甘草次酸,Succinic Anhydride置于吡啶,4-二甲氨基吡啶体系中,化学反应生成 甘珀酸 参考文献:Synthesis And Proteasome Inhibition Of Glycyrrhetinic Acid Derivatives 标题:Synthesis And Proteasome Inhibition Of Glycyrrhetinic Acid Derivatives 摘要:This Study Discovered That Glycyrrhetinic Acid Inhibited The Human 20S Proteasome At 22.3 Mu M. Esterification Of The C-3 Hydroxyl Group On Glycyrrhetinic Acid With Various Carboxylic Acid Reagents Yielded A Series Of Analogs With Marked Improved Potency. Among The Derivatives,Glycyrrhetinic Acid 3-O-Isophthalate (17) Was The Most Potent Compound With Ic50 Of 0.22 Mu M,Which Was Approximately 100-Fold More Potent Than Glycyrrhetinic Acid. (C) 2008 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Bmc.2008.05.078
专利号:US-12264143-B2 优先权日:2020-12-17 标 题:Synthesis of cannabinoids and cannabinoid precursors, and related compounds, formulations, and methods of use 发明人:SAMMIS GLENN M; ROGGEN MARKUS 权利人:NALU BIO INC 摘要:Methods are provided for the synthesis of cannabinoids, including cannabidiol (CBD), cannabinol (CBN), cannabichromene (CBC), cannabidiolic acid (CBDA), cannabigerol (CBG), cannabigerolic acid (CBGA), cannabidivarin (CBDV), cannabidibutol (CBD-C4), dihydrocannabidiol (DCBD), tetrahydrocannabivarin (THCV), analogs thereof, and precursors to the foregoing. One method employs phloroglucinol or a phloroglucinol analog as a starting material. The syntheses are stereospecific, efficient, selective, and cost-effective, with little or no potential for generation of THC ((−)-trans-Δ9-tetrahydro-cannabinol) or any other psychoactive side product. Telescoped syntheses are also provided, as are new cannabinoids, pharmaceutical formulations, and methods of use.
专利号:US-8802660-B2 优先权日:2007-03-12 标 题:De novo synthesis of glucocorticoids in the epidermis and its uses and applications 发明人:TOMIC-CANIC MARJANA; BREM HAROLD; SAMUELS HERBERT H 权利人:TOMIC-CANIC MARJANA; BREM HAROLD; SAMUELS HERBERT H; UNIV NEW YORK 摘要:The present invention relates to methods and compositions that control, i.e., antagonize/inhibit or agonize/stimulate, de novo glucocorticoid production in the skin. Such methods and compositions can be used for the prevention and/or treatment of a variety of skin conditions, including inflammation, acute wounds, chronic non-healing wounds, keloid, fibrotic or hypertrophic scars, and epithelial-derived cancer.
专利号:EP-1886695-A1 优先权日:2006-06-27 标 题:Pharmaceutical combination of an aldosterone synthase inhibitor and a glucocorticoid receptor antagonist or a cortisol synthesis inhibitor or a corticotropin releasing factor antagonist 发明人:SCHUMACHER CHRISTOPH 权利人:SPEEDEL EXPERIMENTA AG 摘要:The invention relates to a pharmaceutical combination comprising (a) an aldosterone synthase inhibitor or a pharmaceutically acceptable salt thereof, and (b) a glucocorticoid receptor antagonist or a cortisol synthesis inhibitor or a cortisol re-synthesis inhibitor or a corticotrophin-releasing hormone receptor antagonist or combinations thereof or in each case a pharmaceutically acceptable salt thereof. Said composition is useful for the manufacture of a medicament, in particular for the manufacture of a medicament for the prevention of, delay of progression of treatment of a disease or condition characterized by the metabolic syndrome.
专利号:US-2024368108-A1 优先权日:2020-12-17 标题:Synthesis of cannabinoids and cannabinoid precursors, and related compounds, formulations, and methods of use
专利号:US-4381301-A 优先权日:1980-05-07 标题 :Substituted tricyclic thieno compounds, their synthesis, their use, their compositions and their medicaments 发明人:RAINER GEORG 权利人:BYK GULDEN LOMBERG CHEM FAB 摘要:Substituted thienobenzodiazepinones of the general formula I (I) [wherein R1 denotes a hydrogen atom (-H) or an alkyl radical with 1 to 4 carbon atoms; R2 represents a halogen atom (halo) or has one of the meanings of R1; R3 denotes a halogen atom (halo) or the group -N(R4)R5; R4 denotes an alkyl radical with 1 to 4 carbon atoms or an alkenyl radical with 3 to 5 carbon atoms; R5 has one of the meanings of R4 or represents the group -(CH2)m-N(R6)R7; or R4 and R5, together with the nitrogen atom to which both are bonded, denote a morpholino group, a pyrrolidino group, a piperidino group, a hexahydroazepin-1-yl group, a piperazin-1-yl group (which is optionally substituted in the 4-position by a methyl, ethyl or benzyl group), a 2,4-dimethylpiperazin-1-yl group, or a hexahydro-1H-1,4-diazepin-1-yl group (which is substituted in the 4-position by a methyl or ethyl group); R6 denotes an alkyl group with 1 to 4 carbon atoms; R7 denotes an alkyl group with 1 to 4 carbon atoms; A denotes a straight-chain or branched alkylene group with 1 to 5 carbon atoms; and m denotes 2 or 3] and their acid-addition salts are new compounds. They either have a protective action on the stomach and intestine and are suitable for treating illnesses based on disorders of the stomach or intestine, or they are intermediates for preparing products having protective action. Processes for the preparation of the new pharmacologically-active compounds and of the intermediate products are presented.
专利号:US-8501954-B2 优先权日:2008-07-29 标题:Asymmetric process for making substituted 2-amino-thiazolones 发明人:CAILLE SEB; CUI SHENG; WANG XIANG; FAUL MARGARET 权利人:CAILLE SEB; CUI SHENG; WANG XIANG; FAUL MARGARET; AMGEN INC 摘要:The invention provides two process for synthesizing substituted aminothiazolone compounds as inhibitors of 11-β-hydroxy steroid dehydrogenase type 1. The processes allow the stereoselective synthesis of the desired compounds without the use of stoichiometric amounts of chiral catalysts.
1: Al-Bader MD, Jasem SA, Kilarkaje N. Carbenoxolone exposure during late gestation in rats alters placental expressions of p53 and estrogen receptors. Eur J Pharmacol. 2016 Nov 15;791:675-685. doi: 10.1016/j.ejphar.2016.09.035. Epub 2016 Sep 28. doi: 10.1016/j.bbrc.2015.11.034. Epub 2015 Nov 11. doi: 10.1016/j.abb.2014.06.027. Epub 2014 Jul 1. 4: Franco-Pérez J, Ballesteros-Zebadúa P, Manjarrez-Marmolejo J. Unilateral microinjection of carbenoxolone into the pontis caudalis nucleus inhibits the pentylenetetrazole-induced epileptiform activity in rats. Neurosci Lett. 2015 Aug 18;602:38-43. doi: 10.1016/j.neulet.2015.06.037. Epub 2015 Jun 30. doi: 10.1016/j.neulet.2014.01.042. Epub 2014 Jan 31. 6: Moustafa YM, El-Azab MF, Fouda A. 15-PGDH inhibitors: the antiulcer effects of carbenoxolone, pioglitazone and verapamil in indomethacin induced peptic ulcer rats. Eur Rev Med Pharmacol Sci. 2013;17(15):2000-9. doi: 10.1007/s12015-015-9628-2.
合成参考文献
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