3-sec-Butyl-1H-indazole | 61485-22-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡唑类
• 英文名称: 3-sec-Butyl-1H-indazole
• 英文别名: 1H-Indazole, 3-(1-methylpropyl)-；3-butan-2-yl-2H-indazole
• CAS: 61485-22-1
• 化学式: C₁₁H₁₄N₂
• 分子量: 174.246
• InChiKey: HUSDCLOYEDNFGW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  28.7
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  1-(2-氨基苯基)-2-甲基丁烷-1-酮 以6%的产率得到
  参考文献：
  名称：

  HANNIG E.; KOLLMORGEN C.; KOERNER M., PHARMAZIE , 1976, 31, NO 8, 534-536

  摘要：

  DOI：

文献信息

• INDAZOLINONE COMPOSITIONS USEFUL AS KINASE INHIBITORS
  申请人：Aronov Alex

  公开号：US20090048250A1

  公开（公告）日：2009-02-19

  The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK2, CDK2, MK2, SRC, SYK, and Aurora-2. Accordingly, compounds and compositions of the invention are useful for treating or lessening the severity of a variety of disorders, including, but not limited to, heart disease, diabetes, Alzheimer's disease, immunodeficiency disorders, inflammatory diseases, allergic diseases, autoimmune diseases, destructive bone disorders such as osteoporosis, proliferative disorders, infectious diseases and viral diseases.

  本发明提供了I式化合物：这些化合物及其药学上可接受的组合物通常用作激酶抑制剂，特别是作为PRAK、GSK3、ERK2、CDK2、MK2、SRC、SYK和Aurora-2的抑制剂。因此，本发明的化合物和组合物可用于治疗或减轻各种疾病的严重程度，包括但不限于心脏疾病、糖尿病、阿尔茨海默病、免疫缺陷病、炎症性疾病、过敏性疾病、自身免疫性疾病、破坏性骨疾病（如骨质疏松症）、增生性疾病、传染病和病毒性疾病。
• COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
  申请人：Vertex Pharmaceuticals Incorporated

  公开号：EP3354650A1

  公开（公告）日：2018-08-01

  The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.

  本发明涉及可用作 ATR 蛋白激酶抑制剂的吡嗪化合物。本发明还涉及包含本发明化合物的药学上可接受的组合物；使用本发明化合物治疗各种疾病、失调和病症的方法；制备本发明化合物的工艺；制备本发明化合物的中间体；以及在体外应用中使用本发明化合物的方法，例如研究生物和病理现象中的激酶；研究由这些激酶介导的细胞内信号转导途径；以及比较评估新的激酶抑制剂。 本发明的化合物具有式 I： 其中变量如本文所定义。
• Urea derivatives and uses thereof
  申请人：Kala Pharmaceuticals, Inc.

  公开号：US10316022B2

  公开（公告）日：2019-06-11

  The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.

  本发明提供了式(I)-(III)中任一项的新型化合物及其药物组合物。本发明还提供了由式（I）-（III）化合物及其药物组合物组成的具有粘液渗透性的颗粒（如纳米颗粒）。本发明还提供了使用本发明化合物及其药物组合物治疗和/或预防与异常或病理性血管生成和/或生长因子（如血管内皮生长因子（VEGF））异常信号转导有关的疾病的方法和试剂盒，如增殖性疾病（如、如增殖性疾病（如癌症、良性肿瘤、炎症性疾病、自身免疫性疾病）和眼部疾病（如黄斑变性、青光眼、糖尿病视网膜病变、视网膜母细胞瘤、水肿、葡萄膜炎、干眼症、睑缘炎和手术后炎症）。
• N-alkyl-2-phenoxyethanamines, their preparation and use
  申请人：The Trustees of Columbia University In the City of New York

  公开号：US10570148B2

  公开（公告）日：2020-02-25

  The present invention provides a compound having the structure: (structurally represented) wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl; R6 is alkyl; A is absent or present, and when present is —C(O)— or —C(O)NH—; B is substituted or unsubstituted monocycle, bicycle, heteromonocycle, heterobicycle, benzyl, CO2H or (C1-C4 alkyl)-CO2H, wherein when B is CO2H, then A is present and is —C(O)—, or a pharmaceutically acceptable salt thereof.

  本发明提供了一种具有以下结构的化合物：(结构表示），其中 R1、R2、R3、R4 和 R5 各自独立地为 H、卤素、CF3 或 C1-C4 烷基；R6 为烷基；A 不存在或存在，存在时为 -C(O)- 或 -C(O)NH- ；B 为取代或未取代的单环、单车、杂单环、杂单车、苄基、CO2H 或 (C1-C4 烷基)-CO2H，其中当 B 为 CO2H 时，则 A 存在且为 -C(O)-，或其药学上可接受的盐。
• Uridine nucleoside derivatives, compositions and methods of use
  申请人：Tufts University

  公开号：US11124536B2

  公开（公告）日：2021-09-21

  This disclosure relates to uridine nucleoside derivatives, compositions comprising therapeutically effective amounts of those nucleoside derivatives and methods of using those nucleoside derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma and inflammatory conditions.

  本公开涉及尿苷核苷衍生物、包含治疗有效量的这些核苷衍生物的组合物以及使用这些核苷衍生物或组合物治疗对P2Y6受体的配体（如激动剂）有反应的疾病的方法，例如神经元疾病，包括神经退行性疾病（如阿尔茨海默病、帕金森病）和创伤性中枢神经系统损伤、疼痛、唐氏综合征（DS）、青光眼和炎症。