(3R,3aR,6aR)-hexahydro-2H-furo[3,2-b]pyrrol-3-ol | 927958-60-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 呋喃吡咯
• 英文名称: (3R,3aR,6aR)-hexahydro-2H-furo[3,2-b]pyrrol-3-ol
• 英文别名: (3R,3aR,6aR)-3,3a,4,5,6,6a-hexahydro-2H-furo[3,2-b]pyrrol-3-ol
• CAS: 927958-60-9
• 化学式: C₆H₁₁NO₂
• 分子量: 129.159
• InChiKey: CDMLEMBRAYSSJQ-KVQBGUIXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.9
• 重原子数：
  9
• 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：
  41.5
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (3R,3aR,6aR)-hexahydro-2H-furo[3,2-b]pyrrol-3-ol 、 Boc-L-环戊基甘氨酸 在 N-甲基吗啉 、 1-羟基苯并三唑 、 O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 3.42h， 生成 tert-butyl (S)-1-cyclopentyl-2-((3R,3aR,6aR)-3-hydroxydihydro-2H-furo[3,2-b]pyrrol-4(5H,6H,6aH)-yl)-2-oxoethylcarbamate
  参考文献：
  名称：

  WO2008/7132

  摘要：

  公开号：
• 作为产物：
  描述：

  (3R,3aR,6R,6aS)-3-hydroxyhexahydro-2H-furo[3,2-b]pyrrol-6-yl 4-methylbenzenesulfonate 在 lithium aluminium tetrahydride 作用下， 以 四氢呋喃 、 乙醚 为溶剂， 反应 18.75h， 生成 (3R,3aR,6aR)-hexahydro-2H-furo[3,2-b]pyrrol-3-ol
  参考文献：
  名称：

  WO2008/7132

  摘要：

  公开号：

文献信息

• [EN] TETRAHYDROFURO [3, 2-B] PYRROL-3-ONE DERIVATIVES AS INHIBITORS OF CYSTEINE PROTEASES<br/>[FR] DÉRIVÉS DE TÉTRAHYDROFURO[3,2-B]PYRROL-3-ONE COMME INHIBITEURS DE CYSTÉINE PROTÉASES
  申请人：AMURA THERAPEUTICS LTD

  公开号：WO2009144450A1

  公开（公告）日：2009-12-03

  A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein one of R1 and R2 is H, and the other is selected fromC1-8-alkyl, C3-6-cycloalkyl and C1-8-alkyl-C5-10-aryl; R3 is selected from tert-butyl, cyclopentyl and 1-methylcyclopentyl; R9 is selected from the following: (F). The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of various diseases.

  一种具有式（I）的化合物，或其药学上可接受的盐、水合物、络合物或前药，其中R1和R2中的一个是H，另一个选自C1-8-烷基、C3-6-环烷基和C1-8-烷基-C5-10-芳基；R3选自叔丁基、环戊基和1-甲基环戊基；R9选自以下内容：（F）。本发明还涉及包括式（I）化合物的药物组合物，以及利用这些化合物治疗各种疾病。
• Furo[3,2-B]pyrrol-3-one derivatives and their use as cysteinyl proteinase inhibitors
  申请人：Amura Therapeutics Limited

  公开号：US07846935B2

  公开（公告）日：2010-12-07

  The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: X is CH or N; and R4 is optionally substituted C3-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.

  本发明涉及公式（I）的化合物及其药学上可接受的盐，其中：X为CH或N；以及R4为可选择取代的C3-8烷基或可选择取代的C3-8环烷基。本发明还涉及包含公式（I）化合物的制药组合物，以及在治疗骨质疏松症、帕盖特病、查加斯病、疟疾、牙龈疾病、高血钙症、代谢性骨病、涉及基质或软骨降解的疾病以及骨癌疾病如骨转移和相关疼痛中使用这种化合物的用途。
• Furo[3, 2-b] pyrrol derivatives
  申请人：Amura Therapeutics Limited

  公开号：US07737150B2

  公开（公告）日：2010-06-15

  The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R3 is tert-butylmethyl, sec-butyl or tert-butyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.

  本发明涉及式(I)的化合物及其药学上可接受的盐，其中：R3为叔丁基甲基、仲丁基或叔丁基；X为CH或N；R4为可选取代的C1-8烷基或可选取代的C3-8环烷基。本发明还涉及含有式(I)化合物的制药组合物，以及在治疗从骨质疏松症、帕盖特病、恶性贫血、疟疾、牙龈疾病、高钙血症、代谢性骨病、涉及基质或软骨降解的疾病以及骨癌性疾病如骨转移和相关疼痛方面使用这些化合物的方法。
• FURO[3. 2-B] PYRROL DERIVATIVES
  申请人：Quibell Martin

  公开号：US20100216811A1

  公开（公告）日：2010-08-26

  The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R 3 is tert-butylmethyl, sec-butyl or tert-butyl; X is CH or N; and R 4 is optionally substituted C 1-8 alkyl or optionally substituted C 3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.

  本发明涉及式（I）的化合物及其药学上可接受的盐，其中：R3是叔丁基甲基、仲丁基或叔丁基；X是CH或N；R4是可选取代的C1-8烷基或可选取代的C3-8环烷基。本发明还涉及包含式（I）的化合物的药物组合物，以及将这些化合物用于治疗从骨质疏松症、帕盖特病、查加斯病、疟疾、牙龈疾病、高钙血症、代谢性骨病、涉及基质或软骨降解的疾病，以及骨癌疾病，如骨转移和相关疼痛。
• Furo[3,2-B] pyrrol-3-one derivatives and their use as cysteinyl proteinase inhibitors
  申请人：Amura Therapeutics Limited

  公开号：US07846934B2

  公开（公告）日：2010-12-07

  The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof (I), wherein: R3 is cyclopentyl or cyclohexyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.

  本发明涉及公式（I）的化合物及其药学上可接受的盐（I），其中：R3为环戊基或环己基；X为CH或N；R4为可选取取代的C1-8烷基或可选取取代的C3-8环烷基。本发明还涉及包含公式（I）化合物的制药组合物，以及在治疗骨质疏松症、帕盖特病、查加斯病、疟疾、牙龈疾病、高钙血症、代谢性骨病、涉及基质或软骨降解的疾病以及骨癌等疾病的治疗中使用这些化合物的用途。