2-Hydroxyamino-chinolin | 18714-33-5

• 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-Hydroxyamino-chinolin
• 英文别名: N-quinolin-2-yl-hydroxylamine；Hydroxyaminoquinoline；N-quinolin-2-ylhydroxylamine
• CAS: 18714-33-5
• 化学式: C₉H₈N₂O
• 分子量: 160.175
• InChiKey: MZQHXMNGFZYJKA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  45.2
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• [EN] ARYL-QUINOLYL COMPOUNDS AND THEIR USE<br/>[FR] COMPOSÉS ARYL-QUINOLÉYLE ET LEUR UTILISATION
  申请人：CANCER REC TECH LTD

  公开号：WO2009130487A1

  公开（公告）日：2009-10-29

  The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain aryl-quinolyl compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.

  本发明一般涉及治疗增殖性疾病、癌症等的治疗化合物领域，更具体地涉及本文所述的某些芳基喹啉化合物，该化合物在诸多方面抑制了RAF（例如B-RAF）活性。本发明还涉及包含这种化合物的药物组合物，以及利用这种化合物和组合物在体外和体内抑制RAF（例如BRAF）活性，抑制受体酪氨酸激酶（RTK）活性，抑制细胞增殖，并用于治疗通过抑制RAF、RTK等而得到改善的疾病和疾病，如癌症（例如结直肠癌、黑色素瘤）等。
• 1-acyl-2,3-dihydro-4(1H)-quinolinone-4-oxime derivatives, process for producing them and use thereof
  申请人：MOCHIDA PHARMACEUTICAL CO., LTD.

  公开号：EP0315115A2

  公开（公告）日：1989-05-10

  The present invention relates to novel 1-acyl-2,3-dihydro-4(1H)-quinoiinone-4-oxime-0-sulfonic acid compound, processes for producing said compounds, intermediate compounds to produce said compounds and compositions containing said compounds with potent diuretic activity that can be used for treating and/or preventing hypertension, oedema and/or for removing ascites. The present invention is based on the selection of 1-acyl-7-halo-2,3-dihydro-4(1H)-quinolinone-4-oxime-O-sulfonic acid compounds, namely heterocyclic-or fused heterocyclic- carbonyl derivatives at 1 position. The compounds of the present invention containing these substituents have potent hypotensive, anti- oedematous and diuretic effect as well as an activity to remove ascites and are extremely useful for the treatment of diseases and disorders mentioned above.

  本发明涉及新型1-酰基-2,3-二氢-4(1H)-喹啉酮-4-肟-0-磺酸化合物、生产所述化合物的工艺、生产所述化合物的中间化合物和含有所述化合物的组合物，所述化合物具有强效利尿活性，可用于治疗和/或预防高血压、水肿和/或去除腹水。 本发明的基础是选择 1-酰基-7-卤-2,3-二氢-4(1H)-喹啉酮-4-肟-O-磺酸化合物，即 1 位上的杂环或融合杂环羰基衍生物。 含有这些取代基的本发明化合物具有强效降血压、抗水肿和利尿作用，并具有清除腹水的活性，对治疗上述疾病和失调极为有用。
• 1-acyl-2,3-dihydro-4(1H)-quinolinone-4-oxime derivative, process for the production thereof, pharmaceutical composition and intermediates
  申请人：MOCHIDA PHARMACEUTICAL CO., LTD.

  公开号：EP0243982B1

  公开（公告）日：1991-04-17
• ARYL-QUINOLYL COMPOUNDS AND THEIR USE
  申请人：Cancer Research Technology Limited

  公开号：EP2285805B1

  公开（公告）日：2014-07-23
• Aryl-Quinolyl Compounds and Their Use
  申请人：Niculescu-Duvaz Ion

  公开号：US20110053946A1

  公开（公告）日：2011-03-03

  The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain aryl-quinolyl compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.