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91. 发明申请

WO2005058876A1 PYRAZINE DERIVATIVES AS EFFECTIVE COMPOUNDS AGAINST INFECTIOUS DISEASES 审中-公开
标题翻译：吡哆醛衍生物作为有效的化合物对抗感染性疾病
公开(公告)号：WO2005058876A1
公开(公告)日：2005-06-30
申请号：PCT/EP2004/014371
申请日：2004-12-16
申请人： AXXIMA PHARMACEUTICALS AG , EIKHOFF, Jan, Eike , ASHTON, Mark, Richard , COURTNEY, Stephen, Martin , YARNOLD, Christopher, John , VARRONE, Maurizio , LOKE, Pui, Leng , HERGET, Thomas , SCHWAB, Wilfried , HAFENBRADL, Doris
发明人： EIKHOFF, Jan, Eike , ASHTON, Mark, Richard , COURTNEY, Stephen, Martin , YARNOLD, Christopher, John , VARRONE, Maurizio , LOKE, Pui, Leng , HERGET, Thomas , SCHWAB, Wilfried , HAFENBRADL, Doris
IPC分类号： C07D403/12
CPC分类号： C07D401/04 , C07D241/20 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D409/14
摘要： The present invention relates to pyrazine derivatives according to the general formula (I) and pharmaceutically acceptable salts thereof and their use as pharmaceutical compounds as well as the use of these compounds for the preparation of a pharmaceutical composition for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases, stroke and especially for the treatment of herpesviral induced infections, including opportunistic infections as well as infections and diseases caused by human cytomegalovirus (HCMV).
摘要翻译：本发明涉及根据通式（I）的吡嗪衍生物及其药学上可接受的盐及其作为药物化合物的用途，以及这些化合物在制备用于预防和/或治疗感染性疾病的药物组合物中的用途疾病，包括机会性疾病，朊病毒疾病，免疫疾病，自身免疫性疾病，双相和临床疾病，心血管疾病，细胞增殖性疾病，糖尿病，炎症，移植排斥，勃起功能障碍，神经变性疾病，中风，特别是治疗疱疹病毒诱导的感染，包括机会性感染以及由巨细胞病毒（HCMV）引起的感染和疾病。

92. 发明申请

WO2004056752A1 PRODUCTION PROCESS OF GAMMA-CYHALOTHRIN 审中-公开
标题翻译： γ-氨基丁酸的生产工艺
公开(公告)号：WO2004056752A1
公开(公告)日：2004-07-08
申请号：PCT/GB2003/005450
申请日：2003-12-09
申请人： SYNGENTA LIMITED , BROWN, Stephen, Martin , GOTT, Brian, David
发明人： BROWN, Stephen, Martin , GOTT, Brian, David
IPC分类号： C07C253/08
CPC分类号： C07C253/30 , C07B2200/07 , C07B2200/09 , C07C253/34 , C07C255/39 , C07C2601/02
摘要： A process for the preparation of gamma-cyahlothrin comprising a) chlorinating 1R cis -Z 3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethyl cyclopropanecarboxylic acid to give 1R cis -Z 3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethyl cyclopropanecarboxylic acid chloride; b) esterifying 1R cis -Z 3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethyl cyclopropanecarboxylic acid chloride with 3-phenoxy benzaldehyde in the presence of a source of cyanide to form a diastereoisomeric mixture of cyhalothrin isomers and c) epimerising the diastereoisomeric mixture under conditions in which the least soluble diastereoisomer crystallises from solution.
摘要翻译：一种制备γ-氰基丙烯腈的方法，包括a）将1R顺式-Z-（2-氯-3,3,3-三氟-1-丙烯基）-2,2-二甲基环丙烷甲酸氯化，得到1R顺式-Z 3-（2-氯-3,3,3-三氟-1-丙烯基）-2,2-二甲基环丙烷甲酰氯; b）在氰化源存在下，用3-苯氧基苯甲醛酯化1R顺式-Z-（2-氯-3,3,3-三氟-1-丙烯基）-2,2-二甲基环丙烷甲酰氯以形成三氟氯氰菊酯异构体的非对映异构体混合物和c）在溶液中结晶最不溶性非对映异构体的条件下使非对映异构体混合物差向异构化。

93. 发明申请

WO2004013132A1 FURANTHIAZOLE DERIVATIVES AS HEPARANASE INHIBITORS 审中-公开
标题翻译：呋喃丹唑衍生物作为HEPARANASE抑制剂
公开(公告)号：WO2004013132A1
公开(公告)日：2004-02-12
申请号：PCT/GB2003/003409
申请日：2003-08-05
申请人： OXFORD GLYCOSCIENCES (UK) LTD , COURTNEY, Stephen, Martin , HAY, Philip, Andrew , SCOPES, David, Ian, Carter
发明人： COURTNEY, Stephen, Martin , HAY, Philip, Andrew , SCOPES, David, Ian, Carter
IPC分类号： C07D417/04
CPC分类号： C07D417/04 , C07D417/14
摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof: (I) wherein the groups Q, R 2 , R 3 , R 4 and R 5 represent various substituent groups, and their use as inhibitors of heparanase.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐或前药：（I）其中基团Q，R 2，R 3，R 4和R 5表示各种取代基，以及它们作为肝素酶抑制剂的用途。

94. 发明申请

WO2003074516A1 PHTHALIMIDE CARBOXYLIC ACID DERIVATIVES 审中-公开
标题翻译：邻苯二甲酸羧酸衍生物
公开(公告)号：WO2003074516A1
公开(公告)日：2003-09-12
申请号：PCT/GB2003/000926
申请日：2003-03-06
申请人： OXFORD GLYCOSCIENCES (UK) LTD , SCOPES, David, Ian, Carter , COURTNEY, Stephen, Martin , HAY, Philip, Andrew
发明人： COURTNEY, Stephen, Martin , HAY, Philip, Andrew
IPC分类号： C07D413/10
CPC分类号： C07D413/10 , C07D413/14
摘要： The present invention relates to phthalimide carboxylic acid derivatives of formula (I), methods for their preparation, pharmaceutical compositions containing them and their use in medicine, specifically in the treatment of cancer. (I), wherein X is O or S; R 1 is a phthalimide carboxylic acid group of formula (II). R is hydrogen, C 1 -C 6 alkyl, aryl or C 1 -C 3 alkylaryl and R 2 , R 3 and R 4 represent various substituents.
摘要翻译：本发明涉及式I的邻苯二甲酰亚胺羧酸衍生物，其制备方法，含有它们的药物组合物及其在医药中的用途，特别涉及治疗癌症。 I，其中X是O或S 1是式II的邻苯二甲酰亚胺羧酸基团。 R是氢，C1-C6烷基，芳基或C1-C3烷基芳基，R2，R3和R4代表各种取代基。

95. 发明申请

WO9943981A3 A LIGHTING SYSTEM 审中-公开
标题翻译：照明系统
公开(公告)号：WO9943981A3
公开(公告)日：1999-10-14
申请号：PCT/IE9900011
申请日：1999-02-25
申请人： CARR STEPHEN MARTIN
发明人： CARR STEPHEN MARTIN
IPC分类号： F21S8/00 , F21V23/06 , F21V33/00 , G09F3/02 , G09F7/18 , G09F13/02 , F21S1/02
CPC分类号： G09F7/18 , F21S8/033 , F21S8/06 , F21V23/06 , F21V33/0032 , F21W2131/304 , G09F13/02 , G09F2007/186
摘要： A lighting unit (1) comprising display means (20) for displaying graphic material (11), lighting means (13) for frontal illumination of the graphic material (11), mounting means (19) for supporting the display means (20) and suspending means (4) for suspending the lighting system (1) above the ground, the display means (20), the lighting means (13), the mounting means (19) and the suspending means (4) comprising an integral lighting and display unit.
摘要翻译：一种照明单元（1），包括用于显示图形材料（11）的显示装置（20），用于正面照明图形材料（11）的照明装置（13），用于支撑显示装置（20）的安装装置（19）用于将照明系统（1）悬挂在地面上的悬挂装置（4），显示装置（20），照明装置（13），安装装置（19）和悬挂装置（4）包括整体照明和显示器单元。

96. 发明申请

WO1998019978A1 NITRATION PROCESS 审中-公开
标题翻译：硝化过程
公开(公告)号：WO1998019978A1
公开(公告)日：1998-05-14
申请号：PCT/GB1997002952
申请日：1997-10-28
申请人： ZENECA LIMITED , BROWN, Stephen, Martin , MUXWORTHY, James, Peter , LENNON, Martin , ATHERTON, John, Heathcote , PREISTLEY, Ian, Jeffrey, Grassham
发明人： ZENECA LIMITED
IPC分类号： C07B43/02
CPC分类号： C07C303/40 , C07B43/02 , C07C201/08 , C07C311/51 , C07C205/59
摘要： A process for the nitration of an aromatic or heteroaromatic compound with a nitrating agent comprising nitric acid or a mixture of nitric and sulphuric acids, characterised in that nitration is performed in a solvent comprising at least 50 % v/v of a C1-C6 alkyl ester of a C1-C4 carboxylic acid. The process is of particular use for the nitration of diphenyl ethers to give compounds which are useful as herbicides or as intermediates in the synthesis of herbicides.
摘要翻译：一种用包含硝酸或硝酸和硫酸的混合物的硝化剂硝化芳族或杂芳族化合物的方法，其特征在于，在包含至少50％v / v的C 1 -C 6烷基的溶剂中进行硝化酯的C 1 -C 4羧酸。该方法特别用于二苯醚的硝化，得到可用作除草剂的化合物或作为除草剂合成中的中间体。

97. 发明申请

WO1997010199A1 PROCESS FOR NITRATING DIPHENYL ETHER COMPOUNDS 审中-公开
标题翻译：硝基二苯醚化合物的方法
公开(公告)号：WO1997010199A1
公开(公告)日：1997-03-20
申请号：PCT/GB1996001892
申请日：1996-08-06
申请人： ZENECA LIMITED , BROWN, Stephen, Martin , MUXWORTHY, James, Peter
发明人： ZENECA LIMITED
IPC分类号： C07C201/08
CPC分类号： C07C201/08 , C07C303/40 , C07C311/51 , C07C205/59
摘要： A process for the preparation of a compound of general formula (I) wherein R is hydrogen or C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl (any of which may optionally be substituted with one or more substituents selected from halogen and OH) or COOH, COH, COOR , COR , CONR R or CONHSO2R ; R and R are each independently hydrogen or C1-C4 alkyl optionally substituted with one or more halogen atoms; R is a halogen atom or a group R ; R is hydrogen or halo; R is C1-C4 alkyl, C2-C4 alkenyl or C2-C4 alkynyl, any of which may optionally be substituted with one or more halogen atoms, or halo; the process comprising reacting a compound of general formula (II) wherein R , R and R are as defined for general formula (I); with a nitrating agent comprising nitric acid or a mixture of nitric and sulphuric acids in the presence of an organic solvent and in the presence of acetic anhydride, characterised in that the molar ratio of acetic anhydride to compound of general formula (I) is from about 1:1 to 3:1.
摘要翻译：制备通式（I）的化合物的方法，其中R 1是氢或C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基（其中任何一个可以任选地被一个或多个取代基所取代 COOH，COH，COOR 4，COR 6，CONR 4 R 5或CONHSO 2 R 4; R 4和R 5各自独立地为氢或任选被一个或多个卤素原子取代的C 1 -C 4烷基; R 6是卤素原子或基团R 4; R 2是氢或卤素; R 3是C 1 -C 4烷基，C 2 -C 4烯基或C 2 -C 4炔基，其中任何一个可以任选地被一个或多个卤素原子或卤素取代; 该方法包括使通式（II）的化合物，其中R 1，R 2和R 3如通式（I）所定义; 在硝酸和硝酸和硫酸的混合物的存在下，在有机溶剂存在下和在乙酸酐存在下，硝酸化剂，其特征在于乙酸酐与通式（I）化合物的摩尔比为约 1：1到3：1。

98. 发明申请

WO1997010192A1 1,1-DIFLUORO-1,4-DICHLOROBUTANE AND PROCESS FOR ITS PREPARATION 审中-公开
标题翻译： 1,1-DIFLUORO-1,4-DICHLOROBUTANE及其制备方法
公开(公告)号：WO1997010192A1
公开(公告)日：1997-03-20
申请号：PCT/GB1996001857
申请日：1996-07-30
申请人： ZENECA LIMITED , WILLIAMS, Alfred, Glyn , BOWDEN, Martin, Charles , BROWN, Stephen, Martin
发明人： ZENECA LIMITED
IPC分类号： C07C19/10
CPC分类号： C07C19/10 , C07C17/206
摘要： The present invention provides the novel chlorofluorohydrocarbon 1,1-difluoro-1,4-dichlorobutane, and a process for its preparation by reacting 1,1,1,4-tetrachlorobutane with hydrogen fluoride in the liquid phase. The product has useful solvent properties and is also useful in synthetic chemistry for the introduction of fluorocarbon functionality.
摘要翻译：本发明提供了新的氯氟烃1,1-二氟-1,4-二氯丁烷，以及通过1,1,1,4-四氯丁烷与氟化氢在液相中反应制备的方法。该产品具有有用的溶剂性质，并且在合成化学中也可用于引入碳氟化合物功能。

99. 发明申请

WO1996022958A1 PROCESS FOR THE PRODUCTION OF 2-(SUBSTITUTED BENZOYL)1,3 CYCLOHEXANEDIONES 审中-公开
标题翻译： 2-（取代苯甲酰基）1,3环己基磺酸的制备方法
公开(公告)号：WO1996022958A1
公开(公告)日：1996-08-01
申请号：PCT/GB1996000082
申请日：1996-01-16
申请人： ZENECA LIMITED , BROWN, Stephen, Martin , RAWLINSON, Howard
发明人： ZENECA LIMITED
IPC分类号： C07C45/54
CPC分类号： C07C45/54 , C07C315/04 , C07C317/24 , C07C49/792
摘要： A process for preparing a compound of formula (I), where R , R , R , R , R and R are independently hydrogen or C1-6 alkyl; R is halogen, cyano, NO2, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy or RaS in which Ra is C1-4 alkyl; R , R and R independently are hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, C1-4 haloalkoxy, CN, NO2, phenoxy or substituted phenoxy; RbS(O)n Om in which m is 0 or 1, n is 0, 1 or 2 and Rb is C1-4 alkyl, C1-4 haloalkyl, phenyl or benzyl, NHCORc in which Rc is C1-4 alkyl, NRdRe in which Rd and Re indenpendently are hydrogen or C1-4 alkyl; RfC(O)- in which Rf is hydrogen, C1-4 alkyl, C1-4 haloalkyl or C1-4 alkoxy; SO2NRgRh in which Rg and Rh independently are hydrogen or C1-4 alkyl; or any two of R , R and R together with the carbon atoms to which they are attached form a 5 or 6 membered heterocyclic ring containing up to three heteroatoms selected from O, N or S and which may be optionally substituted by =NOC1-4 alkyl, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy or halogen; which process comprises the rearrangement of a compound of formula (II) where R , R , R , R , R , R , R , R , R and R are as defined in relation to formula (I), in a non-polar solvent in the presence of a cyanide source, an alkali or alkaline earth metal carbonate, a phase transfer catalyst and 1-6 moles of water with respect to the compound of formula (II).
摘要翻译：制备式（I）化合物的方法，其中R 1，R 2，R 3，R 4，R 5和R 6独立地是氢或C 1-6烷基 ; R 7是卤素，氰基，NO 2，C 1-4烷基，C 1-4卤代烷基，C 1-4烷氧基或R a，其中R a是C 1-4烷基; R 8，R 9和R 10独立地是氢，卤素，C 1-4烷基，C 1-4烷氧基，C 1-4卤代烷基，C 1-4卤代烷氧基，CN，NO 2，苯氧基或取代的苯氧基; RbS（O）n Om，其中m为0或1，n为0,1或2，Rb为C1-4烷基，C1-4卤代烷基，苯基或苄基，NHCORc，其中Rc为C1-4烷基，NRdRe为哪个Rd和Re独立地是氢或C 1-4烷基; RfC（O） - ，其中R f为氢，C 1-4烷基，C 1-4卤代烷基或C 1-4烷氧基; 其中Rg和Rh独立地为氢或C1-4烷基的SO2NRgRh; 或R 8，R 9和R 10中的任何两个与它们所连接的碳原子一起形成含有至多三个选自O，N或S的杂原子的5或6元杂环，其中可以任选被= NOC 1-4烷基，C 1-4烷基，C 1-4卤代烷基，C 1-4烷氧基或卤素取代; 该方法包括式（II）化合物的重排，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 7，在非极性溶剂中，在氰化物源，碱金属或碱土金属碳酸盐，相转移催化剂存在下，R 9和R 10如关于式（I）所定义）和1-6摩尔水相对于式（II）化合物。

100. 发明申请

WO1996016018A1 PREPARATION OF CYCLOPROPANE ESTERS 审中-公开
标题翻译：环孢菌素的制备
公开(公告)号：WO1996016018A1
公开(公告)日：1996-05-30
申请号：PCT/GB1995002570
申请日：1995-11-02
申请人： ZENECA LIMITED , BOWDEN, Martin, Charles , BROWN, Stephen, Martin
发明人： ZENECA LIMITED
IPC分类号： C07C69/743
CPC分类号： C07C69/743
摘要： The invention provides an improved process for the preparation of a lower alkyl ester of 3-(2-chloro-3,3,3-trifluoroprop-1-en-1-yl)-2,2-dimethylcyclopropane carboxylic acid in which the corresponding lower alkyl ester of a carboxylic acid selected from 6-bromo-6-chloro-3,3-dimethyl-7,7,7-trifluorohept-2-enoic acid and 6,6-dichloro-3,3-dimethyl-7,7,7-trifluorohept-2-enoic acid is treated with an alkali metal lower alkoxylate in the presence of an aromatic hydrocarbon solvent under conditions under which the lower alcohol of the alkoxylate is removed from the reaction mixture by distillation with the aromatic solvent. The products are useful as intermediates in the manufacture of pyrethroid insecticides.
摘要翻译：本发明提供了制备3-（2-氯-3,3,3-三氟丙-1-烯-1-基）-2,2-二甲基环丙烷羧酸的低级烷基酯的改进方法，其中相应的选自6-溴-6-氯-3,3-二甲基-7,7,7-三氟庚-2-烯酸和6,6-二氯-3,3-二甲基-7,7-二羧酸的羧酸的低级烷基酯， 7,7-三氟庚-2-烯酸在芳族烃溶剂存在下用碱金属低级烷氧基化物处理，在烷基化物的低级醇通过芳族溶剂蒸馏除去反应混合物的条件下进行处理。该产品可用作制造拟除虫菊酯杀虫剂的中间体。

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