- He the sandbank contains the fluorine derivative and use thereof
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The present invention belongs to the field of pharmaceutical chemistry, and provides 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor, wherein a fragment containing 3-fluoro-caprolactone and a lactone thereof are subjected to ring opening to form a poly-substituted pyrimidine statin fluorine-containing modifier of 1-fluoro-3-hydroxy-pentanoic acid and a salt or ester thereof, ie., the 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor, and the structure formula is defined in the specification. According to the present invention, the test results show that the compounds have the HMG-CoA reductase activity inhibition effects, and can be used as the new generation of the potential HMG-CoA reductase inhibitors.
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Paragraph 0273; 0274; 0275
(2017/08/26)
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- Fermentation Medias and Processes Thereof
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The present invention demonstrates the utility of carbonic acid amides such as urea or its derivatives, carbamates, carbodiimides & thiocarbamides as nitrogenous supplements in fermentation media for production of recombinant proteins to achieve enhanced bioconversion rates and peptides like insulin and insulin analogues, exendin and enzymes such as lipase using methanol inducible fungal expression systems such as Pichia.
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Page/Page column
(2014/05/25)
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- In situ bioconversion of compactin to pravastatin by Actinomadura species in fermentation broth of Penicillium citrinum
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The biocatalytic production of pravastatin from compactin by hydroxylation has found many applications in health care and pharmaceuticals. Actinomadura macra, Actinomadura madurae, and Actinomadura livida can efficiently bioconvert compactin to pravastatin. The fermentation broth (Penicillium citrinum fermented media) harvested on the eighth day contained 388.90 mg L-1 of compactin and an undetectable level of mycotoxin (citrinin). Bioconversion by A. macra was highest (87 %) in the yeast extract-amended medium. The anti-actinomadura effects of citrinin reduce the bioconversion capacity of Actinomadura. The in situ hydroxylation of compactin produced by P. citrinum represents a preferable alternative for the use of purified compactin, as a way to reduce cost and time processing.
- Ahmad, Ajaz,Mujeeb, Mohd,Kapoor, Rohit,Panda, Bibhu Prasad
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p. 667 - 671
(2013/07/26)
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- Methods for predicting the response to statins
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The invention provides methods for optimizing therapeutic efficacy for treating hypercholesterolemia in a subject having a cardiovascular disease (CVD), comprising (a) determining subject characteristics that affect the likelihood of reaching a goal level of low density lipoprotein (LDL); and (b) obtaining success probabilities of a variety of statin treatments for reaching said goal level of LDL using said subject characteristics and a multivariate model; and (c) administrating the optimal statin treatment with the highest success probability of step (b) to said subject thereby optimizing therapeutic efficacy for treating hypercholesterolemia in said subject.
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- Drug or Supplement Combination with Conjugated Linoleic Acid for Fat Loss in Mammals
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Food, feed or drug combinations with conjugated linoleic acid are described that cause enhanced fat loss in mammals more efficiently than any of the individual components of the combination. Food, feed, or drugs that activate AMP activated protein kinase, agonists of nuclear receptors that bind RXR in adipocytes, or statin inhibitors were found to be more effective for fat loss when combined with conjugated linoleic acid.
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- Efficient biotransformations using Escherichia coli with tolC acrAB mutations expressing cytochrome P450 genes
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We report here some efficient biotransformations using Escherichia coli strains with disruptions for the AcrAB-TolC efflux pump system. Biotransformations of compactin into pravastatin (6α-hydroxy-iso- compactin) were performed using E. coli strains with tolC and/or acrAB mutations expressing a cytochrome P450 (P450) gene. The production levels of pravastatin using strains with acrAB, tolC, and tolC acrAB mutations increased by 3.7-, 7.0-, and 7.1-fold, respectively. Likewise, the production levels of 25-hydroxy vitamin D3 and 25-hydroxy 4-cholesten 3-one using tolC acrAB mutant strains expressing an individual P450 gene increased by 2.2- and 16-fold, respectively. The enhancement of this biotransformation efficiency could be explained by increases in the intracellular amounts of substrates and the concentrations of active P450s. These results demonstrate that we have achieved versatile methods for efficient biotransformations using E. coli strains with tolC acrAB mutations expressing P450 genes.
- Fujii, Tadashi,Fujii, Yoshikazu,Machida, Kazuhiro,Ochiai, Atsushi,Ito, Masashi
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experimental part
p. 805 - 810
(2009/10/10)
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- Capillary electrophoresis determination of pravastatin and separation of its degradation products
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A capillary zone electrophoresis method for pravastatin determination was developed and validated. Rapid migration of negatively charged pravastatin molecule was obtained in alkaline buffer by the application of electric field of 30 kV. Influence of the pH value and ionic strength of running buffer, applied voltage and capillary temperature on mobility and sensitivity was evaluated. Detection wavelength was set to 237 nm. The method was applied to the determination of the drug in pharmaceutical dosage form. Pravastatin is a δ-hydroxy acid, which is prone to lactonize and epimerize in a pH-dependent manner. Micellar electrokinetic chromatographic approach was chosen to develop a method able to separate pravastatin and its degradation products in acidic media. The proposed method allows baseline separation of hydroxy acid and neutral lactone forms of the drug that appear as interconversion products depending on the pH value.
- Nigovic, Biljana,Vegar, Ivana
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experimental part
p. 615 - 622
(2009/12/03)
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- Strains of saccharaothrix, process for producing pravastain using the strains and isolation process of (HMG)-CoA reductase
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The present invention provides two new microorganism strains of Saccharothrix, designated as YS-44442 and YS-45494, a process of producing pravastatin using the strains, and an improved process for isolation of (HMG)-CoA reductase inhibitors.
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- PROCESS FOR THE PREPARATION OF PRAVASTATIN
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The invention relates to a process for the preparation of pure pravastatin or a salt thereof using an adsorption chromatography technique. The invention also relates to pharmaceutical compositions that include the pure pravastatin and to use of the compositions for treating hypercholesterolemia.
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Page/Page column 6
(2008/06/13)
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- Method of purifying pravastatin
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The present invention provides pure pravastatin compositions and pure compactin compositions, and methods for the preparation thereof.
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Page/Page column 7
(2008/06/13)
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- Treatment of type 1 diabetes with PDE5 inhibitors
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The use of a PDE5 inhibitor without substantial PDE2 inhibiting activity, or a pharmaceutically acceptable salt thereof in the preparation of a medicament for the treatment of Type 1 Diabetes. A method of treating Type 1 Diabetes in an individual suffering from Type 1 Diabetes, which method comprises administering to said individual an effective amount of a PDE5 inhibitor without substantial PDE2 inhibiting activity, or a pharmaceutically acceptable salt thereof.
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- Process for the purification of pravastatin
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A method of isolating or purifying pravastatin or its pharmaceutically acceptable salt characterized by involving, in the process of isolating or purifying pravastatin or its pharmacologically acceptable salt, the step of extracting pravastatin using an organic solvent represented by the formula CH3CO2R wherein R represents an alkyl group having 3 or more carbon atoms or the step of decomposing impurities using an inorganic acid or an inorganic base; and compositions containing pravastatin sodium thus obtained.
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- Method for producing pharmaceutical dosage forms
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The invention relates to a method for producing a granulate while using spray-dried D-mannitol and to the production of pharmaceutical dosage forms comprised of granulates of this type. The invention additionally relates to granulates obtained by using this method and to pharmaceutical dosage forms, which contain statins, especially cerivastatin, and which can be produced from said granulates.
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- Microbial process for preparing pravastatin
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The present invention relates to a new microbial process for the preparation of the compound formula (I) from a compound of general formula (II) wherein R stands for an alkali metal or ammonium ion, by the submerged cultivation of a mold strain able to 6β-hydroxylate a compound of the Formula (II) in aerobic fermentation and by the separation and purification of the product of Formula (I) formed in the course of the bioconversion. The process comprises cultivating a strain of Mortierella maculata filamentous mold species that is able to 6β-hydroxylate a compound of the general Formula (II), on a nutrient medium containing assimilable carbon and nitrogen sources and mineral salts and separating the product formed from the fermentation broth, then isolating the compound of formula (I) and purifying the same. Novel strains of Mortierella maculata are also disclosed.
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- METHOD FOR PRODUCING MEDICAMENTS CONTAINING HMG-COA-REDUCTASE INHIBITORS
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The invention relates to a process for producing medicaments which comprise HMG CoA reductase inhibitors in the form of their salts, characterized in that the corresponding precursors of the actual active compounds are converted with bases, which contain alkali metal or alkaline earth metal ions, in a solvent, into the active compound, and the resulting active compound-containing solution is processed into the desired administration form.
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- Conversion of compactin to pravastatin by Actinomadura
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A method for converting compactin to pravastatin is described. Compactin is provided and contacted with an agent derived from Actinomadura under conditions in which the agent converts compactin to pravastatin. Also described are an Actinomadura strain, an Actinomadura cell free extract, an Actinomadura hydroxylase, and a method for lowering cholesterol levels in mammals.
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- Biotransformation of compactin to pravastatin by Actinomadura sp. 2966
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Actinomadura sp. strain 2966 can effectively convert compactin to pravastatin. The degree of conversion observed was 65% to 78% of compactin added and 65% to 88% of compactin taken up, depending on the concentration of compactin and duration of the experiment. Increasing the compactin concentration resulted in a higher final pravastatin concentration especially when compactin was added intermittently. Higher glucose concentrations had no effect on the bioconversion although uptake of compactin was inhibited. The conversion was linear over 16 hours. The system requires no induction and thus appears to be different from previously studied hydroxylases from actinomycetes.
- Peng, Yulin,Yashphe, Jacob,Demain, Arnold L.
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p. 1032 - 1035
(2007/10/03)
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