专利号:US-11479577-B2 优先权日:2016-05-18 标题:Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY; DAVIES IEUAN; OTTER CARL; BATCHELOR RHYS 权利人:NZP UK LTD 摘要:The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):wherein:, R1, R2, R3, R4, R5, R6 and Y are as defined herein.The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.
专利号:US-12358871-B2 优先权日:2019-05-15 标 题:Photochemical synthesis of vitamin D3 using sensitizers 发明人:DATLA ANUPAMA; NAGRE PRASHANT; TAMORE JAGDISH; TRIVIKRAM SREENATH; DEGAONKAR GAJANAN 权利人:FERMENTA BIOTECH LTD 摘要:The present invention discloses an improved photochemical synthesis of vitamin D3 from 7-dehydrocholesterol alone or in combination with sterol precursors in presence of the photosensitizer of Formula I in high yield and with reduced levels of impurities.
专利号:US-4360470-A 优先权日:1980-10-22 标题 :Process and intermediates for the synthesis of Vitamin D3 metabolites and chenodeoxycholic acid 发明人:BATCHO ANDREW D; USKOKOVIC MILAN R; WOVKULICH PETER M 权利人:HOFFMANN LA ROCHE 摘要:The present disclosure is directed to a process for the synthesis of chenodeoxychloic acid, 25-hydroxycholesterol and 1α,25-dihydroxycholesterol from 17-keto steroids. A cholic acid side chain is stereospecifically introduced by reaction of the appropriate 17-keto steroid with ethyltriphenylphosphonium halides to produce the 17-ethylidene derivative which is allowed to react with acrylic acid esters or propiolic acid esters followed by hydrogenation.
专利号:US-4310467-A 优先权日:1980-10-22 标题:Process and intermediates for the synthesis of vitamin D3 metabolites 发明人:BATCHO ANDREW D; BERGER JR DONALD E; USKOKOVIC MILAN R 权利人:HOFFMANN LA ROCHE 摘要:The present disclosure is directed to a process and intermediates for the synthesis of Vitamin D 3 metabolites such as 1,25-dihydroxycholecalciferol, 25-hydroxycholecalciferol and 24R,25-dihydroxycholecalciferol from 17-keto steroids via intermediates having the natural steroid configuration at the 20-position. These novel intermediates are prepared from 17-keto steroids by reaction with ethyltriphenylphosphonium halides followed by reaction with formaldehyde to form comounds having the natural steroid configuration at the 20-position and which are suitable substrates for the preparation of the aforementioned Vitamin D 3 metabolites.
专利号:US-11547655-B2 优先权日:2017-08-02 标 题:Use of an extract of the pericarp of Nephelium lappaceum for hydrating the skin and/or mucous membranes 发明人:BONNET ISABELLE; CADAU SÉBASTIEN; DANOUS LOUIS; DERCEVILLE CHARLOTTE; LEOTY-OKOMBI SABRINA 权利人:BASF BEAUTY CARE SOLUTIONS FRANCE S A S 摘要:A subject of the present invention is the cosmetic use of a pericarp extract of the plant Nephelium lappaceum for maintaining and/or increasing the hydration and/or the barrier effect of the skin and/or of the mucous membranes. The pericarp extract increases involucrin synthesis and the hyaluronic acid content and the synthesis of ATP and of the taurine transporter TAUT. Another subject of the invention relates to a cosmetic care process comprising the topical application of the pericarp extract of N. lappaceum. Finally, a subject of the invention relates to the pericarp extract for use, in particular dermatological use, thereof in the treatment and/or prevention of pathological conditions caused by a state of abnormal dryness of the skin and/or of the mucous membranes.
专利号:US-8147883-B1 优先权日:1999-09-22 标题:Use of a plant oil product as an agent for increasing the synthesis of skin lipids 发明人:MSIKA PHILIPPE; PICCIRILLI ANTOINE 权利人:MSIKA PHILIPPE; PICCIRILLI ANTOINE; EXPANSCIENCE LAB 摘要:The invention concerns the use of at least a vegetable oil product selected among the group consisting of vegetable oil oleic distillates, vegetable oil unsaponifiable matters, vegetable oil furan lipids and mixtures thereof, as agents for increasing skin lipid synthesis, in particular lipids of the epidermal skin barrier, in or for preparing a composition containing a pharmaceutically or dermatologically acceptable medium. The use enables to prevent and/or treat deterioration of the skin barrier (dry skin, skin subjected to actinic radiation, ichthyosis, acne, xerosis, atopic dermatitis, sensitive skin, chafing and reactive skin, itching and the like).
1: Mi J, Jiang Q, Qi Z, Liu Z, Bai X, Zheng X, Wu J, Fang Y, Yang A, Chen H. Plasma campesterol and ABCG5/ABCG8 gene loci on the risk of cholelithiasis and cholecystitis: evidence from Mendelian randomization and colocalization analyses. Hum Genomics. 2024 Feb 12;18(1):19. doi: 10.1186/s40246-024-00583-y. 2: Nunes VS, de Campos EVS, Baracat J, França V, Gomes ÉIL, Coelho RP, Nakandakare ER, Zago VHS, de Faria EC, Quintão ECR. Plasma Campesterol Is Positively Associated with Carotid Plaques in Asymptomatic Subjects. Int J Mol Sci. 2022 Oct 9;23(19):11997. doi: 10.3390/ijms231911997. 3: Qian YD, Tan SY, Dong GR, Niu YJ, Hu CY, Meng YH. Increased campesterol synthesis by improving lipid content in engineered Yarrowia lipolytica. Appl Microbiol Biotechnol. 2020 Aug;104(16):7165-7175. doi: 10.1007/s00253-020-10743-4. Epub 2020 Jun 26. 20(7):e202300536. doi: 10.1002/cbdv.202300536. Epub 2023 Jul 4. Molecular Docking Studies. Chem Biodivers. 2023 Dec;20(12):e202301534. doi: 10.1002/cbdv.202301534. Epub 2023 Nov 28.
合成参考文献
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