CAS: 21187-98-4; 1-(Hexahydrocyclopenta[c]Pyrrol-2(1H)-yl)-3-[(4-Methylphenyl)Sulfonyl]Urea

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CAS号70-55-3 对甲苯磺酰胺 | CAS号58108-05-7 N-氨基-3-氮杂双环[3.3...

N-[n-(Hexahydrocyclopenta[c]Pyrrol-2(1H)-yl)-N'-Hydroxycarbamimidoyl]-4-Methylbenzenesulfonamide置于simulated Gastric Fluid体系中,化学反应 2.0H,反应生成格列齐特
参考文献:Synthesis And Characterization Of Novel Oxime Prodrug Of Gliclizide
标题:Synthesis And Characterization Of Novel Oxime Prodrug Of Gliclizide
摘要:糖尿病已成为全球主要的医疗问题.格列齐特是一种广泛使用的磺酰脲类化合物,用于治疗糖尿病.格列齐特属于生物药物分类系统的ⅱ类药物,其溶解度较差.具有限制水溶性的药物分子在以发现为重点的制药公司的研发组合中变得越来越普遍.前药是一种已确立的概念,用于克服如溶解度差等障碍.水溶性是提高药物生物利用度的重要参数.因此,本研究旨在通过合成格列齐特的新型肟前药来增强水溶性,从而提高生物利用度.所制备的前药通过红外光谱(ir),核磁共振(NMR),质谱(mass)和差示扫描量热法(dsc)进行了表征.体外化学水解分析表明,合成的格列齐特肟类衍生物在模拟胃液ph 1.2中具有化学稳定性.Log P值的降低表明合成的格列齐特肟类衍生物的亲水性增强.
Doi:10.14233/ajchem.2014.17642

专利信息

专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

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-9556123-B2
优先权日:2004-07-19
标题:Synthesis of triethylenetetramines
发明人：JONAS MARCO; VAULONT IRENE; SOI ANTONIO; SCHMIDT GUNTHER
权利人:PHILERA NEW ZEALAND LTD
摘要:Methods and intermediates for synthesizing triethylenetetramine and salts thereof, as well as novel triethylenetetramine salts and their crystal structure, and triethylenetetramine salts of high purity.

专利号:US-2025223262-A1
优先权日:2022-03-31
标 题 :Synthesis of morphinans with reduced herg activity and mop binding
发明人：LAMMERT ECKHARD; SCHOLZ OKKA; OTTER SILKE; HEREBIAN DIRAN; HOFFMANN TORSTEN; SANZ MIGUEL ANGEL; KRAMP LAURENZ; LEVY LAURA MARIANA; HRISTEVA STANIMIRA
权利人:HEINRICH HEINE UNIV DUESSELDORF; DEUTSCHE DIABETES FORSCHUNGSGESELLSCHAFT E V; TAROS CHEMICALS GMBH & CO KG
摘要:The invention relates to morphinan-derivatives, processes for their preparation, medicaments containing them and the use of these morphinan-derivatives for the preparation of medicaments.

专利号:US-7956214-B2
优先权日:2001-11-02
标题 :Process for the preparation of aniline-derived thyroid receptor ligands
发明人：CHIDAMBARAM RAMAKRISHNAN; KANT JOYDEEP; WEAVER RAYMOND E; YU JURONG; GHOSH ARUN
权利人:KAROBIO AB; BRISTOL MYERS SQUIBB CO
摘要:Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.

专利号:WO-2005105153-A1
优先权日:2004-04-30
标 题 :Hydroxyalkyl derivatives of biologically active compounds
发明人：DESHPANDE JAYANT VENKATESH; KADAM VAISHALI MADHUKAR; GUPTE VANDANA SANDEEP; RANBHAN KAMLESH JAYANTILAL
权利人:KOPRAN RES LAB LTD; DESHPANDE JAYANT VENKATESH; KADAM VAISHALI MADHUKAR; GUPTE VANDANA SANDEEP; RANBHAN KAMLESH JAYANTILAL
摘要:Hydroxyalkyl derivatives of biologically active compounds represented by the formula VII wherein R2 = H, CI-12 alkyl, C6-12 aryl, or -OH and D = Biologically active agent having functional groups such as Formula (a) epoxy or aziridine and Z' = Formula (b) L= spacer comprising (un)substituted alkyl, hydroxyalkyl or alkoxy alkyl with the condition that the carbon chain length contains 2 to 6 carbon atoms when Z' = Formula (c) and pharmaceutically acceptable acid addition salts and enantiomers thereof Also process for the synthesis of compounds of the Formula VII and pharmaceutically acceptable acid addition salts and enantiomers thereof comprising condensation of the biologically active agents having functional groups such as Formula (d) epoxy or azifidine with substituted alkyl derivatives under alkaline conditions, at 20 - 80°C, in an organic solvent.