CAS: 145599-86-6; (3R,5S,E)-7-(4-(4-Fluorophenyl)-2,6-Diisopropyl-5-(Methoxymethyl)Pyridin-3-yl)-3,5-Dihydroxyhept-6-Enoic Acid

📜(3R,5S)-7-[4-(4-Fluorophenyl)-5-(Methoxymethyl)-2,6-Di(Propan-2-yl)-3-Pyridinyl]-3,5-Dihydroxy-6-Heptenoic Acid,Cerivastatin Sodium,,甲醇,乙醇 以 水,丙酮 用作溶剂,化学反应生成西立伐他汀
参考文献:Liquid Statin Formulation
标题:Liquid Statin Formulation
摘要:本发明涉及适用于人或动物的液态他汀产品的组合物和方法.本发明提供了含有他汀和至少一种溶剂化剂的稳定液体配方.本发明还提供了口服他汀配方的方法.

专利信息

专利号:US-8269001-B2
优先权日:2005-10-05
标题 :Process for the synthesis of HMG-CoA reductase inhibitors
发明人：CASAR ZDENKO
权利人:CASAR ZDENKO; LEK PHARMACEUTICALS
摘要:A novel synthesis of statins uses Wittig reaction of a heterocyclic core of statin with a lactonized side chain already possessing needed stereochemistry. Any separation of diastereoisomers is performed early in the course of synthesis.

专利号:US-9085538-B2
优先权日:2010-07-26
标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof
发明人：CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO
权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS
摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.

专利号:EP-2017267-A1
优先权日:2007-07-16
标 题:Synthesis of statins
发明人：KOPITAR GREGOR; MRAK PETER; OSLAJ MATEJ
权利人:LEK PHARMACEUTICALS
摘要:The process for synthesis of statins is presented where the intermediate intermediate (4 R ,6 S )-6-(dialkoxymethyl)tetrahydro-2 H -pyran-2,4-diol which already possesses the desired stereochemistry corresponding to final statin is prepared by an aldolaze.

专利号:EP-2465936-A1
优先权日:2010-12-20
标题 :Enzymatic synthesis of statins and intermediates thereof
权利人:LEK PHARMACEUTICALS
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 intermdiate 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 interemediate thereof.

专利号:US-8471045-B2
优先权日:2007-04-03
标题 :Synthesis of statins
发明人：CASAR ZDENKO; MESAR TOMAZ; KOPITAR GREGOR; MRAK PETER; OSLAJ MATEJ
权利人:CASAR ZDENKO; MESAR TOMAZ; KOPITAR GREGOR; MRAK PETER; OSLAJ MATEJ; LEK PHARMACEUTICALS
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.

专利号:US-8293290-B2
优先权日:2003-04-08
标题:Annatto extract compositions, including geranyl geraniols and methods of use
发明人：TAN BARRIE
权利人:TAN BARRIE; AMERICAN RIVER NUTRITION INC
摘要:Annatto extract composition (AEC), including cis and trans geranyl geraniols (GG) and tocopherol-free C-5 unsubstituted tocotrienols (T3), increases the de novo synthesis of intermediate isoprenoid and distal protein products, including endogenous coenzyme Q10 (CoQ10), dolichols (DL) and all subsequent GG-prenylated and DL-glycosylated proteins, including GG-porphyrinated hemes. This intermediate and distal product replenishment by AEC reverses maladies of myotoxicity (of both drug and non-drug origins), including maladies that affect the muscle, kidney, eye, GI tract and skin, nerve, blood, and CoQ10-related syndromes of energetics and LDL protection. AEC anabolically increases the endogenous de novo CoQ10 synthesis via GG elongation/prenylation of side-chain and conversely CoQ10 catabolically increases the endogenous de novo GG synthesis via beta-oxidation of CoQ10. Also, such AEC decreases de novo synthesis and increases disposal of triglycerides (TG) in humans via PPAR activation and SREBP deactivation. Such drop in TG by AEC reverses maladies of insulin resistance (IR) and metabolic syndrome (MS), prediabetes, diabetes and diabetes-related cardiovascular diseases (CVD). GG activates PPAR and down regulates SREBP transcription factors. This AEC, containing GG, inhibits cancer growth whether or not GG involvement in protein prenylation is required.