2-azabicyclo[4.2.0]octane | 278-33-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 2-azabicyclo[4.2.0]octane
• CAS: 278-33-1
• 化学式: C₇H₁₃N
• mdl: MFCD13178705
• 分子量: 111.187
• InChiKey: JRDCSGYCSVDPPK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  8
• 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：
  12
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  2-azabicyclo[4.2.0]octane 、 (E)-4-bromo-N-(4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)but-2-enamide 在 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基乙酰胺 为溶剂， 反应 7.0h， 以42%的产率得到(E)-4-(2-azabicyclo[4.2.0]octan-2-yl)-N-(4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)but-2-enamide
  参考文献：
  名称：

  [EN] AMINOQUINAZOLINE DERIVATIVES AND THEIR SALTS AND METHODS OF USE THEREOF
  [FR] DÉRIVÉS D'AMINOQUINAZOLINE, LEURS SELS ET LEURS PROCÉDÉS D'UTILISATION

  摘要：

  本文提供了氨基喹唑啉化合物、盐及其用途。这些化合物具有式(I)，或其立体异构体、几何异构体、互变异构体、N-氧化物、水合物、溶剂合物、代谢物、药学上可接受的盐或其前药。本文还提供了含有上述化合物的药物组合物，以及利用这些化合物或组合物预防、管理、治疗或减轻患者体内增殖性疾病的严重程度，并调节蛋白酪氨酸激酶活性的用途。

  公开号：

  WO2014177038A1
• 作为产物：
  描述：

  Cyclobutapyridin 生成 2-azabicyclo[4.2.0]octane
  参考文献：
  名称：

  THUMMEL R. P.; KOHLI D. K., D1J. ORG. CHEM., 1978, 43, NO 25, 4882-4884

  摘要：

  DOI：

文献信息

• OXINDOLE COMPOUNDS CARRYING A CO-BOUND SPIRO SUBSTITUENT AND USE THEREOF FOR TREATING VASOPRESSIN-RELATED DISEASES
  申请人：AbbVie Deutschland GmbH & Co. KG

  公开号：US20150344489A1

  公开（公告）日：2015-12-03

  The present invention relates to novel substituted oxindole derivatives of formula I wherein the variables are as defined in the claims and the description. The invention further relates to pharmaceutical compositions comprising compounds I and their use for the treatment of vasopressin-related disorders.

  本发明涉及公式I的新型取代氧吲哚衍生物，其中变量如权利要求和描述中所定义。该发明还涉及包含化合物I的药物组合物，以及它们用于治疗与加压素相关的疾病。
• 6-(4-Hydroxy-phenyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
  申请人：SANOFI

  公开号：US20130150340A1

  公开（公告）日：2013-06-13

  The present invention relates to 1H-pyrazolo[3,4-b]pyridine compounds of the formula I, in which R 1 , R 2 , R 3 and R 4 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1H-吡唑并[3,4-b]吡啶化合物，其中R1、R2、R3和R4如下所示。式I的化合物是激酶抑制剂，对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，具有用处。此外，本发明还涉及将式I的化合物用作药物中的活性成分，以及包含它们的药物组合物。
• [EN] 6-(4-HYDROXY-PHENYL)-1H-PYRAZOLO[3,4-B]PYRIDINE-4-CARBOXYLIC ACID AMIDE DERIVATIVES AS KINASE INHIBITORS<br/>[FR] DÉRIVÉS D'AMIDE DE L'ACIDE 6-(4-HYDROXY-PHÉNYL)-1H-PYRAZOLO[3,4-B]PYRIDINE-4-CARBOXYLIQUE EN TANT QU'INHIBITEURS DE KINASES
  申请人：SANOFI SA

  公开号：WO2013060636A1

  公开（公告）日：2013-05-02

  The present invention relates to 1 H-pyrazolo[3,4-b]pyridine compounds of the formula (I) in which R1, R2, R3 and R4 are defined as indicated below. The compounds of the formula I are protein kinase C (PKC) 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, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式(I)的1H-吡唑并[3,4-b]吡啶化合物，其中R1、R2、R3和R4的定义如下所示。式I的化合物是蛋白激酶C（PKC）抑制剂，对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，具有益处。此外，本发明还涉及利用该式化合物，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] HETEROCYCLIC DERIVATIVES AS IAP BINDING COMPOUNDS<br/>[FR] DÉRIVÉS HÉTÉROCYCLIQUES CONVENANT COMME COMPOSÉS SE LIANT AUX INHIBITEURS DE PROTÉINES D'APOPTOSE
  申请人：NUEVOLUTION AS

  公开号：WO2009152824A1

  公开（公告）日：2009-12-23

  The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, solvates thereof, that bind to Inhibitor of Apoptosis Proteins (IAPs). The compounds of the invention may be used as diagnostic and therapeutic agents in the treatment of proliferative diseases, such as cancer, for promoting apoptosis in proliferating cells, and for sensitizing cells to inducers of apoptosis. The present invention furthermore provides a polymeric compound of formulas (VI) or (VII), comprising either at least two monomeric units of compounds of formula (I), or at least one monomeric unit of a compound of formula (I) and an entity E. The present invention further relates to pharmaceutical compositions comprising said compounds of formulas (I), (VI), and (VII) and the use of said compounds in medicine.

  本发明涉及式(I)的化合物，或其药学上可接受的盐、溶剂化合物，这些化合物与凋亡抑制蛋白(IAPs)结合。本发明的化合物可用作诊断和治疗剂，用于治疗增殖性疾病，如癌症，促进增殖细胞中的凋亡，并使细胞对凋亡诱导剂敏感。本发明还提供了具有式(VI)或(VII)的聚合物化合物，包括至少两个式(I)化合物的单体单位，或至少一个式(I)化合物的单体单位和实体E。本发明还涉及包含所述式(I)、(VI)和(VII)化合物的药物组合物以及在医学中使用所述化合物的用途。
• [EN] BENZOIMIDAZOLE-CARBOXYLIC ACID AMIDE DERIVATIVES AS APJ RECEPTOR MODULATORS<br/>[FR] DÉRIVÉS D'AMIDE D'ACIDE BENZIMIDAZOLE-CARBOXYLIQUE UTILISÉS COMME MODULATEURS DU RÉCEPTEUR APJ
  申请人：SANOFI SA

  公开号：WO2014044738A1

  公开（公告）日：2014-03-27

  The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R', R", R"', R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The compounds of the formula I are APJ receptor modulators, and are useful for the treatment of diseases associated with increased blood pressure 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.

  本发明涉及公式I的苯并咪唑羧酸酰胺化合物，其中R'、R"、R"'、R1、R2、R3、R4、R5、R6和Z如下所示定义。公式I的化合物是APJ受体调节剂，可用于治疗与增高血压相关的疾病。此外，本发明还涉及将公式I的化合物用作药物中的活性成分，以及包含它们的药物组合物。