3-methyl-3-(1-methyl-1H-indol-3-yl)butanoic acid | 184434-24-0

• 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: 3-methyl-3-(1-methyl-1H-indol-3-yl)butanoic acid
• 英文别名: 3-methyl-3-(1-methylindol-3-yl)butanoic acid
• CAS: 184434-24-0
• 化学式: C₁₄H₁₇NO₂
• 分子量: 231.294
• InChiKey: OIOWKQLTKUTLBG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  42.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  3-methyl-3-(1-methyl-1H-indol-3-yl)butanoic acid 在 过氧化氢,锂盐(1:1) 、 2,4,6-三异丙基苯磺酰叠氮化物 、 双(三甲基硅烷基)氨基钾 、 三乙胺 、 柠檬酸 、 tin(ll) chloride 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 水 为溶剂， 反应 68.02h， 生成 (2S)-2-[N-(tert-butyloxycarbonyl)amino]-3-methyl-3-(1-methylindol-3-yl)butanoic acid
  参考文献：
  名称：

  （-）-半胱氨酸的全合成，这是一种结构新颖的三肽，具有强力的细胞毒活性

  摘要：

  描述了（-）-半胱氨酸（2）的总合成，这是一种结构新颖的天然存在的三肽，对人乳腺癌MCF7细胞表现出有效的细胞毒性和抗有丝分裂活性。

  DOI：

  10.1016/s0040-4039(96)02335-0
• 作为产物：
  描述：

  methyl 2-methyl-2-(1-methyl-1H-indol-3-yl)propanoate 在 sodium chlorite 、 sodium dihydrogenphosphate 、 四丙基高钌酸铵 、 2-甲基-2-丁烯 、 4 A molecular sieve 、 水 、 二异丁基氢化铝 、 对甲苯磺酸 、 N-甲基吗啉氧化物 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 乙醚 、 二氯甲烷 、 水 、 叔丁醇 为溶剂， 反应 16.0h， 生成 3-methyl-3-(1-methyl-1H-indol-3-yl)butanoic acid
  参考文献：
  名称：

  （-）-半胱氨酸的全合成，这是一种结构新颖的三肽，具有强力的细胞毒活性

  摘要：

  描述了（-）-半胱氨酸（2）的总合成，这是一种结构新颖的天然存在的三肽，对人乳腺癌MCF7细胞表现出有效的细胞毒性和抗有丝分裂活性。

  DOI：

  10.1016/s0040-4039(96)02335-0

文献信息

• CYCLIC AMIDE DERIVATIVES AS INHIBITORS OF 11 - BETA - HYDROXYSTEROID DEHYDROGENASE AND USES THEREOF
  申请人：CONNEXIOS LIFE SCIENCES PVT. LTD.

  公开号：US20150158860A1

  公开（公告）日：2015-06-11

  The present invention relates to certain amide derivatives that have the ability to inhibit 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.

  本发明涉及某些酰胺衍生物，这些衍生物具有抑制11-β-羟基类固醇脱氢酶1型（11β-HSD-1）的能力，因此在预防和治疗可以通过抑制该酶来预防或治疗的某些疾病中是有用的。此外，发明还涉及这些化合物的制备方法、含有这些化合物的药物组合物以及这些化合物在治疗某些疾病中的用途。预计本发明的化合物将在治疗非胰岛素依赖型2型糖尿病（NIDDM）、胰岛素抵抗、肥胖、空腹血糖受损、葡萄糖耐量受损、脂质紊乱（如血脂异常）、高血压以及其他疾病和状况中找到应用。
• [EN] CYCLIC AMIDE DERIVATIVES AS INHIBITORS OF 11 - BETA - HYDROXYSTEROID DEHYDROGENASE AND USES THEREOF<br/>[FR] DÉRIVÉS D'AMIDE CYCLIQUES À UTILISER EN TANT QU'INHIBITEURS DE 11-BÊTA-HYDROXYSTÉROÏDE DÉSHYDROGÉNASE ET UTILISATIONS DE CEUX-CI
  申请人：CONNEXIOS LIFE SCIENCES PVT LTD

  公开号：WO2013128465A1

  公开（公告）日：2013-09-06

  The present invention relates to certain amide derivatives that have the ability to inhibit 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.

  本发明涉及某些酰胺衍生物，这些衍生物具有抑制11-β-羟基类固醇脱氢酶1型（11β-HSD-1）的能力，因此在预防或治疗可通过抑制该酶来预防或治疗的某些疾病中是有用的。此外，本发明还涉及这些化合物的制备方法、含有这些化合物的药物组合物以及这些化合物在治疗某些疾病中的用途。预计本发明的化合物将用于治疗非胰岛素依赖型2型糖尿病（NIDDM）、胰岛素抵抗、肥胖、空腹血糖受损、葡萄糖耐量受损、脂质紊乱（如血脂异常）、高血压以及其它疾病和状况。
• [EN] DERIVATIVES OF AZA ADAMANTANE AND USES THEREOF<br/>[FR] DÉRIVÉS D'AZA-ADAMANTANE ET LEURS UTILISATIONS
  申请人：CONNEXIOS LIFE SCIENCES PVT LTD

  公开号：WO2013111150A1

  公开（公告）日：2013-08-01

  The present invention relates to certain amide derivatives that have the ability to inhibit 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.

  本发明涉及某些酰胺衍生物，具有抑制11-β-羟基类固醇脱氢酶1型（11β-HSD-1）的能力，因此在预防或治疗可以通过抑制该酶而预防或治疗的某些疾病方面具有用处。此外，本发明涉及这些化合物、其制备方法、含有这些化合物的药物组合物以及这些化合物在治疗某些疾病中的用途。预计本发明的化合物将在治疗非胰岛素依赖型2型糖尿病（NIDDM）、胰岛素抵抗、肥胖、空腹血糖受损、糖耐量受损、脂质紊乱如血脂异常、高血压以及其他疾病和病症的治疗中发挥作用。
• DERIVATIVES OF AZA ADAMANTANE AND USES THEREOF
  申请人：CONNEXIOS LIFE SCIENCES PVT. LTD.

  公开号：US20150141650A1

  公开（公告）日：2015-05-21

  The present invention relates to certain amide derivatives that have the ability to inhibit 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.

  本发明涉及某些酰胺衍生物，具有抑制11-β-羟基类固醇脱氢酶1型（11β-HSD-1）的能力，因此在预防或治疗可以通过抑制该酶而预防或治疗的某些疾病方面具有用处。此外，本发明涉及这些化合物、其制备方法、含有这些化合物的药物组合物以及这些化合物在治疗某些疾病中的用途。预计本发明的化合物将在治疗非胰岛素依赖型2型糖尿病（NIDDM）、胰岛素抵抗、肥胖、空腹血糖受损、糖耐量受损、脂质紊乱如血脂异常、高血压以及其他疾病和病症的治疗中发挥作用。
• DERIVATIVES OF AZA ADAMANTANES AND USES THEREOF
  申请人：Connexios Life Sciences Pvt. Ltd.

  公开号：EP3266783A1

  公开（公告）日：2018-01-10

  The present invention relates to certain amide derivatives that have the ability to inhibit 11-beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.

  本发明涉及某些酰胺衍生物，这些衍生物具有抑制11-beta-羟基类固醇脱氢酶1型（11β-HSD-1）的能力，因此可用于治疗某些可通过抑制该酶来预防或治疗的疾病。此外，本发明还涉及这些化合物、其制备方法、含有这些化合物的药物组合物以及这些化合物在治疗某些疾病中的用途。预计本发明的化合物将应用于治疗非胰岛素依赖型 2 型糖尿病（NIDDM）、胰岛素抵抗、肥胖、空腹血糖受损、糖耐量受损、血脂紊乱（如血脂异常）、高血压以及其他疾病和病症。