Sodium Tauroursodeoxycholate置于盐酸体系中,用 水,丙酮 用作溶剂,化学反应 1.0H,反应生成牛磺熊去氧胆酸 参考文献:Process For The Preparation Of Tauroursodesoxycholic Acid 标题:Process For The Preparation Of Tauroursodesoxycholic Acid 摘要:本发明涉及一种制备牛磺胆酸的新方法,包括通过选择性沉淀来去除从水溶性牛磺酸钠与乙酮溶液中的醇氧化胆酸混合酐的烷基氯甲酸酯反应产生的悬浮液中存在的杂质的步骤.
专利号:WO-2020020904-A1 优先权日:2018-07-23 标题:Therapeutic uses of glp-2 agonists 发明人:LINDSTRÖM ERIK; SKARBALIENE JOLANTA 权利人:ZEALAND PHARMA AS 摘要:The invention relates to the use of GLP-2 agonists to modulate bile acid metabolism. In particular, it is believed that GLP-2 agonists may be capable of inhibiting bile acid synthesis, and so are useful for the treatment of conditions in which inhibition of bile acid synthesis is beneficial. Such conditions include primary bile acid diarrhea, secondary bile acid diarrhea and conditions which cause or contribute to cholestasis. The invention further relates to the use of FGF19 and C4 as biomarkers to monitor bile acid synthesis and homoeostasis, e.g. in SBS patients.
专利号:US-11918657-B2 优先权日:2017-11-10 标 题 :Dendrimer delivery system and methods of use thereof 发明人:RANGARAMANUJAM KANNAN; SHARMA RISHI; SHARMA ANJALI; KANNAN SUJATHA; ZHANG ZHI; KAMBHAMPATI SIVA PRAMODH 权利人:UNIV JOHNS HOPKINS 摘要:Low-generation dendrimers containing a high density of surface hydroxyl groups, and methods of synthesis thereof are provided. In particular, oligo ethylene glycol (OEG)-like dendrimers with a high surface functional groups at relatively low generations (e.g. Ëœ120 hydroxyls in the third generation, with a size of just 1-2 nm) is described. Dendrimer formulations including one or more prophylactic, therapeutic, and/or diagnostic agents, and methods of use thereof are also described. The formulations are suitable for topical, enteral, and/or parenteral delivery for treating one or more diseases, conditions, and injuries in the eye, the brain and nervous system (CNS), particularly those associated with pathological activation of microglia and astrocytes.
专利号:US-2014228422-A1 优先权日:2011-03-18 标 题 :Targets for treatment of er stress 发明人:HOTAMISLIGIL GÖKHAN S; FU SUNENG 权利人:HOTAMISLIGIL GÖKHAN S; FU SUNENG; HARVARD COLLEGE 摘要:The embodiments of the invention provide for genetic, chemical or dietary interventions that modulate hepatic phospholipid synthesis and/or endoplasmic reticulum (ER) calcium homeostasis function. More specifically, the present invention addresses modulation of the lipid composition of the hepatic stressed ER and/or improvement of the hepatic ER calcium metabolism to reduce ER stress and thus treat type 2 diabetes, fatty liver disease, atherosclerosis, inflammation, and/or dislipidemia.
专利号:US-9295677-B2 优先权日:2008-02-26 标题 :Polyhydroxylated bile acids for treatment of biliary disorders 发明人:LING VICTOR; WANG RENXUE; SHEPS JONATHAN AHAB 权利人:LING VICTOR; WANG RENXUE; SHEPS JONATHAN AHAB; QING BILE THERAPEUTICS INC 摘要:The invention provides, in part, polyhydroxylated bile acids for treating biliary disorders, for example, biliary disorders arising out of cholestasis of portal hypertension. The invention also provides, in part, polyhydroxylated bile acids for stimulating bile flow. New compounds 2α,3α,7α,12α-tetrahydroxy-5β-cholanoic acid and 3α.4α,7α,12α-tetrahydroxy-5β-cholanoic acid are disclosed, uses thereof and synthesis thereof.
专利号:CN-112588319-A 优先权日:2020-12-22 标题:Application of Silane and Its Catalytic Synthesis of Tauroursodeoxycholic Acid
专利号:IT-1167038-B 优先权日:1983-11-30 标 题:PROCEDURE FOR THE SYNTHESIS OF URSODESOXICOLIC ACID CONJUGED WITH TAURINE
1: WHO Drug Information, Vol. 34, No. 2, 2020 2. Chen F, Ge Z, Li N, Yu Z, Wu R, Zhao Y, He X, Cai G. TUDCA protects against tunicamycin-induced apoptosis of dorsal root ganglion neurons by suppressing activation of ER stress. Exp Ther Med. 2022 Jun 10;24(2):509. doi: 10.3892/etm.2022.11436. 3. Kim SY, Kwon YW, Jung IL, Sung JH, Park SG. Tauroursodeoxycholate (TUDCA) inhibits neointimal hyperplasia by suppression of ERK via PKCα-mediated MKP-1 induction. Cardiovasc Res. 2011 Nov 1;92(2):307-16. doi: 10.1093/cvr/cvr219. Epub 2011 Aug 11. 11(7):1275. doi: 10.3390/antiox11071275. 5. Song M, Zhang F, Fu Y, Yi X, Feng S, Liu Z, Deng D, Yang Q, Yu M, Zhu C, Zhu X, Wang L, Gao P, Shu G, Ma X, Jiang Q, Wang S. Tauroursodeoxycholic acid (TUDCA) improves intestinal barrier function associated with TGR5-MLCK pathway and the alteration of serum metabolites and gut bacteria in weaned piglets. J Anim Sci Biotechnol. 2022 Jun 8;13(1):73. doi: 10.1186/s40104- 022-00713-3. PMCID: PMC9175448
合成参考文献
参考文献:10.3233/jad-2011-100395 摘要:Viana RJ, Steer CJ, Rodrigues CM. Amyloid-β peptide-induced secretion of endoplasmic reticulum chaperone glycoprotein GRP94. J Alzheimers Dis. 2011;27(1):61–73. doi: 10.3233/jad-2011-100395. 参考文献:10.1371/journal.pone.0022094 摘要:Trottier J, Białek A, Caron P, Straka RJ, Milkiewicz P, Barbier O. Profiling Circulating and Urinary Bile Acids in Patients with Biliary Obstruction before and after Biliary Stenting. PLoS ONE. 2011 Jul 08;6(7):e22094. doi: 10.1371/journal.pone.0022094. 参考文献:10.1152/ajpgi.00483.2010 摘要:Seyhun E, Malo A, Schäfer C, Moskaluk CA, Hoffmann R, Göke B, Kubisch CH. Tauroursodeoxycholic acid reduces endoplasmic reticulum stress, acinar cell damage, and systemic inflammation in acute pancreatitis. American Journal of Physiology-Gastrointestinal and Liver Physiology. 2011 Nov;301(5):G773–82. doi: 10.1152/ajpgi.00483.2010.