(N-((1 S)-3-{(2Z)-2-[(4R)-3,4-dimethyl-1,3-thiazolidin-2-ylidene]hydrazino}-2,3-dioxo-1-(tetrahydro-2H-pyran-4-yl)propyl)cycloheptanecarboxamide) | 868273-90-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氧烷类
• 英文名称: (N-((1 S)-3-{(2Z)-2-[(4R)-3,4-dimethyl-1,3-thiazolidin-2-ylidene]hydrazino}-2,3-dioxo-1-(tetrahydro-2H-pyran-4-yl)propyl)cycloheptanecarboxamide)
• 英文别名: ONO-5334；Unii-9tdn93L9FN；N-[(1S)-3-[(2Z)-2-[(4R)-3,4-dimethyl-1,3-thiazolidin-2-ylidene]hydrazinyl]-1-(oxan-4-yl)-2,3-dioxopropyl]cycloheptanecarboxamide
• CAS: 868273-90-9；620614-15-5
• 化学式: C₂₁H₃₄N₄O₄S
• 分子量: 438.591
• InChiKey: BTZCSXIUAFVRTE-CHGLIHOBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  30
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.81
• 拓扑面积：
  125
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• Diketohydrazine derivative compounds and drugs contaiing the compounds as the active ingredient
  申请人：Hatayama Akira

  公开号：US20060111303A1

  公开（公告）日：2006-05-25

  The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).

  本发明涉及一种公式（I）的二酮肼衍生物及其药学上可接受的盐（公式中的符号与说明书中描述的含义相同）。公式（I）的化合物具有对半胱氨酸蛋白酶的抑制活性，可用于治疗炎症性疾病、免疫性疾病、缺血性疾病、呼吸系统疾病、循环系统疾病、血液疾病、神经系统疾病、肝胆系统疾病、骨骼或关节疾病、代谢性疾病等。该化合物具有对弹性蛋白酶的抑制活性，也可用于慢性阻塞性肺疾病（COPD）的治疗。
• BONE DENSIFYING AGENT CHARACTERIZED BY USE OF CATHEPSIN K INHIBITOR WITH PTH
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1741441A1

  公开（公告）日：2007-01-10

  The present invention relates to an agent for increasing BMD characterized by use of a cathepsin K inhibitor as a bone resorption inhibitor in combination with a type of PTH as a bone formation stimulator. This agent for increasing BMD is useful for the treatment of osteoporosis, bone fracture, arthritis, rheumatoid arthritis, osteoarthritis, hypercalcemia, osteometastasis of carcinoma, periodontal disease, bone Paget's disease and other bone metabolic diseases. For example, as the cathepsin K inhibitor, there can be mentioned a compound of formula (W) and a salt thereof, etc.

  本发明涉及一种增加 BMD 的制剂，其特征是使用一种作为骨吸收抑制剂的 cathepsin K 抑制剂与一种作为骨形成刺激剂的 PTH 结合使用。这种增加 BMD 的制剂可用于治疗骨质疏松症、骨折、关节炎、类风湿性关节炎、骨关节炎、高钙血症、癌的骨转移、牙周病、骨 Paget 病和其他骨代谢疾病。例如，作为 cathepsin K 抑制剂，可以提及式（W）化合物及其盐等。
• DIKETOHYDRAZINE DERIVATIVE COMPOUNDS AND DRUGS CONTAINING THE COMPOUNDS AS THE ACTIVE INGREDIENT
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1498411B1

  公开（公告）日：2013-01-16
• 2,3-DIHYDRO-6-NITROIMIDAZO[2,1-b]OXAZOLES
  申请人：OTSUKA PHARMACEUTICAL CO., LTD.

  公开号：EP1555267B1

  公开（公告）日：2013-01-16
• Bone Densifying Agent Characterized By Use Of Cathepsin K Inhibitor With Pth
  申请人：Ochi Yasuo

  公开号：US20070238769A1

  公开（公告）日：2007-10-11

  The present invention relates to an agent for increasing BMD characterized by use of a cathepsin K inhibitor as a bone resorption inhibitor in combination with a type of PTH as a bone formation stimulator. This agent for increasing BMD is useful for the treatment of osteoporosis, bone fracture, arthritis, rheumatoid arthritis, osteoarthritis, hypercalcemia, osteometastasis of carcinoma, periodontal disease, bone Paget's disease and other bone metabolic diseases. For example, as the cathepsin K inhibitor, there can be mentioned a compound of formula (W) and a salt thereof, etc.