(1-{2-[4-(2-ethyl-5-fluoro-1H-indol-3-yl)-piperidin-1-yl]-5-oxo-6,7-dihydro-5H-5λ⁴-thieno[3,2-d]pyrimidin-4-ylamino}-cyclopropyl)-methanol | 1146356-12-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: (1-{2-[4-(2-ethyl-5-fluoro-1H-indol-3-yl)-piperidin-1-yl]-5-oxo-6,7-dihydro-5H-5λ⁴-thieno[3,2-d]pyrimidin-4-ylamino}-cyclopropyl)-methanol
• 英文别名: [1-[[2-[4-(2-ethyl-5-fluoro-1H-indol-3-yl)piperidin-1-yl]-5-oxo-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl]amino]cyclopropyl]methanol
• CAS: 1146356-12-8
• 化学式: C₂₅H₃₀FN₅O₂S
• 分子量: 483.61
• InChiKey: YWMJCSQOAMJVMF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  34
• 可旋转键数：
  6
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  113
• 氢给体数：
  3
• 氢受体数：
  8

文献信息

• SUBSTITUTED PIPERAZINO-DIHYDROTHIENOPYRIMIDINES
  申请人：Pouzet Pascale

  公开号：US20110021501A1

  公开（公告）日：2011-01-27

  The invention relates to new piperidino-dihydrothienopyrimidines of formula 1, as well as pharmacologically acceptable salts thereof, wherein X is SO or SO 2 , but preferably SO, and wherein R 1 , R 2 , R 3 and R 4 may have the meanings given in claim 1 , as well as pharmaceutical compositions which contain these compounds. These new piperidino-dihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers.

  本发明涉及通式1的新哌啶二氢噻吩并嘧啶类化合物及其药理上可接受的盐，其中X为SO或SO2，优选SO，并且其中R1、R2、R3和R4可具有权利要求1中所述的含义，以及含有这些化合物的药物组合物。这些新哌啶二氢噻吩并嘧啶类化合物适用于治疗呼吸系统或胃肠道疾病、关节、皮肤或眼睛的炎症性疾病、周围或中枢神经系统疾病或癌症。
• DRUG COMBINATIONS CONTAINING PDE4 INHIBITORS AND NSAIDS
  申请人：Nickolaus Peter

  公开号：US20120035143A1

  公开（公告）日：2012-02-09

  The present invention relates to new drug combinations which contain in addition to one or more PDE4-inhibitors at least one NSAID (=non-steroidal anti-inflammatory drug) (2), processes for preparing them and their use in treating in particular respiratory complaints such as for example COPD, chronic sinusitis and asthma. The invention particularly relates to those drug combinations which contain, in addition to one or more, preferably one PDE4 inhibitor of general formula 1 wherein X is SO or SO 2 , but preferably SO, and wherein R 1 , R 2 , R 3 and R 4 have the meanings given in claim 1, at least one NSAID (2), the preparation thereof and the use thereof for the treatment of respiratory complaints.

  本发明涉及新的药物组合，除了包含一种或多种 PDE4 抑制剂外，还至少包含一种 NSAID（非甾体抗炎药）(2)，以及制备这些药物组合的方法及其在治疗特别是呼吸系统疾病如慢性阻塞性肺病（COPD）、慢性鼻窦炎和哮喘中的应用。本发明特别涉及那些药物组合，除了包含一种或多种，优选一种 PDE4 抑制剂，其通式为 1，其中 X 是 SO 或 SO2，但优选 SO，并且其中 R1、R2、R3 和 R4 具有权利要求 1 中给出的含义，还至少包含一种 NSAID (2)，其制备方法及其用于治疗呼吸系统疾病的使用。
• COMBINATIONS OF MEDICAMENTS, CONTAINING PDE4-INHIBITORS AND EP4-RECEPTOR-ANTAGONISTS
  申请人：Nickolaus Peter

  公开号：US20130225609A1

  公开（公告）日：2013-08-29

  The present invention relates to new medicament combinations which contain in addition to one or more PDE4-inhibitors (1) at least one EP4 receptor antagonist (2), as well as the use thereof for the treatment of preferably respiratory complaints such as particularly COPD, chronic sinusitis and asthma. The invention relates in particular to those medicament combinations which contain, in addition to one or more, preferably one, PDE4 inhibitor of general formula 1 wherein X is SO or SO 2 , but preferably SO, and wherein R 1 , R 2 , R 3 and R 4 have the meanings given in claim 1, at least one EP4 receptor antagonist (2), the preparation thereof and the use thereof for the treatment of respiratory complaints.

  本发明涉及新的药物组合物，其包含除了一个或多个PDE4抑制剂（1）之外，至少一个EP4受体拮抗剂（2），以及其用于治疗特别是呼吸系统疾病，如慢性阻塞性肺病（COPD）、慢性鼻窦炎和哮喘的用途。本发明特别涉及那些药物组合物，其除了一个或多个，优选一个，PDE4抑制剂的一般通式1之外，还包含至少一个EP4受体拮抗剂（2），其中X是SO或SO2，但优选SO，并且其中R1、R2、R3和R4具有权利要求1中给出的含义，所述组合物的制备及其用于治疗呼吸系统疾病的用途。
• SPECIFIC PDE4B-INHIBITORS FOR THE TREATMENT OF DIABETES MELLITUS
  申请人：Luippold Gerd

  公开号：US20140228286A1

  公开（公告）日：2014-08-14

  A method of treating diabetes mellitus or a microvascular or macrovascular complication of diabetes mellitus in a patient in need thereof, the method comprising administering to the patient a compound of formula 1 wherein R 1 , R 2 , R 3 , and R 4 are as defined in claim 1.

  一种治疗糖尿病或糖尿病微血管或宏血管并发症的方法，包括向需要治疗的患者注射公式1中的化合物，其中R1、R2、R3和R4如权利要求1所定义。
• COMBINATIONS OF MEDICAMENTS, CONTAINING PDE4-INHIBITORS AND EP4-RECEPTOR- ANTAGONISTS
  申请人：NICKOLAUS Peter

  公开号：US20140350035A1

  公开（公告）日：2014-11-27

  The present invention relates to new medicament combinations which contain in addition to one or more PDE4-inhibitors ( 1 ) at least one EP4 receptor antagonist ( 2 ), as well as the use thereof for the treatment of preferably respiratory complaints such as particularly COPD, chronic sinusitis and asthma. The invention relates in particular to those medicament combinations which contain, in addition to one or more, preferably one, PDE4 inhibitor of general formula 1 wherein X is SO or SO 2 , but preferably SO, and wherein R 1 , R 2 , R 3 and R 4 have the meanings given in claim 1, at least one EP4 receptor antagonist ( 2 ), the preparation thereof and the use thereof for the treatment of respiratory complaints.

  本发明涉及一种新的药物组合，除了一种或多种PDE4抑制剂（1）外，还包含至少一种EP4受体拮抗剂（2），以及其在治疗呼吸道疾病，如慢性阻塞性肺疾病、慢性鼻窦炎和哮喘等方面的应用。本发明特别涉及那些药物组合，除了一种或多种，首选一种通式1的PDE4抑制剂，其中X为SO或SO2，但优选为SO，R1、R2、R3和R4具有权利要求1中所给出的含义，还包含至少一种EP4受体拮抗剂（2），其制备和在治疗呼吸道疾病方面的应用。