2-甲基-2-吗啉-4-基丙-1-醇 | 858197-58-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 中文名称: 2-甲基-2-吗啉-4-基丙-1-醇
• 英文名称: 2-methyl-2-morpholinopropan-1-ol
• 英文别名: 2-methyl-2-(morpholin-4-yl)propan-1-ol；2-Methyl-2-(4-morpholinyl)-1-propanol；2-methyl-2-morpholin-4-ylpropan-1-ol
• CAS: 858197-58-7
• 化学式: C₈H₁₇NO₂
• mdl: MFCD11053919
• 分子量: 159.228
• InChiKey: FCCWRGFCAKZCBF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  32.7
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2934999090
• WGK Germany：
  3
• 储存条件：
  室温

反应信息

• 作为反应物：
  描述：

  2-甲基-2-吗啉-4-基丙-1-醇 在 三乙胺 作用下， 以 二氯甲烷 、 甲苯 为溶剂， 生成 3-[(RS)-1-((SR)-2-methylamino-4-oxo-4,5-dihydro-thiazol-5-yl)-ethyl]-indole-1-carboxylic acid 2-methyl-2-morpholin-4-yl-propyl ester
  参考文献：
  名称：

  Easily hydrolyzable, water-soluble derivatives of (.+-.)-.alpha.-5-[1-(indol-3-yl)ethyl]-2-methylamino-.DELTA.2-thiazolin-4-one, a novel antiviral compound

  摘要：

  The preparation of a series of indole N-acyl and N-carbamic esters of (+/-)-alpha-5-[1-(indol-3-yl)ethyl]-2-methylamino-delta2-thiazolin-4-one (1) is reported. These derivatives were synthesized as potential water-soluble precursors of the antiviral thiazolinone 1, for evaluation by intranasal administration against influenza and other respiratory infections caused by viruses. Salts of the basic carbamic esters (16--19) possess the required water solubility, undergo rapid hydrolysis and decarboxylation at pH values greater than 6, and have high activity against influenza A2 and Coxsackie B1 viruses in vitro. In influenza A2 infected ferrets a representative ester (16) reduced the severity and duration of disease symptoms and reduced nasal wash virus titres but caused local irritancy.

  DOI：

  10.1021/jm00188a013
• 作为产物：
  描述：

  ethyl α-methyl-2-morpholinopropionate 在 lithium aluminium tetrahydride 作用下， 以 四氢呋喃 为溶剂， 生成 2-甲基-2-吗啉-4-基丙-1-醇
  参考文献：
  名称：

  [EN] COMPOUNDS
  [FR] COMPOSÉS

  摘要：

  本发明涉及抑制LRRK2激酶活性的新化合物，其制备方法，含有它们的组合物，以及它们在治疗或预防由LRRK2激酶活性特征的疾病中的应用，例如帕金森病、阿尔茨海默病和肌萎缩侧索硬化症（ALS）。

  公开号：

  WO2015113452A1

文献信息

• DIHYDROPYRIDAZINE-3,5-DIONE DERIVATIVE AND PHARMACEUTICALS CONTAINING THE SAME
  申请人：CHUGAI SEIYAKU KABUSHIKI KAISHA

  公开号：US20160002251A1

  公开（公告）日：2016-01-07

  The present invention provides a dihydropyridazine-3,5-dione derivative or a salt thereof, or a solvate of the compound or the salt, a pharmaceutical drug, a pharmaceutical composition, a sodium-dependent phosphate transporter inhibitor, and a preventive and/or therapeutic agent for hyperphosphatemia, secondary hyperparathyroidism, chronic renal failure, chronic kidney disease, and arteriosclerosis associated with vascular calcification comprising the compound as an active ingredient, and a method for prevention and/or treatment.

  本发明提供了一种二氢吡啶嗪-3,5-二酮衍生物或其盐，或化合物或盐的溶剂化合物，一种药物，一种药物组合物，一种钠依赖性磷酸盐转运体抑制剂，以及作为活性成分的化合物的高磷血症、继发性甲状旁腺功能亢进症、慢性肾功能衰竭、慢性肾病和与血管钙化相关的动脉硬化的预防和/或治疗剂，以及预防和/或治疗的方法。
• [EN] 4H-PYRROLO[3,2-C]PYRIDIN-4-ONE DERIVATIVES<br/>[FR] DÉRIVÉS DE 4H-PYRROLO[3,2-C]PYRIDIN-4-ONE
  申请人：BAYER AG

  公开号：WO2020216774A1

  公开（公告）日：2020-10-29

  Compounds of formula (I) for use in the treatment or prophylaxis of a disease, which is a hyperproliferative disease and/or a disorder responsive to induction of cell death, selected from a haematological tumour, a solid tumour and/or metastases thereof, said tumour harbouring a mutant EGFR with exon 19 or 21 mutations, and their use as pharmaceuticals.

  式(I)的化合物用于治疗或预防一种高增殖性疾病和/或对诱导细胞死亡敏感的疾病，所述疾病选自血液肿瘤、实体肿瘤和/或其转移瘤，所述肿瘤携带具有外显子19或21突变的突变EGFR，并将其用作药物。
• DIHYDROPYRIDAZINE-3,5-DIONE DERIVATIVE
  申请人：Chugai Seiyaku Kabushiki Kaisha

  公开号：EP2975030A1

  公开（公告）日：2016-01-20

  The present invention provides a dihydropyridazine-3,5-dione derivative or a salt thereof, or a solvate of the compound or the salt, a pharmaceutical drug, a pharmaceutical composition, a sodium-dependent phosphate transporter inhibitor, and a preventive and/or therapeutic agent for hyperphosphatemia, secondary hyperparathyroidism, and chronic renal failure, comprising the compound as an active ingredient, and a method for prevention and/or treatment.

  本发明提供了一种二氢哒嗪-3,5-二酮衍生物或其盐，或该化合物或该盐的溶液剂、一种药物、一种药物组合物、一种钠依赖性磷酸盐转运体抑制剂，以及一种预防和/或治疗高磷血症、继发性甲状旁腺功能亢进症和慢性肾功能衰竭的药物，其中包含该化合物作为活性成分，以及一种预防和/或治疗方法。
• PHARMACEUTICAL CONTAINING SODIUM-DEPENDENT PHOSPHATE TRANSPORTER INHIBITOR AND PHOSPHORUS ADSORBENT FOR USE IN THE PREVENTION, TREATMENT OR SUPPRESSION OF CHRONIC KIDNEY DISEASE, ARTERIOSCLEROSIS ASSOCIATED WITH VASCULAR CALCIFICATION, OR ECTOPIC CALCIFICATION.
  申请人：Chugai Seiyaku Kabushiki Kaisha

  公开号：EP3928779A1

  公开（公告）日：2021-12-29

  The present invention provides a pharmaceutical composition containing, as an active ingredient, a dihydropyridazine-3,5-dione derivative or a salt thereof or a solvate of these, wherein the composition is administered in combination with a phosphorus adsorbent.

  本发明提供了一种药物组合物，其活性成分为二氢哒嗪-3,5-二酮衍生物或其盐或其溶液，其中该组合物与磷吸附剂结合使用。
• Compounds as LRRK2 kinase inhibitors
  申请人：GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

  公开号：US10087186B2

  公开（公告）日：2018-10-02

  The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of or prevention of diseases characterized by LRRK2 kinase activity, for example Parkinson's disease, Alzheimer's disease and amyotrophic lateral sclerosis (ALS).

  本发明涉及抑制 LRRK2 激酶活性的新型化合物、其制备工艺、含有这些化合物的组合物以及它们在治疗或预防以 LRRK2 激酶活性为特征的疾病（例如帕金森病、阿尔茨海默病和肌萎缩性脊髓侧索硬化症（ALS））中的用途。