1-(2-methoxyethyl)-3-methyl-1H-pyrazol-4-amine | 1296307-33-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 1-(2-methoxyethyl)-3-methyl-1H-pyrazol-4-amine
• 英文别名: 1-(2-methoxyethyl)-3-methylpyrazol-4-amine
• CAS: 1296307-33-9
• 化学式: C₇H₁₃N₃O
• 分子量: 155.2
• InChiKey: VMVMLAPJMPSWAT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  11
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  53.1
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-(2-methoxyethyl)-3-methyl-1H-pyrazol-4-amine 在 ammonium thiocyanate 、 potassium carbonate 、 potassium hydrogencarbonate 、 SnCI_2.H₂O 作用下， 以 甲醇 、 乙醇 、 二氯甲烷 、 丙酮 为溶剂， 反应 24.5h， 生成 4-(4-aminophenyl)-N-(1-(2-methoxyethyl)-3-methyl-1H-pyrazol-4-yl)thiazol-2-amine
  参考文献：
  名称：

  TUBULIN POLYMERIZATION INHIBITORS

  摘要：

  The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt and/or solvate thereof, wherein B is an aryl or a five- or six-membered heteroaryl, and R1-R5, V, W, Y and Z may be various groups. The compounds according to the invention are useful as tubulin polymerization inhibitors, in particular for use in the treatment of hematological disorders and/or proliferative disorders.

  公开号：

  WO2024146923A1
• 作为产物：
  描述：

  1-(2-methoxyethyl)-3-methyl-4-nitro-1H-pyrazole 在 palladium 10% on activated carbon 、 一水合肼 作用下， 以 乙醇 为溶剂， 以7.1 g的产率得到1-(2-methoxyethyl)-3-methyl-1H-pyrazol-4-amine
  参考文献：
  名称：

  TUBULIN POLYMERIZATION INHIBITORS

  摘要：

  The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt and/or solvate thereof, wherein B is an aryl or a five- or six-membered heteroaryl, and R1-R5, V, W, Y and Z may be various groups. The compounds according to the invention are useful as tubulin polymerization inhibitors, in particular for use in the treatment of hematological disorders and/or proliferative disorders.

  公开号：

  WO2024146923A1

文献信息

• [EN] HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS JAK INHIBITORS<br/>[FR] ANALOGUES D'HÉTÉROCYCLYL PYRAZOLOPYRIMIDINE EN TANT QU'INHIBITEURS DE JAK
  申请人：CELLZOME LTD

  公开号：WO2011048082A1

  公开（公告）日：2011-04-28

  The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

  本发明涉及式(I)的化合物，其中X1至X5，Y，Z1至Z3和R的含义如描述和权利要求中所述。所述化合物可用作JAK抑制剂，用于治疗或预防免疫、炎症、自身免疫、过敏性疾病和免疫介导性疾病。该发明还涉及包括所述化合物的药物组合物，以及制备这类化合物以及用作药物的用途。
• [EN] COMPOUNDS<br/>[FR] COMPOSÉS
  申请人：GLAXOSMITHKLINE IP DEV LTD

  公开号：WO2015113452A1

  公开（公告）日：2015-08-06

  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）。
• [EN] SUBSTITUTED PYRIMIDINE COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF<br/>[FR] COMPOSÉS DE PYRIMIDINE SUBSTITUÉE, COMPOSITIONS ET APPLICATIONS MÉDICINALES CORRESPONDANTES
  申请人：JUBILANT BIOSYS LTD

  公开号：WO2015025197A1

  公开（公告）日：2015-02-26

  The present disclosure relates to pyrimidine compounds of formula (I), their stereoisomers, tautomers, pharmaceutically acceptable salts, polymorphs, solvates, and hydrates thereof. The present disclosure also relates to process of preparation of these pyrimidine compounds, and to pharmaceutical compositions containing them. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders mediated by epidermal growth factor receptor (EGFR) family kinases.

  本公开涉及式(I)的嘧啶化合物，它们的立体异构体、互变异构体、药学上可接受的盐、多型体、溶剂合物和水合物。本公开还涉及制备这些嘧啶化合物的方法，以及含有它们的药物组合物。本公开的化合物在治疗、预防或抑制由表皮生长因子受体（EGFR）家族激酶介导的疾病和紊乱方面具有用途。
• [EN] NOVEL KINASE INHIBITORS<br/>[FR] NOUVEAUX INHIBITEURS DE KINASES
  申请人：ORIGENIS GMBH

  公开号：WO2014060113A1

  公开（公告）日：2014-04-24

  The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.

  本发明涉及一种具有公式（I）的新化合物，能够抑制一个或多个激酶，特别是SYK（脾酪氨酸激酶）、LRRK2（富含亮氨酸重复的激酶2）和/或MYLK（肌球蛋白轻链激酶）或其突变体。这些化合物在治疗多种疾病中发挥作用。这些疾病包括自身免疫疾病、炎症性疾病、骨疾病、代谢性疾病、神经和神经退行性疾病、癌症、心血管疾病、过敏、哮喘、阿尔茨海默病、帕金森病、皮肤疾病、眼部疾病、传染病和激素相关疾病。
• [EN] PYRAZOLE AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS<br/>[FR] DÉRIVÉS DE PYRAZOLE AMINOPYRIMIDINE EN TANT QUE MODULATEURS DU LRRK2
  申请人：HOFFMANN LA ROCHE

  公开号：WO2012062783A1

  公开（公告）日：2012-05-18

  Compounds of the formula (I), or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

  化合物的结构式（I）或其药用盐，其中X，R1，R2，R3，R4和R5如本文所定义。还公开了制备这些化合物的方法，并将这些化合物用于治疗与LRRK2受体相关的疾病，如帕金森病。