6-isopropyl-1H-quinazoline-2,4-dione | 1318754-42-5

• 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: 6-isopropyl-1H-quinazoline-2,4-dione
• 英文别名: 6-propan-2-yl-1H-quinazoline-2,4-dione
• CAS: 1318754-42-5
• 化学式: C₁₁H₁₂N₂O₂
• 分子量: 204.228
• InChiKey: ILOBKCVOKGMBEQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  58.2
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  6-isopropyl-1H-quinazoline-2,4-dione 在 sodium hydride 、 N,N-二甲基苯胺 、 三氯氧磷 作用下， 以 四氢呋喃 、 N-甲基吡咯烷酮 、 mineral oil 为溶剂， 反应 1.0h， 生成
  参考文献：
  名称：

  Structure–Activity Relationship and Pharmacokinetic Studies of Sotrastaurin (AEB071), a Promising Novel Medicine for Prevention of Graft Rejection and Treatment of Psoriasis

  摘要：

  Protein kinase C (PKC) isotypes have emerged as key targets for the blockade of early T-cell activation. Herein, we report on the structure - activity relationship and the detailed physicochemical and in vivo pharmacokinetic properties of sotrastaurin (AEB071, 1), a novel maleimide-based PKC inhibitor currently in phase II clinical trials. Most notably, the preferred uptake of sotrastaurin into lymphoid tissues is an important feature, which is likely to contribute to its in vivo efficacy.

  DOI：

  10.1021/jm200469u

文献信息

• [EN] EXON SKIPPING OLIGOMER CONJUGATES FOR MUSCULAR DYSTROPHY<br/>[FR] CONJUGUÉS OLIGOMÈRES DE SAUTS D'EXONS POUR LA DYSTROPHIE MUSCULAIRE
  申请人：SAREPTA THERAPEUTICS INC

  公开号：WO2018118662A1

  公开（公告）日：2018-06-28

  Antisense oligomer conjugates complementary to a selected target site in the human dystrophin gene to induce exon 53 skipping are described.

  与人类肌营养不良基因中选择的靶位点互补的反义寡核苷酸共轭物用于诱导外显子53跳跃。
• FUNCTIONALLY-MODIFIED OLIGONUCLEOTIDES AND SUBUNITS THEREOF
  申请人：Sarepta Therapeutics, Inc.

  公开号：US20140330006A1

  公开（公告）日：2014-11-06

  Functionally-modified oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3′ and/or 5′-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.

  提供了包含修改的亚单位间连接和/或修改的3'和/或5'-末端基团的功能修饰寡核苷酸类似物。所公开的化合物对于治疗需要抑制蛋白质表达或纠正异常mRNA剪接产物以产生有益治疗效果的疾病是有用的。
• EXON SKIPPING OLIGOMER CONJUGATES FOR MUSCULAR DYSTROPHY
  申请人：Sarepta Therapeutics, Inc.

  公开号：US20180177814A1

  公开（公告）日：2018-06-28

  Antisense oligomer conjugates complementary to a selected target site in the human dystrophin gene to induce exon 51 skipping are described.

  抗义核苷酸寡聚体结合到人类肌营养不良基因中的特定靶位点，诱导外显子51跳跃。
• CYCLIC AMINE SUBSTITUTED PYRIMIDINEDIAMINES AS PKC INHIBITORS
  申请人：Singh Rajinder

  公开号：US20100130486A1

  公开（公告）日：2010-05-27

  The invention encompasses compounds having formula I or II and the compositions and methods using these compounds in the treatment of conditions in which inhibition of PKC and PKD is therapeutically useful.

  本发明涵盖具有公式I或II的化合物，以及使用这些化合物治疗抑制PKC和PKD在治疗上有用的情况的组合物和方法。
• OLIGONUCLEOTIDES FOR TREATING EXPANDED REPEAT DISEASES
  申请人：Sarepta Therapeutics, Inc.

  公开号：US20140303238A1

  公开（公告）日：2014-10-09

  The invention provides for a method for selectively reducing the expression of a mutant mRNA and/or protein having an expanded nucleotide repeat relative to a wild-type mRNA, comprising contacting a cell with an antisense oligonucleotide of sufficient length and complementarity to the expanded nucleotide repeat. More particularly it relates to selectively reducing the expression of mutant Huntington protein associated with Huntington's disease. The antisense oligonucleotide comprising either a nucleotide or a repeated three nucleotide sequence as defined in the claims.

  该发明提供了一种选择性减少具有扩展核苷酸重复相对于野生型mRNA的突变型mRNA和/或蛋白质表达的方法，包括将长度和互补性足够的反义寡核苷酸与细胞接触。更具体地，它涉及选择性减少与亨廷顿病相关的突变亨廷顿蛋白的表达。反义寡核苷酸包括在权利要求中定义的核苷酸或重复的三核苷酸序列。