1,2,3,4-Tetrahydro-chinoxalin-carbonsaeure-(2) | 49849-51-6

• 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: 1,2,3,4-Tetrahydro-chinoxalin-carbonsaeure-(2)
• 英文别名: 1,2,3,4-Tetrahydroquinoxaline-2-carboxylic acid
• CAS: 49849-51-6
• 化学式: C₉H₁₀N₂O₂
• 分子量: 178.191
• InChiKey: VRRWYUWUFBCTEZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  61.4
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• [EN] HYDROXYETHYLAMINE DERIVATIVES FOR THE TREATMENT OF ALZHEIMER'S DISEASE<br/>[FR] DERIVES D'HYDROXYETHYLAMINE UTILISES POUR LE TRAITEMENT DE LA MALADIE D'ALZHEIMER
  申请人：GLAXO GROUP LTD

  公开号：WO2004050619A1

  公开（公告）日：2004-06-17

  The present invention relates to novel hydroxyethylamine compounds of formula (I): (I) having Asp2 (-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated - amyloid levels or -amyloid deposits, particularly Alzheimer's disease.

  本发明涉及具有Asp2（-分泌酶，BACE1或Memapsin）抑制活性的新型羟乙基胺化合物的化学式（I）：（I），其制备方法，含有它们的组合物以及它们在治疗由高β-淀粉样蛋白水平或β-淀粉样蛋白沉积所特征的疾病中的应用，特别是阿尔茨海默病。
• [EN] HETEROCYCLIC COMPOUNDS AS PAD INHIBITORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES EN TANT QU'INHIBITEURS DE PAD
  申请人：JUBILANT BIOSYS LTD

  公开号：WO2019058393A1

  公开（公告）日：2019-03-28

  Heterocyclic compounds of Formula (I), (II), and (III) are described herein along with their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof. The compounds described herein, their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosis, cutaneous lupus erythematosis, ulcerative colitis, cancer, cystic fibrosis, asthma, multiple sclerosis and psoriasis.

  公式（I）、（II）和（III）的杂环化合物以及它们的多晶形态、立体异构体、前药、溶剂合物、共晶体、中间体、药学上可接受的盐和代谢物在此处描述。本文描述的化合物及其多晶形态、立体异构体、前药、溶剂合物、共晶体、中间体、药学上可接受的盐和代谢物是PAD4抑制剂，可能在治疗各种疾病中有用，例如类风湿关节炎、血管炎、系统性红斑狼疮、皮肤红斑狼疮、溃疡性结肠炎、癌症、囊性纤维化、哮喘、多发性硬化和牛皮癣。
• [EN] AZAHETEROCYCLIC SMALL MOLECULE MODULATORS OF HUMAN STING<br/>[FR] MODULATEURS AZAHÉTÉROCYCLIQUES À PETITES MOLÉCULES DE STING HUMAIN
  申请人：CURADEV PHARMA LTD

  公开号：WO2019243823A1

  公开（公告）日：2019-12-26

  The present invention relates to compounds of formula (I). The compounds may be used to modulate the Stimulator of Interferon Genes (STING) protein and thereby treat diseases such as cancer and microbial infections.

  本发明涉及式(I)的化合物。这些化合物可用于调节干扰素基因激活蛋白（STING）并因此治疗癌症和微生物感染等疾病。
• [EN] INGENOL-3-ACYLATES III AND INGENOL-3-CARBAMATES<br/>[FR] INGÉNOL-3-ACYLATES III ET INGÉNOL-3-CARBAMATES
  申请人：LEO PHARMA AS

  公开号：WO2012083953A1

  公开（公告）日：2012-06-28

  The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is -NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use -alone or in combination with one or more other pharmaceutically active compounds- in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.

  该发明涉及一般式I的化合物，其中R为杂环芳基，可选择地由R7取代；或R为杂环烷基或杂环烯基，可选择地由R8取代；或R为X，其中X为-NR11R12；以及其在治疗中的药物可接受的盐、水合物或溶剂合物，用于单独使用或与一个或多个其他药用活性化合物结合在一起，用于预防、治疗或改善对中性粒细胞氧化爆发的刺激响应、对角质细胞IL-8释放的刺激响应或对坏死诱导的刺激响应的疾病或症状。
• [EN] SATURATED QUINOXALINE DERIVATIVES AND THEIR USE AS METABOTROPIC GLUTAMATE RECEPTOR LIGANDS<br/>[FR] DERIVES DE QUINOXALINE SATURES ET LEUR UTILISATION EN TANT QUE LIGANDS DU RECEPTEUR DU GLUTAMATE METABOTROPIQUE
  申请人：ASTRAZENECA AB

  公开号：WO2004069813A1

  公开（公告）日：2004-08-19

  The present invention relates to new compounds of formula (I), wherein Q is a partially saturated ring or Nl-oxides, salts, solvates or solvated salts thereof, processes for their preparation and new intermediates used in the preparation thereof and to the use of said compounds as metabotropic glutamate receptors ligands in therapy.

  本发明涉及公式（I）的新化合物，其中Q是部分饱和环或N-氧化物，其盐、溶剂合物或溶剂化合物盐，以及其制备工艺和用于制备中的新中间体，以及将所述化合物用作治疗中的代谢型谷氨酸受体配体。