2-(Oxaloamino)quinoline-3-carboxylic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 2-(Oxaloamino)quinoline-3-carboxylic acid
• 化学式: C₁₂H₈N₂O₅
• 分子量: 260.2
• InChiKey: WDTREEPIHQWTNY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  117
• 氢给体数：
  3
• 氢受体数：
  6

文献信息

• MODULATORS OF PROTEIN TYROSINE PHOSPHATASES (PTPASES)
  申请人：——

  公开号：US20020019412A1

  公开（公告）日：2002-02-14

  The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.

  本发明提供了新型化合物、新型组合物、其使用方法和制造方法，其中这些化合物是药理学上有用的蛋白酪氨酸磷酸酶（PTP酶）抑制剂，如PTP1B、CD45、SHP-1、SHP-2、PTP&agr;、LAR和HePTP或类似物。这些化合物可用于治疗 I 型糖尿病、II 型糖尿病、糖耐量受损、胰岛素抵抗、肥胖、免疫功能障碍（包括凝血系统功能障碍的自身免疫性疾病）、过敏性疾病（包括哮喘）、骨质疏松症、增殖性疾病（包括癌症和牛皮癣）、生长激素合成或作用减少或增加的疾病，调节生长激素释放和/或反应的激素或细胞因子合成减少或增加的疾病，包括阿尔茨海默病和精神分裂症在内的脑部疾病，以及传染病。
• MODULATORS OF PROTEIN TYROSINE PHOSPHATASES (PTPases)
  申请人：NOVO NORDISK A/S

  公开号：EP1062218A1

  公开（公告）日：2000-12-27
• [EN] MODULATORS OF PROTEIN TYROSINE PHOSPHATASES (PTPases)<br/>[FR] MODULATEURS DE PROTEINE TYROSINE PHOSPHATASES (PTPASES)
  申请人：NOVO NORDISK A/S

  公开号：WO1999046268A1

  公开（公告）日：1999-09-16

  (EN) The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPases) such as PTP1B, CD45, SHP-1, SHP-2, PTP$g(a), LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.(FR) L'invention concerne de nouveaux composés, de nouvelles compositions, des méthodes d'utilisation et des méthodes de fabrication associées. Lesdits composés sont des inhibiteurs de protéine tyrosine phosphatases (PTPases) pharmacologiquement utiles, tels que PTP1B, CD45, SHP-1, SHP-2, PTP$g(a), LAR et HePTP ou analogues. Ces composés sont utiles dans le traitement du diabète du type I, du diabète du type II, de l'intolérance au glucose, de la résistance insulinique, de l'obésité, des dysfonctionnements immunitaires parmi lesquels les maladies auto-immunes entraînant un dysfonctionnement du système de coagulation, des maladies allergiques parmi lesquelles l'asthme, de l'ostéoporose, des troubles proliférants parmi lesquels le cancer et le psoriasis, des maladies entraînant une baisse ou une augmentation de la synthèse ou des effets des hormones de croissance, des maladies entraînant une baisse ou une augmentation de la synthèse des hormones ou cytokines qui régulent la libération d'hormones de croissance ou la réaction à ces hormones, des maladies cérébrales parmi lesquelles la maladie d'Alzheimer et la schizophrénie, et des maladies infectieuses.