- Methods for preparing cholesterol, and derivatives and analogs thereof
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The present invention relates to the field of pharmaceutical chemistry, and in particular to methods of preparing cholesterol,and derivatives and analogs thereof. The cholesterol derivatives include, but not limited to, 7-dehydrocholesterol, 25-hydroxycholesterol, 25- hydroxy7dehydrocholesterol and ergosterol. In the invention, phytosterol can be used as a raw material to prepare the compound shown in the formula I through microbial conversion, and then cholesterol and the derivatives and analogues thereof are prepared.
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Paragraph 0394-0395; 0406-008
(2021/04/07)
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- MOLECULARLY IMPRINTED POLYMERS
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The present invention provides methods of designing molecularly imprinted polymers (MIPs) which have applications in extracting bioactive compounds from a range of bioprocessing feedstocks and wastes. The present invention is further directed to MIPs designed by the methods of the present invention.
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- METHODS AND COMPOSITIONS FOR THE TREATMENT OF ESTROGEN-DEPENDENT HYPERPROLIFERATIVE UTERINE DISORDERS
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The present invention relates to the treatment of estrogen-dependent hyperproliferative uterine disorders including endometriosis, uterine fibroids, endometrial hyperplasia, uterine cancer, and their related symptoms by intravaginally administering at least two active agents selected from an aromatase inhibitor,an antiinflammatory agent, and a uterine-selective estrogen receptor antagonist. This combination therapy reduces local estrogen production, blocks local estrogen action, and suppresses inflammation locally, resulting in starvation of the estrogen-dependent diseased tissues, relief of related symptoms, and retardation of disease progression. Intravaginal delivery maximizes local inhibition of estrogen production without significantly affecting systemic circulating estogen levels. This results in enhanced clinical ellicacy and reduced side effects.
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- Facile retro-cycloaddition of adducts derived from steroidal 5,7-diene and 4-phenyl-1,2,4-triazoline-3,5-dione by diisobutylaluminium hydride
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Facile retro-cycloaddition of adducts derived from a steroidal 5,7-diene and 4-phenyl-1,2,4-triazoline-3,5-dione was achieved by diisobutylaluminium hydride under mild conditions.
- Kondo, Fumihiro,Miyashita, Misako,Konno, Katsuhiro,Takayama, Hiroaki
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p. 2679 - 2680
(2007/10/02)
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- EFFECT ON ERGOSTEROL BIOSYNTHESIS OF A FUNGICIDE, SSF-109, IN BOTRYTIS CINEREA
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Treatment of Botrytis cinerea with a novel fungicide SSF-109, (dl)-cis-1-(4-chlorophenyl)-2-(1H-1,2,4-triazol-1-yl)cyclo-heptanol (0.45 μg ml-1), gave five 14α-methyl sterols, 24-methylene-24(25)-dihydrolanosterol, 24-methylene-24(25)-dihydrolanosten-3-one, obtusifoliol, obtusifolione, and 14α-methylfecosterol, together with ergosterol and ergosta-5,8,22-trien-3β-ol.SSF-109 was found to inhibit the biosynthesis of ergosterol at the 14α-demethylation step.
- Shirane, Noboru,Murabayashi, Akira,Masuko, Michio,Uomori, Atsuko,Yoshimura, Yohko,et al.
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p. 2513 - 2520
(2007/10/02)
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- IMPROVED SYNTHESIS OF 1,2,4-TRIAZOLINE-3,5-DIONE DERIVATIVES OF ERGOSTEROL AND A NEW METHOD FOR THEIR RECONVERSION TO ERGOSTEROL
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The ergosterol diene system reacts in excellent yield with a series of 4-substituted 1,2,4-triazoline-3,5-diones generated by in situ oxidation of the appropriate hydrazides with phenylseleninic anhydride or phenylseleninic acid.Diaryltelluroxide and diphenylselenoxide are also efficient oxidants.The diene system can be smoothly regenerated by alkaline hydrolysis.
- Barton, Derek H. R.,Lusinchi, Xavier,Ramirez, Jesus Sandoval
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p. 2995 - 2998
(2007/10/02)
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- Potent Hydrophylic Dienophiles. Synthesis and Aqueous Stability of Several 4-Aryl- and Sulfonated 4-Aryl-1,2,4-triazoline-3,5-diones and Their Immobilization on Silica Gel
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The purpose of this investigation is the development of a series of sulfonated 4-aryl-1,2,4-triazoline-3,5-diones (TADs) useful as potent dienophiles for Diels-Alder reactions in aqueous solution and capable of providing a TAD moiety immobilized on an insoluble support.TADs 4, 5, 23, 24, and 29 were all prepared by oxidation of the corresponding urazoles with N2O4.The urazole precursors were prepared by chlorosulfonation of the appropriate 4-arylurazole, followed in some cases by hydrolysis and neutralization.While TAD sulfonic acids 5 and 29 were not stable toward isolation, the presence of the bulky isopropyl groups in 23 and 24 rendered these TADs isolable in pure form and sufficiently stable in water to allow Diels-Alder reactions to compete successfully with attack on the TAD moiety by the solvent (see following paper).Urazolesulfonyl chlorides 2, 18, and 19 reacted with aminopropylsilylated silica gel 31 to give the corresponding immobilized sulfonamides, which were readily oxidized to TAD silica gels 33 (red) and 34 (purple).TAD acid 23 and 31 gave silica gel 35 in which the TAD moiety was attached to the gel via an ionic bond. 1,3-Dienes were selectively and quantitatively removed from solution by these silica gels and could be recovered quantitatively therefrom.
- Keana, John F.W.,Guzikowski, Anthony P.,Ward, David D.,Morat, Claude,Nice, Faith L. Van
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p. 2654 - 2660
(2007/10/02)
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- PRODUCTION AND PROPERTIES OF 1,4-CYCLIC ADDUCTS OF STEROID 5,7-DIENES WITH 3,6-PYRIDAZINEDIONE AND 1,4-PHTHALAZINEDIONE
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1,3-Phthalazinedione and 3,6-pyridazinedione, obtained by the action of lead tetraacetate or manganese dioxide on phthalohydrazide and of lead tetraacetate on malehydrazide, form 1,4-cyclic adducts in reaction with steroid 5,7-dienes; the reaction is promoted by the presence of aliphatic alcohols.The initial dienes can be regenerated from the synthesized cyclic adducts by reductive cleavage with complex metal hydrides or by electrochemical reduction.In addition to ergosterol, the action of a water-alcohol solution of alkali on the cyclic adduct of ergosterol with 1,4-phthalazinedione gives a salt-like compound, which is converted into 9(11)-dehydroergosterol and phthalohydrazide by the action of acids.
- Bogoslovskii, N. A.,Litvinova, G. E.,Titova, I. A.,Samokhvalov, G. I.,Mairanovskii, V. G.,et al.
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p. 1705 - 1710
(2007/10/02)
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