10H-indolo<3,2-g>pteridine | 243-63-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 蝶啶及其衍生物
• 英文名称: 10H-indolo<3,2-g>pteridine
• 英文别名: 10H-Indolo<3,2-g>pteridin；10H-indolo[3,2-g]pteridine；10H-indolo[3,2-g]pteridine
• CAS: 243-63-0
• 化学式: C₁₂H₇N₅
• 分子量: 221.221
• InChiKey: DBZDODUGFRGEIK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  17
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  67.4
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] PROCESS FOR THE PREPARATION OF 8-(4-AMINOPHENOXY)-4H-PYRIDO[2,3-B]PYRAZIN-3-ONE DERIVATIVES<br/>[FR] PROCÉDÉ DE PRÉPARATION DE DÉRIVÉS DE 8-(4-AMINOPHÉNOXY)- 4H-PYRIDO[2,3-B]PYRAZIN-3-ONE
  申请人：CANCER REC TECH LTD

  公开号：WO2015075482A1

  公开（公告）日：2015-05-28

  The present invention pertains generally to the field of organic chemical synthesis, and in particular to certain methods for the synthesis of 8-(4-aminophenyoxy)- 4H-pyrido[2,3-b]pyrazin-3-one and related compounds (denoted herein as (3)) from 4-(4-aminophenyoxy)pyridine-2,3-diamine and related compounds (denoted herein as (1)), by reaction with glyoxylic acid (denoted herein as (2)). The compounds (3) are useful in the synthesis of known anti-cancer agents, such as 1-(5-tert-butyl-2-(4-methyl- phenyl)-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea.

  本发明一般涉及有机化学合成领域，特别是涉及从4-(4-氨基苯氧基)吡啶-2,3-二胺及相关化合物（以下简称为（1））与甘氧酸（以下简称为（2））反应，合成8-(4-氨基苯氧基)-4H-吡啶并[2,3-b]吡嗪-3-酮及相关化合物（以下简称为（3））的某些方法。这些化合物（3）在合成已知的抗癌药物中起到作用，例如1-(5-叔丁基-2-(4-甲基苯基)-吡唑-3-基)-3-[2-氟-4-[(3-氧代-4H-吡啶并[2,3-b]吡嗪-8-基)氧基]苯基]脲。
• Preventives and remedies for central nervous system diseases
  申请人：——

  公开号：US20030207863A1

  公开（公告）日：2003-11-06

  A prophylactic or therapeutic agent for central nervous system diseases based on amyloid &bgr;40 secretion inhibitory activity of a compound having urotensin II receptor antagonistic activity or a salt thereof.

  一种预防或治疗中枢神经系统疾病的药剂，基于一种具有尿泰松II受体拮抗活性或其盐的化合物对淀粉样蛋白β40分泌抑制活性。
• Agents and crystals for improving excretory potency of urinary bladder
  申请人：——

  公开号：US20020177593A1

  公开（公告）日：2002-11-28

  Agents for improving potentcy of the urinary bladder which comprises an amine compound of non-carbamate-type having an acetylcholinesterase-inhibiting action. Particularly, crystals of a tricyclic, condensed, heterocyclic derivative are provided, which possess an excellent action to inhibit acetylcholine esterase and an action to improve the excretory potency of urinary bladder. As an example, crystals of of 8-[3-[1-[(3-fluorophenyl)-methyl]-4-piperidinyl]-1-oxopropyl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one or a salt thereof and pharmaceutical compositions containing them are disclosed.

  改善膀胱功能的药剂，包括一种非卡巴酯类胺化合物，具有乙酰胆碱酯酶抑制作用。特别地，提供了一种三环、紧凑、杂环衍生物的晶体，具有优异的抑制乙酰胆碱酯酶作用和改善膀胱排泄功能的作用。例如，揭示了8-[3-[1-[(3-氟苯基)-甲基]-4-哌啶基]-1-氧代丙基]-1,2,5,6-四氢-4H-吡咯烷[3,2,1-ij]-喹啉-4-酮或其盐和含有它们的药物组合物。
• Agents for improving excretory potency of urinary bladder
  申请人：——

  公开号：US20040116457A1

  公开（公告）日：2004-06-17

  Agents for improving excretory potency of the urinary bladder which comprises an amine compound of non-carbamate-type having an acetylcholinesterase-inhibiting action.

  改善排泄能力的尿道代理，包括一种非卡巴酯型胺类化合物，具有乙酰胆碱酯酶抑制作用。
• Preventives/remedies for urinary disturbance
  申请人：Ishihara Yuji

  公开号：US20050197362A1

  公开（公告）日：2005-09-08

  Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an α1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.

  具有乙酰胆碱酯酶抑制作用和α1拮抗作用的化合物的预防/治疗措施，可以显著改善膀胱的尿液功能（即改善尿流率和排尿效率的效果），而不影响尿压或血压。