专利号:US-5043328-A 优先权日:1986-05-09 标 题 :Formulations containing unsaturated fatty acids for the synthesis of prostaglandins and hydroxy-fatty acids in biological systems 发明人:WEITHMANN KLAUS U 权利人:HOECHST AG 摘要:The present invention relates to formulations containing unsaturated fatty acids for the synthesis of prostaglandins and hydroxy-fatty acids in biological systems and to the use of such formulations for the preparation of medicaments which are suitable for curing prostaglandin deficiencies in humans or animal, for example healing or preventing diseases of the gastro-intestinal tract.
专利号:US-7598291-B2 优先权日:2004-09-02 标题 :Methods and compositions for enhancing collagen and proteoglycan synthesis in the skin 发明人:NIMNI MARCEL; HAN BO 权利人:NIMNI MARCEL; HAN BO 摘要:A composition for application to the skin can stimulate the in vivo synthesis of collagen and proteoglycans and improve the appearance of the skin, increasing its elasticity and fullness. In general, a composition according to the present invention comprises: (1) an antioxidant compound in a quantity sufficient to enhance collagen synthesis in the skin; (2) an organic penetrant in which the antioxidant compound is soluble in a sufficient quantity that a concentration of the antioxidant compound sufficient to enhance collagen synthesis can be applied topically and penetrate the skin; (3) a mixture of essential amino acids; (4) a supplemental source of sulfur; and (5) a topical pharmaceutically acceptable carrier. The antioxidant compound can be lipoic acid, a lipoic acid analogue or derivative, a bioflavonoid, a constituent of ginkgo, or an isoflavone. The organic penetrant is preferably benzyl alcohol. Other ingredients, such as esters of tocopherol and ascorbic acid, can be included.
专利号:US-2010160244-A1 优先权日:2004-09-02 标 题 :Methods and compositions for enhancing collagen, proteoglycan, and glutathione synthesis in the skin 发明人:NIMNI MARCEL; HAN BO 权利人:NIMNI MARCEL; HAN BO 摘要:A composition for application to the skin can stimulate the in vivo synthesis of collagen and proteoglycans and improve the appearance of the skin, increasing its elasticity and fullness. In general, a composition according to the present invention comprises: (1) an antioxidant compound in a quantity sufficient to enhance collagen synthesis in the skin; (2) an organic penetrant in which the antioxidant compound is soluble in a sufficient quantity that a concentration of the antioxidant compound sufficient to enhance collagen synthesis can be applied topically and penetrate the skin; (3) a mixture of essential amino acids or hydrolyzed whey protein; (4) a supplemental source of sulfur; and (5) a topical pharmaceutically acceptable carrier. The antioxidant compound can be lipoic acid or a lipoic acid analogue or derivative. The organic penetrant is preferably benzyl alcohol. Other ingredients, such as esters of tocopherol and ascorbic acid, can be included.
专利号:US-12129222-B2 优先权日:2016-08-11 标题:Production of bitter principle derivatives 发明人:WYRWA RALF; RODE CLAUDIA; SEEMANN THOMAS; MEINEL LORENZ; RITZER JENNIFER; SCHNABELRAUCH MATTHIAS 权利人:UNIV WUERZBURG J MAXIMILIANS; JULIUS MAXIMILIANS UNIV 摘要:It is an object of the present invention to introduce carboxylic acid-functionalities suitable for coupling into the denatonium structure by means of simple synthesis, namely the synthesis of bitter principle derivatives based on the denatonium structure according to formula 1:For example, according to the invention, lidocaine derivatives may be reacted with carboxylated benzyl halogenides. The carboxylated denatonium derivatives of the present invention are especially applied in medicine, biology, medical engineering as well as cosmetics, the pharmaceutical, chemical, and foodstuff industry.
专利号:US-2002165207-A1 优先权日:2001-05-02 标题 :Compositions and methods for the treatment of diabetic neuropathy 发明人:ROSENBLOOM RICHARD 摘要:Compositions and a method for the treatment of diabetic neuropathy is disclosed. The compositions comprise a mixture of a compound that promotes synthesis of nerve growth factor, an aldose reductase inhibitor and an antioxidant, optionally formulated in a pharmaceutically acceptable carrier. This combination of active agents provides significant, effective relief of the symptoms of diabetic neuropathy, as well as at least partial recovery of lost neurological function in some cases. In addition, the compositions of the present invention, when used in effective amounts to treat diabetic neuropathy, do not exhibit the severe side effects of many prior art compositions proposed for treatment of this ailment. n In a second aspect, a method for the administration of a composition in accordance with the present invention for the treatment of diabetic neuropathy is disclosed. In the method, an effective amount of the composition of the invention is administered on a regular basis over a period of time sufficient to provide the beneficial effects of relief from the symptoms of diabetic neuropathy, as well as at least some recovery of the damaged nerve tissues.
专利号:US-2006115880-A1 优先权日:2002-12-03 标 题 :Enzymatic production of acyl flavonoid derivatives 发明人:GHOUL MOHAMED; ENGASSER JEAN-MARC; MOUSSOU PHILIPPE; PAULY GILLES; ARDHAOUI MELIKA; FALCIMAIGNE AUDE 权利人:COGNIS FRANCE SA 摘要:Disclosed is a method for enzymatic synthesis of esters of flavonoid and flavonoid derivatives, according to which a reaction medium containing an organic solvent, a glycosylated flavonoid or aglycon flavonoid, an acyl group donor, and an enzymatic catalyst is produced, b) additional quantities of flavonoid and/or acyl donor are optionally added during the reaction, and c) the obtained esters are separated from the enzymatic particles and the solvent. The inventive method is characterized by maintaining the concentration of water and/or alcohol which are formed during the reaction to below 150 mM. Advantageously, the molar ratio of flavonoid to acyl donor in the reaction medium is maintained in the range from 0.01 to 20.00 during the reaction.
1: Bharti S, Rani N, Krishnamurthy B, Arya DS. Preclinical evidence for the pharmacological actions of naringin: a review. Planta Med. 2014 Apr;80(6):437-51. doi: 10.1055/s-0034-1368351. Epub 2014 Apr 7. Review. Chinese. doi: 10.1371/journal.pone.0143868. eCollection 2015. 4: Yin FM, Xiao LB, Zhang Y. [Research progress on Drynaria fortunei naringin on inflammation and bone activity]. Zhongguo Gu Shang. 2015 Feb;28(2):182-6. Review. Chinese. doi: 10.1007/s11010-015-2525-9. Epub 2015 Aug 18. doi: 10.1016/j.etap.2015.02.021. Epub 2015 Mar 7. doi: 10.1016/j.pupt.2015.07.002. Epub 2015 Jul 10. doi: 10.3892/ijo.2015.3095. Epub 2015 Jul 20. doi: 10.1007/s10753-014-9994-y. doi: 10.1016/j.cbi.2015.10.010. Epub 2015 Oct 19. doi: 10.3892/mmr.2015.4232. Epub 2015 Aug 20. doi: 10.3892/mmr.2015.3996. Epub 2015 Jun 24. doi: 10.3109/03639045.2014.925918. Epub 2014 Jun 11. doi: 10.1159/000430319. Epub 2015 Jul 10. doi: 10.1016/j.colsurfb.2013.11.006. Epub 2013 Nov 15. doi: 10.1007/s12026-015-8665-x. doi: 10.1007/s10571-015-0201-y. Epub 2015 May 5. doi: 10.1016/j.bbrc.2014.08.117. Epub 2014 Aug 30. doi: 10.3109/0886022X.2015.1074462. Epub 2015 Sep 3. doi: 10.2147/DDDT.S52714. eCollection 2014.
合成参考文献
摘要:Xiong Y, Wang GF, Zhang JY, Wu SY, Xu W, Zhang JJ, Wu SG, Rao JJ. [Naringin inhibits monocyte adhesion to high glucose-induced human umbilical vein endothelial cells]. Nan Fang Yi Ke Da Xue Xue Bao. 2010 Feb;30(2):321–5. 参考文献:10.3390/ijms12063422 摘要:Hendra R, Ahmad S, Sukari A, Shukor MY, Oskoueian E. Flavonoid analyses and antimicrobial activity of various parts of Phaleria macrocarpa (Scheff.) Boerl fruit. Int J Mol Sci. 2011;12(6):3422–31. 参考文献:10.1186/1471-230x-11-81 摘要:Wu H, Jing Z, Tang X, Wang X, Zhang S, Yu Y, Wang Z, Cao H, Huang L, Yu Y, Wang Y. To compare the efficacy of two kinds of Zhizhu pills in the treatment of functional dyspepsia of spleen-deficiency and qi-stagnation syndrome: a randomized group sequential comparative trial. BMC Gastroenterol. 2011 Jul 15;11():81. 参考文献:10.1016/j.archoralbio.2011.06.008 摘要:Chen LL, Lei LH, Ding PH, Tang Q, Wu YM. Osteogenic effect of Drynariae rhizoma extracts and Naringin on MC3T3-E1 cells and an induced rat alveolar bone resorption model. Arch Oral Biol. 2011 Dec;56(12):1655–62. doi: 10.1016/j.archoralbio.2011.06.008. 参考文献:10.1371/journal.pone.0021781 摘要:Kim Y, Hollenbaugh JA, Kim D, Kim B. Novel PI3K/Akt Inhibitors Screened by the Cytoprotective Function of Human Immunodeficiency Virus Type 1 Tat. PLoS ONE. 2011 Jul 12;6(7):e21781. doi: 10.1371/journal.pone.0021781.