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1. 发明申请

US20190337911A1 CENTRALLY ACTIVE AND ORALLY BIOAVAILABLE ANTIDOTES FOR ORGANOPHOSPHATE EXPOSURE AND METHODS FOR MAKING AND USING THEM 审中-公开
公开(公告)号：US20190337911A1
公开(公告)日：2019-11-07
申请号：US16509392
申请日：2019-07-11
申请人： The Regents of the University of California , The Scripps Research Institute
发明人： Palmer TAYLOR , Zoran RADIC , Barry K. SHARPLESS , Valery FOKIN , Rakesh SIT
IPC分类号： C07D295/13 , C07D451/14 , C07D223/06 , C07D209/56 , C07D221/22 , C07D471/08 , C07D451/02 , C07D223/04 , C07D487/08
摘要： In alternative embodiments, the invention provides nucleophilic hydroxyimino-acetamido alkylamine antidotes that cross the blood-brain barrier (BBB) to catalyze the hydrolysis of organophosphate (OP)-inhibited human acetylcholinesterase (hAChE) in the central nerve system (CNS). The hydroxyimino-acetamido alkylamines of the invention are designed to fit within AChE active center gorge dimensions, bind with reasonable affinity, and react with the conjugated phosphate atom in the gorge. The hydroxyimino-acetamido alkylamines of the invention are also designed to possess ionization states that govern affinity and reactivity for the two linked hAChE re-activation steps. In alternative embodiments, the invention provides pumps, devices, subcutaneous infusion devices, continuous subcutaneous infusion devices, infusion pens, needles, reservoirs, ampoules, a vial, a syringe, a cartridge, a disposable pen or jet injector, a prefilled pen or a syringe or a cartridge, a cartridge or a disposable pen or jet injector, a two chambered or multi-chambered pump, a syringe, a cartridge or a pen or a jet injector, comprising a compound of the invention.

2. 发明申请

US20190119237A1 CENTRALLY ACTIVE AND ORALLY BIOAVAILABLE ANTIDOTES FOR ORGANOPHOSPHATE EXPOSURE AND METHODS FOR MAKING AND USING THEM 审中-公开
公开(公告)号：US20190119237A1
公开(公告)日：2019-04-25
申请号：US16029267
申请日：2018-07-06
申请人： The Regents of the University of California , The Scripps Research Institute
发明人： Palmer TAYLOR , Zoran RADIC , Barry K. SHARPLESS , Valery FOKIN , Rakesh SIT
IPC分类号： C07D295/13 , C07D451/14 , C07D223/06 , C07D209/56 , C07D221/22 , C07D471/08 , C07D451/02 , C07D223/04 , C07D487/08
摘要： In alternative embodiments, the invention provides nucleophilic hydroxyimino-acetamido alkylamine antidotes that cross the blood-brain barrier (BBB) to catalyze the hydrolysis of organophosphate (OP)-inhibited human acetylcholinesterase (hAChE) in the central nerve system (CNS). The hydroxyimino-acetamido alkylamines of the invention are designed to fit within AChE active center gorge dimensions, bind with reasonable affinity, and react with the conjugated phosphate atom in the gorge. The hydroxyimino-acetamido alkylamines of the invention are also designed to possess ionization states that govern affinity and reactivity for the two linked hAChE re-activation steps. In alternative embodiments, the invention provides pumps, devices, subcutaneous infusion devices, continuous subcutaneous infusion devices, infusion pens, needles, reservoirs, ampoules, a vial, a syringe, a cartridge, a disposable pen or jet injector, a prefilled pen or a syringe or a cartridge, a cartridge or a disposable pen or jet injector, a two chambered or multi-chambered pump, a syringe, a cartridge or a pen or a jet injector, comprising a compound of the invention.

3. 发明申请

US20150361060A1 CENTRALLY ACTIVE AND ORALLY BIOAVAILABLE ANTIDOTES FOR ORGANOPHOSPHATE EXPOSURE AND METHODS FOR MAKING AND USING THEM 审中-公开
标题翻译：用于有机磷酸酯接触的中心活性和ORALY BIOVAILABLE抗体及其制备和使用它们的方法
公开(公告)号：US20150361060A1
公开(公告)日：2015-12-17
申请号：US14766272
申请日：2014-02-15
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , THE SCRIPPS RESEARCH INSTITUTE
发明人： Palmer TAYLOR , Zoran RADIC , Barry K. SHARPLESS , Valery FOKIN , Rakesh SIT
IPC分类号： C07D295/13 , C07D223/06 , C07D451/02 , C07D487/08 , C07D471/08 , C07D451/14
CPC分类号： C07D295/13 , C07D209/56 , C07D221/22 , C07D223/04 , C07D223/06 , C07D451/02 , C07D451/14 , C07D471/08 , C07D487/08
摘要： In alternative embodiments, the invention provides nucleophilic hydroxyimino-acetamido alkylamine antidotes that cross the blood-brain barrier (BBB) to catalyze the hydrolysis of organophosphate (OP)-inhibited human acetylcholinesterase (hAChE) in the central nerve system (CNS). The hydroxyimino-acetamido alkylamines of the invention are designed to fit within AChE active center gorge dimensions, bind with reasonable affinity, and react with the conjugated phosphate atom in the gorge. The hydroxyimino-acetamido alkylamines of the invention are also designed to possess ionization states that govern affinity and reactivity for the two linked hAChE re-activation steps. In alternative embodiments, the invention provides pumps, devices, subcutaneous infusion devices, continuous subcutaneous infusion devices, infusion pens, needles, reservoirs, ampoules, a vial, a syringe, a cartridge, a disposable pen or jet injector, a prefilled pen or a syringe or a cartridge, a cartridge or a disposable pen or jet injector, a two chambered or multi-chambered pump, a syringe, a cartridge or a pen or a jet injector, comprising a compound of the invention.
摘要翻译：在替代实施方案中，本发明提供了穿过血脑屏障（BBB）以催化中枢神经系统（CNS）中有机磷酸酯（OP）抑制的人乙酰胆碱酯酶（hAChE）的水解的亲核羟基亚氨基 - 乙酰胺基烷基胺解毒剂。本发明的羟基亚氨基 - 乙酰氨基烷基胺被设计成适合于AChE活性中心峡谷尺寸，以合理的亲和力结合，并与峡谷中的共轭磷酸根原子反应。本发明的羟基亚氨基 - 乙酰氨基烷基胺还被设计成具有控制两种连接的hAChE再激活步骤的亲和性和反应性的电离状态。在替代实施例中，本发明提供泵，装置，皮下输注装置，连续皮下输注装置，输液笔，针，储存器，安瓿，小瓶，注射器，药筒，一次性笔或喷射注射器，预充式笔或注射器或药筒，药筒或一次性笔或喷射注射器，包括本发明化合物的两室或多室泵，注射器，药筒或笔或喷射器。

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