公开(公告)号：EP2925803B1

公开(公告)日：2017-11-29

申请号：EP13860053.1

申请日：2013-12-03

申请人： The Scripps Research Institute

发明人： DONG, Jiajia ,  FOKIN, Valery ,  KRASNOVA, Larisa ,  KWISNEK, Luke R. ,  OAKDALE, James S. ,  SHARPLESS, K. Barry

IPC分类号： C08G65/40

CPC分类号： C08G75/00 ,  C08G64/06 ,  C08G64/24 ,  C08G65/40 ,  C08G65/4012 ,  C08G2650/40 ,  C08J5/18 ,  C08J2369/00 ,  C08J2381/00

摘要： Condensation of fluoro-substituted and silyl-substituted monomers provides polymers suitable for use, e.g., as engineering polymers. A monomer composition is condensed in the presence of a basic catalyst. The monomer composition contains a compound of formula F—X—F and a compound of formula (R1)3Si—Z—Si(R1)3, and forms an alternating X—Z polymer chain and a silyl fluoride byproduct. X has the formula -A(-R2-A)n-; each A is SO2, C(═O), or Het; R2 is an organic moiety; n is 0 or 1; Het is an aromatic nitrogen heterocycle; Z has the formula -L-R3-L-; each L is O, S, or N(R4); and each R3 is an organic moiety, and R4 comprises H or an organic moiety.

公开(公告)号：EP1507769B1

公开(公告)日：2010-05-26

申请号：EP03731490.3

申请日：2003-05-30

申请人： THE SCRIPPS RESEARCH INSTITUTE

发明人： SHARPLESS, Barry, K. ,  FOKIN, Valery ,  ROSTOVSEV, Vsevolod ,  GREEN, Luke ,  HIMO, Fahmi

IPC分类号： C07D249/04

CPC分类号： C07D249/04 ,  B01J31/1805 ,  B01J2231/327 ,  B01J2531/16 ,  B01J2531/96 ,  C07D249/06 ,  C07D403/06

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：EP2925803A1

公开(公告)日：2015-10-07

申请号：EP13860053.1

申请日：2013-12-03

申请人： The Scripps Research Institute

发明人： DONG, Jiajia ,  FOKIN, Valery ,  KRASNOVA, Larisa ,  KWISNEK, Luke R. ,  OAKDALE, James S. ,  SHARPLESS, K. Barry

IPC分类号： C08G65/40

CPC分类号： C08G75/00 ,  C08G64/06 ,  C08G64/24 ,  C08G65/40 ,  C08G65/4012 ,  C08G2650/40 ,  C08J5/18 ,  C08J2369/00 ,  C08J2381/00

摘要： Condensation of fluoro-substituted and silyl-substituted monomers provides polymers suitable for use, e.g., as engineering polymers. A monomer composition is condensed in the presence of a basic catalyst. The monomer composition contains a compound of formula F—X—F and a compound of formula (R1)3Si—Z—Si(R1)3, and forms an alternating X—Z polymer chain and a silyl fluoride byproduct. X has the formula -A(-R2-A)n-; each A is SO2, C(═O), or Het; R2 is an organic moiety; n is 0 or 1; Het is an aromatic nitrogen heterocycle; Z has the formula -L-R3-L-; each L is O, S, or N(R4); and each R3 is an organic moiety, and R4 comprises H or an organic moiety.

公开(公告)号：EP1943004A2

公开(公告)日：2008-07-16

申请号：EP06815970.6

申请日：2006-09-29

申请人： THE SCRIPPS RESEARCH INSTITUTE

发明人： FOKIN, Valery ,  JIA, Guochen ,  SHARPLESS, K. Barry

IPC分类号： B01D21/01 ,  B01J13/00

CPC分类号： C07D249/04 ,  C07F17/02

摘要： A convenient process for the regioselective synthesis of 1 ,5-disubstituted 1 ,2,3-triazoles and 1 ,4,5-trisubstituted 1 ,2,3-triazoles from organic azides and alkynes employs catalytic ruthenium.

公开(公告)号：EP1910468A1

公开(公告)日：2008-04-16

申请号：EP06787845.4

申请日：2006-07-18

申请人： THE SCRIPPS RESEARCH INSTITUTE

发明人： WU, Peng ,  FOKIN, Valery ,  SHARPLESS, K., Barry

IPC分类号： C08L67/07 ,  C08F126/06 ,  C08G73/06

CPC分类号： C08G63/06 ,  C08G83/003

摘要： A series of AB-type amphiphilic dendritic polyesters have been prepared divergently, in which two hybrids were coupled via the copper(l)-catalyzed triazole formation.

公开(公告)号：EP1507769B2

公开(公告)日：2017-10-11

申请号：EP03731490.3

申请日：2003-05-30

申请人： THE SCRIPPS RESEARCH INSTITUTE

发明人： SHARPLESS, Barry, K. ,  FOKIN, Valery ,  ROSTOVSEV, Vsevolod ,  GREEN, Luke ,  HIMO, Fahmi

IPC分类号： C07D249/04

CPC分类号： C07D249/04 ,  B01J31/1805 ,  B01J2231/327 ,  B01J2531/16 ,  B01J2531/96 ,  C07D249/06 ,  C07D403/06

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.

公开(公告)号：EP1943004B1

公开(公告)日：2015-06-03

申请号：EP06815970.6

申请日：2006-09-29

申请人： THE SCRIPPS RESEARCH INSTITUTE

发明人： FOKIN, Valery ,  JIA, Guochen ,  SHARPLESS, K. Barry

IPC分类号： C07D249/04 ,  C07F17/02

CPC分类号： C07D249/04 ,  C07F17/02