Acetic acid;2-hydroxypropane-1,2,3-tricarboxylic acid

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Acetic acid;2-hydroxypropane-1,2,3-tricarboxylic acid
• 化学式: C8H12O9
• 分子量: 252.18
• InChiKey: FXAGBTBXSJBNMD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.16
• 重原子数：
  17
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  169
• 氢给体数：
  5
• 氢受体数：
  9

文献信息

• [EN] NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF DISEASES<br/>[FR] NOUVEAUX COMPOSÉS ET COMPOSITIONS PHARMACEUTIQUES ASSOCIÉES POUR LE TRAITEMENT DE MALADIES
  申请人：GALAPAGOS NV

  公开号：WO2020239658A1

  公开（公告）日：2020-12-03

  The present invention discloses compounds according to Formula (I), wherein R1a, R1b, R1c, R2a, W1, W2, X1, X2, X3, Y, and Z are as defined herein. The present invention relates to compounds, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, autoinflammatory diseases, autoimmune diseases, proliferative diseases, fibrotic diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformation, diseases involving impairment of bone turnover, diseases associated with hypersecretion of IL-6, diseases associated with hypersecretion of TNFα, interferons, IL-12 and/or IL-23, respiratory diseases, endocrine and/or metabolic diseases, cardiovascular diseases, dermatological diseases, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.

  本发明公开了根据式（I）的化合物，其中R1a、R1b、R1c、R2a、W1、W2、X1、X2、X3、Y和Z如本文所定义。本发明涉及化合物、其生产方法、包括其在内的制药组合物，以及使用这些化合物进行预防和/或治疗炎症性疾病、自身炎症性疾病、自身免疫性疾病、增生性疾病、纤维化疾病、移植排斥、涉及软骨周转障碍的疾病、先天软骨畸形、涉及骨周转障碍的疾病、与IL-6过度分泌有关的疾病、与TNFα、干扰素、IL-12和/或IL-23过度分泌有关的疾病、呼吸系统疾病、内分泌和/或代谢性疾病、心血管疾病、皮肤病和/或异常血管生成相关疾病的治疗方法，通过给予本发明的化合物。
• [EN] HETEROCYCLIC DERIVATIVES MODULATING ACTIVITY OF CERTAIN PROTEIN KINASES<br/>[FR] DÉRIVÉS HÉTÉROCYCLIQUES MODULANT L'ACTIVITÉ DE CERTAINES PROTÉINES KINASES
  申请人：EUDENDRON S R L

  公开号：WO2016096709A1

  公开（公告）日：2016-06-23

  The present invention relates to novel heterocyclic derivatives having general formula (I) and their therapeutic use for diseases such as cancer, inflammation, pain, autoimmune diseases or neurodegenerative diseases like Alzheimer's or Parkinson's disease that can be treated by modulation of certain protein kinases. Compounds of formula (I) can be used for treatment of patients who do not respond to kinase inhibition therapy that comprises currently available medications.

  本发明涉及具有通式（I）的新型杂环衍生物及其在癌症、炎症、疼痛、自身免疫疾病或阿尔茨海默病、帕金森病等神经退行性疾病的治疗中的应用，这些疾病可以通过调节特定蛋白激酶来治疗。通式（I）的化合物可用于治疗对目前可用药物组成的激酶抑制疗法无反应的患者。
• 11beta-HSD1 Inhibitors
  申请人：Evotec OAI AG

  公开号：EP1655283A1

  公开（公告）日：2006-05-10

  The invention relates to compounds of formula (I) wherein A, Y, Z1, Z2, R1 to R3 and X1 to X4 have the meaning as cited in the description and the claims. For example A is 4'-fluorobiphen-4-yl; Y is -S(O)2NH-; R1, R2 are H; X1, X2, X4 are CH; X3 is C-F; Z1 is =O; and Z2-R3 is N(CH2CH3)2. Said compounds are useful as 11β-HSD1 inhibitors. The invention also relates to the preparation of such compounds as well as the production and use as medicament.

  该发明涉及具有如下式（I）的化合物，其中A、Y、Z1、Z2、R1至R3和X1至X4的含义如描述和权利要求中所述。例如，A为4'-氟联苯-4-基；Y为-S（O）2NH-；R1、R2为H；X1、X2、X4为CH；X3为C-F；Z1为=O；Z2-R3为N（CH2CH3）2。所述化合物可用作11β-HSD1抑制剂。该发明还涉及制备此类化合物以及作为药物的生产和使用。
• 11beta-hsdi inhibitors
  申请人：Coulter Thomas Stephen

  公开号：US20090069323A1

  公开（公告）日：2009-03-12

  The invention relates to compounds of formula (I) wherein A, Y, Z 1 , Z 2 , R 1 to R 3 and X 1 to X 4 have the meaning as cited in the description and the claims. For example A is 4′-fluorobiphen-4-yl; Y is —S(O) 2 NH—; R 1 , R 2 are H; X 1 , X 2 , X 4 are CH; X 3 is C—F; Z 1 is ═O; and Z 2 -R 3 is N(CH 2 CH 3 ) 2 . Said compounds are useful as 11β-HSD1 inhibitors. The invention also relates to the preparation of such compounds as well as the production and use as medicament.

  本发明涉及式(I)的化合物，其中A，Y，Z1，Z2，R1至R3和X1至X4的含义如说明书和权利要求中所述。例如，A是4'-氟联苯-4-基；Y是—S（O）2NH—；R1，R2为H；X1，X2，X4为CH；X3为C—F；Z1为═O；Z2-R3为N（CH2CH3）2。所述化合物可用作11β-HSD1抑制剂。本发明还涉及制备这些化合物以及作为药物的生产和使用。
• Therapeutic Compositions
  申请人：LEO Laboratories Limited

  公开号：US20160263070A1

  公开（公告）日：2016-09-15

  Ingenol angelate is a potent anticancer agent, and can be stabilised by dissolving it in an aprotic solvent in the presence of an acidic buffer.

  英文原文已经被翻译成中文了，以下是翻译结果： Ingenol angelate是一种有效的抗癌剂，可以通过在无质子溶剂中加入酸性缓冲剂来稳定它。