4-isopropyl-8-(2,4,6-trimethylphenylamino)-2H-phthalazin-1-one | 1072157-22-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 4-isopropyl-8-(2,4,6-trimethylphenylamino)-2H-phthalazin-1-one
• 英文别名: 4-propan-2-yl-8-(2,4,6-trimethylanilino)-2H-phthalazin-1-one
• CAS: 1072157-22-2
• 化学式: C₂₀H₂₃N₃O
• 分子量: 321.422
• InChiKey: RSIURMDISUBNRV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  24
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  53.5
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• Treatment of familial exudative vitreoretinopathy through S1PR2 inhibition
  申请人：DALHOUSIE UNIVERSITY

  公开号：US10058543B2

  公开（公告）日：2018-08-28

  Methods and compositions are provided for the treatment of familial exudative vitreoretinopathy (FEVR) and retinopathy of prematurity (ROP) through the administration of a therapeutically effective amount of a Sphingosine-1-phosphate receptor type 2 (S1PR2) inhibitor.

  本研究提供了通过施用治疗有效量的2型磷酸肾上腺素受体（S1PR2）抑制剂来治疗家族性渗出性玻璃体视网膜病变（FEVR）和早产儿视网膜病变（ROP）的方法和组合物。
• S1PR2 antagonists and uses therefor
  申请人：DALHOUSIE UNIVERSITY

  公开号：US10487082B2

  公开（公告）日：2019-11-26

  Methods and compositions are provided for the treatment of familial exudative vitreoretinopathy (FEVR) through the administration of a therapeutically effective amount of a sphingosine-1-phosphate receptor type 2 (S1PR2) antagonist. Also provided herein are (Z)-3-((2,6-dichloropyridin-4-yl)amino)-3-(((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)amino)acrylonitrile and analogs thereof, and their use in treating retinopathies and diseases characterized by insufficient angiogenesis.

  本文提供了通过施用治疗有效量的鞘氨醇-1-磷酸受体 2 型（S1PR2）拮抗剂治疗家族性渗出性玻璃体视网膜病变（FEVR）的方法和组合物。本文还提供了(Z)-3-((2,6-二氯吡啶-4-基)氨基)-3-(((4-异丙基-1,3-二甲基-1H-吡唑并[3,4-b]吡啶-6-基)甲基)氨基)丙烯腈及其类似物，以及它们在治疗视网膜病变和以血管生成不足为特征的疾病中的用途。
• TREATMENT OF FAMILIAL EXUDATIVE VITREORETINOPATHY THROUGH S1PR2 INHIBITION
  申请人：Dalhousie University

  公开号：EP3148550A1

  公开（公告）日：2017-04-05
• S1PR2 ANTAGONISTS AND USES THEREFOR
  申请人：Dalhousie University

  公开号：US20180141942A1

  公开（公告）日：2018-05-24

  Methods and compositions are provided for the treatment of familial exudative vitreoretinopathy (FEVR) through the administration of a therapeutically effective amount of a sphingosine-1-phosphate receptor type 2 (S1PR2) antagonist. Also provided herein are compounds which contain bioisosteric replacements of the urea group of JTE-013 and analogs thereof, and their use in treating retinopathies and diseases characterized by insufficient angiogenesis.
• [EN] BLOCKERS OF THE NOGO-A S1PR PATHWAY FOR THE TREATMENT OF DISEASES CHARACTERIZED BY NEURONAL DAMAGE AND LACK OF SUBSEQUENT REPAIR<br/>[FR] BLOQUEURS DE LA VOIX NOGO-A S1PR POUR LE TRAITEMENT DE MALADIES CARACTÉRISÉES PAR UNE LÉSION NEURONALE ET UN DÉFAUT DE RÉPARATION ULTÉRIEURE
  申请人：UNIV ZUERICH

  公开号：WO2012164103A2

  公开（公告）日：2012-12-06

  The present invention provides inhibitors capable of binding to a member of the S1PR receptor group comprised of S1PR2 and S1PR5 with a dissociation constant of 5x10-7 mol/l or smaller for treating neuronal damage, specifically an antibody, an antibody fragment, an antibody-like molecule, a nucleic acid aptamer or an oligopeptide with 6 to 30 amino acid residues in length. Similarly, an interfering RNA or an antisense modulator of gene expression of G13 or a member of the S1PR receptor group described above are provided for treating of neuronal damage.