公开(公告)号：EP3312168A1

公开(公告)日：2018-04-25

申请号：EP16194629.8

申请日：2016-10-19

申请人： Koninklijke Coöperatie Cosun U.A.

发明人： Lazeroms, Robert ,  Raaijmakers, Harry

IPC分类号： C07D317/22 ,  C07H9/04 ,  C07H13/10 ,  C07H13/12

CPC分类号： C07D317/22 ,  C07H9/04 ,  C07H13/10 ,  C07H13/12

摘要： The present invention relates to new bi-functional and polyfunctional bis-dioxolanes and bis-dioxanes. The present inventors have established that the bis-dioxolanes and bis-dioxanes of the invention are highly advantageous as building blocks, cross-linking and/or coupling agents in polymer engineering. They can be derived from biomass sources in a highly efficient manner. The production of the present bis-dioxolanes and bis-dioxanes from biomass has the particular advantage that it facilitates the introduction of desired functionality in a highly flexible manner. Hence, the present invention provides novel bi- or polyfunctional bis-dioxolanes and bis-dioxanes, their production from renewable (biomass) sources, as well as their use in the engineering of polymers.

摘要翻译： 本发明涉及新的双官能和多官能双二氧戊环和双二恶烷。 本发明人已经确定，本发明的双二氧戊环和双二恶烷作为聚合物工程中的结构单元，交联和/或偶联剂是非常有利的。 它们可以以高效的方式从生物质来源获得。 从生物质生产本发明的双二氧戊环和双二恶烷具有特别的优点，即它以高度灵活的方式促进了所需功能的引入。 因此，本发明提供了新的双或多官能双二氧戊环和双二恶烷，它们由可再生（生物质）来源生产，以及它们在聚合物工程中的用途。

公开(公告)号：EP2905620B1

公开(公告)日：2017-12-13

申请号：EP13843405.5

申请日：2013-10-01

申请人： Hirosaki University

发明人： YAMADA, Katsuya ,  TESHIMA, Tadashi ,  YAMAMOTO, Toshihiro

IPC分类号： G01N33/58 ,  A61K49/00 ,  C07H5/06 ,  C07H15/12 ,  C12Q1/02

CPC分类号： G01N33/5091 ,  A61K49/0039 ,  A61K49/0052 ,  C07H3/02 ,  C07H13/10 ,  G01N33/533 ,  G01N33/574 ,  G01N33/582 ,  G01N2400/00 ,  G01N2800/7028

摘要： The present invention aims at providing: a sugar derivative capable of producing a blue fluorescent col-or, which can be used for the imaging of a cell or an intracellular molecule; and a method for imaging a cell using the derivative. The present invention also aims at providing: a method for detecting a cancer cell with high accuracy by means of imaging; and an imaging agent for use in the method. The present invention provides: a fluorescence-labeled sugar derivative having, in the molecule thereof, 3-carboxy-6,8-difluoro-7-hydroxycoumarin or 3-carboxymethyl-6,8-di-fluoro-7-hydroxy-4-methylcoumarin as a fluorescent molecular group; and an imaging agent for a cell and a method for imaging a cell, in each of which the derivative is used. The present invention also provides an imaging agent for a cancer cell and a method for imaging a cancer cell, in each of which an L-glucose derivative having, in the molecule thereof, the fluorescent molecular group is used.

公开(公告)号：EP2966078A3

公开(公告)日：2016-03-09

申请号：EP14194168.2

申请日：2007-10-26

申请人： MethylGene Inc. ,  Forum Pharmaceuticals Inc.

发明人： Deziel, Robert ,  Leit, Silvana ,  Beaulieu, Patrick ,  Chantigny, Yves, Andre ,  Mancuso, John ,  Tessier, Pierre ,  Shapiro, Gideon ,  Chesworth, Richard ,  Smil, David

IPC分类号： C07D498/04 ,  C07D487/08 ,  C07D223/28 ,  A61P25/00 ,  A61K31/553 ,  A61K31/55 ,  A61K31/4995

CPC分类号： C07D498/04 ,  C07C259/06 ,  C07C259/10 ,  C07D209/02 ,  C07D209/08 ,  C07D209/52 ,  C07D209/94 ,  C07D221/12 ,  C07D223/16 ,  C07D223/20 ,  C07D223/22 ,  C07D223/24 ,  C07D223/26 ,  C07D223/28 ,  C07D225/08 ,  C07D239/28 ,  C07D239/34 ,  C07D239/42 ,  C07D243/24 ,  C07D243/38 ,  C07D265/38 ,  C07D267/14 ,  C07D267/18 ,  C07D267/20 ,  C07D279/22 ,  C07D279/26 ,  C07D281/16 ,  C07D285/36 ,  C07D291/08 ,  C07D295/155 ,  C07D313/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/06 ,  C07D413/12 ,  C07D471/04 ,  C07D471/08 ,  C07D471/14 ,  C07D487/04 ,  C07D487/08 ,  C07D487/14 ,  C07D491/08 ,  C07D495/04 ,  C07D513/04 ,  C07H13/10

摘要： This invention relates to five specific N-hydroxybenzamide compounds for the inhibition of histone deacetylase: N-hydroxy-4-(5-(p-tolyl)-2,5-diazabicyclo[2.2.1]heptan-2-yl)benzamide; N-hydroxy-4-(5-(3-methoxyphenyl)-2,5-diazabicyclo[2.2.1]heptan-2-yl)benzamide; N-hydroxy-4-(5-(4-(trifluoromethyl)pyridin-2-yl)-2,5-diazabicyclo[2.2.1]heptan-2-yl)benzamide; 4-(benzo[b]thieno[2,3-f][1,4]oxazepin-10-yl)-N-hydroxybenzamide; and 4-(10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)-N-hydroxybenzamide.

公开(公告)号：EP2320951B1

公开(公告)日：2016-01-06

申请号：EP09787810.2

申请日：2009-07-29

申请人： Stewart Italia SRL ,  Rimoli, Maria Grazia ,  Calignano, Antonio ,  Cuomo, Rosario ,  Boatto, Gianpiero

发明人： ABIGNENTE, Enrico ,  MELISI, Daniela ,  CURCIO, Annalisa ,  LUONGO, Elvira ,  LA RANA, Giovanna ,  SASSO, Oscar ,  SARNELLI, Giovanni ,  RUSSO, Roberto ,  NIEDDU, Maria ,  CIRILLO, Carla ,  DE LUCIA, Salvatore

IPC分类号： A61K47/48 ,  A61P29/00 ,  C07H13/02 ,  C07H13/04 ,  C07H13/08 ,  C07H13/10 ,  A61K31/7024

CPC分类号： A61K31/7024 ,  A61K47/549 ,  C07H13/02 ,  C07H13/04 ,  C07H13/08 ,  C07H13/10

公开(公告)号：EP2343286B1

公开(公告)日：2014-12-31

申请号：EP11152576.2

申请日：2007-10-26

申请人： MethylGene Inc. ,  Forum Pharmaceuticals Inc.

发明人： Deziel, Robert ,  Leit, Silvana. ,  Beaulieu, Patrick. ,  Chantigny, Yves Andre. ,  Mancuso, John ,  Tessier, Pierre. ,  Shapiro, Gideon. ,  Chesworth, Richard. ,  Smil, David

IPC分类号： C07D267/20 ,  C07D281/16

CPC分类号： C07D498/04 ,  C07C259/06 ,  C07C259/10 ,  C07D209/02 ,  C07D209/08 ,  C07D209/52 ,  C07D209/94 ,  C07D221/12 ,  C07D223/16 ,  C07D223/20 ,  C07D223/22 ,  C07D223/24 ,  C07D223/26 ,  C07D223/28 ,  C07D225/08 ,  C07D239/28 ,  C07D239/34 ,  C07D239/42 ,  C07D243/24 ,  C07D243/38 ,  C07D265/38 ,  C07D267/14 ,  C07D267/18 ,  C07D267/20 ,  C07D279/22 ,  C07D279/26 ,  C07D281/16 ,  C07D285/36 ,  C07D291/08 ,  C07D295/155 ,  C07D313/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/06 ,  C07D413/12 ,  C07D471/04 ,  C07D471/08 ,  C07D471/14 ,  C07D487/04 ,  C07D487/08 ,  C07D487/14 ,  C07D491/08 ,  C07D495/04 ,  C07D513/04 ,  C07H13/10

公开(公告)号：EP2750677A1

公开(公告)日：2014-07-09

申请号：EP12828501.2

申请日：2012-08-28

申请人： CHDI Foundation, Inc.

发明人： COURTNEY, Stephen Martin ,  PRIME, Michael ,  MITCHELL, William ,  BROWN, Christopher John ,  DE AGUIAR PENA, Paula C. ,  JOHNSON, Peter ,  DOMINGUEZ, Celia ,  TOLEDO-SHERMAN, Leticia M. ,  MUNOZ, Ignacio

IPC分类号： A61K31/44 ,  C07D401/00

CPC分类号： C07D239/28 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D491/048 ,  C07D491/052 ,  C07H13/10

摘要： Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

摘要翻译： 本文提供了某些化学实体。 还提供了包含至少一种化学实体和一种或多种药学上可接受的载体的药物组合物。 描述了治疗患有对抑制KMO活性有响应的某些疾病和病症的患者的方法，其包括向这些患者施用有效量的至少一种化学实体，以减轻疾病或病症的体征或症状。 这些疾病包括神经退行性疾病，如亨廷顿病。 还描述了治疗方法，包括施用至少一种化学实体作为单一活性剂或施用与一种或多种其他治疗剂组合的至少一种化学实体。 还提供了筛选能够抑制KMO活性的化合物的方法。

公开(公告)号：EP1577316A1

公开(公告)日：2005-09-21

申请号：EP03768216.8

申请日：2003-12-25

申请人： Kajihara, Yasuhiro ,  OTSUKA CHEMICAL COMPANY, LIMITED

发明人： KAJIHARA, Yasuhiro ,  KAKEHI, Kazuaki ,  FUKAE, Kazuhiro, c/o OTSUKA CHEMICAL CO., LTD.

IPC分类号： C07H15/26 ,  C08B37/00 ,  G01N30/48

CPC分类号： C07H13/10 ,  B01D15/3823 ,  B01J20/286 ,  B01J20/3274 ,  B01J20/328 ,  B01J2220/54 ,  C07H15/26

摘要： An asparagine-linked oligosaccharide of the formula (1) given below having undeca- to tri-saccharides
wherein R 1 and R 2 are each a hydrogen atom or a group of the formulae (2) to (6) disclosed in the specification and may be the same or different, and Q is a biotin group or FITC group,
   an asparagine-linked oligosaccharide derivative containing at least one fucose in N-acetylglucosamine on the nonreducing terminal side of an asparagine-linked oligosaccharide wherein the amino group of asparagine is modified with a biotin group or FITC group,
   a microplate having immobilized thereto a biotinated asparagine-linked oligosaccharide, and
   an affinity column having immobilized thereto a biotinated asparagine-linked oligosaccharide.

公开(公告)号：EP1549598A1

公开(公告)日：2005-07-06

申请号：EP03724672.5

申请日：2003-06-06

申请人： Cortical Pty Ltd

发明人： MORAND, Eric, Francis ,  ISKANDER, Magdy, Naguib ,  DANYLEC, Basil

IPC分类号： C07C43/205

CPC分类号： C07D403/12 ,  A61K31/4184 ,  A61K31/585 ,  C07C43/225 ,  C07C43/23 ,  C07C45/004 ,  C07C45/46 ,  C07C59/58 ,  C07C65/24 ,  C07C65/28 ,  C07C69/94 ,  C07C205/59 ,  C07C229/70 ,  C07C255/37 ,  C07C309/60 ,  C07C309/75 ,  C07C333/04 ,  C07D235/26 ,  C07D307/83 ,  C07D319/18 ,  C07H13/10 ,  Y02A50/401 ,  Y02A50/411 ,  C07C47/575 ,  C07C49/84

摘要： Where Y, R 1 -R 8 and R 101 -R 108 are as defined in the specification. Compounds of formula (II) and methods of inhibiting the cytokine or biological activity of Macrophage Migrating Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) are provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (1), either alone or as part of a combination therapy.

公开(公告)号：EP1421093B1

公开(公告)日：2005-06-29

申请号：EP02768713.6

申请日：2002-08-26

申请人： Pharmacia Corporation

发明人： CHAO, Robert, S. ,  HAWLEY, Michael ,  REEDER, Lisa, M. ,  JONES, Donald, P.

IPC分类号： C07H15/00

CPC分类号： C07H13/10 ,  C07H15/16 ,  C07H15/26

摘要： The antibiotic drug clindamycin is provided as a crystalline free base. Three polymorphic/pseudopolymorphic forms of crystalline clindamycin free base are disclosed. Also provided are pharmaceutical compositions comprising crystalline clindamycin free base. Processes for preparing crystalline clindamycin free base and compositions thereof are also provided along with methods for treating medical conditions with the pharmaceutical compositions.

公开(公告)号：EP0698031A1

公开(公告)日：1996-02-28

申请号：EP94917377.0

申请日：1994-05-13

申请人： CYTEL CORPORATION

发明人： DeFREES, Shawn, A. ,  GAETA, Federico, C., A. ,  GAUDINO, John, J. ,  ZHENG, Zhongli ,  HAYASHI, Masaji 2-17, Fujiwaradai-naka 6-chome

IPC分类号： C07H13 ,  A61K31 ,  A61K38 ,  A61P7 ,  A61P9 ,  A61P29 ,  C07H3 ,  C07H15

CPC分类号： A61K31/702 ,  A61K31/70 ,  C07H3/04 ,  C07H3/06 ,  C07H13/08 ,  C07H13/10 ,  C07H15/04

摘要： The present invention relates to analogues of Sialyl Lewisx that inhibit cellular adhesion between a selectin receptor and cells that express sialyl Lex on their surfaces, as well as methods and compositions using the same, intermediates and methods for the preparation of the cellular adhesion inhibitor compounds and their intermediates. A contemplated intermediate or inhibitor compound has the 2-N-acetyl moiety of the GlcNAc substituted with YR1 wherein Y is C(O), SO¿2?, HNC(O) or SC(O) and R?1¿ is aryl, substituted aryl, or phenyl C¿1?-C3 alkylene moieties.