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公开(公告)号：US20230002326A1
公开(公告)日：2023-01-05
申请号：US17582851
申请日：2022-01-24
IPC分类号： C07D231/16 , A61K31/4192 , A61K9/00 , A61K45/06 , C07D207/34 , A61K31/40 , C07D233/68 , A61K31/4164 , C07D207/06 , C07D295/15 , A61K31/5375 , C07D249/08 , A61K31/4196 , C07D213/84 , A61K31/44 , C07D239/74 , A61K31/517 , C07C255/60 , A61K31/277 , C07D401/12 , A61K31/4439 , C07D249/04 , A61K31/415 , C07C317/46 , C07D209/08
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 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 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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公开(公告)号：US10010521B2
公开(公告)日：2018-07-03
申请号：US15153690
申请日：2016-05-12
IPC分类号： A61K31/277 , C07C255/60 , A23K20/111 , A23K50/10 , A23K50/75 , A23K50/30 , 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 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：US09844528B2
公开(公告)日：2017-12-19
申请号：US15190732
申请日：2016-06-23
IPC分类号： A61K31/277 , A61K45/06
CPC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：US12128026B2
公开(公告)日：2024-10-29
申请号：US17694183
申请日：2022-03-14
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.
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公开(公告)号：US11591290B2
公开(公告)日：2023-02-28
申请号：US16776395
申请日：2020-01-29
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.
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公开(公告)号：US10806719B2
公开(公告)日：2020-10-20
申请号：US15981849
申请日：2018-05-16
IPC分类号： A61K31/4164 , A61K31/40 , A61K31/415 , A61K31/5375 , A61K31/4196 , A61K31/41 , A61K31/44 , A61K31/517 , A61K31/277 , A61K31/655 , A61K31/4192 , A61K31/4439 , C07D209/08 , C07D213/75 , C07D231/18 , C07D231/40 , C07D233/56 , C07D303/48 , C07D249/06 , C07D231/12 , C07D207/32 , C07D231/38 , C07D249/14 , C07D207/33 , C07D257/04 , C07D213/84 , C07D231/16 , C07D233/68 , C07D401/12 , C07D239/74 , C07D249/08 , C07D207/06 , C07D207/34 , C07D295/15 , A61P35/00 , C07C317/46 , C07C255/60 , C07D249/04
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.
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公开(公告)号：US10654809B2
公开(公告)日：2020-05-19
申请号：US15923668
申请日：2018-03-16
IPC分类号： C07D231/16 , C07D207/34 , C07D233/68 , C07D207/06 , C07D295/15 , C07D249/08 , C07D213/84 , C07D239/74 , C07D401/12 , C07D249/04 , C07D209/08 , C07C317/46 , C07C255/60 , A61K31/4192 , A61K9/00 , A61K45/06 , A61K31/40 , A61K31/4164 , A61K31/5375 , A61K31/4196 , A61K31/44 , A61K31/517 , A61K31/277 , A61K31/4439 , A61K31/415
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.
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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：US09884038B2
公开(公告)日：2018-02-06
申请号：US14963130
申请日：2015-12-08
IPC分类号： A61K31/277
CPC分类号： C07C255/54 , A61K31/277
摘要： This invention provides 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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