CAS: 59865-13-3; (3S,6S,9R,12R,15S,18S,21S,24S,30S,33S)-30-Ethyl-33-((1R,2R,E)-1-Hydroxy-2-Methylhex-4-En-1-yl)-6,9,18,24-Tetraisobutyl-3,21-Diisopropyl-1,4,7,10,12,15,19,25,28-Nonamethyl-1,4,7,10,13,16,19,22,25,28,31-Undecaazacyclotritriacontan-2,5,8,11,14,17,20,23,26,29

该化合物是一种循环性,不失节的免疫抑制剂,广泛用于器官移植和自动免疫疗法,有选择性地抑制卡列胆素,阻止T细胞活化和细胞基素生产,从而防止移植排斥和调节免疫反应.T-淋巴细胞的高度特性最大限度地减少了广泛的免疫抑制效应,减少了二次感染风险.Cyclospolin A在水中表现出低溶性,但在基于脂质的运载系统中形成,以提高生物利用率.该化合物的特点是生理状况稳定,可以预测的药用植物基因,可以精确剂量.它的临床效用有据可查,可以防止急性排斥和治疗诸如鼠麦病和风湿性动脉炎等病症.Cycloporin A的分析标准在高纯度的研究应用中可用.

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CAS号59865-15-5 二氢环孢菌素A | CAS号121584-52-9 6-[(3R,4R)-3-(乙...

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    专利信息


    专利号:US-4396542-A
    优先权日:1980-02-14
    标 题 :Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production
    发明人:WENGER ROLAND
    权利人:SANDOZ LTD
    摘要:A method for the total synthesis of cyclosporins, in particular Cyclosporin A, cyclosporins produced in accordance with the method of the invention and novel intermediates, in particular novel [1S, 2R, 3R]- and [1R, 2S, 3S]-1-nitrilo-1-carbonyl-3-methyl-2-oxy-heptanes and -hept-5-enes, employed in the method of the invention.

    专利号:US-4554351-A
    优先权日:1980-02-14
    标 题:Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production
    发明人:WENGER ROLAND
    权利人:SANDOZ LTD
    摘要:A method for the total synthesis of cyclosporins, in particular Cyclosporin A, cyclosporins produced in accordance with the method of the invention and novel intermediates, in particular novel [1S, 2R, 3R]- and [1R, 2S, 3S]-1-nitrilo-1-carbonyl-3-methyl-2-oxy-heptanes and -hept-5-enes, employed in the method of the invention.

    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.

    专利号:US-5948693-A
    优先权日:1994-09-01
    标题:Solid phase synthesis of immunosuppressive agents
    发明人:RICH DANIEL H; RAMAN PRAKASH; ANGELL YVONNE M
    权利人:WISCONSIN ALUMNI RES FOUND
    摘要:The present invention relates generally to cyclosporin analogs, and more paritcularly to methods for the solid-phase synthesis and on-resin cyclization of cyclosporin analogs. Methods are described for the on-resin cyclization of sterically hindered compounds synthesized through solid phase synthesis techniques. The methods utilize solvent, temperature, and washing conditions that allow the efficient on-resin cyclization of compounds like analogs of cyclosporin A.

    专利号:US-2009143426-A1
    优先权日:2007-12-04
    标 题:Synthesis of 1,3,6-trisubstituted-2-carboxyquinol-4-ones as selective ET A antagonists and their use as medicaments
    发明人:STEPHANI RALPH ANTHONY; PATEL HARDIK JITENDRA; REZNIK SANDRA EVE; CANTOR JEROME OWEN
    权利人:STEPHANI RALPH ANTHONY; PATEL HARDIK JITENDRA; REZNIK SANDRA EVE; CANTOR JEROME OWEN
    摘要:The invention discloses the composition and preparation of various 1,3,6-trisubstituted-2-carboxy-quinol-4-ones of the formula 1 where R is H, alkyl, haloalkyl or hydroxyalkyl, R′ is alkyl, nitro, halogen or NR 2 ′″ where R′″ is alkyl or cycloalkyl, and R″ is H or alkyl. The composition of the invented compounds as methods of antagonizing the action of endothelin-1 to treat cardiovascular, pulmonary diseases and obstetric disorders and preterm labor and preeclampsia in mammals is disclosed.

    专利号:WO-0031134-A9
    优先权日:1998-11-20
    标题:Regulation of hair follicle morphogenesis based on beta-catenin
    发明人:GAT URI; DASGUPTA RAMANUJ; DEGENSTEIN LINDA; FUCHS ELAINE
    权利人:ARCH DEV CORP; GAT URI; DASGUPTA RAMANUJ; DEGENSTEIN LINDA; FUCHS ELAINE
    摘要:The present invention provides a method for inducing hair growth by providing beta-catenin activity to a skin cell. This may be achieved by providing a beta-catenin polypeptide, providing a beta-catenin agonist, providing a polynucleotide encoding a beta-catenin polypeptide, enhancing the de novo synthesis of beta-catenin, increasing the stability or decreasing the degradation of beta-catenin polypeptides.
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    主要参考文献


    1: Colombo D, Ammirati E. Cyclosporine in transplantation - a history of converging timelines. J Biol Regul Homeost Agents. 2011 Oct-Dec;25(4):493-504. Review. Cyclosporine]. Nihon Naika Gakkai Zasshi. 2011 Oct 10;100(10):2942-7. Review. Japanese. Epub 2011 Sep 1. Review. Epub 2011 May 26. Review. Epub 2011 May 17. Review. Review. Chinese. Epub 2011 Apr 21. Review. Review. Review. Review.

    合成参考文献


    参考文献:10.1371/journal.pone.0218897
    摘要:Miller TW, Amason JD, Garcin ED, Lamy L, Dranchak PK, Macarthur R, Braisted J, Rubin JS, Burgess TL, Farrell CL, Roberts DD, Inglese J. Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. PLoS ONE. 2019 Jul 05;14(7):e0218897. doi: 10.1371/journal.pone.0218897.
    摘要:S10 | SWISSPHARMA | Pharmaceutical List with Consumption Data | DOI:10.5281/zenodo.2623484
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