2-羟基-6-甲基-5,6,7,8-四氢-1,6-二氮杂萘 | 14757-35-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 2-羟基-6-甲基-5,6,7,8-四氢-1,6-二氮杂萘
• 英文名称: 6-methyl-5,6,7,8-tetrahydro-1,6-naphthyridin-2(1H)-one
• 英文别名: 6-methyl-1,5,7,8-tetrahydro-1,6-naphthyridin-2-one
• CAS: 14757-35-8
• 化学式: C₉H₁₂N₂O
• 分子量: 164.207
• InChiKey: YMIHNICOLWKMKW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  32.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-羟基-6-甲基-5,6,7,8-四氢-1,6-二氮杂萘 在 五氯化磷 、 三氯氧磷 、 sodium hydroxide 作用下， 以 水 为溶剂， 生成 2-chloro-6-methyl-7,8-dihydro-5H-1,6-naphthyridine
  参考文献：
  名称：

  [EN] TETRAHYDRONAPHTHYRIDINES AND AZA DERIVATIVES THEREOF AS HISTAMINE H3 RECEPTOR ANTAGONISTS
  [FR] TÉTRAHYDRONAPHTHYRIDINES ET SES DÉRIVÉS AZA À TITRE D'ANTAGONISTES DES RÉCEPTEURS D'HISTAMINE H3

  摘要：

  该发明涉及式(I)的化合物，其中X1a，X1至X5，Ra，Rb，n和R的含义如描述和权利要求中所述。所述化合物可用作组胺H3受体拮抗剂。该发明还涉及药物组合物，以及制备此类化合物的方法，以及作为药物的生产和使用。

  公开号：

  WO2009121812A1

文献信息

• [EN] COMPOUNDS AS CDK SMALL-MOLECULE INHIBITORS AND USES THEREOF<br/>[FR] COMPOSÉS EN TANT QUE PETITES MOLÉCULES INHIBITRICES DE LA CDK ET LEURS UTILISATIONS
  申请人：SUNSHINE LAKE PHARMA CO LTD

  公开号：WO2016015604A1

  公开（公告）日：2016-02-04

  The invention provides compounds as CDK small-molecule inhibitors and uses thereof, the compounds can be used for treating inflammation and cell proliferation diseases. The novel compound of the invention is a powerful cyclin-dependent kinase 4 (CDK 4) or cyclin-dependent kinase-6 (CDK 6) inhibitor.

  这项发明提供了作为CDK小分子抑制剂的化合物及其用途，这些化合物可用于治疗炎症和细胞增殖性疾病。该发明的新化合物是一种强效的细胞周期蛋白依赖激酶4（CDK 4）或细胞周期蛋白依赖激酶6（CDK 6）抑制剂。
• [EN] BICYCLIC COMPOUNDS AS AUTOTAXIN (ATX) AND LYSOPHOSPHATIDIC ACID (LPA) PRODUCTION INHIBITORS<br/>[FR] COMPOSÉS BICYCLIQUES EN TANT QU'INHIBITEURS DE PRODUCTION D'AUTOTAXINE (ATX) ET D'ACIDE LYSOPHOSPHATIDIQUE (LPA)
  申请人：HOFFMANN LA ROCHE

  公开号：WO2015144605A1

  公开（公告）日：2015-10-01

  The invention provides novel compounds having the general formula (I) wherein R1, R2, A, W, m, n, p and q are as described herein, compositions including the compounds. The compounds of formula (I) are useful as autotaxin (ATX) inhibitors which are inhibitors of lysophosphatidic acid (LPA) production and thus modulators of LPA levels and associated signaling; in particular they are useful for the treatment or prophylaxis of renal conditions, liver conditions, inflammatory conditions, conditions of the nervous system, conditions of the respiratory system, vascular and cardiovascular conditions, fibrotic diseases, cancer, ocular conditions, metabolic conditions, cholestatic and other forms of chronic pruritus and acute and chronic organ transplant rejection.

  该发明提供了具有通式（I）的新化合物，其中R1、R2、A、W、m、n、p和q如本文所述，包括这些化合物的组合物。通式（I）的化合物可用作自体税肽酶（ATX）抑制剂，这些抑制剂是溶磷脂酸（LPA）产生的抑制剂，从而调节LPA水平和相关信号传导；特别是它们可用于治疗或预防肾脏疾病、肝脏疾病、炎症性疾病、神经系统疾病、呼吸系统疾病、血管和心血管疾病、纤维化疾病、癌症、眼部疾病、代谢性疾病、胆汁淤积和其他形式的慢性瘙痒以及急性和慢性器官移植排斥反应的治疗。
• [EN] CONDENSED [1,4]DIAZEPINE COMPOUNDS AS AUTOTAXIN (ATX) AND LYSOPHOSPHATIDIC ACID (LPA) PRODUCTION INHIBITORS<br/>[FR] COMPOSÉS CONDENSÉS DE [1,4]DIAZÉPINE EN TANT QU'INHIBITEURS D'AUTOTAXINE (ATX) ET DE PRODUCTION D'ACIDE LYSOPHOSPHATIDIQUE (LPA)
  申请人：HOFFMANN LA ROCHE

  公开号：WO2015144609A1

  公开（公告）日：2015-10-01

  The invention provides novel compounds having the general formula (I) wherein R1, R2, A1 and A2 are as described herein, compositions including the compounds. These compounds of formula (I) are useful for therapy or prophylaxis in a mammal, and in particular to autotaxin (ATX) inhibitors which are inhibitors of lysophosphatidic acid (LPA) production and thus modulators of LPA levels and associated signaling, for the treatment or prophylaxis of renal conditions, liver conditions, inflammatory conditions, conditions of the nervous system, conditions of the respiratory system, vascular and cardiovascular conditions, fibrotic diseases, cancer, ocular conditions, metabolic conditions, cholestatic and other forms of chronic pruritus and acute and chronic organ transplant rejection.

  该发明提供了具有一般式（I）的新化合物，其中R1、R2、A1和A2如本文所述，包括这些化合物的组合物。这些一般式（I）的化合物对于治疗或预防哺乳动物特别是对于自动税酯酶（ATX）抑制剂是有用的，这些抑制剂是溶磷脂酸（LPA）产生的抑制剂，从而调节LPA水平和相关信号，用于治疗或预防肾脏疾病、肝脏疾病、炎症性疾病、神经系统疾病、呼吸系统疾病、血管和心血管疾病、纤维化疾病、癌症、眼部疾病、代谢性疾病、胆汁淤积和其他形式的慢性瘙痒以及急性和慢性器官移植排斥。
• Tetrahydronaphthyridine Derivatives
  申请人：Lunn Graham

  公开号：US20090258861A1

  公开（公告）日：2009-10-15

  The present invention relates to tetrahydronaphthyridine derivatives of the general formula (I): or of the general formula (I′) in which A and R 1 are as defined within, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, including the treatment diseases mediated by H3 ligands, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

  本发明涉及一般式(I)的四氢萘啉衍生物或一般式(I′)的四氢萘啉衍生物，其中A和R1如定义中所述，以及用于制备中间体，制备含有该衍生物的组合物，以及用于治疗由H3配体介导的疾病，特别是炎症、过敏和呼吸系统疾病、失调和状况的方法。
• TETRAHYDRONAPHTHYRIDINES AND AZA DERIVATIVES THEREOF AS HISTAMINE H3 RECEPTOR ANTAGONISTS
  申请人：Davenport Adam James

  公开号：US20110046130A1

  公开（公告）日：2011-02-24

  The invention relates to compounds of formula (I), wherein X 1a , X 1 to X 5 , R a , R b , n and R have the meaning as cited in the description and the claims. Said compounds are useful as Histamine H3 receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.

  本发明涉及化合物的公式（I），其中X1a、X1至X5、Ra、Rb、n和R的含义如所述及权利要求所述。所述化合物可用作组胺H3受体拮抗剂。本发明还涉及制药组合物，制备这种化合物以及作为药物的生产和使用。