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2. 发明公开

EP3312168A1 BIS-DIOX(OL)ANE COMPOUNDS 审中-公开
标题翻译： BIS-DIOX（OL）ANE化合物
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。

3. 发明授权

EP2320951B1 GALACTOSYLATED PRO-DRUGS OF NON-STEROIDAL ANTI-INFLAMMATORIES WITH IMPROVED PHARMACOKINETIC CHARACTERISTICS AND REDUCED TOXICITY OF THE STARTING DRUG 有权
标题翻译：半乳糖的NSAIDs药物前改善的药物动力学特性，减少毒性主要产品
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

4. 发明公开

EP2426107A1 Transition metal conjugated radiopharmaceuticals useful as therapeutic and/or diagnostic agents 审中-公开
标题翻译： ÜbergangsmetallkonjugierteRadiopharmazeutika als Therapie- und / oder Diagnosemittel
公开(公告)号：EP2426107A1
公开(公告)日：2012-03-07
申请号：EP10382219.3
申请日：2010-08-05
申请人： Universitat Autònoma De Barcelona
发明人： Suades I Ortuno, Joan , Lecina I Vicente, Joan , Carrer, Alessia , Mazzi, Ulderico
IPC分类号： C07D211/62 , C07D401/12 , A61K51/04 , C07F13/00 , C07H13/10
CPC分类号： C07D401/12 , A61K51/0478 , A61K51/0497 , C07D211/62 , C07F13/005
摘要： It is provided new compounds, succinimidyl ester of the Zn(II) dithiocarbamate of isonipecotic acid and succinimidyl ester of the Zn(II) dithiocarbamate of nipecotic acid; their preparation processes by reacting any salt of the above compounds with TSTU; conjugated compounds of the above ones, and their preparation processes comprising reacting the succinimidyl ester of the Zn(II) dithiocarbamate of isonipecotic acid or the succinimidyl ester of the Zn(II) dithiocarbamate of nipecotic acid with a molecule which comprises at least a primary and/or secondary amine; and transition metal conjugated compounds, and their preparation processes comprising a transmetallation reaction between the conjugated succinimidyl ester of the Zn(II) dithiocarbamate of isonipecotic acid or the succinimidyl ester of the Zn(II) dithiocarbamate of nipecotic acid with [M(CO) 3 (H 2 O) 3 ]X wherein M is a transition metal; and X is a halide anion. The invention further provides the use of the transition metal conjugated compounds as therapeutic and/or diagnostic agents.
摘要翻译：提供了新的化合物，异头otic酸的Zn（II）二硫代氨基甲酸酯的琥珀酰亚胺酯和罂粟酸的Zn（II）二硫代氨基甲酸酯的琥珀酰亚胺酯; 它们的制备方法是将上述化合物的任何盐与TSTU反应; 共轭化合物及其制备方法，其包括使异癸酸的Zn（II）二硫代氨基甲酸酯的琥珀酰亚胺酯或哌啶糖酸的Zn（II）二硫代氨基甲酸酯的琥珀酰亚胺酯与至少包含伯或二 /或仲胺; 和其过渡金属共轭化合物及其制备方法，其包括异辛酸的Zn（II）二硫代氨基甲酸酯的偶联的琥珀酰亚胺酯与哌啶酸的Zn（II）二硫代氨基甲酸的琥珀酰亚胺酯与[M（CO）3 （H 2 O）3] X其中M是过渡金属; X为卤素阴离子。本发明还提供了过渡金属共轭化合物作为治疗和/或诊断剂的用途。

5. 发明公开

EP0560055A1 Immuno-suppressing enepyranose derivatives 失效
标题翻译：免疫抑制剂。
公开(公告)号：EP0560055A1
公开(公告)日：1993-09-15
申请号：EP93101822.0
申请日：1993-02-05
申请人： ISHIHARA SANGYO KAISHA, LTD.
发明人： Mizukoshi, Sadanori, c/o Ishihara Sangyo Kaisha , Kato, Fuminori, c/o Ishihara Sangyo Kaisha , Tsukamoto, Masamitsu, c/o Ishihara Sangyo Kaisha , Kon, Kenji, c/o Ishihara Sangyo Kaisha
IPC分类号： C07H3/08 , C07H3/10 , A61K31/70 , C07H13/04 , C07H13/06 , C07H13/08 , C07H13/10 , C07H13/12 , C07H15/04 , C07H15/207 , C07D491/08
CPC分类号： C07H13/04 , C07H3/08 , C07H3/10 , C07H7/02 , C07H11/00 , C07H13/06 , C07H13/08 , C07H13/12 , C07H15/04 , C07H15/18 , C07H15/207
摘要： An immuno-suppressive agent containing, as an effective component, an enopyranose derivative of the following formula (I) or its salt:
wherein R 1 is a hydrogen atom, alkyl which may be substituted, alkenyl, alkynyl, -OSO 2 R 7 , a halogen atom, -OCOR 7 , -NHCOR 8 , alkoxy, phenyl which may be substituted or a saccharose residue, R 2 is a hydrogen atom or alkyl, R 3 is a hydrogen atom or a halogen atom, R 4 is a hydrogen atom, -COR 9 , silyl which may be substituted or alkyl which may be substituted, one of R 5 and R 6 is hydroxyl, alkoxy which may be substituted, a saccharose residue, cycloalkyloxy which may be substituted or -OCOR 10 and the other is a hydrogen atom or alkyl which may be substituted, or R 4 and R 5 together form a single bond, while R 6 is a hydrogen atom or alkyl which may be substituted, each of R 7 , R 9 and R 10 is alkyl or phenyl which may be substituted, R 8 is alkyl, phenyl which may be substituted or benzyloxy, X is a hydrogen atom, alkyl which may be substituted, alkenyl which may be substituted, alkynyl which may be substituted, cycloalkyl which may be substituted, phenyl which may be substituted, pyridyl which may be substituted, furanyl which may be substituted, thienyl which may be substituted, formyl, -COR 11 , -C(W 1 )W 2 R 11 or -SO 2 R 11 , R 11 is a chain hydrocarbon group which may be substituted, a monocyclic hydrocarbon group which may be substituted, a polycyclic hydrocarbon group which may be substituted, a monocyclic heterocycle group which may be substituted, or a polycyclic heterocycle group which may be substituted, W 1 is an oxygen atom or a sulfur atom, W 2 is an oxygen atom, a sulfur atom or -NH-, Y is a hydrogen atom, alkyl which may be substituted, alkenyl which may be substituted or alkynyl which may be substituted.
摘要翻译：含有作为有效成分的下式（I）的吡喃葡萄糖衍生物或其盐的免疫抑制剂：其中R 1为氢原子，可被取代的烷基，烯基，炔基， - OSO 2 R 7，卤素原子，-OCOR 7，-NHCOR 8，烷氧基，可被取代的苯基或蔗糖残基，R 2是氢原子或烷基，R 3是氢原子或卤素原子，R 4是氢原子，-COR 9，可被取代的甲硅烷基或可被取代的烷基，R 5和R 6之一是羟基，烷氧基可以被取代，可以被取代的蔗糖残基，可以被取代的环烷氧基或-OCOR 1，另一个是可以被取代的氢原子或烷基，或者R 4和R 5一起形成一个键，而R 6为氢原子或可被取代的烷基，R 7，R 9和R 10各自为可被取代的烷基或苯基，R 8，是烷基，可被取代的苯基或苄氧基，X是氢原子，烷基可被取代的烯基，可被取代的链烯基，可被取代的环烷基，可被取代的苯基，可被取代的吡啶基，可被取代的呋喃基，可被取代的噻吩基，甲酰基， -COR 1，-C（W 1）W 2 R 1或-SO 2 R 1，R 1是链烃基可被取代的单环烃基，可被取代的多环烃基，可被取代的多环烃基，可被取代的单环杂环基或可被取代的多环杂环基，W 1是氧原子或硫原子，W 2为氧原子，硫原子或-NH-，Y为氢原子，可被取代的烷基，可被取代的烯基或可被取代的炔基。

6. 发明授权

EP0053257B1 Verfahren zur Herstellung eines beta-D-Glucopyranosederivates 失效
标题翻译：制备β-D-吡喃葡萄糖苷衍生物的方法
公开(公告)号：EP0053257B1
公开(公告)日：1984-07-25
申请号：EP81108459.9
申请日：1981-10-17
申请人： F. HOFFMANN-LA ROCHE & CO. Aktiengesellschaft
发明人： Kiss, Joseph, Prof.
IPC分类号： C07H13/10
CPC分类号： C07H13/10

7. 发明公开

EP3990441A1 IONIZABLE LIPIDS FOR NUCLEIC ACID DELIVERY 审中-实审转让
公开(公告)号：EP3990441A1
公开(公告)日：2022-05-04
申请号：EP20835492.8
申请日：2020-06-26
申请人： Precision Nanosystems Inc
发明人： THOMAS, Anitha , JAIN, Nikita , BROWN, Andrew William
IPC分类号： C07D307/20 , A61K47/22 , A61K47/28 , A61K47/30 , A61K9/14 , C07D405/12 , C07D453/02 , C12N15/87 , C07H13/06 , C07H13/10

8. 发明授权

EP3250581B1 ALPHA-D-GALACTOSIDE INHIBITORS OF GALECTINS 有权
公开(公告)号：EP3250581B1
公开(公告)日：2021-01-20
申请号：EP16701941.3
申请日：2016-01-28
发明人： BRIMERT, Thomas , JOHNSSON, Richard , LEFFLER, Hakon , NILSSON, Ulf , ZETTERBERG, Fredrik
IPC分类号： C07H15/26 , C07H19/056 , A61K31/7056 , A61P11/00 , C07H13/08 , C07H13/10

9. 发明公开

EP3243515A1 KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF 有权
公开(公告)号：EP3243515A1
公开(公告)日：2017-11-15
申请号：EP17161699.8
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 , C07D403/04 , C07D405/14 , C07D405/04 , C07D409/04 , C07D413/04 , C07H13/10
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.

10. 发明公开

EP2481746A1 Process for producing sugar chain asparagine derivative 审中-公开
标题翻译： Verfahren zur Herstellung von eines Zuckerketten-Asparaginderivats
公开(公告)号：EP2481746A1
公开(公告)日：2012-08-01
申请号：EP12162076.9
申请日：2002-06-19
申请人： Otsuka Chemical Co., Ltd. , Kajihara, Yasuhiro
发明人： Kajihara, Yasuhiro , Sasaki, Ken
IPC分类号： C07H13/10 , C07H15/12 , C07H5/06 , C07H7/027 , C12P13/04 , C12P19/04
CPC分类号： C07H13/10 , C07H5/06 , C07H7/027 , C07H15/12 , C12P13/04 , C12P19/04 , C12P19/28 , Y02P20/55
摘要： The present invention provides a process for preparing a sugar chain asparagine derivative. According to the process, various isolated sugar chain asparagine derivatives useful in the field of the development of pharmaceutical and the like can be conveniently obtained in a large amount as compared to that of the prior art. The present invention also provides a process for preparing a sugar chain asparagine and a process for preparing a sugar chain via a step for preparing a sugar chain asparagine derivative. The present invention further provides a novel sugar chain asparagine derivative, a sugar chain asparagine and a sugar chain.
摘要翻译：本发明提供了制备糖链天冬酰胺衍生物的方法。根据该方法，与现有技术相比，可以容易地获得用于药物开发领域的各种分离的糖链天冬酰胺衍生物。本发明还提供了制备糖链天冬酰胺的方法和通过制备糖链天冬酰胺衍生物的步骤制备糖链的方法。本发明还提供了一种新型糖链天冬酰胺衍生物，糖链天冬酰胺和糖链。

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