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61. 发明公开

EP1676853A4 ALPHA-1-PHOSPHORYLATED-2-DEOXY-2-FLUOROARABINOSIDE AND PROCESS FOR PRODUCING 2 -DEOXY-2 -FLUORO-BETA-D-ARABINONUCLEOSID E 审中-公开
标题翻译： ALPHA-1磷酸化的-2-脱氧-2- FLUORARABINOSID及其制造方法的2-脱氧-2-氟-β-D-ARABINONUKLEOSID
公开(公告)号：EP1676853A4
公开(公告)日：2009-12-23
申请号：EP04792854
申请日：2004-10-22
申请人： YAMASA CORP
发明人： YAMADA KOHEI , MATSUMOTO NORITAKE , HAYAKAWA HIROYUKI
IPC分类号： C07H1/02 , C07H11/04 , C12P19/40
CPC分类号： C12P19/40 , C07H1/02 , C07H11/04

62. 发明授权

EP1709056B1 PHOSPHORAMIDATE DERIVATIVES 有权
标题翻译：磷酰胺衍生物
公开(公告)号：EP1709056B1
公开(公告)日：2009-06-17
申请号：EP05701927.5
申请日：2005-01-18
申请人： University College Cardiff Consultants Limited
发明人： MCGUIGAN, Christopher , CARANGIO, Antonella , CATERSON, Bruce , HUGHES, Clare, Elizabeth , CURTIS, Clare Louise
IPC分类号： C07H11/04 , A61K31/7024 , A61P29/00
CPC分类号： C07H11/04 , Y02P20/55
摘要： The present invention provides a phosphoramidate compound comprising the structure (I) Formula (I)wherein: X comprises a monosaccharide group comprising the structure (II) or (III),8Formula (II) , (III) B and B are independently selected from the group consisting of -O-, -CH2- and a bond, preferably -O-; R is selected from the group consisting of -H, protecting groups and monovalent hydrocarbon radicals; R and R are independently selected from the group consisting of -H and monovalent hydrocarbon radicals, or R2 and R3 together form an alkylene or heteroalkylene chain so as to provide, together with the C atom to which they are attached, a cyclic system; R is selected from the group consisting of -H and monovalent hydrocarbon radicals; R -R are independently selected from the group consisting of -H, -OH, N3, halogen, -SH,-OR , -SR , -NHR , -NR 2 and group Formula (1) wherein B" is selected from the group consisting of -O-, -CH2- and a bond, preferably -O-; R -R are independently selected and are as defined above, wherein R and R are independently selected from the group consisting of -H, monovalent hydrocarbon radicals, protecting groups and -C(O)R , and wherein R is selected from the group consisting of -H, monovalent hydrocarbon radicals, protecting groups and -C(O)R , wherein R is selected from the group consisting of -H and monovalent hydrocarbon radicals; or a pharmaceutically acceptable derivative or metabolite of a compound of formula (I). The present invention also provides processes for the production of (I) and uses thereof.
摘要翻译：本发明提供了包含结构（I）式（I）的氨基磷酸酯化合物，其中：X包含包含结构（II）或（III）的单糖基团，式（II），（III）B和B独立地选自由-O - ， - CH 2 - 和键组成的基团，优选-O-; R 1选自-H，保护基和单价烃基; R 2和R 3独立地选自-H和一价烃基，或者R 2和R 3一起形成亚烷基或亚杂烷基链，从而与它们所连接的C原子一起提供，一个循环系统; R 4选自-H和一价烃基; R 5 -R 12独立地选自-H，-OH，N 3，卤素，-SH，-OR 13，-SR 13'，-NHR 14， - NR 14 2和式（1）的基团，其中B“选自-O - ， - CH 2 - 和键，优选-O-; R 1 -R 4独立地选自如上所定义，其中R 13和R 13'独立地选自-H，一价烃基，保护基和-C（O）R 15，并且其中R 14和R 14独立地选自-H，选自-H，一价烃基，保护基和-C（O）R 15，其中R 15选自-H和一价烃基;或药学上可接受的基团（I）化合物的衍生物或代谢物，本发明还提供了用于生产（I）的方法及其用途。

63. 发明公开

EP2019147A1 NOVEL K04-0144 SUBSTANCES AND PROCESS FOR PRODUCTION THEREOF 有权
标题翻译： NOVEL K04-0144物质及其生产方法
公开(公告)号：EP2019147A1
公开(公告)日：2009-01-28
申请号：EP06732665.2
申请日：2006-05-16
申请人： THE KITASATO INSTITUTE
发明人： TOMODA, Hiroshi , KIM, Yong-pil , HANAKI, Hideaki , MATSUMOTO, Atsuko , TAKAHASHI, Yoko , OMURA, Satoshi
IPC分类号： C12P19/26 , C07H11/04 , A61K31/7024 , A61P31/04
CPC分类号： C07H11/04 , C07C323/59 , C12P13/02 , C12P19/26 , C12P19/44 , C12R1/465
摘要： Amicroorganism represented by a strain K04-0144 belonging to Streptomyces sp. having ability to produce K04-0144 substance is cultured in the medium, and the isolated K04-0144A substance, K04-0144B substance and K04-0144C substance therefrom have strong antibacterial activities against Gram-positive bacteria including methicillin-resistant Streptococcus aureus (MRSA), consequently these are useful as the therapeutic agents for infectious disease caused by MRSA as well as infectious diseases caused by multidrug including β-lactam antibiotics resistant bacteria. Further, similarly, since the novel K04-0144D substance isolated from the cultured liquid has the action for enhancing the effect of β-lactam antibiotics, which are utilized as the antibacterial agents, in combination with them, it is useful as the therapeutic agent for infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA) and multidrug including β-lactam antibiotics resistant bacteria.
摘要翻译：由属于链霉菌属的菌株K04-0144代表的微生物。在培养基中培养具有产生K04-0144物质的能力，并且分离出的K04-0144A物质，K04-0144B物质和K04-0144C物质对包括耐甲氧西林金黄色葡萄球菌（MRSA）在内的革兰氏阳性菌具有强的抗菌活性，因此它们可用作由MRSA引起的感染性疾病的治疗剂以及由包括β-内酰胺抗生素抗性细菌在内的多种药物引起的感染性疾病。此外，类似地，由于从培养液中分离出的新型K04-0144D物质具有提高作为抗菌剂使用的β-内酰胺抗生素的效果的作用，因此与它们组合使用时，可用作由耐甲氧西林金黄色葡萄球菌（MRSA）引起的传染病和包括β-内酰胺抗生素耐药细菌在内的多种药物。

64. 发明公开

EP1995323A1 Method for preparing C-6 phosphorylated D-aldohexoses and C-6 phosphorylated D-aldohexose derivatives 审中-公开
标题翻译： Verfahren zur Herstellung von C-6-phosphorylierten D-Aldohexosen und C-6-phosphorylierten D-Aldohexosederivaten
公开(公告)号：EP1995323A1
公开(公告)日：2008-11-26
申请号：EP07108889.2
申请日：2007-05-24
申请人： Libragen
发明人： Auriol, Daniel , Nalin, Renaud , Lefevre, Fabrice , Ginolhac, Aurélien , de Guembecker, Daphné , Zago, Caroline
IPC分类号： C12P17/00 , C12P19/02 , C12P19/26 , C12P19/28 , C07D309/10 , C07D309/14 , C07D335/02 , C07H1/02 , C07H5/10 , C07H11/04 , C07H15/04 , C07H15/12 , C07D211/40 , C07D211/54 , C07D211/56 , C07D309/08
CPC分类号： C12P19/02 , C07D211/46 , C07D211/54 , C07D309/10 , C07D309/14 , C07D335/02 , C07H11/04 , C07H15/04 , C12P17/00 , C12P19/26 , C12P19/28
摘要： The present invention concerns a method for preparing C-6 phosphorylated D-aldohexoses and C-6 phosphorylated D-aldohexose derivatives, and uses thereof. The method comprises incubating polyphosphate as sole source of phosphate donor and a polyphosphate-glucose phosphotransferase (polyphosphate: D-glucose 6-phosphotransferase, EC 2.7.1.63) in an aqueous solution with a D-aldohexose or a D-aldohexose derivative.
摘要翻译：本发明涉及一种制备C-6磷酸化D-己内酯和C-6磷酸化D-己糖衍生物的方法及其应用。该方法包括将多磷酸盐作为磷酸供体的唯一来源和在D-二氢己糖或D-己糖糖衍生物的水溶液中的多磷酸 - 葡萄糖磷酸转移酶（多磷酸：D-葡萄糖-6-磷酸转移酶，EC 2.7.1.63）。

65. 发明公开

EP1991557A1 MANNOSYL-1 PHOSPHATES, PROCEDE DE PREPARATION ET UTILISATION EN THERAPEUTIQUE, NOTAMMENT VIS-A-VIS DU SYNDROME CDG-IA 有权
标题翻译：甘露糖1-磷酸，制备方法和治疗剂的用途，特别是与CDG-IA综合征
公开(公告)号：EP1991557A1
公开(公告)日：2008-11-19
申请号：EP07731037.3
申请日：2007-02-23
申请人： OE Operations , Université René Descartes (Paris V) , Centre National de la Recherche Scientifique - CNRS
发明人： GRAVIER-PELLETIER, Christine , HARDRE, Renaud , KHALED, Amira , LE MERRER, Yves
IPC分类号： C07H11/04 , A61K31/7024
CPC分类号： C07H11/04 , A61K31/7024 , Y02P20/55
摘要： The invention concerns α-D-mannopyranosyl-1 phosphate derivatives of formulae (I), (II) and (II) as medicines, wherein each R11 to R14, R21 to R24, R31 to R34 is H or a OH-protecting group, and R and R' are such as defined in the description, useful as cellular sources of Man-1 P, against the CDG-I syndrome and in particular the CDG-Ia syndrome. The invention also concerns said derivatives as industrial products as well as their preparation method.

66. 发明公开

EP1776375A2 CERTAIN AMINOALKYL GLUCOSAMINIDE PHOSPHATE COMPOUNDS AND THEIR USE 有权转让
标题翻译：某些AMINOALKYLGLUKOSAMINIDPHOSPHATVERBINDUNGEN及其用途
公开(公告)号：EP1776375A2
公开(公告)日：2007-04-25
申请号：EP05785550.4
申请日：2005-06-24
申请人： CORIXA CORPORATION
发明人： JOHNSON, David, A. , PERSING, David, H.
IPC分类号： C07H15/04
CPC分类号： C07H5/02 , C07H11/04 , C07H13/04 , C07H15/04
摘要： Compounds that are adjuvants and immunoeffectors are described and claimed. The compounds augment antibody production in immunized animals as well as stimulate cytokine production and activate macrophages. Compositions and methods for using the compounds as adjuvants and immunoeffectors are also disclosed.

67. 发明公开

EP1676853A1 ALPHA-1-PHOSPHORYLATED-2-DEOXY-2-FLUOROARABINOSIDE AND PROCESS FOR PRODUCING 2 -DEOXY-2 -FLUORO-BETA-D-ARABINONUCLEOSID E 审中-公开
标题翻译： ALPHA-1-PHOSPHORYLIERTES-2-DESOXY-2-FLUORARABINOSID UND VERFAHREN ZUR HERSTELLUNG VON 2 -DESOXY-2 -FLUOR-BETA-D-ARABINONUKLEOSID
公开(公告)号：EP1676853A1
公开(公告)日：2006-07-05
申请号：EP04792854.4
申请日：2004-10-22
申请人： YAMASA CORPORATION
发明人： YAMADA, Kohei , MATSUMOTO, Noritake , HAYAKAWA, Hiroyuki
IPC分类号： C07H1/02 , C07H11/04 , C12P19/40
CPC分类号： C12P19/40 , C07H1/02 , C07H11/04
摘要： A method for producing 2'-deoxy-2'-fluoro-β-D-arabinonucleoside represented by formula (II):

(wherein B represents a base), in particular, 2'-deoxy-2'-fluoro-β-D-arabinopurinenucleoside, which method comprises causing a nucleoside phosphorylase to act on α-1-phosphorylated-2-deoxy-2-fluoroarabinoside represented by formula (I):

or a mixture of α- and β-isomers of 1-phosphorylated-2-deoxy-2-fluoroarabinoside represented by formula (V'):

and on a base. The compound can be produced at high yield and in a convenient and highly stereoselective manner.
摘要翻译：由式（II）表示的2'-脱氧-2'-氟-2-D-阿拉伯核苷的制备方法：其中B表示碱，特别是2'-脱氧-2'-氟-2 所述方法包括使核苷磷酸化酶作用于由式（I）表示的±-1-磷酸化-2-脱氧-2-氟阿拉伯糖苷：或1-磷酸化-2-磷酸二磷酸酯的±和2-异构体的混合物，由式（V'）表示的脱氧-2-氟阿拉伯糖苷：和在碱上。该化合物可以以高产率和方便且高度立体选择的方式制备。

68. 发明公开

EP1114827A4 NOVEL NUCLEIC ACID BASE PAIR 有权
标题翻译： NUCLEIC碱基对
公开(公告)号：EP1114827A4
公开(公告)日：2005-11-23
申请号：EP00946311
申请日：2000-07-14
申请人： JAPAN SCIENCE & TECH AGENCY
发明人： HIRAO ICHIRO , ISHIKAWA MASAHIDE , FUJIHARA TSUYOSHI , YOKOYAMA SHIGEYUKI
IPC分类号： C07H11/04 , C07H19/207 , C07H21/00 , C12N1/21 , C12N15/11 , C12P21/02 , C07H21/02 , C07H21/04 , C12N5/10 , C12N15/00 , G01N33/15 , G01N33/50
CPC分类号： C07H11/04 , C07H19/207 , C07H21/00 , C12N15/11 , C12P21/02
摘要： A novel artificial nucleic acid base pair which is obtained by forming a selective base pair by introducing a group having steric hindrance (preferably a group having steric hindrance and static repulsion and a stacking effect) and can be recognized by a polymerase such as DNA polymerase; a novel artificial gene; and a method of designing nucleic acid bases so as to form a selective base pair with the use of steric hindrance, static repulsion and stacking effect at the base moiety of the nucleic acid. An artificial nucleic acid comprising these bases; a process for producing the same; a codon containing the same; a nucleic acid molecule containing the same; a process for producing a non-natural gene by using the same; a process for producing a novel protein by using the above nucleic acid molecule or non-natural gene, and the like.

69. 发明公开

EP1589934A2 CERTAIN AMINOALKYL GLUCOSAMINIDE PHOSPHATE COMPOUNDS AND THEIR USE 有权
标题翻译：某些氨基葡萄糖苷磷酸盐化合物及其用途
公开(公告)号：EP1589934A2
公开(公告)日：2005-11-02
申请号：EP04700403.1
申请日：2004-01-06
申请人： CORIXA CORPORATION
发明人： JOHNSON, David, A.
IPC分类号： A61K7/00
CPC分类号： C07H13/04 , C07H5/02 , C07H11/04 , C07H15/04
摘要： Compounds that are adjuvants and immunoeffectors are described and claimed. The compounds augment antibody production in immunized animals as well as stimulate cytokine production and activate macrophages. Compositions and methods for using the compounds as adjuvants and immunoeffectors are also disclosed.

70. 发明公开

EP1301522A4 NOVEL COMPOUNDS AND METHODS 审中-公开
标题翻译：新化合物和方法
公开(公告)号：EP1301522A4
公开(公告)日：2004-04-14
申请号：EP01949109
申请日：2001-07-11
申请人： PHARMAXIS PTY LTD
发明人： COWDEN WILLIAM BUTLER , ESCHLER BART MICHAEL , MARCH DARREN RAY , FRANCIS DOUGLAS JOHN , GERBA SENDABA , BARTELL GAVIN JAMES , CHARLTON BRETT
IPC分类号： C07H11/04 , A61K31/7024 , A61P1/00 , A61P3/10 , A61P5/14 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P27/02 , A61P29/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07F9/655 , C07F9/6558 , A61K31/665 , A61K31/70
CPC分类号： C07H11/04 , C07F9/6552 , C07F9/65586
摘要： The present invention provides phosphotetrahydropyran compounds and the use thereof in treating diseases or conditions that are dependent on T-lymphocyte migration, as well as compositions containing said compounds.

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