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1. 发明申请

WO1996028420A2 PREPARATION OF N-ARYLMETHYL AZIRIDINE DERIVATIVES, 1,4,7,10-TETRAAZACYCLODODECANE DERIVATIVES OBTAINED THEREFROM AND N-ARYLMETHYL-ETHANOL-AMINE SULPHONATE ESTERS AS INTERMEDIATES 审中-公开
标题翻译： N-芳基甲基咪唑衍生物的制备，其中获得的1,4,7,10-四氮杂环十二烷基衍生物和作为中间体的N-亚磺酰基 - 乙磺酰胺磺酸盐
公开(公告)号：WO1996028420A2
公开(公告)日：1996-09-19
申请号：PCT/GB1996000552
申请日：1996-03-08
申请人： NYCOMED SALUTAR, INC. , UNIVERSITY OF IOWA RESEARCH FOUNDATION , COCKBAIN, Julian , MESSERLE, Louis , AMARASINGHE, Gandara , FELLMANN, Jere, Douglas , GARRITY, Martha , VARADARAJAN, John , VASILEVSKIS, Janis
发明人： NYCOMED SALUTAR, INC. , UNIVERSITY OF IOWA RESEARCH FOUNDATION , COCKBAIN, Julian
IPC分类号： C07D203/08
CPC分类号： C07D203/08 , A61K49/0002 , A61K49/06 , C07C303/44 , C07D255/00 , C07D257/02 , C07D259/00 , C07C305/06
摘要： Aziridines may be subjected to a cyclooligomerization reaction to produce polyazacycloalkane compounds useful for example in the preparation of chelating agents for use in diagnostic imaging contrast agents. N-benzyl-aziridine in particular is useful as it can be cyclotetramerized and debenzylated to yield cyclen, a key intermediate in chelating agent preparation. The invention provides a particularly attractive route to production of N-benzyl and other N-arylmethyl aziridines of formula (I), (where each R1 independently is hydrogen or a group Ar and Ar is an optionally substituted phenyl group), said process comprising reacting a purified N-arylmethylethanolamine-sulphonate ester with a base. N-arylmethyl-ethanolamine sulphonate ester of the formula: R'NHCH2CH2OSO3H, wherein the N-arylmethyl group R' is an N-(bisarylmethyl) or N-(triarylmethyl) group, as intermediates. In a further aspect the invention provides compounds of formula (II), where Ar and R1 are as hereinbefore defined and at least two differing ArCHR1 moieties are present.
摘要翻译：氮丙啶可以进行环烯基化反应以产生用于例如制备用于诊断成像造影剂的螯合剂的多氮杂环烷烃化合物。特别是N-苄基 - 氮丙啶是有用的，因为它可以进行环化聚合和脱苄基化，以产生螯合剂，螯合剂制备中的关键中间体。本发明提供了生产式（I）的N-苄基和其它N-芳基甲基氮丙啶的特别有吸引力的途径（其中每个R 1独立地为氢或基团Ar，Ar为任选取代的苯基），所述方法包括使纯化的N-芳基甲基乙醇胺 - 磺酸酯与碱。具有下式的N-芳基甲基 - 乙醇胺磺酸酯：R'NHCH2CH2OSO3H，其中N-芳基甲基R'为N-（二芳基甲基）或N-（三芳基甲基）基团，为中间体。在另一方面，本发明提供式（II）化合物，其中Ar和R 1如上所定义，并且存在至少两个不同的ArCHR 1部分。

2. 发明申请

WO1995028967A1 CONTRAST AGENTS 审中-公开
标题翻译：对比剂
公开(公告)号：WO1995028967A1
公开(公告)日：1995-11-02
申请号：PCT/GB1995000899
申请日：1995-04-20
申请人： NYCOMED IMAGING AS , COCKBAIN, Julian , MARGERUM, Larry , CAMPION, Brian , FELLMANN, Jere, Douglas , GARRITY, Martha , VARADARAJAN, John
发明人： NYCOMED IMAGING AS , COCKBAIN, Julian
IPC分类号： A61K49/00
CPC分类号： A61K49/124 , A61K47/60 , A61K49/085 , A61K49/106 , A61K49/1812 , A61K51/065 , A61K2121/00 , A61K2123/00 , C08G79/00
摘要： The invention provides a blood pool contrast agent having an overall molecular weight of at least 10KD comprising a macrostructure which has bound thereto a plurality of opsonization inhibiting moieties and carries chelated ionic paramagnetic or heavy metal moieties, the chelant groups for said chelated moieties being macrocyclic where said macrostructure is liposomal.
摘要翻译：本发明提供了总体分子量至少为10KD的血液池造影剂，其包含宏观结构，其结合有多个调理作用抑制部分并携带螯合的离子顺磁性或重金属部分，所述螯合部分的螯合剂基团是大环的，其中所述宏观结构是脂质体。

3. 发明申请

WO1995007270A1 CHELANTS AS CONTRAST ENHANCING AGENTS 审中-公开
标题翻译：作为对比增强剂的CHELANTS
公开(公告)号：WO1995007270A1
公开(公告)日：1995-03-16
申请号：PCT/GB1994001931
申请日：1994-09-06
申请人： NYCOMED SALUTAR, INC. , COCKBAIN, Julian , GARRITY, Martha , CROFTS, Shaun, Paul , CARVALHO, Joan , STRANDE, Per , DUGSTAD, Harald
发明人： NYCOMED SALUTAR, INC. , COCKBAIN, Julian
IPC分类号： C07D257/02
CPC分类号： A61K49/0002 , C07D257/02 , Y10S514/836
摘要： The present invention provides a polychelant compound of formula (VII), (wherein each X which may be the same or different is NZ, O or S, at least two Xs being NZ; B is (CR Y) or -N(CR 2Y)-; each Z is a group R or a group CR 2Y, at least one Z being a group CR 2Y; each Y is a group CO2H, PO3H, SO3H, CONR 2, CON(OR )R , CNS or CONR NR 2; m is 0 or 1 or 2; each n is 2 or 3; q is 0 or 1 when B is (CR Y) and 2 when B is N(CR 2Y); p is an integer having a value of at least 2; each R which may be the same or different is a hydrogen atom or an alkyl, aryl or aralkyl group optionally substituted by one or more hydroxy or alkoxy groups, or two R groups on ring atoms or in Z groups together represent a linker group L; each L which may be the same or different represents a bond or an organic linker group having a molecular weight of less than 1000 and salts and chelates thereof. These compounds, especially the di- and trichelates with paramagnetic or heavy metal ions are especially useful as diagnostic imaging contrast agents.
摘要翻译：本发明提供一种式（Ⅶ）的聚合物化合物，其中每个X可以相同或不同，为NZ，O或S，至少两个X为NZ; B为（CR 1 Y）或-N （CR 1 2Y） - ;每个Z是基团R 1或基团CR 1Y 2，至少一个Z是基团CR 2Y;每个Y是基团CO 2 H，PO 3 H，SO 3 H ，CONR 1，CON（OR 1）R 1，CNS或CONR 1 NR 12，m为0或1或2;每个n为2或3; q为0或 1，当B为（CR 1）Y）时为2，B为N时为2（CR 1 2Y）; p为值至少为2的整数;每个R 1可以相同或不同任选被一个或多个羟基或烷氧基取代的烷基，芳基或芳烷基或环原子上或Z基团中的两个R 1一起表示连接基团L;每个L可以相同或不同的表示分子量小于1000的键或有机连接基团及其盐和螯合物，这些化合物，特别是具有顺磁或重金属离子的二 - 和三 - s作为诊断成像造影剂是特别有用的。

4. 发明申请

WO1996028432A1 PROCESS FOR TETRAAZACYCLOALKANE PREPARATION 审中-公开
标题翻译：四氯化碳制剂的制备方法
公开(公告)号：WO1996028432A1
公开(公告)日：1996-09-19
申请号：PCT/GB1996000462
申请日：1996-03-01
申请人： NYCOMED IMAGING A/S , COCKBAIN, Julian , SANDNES, Rolf, Wiggo , VASILEVSKIS, Janis , UNDHEIM, Kjell , GACEK, Michel
发明人： NYCOMED IMAGING A/S , COCKBAIN, Julian
IPC分类号： C07D257/02
CPC分类号： C07D257/02
摘要： The present invention provides a synthetic route for tetraazacycloalkane preparation which facilitates heteropoly-N-alkylation of the macrocyclic product, and is thereby beneficial for the production of chelating agents and chelates useful in diagnostic imaging. The process involves (i) reacting a tetraazaalkane with a bridging agent to couple for amine nitrogens of said tetraazaalkane to a bridging moiety to yield a fused tricyclic intermediate, (ii) reacting said intermediate to introduce an alkylene bridge between the secondary amine nitrogens in the outer rings of the fused tricyclic intermediate, optionally be decoupling an alkanediylidene bridging moiety from the tertiary amine nitrogens at the ring fusion sites of the fused tricyclic intermediate, and (iii) where necessary, decoupling said bridging moiety to yield a macrocyclic tetraazacycloalkane.
摘要翻译：本发明提供了促进大环杂多杂-N-烷基化的四氮杂环烷烃制备的合成路线，从而有利于制备可用于诊断成像的螯合剂和螯合物。该方法包括（i）使四氮杂链烷烃与桥连剂反应以将所述四氮杂烷的胺氮偶联至桥连部分以产生稠合的三环中间体，（ii）使所述中间体在仲胺氮中引入亚烷基桥，稠合三环中间体的外环任选地在稠合三环中间体的环融合位点处将烷二亚烷基桥连部分与叔胺氮键分离，和（iii）必要时将所述桥连部分解偶联以产生大环四氮杂环烷烃。

5. 发明申请

WO1995028966A1 DENDRIMERIC COMPOUNDS 审中-公开
标题翻译： DENDRIMERIC化合物
公开(公告)号：WO1995028966A1
公开(公告)日：1995-11-02
申请号：PCT/GB1995000898
申请日：1995-04-20
申请人： NYCOMED IMAGING AS , COCKBAIN, Julian , MARGERUM, Larry , CAMPION, Brian , FELLMAN, Jere, Douglas , GARRITY, Martha
发明人： NYCOMED IMAGING AS , COCKBAIN, Julian
IPC分类号： A61K49/00
CPC分类号： A61K49/124 , A61K47/60 , A61K49/085 , A61K51/065 , A61K2121/00 , A61K2123/00 , C08G79/00 , Y10S424/16
摘要： The invention provides a dendrimeric compound comprising a dendrimeric backbone moiety with linked thereto a plurality of diagnostically or therapeutically active moieties, characterised in that the molecular skeleton of said compound contains at least one biodegradable cleavage site such that on cleavage thereof said active moieties are released in renally excretable form.
摘要翻译：本发明提供了包含树枝状大分子主链部分的树枝状化合物，其连接有多个诊断或治疗活性部分，其特征在于所述化合物的分子骨架含有至少一个可生物降解的切割位点，使得在其切割时，所述活性部分被释放在肾脏排泄的形式。

6. 发明申请

WO1995028392A1 CHELANT COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO1995028392A1
公开(公告)日：1995-10-26
申请号：PCT/GB1995000833
申请日：1995-04-12
申请人： NYCOMED IMAGING A/S , COCKBAIN, Julian , VARADARAJAN, John , WATSON, Alan, David , BERG, Arne
发明人： NYCOMED IMAGING A/S , COCKBAIN, Julian
IPC分类号： C07D257/02
CPC分类号： A61K49/06 , C07C237/08 , C07D255/02 , C07D257/02 , C07D259/00 , C07D273/00
摘要： The invention provides amphiphilic compounds of the formula (I) Ch-(-L-Ar-(-AH)n)m (where Ch is a hydrophilic chelant moiety or a salt or a chelate thereof); each L is an optionally oxo substituted C2-25-alkylene linker wherein at least one CH2 moiety is replaced by a group X (e.g. L may include a chain sequence, an X (CH2CH2X )u (where u is a positive integer) such as X CH2CH2X , CH2X CH2CH2X CH2CH2X , CH2X CH2CH2X CH2CH2X CH2CH2X , etc.), and wherein L is optionally interrupted by a metabolizable group M but with the provisos that the terminus of L adjacent Ch is CH2 and that the terminus of L adjacent Ar is X or a CH2 group adjacent or separated by one CH2 from a group X (thus, for example the L-Ar linkage may be L -X -Ar, L -CH2-Ar, L -X CH2-Ar or L -X CH2CH2-Ar, where L is the residue of L; each Ar is an aryl ring optionally substituted by or having fused thereto a further aryl ring; each AH is a protic acid group, preferably an oxyacid, e.g. a carbon, sulphur or phosphorus oxyacid or a salt thereof; each X is O, S, NR or PR , preferably no more than 3 X groups being present in L; each R is hydrogen, alkyl or aryl; and m and n are positive integers, m being for example 1 to 4, especially 1 or 2 and n being for example 1, 2 or 3) which are especially suited for use in diagnostic imaging of the hepatobiliary system.
摘要翻译：本发明提供式（I）Ch - （ - L-Ar - （ - AH）n）m（其中Ch是亲水性螯合剂部分或其盐或螯合物）的两亲化合物; 每个L是任选氧代取代的C2-25-亚烷基接头，其中至少一个CH 2部分被基团X 1取代（例如L可以包括链序列，X 1（CH 2 CH 2 X 1）u（其中u是正整数），例如X 1 CH 2 CH 2 X 1，CH 2 X 1 CH 2 CH 2 X 1 CH 2 CH 2 X 1，CH 2 X 1 CH 2 CH 2 X 1 CH 2 CH 2 X 1 CH 2 CH 2 X 1等），并且其中L任选地被可代谢基团M中断，但条件是邻近Ch的L的末端是CH 2，并且L相邻的Ar的末端是X 1或与一个CH 2相邻或分隔的CH2基团基团X 1（因此，例如L-Ar键可以是L 1 -X 1 -Ar，L 1 -CH 2 -Ar，L 1 -X 1 CH 2 - Ar或L 1 -X 1 CH 2 CH 2 -Ar，其中L 1是L的残基;每个Ar是任选被另外的芳基环取代或与其稠合的芳基;每个AH是质子酸基团，优选含氧酸，例如碳，硫或磷的含氧酸或其盐;每个X 1为O，S，NR 1或PR 1，优选不超过3个X 1为存在于升; 每个R 1是氢，烷基或芳基; m和n为正整数，m为例如1至4，特别是1或2，n为例如1,2或3），其特别适用于肝胆系统的诊断成像。

7. 发明申请

WO2010018387A3 PROCESS FOR THE PRODUCTION OF ALCOHOL 审中-公开
公开(公告)号：WO2010018387A3
公开(公告)日：2010-02-18
申请号：PCT/GB2009/002000
申请日：2009-08-14
申请人： STATOILHYDRO ASA , KOTLAR, Hans, Kristian , NYGÅRD, Per , THRONE-HOLST, Mimmi , COCKBAIN, Julian
发明人： KOTLAR, Hans, Kristian , NYGÅRD, Per , THRONE-HOLST, Mimmi , COCKBAIN, Julian
IPC分类号： C12P7/06 , C12P7/10 , C12P7/16 , C12N1/20
摘要： The invention provides a process for the production of an alcohol which comprises cleaving polysaccharides in a cellulosic material in an aqueous medium at a temperature of at least 45°C using a thermophilic microorganism to yield fermentable sugars, fermenting an aqueous solution of said sugars at a temperature of at least 45°C with a thermophilic microorganism to yield an alcohol or an alkanoate, if necessary reducing said alkanoate to yield an alcohol, and removing said alcohol from said aqueous solution.

8. 发明申请

WO2008035101A3 DISINFECTANT EMULSIONS CONTAINING AN ANTIMICROBIAL COMPOUND IN EACH PHASE 审中-公开
公开(公告)号：WO2008035101A3
公开(公告)日：2008-03-27
申请号：PCT/GB2007/003606
申请日：2007-09-21
申请人： MAINSANI AS , COCKBAIN, Julian , KILAAS, Lars , AASEN, Inga , DYRLI, Anne , JOHNSEN, Heidi , KLAVENESS, Jo , MEHREN, Petter
发明人： COCKBAIN, Julian , KILAAS, Lars , AASEN, Inga , DYRLI, Anne , JOHNSEN, Heidi , KLAVENESS, Jo , MEHREN, Petter
IPC分类号： A01N25/04 , A01N43/40 , A01N33/12 , A01N31/08 , A01N49/00 , A01N47/44 , A01N31/16 , A01N31/02 , A01N31/12 , A01P1/00
摘要： The invention provides a disinfectant emulsion composition having a continuous phase having dissolved therein a first antimicrobial agent and a discontinuous phase having dissolved therein a second antimicrobial agent.

9. 发明申请

WO2003097910A3 PROCESS FOR PROCESSING CARBON MATERIAL 审中-公开
公开(公告)号：WO2003097910A3
公开(公告)日：2003-11-27
申请号：PCT/GB2003/002221
申请日：2003-05-22
申请人： STATOIL ASA , COCKBAIN, Julian , EDWIN, Emil , RUSTEN, Bernt, Henning , ARNESEN, Tore
发明人： COCKBAIN, Julian , EDWIN, Emil , RUSTEN, Bernt, Henning , ARNESEN, Tore
IPC分类号： D01F9/127
摘要： This invention relates to a process for the preparation of fibrous carbon which comprises contacting a metallic catalyst with a carbon-containing gas at elevated temperature, characterized in that said catalyst is a porous metal comprising a transition metal or an alloy thereof.

10. 发明申请

WO1998018496A3 CONTRAST AGENTS 审中-公开
公开(公告)号：WO1998018496A3
公开(公告)日：1998-05-07
申请号：PCT/GB1997002956
申请日：1997-10-28
申请人： NYCOMED IMAGING AS , COCKBAIN, Julian , KLAVENESS, Jo , NAEVESTAD, Anne , CUTHBERTSON, Alan
发明人： NYCOMED IMAGING AS , COCKBAIN, Julian
IPC分类号： A61K49/00

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