CAS: 652-37-9; 2-(1,3-Dimethyl-2,6-Dioxo-1,2,3,6-Tetrahydro-7H-Purin-7-yl)Acetic Acid

上下游产品

多索茶碱杂质29 Ethyl 2-(1,3-Dimethyl-2,6-Dioxo-2,3-Dihydro-1H-Purin-7(6H)-yl)Acetate 7029-96-1
茶碱 Theophylline 58-55-9

茶碱置于lithium Hydroxide Monohydrate,Potassium Carbonate体系中,用 四氢呋喃,水,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 14.0H,反应生成 茶碱乙酸
参考文献:茶碱的设计,合成和生物学评估,其中含有作为α-淀粉酶抑制剂的乙炔衍生物.
标题:茶碱的设计,合成和生物学评估,其中含有作为α-淀粉酶抑制剂的乙炔衍生物.
摘要:利用基于片段的药物设计方法构建了具有茶碱和乙炔部分的新型药效团,设计并合成了二十多种含茶碱的乙炔共轭物,并通过基于酶的体外α-淀粉酶抑制活性对所有化合物进行了评价.在体外评价表明大多数化合物表现出非常好的抑制活性,以及它们之间9个类似物13-15,20,21和24-27分别显示出更多或几乎与ic等效抑制活性50与标准阿卡波糖1.37+/-0.26μm相比,值分别为1.11+/-0.07,1.14+/-0.17,1.07+/-0.01和1.21+/-0.03,1.33+/-0.09,1.17+/-0.01,1.05+/-0.02,1.61+/-0.04,1.02+/-0.03μm.此外,进行分子对接模拟研究以鉴定合成的类似物在α-淀粉酶(pbd Id:4Gqr)的结合位点的相互作用和结合模式.在合成的类似物中,基于α-淀粉酶抑制活性选择了两种化合物25和27,并通过高脂饮食-链脲佐菌素(hfd-Stz)模型对正常大鼠的体内抗糖尿病活性进行了评估.剂量为10
DOI:10.1016/j.Bioorg.2019.103120

专利信息

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

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:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人：MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

专利号:EP-0658564-B1
优先权日:1986-04-30
标题 :Electroluminescent compounds and intermediates in their synthesis
发明人：MASSEY RICHARD J; POWELL MICHAEL J; MIED PAUL A; POONIAN MOHINDAR S; FENG PETER; CIANA LEOPOLDO DELLA; DRESSICK WALTER J
权利人:IGEN INT INC
摘要:Novel compounds for use in electrochemiluminescent assays and characterised by containing the structure        X - Y - ZwhereinX represents one or more nucleotides which may be the same or different, one or more amino acids which may be the same or different, an antibody, an analyte of interest or an analogue of an analyte of interestY represents a linker group attached to X and Z,andZ represents an electrochemiluminescent moiety, and intermediates employed in their synthesis.

专利号:US-10814013-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications