公开(公告)号：EP2748204A1

公开(公告)日：2014-07-02

申请号：EP12838521.8

申请日：2012-10-03

申请人： Nanyang Technological University

发明人： CHAN, Bee Eng Mary ,  LI, Peng

IPC分类号： C08B37/00 ,  C08L5/00 ,  A61K31/715 ,  A61P31/04 ,  A61P31/10 ,  C07H15/12 ,  C07H15/18 ,  A61K31/7016 ,  A61K31/702 ,  A61P31/12 ,  A61P33/02

CPC分类号： C07K14/001 ,  A01N43/16 ,  C07H13/04 ,  C07H15/12 ,  C07H15/18 ,  C07K4/00 ,  C08B37/003 ,  C08H1/00 ,  C08L5/08 ,  C08L89/00

摘要： The disclosure provides cationic peptidopolysaccharides of Formula I: which has a bacterial peptidoglycan-mimetic structure, and shows outstanding broad spectrum activities against clinically significant bacteria and fungi. The structural affinity of these compounds with microbial cell wall constituents promotes its passage to the cytoplasmic membrane resulting in excellent antimicrobial activity and record high selectivity. The disclosure also describes methods of making and using cationic peptidopolysaccharides of Formula I.

公开(公告)号：EP2691407A1

公开(公告)日：2014-02-05

申请号：EP12765063.8

申请日：2012-03-20

申请人： Alectos Therapeutics Inc. ,  Merck Sharp & Dohme Corp.

发明人： KAUL, Ramesh ,  MCEACHERN, Ernest J. ,  VOCADLO, David J. ,  ZHOU, Yuanxi ,  LIU, Kun ,  SELNICK, Harold G. ,  WEI, Zhongyong ,  MU, Changwei ,  WANG, Yaode ,  WANG, Xiaona

IPC分类号： C07H15/12 ,  A61K31/7056 ,  C07H11/00 ,  C07H13/00 ,  C07H13/12 ,  C07H15/18 ,  C07H17/07 ,  C07H19/04 ,  C07H9/06 ,  C12N9/24 ,  C12Q1/34

CPC分类号： C07H19/24 ,  A61K31/7056 ,  C07D513/04 ,  C07H9/06 ,  C07H11/00 ,  C07H13/12 ,  C07H15/04 ,  C07H15/12 ,  C07H15/18 ,  C07H15/203 ,  C07H15/207 ,  C07H17/02 ,  C07H17/04 ,  C12N9/99 ,  C12Q1/34 ,  C12Y302/01169

摘要： The invention provides compounds of formula (I) with substituents as specified in Claim 1 for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceuticals compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to over-expression of O-GlcNAcase or accumulation of O-GlcNac.

摘要翻译： 本发明提供了具有权利要求1中指定的取代基的式（I）化合物用于选择性抑制糖苷酶，所述化合物的前药和包含所述化合物的化合物或前药的药物组合物。 本发明还提供了治疗与O-GlcNAcase的过度表达或O-GlcNac的积累有关的疾病和病症的方法。

公开(公告)号：EP2604619A3

公开(公告)日：2014-01-22

申请号：EP13158420.3

申请日：2010-12-13

申请人： University of Basel

发明人： Ernst, Beat ,  Herold, Janno

IPC分类号： C07H15/18 ,  C07H15/203 ,  C07H15/26 ,  A61K31/7034 ,  A61P31/04

CPC分类号： C07H15/26 ,  C07H15/18 ,  C07H15/203 ,  C07H15/207

摘要： Compounds of the formula (I)

wherein n is 0, 1 or 2, R 1 is aryl, heteroaryl or heterocyclyl, and R 2 and R 3 are hydrogen or a substituent as described in the specification, are useful for the prevention and treatment of bacterial infections, in particular of urinary infections caused by E. coli.

公开(公告)号：EP2536737A4

公开(公告)日：2013-10-02

申请号：EP11744298

申请日：2011-02-21

申请人： GLYCOM AS

发明人： BAJZA ISTVAN ,  DEKANY GYULA ,  AGOSTON KAROLY ,  PEREZ IGNACIO FIGUEROA ,  BOUTET JULIEN ,  HEDEROS MARKUS ,  HORVATH FERENC ,  KOVACS-PENZES PIROSKA ,  KROEGER LARS ,  ROEHRIG CHRISTOPH ,  SCHROVEN ANDREAS ,  VRASIDAS IOANNIS ,  TRINKA PETER ,  KALMAR LASZLO ,  KOVACS IMRE ,  DEMKO SANDOR ,  AGOSTON AGNES ,  RISINGER CHRISTIAN

IPC分类号： C07H15/18 ,  A23L1/29 ,  A61K31/702 ,  C07H11/00 ,  C07H13/04

CPC分类号： C07H3/06 ,  A23L29/30 ,  A23L33/10 ,  A23V2002/00 ,  C07H1/00 ,  C07H11/00 ,  C07H13/04 ,  C07H15/18 ,  A23V2250/28

摘要： The present invention relates to a new polymorphic form of the tetrasaccharide of formula (I) and the preperation thereof.

公开(公告)号：EP2155001A4

公开(公告)日：2013-06-26

申请号：EP08741608

申请日：2008-04-14

申请人： MALAYSIAN PALM OIL BOARD

发明人： TAN YEW AI ,  RAVIGADEVI A P SAMBANTHMURTHI ,  KALYANA SUNDRAM A L MANICKAM ,  MOHD BASRI BIN WAHID

IPC分类号： A23L3/3472 ,  A61K36/889 ,  C07H15/18

CPC分类号： A61K36/889 ,  A23D9/007 ,  A23L3/3472 ,  A23L3/3481 ,  A23L3/3544 ,  A23V2002/00 ,  A23V2200/02 ,  A23V2250/2132 ,  A23V2250/2116

公开(公告)号：EP2511282A1

公开(公告)日：2012-10-17

申请号：EP12176402.1

申请日：2010-05-11

申请人： Janssen Products, L.P. ,  MEDIVIR AB

发明人： Jonckers, Tim Hugo Maria ,  Raboisson, Pierre Jean-Marie Bernard ,  Vandyck, Koen ,  Van Hoof, Steven Maurice Paula ,  Hu, Lili ,  Tahri, Abdellah

IPC分类号： C07H19/06 ,  C07H19/10 ,  C07H19/067 ,  A61K31/7072 ,  C07D493/10 ,  C07H15/18 ,  C07H15/04 ,  C07D201/00

CPC分类号： C07H19/10 ,  C07D493/10 ,  C07H15/04 ,  C07H15/18 ,  C07H19/067

摘要： Compounds of the formula I:

including any possible stereoisomers thereof, wherein:
R 4
is a monophosphate, diphosphate or triphosphate ester; or R 4 is

R 7
is optionally substituted phenyl, optionally substituted naphthyl, or optionally substituted indolyl;
R 8 and R 8'
are hydrogen, C 1 -C 6 alkyl, benzyl, or phenyl; or R 8 and R 8' form C 3 -C 7 cycloalkyl;
R 9
is C 1 -C 10 alkyl, C 3 -C 7 cycloalkyl, phenyl or phenyl-C 1 -C 6 alkyl, wherein the phenyl moiety in phenyl or phenyl-C 1 -C 6 alkyl is optionally substituted;

or a pharmaceutically acceptable salt or solvate thereof;
pharmaceutical formulations and the use of compounds I as HCV inhibitors.

摘要翻译： 式I化合物：包括其任何可能的立体异构体，其中：R 4是单磷酸酯，二磷酸酯或三磷酸酯; 或R 4为R 7为任选取代的苯基，任选取代的萘基或任选取代的吲哚基; R 8和R 8'是氢，C 1 -C 6烷基，苄基或苯基; 或R 8和R 8'形成C 3 -C 7环烷基; R 9是C 1 -C 10烷基，C 3 -C 7环烷基，苯基或苯基-C 1 -C 6烷基，其中苯基或苯基-C 1 -C 6烷基中的苯基部分任选被取代; 或其药学上可接受的盐或溶剂化物; 药物制剂和化合物I作为HCV抑制剂的用途。

公开(公告)号：EP2454268A1

公开(公告)日：2012-05-23

申请号：EP10799312.3

申请日：2010-07-15

申请人： The University of British Columbia

发明人： WITHERS, Stephen ,  WATTS, Andrew Graham ,  KIM, Jin Hyo ,  WENNEKES, Tom

IPC分类号： C07H5/02 ,  A61K31/7012 ,  A61P31/16 ,  C07H13/04 ,  C07H13/12 ,  C07H15/12 ,  C07H15/18 ,  C12N9/24

CPC分类号： C07D309/14 ,  A61K31/351 ,  A61K31/655 ,  C07H1/00 ,  C07H13/00 ,  C07H13/04 ,  C07H13/12 ,  C07H15/12 ,  C07H15/18

摘要： Compounds of structural formula (I) useful for the treatment or prophylaxis of viral infection, particularly viral influenza are provided Pharmaceutical preparations thereof and methods for their preparation are also described. The therapeutic effect is achieved via inhibition of viral neuraminidases, also known as viral sialidases. These neuraminidases are classified under the GH34 family of viral enzymes.

摘要翻译： 提供可用于治疗或预防病毒感染的结构式（I）的化合物，特别是病毒性流感。还描述了其药物制剂及其制备方法。 治疗效果通过抑制病毒性神经氨酸酶（也称为病毒性唾液酸酶）来实现。 这些神经氨酸酶分类为GH34家族的病毒酶。

公开(公告)号：EP2276773A2

公开(公告)日：2011-01-26

申请号：EP09741892.5

申请日：2009-05-07

申请人： La Ferla, Barbara ,  Nicotra, Francesco ,  Balsari, Andrea ,  Rumio, Cristiano

发明人： LA FERLA, Barbara ,  NICOTRA, Francesco ,  BALSARI, Andrea ,  PALAZZO, Marco ,  RUMIO, Cristiano

IPC分类号： C07H7/04 ,  C07H15/18 ,  A61K31/7034 ,  A61P29/00

CPC分类号： C07H7/04 ,  C07H15/18

摘要： Compounds of the general formula (I) and (II) (including formulae (III) to (V)), wherein X - -CH
2 -, -O-, -S- n = 0-10 Y = -NH-, -NHSO
2 -, -NHSO-, -NHCO-, -S-, -O-, -CH=CH- R
1 -R
7 , equal or different can be hydrogen, alkyl C
1 -C
4 , alkenyl C
2 -C
4 , cycloalkyl C
3 -C
7 , aryl or heteroaryl; may be substituted with one or more alkyl C
1 -C
4 , alkoxyl C
1 -C
4 , alkylthio C
1 -C
4 or halogens; -NR
8 R
9 , where R
8 e R
9 , equal or different, represent hydrogen, alkyl C
1 -C
4 , alkenyl C
2 -C
4 , cycloalkyl C
3 -C
7 , aryl or heteroaryl, may be substituted with one or more C
1 -C
4 , alkoxyl C
1 -C
4 , alkylthio C
1 -C
4 or halogens; -(CH
2 )
n ,-COOR
10 , with n' = 0-4 and R
3 = hydrogen or alkyl C
1 -C
4 , and their addition salts with organic and inorganic acids, or alkaline and alkaline earth metal or ammonium ions, with the exclusion of the compounds having the following formulae ((VI) to (IX)).

公开(公告)号：EP2272855A2

公开(公告)日：2011-01-12

申请号：EP10013163.0

申请日：2006-05-30

申请人： The University Of Manchester

发明人： The designation of the inventor has not yet been filed

IPC分类号： C07H15/18 ,  C08B37/10 ,  C07H1/00

CPC分类号： C08B37/006 ,  C07H1/00 ,  C07H15/18 ,  C08B37/00 ,  C08B37/0075

摘要： The present invention provides processes for the production of polysaccharides containing the L-iduronate subunit, for example, heparin-type polysaccharides. New intermediate compounds and processes developed during the production of said polysaccharides are also presented.

摘要翻译： 本发明提供了生产含有L-艾杜糖醛酸亚基的多糖的方法，例如肝素型多糖。 还介绍了在生产所述多糖期间开发的新中间体化合物和工艺。

公开(公告)号：EP2247603A1

公开(公告)日：2010-11-10

申请号：EP09711166.0

申请日：2009-02-11

申请人： Dow AgroSciences LLC

发明人： CROUSE, Gary ,  SPARKS, Thomas ,  MCLEOD, CaSandra ,  DEMETER, David ,  BRYAN, Kristy ,  BROWN, Annette ,  DENT, William ,  CUDWORTH, Denise ,  NUGENT, Jaime ,  HUNTER, Ricky ,  SAMARITONI, Jack

IPC分类号： C07H13/12 ,  C07H15/18 ,  C07H15/26 ,  A01N43/40 ,  A01N43/50 ,  A01N43/653 ,  A01N47/02 ,  A01N47/18

CPC分类号： C07H13/12 ,  A01N43/00 ,  A01N43/16 ,  A01N43/36 ,  A01N43/40 ,  A01N43/50 ,  A01N43/56 ,  A01N43/653 ,  A01N43/72 ,  A01N43/76 ,  A01N43/78 ,  A01N43/80 ,  A01N43/82 ,  A01N47/02 ,  A01N47/06 ,  A01N47/18 ,  A01N51/00 ,  C07D309/10 ,  C07D309/12 ,  C07D405/14 ,  C07D407/14 ,  C07H15/18 ,  C07H15/26 ,  G06Q99/00

摘要： The invention disclosed in this document is related to the field of pesticides and their use in controlling pests. A compound having the following structure is disclosed.

摘要翻译： 本文件披露的发明涉及农药领域及其在防治害虫方面的应用。 公开了具有以下结构的化合物。