(2S,4R)-methanesulfonic acid 2-tert-butoxycarbonylamino-5-methanesulfonyloxy-4-methyl-pentyl ester | 1203651-05-1

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机磺酸及其衍生物
• 英文名称: (2S,4R)-methanesulfonic acid 2-tert-butoxycarbonylamino-5-methanesulfonyloxy-4-methyl-pentyl ester
• 英文别名: (2S,4R)-2-((tert-butoxycarbonyl)amino)-4-methylpentane-1,5-diyl dimethanesulfonate；[(2R,4S)-2-methyl-4-[(2-methylpropan-2-yl)oxycarbonylamino]-5-methylsulfonyloxypentyl] methanesulfonate
• CAS: 1203651-05-1
• 化学式: C₁₃H₂₇NO₈S₂
• 分子量: 389.491
• InChiKey: NQPSKPGQESKQCB-MNOVXSKESA-N

物化性质

• 沸点：
  588.9±45.0 °C(Predicted)
• 密度：
  1.252±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  24
• 可旋转键数：
  11
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.92
• 拓扑面积：
  142
• 氢给体数：
  1
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  (2S,4R)-methanesulfonic acid 2-tert-butoxycarbonylamino-5-methanesulfonyloxy-4-methyl-pentyl ester 在 palladium 10% on activated carbon 、 氢气 、 铁粉 、 溶剂黄146 、 N,N-二异丙基乙胺 、 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 作用下， 以 乙醇 、 水 、 N,N-二甲基甲酰胺 为溶剂， 20.0~130.0 ℃ 、344.75 kPa 条件下， 反应 22.0h， 生成 tert-butyl (3S,5R)-5-methyl-1-(3-(2-propylthieno[3,2-b]pyridine-5-carboxamido)pyridin-4-yl)piperidin-3-ylcarbamate
  参考文献：
  名称：

  [EN] BICYCLIC HETEROAROMATIC CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS
  [FR] COMPOSÉS CARBOXAMIDE HÉTÉROAROMATIQUES BICYCLIQUES UTILES EN TANT QU'INHIBITEURS DE KINASES PIM

  摘要：

  本公开说明描述了式（I）的双环杂芳基羧酰胺衍生物，以及它们的组合物和使用方法。这些化合物抑制Pim激酶的活性，并且在治疗与Pim激酶活性相关的疾病方面具有用途，例如癌症和其他疾病。

  公开号：

  WO2016010897A1
• 作为产物：
  描述：

  L-焦谷氨酸甲酯 在 4-二甲氨基吡啶 lithium hexamethyldisilazane 作用下， 以 四氢呋喃 、 乙酸乙酯 为溶剂， 反应 7.75h， 生成 (2S,4R)-methanesulfonic acid 2-tert-butoxycarbonylamino-5-methanesulfonyloxy-4-methyl-pentyl ester
  参考文献：
  名称：

  [EN] BICYCLIC PYRIDAZINE COMPOUNDS AS PIM INHIBITORS
  [FR] COMPOSÉS PYRIDAZINES BICYCLIQUES EN TANT QU'INHIBITEURS DE PIM

  摘要：

  该发明涉及公式I和I'的双环化合物及其盐。在某些实施例中，该发明涉及Pim-1和/或Pim-2以及/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。在更进一步的实施例中，该发明涉及包含本文披露的化合物的药物组合物，以及它们在预防和治疗Pim激酶相关疾病和病症，尤其是癌症中的应用。

  公开号：

  WO2012148775A1

文献信息

• THIAZOLECARBOXAMIDES AND PYRIDINECARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS
  申请人：Incyte Corporation

  公开号：US20140200227A1

  公开（公告）日：2014-07-17

  The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.

  本公开描述了噻唑和吡啶羧酰胺衍生物，它们的组成以及使用方法。这些化合物抑制Pim激酶的活性，并且在治疗与Pim激酶活性相关的疾病方面具有用途，例如癌症和其他疾病。
• [EN] CHEMICAL COMPOUNDS<br/>[FR] COMPOSÉS CHIMIQUES
  申请人：GLAXOSMITHKLINE LLC

  公开号：WO2010059658A1

  公开（公告）日：2010-05-27

  The invention is directed to 6-(4-pyιϊmidinyl)-1 H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R1 - R4 are defined herein. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

  这项发明涉及6-(4-吡咯嗪基)-1 H-吲唑衍生物。具体而言，该发明涉及符合式(I)的化合物，其中R1-R4在此处被定义。该发明的化合物是PDK1的抑制剂，可用于治疗由于恒定激活的ACG激酶所特征化的免疫和代谢性疾病和紊乱，如癌症，更具体地说是乳腺癌、结肠癌和肺癌。因此，该发明进一步涉及包括该发明化合物的药物组合物。该发明还进一步涉及使用该发明化合物或包括该发明化合物的药物组合物来抑制PDK1活性和治疗相关疾病的方法。
• CHEMICAL COMPOUNDS
  申请人：Axten Jeffrey Michael

  公开号：US20110275611A1

  公开（公告）日：2011-11-10

  The invention is directed to 6-(4-pyrimidinyl)-1H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R 1 -R 4 are defined herein. The compounds of the invention axe inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention

  本发明涉及6-(4-嘧啶基)-1H-吲唑衍生物。具体而言，本发明涉及公式（I）中R1-R4所定义的化合物。本发明的化合物是PDK1的抑制剂，可用于治疗免疫和代谢性疾病和障碍，这些疾病和障碍以恒定激活的ACG激酶为特征，例如乳腺、结肠和肺癌等。因此，本发明还涉及包含本发明化合物的制药组合物。本发明还涉及使用本发明化合物或包含本发明化合物的制药组合物抑制PDK1活性和治疗相关障碍的方法。
• ANTIBIOTIC DRUG
  申请人：Hsu Ming-Chu

  公开号：US20120157492A1

  公开（公告）日：2012-06-21

  This invention relates to a malic acid salt of (3S,5R)-7-[3-amino-5-methyl-piperidinyl]-1-cyclopropyl-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid. Also disclosed is a method of treating bacterial infection by an effective amount of this salt.

  本发明涉及(3S,5R)-7-[3-氨基-5-甲基哌啶基]-1-环丙基-1,4-二氢-8-甲氧基-4-氧代-3-喹啉羧酸的苹果酸盐。本发明还公开了一种通过有效量的该盐治疗细菌感染的方法。
• Bicyclic Pyridazine Compounds as PIM Inhibitors
  申请人：D'amico Derin C.

  公开号：US20140221344A1

  公开（公告）日：2014-08-07

  The invention relates to bicyclic compounds of formulas I and I′, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.

  本发明涉及式I和I'的双环化合物及其盐。在某些实施例中，本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。在更进一步的实施例中，本发明涉及包含所述化合物的制药组合物，以及它们在预防和治疗Pim激酶相关疾病和病症，尤其是癌症方面的应用。