t-butyl 5-chlorospiro[indoline-3,3'-pyrrolidine]-1'-carboxylate | 1172588-23-6

• 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: t-butyl 5-chlorospiro[indoline-3,3'-pyrrolidine]-1'-carboxylate
• 英文别名: tert-butyl 5-chlorospiro[indoline-3,3'-pyrrolidine]-1'-carboxylate；tert-butyl 5-chlorospiro[1,2-dihydroindole-3,3'-pyrrolidine]-1'-carboxylate
• CAS: 1172588-23-6
• 化学式: C₁₆H₂₁ClN₂O₂
• 分子量: 308.808
• InChiKey: SIZHVJPDRZVKGA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  41.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  t-butyl 5-chlorospiro[indoline-3,3'-pyrrolidine]-1'-carboxylate 、 三氟乙酸酐 在 吡啶 作用下， 以 二氯甲烷 为溶剂， 反应 0.17h， 以94%的产率得到t-butyl 5-chloro-1-(2,2,2-trifluoroacetyl)spiro[indoline-3,3'-pyrrolidine]-1'-carboxylate
  参考文献：
  名称：

  EP2781521

  摘要：

  公开号：
• 作为产物：
  描述：

  tert-butyl 5-chloro-2-oxospiro[indoline-3,3‘-pyrrolidine]-1‘-carboxylate 在 sodium tetrahydroborate 、 碘 、 水 、 氯化铵 作用下， 以 四氢呋喃 为溶剂， 以100%的产率得到t-butyl 5-chlorospiro[indoline-3,3'-pyrrolidine]-1'-carboxylate
  参考文献：
  名称：

  [EN] PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS
  [FR] PYRIMIDYL CYCLOPENTANES EN TANT QU'INHIBITEURS DE PROTÉINE KINASE AKT

  摘要：

  本发明提供了式（I）的化合物，包括互变异构体、已分离的对映体、已分离的非对映异构体、溶剂合物、代谢物、盐以及其药学上可接受的前药。本发明还提供了使用这些化合物作为Akt蛋白激酶抑制剂以及用于治疗Akt介导的疾病，例如，高增殖性疾病如癌症的方法。

  公开号：

  WO2009089454A1

文献信息

• PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS
  申请人：Banka Anna

  公开号：US20110053959A1

  公开（公告）日：2011-03-03

  The present invention provides compounds of Formula (I) including tautomers, resolved enantiomers, resolved diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as Akt protein kinase inhibitors and for the treatment of Akt-mediated diseases, for example, hyperproliferative diseases such as cancer.

  本发明提供了公式（I）的化合物，包括互变异构体、分离的对映体、分离的二对映异构体、溶剂化物、代谢物、盐和其药学上可接受的前药。还提供了使用本发明化合物作为Akt蛋白激酶抑制剂和用于治疗Akt介导的疾病（例如，癌症等增殖性疾病）的方法。
• Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
  申请人：Array Biopharma Inc.

  公开号：US08324221B2

  公开（公告）日：2012-12-04

  The present invention provides compounds of Formula (I) including tautomers, resolved enantiomers, resolved diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as Akt protein kinase inhibitors and for the treatment of Akt-mediated diseases, for example, hyperproliferative diseases such as cancer.

  本发明提供了Formula (I) 化合物，包括互变异构体、分离对映体、分离二对映异构体、溶剂化物、代谢产物、盐和药学上可接受的前药。同时，还提供了使用该发明中的化合物作为Akt蛋白激酶抑制剂和用于治疗Akt介导的疾病，例如，癌症等增生性疾病的方法。
• NOVEL SPIROINDOLINE COMPOUND, AND MEDICINAL AGENT COMPRISING SAME
  申请人：KOWA COMPANY, LTD.

  公开号：US20140309207A1

  公开（公告）日：2014-10-16

  The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic β-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R 1 and R 2 , which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C 1-6 alkyl group, a C 6-10 aryl group, a cyano group, a C 1-6 alkyl group optionally having a substituent, a C 2-6 alkenyl group optionally having a substituent, etc.; R 3 represents a hydrogen atom, a C 1-6 alkyl group optionally having a substituent, etc.; and R 4 represents a hydrogen atom, a halogen atom, a C 1-6 alkyl group optionally having a substituent, etc.]

  本发明提供了一种新型化合物，其通式（1）如下所示，具有在肝脏和胰岛β细胞中激活葡萄糖激酶的作用，并可用作预防和/或治疗由高血糖引起的疾病，如糖尿病的药物。该通式（1）表示的螺环吲哚化合物，或其盐，或化合物或盐的溶剂：[其中环A代表含氮的5-10成员杂环基；R1和R2，相同或不同，分别代表氢原子，卤原子，卤代C1-6烷基，C6-10芳基，氰基，C1-6烷基，可选取代基，C2-6烯基，可选取代基等；R3代表氢原子，C1-6烷基，可选取代基等；R4代表氢原子，卤原子，C1-6烷基，可选取代基等。]
• Spiroindoline compound, and medicinal agent comprising same
  申请人：Kowa Company, Ltd.

  公开号：US08921576B2

  公开（公告）日：2014-12-30

  The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic β-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.]

  本发明提供了一种新型化合物，其通式（1）如下所示，具有在肝脏和胰岛β细胞中激活葡萄糖激酶的作用，并且可用作预防和/或治疗由高血糖引起的疾病，如糖尿病的药物。通式（1）表示的螺内酰胺化合物，或其盐，或化合物或盐的溶剂:[其中，环A表示含氮的5-10成员杂环基；R1和R2，它们相同或不同，每个表示氢原子，卤原子，卤代C1-6烷基，C6-10芳基，氰基，可选有取代基的C1-6烷基，可选有取代基的C2-6烯基等；R3表示氢原子，可选有取代基的C1-6烷基等；R4表示氢原子，卤原子，可选有取代基的C1-6烷基等。]
• US8324221B2
  申请人：——

  公开号：US8324221B2

  公开（公告）日：2012-12-04