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公开(公告)号：US20200069677A1
公开(公告)日：2020-03-05
申请号：US16467396
申请日：2017-12-08
发明人： John McGrath , Patrick Trojer
IPC分类号： A61K31/495 , C12Q1/6886 , A61K45/06 , A61P35/00 , A61K9/00 , A61K31/445 , A61K31/136 , A61K31/4155 , A61K31/397 , A61K31/506 , A61K31/505 , A61K31/496 , A61K31/40
摘要： Provided herein are methods of treating cancers characterized by a high expression of GFIIB, comprising administering a therapeutically effective amount of a KDMIA inhibitor.
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2.发明公开公开(公告)号：US20230414593A1
公开(公告)日：2023-12-28
申请号：US18037120
申请日：2021-11-18
发明人： William D. Bradley , Jike Cui , Kaiming Sun , Patrick Trojer , Jing Wang , Rentian Wu
IPC分类号： A61K31/443 , A61K31/4166 , A61P35/00
CPC分类号： A61K31/443 , A61P35/00 , A61K31/4166
摘要： Provided herein are methods of treating prostate cancer having at least one pathogenic AR mutation using 7-chloro-2-(4-(3-methoxyazetidin-1-yl)cyclohexyl)-2,4-dimethyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3- yl)methyl)benzo[d][1,3]dioxole-5-carboxamide, or a pharmaceutically acceptable salt thereof, alone or in combination with a therapeutically effective amount of an androgen receptor signaling inhibitor (ARSI) such as enzalutamide.
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![2-((4S)-6-(4-CHLOROPHENYL)-1-METHYL-4H-BENZO[C]ISOXAZOLO[4,5-E]AZEPIN-4-YL)ACETAMIDE FOR TREATING THROMBOCYTHEMIA](/abs-image/US/2023/09/28/US20230302010A1/abs.jpg.150x150.jpg)
3.发明公开公开(公告)号：US20230302010A1
公开(公告)日：2023-09-28
申请号：US18019634
申请日：2021-08-03
发明人： Adrian Senderowicz
摘要： The present disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, and pharmaceutically acceptable salts thereof, for treating thrombocythemia.
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![CRYSTALLINE FORMS OF 7-CHLORO-2-(4-(3-METHOXYAZETIDIN-1-YL)CYCLOHEXYL)-2,4-DIMETHYL-N-((6-METHYL-4-(METHYLTHIO)-2-OXO-1,2-DIHYDROPYRIDIN-3-YL)METHYL)BENZO[D][1,3]DIOXOLE-5-CARBOXAMIDE](/abs-image/US/2022/08/11/US20220251073A1/abs.jpg.150x150.jpg)
公开(公告)号：US20220251073A1
公开(公告)日：2022-08-11
申请号：US17628947
申请日：2020-07-23
发明人： Alamelu Banda , Victor S. Gehling
IPC分类号： C07D405/14
摘要： The present disclosure relates to a crystalline Form 1 of 7-chloro-2-(4-(3-methoxyazetidin-1-yl)cyclohexyl)-2,4-di -methyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)benzo[d] [1,3]dioxole-5-carboxamide, which is useful as modulators the activity of histone methyl modifying enzymes. The present disclosure also provides pharmaceutically acceptable compositions comprising the crystalline form and methods of using said compositions in the treatment of various disorders.
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公开(公告)号：US20220017502A1
公开(公告)日：2022-01-20
申请号：US17311526
申请日：2019-12-06
发明人： Anna Gardberg , Victor S. Gehling , Avinash Khanna , Julian R. Levell , Jonathan E. Wilson , Kennedy Taveras
IPC分类号： C07D413/12 , C07D413/14 , A61P35/00
摘要： Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.
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公开(公告)号：US20210206776A1
公开(公告)日：2021-07-08
申请号：US17057225
申请日：2019-05-17
发明人： Alexandre Côté , Avinash Khanna , Ludivine Moine
IPC分类号： C07D491/056 , A61P35/00
摘要： Provided are novel compounds of Formula (I): Formula (I); and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with methyl modifying enzymes. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with methyl modifying enzymes.
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公开(公告)号：US10918646B1
公开(公告)日：2021-02-16
申请号：US17065316
申请日：2020-10-07
发明人： Adrian Senderowicz , Michael Cooper
摘要： The present disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, and pharmaceutically acceptable salts thereof, for treating myelofibrosis.
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公开(公告)号：US20210030763A1
公开(公告)日：2021-02-04
申请号：US17065316
申请日：2020-10-07
发明人： Adrian Senderowicz , Michael Cooper
摘要： The present disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, and pharmaceutically acceptable salts thereof, for treating myelofibrosis.
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公开(公告)号：US10183009B2
公开(公告)日：2019-01-22
申请号：US15592013
申请日：2017-05-10
发明人： Brian K. Albrecht , Steven F. Bellon , Daniel J. Burdick , Alexandre Cote , Terry Crawford , Les A. Dakin , Vickie Hsiao-Wei Tsui , Michael Charles Hewitt , Yves LeBlanc , Steven R. Magnuson , Christopher G. Nasveschuk , F. Anthony Romero , Yong Tang , Alexander M. Taylor , Shumei Wang
IPC分类号： A61K31/40 , C07D471/04
摘要： The present invention relates to compounds of formula (I): and to salts thereof, wherein R1, R2, and Q have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of bromodomains. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various bromodomain-mediated disorders.
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公开(公告)号：US10155764B2
公开(公告)日：2018-12-18
申请号：US15449692
申请日：2017-03-03
发明人： Brian K. Albrecht , Alexandre Cote , Terry Crawford , Martin Duplessis , Andrew Charles Good , Yves LeBlanc , Steven Magnuson , Christopher G. Nasveschuk , Richard Pastor , Anthony F. Romero , Alexander M. Taylor
IPC分类号： C07D487/04 , C07D403/12 , C07D401/12 , C07D237/32 , C07D471/04 , A61K31/502 , A61K31/5025 , A61K31/5377 , A61K31/55 , C07D237/34 , C07D405/12
摘要： The present invention relates to methods for treating PCAF and GCN5 mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein ring A, R1, R3, R4, R5, and each Re have any of the values defined in the specification. Also included are novel compounds of Formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.
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