2-乙氧基-3-吡啶甲烷胺 | 851773-43-8

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 2-乙氧基-3-吡啶甲烷胺
• 英文名称: (2-ethoxypyridin-3-yl)methanamine
• CAS: 851773-43-8
• 化学式: C₈H₁₂N₂O
• mdl: MFCD09734870
• 分子量: 152.196
• InChiKey: STCIIFCOOYREBT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  11
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.375
• 拓扑面积：
  48.1
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2933399090

反应信息

• 作为反应物：
  描述：

  2-乙氧基-3-吡啶甲烷胺 、 5-(4-氯苯基)-3-吡啶羧酸 在 (benzotriazo-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 生成 C₂₀H₁₈ClN₃O₂
  参考文献：
  名称：

  Subtype-selective Nav1.8 sodium channel blockers: Identification of potent, orally active nicotinamide derivatives

  摘要：

  A series of aryl-substituted nicotinamide derivatives with selective inhibitory activity against the Na(v)1.8 sodium channel is reported. Replacement of the furan nucleus and homologation of the anilide linker in subtype-selective blocker A-803467 (1) provided potent, selective derivatives with improved aqueous solubility and oral bioavailability. Representative compounds from this series displayed efficacy in rat models of inflammatory and neuropathic pain. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.08.121
• 作为产物：
  描述：

  3-溴-2-氯吡啶 在 盐酸 、 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 potassium tert-butylate 、 氢气 作用下， 以 1,4-二氧六环 、 N-甲基吡咯烷酮 、 乙醇 为溶剂， 20.0~140.0 ℃ 、310.27 kPa 条件下， 反应 27.0h， 生成 2-乙氧基-3-吡啶甲烷胺
  参考文献：
  名称：

  [EN] COMBINATION TREATMENTS COMPRISING ADMINISTRATION OF 1H-PYRAZOLO[4,3-B]PYRIDINES
  [FR] TRAITEMENTS COMBINÉS COMPRENANT L'ADMINISTRATION DE 1H-PYRAZOLO [4,3-B] PYRIDINES

  摘要：

  本发明提供了式(I)的1H-吡唑并[4,3-b]吡啶-7-胺作为PDE1抑制剂，以及一种第二化合物，该化合物在治疗精神障碍方面是有用的，并且它们的联合使用作为药物，特别用于治疗精神和/或认知障碍。

  公开号：

  WO2019115566A1

文献信息

• [EN] 1H-PYRAZOLO[4,3-B]PYRIDINES AS PDE1 INHIBITORS<br/>[FR] 1H-PYRAZOLO [4,3-B] PYRIDINES EN TANT QU'INHIBITEURS DE PDE1
  申请人：H LUNDBECK AS

  公开号：WO2018007249A1

  公开（公告）日：2018-01-11

  The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

  本发明提供了式(I)的1H-吡唑并[4,3-b]吡啶-7-胺作为PDE1抑制剂，并将其用作药物，特别用于治疗神经退行性疾病和精神疾病。
• 1H-PYRAZOLO[4,3-B]PYRIDINES AS PDE1 INHIBITORS
  申请人：H. Lundbeck A/S

  公开号：US20190194189A1

  公开（公告）日：2019-06-27

  The present invention provides 1H-pyrazolo[4,3-b]pyridines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

  本发明提供了式(I)的1H-吡唑并[4,3-b]吡啶类化合物作为PDE1抑制剂，并将其用作药物，特别用于治疗神经退行性疾病和精神疾病。
• [EN] COMBINATION TREATMENTS COMPRISING ADMINISTRATION OF 1H-PYRAZOLO[4,3-B]PYRIDINES<br/>[FR] TRAITEMENTS COMBINÉS COMPRENANT L'ADMINISTRATION DE 1H-PYRAZOLO [4,3-B] PYRIDINES
  申请人：H LUNDBECK AS

  公开号：WO2019115567A1

  公开（公告）日：2019-06-20

  The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors together with a second compound useful in the treatment of a neurodegenerative disorder and their combined use as a medicament, in particular for the treatment of neurodegenerative and/or cognitive disorders.

  本发明提供了式(I)的1H-吡唑并[4,3-b]吡啶-7-胺作为PDE1抑制剂，以及在治疗神经退行性疾病中有用的第二化合物，以及它们的联合使用作为药物，特别用于治疗神经退行性和/或认知障碍。
• Pyrazole compounds and their use as antidiabetes agents
  申请人：Takagi Masaki

  公开号：US20070032529A1

  公开（公告）日：2007-02-08

  The present invention provides a pyrazole compound that has liver glycogen phosphorylase inhibitory activity and is useful as a therapeutic or prophylactic agent for diabetes, the pyrazole compound represented by the following general formula (I): wherein Ring Q represents an aryl or heteroaromatic group, R 1 represents a hydrogen atom, a halogen atom, a C 1-6 alkyl group or a C 1-6 alkoxy group, R 2 represents a halogen atom, a C 1-6 alkyl group, a C 1-6 alkoxy group or an azido group, R 3 represents a halogen atom, a hydroxyl group, a C 1-6 alkyl group, a halo C 1-6 alkyl group, a C 1-6 alkoxy group, an azido group, an amino group, an acylamino group or a C 1-6 alkylsulfonylamino group, R 4 and R 5 are identical with or different from each other and represent a hydrogen atom, a substituted or unsubstituted C 1-6 alkyl group, a C 3-8 cycloalkyl group, a substituted or unsubstituted saturated heterocyclic group, a substituted or unsubstituted aryl group, a C 7-14 aralkyl group, a heteroaromatic group, or the like, or a pharmacologically acceptable salt thereof.

  本发明提供了一种具有肝糖原磷酸化酶抑制活性的吡唑化合物，用作糖尿病的治疗或预防剂，所述吡唑化合物由以下通用式（I）表示：其中环Q代表芳基或杂芳基，R1代表氢原子、卤原子、C1-6烷基或C1-6烷氧基，R2代表卤原子、C1-6烷基、C1-6烷氧基或偶氮基，R3代表卤原子、羟基、C1-6烷基、卤代C1-6烷基、C1-6烷氧基、偶氮基、氨基、酰胺基或C1-6烷基磺酰胺基，R4和R5彼此相同或不同，代表氢原子、取代或未取代的C1-6烷基、取代或未取代的C3-8环烷基、取代或未取代的饱和杂环基、取代或未取代的芳基、C7-14芳基烷基、杂芳基等，或其药理学上可接受的盐。
• COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
  申请人：Ibrahim Prabha N.

  公开号：US20090286782A1

  公开（公告）日：2009-11-19

  Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one of Fms protein kinase or Kit protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinases and/or Kit protein kinases, including rheumatoid arthritis, osteoarthritis, osteoporosis, peri-prosthetic osteolysis, systemic sclerosis, demyelinating disorders, multiple sclerosis, Charcot Marie Tooth syndrome, amyotrophic lateral sclerosis, Alzheimer's disease, Parkinson's disease, ulcerative colitis, Crohn's disease, immune thrombocytopenic purpura, myelopreparation for autologous transplantation, transplant rejection, nephritis, nephropathy, type I diabetes, acute pain, inflammatory pain, neuropathic pain, breast cancer, prostate cancer, pancreatic cancer, lung cancer, ovarian cancer, gliomas, glioblastomas, neurofibromatosis, osteolytic bone metastases, and giant cell tumors.

  描述了化合物及其盐，配方，共轭物，衍生物，形式和用途。在某些方面和实施例中，所述的化合物或其盐，配方，共轭物，衍生物，形式对Fms蛋白激酶或Kit蛋白激酶至少有一种活性。还描述了使用这些方法来治疗疾病和症状，包括与Fms蛋白激酶和/或Kit蛋白激酶活性相关的疾病和症状，包括类风湿关节炎，骨关节炎，骨质疏松症，周围假体周围骨溶解，系统性硬化症，脱髓鞘疾病，多发性硬化症，沙科特-玛丽-屈特综合症，肌萎缩侧索硬化症，阿尔茨海默病，帕金森病，溃疡性结肠炎，克罗恩病，免疫性血小板减少性紫癜，自体移植的骨髓准备，移植排斥反应，肾炎，肾病，I型糖尿病，急性疼痛，炎症性疼痛，神经病性疼痛，乳腺癌，前列腺癌，胰腺癌，肺癌，卵巢癌，神经胶质瘤，胶质母细胞瘤，神经纤维瘤病，骨转移性溶骨病和巨细胞瘤。