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公开(公告)号：US11649242B2
公开(公告)日：2023-05-16
申请号：US17239364
申请日：2021-04-23
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 , C07D519/00 , A61P7/00 , A61K9/00 , A61K31/407
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：US20220378756A1
公开(公告)日：2022-12-01
申请号：US17761795
申请日：2020-09-18
发明人： Anna Ericsson , Sanjeev Forsyth , Neal Green , Gary Gustafson , Patrick F. Kelly , David R. Lancia, JR. , Gary Marshall , Lorna Mitchell , Madhu Mondal , Maria Ribadeneira , David Richard , Patricia Schroeder , Zhongguo Wang
IPC分类号： A61K31/436 , A61K9/48 , A61K9/00 , A61P7/06
摘要： The compound (S)-1-(5-((2,3-dihydro-[1,4]dioxino[2,3-b]pyridin-7-yl)sulfonyl)-3,4,5,6-tetrahydropyrrolo[3,4-c]pyrroll-2(1H)-yl)-3-hydroxy-2-phenylpropan-1-one, or a pharmaceutically acceptable salt thereof, is useful to increase the affinity of hemoglobin for oxygen. Methods and compositions for the treatment of a hemoglobinopathies are provided herein, including certain pharmaceutical compositions for activating PKR.
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公开(公告)号：US10675274B2
公开(公告)日：2020-06-09
申请号：US16576360
申请日：2019-09-19
发明人： Anna Ericsson , Neal Green , Gary Gustafson , David R. Lancia, Jr. , Gary Marshall , Lorna Mitchell , David Richard , Zhongguo Wang
IPC分类号： A61K31/436 , C07D487/04
摘要： This disclosure provides compounds and compositions for activating pyruvate kinase R (PKR) and related methods of manufacturing and using these compounds and compositions.
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公开(公告)号：US20220087983A1
公开(公告)日：2022-03-24
申请号：US17477751
申请日：2021-09-17
发明人： Anna Ericsson , Neal Green , Gary Gustafson , David R. Lancia, JR. , Gary Marshall , Lorna Mitchell , David Richard , Zhongguo Wang , Sanjeev Forsyth , Patrick F. Kelly , Madhu Mondal , Maria Ribadeneira , Patricia Schroeder
IPC分类号： A61K31/436 , A61P7/00
摘要： The compound (S)-1-(5-((2,3-dihydro-[1,4]dioxino[2,3-b]pyridin-7-yl)sulfonyl)-3,4,5,6-tetrahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)-3-hydroxy-2-phenylpropan-1-one, or a pharmaceutically acceptable salt thereof, is useful to increase the affinity of hemoglobin for oxygen. Methods and compositions for the treatment of a hemoglobinopathies are provided herein, including certain pharmaceutical compositions for activating PKR.
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公开(公告)号：US11071725B2
公开(公告)日：2021-07-27
申请号：US15929436
申请日：2020-05-01
发明人： Anna Ericsson , Neal Green , Gary Gustafson , David R. Lancia, Jr. , Gary Marshall , Lorna Mitchell , David Richard , Zhongguo Wang
IPC分类号： A61K31/436 , A61P7/06 , A61K9/00 , C07D487/04
摘要： This disclosure provides compounds and compositions for activating pyruvate kinase R (PKR) and related methods of manufacturing and using these compounds and compositions.
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公开(公告)号：US11014927B2
公开(公告)日：2021-05-25
申请号：US16496279
申请日：2018-03-20
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 , C07D519/00 , A61P7/00 , A61K9/00 , A61K31/407
摘要： The disclosure relates to modulating pyruvate kinase and provides novel chemical compounds of formula (I) 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：US20200085798A1
公开(公告)日：2020-03-19
申请号：US16576360
申请日：2019-09-19
发明人： Anna Ericsson , Neal Green , Gary Gustafson , David R. Lancia, JR. , Gary Marshall , Lorna Mitchell , David Richard , Zhongguo Wang
IPC分类号： A61K31/436
摘要： This disclosure provides compounds and compositions for activating pyruvate kinase R (PKR) and related methods of manufacturing and using these compounds and compositions.
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公开(公告)号：US20200017525A1
公开(公告)日：2020-01-16
申请号：US16077407
申请日：2017-02-13
发明人： David Joseph Guerin , Kenneth W. Bair , Justin A. Caravella , Stephanos Ioannidis, Jr. , David R. Lancia, Jr. , Hongbin Li , Steven Mischke , Pui Yee Ng , David Richard , Shawn E.R. Schiller , Tatiana Shelekhin , Zhongguo Wang
IPC分类号： C07D519/00 , C07D495/04
摘要： The disclosure relates to inhibitors of USP28 and/or USP25 useful in the treatment of cancers, inflammation, autoimmune diseases, and infectious diseases, having the Formula: where R1, R2, R3, R4, R5, R5′, R6, R7, X, m, and n are described herein.
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公开(公告)号：US20220304987A1
公开(公告)日：2022-09-29
申请号：US17698505
申请日：2022-03-18
发明人： Anna Ericsson , Neal Green , Gary Gustafson , David R. Lancia, JR. , Gary Marshall , Lorna Mitchell , David Richard , Zhongguo Wang , Sanjeev Forsyth , Patrick F. Kelly , Madhu Mondal , Maria Ribadeneira , Patricia Schroeder
IPC分类号： A61K31/436 , A61P9/00
摘要： The compound (S)-1-(5-((2,3-dihydro-[1,4]dioxino[2,3-b]pyridin-7-yl)sulfonyl)-3,4,5,6-tetrahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)-3-hydroxy-2-phenylpropan-1-one, or a pharmaceutically acceptable salt thereof, is useful to increase the affinity of hemoglobin for oxygen. Methods and compositions for the treatment of a hemoglobinopathies are provided herein, including certain pharmaceutical compositions for activating PKR.
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公开(公告)号：US20210221816A1
公开(公告)日：2021-07-22
申请号：US17223783
申请日：2021-04-06
发明人： David R. Lancia, JR. , Gary Gustafson , Neal Green , Lorna Mitchell , Anna Ericsson , David Richard
IPC分类号： C07D487/04 , A61K9/00
摘要： The disclosure provides chemical compounds useful as activators of PKR. PKR activating compounds are useful in the treatment of disease and disorders associated with modulation of PKR and/or PKM2, such as pyruvate kinase deficiency (PKD).
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