2-(溴甲基)-5,8-二氧杂螺[3.4]辛烷 | 1057641-71-0

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 2-(溴甲基)-5,8-二氧杂螺[3.4]辛烷
• 中文别名: 2-溴甲基-5,8-二氧杂螺[3.4]辛烷
• 英文名称: 2-(bromomethyl)-5,8-dioxaspiro[3.4]octane
• CAS: 1057641-71-0
• 化学式: C₇H₁₁BrO₂
• 分子量: 207.067
• InChiKey: MKHPFTGDMWUGRW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  18.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-(溴甲基)-5,8-二氧杂螺[3.4]辛烷 在 polyethylene glycol 、 sodium hydroxide 作用下， 以 水 、 苯 为溶剂， 反应 12.0h， 以33%的产率得到2-亚甲基5,8-二氧杂螺[3.4]辛烷
  参考文献：
  名称：

  WO2008/111010

  摘要：

  公开号：
• 作为产物：
  描述：

  5,8-二氧杂螺[3.4]辛-2-基甲醇 在 四溴化碳 、 三苯基膦 作用下， 以 二氯甲烷 为溶剂， 反应 6.0h， 以39.4%的产率得到2-(溴甲基)-5,8-二氧杂螺[3.4]辛烷
  参考文献：
  名称：

  WO2008/111010

  摘要：

  公开号：

文献信息

• Pyrazolo (3, 4-B) pyridine derivatives as phosphodiesterase inhibitors
  申请人：Rudra Sonali

  公开号：US08420666B2

  公开（公告）日：2013-04-16

  The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4/PDE type 7 inhibitors. Compounds disclosed herein having the structure of Formula 1: can be useful in the treatment, prevention, inhibition or suppression of CNS diseases, for example, multiple sclerosis; various pathological conditions such as diseases affecting the immune system, including AIDS, rejection of transplant, auto-immune disorders such as T-cell related diseases, for example, rheumatoid arthritis; inflammatory diseases such as respiratory inflammation diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchitis, allergic rhinitis, adult respiratory distress syndrome (ARDS) and other inflammatory diseases including but not limited to psoriasis, shock, atopic dermatitis, eosinophilic granuloma, allergic conjunctivitis, osteoarthritis; gastrointestinal inflammation diseases such as Crohn's disease, colitis, pancreatitis as well as different types of cancers including leukaemia; especially in humans. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type 4, PDE type 7 and dual PDE type 4/PDE type 7 inhibitors are provided.

  本发明涉及磷酸二酯酶（PDE）类型4、磷酸二酯酶（PDE）类型7和双重PDE类型4/PDE类型7抑制剂。本文所披露的结构为式1的化合物可用于治疗、预防、抑制或抑制中枢神经系统疾病，例如多发性硬化症；各种影响免疫系统的病理条件，包括艾滋病、移植排斥、自身免疫性疾病如T细胞相关疾病，例如类风湿性关节炎；炎症性疾病，如呼吸道炎症性疾病，包括慢性阻塞性肺疾病（COPD）、哮喘、支气管炎、过敏性鼻炎、成人呼吸窘迫综合症（ARDS）以及其他炎症性疾病，包括但不限于银屑病、休克、特应性皮炎、嗜酸性肉芽肿、过敏性结膜炎、骨关节炎；胃肠道炎症性疾病，如克罗恩病、结肠炎、胰腺炎以及不同类型的癌症，包括白血病；特别适用于人类。本文还提供了所披露的化合物的制备方法、含有所披露的化合物的制药组合物以及它们作为PDE类型4、PDE类型7和双重PDE类型4/PDE类型7抑制剂的用途。
• PYRAZOLO (3, 4-B) PYRIDINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
  申请人：Rudra Sonali

  公开号：US20100292196A1

  公开（公告）日：2010-11-18

  The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4/PDE type 7 inhibitors. Compounds disclosed herein having the structure of Formula 1: can be useful in the treatment, prevention, inhibition or suppression of CNS diseases, for example, multiple sclerosis; various pathological conditions such as diseases affecting the immune system, including AIDS, rejection of transplant, auto-immune disorders such as T-cell related diseases, for example, rheumatoid arthritis; inflammatory diseases such as respiratory inflammation diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchitis, allergic rhinitis, adult respiratory distress syndrome (ARDS) and other inflammatory diseases including but not limited to psoriasis, shock, atopic dermatitis, eosinophilic granuloma, allergic conjunctivitis, osteoarthritis; gastrointestinal inflammation diseases such as Crohn's disease, colitis, pancreatitis as well as different types of cancers including leukaemia; especially in humans. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type 4, PDE type 7 and dual PDE type 4/PDE type 7 inhibitors are provided.

  本发明涉及磷酸二酯酶（PDE）类型4、磷酸二酯酶（PDE）类型7和双重PDE类型4/PDE类型7抑制剂。本文所披露的具有公式1结构的化合物可以用于治疗、预防、抑制或抑制中枢神经系统疾病，例如多发性硬化症；各种影响免疫系统的病理条件，包括艾滋病、移植排斥、自身免疫性疾病（例如T细胞相关疾病，例如类风湿性关节炎）；炎症性疾病，例如呼吸道炎症性疾病，包括慢性阻塞性肺疾病（COPD）、哮喘、支气管炎、过敏性鼻炎、成人呼吸窘迫综合症（ARDS）以及其他炎症性疾病，包括但不限于牛皮癣、休克、特应性皮炎、嗜酸性肉芽肿、过敏性结膜炎、骨关节炎；胃肠道炎症性疾病，如克罗恩病、结肠炎、胰腺炎以及不同类型的癌症，包括白血病；特别是在人类中。提供了所披露的化合物的制备过程、含有所披露的化合物的药物组合物以及它们作为PDE类型4、PDE类型7和双重PDE类型4/PDE类型7抑制剂的用途。
• Pyrazolo[3,4-b]pyridine derivatives as phosphodiesterase inhibitors
  申请人：Ranbaxy Laboratories Limited

  公开号：EP2124944B1

  公开（公告）日：2012-02-15
• US8420666B2
  申请人：——

  公开号：US8420666B2

  公开（公告）日：2013-04-16
• [EN] PYRAZOLO (3, 4-B) PYRIDINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS<br/>[FR] DÉRIVÉS DE PYRAZOLO(3,4-B)PYRIDINE COMME INHIBITEURS DE PHOSPHODIESTÉRASE
  申请人：RANBAXY LAB LTD

  公开号：WO2008111010A1

  公开（公告）日：2008-09-18

  [EN] The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4 /PDE type 7 inhibitors. Compounds disclosed herein having the structure of Formura 1: can be useful in the treatment, prevention, inhibition or suppression of CNS diseases, for example, multiple sclerosis; various pathological conditions such as diseases affecting the immune system, including AIDS, rejection of transplant, auto-immune disorders such as T-cell related diseases, for example, rheumatoid arthritis; inflammatory diseases such as respiratory inflammation diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchitis, allergic rhinitis, adult respiratory distress syndrome (ARDS) and other inflammatory diseases including but not limited to psoriasis, shock, atopic dermatitis, eosinophilic granuloma, allergic conjunctivitis, osteoarthritis; gastrointestinal inflammation diseases such as Crohn's disease, colitis, pancreatitis as well as different types of cancers including leukaemia; especially in humans. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type 4, PDE type 7 and dual PDE type 4 /PDE type 7 inhibitors are provided.
  [FR] La présente invention porte sur des inhibiteurs de la phosphodiestérase (PDE) de type 4, la phosphodiestérase (PDE) de type 7 et la PDE de type 4/PDE de type 7 double. Les composés décrits ici ayant la structure représentée par la Formule 1 peuvent être utiles dans le traitement, la prévention, l'inhibition ou la suppression de maladies du système nerveux central, par exemple, la sclérose en plaques ; divers états pathologiques tels que des maladies affectant le système immunitaire, comprenant le SIDA, le rejet de greffe, des troubles auto-immuns tels que des maladies apparentées aux lymphocytes T, par exemple, la polyarthrite rhumatoïde ; des maladies inflammatoires telles que des maladies inflammatoires respiratoires comprenant la maladie pulmonaire obstructive chronique (COPD), l'asthme, la bronchite, la rhinite allergique, le syndrome de détresse respiratoire chez les adultes (ARDS) et d'autres maladies inflammatoires comprenant, mais sans y être limitées, le psoriasis, l'accident cérébro-vasculaire, la dermatite atopique, le granulome éosinophile, la conjonctivite allergique, l'ostéoarthrite ; les maladies inflammatoires gastro-intestinales telles que la maladie de Crohn, la colite, la pancréatite ainsi que différents types de cancers comprenant la leucémie, notamment chez les êtres humains. L'invention porte également sur des procédés pour la préparation des composés décrits, sur des compositions pharmaceutiques contenant les composés décrits, et sur leur utilisation en tant qu'inhibiteurs de la PDE de type 4, de la PDE de type 7 et de la PDE de type 4/PDE de type 7 double.