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公开(公告)号：US20220363648A1
公开(公告)日：2022-11-17
申请号：US16973941
申请日：2019-06-25
发明人： Kevin G. Liu , Kellen L. Olszewski , Ji-in Kim , Masha V. Poyurovsky , Koi Morris , Xuemei Yu , Christopher Lamarque
IPC分类号： C07D239/42 , C07D495/04 , C07D519/00 , C07D491/048 , C07D403/12 , C07D239/94 , C07D401/12 , C07D491/052 , C07D471/04 , C07D405/12 , C07D417/12 , C07D405/14 , C07D413/12 , C07D401/14 , C07D403/04 , C07D409/12 , C07D413/14 , C07D473/34
摘要： This invention provides compounds that modulate glucose uptake activity and cellular transport/uptake of glucose, and particularly GLUTS3, but also including but not limited to GLUT1-14 (SLC2A1-SLC2A14). Compounds of the invention are useful for treating diseases, including cancer, autoimmune diseases and inflammation, infectious diseases, and metabolic diseases.
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公开(公告)号：US11479533B2
公开(公告)日：2022-10-25
申请号：US16632662
申请日：2018-07-23
发明人： Eduardas Skucas , Kevin G. Liu , Ji-In Kim , Masha V. Poyurovsky , Rigen Mo , Jingya Zhang
IPC分类号： C07D231/40 , C07D231/12 , C07D401/12 , C07D403/10 , C07D403/12 , C07D413/12 , C07D417/12
摘要： The invention relates to inhibitors of ROCK1 and/or ROCK2. Also provided are methods of inhibiting ROCK1 and/or ROCK2 that are useful for the treatment of disease.
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公开(公告)号：US10729691B2
公开(公告)日：2020-08-04
申请号：US15737916
申请日：2016-06-24
IPC分类号： A61K31/519 , A61K31/52 , C07D239/70 , C07D231/16 , A61K31/5377 , C07D513/04 , C07D471/04 , C07D491/048 , C07D473/34 , C07D495/04 , C07D487/04 , C07D491/052 , A61P33/06
摘要： Provided are methods of treating infectious diseases in mammals comprising administering a compound that inhibits glucose uptake. Particular infectious diseases that may be treated include malaria, leishmaniasis, African trypanosomiasis, tuberculosis, HIV, HCMV or herpes virus. In a first aspect, the invention features a method of treating infectious diseases in a mammal, comprising administering to a mammalian subject in need thereof a therapeutically effective amount of a compound or prodrug thereof, or pharmaceutically acceptable salt or ester of said compound or prodrug, wherein the compound is an inhibitor of glucose uptake.
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公开(公告)号：US20180298029A1
公开(公告)日：2018-10-18
申请号：US15737911
申请日：2016-06-24
发明人： Kellen Olszewski , Ji-Ln Kim , Masha Poyurovsky , Kevin G. Liu , Anthony Barsotti , Koi Morris
IPC分类号： C07D513/04 , C07D495/04 , C07D491/048 , C07D487/04 , C07D473/34 , C07D471/04 , A61P35/04
CPC分类号： C07D513/04 , A61K31/519 , A61K31/52 , A61K31/5377 , A61K45/06 , A61P35/04 , C07D471/04 , C07D473/34 , C07D487/04 , C07D491/048 , C07D495/04 , A61K2300/00
摘要： Provided herein are compounds that modulate glucose uptake activity and are useful for treating cancer, autoimmune diseases, inflammation, infectious diseases, and metabolic diseases. In certain embodiments, the compounds modulate glucose uptake activity by modulating cellular components, including, but not limited to those related to glycolysis and known transporters/co-transporters of glucose such as GLUT1 and other GLUT family members/alternative hexose transporters. In certain embodiments, the compounds have the structure of formula I: Formula (I) wherein the variables have the values disclosed herein.
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公开(公告)号：US11926596B2
公开(公告)日：2024-03-12
申请号：US16632659
申请日：2018-07-23
发明人： Eduardas Skucas , Kevin G. Liu , Ji-In Kim , Masha V. Poyurovsky , Rigen Mo , Jingya Zhang
IPC分类号： C07D231/56 , A61P19/04 , A61P25/28 , C07D401/12 , C07D403/12
CPC分类号： C07D231/56 , A61P19/04 , A61P25/28 , C07D401/12 , C07D403/12
摘要： The invention relates to inhibitors of ROCK1 and/or ROCK2 having the formula I:
Also provided are methods of inhibiting ROCK1 and/or ROCK2 useful for the treatment of disease.-
公开(公告)号：US10696660B2
公开(公告)日：2020-06-30
申请号：US16251952
申请日：2019-01-18
IPC分类号： C07D403/12 , C07D401/14 , C07D239/42 , C07D409/14 , C07D403/14 , A61K31/506
摘要： The invention relates to inhibitors of ROCK1 and/or ROCK2. Also provided are methods of treating diseases and disorders involving inhibiting ROCK1 and/or ROCK2.
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公开(公告)号：US20200165206A1
公开(公告)日：2020-05-28
申请号：US16632662
申请日：2018-07-23
发明人： Eduardas Skucas , Kevin G. Liu , Ji-In Kim , Masha V. Poyurovsky , Rigen Mo , Jingya Zhang
IPC分类号： C07D231/40 , C07D417/12 , C07D231/12 , C07D401/12 , C07D403/10 , C07D403/12 , C07D413/12
摘要： The invention relates to inhibitors of ROCK1 and/or ROCK2. Also provided are methods of inhibiting ROCK1 and/or ROCK2 that are useful for the treatment of disease.
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公开(公告)号：US20190060314A1
公开(公告)日：2019-02-28
申请号：US15737916
申请日：2016-06-24
IPC分类号： A61K31/519 , A61P33/06 , A61K31/52
CPC分类号： A61K31/519 , A61K31/52 , A61K31/5377 , A61P33/06 , C07D231/16 , C07D239/70 , C07D471/04 , C07D473/34 , C07D487/04 , C07D491/048 , C07D491/052 , C07D495/04 , C07D513/04 , Y02A50/409 , Y02A50/411
摘要： Provided are methods of treating infectious diseases in mammals comprising administering a compound that inhibits glucose uptake. Particular infectious diseases that may be treated include malaria, leishmaniasis, African trypanosomiasis, tuberculosis, HIV, HCMV or herpes virus. In a first aspect, the invention features a method of treating infectious diseases in a mammal, comprising administering to a mammalian subject in need thereof a therapeutically effective amount of a compound or prodrug thereof, or pharmaceutically acceptable salt or ester of said compound or prodrug, wherein the compound is an inhibitor of glucose uptake.
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公开(公告)号：US20240360085A1
公开(公告)日：2024-10-31
申请号：US18672406
申请日：2024-05-23
发明人： Kevin G. Liu , Kellen Olszewski , Ji-In Kim , Masha V. Poyurovsky , Koi Morris , Xuemei Yu , Christophe Lamarque
IPC分类号： C07D239/42 , C07D239/94 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D473/34 , C07D491/048 , C07D491/052 , C07D495/04 , C07D519/00
CPC分类号： C07D239/42 , C07D239/94 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D473/34 , C07D491/048 , C07D491/052 , C07D495/04 , C07D519/00
摘要： This invention provides compounds that modulate glucose uptake activity and cellular transport/uptake of glucose, and particularly GLUT3, but also including but not limited to GLUT1-14 (SLC2A1-SLC2A14). Compounds of the invention are useful for treating diseases, including cancer, autoimmune diseases and inflammation, infectious diseases, and metabolic diseases.
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公开(公告)号：US20240190827A1
公开(公告)日：2024-06-13
申请号：US18434994
申请日：2024-02-07
发明人： Eduardas Skucas , Kevin G. Liu , Ji-In Kim , Masha V. Poyurovsky , Rigen Mo , Jingya Zhang
IPC分类号： C07D231/56 , A61P19/04 , A61P25/28 , C07D401/12 , C07D403/12
CPC分类号： C07D231/56 , A61P19/04 , A61P25/28 , C07D401/12 , C07D403/12
摘要： The invention relates to inhibitors of ROCK1 and/or ROCK2. Also provided are methods of inhibiting ROCK1 and/or ROCK2 that are useful for the treatment of disease.
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