公开(公告)号：EP3010345A1

公开(公告)日：2016-04-27

申请号：EP14814257.3

申请日：2014-06-20

申请人： The Regents of the University of California ,  The Scripps Research Institute Office of Patent Counsel TPC8

发明人： FOKIN, Valery ,  SHARPLESS, Karl Barry ,  ECKMANN, Lars ,  MIYAMOTO, Yukiko

IPC分类号： A01N43/64 ,  A61K31/41 ,  A61K31/415 ,  C07D233/91

CPC分类号： C07D405/14 ,  A01N43/647 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/427 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/502 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D233/91 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D409/04 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07H15/26 ,  Y02A50/491 ,  A61K2300/00

摘要： Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to imidazole, thiazole, and furan derivatives and their use as therapeutic agents.

公开(公告)号：EP2956451A1

公开(公告)日：2015-12-23

申请号：EP14751631.4

申请日：2014-02-15

申请人： The Regents of the University of California ,  The Scripps Research Institute

发明人： TAYLOR,Palmer ,  RADIC, Zoran ,  SHARPLESS, K., Barry ,  FOKIN, Valery ,  SIT, Rakesh

IPC分类号： C07D403/02 ,  C07D225/02 ,  A61K31/46 ,  A61P25/00

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.

公开(公告)号：EP3057582A1

公开(公告)日：2016-08-24

申请号：EP14853603.0

申请日：2014-10-15

申请人： The Regents of the University of California ,  The Scripps Research Institute

发明人： TAYLOR, Palmer ,  RADIC, Zoran ,  FOKIN, Valery

IPC分类号： A61K31/15 ,  A61K31/415 ,  A01N33/24

CPC分类号： A61K31/4164 ,  A61K31/4439 ,  A61K31/5377 ,  A61K38/465 ,  A61K45/06 ,  C12Y301/01008

摘要： Provided are N-alkyl imidazole 2-aldoximes, including cationic imidazolium and uncharged tertiary imidazole aldoximes, and compositions and methods for making and using them, including methods for reactivating human butyrylcholinesterase (hBChE) or acetylcholinesterase (hAChE ) inhibited by organophosphate (OP). By administration of a composition of the invention, the inactive or conjugated hBChE-OP or hAChE-OP is reactivated and the catalytic cycle of turnover and inactivation of the OP is completed; and in alternative embodiments, secondary mechanisms of reversible protection of hBChE and hAChE from irreversible inactivation by OPs and reactivation of tissue AChE also contribute to overall efficacy.