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1.发明公开ENZYMATIC SYNTHESIS OF ACTIVE PHARMACEUTICAL INGREDIENT AND INTERMEDIATES THEREOF 有权ENZYMATISCHE SYNTHESE EINES PHARMAZEUTISCHEN WIRKSTOFFS UND ZWISCHENPRODUKTE DAVON
公开(公告)号：EP2655650A2
公开(公告)日：2013-10-30
申请号：EP11811536.9
申请日：2011-12-20
发明人： MRAK, Peter , ZOHAR, Tadeja , OSLAJ, Matej , KOPITAR, Gregor
摘要： The present invention discloses a process for preparing an active pharmaceutical ingredient (API) or intermediates thereof, notably particular step in the synthesis of an intermediate useful for example in the preparation of statins, by using an enzyme capable of catalyzing oxidation or dehydrogenation. The invention further provides an expression system effectively translating said enzyme. In addition, the invention relates to a specific use of such enzyme for preparing API or intermediate thereof, and in particular for preparing statin or intermediate thereof.
摘要翻译： 本发明公开了一种制备活性药物成分（API）或其中间体的方法，特别是通过使用能够催化氧化或脱氢的酶合成可用于制备他汀类的中间体的特别步骤。 本发明还提供了有效翻译所述酶的表达系统。 此外，本发明涉及这种酶用于制备API或其中间体，特别是用于制备他汀类或其中间体的具体用途。
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2.发明公开((2S,4R)-4,6-DIHYDROXYTETRAHYDRO-2H-PYRAN-2-YL) METHYL CARBOXYLATE AND PROCESS FOR ITS PRODUCTION EMPLOYING A 2-DEOXYRIBOSE-5-PHOSPHATE ALDOLASE 有权（（2S，4R）-4,6-二羟基四氢-2H-吡喃-2-基）一种制造THEREOF使用2-脱氧核糖-5-磷酸醛缩酶-METHYLCARBONSÄUREESTERAND METHOD
公开(公告)号：EP2247739A2
公开(公告)日：2010-11-10
申请号：EP09703893.9
申请日：2009-01-20
发明人： CLUZEAU, Jerome , CASAR, Zdenko , MRAK, Peter , OSLAJ, Matej , KOPITAR, Gregor
IPC分类号： C12P17/06 , C07C67/00 , C07D239/00 , C07D309/00
CPC分类号： C12P17/06 , C07D309/10
摘要： The present invention relates to ((2S,4R)-4,6-dihydroxytetrahydro-2H-pyran-2-yl)methyl carboxylates and a process for the production thereof. Furthermore, the present invention relates to a process for the production of statins and in particular of Rosuvastatin and derivates thereof, wherein the above mentioned compounds are used as intermediates.
摘要翻译： 本发明涉及（（2S，4R）-4,6-二羟基四氢-2H-吡喃-2-基）甲基羧酸盐和其生产方法。 进一步地，本发明涉及一种用于生产他汀类药物和瑞舒伐他汀中的具体和其衍生物，worin上述化合物被用作中间体。
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3.发明授权((2S,4R)-4,6-DIHYDROXYTETRAHYDRO-2H-PYRAN-2-YL)METHYL CARBOXYLATE AND PROCESS FOR ITS PRODUCTION EMPLOYING A 2-DEOXYRIBOSE-5-PHOSPHATE ALDOLASE (DERA) 有权（（2S，4R）-4,6-二羟基四氢-2H-吡喃-2-基）甲基羧酸酯及其生产使用2-脱氧核糖-5-磷酸脱醛酶（DERA）
公开(公告)号：EP2247739B1
公开(公告)日：2018-05-16
申请号：EP09703893.9
申请日：2009-01-20
发明人： CLUZEAU, Jerome , CASAR, Zdenko , MRAK, Peter , OSLAJ, Matej , KOPITAR, Gregor
IPC分类号： C12P17/06 , C07D309/10
CPC分类号： C12P17/06 , C07D309/10
摘要： The present invention relates to ((2S,4R)-4,6-dihydroxytetrahydro-2H-pyran-2-yl)methyl carboxylates and a process for the production thereof. Furthermore, the present invention relates to a process for the production of statins and in particular of Rosuvastatin and derivates thereof, wherein the above mentioned compounds are used as intermediates.
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4.发明授权
公开(公告)号：EP2655650B1
公开(公告)日：2017-12-20
申请号：EP11811536.9
申请日：2011-12-20
发明人： MRAK, Peter , ZOHAR, Tadeja , OSLAJ, Matej , KOPITAR, Gregor
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5.发明公开
公开(公告)号：EP2134696A2
公开(公告)日：2009-12-23
申请号：EP08718383.6
申请日：2008-04-02
发明人： CASAR, Zdenko , MESAR, Tomaz , KOPITAR, Gregor , MRAK, Peter , OSLAJ, Matej
IPC分类号： C07D239/42 , C07D309/30 , C07H3/02 , A61K31/506
CPC分类号： C07H3/02 , C07D239/42 , C07D309/30 , C07D405/06
摘要： The process for the synthesis of statins featuring the use of an early intermediate (4R,6S)-6-(dialkoxymethyl)tetrahydro-2H-pyran-2,4-diol which already possesses the desired stereochemistry corresponding to the final statin.
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6.发明授权
公开(公告)号：EP2134696B1
公开(公告)日：2017-05-17
申请号：EP08718383.6
申请日：2008-04-02
发明人： CASAR, Zdenko , MESAR, Tomaz , KOPITAR, Gregor , MRAK, Peter , OSLAJ, Matej
IPC分类号： C07D239/42 , C07D309/30 , C07H3/02 , A61K31/506
CPC分类号： C07H3/02 , C07D239/42 , C07D309/30 , C07D405/06
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