专利号:US-7605241-B2 优先权日:2005-01-10 标题 :Synthesis of inhibitors of p90Rsk 发明人:HECHT SIDNEY M; MALONEY DAVID J 权利人:UNIV VIRGINIA 摘要:The synthesis of the naturally occurring kaempferol glycoside SLO1O1-1, as well as analogs thereof, has been accomplished, as has its biochemical evaluation. SLO1O1-1 exhibits selective and potent p90 Rsk inhibitory activity at nanomolar concentrations without inhibiting the function of upstream kinases such as MEK, Raf, or PKC. The synthetic scheme of the invention verified the structural assignment of the natural product and has provided access to material sufficient for detailed biological evaluation.
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-2017268027-A1 优先权日:2014-12-22 标题:Method for synthesis of fatty acids 发明人:CESCUT JULIEN; URIBELARREA JEAN-LOUIS; GUILLOUET STEPHANE; MOLINA-JOUVE CAROLE; SAGNAK RANA 权利人:INST NAT DES SCIENCES APPLIQUEES DE TOULOUSE; CENTRE NAT RECH SCIENT; AGRONOMIQUE INST NAT RECH; FIDOP (FONDS DE DEV DES FILIERES DES OLEAGINEUX ET DES PROTEAGINEUX) 摘要:Disclosed is a method for synthesis of fatty acids by culturing a eukaryotic microorganism from the fungi kingdom, that is naturally oleaginous or rendered oleaginous. The culture is performed in the presence a fatty acid synthase inhibitor in the culture medium.
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-2008287407-A1 优先权日:2003-12-10 标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use 发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
参考文献:10.1016/j.phytochem.2006.05.015 摘要:Logendra S, Ribnicky DM, Yang H, Poulev A, Ma J, Kennelly EJ, Raskin I. Bioassay-guided isolation of aldose reductase inhibitors from Artemisia dracunculus. Phytochemistry. 2006 Jul;67(14):1539–46. doi: 10.1016/j.phytochem.2006.05.015.