(1S, 2S)-2-(1-methylhydrazino)-1-indanol | 488123-42-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚满类
• 英文名称: (1S, 2S)-2-(1-methylhydrazino)-1-indanol
• 英文别名: (1S,2S)-2-[amino(methyl)amino]-2,3-dihydro-1H-inden-1-ol
• CAS: 488123-42-8
• 化学式: C₁₀H₁₄N₂O
• 分子量: 178.234
• InChiKey: DYPFWPZTPLZNEM-UWVGGRQHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  49.5
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (1S, 2S)-2-(1-methylhydrazino)-1-indanol 、 L-酒石酸 以 乙醚 、 乙酸乙酯 为溶剂， 以68%的产率得到(1S,2S)-2-(1-methylhydrazino)-1-indanol (R, R)-tartrate
  参考文献：
  名称：

  JP2005/501035

  摘要：

  公开号：
• 作为产物：
  描述：

  (lS, 2S)-2-methylamino-N-nitroso-l-indanol 在 lithium aluminium tetrahydride 作用下， 以 四氢呋喃 为溶剂， 反应 3.0h， 以75%的产率得到(1S, 2S)-2-(1-methylhydrazino)-1-indanol
  参考文献：
  名称：

  JP2005/501035

  摘要：

  公开号：

文献信息

• [EN] VAP-1 INHIBITORS FOR TREATING PAIN<br/>[FR] INHIBITEURS DE VAP-1 POUR LE TRAITEMENT DE LA DOULEUR
  申请人：PROXIMAGEN LTD

  公开号：WO2017098236A1

  公开（公告）日：2017-06-15

  This invention relates to the use of inhibitors of VAP-1/SSAO activity, and pharmaceutical compositions comprising the same, for the treatment of pain; and to a combined preparation comprising an inhibitor of VAP-1/SSAO activity and a steroid, and the use of the combined preparation in medicine, particularly for treatment of pain.

  这项发明涉及使用VAP-1/SSAO活性抑制剂以及包含相同成分的药物组合物，用于治疗疼痛；以及包含VAP-1/SSAO活性抑制剂和类固醇的联合制剂，以及在医学中使用该联合制剂，特别是用于治疗疼痛。
• [EN] CARBOCYCLIC HYDRAZINO INHIBITORS OF COPPER-CONTAINING AMINE OXIDASES<br/>[FR] INHIBITEURS HYDRAZINO CARBOCYCLIQUES DES AMINE OXYDASES A TENEUR EN CUIVRE
  申请人：BIOTIE THERAPIES CORP

  公开号：WO2003006003A1

  公开（公告）日：2003-01-23

  The present invention is directed to carbocyclic hydrazino compounds that function as inhibitors of copper-containing amine oxidases commonly known as semicarbazide-sensitive amine oxidases (SSAO), including the human SSAO known as Vascular Adhesion Protein-1 (VAP-1). These SSAO inhibitors have therapeutic utility as drugs to treat conditions and diseases including, but not limited to, a number of inflammatory conditions and diseases (in particular chronic inflammatory conditions such as chronic arthritis, inflammatory bowel diseases, and chronic skin dermatoses), diseases related to carbohydrate metabolism and to aberrations in adipocyte differentiation or function and smooth muscle cell function, and vascular diseases. The novel compounds have the general formula: or a pharmaceutically acceptable solvate, hydrate, or salt thereof, wherein R?1 to R11¿ are as defined herein.

  本发明涉及碳环肼类化合物，作为含铜胺氧化酶（常称为半卡巴肼敏感的胺氧化酶（SSAO））的抑制剂，包括人类SSAO，即血管粘附蛋白-1（VAP-1）。这些SSAO抑制剂具有治疗作用，可用作药物治疗包括但不限于多种炎症状况和疾病（尤其是慢性炎症状况，如慢性关节炎、炎症性肠病和慢性皮肤病）、与碳水化合物代谢和脂肪细胞分化或功能异常以及平滑肌细胞功能相关的疾病以及血管疾病。新型化合物的一般式为：或其药学上可接受的溶剂、水合物或盐，其中R？1到R11？如本文所定义。
• Carbocyclic hydrazino inhibitors of copper-containing amine oxidases
  申请人：——

  公开号：US20040236108A1

  公开（公告）日：2004-11-25

  The present invention is directed to carbocyclic hydrazino compounds that function as inhibitors of copper-containing amine oxidases commonly known as semicarbazide-sensitive amine oxidases (SSAO), including the human SSAO known as Vascular Adhesion Protein-1 (VAP-1). These SSAO inhibitors have therapeutic utility as drugs to treat conditions and diseases including, but not limited to, a number of inflammatory conditions and diseases (in particular chronic inflammatory conditions such as chronic arthritis, inflammatory bowel diseases, and chronic skin dermatoses), diseases related to carbohydrate metabolism and to aberrations in adipocyte differentiation or function and smooth muscle cell function, and vascular diseases. The novel compounds have the general formula: 1 or a pharmaceutically acceptable solvate, hydrate, or salt thereof, wherein R 1 to R 11 are as defined herein.

  本发明涉及碳环酰肼化合物，其作为含铜胺氧化酶抑制剂，通常被称为半卡巴肼敏感胺氧化酶（SSAO）的抑制剂，包括人类SSAO，即血管黏附蛋白-1（VAP-1）。这些SSAO抑制剂具有治疗效用，可用作治疗条件和疾病的药物，包括但不限于多种炎症条件和疾病（特别是慢性炎症条件，如慢性关节炎，炎症性肠病和慢性皮肤皮疹），与碳水化合物代谢和脂肪细胞分化或功能异常以及平滑肌细胞功能和血管疾病有关的疾病。新型化合物的一般公式为：1或其药学上可接受的溶剂化合物、水合物或盐，其中R1到R11的定义如本文所述。
• HALOALLYLAMINE INHIBITORS OF SSAO/VAP-1 AND USES THEREFOR
  申请人：McDonald Ian A.

  公开号：US20100298330A1

  公开（公告）日：2010-11-25

  The present invention is related to the preparation and pharmaceutical In use of novel haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification:(I). The invention also relates to methods of using invention compounds, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases.

  本发明涉及一种具有I式结构的新型卤代烯丙胺衍生物的制备和药物应用，所述衍生物可作为SSAO/VAP-1抑制剂，I式结构如规范中定义。本发明还涉及使用本发明化合物或其药学上可接受的盐或衍生物的方法，用于治疗多种适应症，例如炎症性疾病。
• Use of VAP-1 inhibitors for treating fibrotic conditions
  申请人：BIOTIE THERAPIES CORP.

  公开号：US10576148B2

  公开（公告）日：2020-03-03

  The present invention relates to inhibitors of VAP-1 and their use as medicaments in treating fibrotic conditions. Furthermore, the present invention relates to a method of diagnosing a fibrotic condition on the basis of elevated level of soluble VAP-1 or SSAO activity in a bodily fluid, and to a kit for use in said diagnostic method.

  本发明涉及 VAP-1 的抑制剂及其在治疗纤维化病症中作为药物的用途。此外，本发明还涉及一种根据体液中可溶性 VAP-1 或 SSAO 活性水平升高来诊断纤维化病症的方法，以及用于上述诊断方法的试剂盒。