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![Process for the preparation of N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrroldin-1-yl)cyclohexyl)acetamide](/abs-image/US/2022/02/22/US11254679B2/abs.jpg.150x150.jpg)
公开(公告)号：US11254679B2
公开(公告)日：2022-02-22
申请号：US16631915
申请日：2018-07-19
发明人： Burcu Selin Aytar , Alina Borovika , Collin Chan , Joerg Deerberg , Nathan R. Domagalski , Martin D. Eastgate , Yu Fan , Michael David Bengt Fenster , Robert V. Forest , Francisco Gonzalez-Bobes , Rebecca A. Green , Matthew R. Hickey , Nathaniel David Kopp , Thomas E. La Cruz , Kathleen Lauser , Hong Geun Lee , David K. Leahy , Helen Y. Luo , Thomas M. Razler , Scott A. Savage , Chris Sfouggatakis , Maxime C. D. Soumeillant , Serge Zaretsky , Bin Zheng , Ye Zhu
IPC分类号： C07D487/04
摘要： The invention generally relates to an improved process for the preparation of N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, as well as novel intermediates employed in the process, which may be useful for the treatment of cancer.
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![PROCESS FOR THE PREPARATION OF N,N-DICYCLOPROPYL-4-(1,5-DIMETHYL-1H-PYRAZOL-3-YLAMINO)-6-ETHYL-1-METHYL-1,6-DIHYDROIMIDAZO[4,5-d]PYRROLO[2,3-b]PYRIDINE-7-CARBOXAMIDE](/abs-image/US/2016/08/11/US20160229854A1/abs.jpg.150x150.jpg)
2.发明申请PROCESS FOR THE PREPARATION OF N,N-DICYCLOPROPYL-4-(1,5-DIMETHYL-1H-PYRAZOL-3-YLAMINO)-6-ETHYL-1-METHYL-1,6-DIHYDROIMIDAZO[4,5-d]PYRROLO[2,3-b]PYRIDINE-7-CARBOXAMIDE 审中-公开制备N，N-二异丙基-4-（1,5-二甲基-1H-吡唑-3-基氨基）-6-乙基-1-甲基-1,6-二氢吲哚并[4,5-d]吡咯的方法 [2,3-b]吡啶-7-羧酰胺公开(公告)号：US20160229854A1
公开(公告)日：2016-08-11
申请号：US14914330
申请日：2014-08-28
发明人： Martin D. Eastgate , Gregory L. Beutner , Benjamin Cohen , Nicolas Cuniere , Lopa V. Desai , Monica Fitzgerald , Qi Gao , Michael Bryan Hay , Michael Joseph Lawler , Paul C. Lobben , Christopher S. Regens , Thorsten Rosner , Neil Strotman , Carolyn S. Wei , Yi Xiao , Bin Zheng , Keming Zhu
IPC分类号： C07D471/14 , C07D403/04 , C07D231/16 , C07D207/42
CPC分类号： C07D471/14 , C07D207/42 , C07D231/16 , C07D403/04
摘要： The invention relates to an improved process for synthesizing N,N-dicyclopropyl-4-(1,5-dimethyl-1H-pyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide of the formula: (I) Compound (I) is currently in clinical trials for the treatment of myeloproliferative disorders, such as polycythaemia vera, thrombocythaemia and primary myelofibrosis.
摘要翻译： 本发明涉及一种合成N，N-二环丙基-4-（1,5-二甲基-1H-吡唑-3-基氨基）-6-乙基-1-甲基-1,6-二氢咪唑并[4,5 d]吡咯并[2,3-b]吡啶-7-甲酰胺，其化学式（I）化合物（I）目前正在临床试验中用于治疗骨髓增生性疾病，如多发性红血球病，血小板减少症和原发性骨髓纤维化。
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公开(公告)号：US12077558B2
公开(公告)日：2024-09-03
申请号：US18167772
申请日：2023-02-10
发明人： Michael Anthony Schmidt , Bin Zheng , Kyle Knouse , Justine deGruyter , Martin D. Eastgate , Phil Baran , William R. Ewing , Richard E. Olson , Ivar M. McDonald
IPC分类号： C07H21/00 , C07H19/11 , C07H19/213
CPC分类号： C07H21/00
摘要： The present invention relates to novel phosphorous (V) (P(V)) reagents, methods for preparing thereof, and methods for preparing organophosphorous (V) compounds by using the novel reagents.
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公开(公告)号：US11613554B2
公开(公告)日：2023-03-28
申请号：US16382692
申请日：2019-04-12
发明人： Michael Anthony Schmidt , Bin Zheng , Kyle Knouse , Justine deGruyter , Martin D. Eastgate , Phil Baran , William R. Ewing , Richard E. Olson , Ivar M. McDonald
IPC分类号： C07H21/00
摘要： The present invention relates to novel phosphorous (V) (P(V)) reagents, methods for preparing thereof, and methods for preparing organophosphorous (V) compounds by using the novel reagents.
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公开(公告)号：US20210107897A1
公开(公告)日：2021-04-15
申请号：US17131718
申请日：2020-12-22
发明人： Ke Chen , Joerg Deerberg , Dong Lin , Michael Dummeldinger , Bahar Inankur , Sergei Kolotuchin , Jun Li , Amanda J. Rogers , Victor W. Rosso , Eric M. Simmons , Maxime C.D. Soumeillant , Daniel S. Treitler , Jianji Wang , Bin Zheng , Michael J. Smith , Neil A. Strotman , Steven Tymonko , Tamas Benkovics
IPC分类号： C07D403/12 , C07C211/09 , C07D237/24 , C07D249/08
摘要： The invention relates to an improved process for synthesizing 6-(cyclopropaneamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide of the formula: Compound I is currently in clinical trials for the treatment of auto-immune and auto-inflammatory diseases such as psoriasis.
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6.发明申请Pyrazolopyrimidine Macrocycles as Inhibitors of Human Immunodeficiency Virus Replication 有权吡唑并嘧啶大环化合物作为人类免疫缺陷病毒复制的抑制剂公开(公告)号：US20150232481A1
公开(公告)日：2015-08-20
申请号：US14619728
申请日：2015-02-11
发明人： B. Narasimhulu Naidu , Michael A. Walker , Margaret E. Sorenson , Manoj Patel , Zhizhen Barbara Zheng , John F. Kadow , Bin Zheng , Martin D. Eastgate , Ke Chen , Francisco Gonzalez-Bobes
IPC分类号： C07D498/22
CPC分类号： C07D498/22 , C07D211/48
摘要： The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for making and using these compounds in the treatment of HIV infection.
摘要翻译： 本公开一般涉及式I化合物，包括用于治疗人类免疫缺陷病毒（HIV）感染的组合物和方法。 本公开提供了HIV的新型抑制剂，含有这些化合物的药物组合物，以及制备和使用这些化合物治疗HIV感染的方法。
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公开(公告)号：US20230271946A1
公开(公告)日：2023-08-31
申请号：US18134564
申请日：2023-04-13
发明人： Ke Chen , Joerg Deerberg , Dong Lin , Michael Dummeldinger , Bahar Inankur , Sergei Kolotuchin , Jun Li , Amanda J. Rogers , Victor W. Rosso , Eric M. Simmons , Maxime C.D. Soumeillant , Daniel S. Treitler , Jianji Wang , Bin Zheng , Michael J. Smith , Neil A. Strotman , Steven Tymonko , Tamas Benkovics
IPC分类号： C07D403/12 , C07C211/09 , C07D237/24 , C07D249/08
CPC分类号： C07D403/12 , C07C211/09 , C07D237/24 , C07D249/08 , C07B2200/13
摘要： The invention relates to an improved process for synthesizing 6-(cyclopropaneamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-5N-(methyl-d3)pyridazine-3-carboxamide of the formula:
Compound I is currently in clinical trials for the treatment of auto-immune and auto-inflammatory diseases such as psoriasis.-
公开(公告)号：US10106560B2
公开(公告)日：2018-10-23
申请号：US15623570
申请日：2017-06-15
发明人： Adrian Ortiz , Carlos A. Guerrero , Bin Zheng , Jason J. Zhu , Michael Anthony Schmidt , Michael R. Luzung , Martin D. Eastgate
IPC分类号： C07D417/12 , C07F7/18 , C07D211/28 , C07F7/08
摘要： An improved process for making a compound B of the structure wherein n, R1, R2, and R3 are as defined in the specification. Compound B can be used to make tubulysin analogs that are, in turn, useful as anti-cancer agents, particularly when deployed in an antibody-drug conjugate.
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9.发明授权Pyrazolopyrimidine macrocycles as inhibitors of human immunodeficiency virus replication 有权吡唑并嘧啶大环化合物作为人类免疫缺陷病毒复制的抑制剂公开(公告)号：US09273067B2
公开(公告)日：2016-03-01
申请号：US14619728
申请日：2015-02-11
发明人： B. Narasimhulu Naidu , Michael A. Walker , Margaret E. Sorenson , Manoj Patel , Zhizhen Barbara Zheng , John F. Kadow , Bin Zheng , Martin D. Eastgate , Ke Chen , Francisco Gonzalez-Bobes
IPC分类号： C07D498/22 , C07D211/48
CPC分类号： C07D498/22 , C07D211/48
摘要： The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for making and using these compounds in the treatment of HIV infection.
摘要翻译： 本公开一般涉及式I化合物，包括用于治疗人类免疫缺陷病毒（HIV）感染的组合物和方法。 本公开提供了HIV的新型抑制剂，含有这些化合物的药物组合物，以及制备和使用这些化合物治疗HIV感染的方法。
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![PROCESS FOR THE PREPARATION OF N-((1R,2S,5R)-5-(TERT-BUTYLAMINO)-2-((S)-3-(7-TERT-BUTYLPYRAZOLO[1,5-A][1,3,5]TRIAZIN-4-YLAMINO)-2-OXOPYRROLIDIN-1-YL)CYCLOHEXYL)ACETAMIDE](/abs-image/US/2022/06/09/US20220177482A1/abs.jpg.150x150.jpg)
公开(公告)号：US20220177482A1
公开(公告)日：2022-06-09
申请号：US17677312
申请日：2022-02-22
发明人： Burcu Selin Aytar , Alina Borovika , Collin Chan , Joerg Deerberg , Nathan R. Domagalski , Martin D. Eastgate , Yu Fan , Michael David Bengt Fenster , Robert V. Forest , Francisco Gonzalez-Bobes , Rebecca A. Green , Matthew R. Hickey , Nathaniel David Kopp , Thomas E. La Cruz , Kathleen Lauser , Hong Geun Lee , David K. Leahy , Helen Y. Luo , Thomas M. Razler , Scott A. Savage , Chris Sfouggatakis , Maxime C.D. Soumeillant , Serge Zaretsky , Bin Zheng , Ye Zhu
IPC分类号： C07D487/04
摘要： The invention generally relates to an improved process for the preparation of N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, as well as novel intermediates employed in the process, which may be useful for the treatment of cancer.
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