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公开(公告)号：US20230114064A1
公开(公告)日：2023-04-13
申请号：US17933234
申请日：2022-09-19
摘要： The present disclosure sets forth novel compounds and compositions including heteroaromatic silicon-fluoride-acceptors, which are useful for PET scanning. The present disclosure further includes novel methods of 8F imaging for PET scanning, the methods comprising the preparation of conjugates and bioconjugates of biological ligands of interest with heteroaromatic silicon-fluoride-acceptors. In certain embodiments the invention is practiced in the form of a kit.
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公开(公告)号：US20230096051A1
公开(公告)日：2023-03-30
申请号：US17784215
申请日：2020-12-04
IPC分类号： C07D401/14 , C07B59/00 , A61K51/04
摘要： The present invention provides a compound of Formula I: wherein R1 is hydrogen, F, or 18F; and R2 is hydrogen, F, or 18F; or a pharmaceutically acceptable salt thereof, provided that when R1 is 18F then R2 is not 18F, useful as a CGRP receptor antagonist for PET imaging.
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3.发明申请公开(公告)号：US20230088127A1
公开(公告)日：2023-03-23
申请号：US17793089
申请日：2021-01-15
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVIC
发明人： Chandrasekhar Mushti , Deepak Sail , Rolf Eric Swenson , Murali Krishna Cherukuri , Shingo Matsumoto , Aparna Kesarwala
摘要： A compound of the Formula I or a pharmaceutically acceptable salt thereof, wherein R1, Ca, Cb, Cd, and n are the same as described in the specification. Disclosed is a method of diagnosing or monitoring a patient suffering from cancer, the method comprising: administering a pharmaceutical composition comprising an effective amount of an active agent, wherein the active agent is the compound of Formula I, a pharmaceutically acceptable salt of any of the foregoing thereof, or a combination thereof, together with a pharmaceutically acceptable carrier to the patient and diagnosing or monitoring the patient by hyperpolarized 13C-MRI. Also disclosed is a method of synthesizing 1-13C-5-12C-diacid.
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公开(公告)号：US11591316B2
公开(公告)日：2023-02-28
申请号：US17401833
申请日：2021-08-13
发明人： Javier de Vicente Fidalgo , Anthony A. Estrada , Jianwen A. Feng , Joseph P. Lyssikatos , Zachary K. Sweeney
IPC分类号： C07D403/12 , C07D401/14 , C07D413/14 , C07D417/14 , C07D491/20 , C07D498/04 , C07B59/00 , C07D403/14 , C07D405/14 , C07D409/14 , C07D487/04
摘要： The present disclosure relates generally to LRRK2 inhibitors, or a pharmaceutically acceptable salt, deuterated analog, prodrug, tautomer, stereoisomer, or mixture of stereoisomers thereof, and methods of making and using thereof.
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公开(公告)号：US11565004B2
公开(公告)日：2023-01-31
申请号：US16303599
申请日：2017-05-19
摘要： The present invention provides a method of imaging a subject's lung which comprises contacting the subject's lung with a matrix metalloproteinase inhibitor labeled with a radioisotope under conditions such that the inhibitor binds to matrix metalloproteinase in the lung, and then imaging the radiolabeled inhibitor bound to matrix metalloproteinase in the subject's lung.
The invention also provides Ro 32-3555 labeled with a radioisotope.-
公开(公告)号：US11510888B2
公开(公告)日：2022-11-29
申请号：US16669387
申请日：2019-10-30
申请人： Retrotope, Inc.
IPC分类号： A61K31/20 , A61K31/201 , A61K31/202 , C07B59/00
摘要： Some aspects of the invention provide for essential fatty acids which are substituted in specific positions to slow down oxidative damage by Reactive Oxygen Species (ROS), and to suppress the rate of consequent formation of reactive products, for the purpose of preventing or reducing the damage associated with oxidative stress associated diseases such as neurological diseases and age-related macular degeneration (AMD).
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公开(公告)号：US20220348577A1
公开(公告)日：2022-11-03
申请号：US17190266
申请日：2021-03-02
申请人： Proximagen, LLC
发明人： Giles Brown , Michael Higginbottom , Alison Stewart , Lee Patient , Allison Carley , Iain Simpson , Edward Daniel Savory , Kathryn Oliver , Andrew Graham Cole
IPC分类号： C07D471/08 , A61K45/06 , C07D405/14 , C07D413/14 , C07D417/14 , C07D401/14 , C07D401/12 , C07D471/04 , C07B59/00 , C07D401/04 , C07D413/12 , C07D417/12
摘要： The compounds of formula (I) are antagonists of the CXCR4 receptor Wherein R1, X, Y and R2 are as defined in the claims.
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公开(公告)号：USRE49238E1
公开(公告)日：2022-10-11
申请号：US16997692
申请日：2020-08-19
申请人： Retrotope, Inc.
IPC分类号： A61K31/20 , A61K31/23 , C07C57/03 , A61K31/201 , A61K31/202 , C07B59/00
摘要： Some aspects of the invention provide for essential fatty acids which are substituted in specific positions to slow down oxidative damage by Reactive Oxygen Species (ROS), and to suppress the rate of consequent formation of reactive products, for the purpose of preventing or reducing the damage associated with oxidative stress associated diseases such as neurological diseases and age-related macular degeneration (AMD).
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公开(公告)号：US20220313832A1
公开(公告)日：2022-10-06
申请号：US17618298
申请日：2020-06-12
发明人： Ahmed MAMAI
IPC分类号： A61K47/68 , C07K16/32 , A61P35/00 , C07B59/00 , C07D213/55 , C07D213/56 , C07D401/12 , C07D401/14 , C07D405/12
摘要： The present application relates to nicotinamide phosphoribosyltransferase (NAMPT) inhibitor-linker conjugates of Formula (I) comprising NAMPT inhibitors linked to linker groups, to processes and intermediates for their preparation, and to compositions comprising these compounds, as well as their use, for example, in the treatment or diagnosis of diseases and conditions, including, but not limited to, cancer.
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公开(公告)号：US20220306636A1
公开(公告)日：2022-09-29
申请号：US17428850
申请日：2020-02-06
发明人： Robert S. Lewis , Mahender Reddy Karla , Kathryn E. Kavouris , Yong Dong , Adam J. Morgan , Cameron J. Cowden
IPC分类号： C07D487/04 , C07D403/04 , C07C309/65 , C07B59/00
摘要： Improved processes and intermediates for preparing ruxolitinib and deuterated analogs of ruxolitinib are disclosed.
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