2-cyclopropylacetohydrazide | 55277-83-3

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 2-cyclopropylacetohydrazide
• CAS: 55277-83-3
• 化学式: C₅H₁₀N₂O
• mdl: MFCD11644083
• 分子量: 114.147
• InChiKey: GVPVKNZZLIICEQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  8
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  55.1
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-cyclopropylacetohydrazide 、 7-bromo-6,8-difluoro-3,3-dimethyl-3,4-dihydroquinoxaline-2(1H)-thione 在 溶剂黄146 作用下， 以 正丁醇 为溶剂， 反应 16.0h， 以79%的产率得到8-bromo-1-(cyclopropylmethyl)-7,9-difluoro-4,4-dimethyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoxaline
  参考文献：
  名称：

  [EN] SUBSTITUTED TRIAZOLO QUINOXALINE DERIVATIVES
  [FR] DÉRIVÉS DE TRIAZOLO-QUINOXALINE SUBSTITUÉS

  摘要：

  本发明涉及符合一般式(I)的化合物，其作为糖皮质激素受体的调节剂，并可用于治疗和/或预防至少部分由糖皮质激素受体介导的疾病。

  公开号：

  WO2020016453A1

文献信息

• [EN] CYCLOHEXYL ACID TRIAZOLE AZOLES AS LPA ANTAGONISTS<br/>[FR] AZOLES TRIAZOLES D'ACIDE CYCLOHEXYLE UTILISÉS EN TANT QU'ANTAGONISTES DE LPA
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2019126094A1

  公开（公告）日：2019-06-27

  The present invention provides compounds of Formula (I): Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

  本发明提供了化合物的结构式（I）：结构式（I）或其立体异构体、互变异构体或药学上可接受的盐或溶剂，其中所有变量如本文所定义。这些化合物是选择性LPA受体抑制剂。
• Imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepines as potent and highly selective GABAA α5 inverse agonists with potential for the treatment of cognitive dysfunction
  作者：Bernd Buettelmann、Theresa M. Ballard、Rodolfo Gasser、Holger Fischer、Maria-Clemencia Hernandez、Frédéric Knoflach、Henner Knust、Heinz Stadler、Andrew W. Thomas、Gerhard Trube

  DOI：10.1016/j.bmcl.2009.08.027

  日期：2009.10

  search for GABAA α5 ligands that combine high subtype binding selectivity with a marked inverse agonism imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepines were identified as a promising class. A short tandem reaction allowed rapid access to this chemical series, thereby facilitating rapid SAR generation which guided the optimization process. Two compounds (10e and 11f) were found to be active

  在用于GABA搜索甲α5的配体相结合的高亚型与标记反向激动咪唑并[1,5-结合选择性一个] [1,2,4] -三唑并[1,5- d ] [1,4]苯并二氮杂类是被确定为有前途的一类。短串联反应允许快速进入该化学序列，从而有助于快速生成SAR，从而引导了优化过程。发现两种化合物（10e和11f）在体内改善认知的范式中具有活性。
• Indazole compounds and methods of use thereof
  申请人：Bhagwat S. Shripad

  公开号：US20060004043A1

  公开（公告）日：2006-01-05

  This invention is directed to Indazole Compounds or pharmaceutically acceptable salts, solvates and hydrates thereof. The Indazole Compounds have utility in the treatment or prevention of a wide range of diseases and disorders that are responsive to the inhibition, modulation or regulation of kinases, such as inflammatory diseases, abnormal angiogenesis and diseases related thereto, cancer, atherosclerosis, a cardiovascular disease, a renal disease, an autoimmune condition, macular degeneration, disease-related wasting, an asbestos-related condition, pulmonary hypertension, diabetes, obesity, pain and others. Thus, methods of treating or preventing such diseases and disorders are also disclosed, as are pharmaceutical compositions comprising one or more of the Indazole Compounds. This invention is based, in part, upon the discovery of a novel class of 5-triazolyl substituted indazole molecules that have potent activity with respect to the modulation of protein kinases. Thus, the invention encompasses orally active molecules as well as parenterally active molecules which can be used at lower doses or serum concentrations for treating diseses or disorders associated with protein kinase signal transduction.

  本发明涉及吲唑化合物或其药学上可接受的盐、溶剂合物和水合物。这些吲唑化合物在治疗或预防广泛的疾病和紊乱方面具有实用性，这些疾病和紊乱对激酶的抑制、调节或调控具有反应性，例如炎症性疾病、异常血管生成及相关疾病、癌症、动脉硬化、心血管疾病、肾脏疾病、自身免疫疾病、黄斑变性、与疾病有关的消耗、石棉相关疾病、肺动脉高压、糖尿病、肥胖症、疼痛和其他疾病。因此，本发明还揭示了治疗或预防此类疾病和紊乱的方法，以及包含一种或多种吲唑化合物的药物组成物。本发明部分基于发现一类新型的5-三唑基取代吲唑分子，它们在蛋白激酶调节方面具有强效活性。因此，本发明包括口服活性分子以及可用于治疗与蛋白激酶信号转导相关的疾病或紊乱的肠外活性分子，其剂量或血清浓度较低。
• INDAZOLE COMPOUNDS AND METHODS OF USE THEREOF
  申请人：Bhagwat Shripad S.

  公开号：US20090099178A1

  公开（公告）日：2009-04-16

  This invention is directed to Indazole Compounds or pharmaceutically acceptable salts, solvates and hydrates thereof. The Indazole Compounds have utility in the treatment or prevention of a wide range of diseases and disorders that are responsive to the inhibition, modulation or regulation of kinases, such as inflammatory diseases, abnormal angiogenesis and diseases related thereto, cancer, atherosclerosis, a cardiovascular disease, a renal disease, an autoimmune condition, macular degeneration, disease-related wasting, an asbestos-related condition, pulmonary hypertension, diabetes, obesity, pain and others. Thus, methods of treating or preventing such diseases and disorders are also disclosed, as are pharmaceutical compositions comprising one or more of the Indazole Compounds. This invention is based, in part, upon the discovery of a novel class of 5-triazolyl substituted indazole molecules that have potent activity with respect to the modulation of protein kinases. Thus, the invention encompasses orally active molecules as well as parenterally active molecules which can be used at lower doses or serum concentrations for treating diseases or disorders associated with protein kinase signal transduction.

  本发明涉及吲唑化合物或其药学上可接受的盐、溶剂合物和水合物。这些吲唑化合物在治疗或预防许多对激酶的抑制、调节或调控具有反应性的疾病和障碍方面具有用途，例如炎症性疾病、异常血管生成及相关疾病、癌症、动脉粥样硬化、心血管疾病、肾脏疾病、自身免疫疾病、黄斑变性、与疾病相关的消耗、石棉相关疾病、肺动脉高压、糖尿病、肥胖症、疼痛等。因此，本发明还揭示了治疗或预防这些疾病和障碍的方法，以及包含一种或多种吲唑化合物的制药组合物。本发明部分基于发现一类新型的5-三唑基取代吲唑分子，这些分子在调节蛋白激酶方面具有强效活性。因此，本发明包括口服活性分子和经肠道给药的活性分子，可用于治疗与蛋白激酶信号转导相关的疾病或障碍，且可用较低剂量或血清浓度。
• [EN] SUBSTITUTED TRIAZOLO QUINOXALINE DERIVATIVES<br/>[FR] DÉRIVÉS DE TRIAZOLO-QUINOXALINE SUBSTITUÉS
  申请人：GRUENENTHAL GMBH

  公开号：WO2020016453A1

  公开（公告）日：2020-01-23

  The present invention relates to compounds according to general formula (I) which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.

  本发明涉及符合一般式(I)的化合物，其作为糖皮质激素受体的调节剂，并可用于治疗和/或预防至少部分由糖皮质激素受体介导的疾病。