yali He
IPC分类号： C07D209/08 , A61K9/00 , C07D209/42 , C07D235/04 , C07D471/04 , C07D231/56 , C07D217/04 , C07D215/00
CPC分类号： C07D209/08 , A61K9/0014 , C07D209/42 , C07D209/86 , C07D209/88 , C07D215/00 , C07D215/06 , C07D217/04 , C07D231/56 , C07D235/04 , C07D235/06 , C07D471/04
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, 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.
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公开(公告)号：US10597354B2
公开(公告)日：2020-03-24
申请号：US16153193
申请日：2018-10-05
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： A61P25/00 , C07C237/20 , A61P35/00 , 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.
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公开(公告)号：US10017471B2
公开(公告)日：2018-07-10
申请号：US15222734
申请日：2016-07-28
发明人： Ramesh Narayanan , Duane D. Miller , Thamarai Ponnusamy , Dong-Jin Hwang , Jayaprakash Pagadala , Charles B. Duke , Christopher C. Coss , James T. Dalton , Yali He
IPC分类号： C07D209/08 , C07D209/42 , C07D235/04 , C07D471/04 , C07D231/56 , C07D217/04 , C07D215/00
CPC分类号： C07D209/08 , C07D209/42 , C07D215/00 , C07D217/04 , C07D231/56 , C07D235/04 , C07D471/04
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, 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.
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公开(公告)号：US09834507B2
公开(公告)日：2017-12-05
申请号：US15331751
申请日：2016-10-21
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： C07C255/60 , A61K9/00 , A61K31/277
CPC分类号： C07C255/60 , A61K9/0014 , A61K31/277 , A61K45/06 , C07B2200/07 , A61K2300/00
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.
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公开(公告)号：US09815776B2
公开(公告)日：2017-11-14
申请号：US15135151
申请日：2016-04-21
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： C07C255/58 , C07C255/60 , A61K9/00 , A61K31/277
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.
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公开(公告)号：US11273147B2
公开(公告)日：2022-03-15
申请号：US16556828
申请日：2019-08-30
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.
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