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公开(公告)号：US20170312252A1
公开(公告)日：2017-11-02
申请号：US15482584
申请日：2017-04-07
发明人： Kwong Wah Lai , Jun Liang , Birong Zhang , Sharada Labadie , Daniel Ortwine , Peter Dragovich , James Kiefer , Victor S. Gehling , Jean-Christophe Harmange
IPC分类号： A61K31/41 , A61K31/4025 , C07D207/04 , C07D237/04
CPC分类号： A61K31/41 , A61K31/4025 , C07D207/04 , C07D237/04 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14
摘要： The present invention relates to compounds useful as inhibitors of one or more histone demethylses, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
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公开(公告)号：US10301253B2
公开(公告)日：2019-05-28
申请号：US15658219
申请日：2017-07-24
发明人： Brian K. Albrecht , James Edmund Audia , Alexandre Cote , Martin Duplessis , Victor S. Gehling , Andrew Charles Good , Jean-Christophe Harmange , Yves LeBlanc , Christopher G. Nasveschuk , Alexander M. Taylor , Rishi G. Vaswani
IPC分类号： C07C211/39 , C07C211/38 , C07C211/17 , C07C211/19 , A61K31/137 , A61K31/136 , A61K31/135 , A61K31/4465 , C07C211/42 , C07D231/12 , C07D401/12 , C07D405/12 , C07D211/78 , C07D213/38 , C07C255/58 , C07C217/74 , C07C229/50 , C07C237/48 , A61K31/166 , A61K31/196 , A61K31/277 , A61K31/337 , A61K31/351 , A61K31/397 , A61K31/40 , A61K31/415 , A61K31/4155 , A61K31/437 , A61K31/4406 , A61K31/445 , A61K31/4545 , A61K31/4747 , A61K31/495 , A61K31/517 , A61K45/06 , C07C317/36 , C07D205/04 , C07D205/12 , C07D207/06 , C07D211/26 , C07D211/46 , C07D215/08 , C07D295/185 , C07D305/08 , C07D309/04
摘要： Provided herein are compounds of formula I: and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. 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 LSD1-mediated disorders.
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公开(公告)号：US10022354B2
公开(公告)日：2018-07-17
申请号：US15482584
申请日：2017-04-07
发明人： Kwong Wah Lai , Jun Liang , Birong Zhang , Sharada Labadie , Daniel Ortwine , Peter Dragovich , James Kiefer , Victor S. Gehling , Jean-Christophe Harmange
IPC分类号： C07D237/04 , A61K31/41 , A61K31/4025 , C07D207/04
摘要： The present invention relates to compounds useful as inhibitors of one or more histone demethylases, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
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公开(公告)号：US20180009735A1
公开(公告)日：2018-01-11
申请号：US15658219
申请日：2017-07-24
发明人： Brian K. Albrecht , James Edmund Audia , Alexandre Cote , Martin Duplessis , Victor S. Gehling , Andrew Charles Good , Jean-Christophe Harmange , Yves LeBlanc , Christopher G. Nasveschuk , Alexander M. Taylor , Rishi G. Vaswani
IPC分类号： C07C211/42 , C07D401/12 , A61K31/135 , A61K31/166 , C07D309/04 , C07D305/08 , C07D295/185 , C07D231/12 , C07D215/08 , C07D213/38 , C07D211/46 , C07D211/26 , C07D207/06 , C07D205/12 , C07D205/04 , C07C317/36 , C07C255/58 , C07C237/48 , C07C229/50 , C07C217/74 , A61K45/06 , A61K31/517 , A61K31/495 , A61K31/4747 , A61K31/4545 , A61K31/445 , A61K31/4406 , A61K31/437 , A61K31/4155 , A61K31/415 , A61K31/40 , A61K31/397 , A61K31/351 , A61K31/337 , A61K31/277 , A61K31/196 , C07D405/12
CPC分类号： C07C211/42 , A61K31/135 , A61K31/166 , A61K31/196 , A61K31/277 , A61K31/337 , A61K31/351 , A61K31/397 , A61K31/40 , A61K31/415 , A61K31/4155 , A61K31/437 , A61K31/4406 , A61K31/445 , A61K31/4545 , A61K31/4747 , A61K31/495 , A61K31/517 , A61K45/06 , C07C217/74 , C07C229/50 , C07C237/48 , C07C255/58 , C07C317/36 , C07C2601/02 , C07C2601/04 , C07C2603/94 , C07D205/04 , C07D205/12 , C07D207/06 , C07D211/26 , C07D211/46 , C07D211/78 , C07D213/38 , C07D215/08 , C07D231/12 , C07D295/185 , C07D305/08 , C07D309/04 , C07D401/12 , C07D405/12
摘要： Provided herein are compounds of formula I: and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. 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 LSD1-mediated disorders.
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公开(公告)号：US10035801B2
公开(公告)日：2018-07-31
申请号：US14775405
申请日：2014-03-13
发明人： Brian K. Albrecht , Steven F. Bellon , Victor S. Gehling , Jean-Christophe Harmange , Kwong Wah Lai , Jun Liang , Peter Dragovich , Daniel F. Ortwine , Sharada Labadie , Birong Zhang , James Richard Kiefer
IPC分类号： C07D487/04 , A61K31/519 , A61K45/06 , A61K31/5377 , A61K31/337 , A61K31/517 , A61K31/437 , C12N9/99 , C07D498/04 , C07D487/14
CPC分类号： C07D487/04 , A61K31/337 , A61K31/437 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D487/14 , C07D498/04 , C12N9/99
摘要： Provided are compounds useful as inhibitors of one or more histone demethylases, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using the present composition in the treatment of various disorders.
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![Pyrazolo[1,5-A]pyrimidin-7(4H)-onehistone demethylase inhibitors](/abs-image/US/2016/11/29/US09505767B2/abs.jpg.150x150.jpg)
6.发明授权公开(公告)号：US09505767B2
公开(公告)日：2016-11-29
申请号：US14477566
申请日：2014-09-04
发明人： Brian K. Albrecht , Steven F. Bellon , Victor S. Gehling , Jean-Christophe Harmange , Yves LeBlanc , Jun Liang , Steven R. Magnuson , Vickie Hsiao-Wei Tsui , Birong Zhang
IPC分类号： C07D487/04 , A61K31/519 , A61K45/06 , A61N5/10
CPC分类号： C07D487/04 , A61K31/519 , A61K45/06 , A61N5/10
摘要： The present invention relates to compounds formula (I): and to salts thereof, wherein R1-R4 and A have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of histone demethylases, such as KDM5. Also included are pharmaceutically acceptable compositions comprising the compounds of the present invention and methods of using said compositions in the treatment of various disorders.
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公开(公告)号：US20160143910A1
公开(公告)日：2016-05-26
申请号：US14776586
申请日：2014-03-14
申请人： Shilpi ARORA , Michael Robert COSTA , Ted LAU , Patrick TROJER , GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC.
发明人： Shilpi Arora , Michael Robert Costa , Ted Lau , Patrick Trojer , Brian K. Albrecht , Shane Buker , Marie Classon , Victor S. Gehling , Jean-Christophe Harmange , Erica L. Jackson , Jun Liang , Heidi Phillips , Peter Sandy , Jeffrey Settleman , Jean-Philippe Stephan
IPC分类号： A61K31/519 , A61K31/437 , A61K31/517 , A61K45/06 , A61K31/337
CPC分类号： A61K31/519 , A61K31/337 , A61K31/437 , A61K31/517 , A61K31/555 , A61K31/713 , A61K33/24 , A61K45/06 , C12N15/113 , C12N2310/14 , C12N2310/531 , A61K2300/00
摘要： Provided herein are methods of treating and/or preventing cancer drug resistance using antagonists of KDM5.
摘要翻译： 本文提供使用KDM5拮抗剂治疗和/或预防癌症耐药性的方法。
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公开(公告)号：US20160060267A1
公开(公告)日：2016-03-03
申请号：US14775405
申请日：2014-03-13
发明人： Brian K. Albrecht , Steven F. Bellon , Victor S. Gehling , Jean-Christophe Harmange , Kwong Wah Lai , Jun Liang , Peter Dragovich , Dan Ortwine , Sharada Labadie , Birong Zhang , Jim Kiefer
IPC分类号： C07D487/04 , A61K45/06 , C12N9/99 , A61K31/337 , A61K31/517 , A61K31/437 , A61K31/519 , A61K31/5377
CPC分类号： C07D487/04 , A61K31/337 , A61K31/437 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D487/14 , C07D498/04 , C12N9/99
摘要： Provided are compounds useful as inhibitors of one or more histone demethylases, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using the present composition in the treatment of various disorders.
摘要翻译： 提供了可用作一种或多种组蛋白脱甲基酶抑制剂的化合物，例如KDM5。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用本发明组合物治疗各种疾病的方法。
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公开(公告)号：US20150065522A1
公开(公告)日：2015-03-05
申请号：US14477566
申请日：2014-09-04
发明人： Brian K. Albrecht , Steven F. Bellon , Victor S. Gehling , Jean-Christophe Harmange , Yves LeBlanc , Jun Liang , Steven Magnuson , Vicki Tsui , Birong Zhang
IPC分类号： C07D487/04 , A61K45/06 , A61N5/10 , A61K31/519
CPC分类号： C07D487/04 , A61K31/519 , A61K45/06 , A61N5/10
摘要： The present invention relates to compounds formula (I): and to salts thereof, wherein R1-R4 and A have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of histone demethylases, such as KDM5. Also included are pharmaceutically acceptable compositions comprising the compounds of the present invention and methods of using said compositions in the treatment of various disorders.
摘要翻译： 本发明涉及式（I）化合物及其盐，其中R 1 -R 4和A具有说明书中定义的任何值及其组成和用途。 该化合物可用作组蛋白脱甲基酶的抑制剂，例如KDM5。 还包括包含本发明化合物的药学上可接受的组合物和使用所述组合物治疗各种疾病的方法。
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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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