📜7-Acetonyltheophyllin置于乙醇,镍体系中,100.0~120.0 °C,8.83 Mpa 条件下,反应生成 羟丙茶碱 参考文献:Zelnik Et Al.,Bulletin De La Societe Chimique De France,1956,P. 1773,1775 标题:Zelnik Et Al.,Bulletin De La Societe Chimique De France,1956,P. 1773,1775
专利号:US-7173021-B2 优先权日:2004-09-02 标题:Synthesis of temozolomide esters as potent anticancer pro-drugs for topical and transdermal applications in treatments of cancers 发明人:WANG YONGFENG; CONWAY BARBARA R; SUPPASANSATORN PANASSAYA 权利人:TIANJIN NORTH PHARM SCI TECH C 摘要:This invention relates to the use of temozolomide esters (4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylate esters) Formula 1 as potent anticancer pro-drugs for treatment of cancers by topical and transdermal applications, and to a novel process for synthesis of temozolomide esters by a direct esterification of temozolomide acid (3,4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylic acid) with a halogeno-aliphatic compound in presence of a base, or with an alcohol in presence of a dehydrate agent
专利号:EP-1334714-B1 优先权日:2002-02-07 标 题:Use of ascorbic acid to stergthen the dermal-epidermal junction 发明人:BERNERD FRANCOISE 权利人:OREAL 摘要:Cosmetic use of a composition (A), comprising ascorbic acid or its analog (I) in a cosmetic medium, is claimed for improving the cohesion of the epidermis-dermis junction, promoting the synthesis of tenascin and/or promoting the synthesis of type VII collagen. Independent claims are included for: (i) use of (I) for the production of a pharmaceutical (specifically dermatological) composition (B) for treating disorders associated with deficiency in cohesion of the epidermis-dermis junction, synthesis of tenascin and/or synthesis of type VII collagen; and (ii) use of (I) in the culture medium for reconstructed skin, for improving the cohesion of the epidermis-dermis junction in the reconstructed skin.
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.
专利号:US-2004005342-A1 优先权日:2002-02-07 标题 :Topical administration of ascorbic acid to reinforce the cohesion of the dermo-epidermal junction 发明人:BERNERD FRANCOISE 权利人:OREAL 摘要:The present invention relates to the pharmaceutical or cosmetic use of a composition comprising, in a pharmaceutically or cosmetically acceptable medium, ascorbic acid or an analogue thereof to reinforce the cohesion of the dermo-epidermal junction. n The invention also relates to the pharmaceutical or cosmetic use of a composition comprising, in a pharmaceutically or cosmetically acceptable medium, ascorbic acid or an analogue thereof to increase the synthesis of tenascin and/or collagen VII. n The invention also relates to the use of ascorbic acid or of an analogue thereof to reinforce the cohesion of the dermo-epidermal junction of reconstructed skins.
专利号:CN-110184247-A 优先权日:2019-05-09 标题 :Alfalfa melatonin synthesis gene MsASMT and its application in regulating the synthesis of melatonin and flavonoids in plants
专利号:EP-1541127-B1 优先权日:2003-12-10 标题 :Use of modulators of aquaglyceroporins as slimming agents 发明人:CALS-GRIERSON MARIE-MADELEINE 权利人:OREAL 摘要:Adipose aquaglyceroporin (AQPap) modulators that stimulate the AQPap activity of adipocytes are used in cosmetic compositions as slimming agents for reducing the volume of adipocytes, are new. Independent claims are also included for: (1) cosmetic composition comprising an adipose aquaglyceroporin modulator as above and a lipolytic agent; (2) use of escin, proanthocyanidins, diosgenin and ginkgo extracts for modulating the aquaglyceroporins of adipose tissue. ACTIVITY : Anorectic. No biological data given. MECHANISM OF ACTION : Adipose aquaglyceroporin modulator; phosphodiesterase inhibitor; alpha -2 receptor inhibitors, neuropeptide Y inhibitors, LDL or VLDL receptor synthesis inhibitors, beta receptor activators, G-protein activators, glucose transport blockers, adenylcyclase activator. No biological data given.
1: Borowiecki P, Paprocki D, Dudzik A, Plenkiewicz J. Chemoenzymatic Synthesis of Proxyphylline Enantiomers. J Org Chem. 2016 Jan 15;81(2):380-95. doi: 10.1021/acs.joc.5b01840. Epub 2016 Jan 6. doi: 10.1016/j.ijpharm.2012.01.056. Epub 2012 Feb 6.
合成参考文献
摘要:Drugs in Japan, -(1178), 1995 摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664 参考文献:10.1021/jm980469t 摘要:Cavallaro RA, Filocamo L, Galuppi A, Galione A, Brufani M, Genazzani AA. Potentiation of cADPR-induced Ca(2+)-release by methylxanthine analogues. J Med Chem. 1999 Jul 15;42(14):2527–34. doi: 10.1021/jm980469t.