[EN] SULFONAMIDE COMPOUNDS HAVING TNAP INHIBITORY ACTIVITY<br/>[FR] COMPOSÉS DE SULFONAMIDE AYANT UNE ACTIVITÉ INHIBITRICE DE TNAP
申请人:DAIICHI SANKYO CO LTD
公开号:WO2018119444A1
公开(公告)日:2018-06-28
The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I) or a pharmacologically acceptable salt thereof.
Asymmetric Syntheses of All Stereoisomers of 3-Hydroxyproline; A Constituent of Several Bioactive Compounds
作者:Srivari Chandrasekhar、Togapur Kumar
DOI:10.1055/s-0032-1316734
日期:——
3-hydroxyproline, and its derivatives have been achieved enantioselectively by employing Sharpless asymmetric epoxidation and reductive cyclization as the key steps. Synthesis of an unusual β-hydroxy-α-amino acid, 3-hydroxyproline, and its derivatives have been achieved enantioselectively by employing Sharpless asymmetric epoxidation and reductive cyclization as the key steps.
Water-Soluble Calix[4]resorcinarenes with Hydroxyproline Groups as Chiral NMR Solvating Agents
作者:Courtney M. O'Farrell、J. Matthew Chudomel、Jan M. Collins、Catherine F. Dignam、Thomas J. Wenzel
DOI:10.1021/jo702751z
日期:2008.4.1
associate within the cavity of the calix[4]resorcinarenes, as do naphthyl rings with mono-, 2,3-, and 1,8-substitution patterns. Anthracene derivatives with an amino or sulfonyl group at the 1-position bind within the cavity, as well. Aromatic resonances of the substrates exhibit substantial upfield shifts because of shielding from the aromatic rings of the calix[4]resorcinarene. The effectiveness of the reagents
水溶性杯[4]间苯二甲酰基芳烃,其含有3-和4-羟基脯氨酸,d-庚酸,(S)-2-(甲氧基甲基)吡咯烷,(S)-2-吡咯烷甲醇和(S,S合成)-(+)-2,4-双(甲氧基甲基)吡咯烷取代基并作为手性NMR溶剂化剂进行评估。具有羟基脯氨酸基团的衍生物在引起具有吡啶基,苯基和双环芳族环的水溶性阳离子和阴离子化合物的光谱中,特别有效地引起对映体鉴别。结合研究表明,杯状[4]间苯二芳烃腔内单和邻位取代的苯环与具有单,2、3-和1,8取代模式的萘环一样缔合。在1-位具有氨基或磺酰基的蒽衍生物也结合在空腔内。由于与杯[4]间苯二芳烃的芳环相屏蔽,所以底物的芳族共振表现出明显的高场偏移。该试剂在产生手性识别中的有效性。用扁桃酸钠,色氨酸钠盐和琥珀酸多西拉敏证明了1 H NMR光谱。虽然没有一种试剂始终是最有效的,但是带有反式-4-羟基脯氨酸和反式-3-羟基脯氨酸部分的杯[4]间苯二碳烯芳烃通常在底物的1
EP3643703
申请人:——
公开号:——
公开(公告)日:——
5-aminomethylquinoxaline-2,3-diones. Part I: A novel class of AMPA receptor antagonists
作者:Yves P Auberson、Serge Bischoff、Robert Moretti、Markus Schmutz、Siem J Veenstra
DOI:10.1016/s0960-894x(97)10186-x
日期:1998.1
A series of 5-aminomethylquinoxaline-2,3-diones have been identified as potent and selective AMPA antagonists. Some of these compounds are also active at the glycine-binding site of the NMDA receptors. A number of these novel, water-soluble quinoxaline-2,3-dione derivatives display protective effects in the electroshock-induced convulsion model in mice. (C) 1997 Elsevier Science Ltd. All rights reserved.