4-hydroxy-1,2,3-benzenetricarboxylic acid | 113665-36-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-hydroxy-1,2,3-benzenetricarboxylic acid
• 英文别名: 4-hydroxy-benzene-1,2,3-tricarboxylic acid；4-Hydroxy-benzol-1,2,3-tricarbonsaeure；Phenoltricarbonsaure；4-hydroxybenzene-1,2,3-tricarboxylic acid
• CAS: 113665-36-4
• 化学式: C₉H₆O₇
• 分子量: 226.142
• InChiKey: GFXOKWDRTPZVRK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  132
• 氢给体数：
  4
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  重氮甲烷 、 4-hydroxy-1,2,3-benzenetricarboxylic acid 生成 4-methoxy-benzene-1,2,3-tricarboxylic acid trimethyl ester
  参考文献：
  名称：

  4-Hydroxybenzene-1,2,3-tricarboxylic Acid, 5-Hydroxybenzene-1,2,4-tricarboxylic Acid and their Derivatives

  摘要：

  DOI：

  10.1021/ja01169a003
• 作为产物：
  描述：

  alkaline earth salt of/the/ methylsulfuric acid 在 sodium hydroxide 、 potassium permanganate 作用下， 生成 4-hydroxy-1,2,3-benzenetricarboxylic acid
  参考文献：
  名称：

  4-Hydroxybenzene-1,2,3-tricarboxylic Acid, 5-Hydroxybenzene-1,2,4-tricarboxylic Acid and their Derivatives

  摘要：

  DOI：

  10.1021/ja01169a003

文献信息

• [EN] AROMATIC COMPOUNDS FROM FURANICS<br/>[FR] COMPOSÉS AROMATIQUES DÉRIVÉS DES FURANIQUES
  申请人：NEDERLANDSE ORGANISATIE VOOR TOEGEPAST-NATUURWETENSCHAPPELIJK ONDERZOEK TNO

  公开号：WO2017146581A1

  公开（公告）日：2017-08-31

  Described are methods for preparing phenols, benzene carboxylic acids, esters and anhydrides thereof from furanic compounds by reaction with a dienophile, wherein the furanic compounds are reacted with a hydrazine and/or oxime and then reacted with a dienophile.

  描述了一种从呋喃化合物通过与二烯醚反应制备酚、苯甲酸、酯和酐的方法，其中呋喃化合物与肼和/或肟反应，然后与二烯醚反应。
• [EN] PFKFB3 INHIBITORS AND THEIR USES<br/>[FR] INHIBITEURS DE PFKFB3 ET LEURS UTILISATIONS
  申请人：GERO DISCOVERY LLC

  公开号：WO2020080979A1

  公开（公告）日：2020-04-23

  This disclosure relates to new phthalimide and isoindolinone derivatives and other PFKFB3 inhibitors for use in the treatment of diseases. The invention further relates to pharmaceutical compositions containing such PFKFB3 inhibitors, methods of preparation thereof, methods for their use as therapeutic agents, and methods of preparation of a medicament for use in therapy, as well as kits and other inventiions comprising such PFKFB3 inhibitors. These PFKFB3 inhibitors are useful for the treatment and prophylaxis of cancer, neurodegenerative diseases, autoimmune diseases, inflammatory disorders, multiple sclerosis, metabolic diseases, inhibition of angiogenesis and other diseases and conditions, where the modulation of PFKFB3 and/or PFKFB4 has beneficial effect as well as neuroprotection.

  这项披露涉及新的邻苯二甲酰亚胺和异吲哚酮衍生物以及其他PFKFB3抑制剂，用于治疗疾病。该发明还涉及含有此类PFKFB3抑制剂的药物组合物，其制备方法，作为治疗剂的使用方法，以及用于治疗的药物的制备方法，以及包含此类PFKFB3抑制剂的工具包和其他发明。这些PFKFB3抑制剂对于治疗和预防癌症、神经退行性疾病、自身免疫疾病、炎症性疾病、多发性硬化症、代谢性疾病、抑制血管生成以及其他疾病和情况具有用途，在这些情况下，PFKFB3和/或PFKFB4的调节具有益处，以及神经保护作用。
• [EN] PROCESSES FOR PREPARING ISOINDOLINE-1,3-DIONE COMPOUNDS<br/>[FR] PROCÉDÉS DE PRÉPARATION DE COMPOSÉS ISOINDOLINE-1,3-DIONE
  申请人：CELGENE CORP

  公开号：WO2014018866A1

  公开（公告）日：2014-01-30

  Provided herein are processes for preparing an isoindoline- 1.3-dione compound, or an enantiomer or a mixture of enantiomers thereof; or a pharmaceutically acceptable salt, solvate, hydrate, or polymorph thereof.

  本文提供了制备异吲哚啉-1,3-二酮化合物的过程，或其对映体或对映体的混合物；或其药用可接受的盐、溶剂化合物、水合物或多晶形式。
• [EN] PRODUCTION OF AROMATIC ACIDS AND PHENOLICS<br/>[FR] PRODUCTION D'ACIDES AROMATIQUES ET DE COMPOSÉS PHÉNOLIQUES
  申请人：TNO

  公开号：WO2021080426A1

  公开（公告）日：2021-04-29

  The invention is directed to a process for the preparation of an aromatic acid or a phenolic compound, said process comprising reacting a dienophile and a furanic compound comprising an acetal moiety in a Diels-Alders reaction to obtain an aromatic compound comprising said acetal moiety, followed by hydrolysis and oxidation of said acetal moiety into a hydroxide or carboxylate moiety to form the aromatic acid or phenolic compound, wherein said dienophile is selected from the group consisting of alkylenes, acetylenes, acrylates, maleates, fumarates, maleimides, propiolates, acetylene dicarboxylates, and benzynes and wherein said acetal moiety is bound directly to the 2-position of the furanic compound.

  该发明涉及一种制备芳香酸或酚类化合物的方法，该方法包括将二烯酸酯和含有缩醛基团的呋喃化合物在Diels-Alder反应中反应，以获得含有该缩醛基团的芳香化合物，随后对该缩醛基团进行水解和氧化，将其转化为羟基或羧酸基团，形成芳香酸或酚类化合物。其中，所述二烯酸酯选自烯烃、乙炔、丙烯酸酯、马来酸酯、富马酸酯、马来酰亚胺、丙炔酸酯、乙炔二羧酸酯和苯炔，所述缩醛基团直接与呋喃化合物的2位结合。
• [EN] CONTROLLED RELEASE FORMULATIONS FOR THE DELIVERY OF HIF-1 INHIBITORS<br/>[FR] FORMULATIONS À LIBÉRATION CONTRÔLÉE POUR L'ADMINISTRATION D'INHIBITEURS DU HIF-1
  申请人：UNIV JOHNS HOPKINS

  公开号：WO2013138343A1

  公开（公告）日：2013-09-19

  Controlled release dosage formulations for the delivery of one or more HIF-1 inhibitors are provided. The controlled release formulations contain one or more HIF-1 inhibitors conjugated to or dispersed in a polymeric vehicle. In some cases, one or more HIF-1 inhibitors are dispersed or encapsulated in a polymeric matrix. In preferred embodiments, the one or more HIF- 1 inhibitors are covalently bound to a polymer, forming a polymer-drug conjugate. Polymeric vehicles can be formed into implants, microparticles, nanoparticles, or combinations thereof for administration. Controlled release HIF-1 formulations provide prolonged therapeutic benefit while lowering side effects by releasing low levels of one or more HIF-1 inhibitors and/or HIF-1 inhibitor conjugates over a prolonged period of time. Controlled release dosage formulations for the delivery of one or more HIF-1 inhibitors can be used to treat or prevent a disease or disorder in a patient associated with vascularization, including cancer, obesity, and ocular diseases such as wet AMD.

  本发明提供了用于输送一种或多种HIF-1抑制剂的控释剂型制剂。这些控释制剂型制剂包含一种或多种HIF-1抑制剂与聚合物载体结合或分散。在某些情况下，一种或多种HIF-1抑制剂分散或封装在聚合物基质中。在优选实施例中，一种或多种HIF-1抑制剂与聚合物共价结合，形成聚合物-药物共轭物。聚合物载体可以形成成植入物、微粒子、纳米粒子或其组合物以供给药。控释HIF-1制剂提供长效治疗效果，同时通过在长时间内释放低水平的一种或多种HIF-1抑制剂和/或HIF-1抑制剂共轭物来降低副作用。用于输送一种或多种HIF-1抑制剂的控释剂型制剂可用于治疗或预防与血管化有关的患者疾病或障碍，包括癌症、肥胖症和激素性黄斑病变等眼部疾病。