8-Tert-butyl-2-oxa-8-azaspiro[3.5]nonane

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 8-Tert-butyl-2-oxa-8-azaspiro[3.5]nonane
• 英文别名: 8-tert-butyl-2-oxa-8-azaspiro[3.5]nonane
• 化学式: C₁₁H₂₁NO
• 分子量: 183.29
• InChiKey: QYHSHZSGYYSYAJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  13
• 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：
  12.5
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• QUINAZOLINE DERIVATIVE AS TYROSINE-KINASE INHIBITOR, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
  申请人：Wu Frank

  公开号：US20140161801A1

  公开（公告）日：2014-06-12

  The invention relates to a quinazoline derivative represented by the general formula (I), a pharmaceutical acceptable salt and a stereoisomer thereof as tyrosine kinase inhibitor, wherein R 1 , R 2 , R 3 , R 3′ , R 4 , R 5 , R 6 , X, L, T, Z and q are as defined in the specification. The invention also relates to a process for preparing the same, a pharmaceutical composition and a pharmaceutical formulation containing the derivative, use of the derivative for treating excessive proliferative diseases and chronic obstructive pulmonary disease and use of the derivative in the manufacture of a medicament for treating excessive proliferative diseases and chronic obstructive pulmonary disease.

  该发明涉及一种喹唑啉衍生物，其通式表示为(I)，作为酪氨酸激酶抑制剂的药用可接受盐和立体异构体，其中R1、R2、R3、R3'、R4、R5、R6、X、L、T、Z和q如规范中所定义。该发明还涉及一种制备该衍生物的方法，包含该衍生物的药用组合物和药用配方，以及将该衍生物用于治疗过度增殖性疾病和慢性阻塞性肺病，以及将该衍生物用于制造用于治疗过度增殖性疾病和慢性阻塞性肺病的药物。
• N-(4-(AZAINDAZOL-6-YL)-PHENYL)-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS
  申请人：SANOFI

  公开号：US20160024097A1

  公开（公告）日：2016-01-28

  The present invention relates to N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides of the formula I, wherein Ar, n, X, Z, R1, R2 and R3 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式I中的N-(4-(氮杂吲唑-6-基)-苯基)-磺酰胺，其中Ar、n、X、Z、R1、R2和R3在权利要求中指定了它们的含义。式I化合物是有价值的药理活性化合物，可以调节蛋白激酶活性，特别是血清和糖皮质激素调节激酶（SGK）的活性，特别是血清和糖皮质激素调节激酶亚型1（SGK-1，SGK1）的活性，并适用于治疗SGK活性不当的疾病，例如退行性关节疾病或炎症过程，如骨关节炎或风湿病。此外，本发明还涉及制备式I化合物的方法，它们作为药物的用途以及包含它们的制剂。
• Triazoles for the treatment of demyelinating dieases
  申请人：Vertex Pharmaceuticals Incorporated

  公开号：US10766869B2

  公开（公告）日：2020-09-08

  The invention relates to triazole compounds of formula I and I′ or pharmaceutically acceptable salts thereof, useful as modulators of demyelinating diseases: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention, methods of using the compositions and kits thereof in the treatment of various demyelinating and neurodegenerative diseases, including multiple sclerosis.

  本发明涉及式 I 和 I′ 的三唑化合物或其药学上可接受的盐类，可用作脱髓鞘疾病的调节剂： 本发明还提供了包含本发明化合物的药学上可接受的组合物、使用组合物的方法及其试剂盒，用于治疗各种脱髓鞘和神经退行性疾病，包括多发性硬化症。
• 1,3-DIARYL-SUBSTITUTED HETEROCYCLIC PESTICIDES
  申请人：E I DU PONT DE NEMOURS AND COMPANY

  公开号：US20140249025A1

  公开（公告）日：2014-09-04

  Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Q is and Z 1 , Z 2 , J 1 , J 2 , M, R 1a , R 1b , R 2a , R 2b , R 2c , R 2d and R 14 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
• TRIAZOLES FOR THE TREATMENT OF DEMYELINATING DISEASES
  申请人：Vertex Pharmaceuticals Incorporated

  公开号：US20160355488A1

  公开（公告）日：2016-12-08

  The invention relates to triazole compounds of formula I and I′ or pharmaceutically acceptable salts thereof, useful as modulators of demyelinating diseases: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention, methods of using the compositions and kits thereof in the treatment of various demyelinating and neurodegenerative diseases, including multiple sclerosis.