5HPP-33 | 105624-86-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: 5HPP-33
• 英文别名: 2-(2,6-Diisopropylphenyl)-5-hydroxyisoindoline-1,3-dione；2-[2,6-di(propan-2-yl)phenyl]-5-hydroxyisoindole-1,3-dione
• CAS: 105624-86-0
• 化学式: C₂₀H₂₁NO₃
• 分子量: 323.392
• InChiKey: LAKWINYVWJPHQW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 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：
  57.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5HPP-33 在 2,6-二叔丁基-4-甲基吡啶 、 氨基磺酰氯 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 24.0h， 生成 [2-[2,6-Di(propan-2-yl)phenyl]-1,3-dioxoisoindol-5-yl] sulfamate
  参考文献：
  名称：

  Inhibitors of NF-κB derived from thalidomide

  摘要：

  A series of compounds originally derived from thalidomide were synthesized and evaluated. The most potent compounds in this series, 5HPP-33 and compound 20, inhibited NF-kappaB activation in HeLa cells. Preliminary study indicated that the mechanism of inhibition of NF-kappaB activation is through inhibition of its translocation from the cytoplasm to the nucleus.

  DOI：

  10.1016/j.bmcl.2007.01.088
• 作为产物：
  描述：

  4-羟基苯酐 生成 5HPP-33
  参考文献：
  名称：

  摘要：

  DOI：

文献信息

• Methods for treating autoimmune disorders, and reagents related thereto
  申请人：Bachovchin W. William

  公开号：US20050070459A1

  公开（公告）日：2005-03-31

  The invention generally relates to improved methods for treatment or prophylaxis in animal subjects (including humans) of autoimmune disorders including Type I diabetes, septic shock, multiple sclerosis, inflammatory bowel disease (IBD) and Crohn's disease.

  这项发明通常涉及改进的方法，用于治疗或预防动物主体（包括人类）的自身免疫性疾病，包括I型糖尿病、感染性休克、多发性硬化、炎症性肠病（IBD）和克罗恩病。
• THALIDOMIDE ANALOGS FOR TREATING VASCULAR ABNORMALITIES
  申请人：Chen Danyang

  公开号：US20080306134A1

  公开（公告）日：2008-12-11

  Thalidomide analog compounds having a general structure are described. R 1 is selected from a group comprising of hydroxy, hydrogen, and amino. Also described is a method for treating vascular abnormalities, such as neovascularization and vascular leakage. A therapeutically effective amount of a composition containing the thalidomide analog compound is administered to a patient. The composition may further include agents, such as solubilizing agents, inert fillers, diluents, excipients, or flavoring agents.

  本文描述了具有一般结构的沙利度胺类似化合物。其中，R1从羟基、氢和氨基组成的一组中选择。同时还描述了一种治疗血管异常的方法，例如新生血管形成和血管渗漏。将含有沙利度胺类似化合物的治疗有效量的组合物给患者进行治疗。该组合物还可以包括溶解剂、惰性填充剂、稀释剂、辅料或调味剂等药剂。
• SCREENING METHOD UTILIZING THALIDOMIDE-TARGETING FACTOR
  申请人：Tokyo Institute of Technology

  公开号：EP2492686A1

  公开（公告）日：2012-08-29

  With an aim to provide means for developing a compound devoid of teratogenicity but retaining beneficial actions, a screening method for a non-teratogenic substance comprising bringing a test substance into contact with cereblon or a fragment of cereblon, evaluating the bindability of the test substance with cereblon or the fragment of cereblon, and selecting a test substance that does not bind to cereblon or the fragment of cereblon or a test substance exhibiting lower bindability with cereblon or the fragment of cereblon than does thalidomide is provided.

  为了提供开发无致畸性但保留有益作用的化合物的方法，提供了一种无致畸性物质的筛选方法，该方法包括使试验物质与脑龙或脑龙片段接触，评估试验物质与脑龙或脑龙片段的结合力，并选择不与脑龙或脑龙片段结合的试验物质或与脑龙或脑龙片段的结合力低于沙利度胺的试验物质。
• Pretargeted activatable cell penetrating peptide with intracellularly releasable prodrug
  申请人：The Regents of the University of California

  公开号：US10029017B2

  公开（公告）日：2018-07-24

  Disclosed herein, the invention pertains to methods and compositions that find use in treatment, diagnosis, prognosis and characterization of disease and disease samples based on the ability of a disease sample to cleave a MTS molecule of the present invention. The MTS molecules of the present invention have a formula as disclosed herein and wherein A is a peptide with a sequence comprising 5 to 9 consecutive acidic amino acids, wherein the amino acids are selected from: aspartates and glutamates; B is a peptide with a sequence comprising 5 to 20 consecutive basic amino acids; X and Y are linkers; P is a pre-targeting moiety; M is a macromolecular carrier, C is a detectable moiety; and T is a compound for delivery to a target, including for example a therapeutic compound.

  在此公开的本发明涉及根据疾病样本裂解本发明的 MTS 分子的能力用于疾病和疾病样本的治疗、诊断、预后和表征的方法和组合物。本发明的 MTS 分子具有如本文所公开的式，其中 A 是多肽，其序列包括 5 至 9 个连续的酸性氨基酸，其中氨基酸选自天冬氨酸和谷氨酸；B 是多肽，其序列包括 5 至 20 个连续的碱性氨基酸；X 和 Y 是连接体；P 是预靶向分子；M 是大分子载体；C 是可检测分子；T 是用于递送至靶点的化合物，例如包括治疗化合物。
• Personalized protease assay to measure protease activity in neoplasms
  申请人：The Regents of the University of California

  公开号：US10385380B2

  公开（公告）日：2019-08-20

  Disclosed herein, the invention pertains to methods and compositions that find use in diagnostic, prognostic and characterization of neoplasia samples based on the ability of a neoplasia sample to cleave a MTS molecule of the present invention. In some embodiments, a MTS molecule disclosed herein has the formula (A-X-B-C), wherein A is a peptide with a sequence comprising 5 to 9 consecutive acidic amino acids, wherein the amino acids are selected from: aspartates and glutamates; B is a peptide with a sequence comprising 5 to 20 consecutive basic amino acids; X is a linker; and C is a detectable moiety.

  本发明涉及根据肿瘤样本裂解本发明 MTS 分子的能力，用于诊断、预后和表征肿瘤样本的方法和组合物。在一些实施方案中，本发明公开的 MTS 分子具有式（A-X-B-C），其中 A 是多肽，其序列包括 5 至 9 个连续的酸性氨基酸，其中氨基酸选自天冬氨酸和谷氨酸；B 是多肽，其序列包括 5 至 20 个连续的碱性氨基酸；X 是连接体；C 是可检测分子。