1-Methyl-decahydro-1,6-naphthyridine | 933733-46-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 1-Methyl-decahydro-1,6-naphthyridine
• 英文别名: 1-methyl-3,4,4a,5,6,7,8,8a-octahydro-2H-1,6-naphthyridine
• CAS: 933733-46-1
• 化学式: C₉H₁₈N₂
• 分子量: 154.25
• InChiKey: KAWCNZLKKVCXSN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  15.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• 3-ARYL-5-SUBSTITUTED-ISOQUINOLIN-1-ONE COMPOUNDS AND THEIR THERAPEUTIC USE
  申请人：INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)

  公开号：US20150099732A1

  公开（公告）日：2015-04-09

  The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2H-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. 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 PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc.

  本发明通常涉及治疗化合物领域。更具体地，本发明涉及某些3-芳基-5-取代-2H-异喹啉-1-酮化合物，该化合物在抑制PARP（例如PARP1，TNKS1，TNKS2等）和/或Wnt信号传导方面具有作用。本发明还涉及包含这些化合物的药物组合物，以及利用这些化合物和组合物，在体内和体外，来抑制PARP（例如PARP1，TNKS1，TNKS2等）；抑制Wnt信号传导；治疗通过抑制PARP（例如PARP1，TNKS1，TNKS2等）改善的疾病；治疗通过抑制Wnt信号传导改善的疾病；治疗癌症等增生症状。
• [EN] 3-ARYL-5-SUBSTITUTED-ISOQUINOLIN-1-ONE COMPOUNDS AND THEIR THERAPEUTIC USE<br/>[FR] COMPOSÉS DE 3-ARYLISOQUINOL-1-ONE 5-SUBSTITUÉE ET LEUR UTILISATION THÉRAPEUTIQUE
  申请人：CANCER RES INST ROYAL

  公开号：WO2015036759A1

  公开（公告）日：2015-03-19

  The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted- 2/-/-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. 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 PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc. Formula (I)

  本发明涉及治疗化合物领域。更具体地，本发明涉及某些3-芳基-5-取代-2/-/-异喹啉-1-酮化合物，该化合物在抑制PARP（例如PARP1、TNKS1、TNKS2等）和/或Wnt信号传导方面具有作用。本发明还涉及包含此类化合物的药物组合物，以及使用这些化合物和组合物在体外和体内抑制PARP（例如PARP1、TNKS1、TNKS2等）；抑制Wnt信号传导；治疗通过抑制PARP（例如PARP1、TNKS1、TNKS2等）改善的疾病；治疗通过抑制Wnt信号传导改善的疾病；治疗增生性疾病如癌症等。公式（I）
• [EN] AMIDO-THIOPHENE COMPOUNDS AND THEIR USE<br/>[FR] COMPOSÉS AMIDO-THIOPHÈNE ET LEUR UTILISATION
  申请人：UNIV EDINBURGH

  公开号：WO2009112845A1

  公开（公告）日：2009-09-17

  The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11 β-hydroxysteroid dehydrogenase type 1 (11 β-HSD1 ). 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 11 β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11 β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.

  本发明一般涉及治疗化合物领域。更具体地，本发明涉及某些酰胺-噻吩化合物，其中包括抑制11β-羟基类固醇脱氢酶1（11β-HSD1）的作用。本发明还涉及包含这些化合物的药物组合物，以及使用这些化合物和组合物，在体内和体外，抑制11β-羟基类固醇脱氢酶1；治疗通过抑制11β-羟基类固醇脱氢酶1而得到改善的疾病；治疗代谢综合征，其中包括糖尿病和肥胖等疾病，以及相关疾病，包括胰岛素抵抗、高血压、脂质紊乱和心血管疾病，如缺血性（冠状）心脏病；治疗中枢神经系统疾病，如轻度认知障碍和早期痴呆，包括阿尔茨海默病等。
• 6-(4-Hydroxy-phenyl)-3-alkyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
  申请人：SANOFI

  公开号：US20130085128A1

  公开（公告）日：2013-04-04

  The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式I的吡唑并[3,4-b]吡啶化合物，其中R1、R2、R3、R4、R5、R6和R7如下所示。式I的化合物是激酶抑制剂，适用于治疗与糖尿病及糖尿病并发症相关的疾病，如糖尿病肾病、糖尿病神经病变和糖尿病视网膜病变等。此外，本发明还涉及式I的化合物的用途，特别是作为药物中的活性成分以及包含它们的药物组合物。
• [EN] AMIDO-ISOTHIAZOLE COMPOUNDS AND THEIR USE AS INHIBITORS OF 11BETA-HSD1 FOR THE TREATMENT OF METABOLIC SYNDROME AND RELATED DISORDERS<br/>[FR] COMPOSÉS AMIDO-ISOTHIAZOLE ET LEUR UTILISATION COMME INHIBITEURS DE LA 11 ?-HSD1 DANS LE TRAITEMENT DU SYNDROME MÉTABOLIQUE ET DES TROUBLES APPARENTÉS
  申请人：UNIV EDINBURGH

  公开号：WO2010146338A1

  公开（公告）日：2010-12-23

  The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-isothiazole compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). 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 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.

  本发明涉及治疗化合物领域。更具体地，本发明涉及某些酰胺异硫唑化合物，其中包括抑制11β-羟基类固醇脱氢酶1（11β-HSD1）。本发明还涉及包含这些化合物的药物组合物，以及使用这些化合物和组合物，无论在体外还是体内，来抑制11β-羟基类固醇脱氢酶1；治疗通过抑制11β-羟基类固醇脱氢酶1得到改善的疾病；治疗代谢综合征，其中包括疾病，如2型糖尿病和肥胖症，以及相关疾病，包括胰岛素抵抗、高血压、血脂紊乱和心血管疾病，如缺血性（冠状动脉）心脏病；治疗中枢神经系统疾病，如轻度认知障碍和早期痴呆，包括阿尔茨海默病等。