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1. 发明申请

WO2005123755A2 PURINE NUCLEOTIDE DERIVATIVES 审中-公开
标题翻译：嘌呤核苷衍生物
公开(公告)号：WO2005123755A2
公开(公告)日：2005-12-29
申请号：PCT/GB2005/002418
申请日：2005-06-20
申请人： LAURAS AS , COCKBAIN, Julian , UNDHEIM, Kjell , TASKÉN, Kjetil , KLAVENESS, Jo , LANGLI, Geir , BJØRNSTAD, Vidar
发明人： UNDHEIM, Kjell , TASKÉN, Kjetil , KLAVENESS, Jo , LANGLI, Geir , BJØRNSTAD, Vidar
IPC分类号： C07H
CPC分类号： C07H19/213 , Y10T436/143333
摘要： This invention provides novel 8-carbyl substituted cAMPS and a novel procedures for the preparation of 8-Br-cAMP, a key starting material.
摘要翻译：本发明提供新的8-羰基取代的cAMPS和用于制备8-Br-cAMP（一种关键起始物质）的新方法。

2. 发明申请

WO2008032103A2 PROCESS FOR THE PREPARATION OF AN (RP)-8-SUBSTITUTED CAMPS 审中-公开
标题翻译：制备（RP）-8-取代的樟脑的方法
公开(公告)号：WO2008032103A2
公开(公告)日：2008-03-20
申请号：PCT/GB2007/003522
申请日：2007-09-17
申请人： LAURAS AS , COCKBAIN, Julian , UNDHEIM, Kjell , ANDREI, Mioara
发明人： UNDHEIM, Kjell , ANDREI, Mioara
IPC分类号： C07H19/20 , A61K31/7076
CPC分类号： C07H19/20
摘要： This invention relates to a process for the preparation of an ( R p)-8-substituted adenosine-3',5'-cyclic phosphorothioic acid, or a salt or ester thereof, which comprises P-amidating 8-bromoadenosine-3',5'-cyclic phosphoric acid, and reacting the P-amidate with a base and with carbon disulphide to yield ( R p)-8-bromoadenosine-3',5'-cyclic phosphorothioic acid or a salt or ester thereof.
摘要翻译：本发明涉及制备（R）-β-取代的腺苷-3'，5'-环硫代磷酸或其盐的方法，或者其包括P-酰胺化8-溴腺苷-3'，5'-环磷酸，并且使该P-酰胺化物与碱和二硫化碳反应以产生（Rp）-8 - 溴腺苷-3'，5'-环硫代磷酸或其盐或酯。

3. 发明申请

WO2004056843A2 MACROLIDES 审中-公开
标题翻译：大环内酯类
公开(公告)号：WO2004056843A2
公开(公告)日：2004-07-08
申请号：PCT/GB2003/005659
申请日：2003-12-22
申请人： ALPHARMA APS , COCKBAIN, Julian , UNDHEIM, Kjell , GUNNES, Sølvi
发明人： UNDHEIM, Kjell , GUNNES, Sølvi
IPC分类号： C07H17/00
CPC分类号： C07H17/08
摘要： The invention provides antibiotic 10-desmethyl macrolides.
摘要翻译：本发明提供抗生素10-去甲基大环内酯类。

4. 发明公开

EP1765844A2 PURINE NUCLEOTIDE DERIVATIVES 失效转让
标题翻译：嘌呤核苷酸衍生物
公开(公告)号：EP1765844A2
公开(公告)日：2007-03-28
申请号：EP05755520.3
申请日：2005-06-20
申请人： Lauras AS , Cockbain, Julian
发明人： UNDHEIM, Kjell , TASKÉN, Kjetil , KLAVENESS, Jo , LANGLI, Geir , BJØRNSTAD, Vidar
IPC分类号： C07H19/213 , A61K31/7076
CPC分类号： C07H19/213 , Y10T436/143333
摘要： This invention provides novel 8-carbyl substituted Camps (adenosine 3′, 5′-cyclic monophosphorothioate) and a novel procedures for the preparation of 8-Br-cAMP, a key starting material.
摘要翻译：本发明提供了新的8-碳基取代的Cam（腺苷3'，5'-环状单硫代磷酸酯）和用于制备作为关键起始材料的8-Br-cAMP的新程序。

5. 发明申请

WO2009024214A1 PROCESS FOR THE PRODUCTION OF VORICONAZOLE 审中-公开
标题翻译：生产呋喃唑酮的方法
公开(公告)号：WO2009024214A1
公开(公告)日：2009-02-26
申请号：PCT/EP2008/005649
申请日：2008-07-10
申请人： AXELLIA PHARMACEUTICALS APS , HEGGELUND, Audun , UNDHEIM, Kjell
发明人： HEGGELUND, Audun , UNDHEIM, Kjell
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： A process for the preparation of voriconazole is described wherein alkylthio substituted pyrimidines are key intermediates. The alkylthio substituents render the pyrimidines particularly suitable for metal mediated addition to ketones. This is demonstrated in a cross-coupling reaction for the preparation of voriconazole.
摘要翻译：描述了制备伏立康唑的方法，其中烷硫基取代的嘧啶是关键中间体。烷硫基取代基使嘧啶特别适合金属介导的加成酮。这在用于制备伏立康唑的交叉偶联反应中证明。

6. 发明公开

EP0815090A1 PROCESS FOR TETRAAZACYCLOALKANE PREPARATION 失效
标题翻译：四氮杂环庚烷制备方法
公开(公告)号：EP0815090A1
公开(公告)日：1998-01-07
申请号：EP96904202.0
申请日：1996-03-01
申请人： NYCOMED IMAGING AS , COCKBAIN, Julian Roderick Michaelson
发明人： SANDNES, Rolf, Wiggo , VASILEVSKIS, Janis , UNDHEIM, Kjell , GACEK, Michel
IPC分类号： C07D487 , C07D257
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：本发明提供了用于促进大环产物的杂多-N-烷基化的四氮杂环烷制备的合成路线，并且因此有利于制备用于诊断成像的螯合剂和螯合物。该方法包括（i）使四烷基烷与桥联剂反应以将所述四烷基烷的胺氮偶联至桥连部分以产生稠合的三环中间体，（ii）使所述中间体在所述仲胺氮之间引入亚烷基桥稠合的三环中间体的外环，任选地将烷二亚基桥连部分从稠合三环中间体的环稠合位点处的叔胺氮上去偶联，和（iii）必要时将所述桥连部分去偶合以产生大环四氮杂环烷。

7. 发明公开

EP2081947A2 PROCESS FOR THE PREPARATION OF AN (RP)-8-SUBSTITUTED CAMPS 审中-公开
标题翻译：用于生产（RP）-8-取代CAMPS
公开(公告)号：EP2081947A2
公开(公告)日：2009-07-29
申请号：EP07804308.0
申请日：2007-09-17
申请人： Lauras AS
发明人： UNDHEIM, Kjell , ANDREI, Mioara
IPC分类号： C07H19/20 , A61K31/7076
CPC分类号： C07H19/20
摘要： This invention relates to a process for the preparation of an (Rp)-8-substituted adenosine-3',5'-cyclic phosphorothioic acid, or a salt or ester thereof, which comprises P-amidating 8-bromoadenosine-3',5'-cyclic phosphoric acid, and reacting the P-amidate with a base and with carbon disulphide to yield (Rp)-8-bromoadenosine-3',5'-cyclic phosphorothioic acid or a salt or ester thereof.

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