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公开(公告)号：US20210340122A1
公开(公告)日：2021-11-04
申请号：US17273726
申请日：2019-09-05
IPC分类号： C07D401/12 , C07D231/16 , A61P35/00 , A61P5/28
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.
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公开(公告)号：US20200039924A1
公开(公告)日：2020-02-06
申请号：US16425865
申请日：2019-05-29
IPC分类号： C07C235/64
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.
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公开(公告)号：US20180273470A1
公开(公告)日：2018-09-27
申请号：US15887076
申请日：2018-02-02
IPC分类号： C07C255/54
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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公开(公告)号：US20210196678A1
公开(公告)日：2021-07-01
申请号：US17055988
申请日：2019-05-16
IPC分类号： A61K31/404 , A61K31/416 , A61K31/4192 , A61K31/4155 , A61K31/277 , A61K31/336 , A61K31/4439 , A61K45/06 , 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.
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5.发明申请SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 有权选择性受体降解剂（SARD）配体及其使用方法公开(公告)号：US20170050921A1
公开(公告)日：2017-02-23
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 , A61K31/277 , A61K9/00
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。
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公开(公告)号：US20170014371A1
公开(公告)日：2017-01-19
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.
摘要翻译： 本发明涉及取代的酰基酰苯胺化合物及其用于治疗肌营养不良症如杜氏肌营养不良症和贝克肌营养不良症，以及改善或维持患有杜氏肌营养不良症的受试者的肺功能和心脏功能。
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公开(公告)号：US20210161864A1
公开(公告)日：2021-06-03
申请号：US17007143
申请日：2020-08-31
IPC分类号： A61K31/4164 , A61K31/40 , A61P35/00 , A61K31/415 , A61K31/4439 , A61K31/4196 , A61K31/5375
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：US20190144387A1
公开(公告)日：2019-05-16
申请号：US16122862
申请日：2018-09-05
IPC分类号： C07D209/08 , C07D209/42 , C07D401/12 , C07D235/06 , C07D471/04 , C07D231/56 , C07D249/18 , C07D215/06 , C07D217/04 , C07D209/88 , C07D209/86 , A61P35/00 , A61P25/00 , A61P17/10 , A61P17/14 , A61P5/26
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：US20190015387A1
公开(公告)日：2019-01-17
申请号：US15981849
申请日：2018-05-16
IPC分类号： A61K31/4164 , A61P35/00 , A61K31/40 , A61K31/415 , A61K31/5375 , A61K31/4196 , A61K31/4439 , A61K31/44 , A61K31/517 , A61K31/277 , A61K31/655 , A61K31/4192 , A61K31/41
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：US20180273487A1
公开(公告)日：2018-09-27
申请号：US15923668
申请日：2018-03-16
IPC分类号： C07D231/16 , A61K31/415 , 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 , A61K31/4192
CPC分类号： C07D231/16 , A61K9/0014 , A61K31/277 , A61K31/40 , A61K31/415 , A61K31/4164 , A61K31/4192 , A61K31/4196 , A61K31/44 , A61K31/4439 , A61K31/517 , A61K31/5375 , A61K45/06 , C07C255/60 , C07C317/46 , C07D207/06 , C07D207/34 , C07D209/08 , C07D213/84 , C07D233/68 , C07D239/74 , C07D249/04 , C07D249/08 , C07D295/15 , C07D401/12
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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