US9533969, Tdrl-521

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: US9533969, Tdrl-521
• 英文别名: 4-[5-(4-methoxyphenyl)-3-[3-(4-methylphenyl)-1-phenylpyrazol-4-yl]-3,4-dihydropyrazol-2-yl]-4-oxobutanoic acid
• 化学式: C₃₀H₂₈N₄O₄
• 分子量: 508.6
• InChiKey: KCAJOKMGJJTAKA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  38
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  97
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• PYRAZOLYLACYLPYRAZOLINE COMPOUNDS AND METHOD FOR TREATING PAIN
  申请人：THE TRUSTEES OF INDIANA UNIVERSITY

  公开号：US20210155609A1

  公开（公告）日：2021-05-27

  This invention relates to pyrazolylacylpyrazoline compounds or pharmaceutically acceptable salts thereof, and for the use of the compounds to treat neurological disorders.

  这项发明涉及吡唑基酰基吡唑啉化合物或其药用盐，以及利用这些化合物治疗神经系统疾病。
• MATERIALS AND METHOD FOR INHIBITING REPLICATION PROTEIN A AND USES THEREOF
  申请人：Turchi John J.

  公开号：US20130028989A1

  公开（公告）日：2013-01-31

  Targeting uncontrolled cell proliferation and resistance to DNA damaging chemotherapeutics with at least one reagent has significant potential in cancer treatment. Replication Protein A, the eukaryotic single-strand (ss) DNA binding protein, is essential for genomic maintenance and stability via roles in both DNA replication and repair. Reported herein are small molecules that inhibits the in vitro, in vivo, and cellular ssDNA binding activity of RPA, thereby disrupting the eukaryotic cell cycle, inducing cytotoxicity and increasing the efficacy of chemotherapeutic agents damage DNA, and/or disrupt its replication and/or function. These results provide new insights into the mechanism of RPA-ssDNA interactions in chromosome maintenance and stability. This represents a molecularly targeted eukaryotic DNA binding inhibitor and demonstrates the utility of targeting a protein-DNA interaction as a means of studying the cell cycle and providing a therapeutic strategy for cancer treatment.
• MATERIALS AND METHOD FOR INHIBITING REPLICATION PROTEIN A AND USES THEREOF
  申请人：Indiana University Research and Technology Corp.

  公开号：US20140370121A1

  公开（公告）日：2014-12-18

  Targeting uncontrolled cell proliferation and resistance to DNA damaging chemotherapeutics with at least one reagent has significant potential in cancer treatment. Replication Protein A, the eukaryotic single-strand (ss) DNA binding protein, is essential for genomic maintenance and stability via roles in both DNA replication and repair. Reported herein are small molecules that inhibits the in vitro, in vivo, and cellular ssDNA binding activity of RPA, thereby disrupting the eukaryotic cell cycle, inducing cytotoxicity and increasing the efficacy of chemotherapeutic agents damage DNA, and/or disrupt its replication and/or function. These results provide new insights into the mechanism of RPA-ssDNA interactions in chromosome maintenance and stability. This represents a molecularly targeted eukaryotic DNA binding inhibitor and demonstrates the utility of targeting a protein-DNA interaction as a means of studying the cell cycle and providing a therapeutic strategy for cancer treatment.
• US8859532B2
  申请人：——

  公开号：US8859532B2

  公开（公告）日：2014-10-14
• US9533969B2
  申请人：——

  公开号：US9533969B2

  公开（公告）日：2017-01-03