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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：US10300037B2
公开(公告)日：2019-05-28
申请号：US15786811
申请日：2017-10-18
IPC分类号： A61K31/277 , A61K45/06
摘要： This invention is directed to substituted acylanilide compounds and uses thereof in treating muscular dystrophies such as Duchenne muscular dystrophy and Becker muscular dystrophy and in improving or preserving lung function and cardiac function in a subject suffering from Duchenne muscular dystrophy.
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公开(公告)号：US20190040000A1
公开(公告)日：2019-02-07
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： C07C237/20 , A61P25/00 , A61P5/28 , A61P35/00
CPC分类号： C07C237/20 , A61P5/28 , A61P25/00 , A61P35/00
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 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：US09730908B2
公开(公告)日：2017-08-15
申请号：US14963054
申请日：2015-12-08
IPC分类号： A61K31/277 , C07C255/60 , A23K20/111 , A23K50/10 , A23K50/30 , A23K50/75 , A23K50/80
CPC分类号： A61K31/277 , A23K20/111 , A23K50/10 , A23K50/30 , A23K50/75 , A23K50/80 , C07C255/60
摘要： This invention is directed to 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.
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公开(公告)号：US11648234B2
公开(公告)日：2023-05-16
申请号：US17007143
申请日：2020-08-31
IPC分类号： A61K31/4164 , A61K31/40 , A61K31/415 , A61P35/00 , A61K31/4196 , A61K31/4439 , A61K31/5375
CPC分类号： A61K31/4164 , A61K31/40 , A61K31/415 , A61K31/4196 , A61K31/4439 , A61K31/5375 , A61P35/00
摘要： 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.
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公开(公告)号：US20230146829A1
公开(公告)日：2023-05-11
申请号：US17894482
申请日：2022-08-24
IPC分类号： A61K31/404 , A61K31/4245 , A61K31/416 , A61K31/4439 , A61K31/422 , A61K31/4188 , A61K31/415 , A61K31/4192
CPC分类号： A61K31/404 , A61K31/4245 , A61K31/416 , A61K31/4439 , A61K31/422 , A61K31/4188 , A61K31/415 , A61K31/4192
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.
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公开(公告)号：US20230115515A1
公开(公告)日：2023-04-13
申请号：US17957539
申请日：2022-09-30
IPC分类号： A61K31/415 , A61K31/4439 , A61K31/517 , A61K31/4192 , A61K31/506 , A61K31/422 , A61P35/00
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.
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