5-{1-[(3-ethoxyphenyl)methyl]-5-methyl-1H-1,2,4-triazol-3-yl}-3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazole | 1570495-83-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 5-{1-[(3-ethoxyphenyl)methyl]-5-methyl-1H-1,2,4-triazol-3-yl}-3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazole
• 英文别名: 5-[1-[(3-Ethoxyphenyl)methyl]-5-methyl-1,2,4-triazol-3-yl]-3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazole
• CAS: 1570495-83-8
• 化学式: C₂₁H₁₈F₃N₅O₃
• 分子量: 445.401
• InChiKey: MAAALOIGKBFCKU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.1
• 重原子数：
  32
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  88.1
• 氢给体数：
  0
• 氢受体数：
  10

文献信息

• ANTI-B7-H3 ANTIBODIES AND ANTIBODY DRUG CONJUGATES
  申请人：AbbVie Inc.

  公开号：US20170355769A1

  公开（公告）日：2017-12-14

  The invention relates to B7 homology 3 protein (B7-H3) antibodies and antibody drug conjugates (ADCs), including compositions and methods of using said antibodies and ADCs.

  这项发明涉及B7同源物3蛋白（B7-H3）抗体和抗体药物结合物（ADCs），包括使用所述抗体和ADCs的组合物和方法。
• [EN] ANTIBODY-DRUG CONJUGATES COMPRISING ANTI-B7-H3 ANTIBODIES<br/>[FR] CONJUGUÉS ANTICORPS-MÉDICAMENT COMPRENANT DES ANTICORPS ANTI-B7-H3
  申请人：INTOCELL INC

  公开号：WO2021260438A1

  公开（公告）日：2021-12-30

  The present disclosure relates to antibody-drug conjugates (ADCs) wherein one or more active agents are conjugated to an anti-B7-H3 antibody through a linker. The linker may comprise a unit that covalently links active agents to the antibody. The disclosure further relates to monoclonal antibodies and antigen binding fragments, variants, multimeric versions, or bispecifics thereof that specifically bind B7-H3, as well as methods of making and using these anti-B7-H3 antibodies and antigen-binding fragments thereof in a variety of therapeutic, diagnostic and prophylactic indications

  本公开涉及抗体药物结合物（ADCs），其中一个或多个活性剂通过连接剂与抗B7-H3抗体结合。连接剂可能包括一个单位，将活性剂共价连接到抗体上。本公开进一步涉及特异性结合B7-H3的单克隆抗体和抗原结合片段、变体、多聚体版本或双特异性抗体，以及在各种治疗、诊断和预防适应症中制备和使用这些抗B7-H3抗体和抗原结合片段的方法。
• HETEROCYCLIC MODULATORS OF HIF ACTIVITY FOR TREATMENT OF DISEASE
  申请人：Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer Center

  公开号：US20140066424A1

  公开（公告）日：2014-03-06

  The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.

  本发明涉及化合物和方法，可用作HIF通路活性的抑制剂，用于治疗或预防癌症和其他缺氧介导的疾病。
• METHOD OF SYNTHESIS OF SUBSTITUTED HEXITOLS SUCH AS DIANHYDROGALACTITOL
  申请人：DEL MAR PHARMACEUTICALS

  公开号：US20150329511A1

  公开（公告）日：2015-11-19

  The present invention provides an efficient method of synthesizing and purifying dianhydrohexitols such as dianhydrogalactitol. In general, as applied to dianhydrogalactitol, the method comprises: (1) reacting dulcitol with a concentrated solution of hydrobromic acid at a temperature of about 80° C. to produce dibromogalactitol; (2) reacting the dibromogalactitol with potassium carbonate in t-butanol to produce dianhydrogalactitol; and (3) purifying the dianhydrogalactitol using a slurry of ethyl ether to produce purified dianhydrogalactitol. Another method produces dianhydrogalactitol from dulcitol; this method comprises: (1) reacting dulcitol with a reactant to convert the 1,6-hydroxy groups of dulcitol to an effective leaving group to generate an intermediate; and (2) reacting the intermediate with an inorganic weak base to produce dianhydrogalactitol through an intramolecular S N 2 reaction. Other methods for the synthesis of dianhydrogalactitol from dulcitol are described.

  本发明提供了一种合成和纯化二缩醇的有效方法，例如二缩乳糖醇。一般而言，针对二缩乳糖醇，该方法包括：（1）在约80℃的温度下，将甜菜醇与浓盐酸溶液反应，以产生二溴缩乳糖醇；（2）将二溴缩乳糖醇与t-丁醇中的碳酸钾反应，以产生二缩乳糖醇；以及（3）使用乙醚的悬浮液纯化二缩乳糖醇，以产生纯化的二缩乳糖醇。另一种方法从甜菜醇中产生二缩乳糖醇；该方法包括：（1）将甜菜醇与反应物反应，将甜菜醇的1,6-羟基转化为有效的离去基，以生成中间体；（2）将中间体与无机弱碱反应，通过分子内SN2反应产生二缩乳糖醇。还描述了从甜菜醇合成二缩乳糖醇的其他方法。
• Anti-EGFR antibodies and antibody drug conjugates
  申请人：AbbVie Inc.

  公开号：US10098968B2

  公开（公告）日：2018-10-16

  The invention relates to anti-epidermal growth factor (EGFR) antibodies and antibody drug conjugates (ADCs), including compositions and methods of using said antibodies and ADCs.

  本发明涉及抗表皮生长因子（EGFR）抗体和抗体药物共轭物（ADC），包括使用所述抗体和 ADC 的组合物和方法。