5-(Ethyl phosphono).3-carboxy-1,2,3,4-tetrahydroisoquinoline | 129682-89-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 四氢异喹啉
• 英文名称: 5-(Ethyl phosphono).3-carboxy-1,2,3,4-tetrahydroisoquinoline
• 英文别名: 5-[Ethoxy(hydroxy)phosphoryl]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
• CAS: 129682-89-9
• 化学式: C₁₂H₁₆NO₅P
• 分子量: 285.236
• InChiKey: KOFSFJYKXNRFNJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.4
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  95.9
• 氢给体数：
  3
• 氢受体数：
  6

文献信息

• Phosphono-hydroisoquinoline compounds useful in reducing neurotoxic injury
  申请人：G.D. Searle & Co.

  公开号：EP0364996A2

  公开（公告）日：1990-04-25

  A class of phosphono-hydroisoquinoline compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a phosphono-hydroisoquinoline compound alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of Formula 1: wherein each of R' through R4 is hydrido, wherein each of Z1 and Z2 is hydroxyl, wherein W is a single bond connecting the phosphorus atom with the aromatic ring and wherein the A ring is aromatic. Also disclosed are two classes of intermediate compounds having a fully unsaturated A ring, which intermediate compounds are useful in methods to make product compounds of Formula I.

  描述了一类膦酰基氢化异喹啉化合物，用于治疗减少与缺氧或缺血相关的神经毒性损伤，缺氧或缺血通常发生在中风、心脏骤停或围产期窒息之后。治疗方法包括单独施用或在组合物中施用膦酰基氢化异喹啉化合物，施用量应能有效地作为拮抗剂抑制主要神经元兴奋性氨基酸受体部位的兴奋毒性作用。最令人感兴趣的化合物是式 1： 其中，R'到 R4 中的每一个都是氢基，Z1 和 Z2 中的每一个都是羟基，W 是连接磷原子和芳香环的单键，A 环是芳香环。还公开了两类具有完全不饱和 A 环的中间体化合物，这些中间体化合物在制造式 I 产品化合物的方法中是有用的。
• PROBENECID FOR USE IN TREATING EPILEPTIC DISEASES, DISORDERS OR CONDITIONS
  申请人：Paris Sciences et Lettres - Quartier Latin

  公开号：EP3651758A1

  公开（公告）日：2020-05-20
• US4997821A
  申请人：——

  公开号：US4997821A

  公开（公告）日：1991-03-05
• [EN] PROBENECID FOR USE IN TREATING EPILEPTIC DISEASES, DISORDERS OR CONDITIONS<br/>[FR] PROBÉNÉCIDE POUR UTILISATION DANS LE TRAITEMENT DE MALADIES, TROUBLES OU AFFECTIONS ÉPILEPTIQUES
  申请人：PARIS SCIENCES LETTRES QUARTIER LATIN

  公开号：WO2019012109A1

  公开（公告）日：2019-01-17

  The present invention relates to probenecid or a pharmaceutical acceptable salt thereof for use in the treatment of a neurological disorder in a subject in need thereof, wherein administration of probenecid or a pharmaceutical acceptable salt thereof controls clinical or electrographic seizures in said subject. Preferably, said neurological disorder is an epileptic disease, disorder or condition.