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1. 发明申请

WO2007017087A1 PROCESS FOR THE PREPARATION OF CRYSTALLINE PERINDOPRIL 审中-公开
标题翻译：制备结晶白蛋白的方法
公开(公告)号：WO2007017087A1
公开(公告)日：2007-02-15
申请号：PCT/EP2006/007258
申请日：2006-07-24
申请人： LEK PHARMACEUTICALS D.D. , JENKO, Branko , COPAR, Anton
发明人： JENKO, Branko , COPAR, Anton
IPC分类号： C07D209/42 , C07K1/00 , A61K31/404 , A61P9/00
CPC分类号： C07K5/06026 , C07D209/42
摘要： The present invention relates to a new process for the preparation of crystalline perindopril. The present invention also relates to new alkyl ammonium salts of perindopril and the processes for the preparation thereof.
摘要翻译：本发明涉及一种制备结晶培哚普利的新方法。本发明还涉及培哚普利的新的烷基铵盐及其制备方法。

2. 发明申请

WO2012089349A2 NOVEL POLYKETIDE COMPOUNDS AND METHODS OF MAKING SAME 审中-公开
标题翻译：新型的聚酮化合物及其制备方法
公开(公告)号：WO2012089349A2
公开(公告)日：2012-07-05
申请号：PCT/EP2011/006615
申请日：2011-12-30
申请人： ACIES BIO D.O.O. , KOSEC, Gregor , GORANOVIČ, Dušan , HORVAT, Jaka , FUJS, Štefan , JENKO, Branko , PETKOVIĆ, Hrvoje
发明人： KOSEC, Gregor , GORANOVIČ, Dušan , HORVAT, Jaka , FUJS, Štefan , JENKO, Branko , PETKOVIĆ, Hrvoje
IPC分类号： C07D407/12 , C07D498/04 , C12P17/16 , C12P19/62
CPC分类号： C07D407/12 , C07D498/04 , C12N9/1025 , C12N15/52 , C12P17/188 , C12P19/62
摘要： The present invention relates to novel polyketide compounds and to enzymes and production organisms for obtaining such novel polyketide compounds. Polyketides of the present invention include non-natural, chemically active extender units, which are incorporated into the polyketide molecule by virtue of promiscuous acyl transferase domains of the polyketide synthase enzyme. Such polyketides including chemically active side chains can easily be chemically modified to yield novel polyketide drugs or drug candidates.
摘要翻译：本发明涉及新型聚酮化合物以及用于获得这种新型聚酮化合物的酶和生产有机体。本发明的聚酮化合物包括非天然的化学活性增量剂单元，其通过聚酮化合物合酶的混杂酰基转移酶结构域被并入聚酮化合物分子中。包括化学活性侧链的这些聚酮化合物可以容易地进行化学修饰以产生新的聚酮化合物药物或候选药物。

3. 发明申请

WO2010112482A1 A PROCESS FOR DIMETHYLATION OF ACTIVE METHYLENE GROUPS 审中-公开
标题翻译：活性甲基团的二甲基化方法
公开(公告)号：WO2010112482A1
公开(公告)日：2010-10-07
申请号：PCT/EP2010/054151
申请日：2010-03-30
申请人： LEK PHARMACEUTICALS D.D. , JENKO, Branko , COPAR, Anton
发明人： JENKO, Branko , COPAR, Anton
IPC分类号： C07C231/12 , C07C253/30 , C07C255/19 , C07C237/06 , A61K31/275 , A61K31/16
CPC分类号： C07C253/30 , C07C231/12 , C07C237/06 , C07C255/19
摘要： The present invention discloses a process for dimethylation of active methylene groups. Specifically, the invention discloses aprocess for preparing3-amino-2,2- dimethylpropanamide. Compounds produced by the present dimethylation process such as 3-amino-2,2-dimethylpropanamide can be used as intermediates in the route of synthesis of therapeutic, prophylactic or diagnostic agent, for example aliskiren or cryptophycin. Particularly, the invention relates to embodiments further extending to processesfor preparing pharmaceutical dosage form comprising said therapeutic, prophylactic or diagnostic agents. More specifically, the invention relates to the use of compounds produced by the present dimethylation process for the manufacture of therapeutic, prophylactic or diagnostic agents or for the manufacture of pharmaceutical dosage forms comprising said therapeutic, prophylactic or diagnostic agents. The processes according to the present invention can be beneficially applied for the synthesis of various active pharmaceutical ingredients, such as aliskiren or crypthophycin.
摘要翻译：本发明公开了一种活性亚甲基二甲基化方法。具体地说，本发明公开了3-氨基-2,2-二甲基丙酰胺的制备方法。通过本发明的二甲基化方法制备的化合物如3-氨基-2,2-二甲基丙酰胺可用作合成治疗，预防或诊断剂例如阿利吉仑或隐霉素的途径中的中间体。特别地，本发明涉及进一步延伸至制备包含所述治疗性预防或诊断剂的药物剂型的方法的实施方案。更具体地，本发明涉及通过本发明的二甲基化方法制备的化合物在制备治疗，预防或诊断剂中的用途，或用于制备包含所述治疗，预防或诊断剂的药物剂型。根据本发明的方法可有利地用于合成各种活性药物成分，例如阿利吉仑或crypthophycin。

4. 发明申请

WO2004101515A1 A PROCESS FOR THE PREPARATION OF COMPOUNDS HAVING AN ACE INHIBITORY ACTION 审中-公开
标题翻译：制备具有ACE抑制作用的化合物的方法
公开(公告)号：WO2004101515A1
公开(公告)日：2004-11-25
申请号：PCT/SI2004/000021
申请日：2004-05-07
申请人： LEK PHARMACEUTICALS D.D. , JENKO, Branko
发明人： JENKO, Branko
IPC分类号： C07D207/16
CPC分类号： C07D207/16 , C07D209/42
摘要： The present invention relates to the process for the preparation of compounds of formula (I) having an ACE inhibitory action wherein carboxy group of stereospecific amino acid is activated with an uronium salt in in the presence of an aprotic solvent and an activated amino acid is further transformed with appropriate amine into ACE inhibitor or its precursor.
摘要翻译：本发明涉及制备具有ACE抑制作用的式（I）化合物的方法，其中立体特异性氨基酸的羧基在非质子溶剂和活化的氨基酸存在下用脲盐活化，进一步用适当的胺转化成ACE抑制剂或其前体。

5. 发明申请

WO2012089349A3 NOVEL POLYKETIDE COMPOUNDS AND METHODS OF MAKING SAME 审中-公开
标题翻译：新型聚合物化合物及其制备方法
公开(公告)号：WO2012089349A3
公开(公告)日：2012-12-27
申请号：PCT/EP2011006615
申请日：2011-12-30
申请人： ACIES BIO D O O , KOSEC GREGOR , GORANOVIC DUSAN , HORVAT JAKA , FUJS STEFAN , JENKO BRANKO , PETKOVIC HRVOJE
发明人： KOSEC GREGOR , GORANOVIC DUSAN , HORVAT JAKA , FUJS STEFAN , JENKO BRANKO , PETKOVIC HRVOJE
IPC分类号： C07D407/12 , C07D498/04 , C12N9/10 , C12N15/52 , C12P17/18 , C12P19/62
CPC分类号： C07D407/12 , C07D498/04 , C12N9/1025 , C12N15/52 , C12P17/188 , C12P19/62
摘要： The present invention relates to novel polyketide compounds and to enzymes and production organisms for obtaining such novel polyketide compounds. Polyketides of the present invention include non-natural, chemically active extender units, which are incorporated into the polyketide molecule by virtue of promiscuous acyl transferase domains of the polyketide synthase enzyme. Such polyketides including chemically active side chains can easily be chemically modified to yield novel polyketide drugs or drug candidates.
摘要翻译：本发明涉及新颖的聚酮化合物和用于获得这种新型聚酮化合物的酶和生产生物。本发明的聚酮化合物包括非天然的，化学活性的增量剂单元，其通过聚酮化合物合酶的混合酰基转移酶结构域结合到聚酮化合物分子中。包括化学活性侧链的这种聚酮化合物可以容易地进行化学修饰以产生新的聚酮化合物药物或候选药物。

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