5-aminoethanoylsalicylic acid | 19834-23-2

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 5-aminoethanoylsalicylic acid
• 英文别名: 5-aminoacetylsalicylic acid；5-Glycyl-2-hydroxybenzoic acid；5-(2-aminoacetyl)-2-hydroxybenzoic acid
• CAS: 19834-23-2
• 化学式: C₉H₉NO₄
• 分子量: 195.175
• InChiKey: DJZRSPASHYGCDS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  101
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• ENHANCED ANTI-INFLUENZA AGENTS CONJUGATED WITH ANTI-INFLAMMATORY ACTIVITY
  申请人：ACADEMIA SINICA

  公开号：US20130274229A1

  公开（公告）日：2013-10-17

  Novel dual-targeted, bifunctional anti-influenza drugs formed by conjugation with anti-inflammatory agents are disclosed. Exemplary drugs according to the invention include caffeic acid (CA)-bearing zanamivir (ZA) conjugates ZA-7-CA (1), ZA-7-CA-amide (7) and ZA-7-Nap (43) for simultaneous inhibition of influenza virus neuraminidase and suppression of proinflammatory cytokines. Synthetic methods for preparation of these enhanced anti-influenza conjugate drugs are provided. The synthetic bifunctional ZA conjugates act synergistically towards protection of mice lethally infected by H1N1 or H5N1 influenza viruses. The efficacy of ZA-7-CA, ZA-7-CA-amide and ZA-7-Nap conjugates is much greater than the combination therapy of ZA with anti-inflammatory agents.

  新型双靶向、双功能抗流感药物通过与抗炎药物结合形成。根据本发明的示例药物包括咖啡酸（CA）基底的扎那米韦（ZA）共轭物ZA-7-CA（1）、ZA-7-CA酰胺（7）和ZA-7-Nap（43），用于同时抑制流感病毒神经氨基酸酶和抑制促炎细胞因子。提供了用于制备这些增强型抗流感共轭药物的合成方法。合成的双功能ZA共轭物对保护由H1N1或H5N1流感病毒致命感染的小鼠具有协同作用。ZA-7-CA、ZA-7-CA酰胺和ZA-7-Nap共轭物的疗效远远优于ZA与抗炎药物的联合治疗。
• [EN] CYCLOOXYGENASE-2 INHIBITORS<br/>[FR] INHIBITEURS DE CYCLOOXIGENASE-2
  申请人：NICOX SA

  公开号：WO2004000300A1

  公开（公告）日：2003-12-31

  Use of compounds of formula (I) or salts thereof for the preparation of COX-2 inhibitor drugs: R-T1-B-Cc0-N(O)s (formula I), for the treatment and/or prophylaxis of inflammatory processes.

  使用式(I)的化合物或其盐，制备COX-2抑制剂药物：R-T1-B-Cc0-N(O)s（式I），用于治疗和/或预防炎症过程。
• [EN] MACROLIDE-CONJUGATES WITH ANTI-INFLAMMATORY ACTIVITY<br/>[FR] CONJUGUES MACROLIDES A ACTIVITE ANTI-INFLAMMATOIRE
  申请人：PLIVA PHARMACEUTICAL INDUSTRY

  公开号：WO2004094449A1

  公开（公告）日：2004-11-04

  The present invention relates to new compounds represented by Formula (I); wherein M represents a macrolide subunit of the substructure II, Formula (II); L represents the chain of the substructure III, Formula (III); D represents the steroid or nonsteroidal subunit derived from steroid or nonsteroidal (NSAID) drugs with anti-inflammatory activity. The present invention relates also to pharmaceutically acceptable salts and solvates of such prepared compounds, to processe and intermediates for their preparation, as well as to the improved therapeutic action and the use in the treatment of inflammatory diseases and conditions in humans and animals.

  本发明涉及由式（I）表示的新化合物；其中M表示亚结构II，式（II）的大环内酯亚基；L表示亚结构III，式（III）的链；D表示从类固醇或非类固醇（NSAID）药物中衍生的类固醇或非类固醇亚基，具有抗炎活性。本发明还涉及制备这些化合物的药学上可接受的盐和溶剂化物，以及用于它们的制备的过程和中间体，以及在人类和动物的炎症性疾病和病况的治疗中的改进治疗作用和用途。
• [EN] PHENOL DERIVATIVES<br/>[FR] DERIVES DE PHENOL
  申请人：NICOX SA

  公开号：WO2006015930A1

  公开（公告）日：2006-02-16

  The present invention relates to the use of a compound of the general formula (I): wherein: n is an integer from 1 to 20; R is H, an halogen atom, a linear or branched (C1-C10)- alkoxy group, an hydroxy group, -CF3, -NHR' wherein R' is H or a linear or branched (C1-C10)-alkyl; or a salt thereof for treating inflammatory disease states or disorders, cardiovascular and/or peripheral vascular diseases.

  本发明涉及使用一般式(I)的化合物，其中：n为1至20的整数；R为H、卤素原子、线性或支链(C1-C10)烷氧基、羟基、-CF3、-NHR'，其中R'为H或线性或支链(C1-C10)烷基；或其盐，用于治疗炎性疾病状态或紊乱、心血管和/或外周血管疾病。
• Pharmaceutical compounds
  申请人：Soldato Del Piero

  公开号：US20050261242A1

  公开（公告）日：2005-11-24

  Compounds or their salts having general formula: A-B—C—NO 2 wherein: A is a drug radical; B is a linker; and C is a bivalent radical.

  化合物或其盐的一般式为：A-B-C-NO2，其中：A是药物基团；B是连接剂；C是双价基团。