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公开(公告)号:US09771349B2
公开(公告)日:2017-09-26
申请号:US14858170
申请日:2015-09-18
发明人: Jian Lin , Anna Ericsson , Ann-Marie Campbell , Gary Gustafson , Zhongguo Wang , R. Bruce Diebold , Susan Ashwell , David R. Lancia, Jr. , Justin Andrew Caravella , Wei Lu
IPC分类号: C07D401/12 , A61K31/4704 , C07D413/14 , C07D401/14 , C07D417/14 , C07D405/14
CPC分类号: C07D401/12 , A61K31/4704 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要: The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where A, B, U, V, Z, W1, W2, W3, and R1-R6 are described herein.
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公开(公告)号:US09630922B2
公开(公告)日:2017-04-25
申请号:US15130613
申请日:2016-04-15
发明人: Pui Yee Ng , Heather Davis , Kenneth W. Bair , David S. Millan , Aleksandra Rudnitskaya , Xiaozhang Zheng , Bingsong Han , Nicholas Barczak , David R. Lancia, Jr.
IPC分类号: C07D221/20 , C07D403/04 , C07D209/96 , C07D401/04 , C07D417/06 , C07D519/00 , C07D401/06 , C07D413/06 , C07D405/04 , C07D471/04 , C07D497/10 , C07D491/107 , C07D405/06 , C07D403/06 , C07D405/10
CPC分类号: C07D209/96 , C07D221/20 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/06 , C07D405/10 , C07D413/06 , C07D417/06 , C07D471/04 , C07D491/107 , C07D497/10 , C07D519/00
摘要: The present invention is directed to inhibitors of histone deacetylases (HDACs) such as HDAC6, and their use in the treatment of diseases such as cell proliferative diseases (e.g., cancer), neurological (e.g., neurodegenerative disease or neurodevelopmental disease), inflammatory or autoimmune disease, infection, metabolic disease, hematologic disease, or cardiovascular disease.
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公开(公告)号:US20140163222A1
公开(公告)日:2014-06-12
申请号:US13949712
申请日:2013-07-24
发明人: KRISHNA MURTHI , REBECCA CASAUBON , ARTHUR F. KLUGE , CHASE SMITH , JOACHIM VOGT
IPC分类号: C07D471/04
CPC分类号: C07D471/04 , A61K31/519 , A61K31/5377 , A61K31/551 , A61K45/06
摘要: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.
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公开(公告)号:US12053463B2
公开(公告)日:2024-08-06
申请号:US18215727
申请日:2023-06-28
发明人: George P. Luke , Pratik Sheth
IPC分类号: A61K31/4709 , A61K9/00 , A61K47/12 , A61K47/38
CPC分类号: A61K31/4709 , A61K9/0053 , A61K47/12 , A61K47/38
摘要: The present disclosure reports solid forms of ((S)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile.
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公开(公告)号:US12049466B2
公开(公告)日:2024-07-30
申请号:US17055161
申请日:2019-05-16
IPC分类号: C07D487/04 , C07D471/04
CPC分类号: C07D487/04 , C07D471/04
摘要: The present disclosure relates to compounds of formula (I′) and pharmaceutically acceptable salts thereof useful as inhibitors of Ubiquitin Specific Peptidase 30 (USP30), pharmaceutical compositions thereof, and methods of use thereof. Compounds as disclosed herein can be useful in the treatment of a disease or disorder involving mitochondrial dysfunction, including neurodegenerative diseases.
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公开(公告)号:US12043623B2
公开(公告)日:2024-07-23
申请号:US17490482
申请日:2021-09-30
发明人: Alexandre Joseph Buckmelter , Stephanos Ioannidis , Bruce Follows , Gary Gustafson , Minghua Wang , Justin Andrew Caravella , Zhongguo Wang , Edward L. Fritzen , Jian Lin
IPC分类号: C07D473/00 , A61K31/522
CPC分类号: C07D473/00 , A61K31/522
摘要: The application relates to inhibitors of USP1 useful in the treatment of cancers, and other USP1 associated diseases and disorders, having the Formula:
where R1, R2, R3, R3′, R4, R5, X1, X2, X3, X4, and n are described herein.-
公开(公告)号:US20240239808A1
公开(公告)日:2024-07-18
申请号:US18286053
申请日:2022-04-06
IPC分类号: C07D498/04 , A61K31/519 , A61K31/5365 , A61K31/5383 , C07D471/04 , C07D487/04 , C07D513/04 , C07D519/00
CPC分类号: C07D498/04 , A61K31/519 , A61K31/5365 , A61K31/5383 , C07D471/04 , C07D487/04 , C07D513/04 , C07D519/00
摘要: The present disclosure provides compounds for inhibiting USP1, and related methods of preparing and using the compounds.
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公开(公告)号:US20240083901A1
公开(公告)日:2024-03-14
申请号:US18124071
申请日:2023-03-21
发明人: Anna ERICSSON , Neal GREEN , Gary GUSTAFSON , Bingsong HAN , David R. LANCIA, JR. , Lorna MITCHELL , David RICHARD , Tatiana SHELEKHIN , Chase C. SMITH , Zhongguo WANG , Xiaozhang ZHENG
IPC分类号: C07D487/04 , A61K9/00 , A61K31/407 , A61P7/00 , C07D519/00
CPC分类号: C07D487/04 , A61K9/0053 , A61K31/407 , A61P7/00 , C07D519/00
摘要: The disclosure relates to modulating pyruvate kinase and provides novel chemical compounds useful as activators of PKR, as well as various uses of these compounds. PKR activating compounds are useful in the treatment of diseases and disorders associated with PKR and/or PKM2, such as pyruvate kinase deficiency (PKD), sickle cell disease (SCD), and thalassemia.
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公开(公告)号:US11801243B2
公开(公告)日:2023-10-31
申请号:US17482720
申请日:2021-09-23
发明人: Sylvie Guichard , Maureen Caligiuri , Anna Ericsson , Qunli Xu , Hesham Mohamed
IPC分类号: A61K31/4745 , A61P35/00
CPC分类号: A61K31/4745 , A61P35/00
摘要: Methods for treating certain androgen receptor-positive forms of cancer using inhibitors of the CREB binding protein bromodomain are disclosed. In some methods, the AR-positive forms of cancer may be breast cancer, including triple negative forms, hormone receptor positive forms, and HER2-positive forms. In other methods, the AR-positive forms of cancer may be prostate cancer, including metastatic castration resistant prostate cancer. In some embodiments, methods of treating prostate cancer comprise the step of administering to a patient in need thereof the compound (1R,3R)-3-[(7S)-2-[(R)-(5-fluoro-2-methoxyphenyl)(hydroxy)methyl]-6-(methoxycarbonyl)-7-methyl-3H,6H,7H,8H,9H-imidazo[4,5-f]quinolin-3-yl]cyclohexane-1-carboxylic acid, or a pharmaceutically acceptable salt thereof.
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公开(公告)号:US11723905B2
公开(公告)日:2023-08-15
申请号:US17183606
申请日:2021-02-24
发明人: George P. Luke , Pratik Sheth
IPC分类号: A61K31/4709 , A61K9/00 , A61K47/12 , A61K47/38
CPC分类号: A61K31/4709 , A61K9/0053 , A61K47/12 , A61K47/38
摘要: The present disclosure reports solid forms of ((S)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile.
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