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公开(公告)号：US20240336566A1
公开(公告)日：2024-10-10
申请号：US18622152
申请日：2024-03-29
发明人： Chungpin Herman Chen , Maxwell Marco Reeve , Nitinchandra Dahyabhai Patel , Royal J. Haskell, III
IPC分类号： C07D211/88
CPC分类号： C07D211/88
摘要： The present disclosure relates to novel solid forms, including salts and solid forms thereof, of Compound A:
and to processes for their preparation. The disclosure is also directed to pharmaceutical compositions containing at least one salt or salt form and to the therapeutic and/or prophylactic use of such salts, salt forms, and compositions thereof.-
公开(公告)号：US20240335444A1
公开(公告)日：2024-10-10
申请号：US18407150
申请日：2024-01-08
发明人： Dan SHERMAN , Sheryl Maxine GOUGH
IPC分类号： A61K31/506 , A61P35/00
CPC分类号： A61K31/506 , A61P35/00
摘要： This application pertains to the use of compounds, e.g., Compound A:
or a pharmaceutically acceptable salt thereof, for the treatment of various diseases or disorders, including, for example, diffuse large B-cell lymphoma (DLBCL) and angioimmunoblastic T-cell lymphoma.-
公开(公告)号：US12053469B2
公开(公告)日：2024-08-06
申请号：US17207325
申请日：2021-03-19
发明人： Erika Araujo , Michael M. Berlin , Steven M. Sparks , Jing Wang , Wei Zhang
IPC分类号： A61K31/506 , A61K31/496 , A61K31/5377 , A61K45/06 , A61P25/16 , C07D401/14 , C07D413/14 , C07D487/10
CPC分类号： A61K31/506 , A61K31/496 , A61K31/5377 , A61K45/06 , A61P25/16 , C07D401/14 , C07D413/14 , C07D487/10
摘要： Bifunctional compounds, which find utility as modulators of leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
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公开(公告)号：US20240180900A1
公开(公告)日：2024-06-06
申请号：US18493773
申请日：2023-10-24
发明人： Ronald PECK , Sarah Deborah CHIRNOMAS , Edward CHAN , Richard Walter GEDRICH , Elmer J. BERGHORN, Jr. , Jeanette Toni ALICEA , Lawrence B. SNYDER , SangHyun LEE , Taavi NEKLESA
IPC分类号： A61K31/496 , A61K31/573 , A61K31/58 , A61P35/00
CPC分类号： A61K31/496 , A61K31/573 , A61K31/58 , A61P35/00
摘要： This disclosure pertains to methods of treating prostate cancer in a subject, including prostate cancer comprising at least one somatic AR tumor mutation, such as metastatic prostate cancer, castrate-resistant prostate cancer, metastatic castrate-resistant prostate cancer, progressive metastatic castrate-resistant prostate cancer, castrate-sensitive prostate cancer, metastatic castrate-sensitive prostate cancer, prostate cancer naïve to novel hormonal agents (NHAs), metastatic prostate cancer naïve NHAs, castrate-resistant prostate cancer naïve to NHAs, castrate-sensitive prostate cancer naïve to NHAs, metastatic castrate-resistant prostate cancer naïve to NHAs, and metastatic castrate-sensitive prostate cancer naïve to NHAs, wherein the method comprises administering to a subject in need thereof a therapeutically effective amount of Compound A, or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US11981683B2
公开(公告)日：2024-05-14
申请号：US17699082
申请日：2022-03-19
发明人： Erika Marina Vieira Araujo , Michael Berlin , Hanqing Dong , Steven M. Sparks , Jing Wang , Wei Zhang
IPC分类号： C07D401/14 , A61K45/06 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/08 , C07D487/10 , C07D498/10
CPC分类号： C07D498/10 , A61K45/06 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/08 , C07D487/10
摘要： Bifunctional compounds, which find utility as modulators of leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
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公开(公告)号：US20240131023A1
公开(公告)日：2024-04-25
申请号：US18460063
申请日：2023-09-01
发明人： LAWRENCE B. Snyder , Andrew P. Crew , Jing Wang , Hanqing Dong
IPC分类号： A61K31/496 , A61K31/167 , A61K31/277 , A61K31/337 , A61K31/417 , A61K31/4523 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/5386 , A61K31/57 , A61K31/661 , A61K31/663 , A61K31/675 , A61K38/09 , A61K47/54 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D498/10
CPC分类号： A61K31/496 , A61K31/167 , A61K31/277 , A61K31/337 , A61K31/417 , A61K31/4523 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/5386 , A61K31/57 , A61K31/661 , A61K31/663 , A61K31/675 , A61K38/09 , A61K47/545 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D498/10
摘要： This disclosure pertains to compounds, the preparation thereof, and the use of these compounds in the treatment of prostate cancer, including metastatic and/or castrate-resistant prostate cancer, in subjects in need thereof.
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公开(公告)号：US11957759B1
公开(公告)日：2024-04-16
申请号：US18243177
申请日：2023-09-07
发明人： Keith R. Hornberger
CPC分类号： A61K47/55 , A61K47/545
摘要： Provided herein are bifunctional compounds having the chemical structure I:
PTM-L-CLM (I):
or pharmaceutically acceptable salts thereof, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (Raf, such as c-Raf, A-Raf, and/or B-RAF) and are useful in the treatment of a variety of Raf mediated conditions or diseases, such as cancer, specifically lung cancer, skin cancer, or colorectal cancer.-
公开(公告)号：US20240091204A1
公开(公告)日：2024-03-21
申请号：US18309867
申请日：2023-09-18
发明人： Andrew P. Crew , Hanqing Dong , Michael Berlin , Steven M. Sparks
IPC分类号： A61K31/427 , A61K31/4035 , A61K31/4245 , A61K31/437 , A61K31/4439 , A61K31/496 , A61K31/541 , A61K47/54
CPC分类号： A61K31/427 , A61K31/4035 , A61K31/4245 , A61K31/437 , A61K31/4439 , A61K31/496 , A61K31/541 , A61K47/555
摘要： The present disclosure relates to bifunctional compounds, which find utility as modulators of α-synuclein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon. Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
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公开(公告)号：US11707452B2
公开(公告)日：2023-07-25
申请号：US16545983
申请日：2019-08-20
发明人： Andrew P. Crew , Hanqing Dong , Michael Berlin , Steven M. Sparks
IPC分类号： A61K31/427 , A61K47/54 , A61K31/4035 , A61K31/4245 , A61K31/437 , A61K31/4439 , A61K31/496 , A61K31/541
CPC分类号： A61K31/427 , A61K31/4035 , A61K31/4245 , A61K31/437 , A61K31/4439 , A61K31/496 , A61K31/541 , A61K47/555
摘要： The present disclosure relates to bifunctional compounds, which find utility as modulators of α-synuclein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon. Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
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公开(公告)号：US20230203030A1
公开(公告)日：2023-06-29
申请号：US17931814
申请日：2022-09-13
发明人： Andrew P. Crew , Craig M. Crews , Xin Chen , Hanqing Dong , Caterina Ferraro , Yimin Qian , Kam Siu , Jing Wang , Meizhong Jin , Michael Berlin , Kurt Zimmermann , Lawrence Snyder
IPC分类号： C07D471/04 , C07D417/14 , A61K45/06 , C07D417/12 , C07D403/06 , C07D403/14 , C07D401/14 , C07D413/14 , C07D405/14 , C07D495/04
CPC分类号： C07D471/04 , A61K45/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D495/04
摘要： The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.
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