(R)-6-(5-bromo-2-fluoro-phenyl)-3-fluoro-2,6-dimethyl-6,7-dihydro-5H-pyrazolo[1,5-a]pyrazine-4-thione | 1397683-89-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 三嗪类
• 英文名称: (R)-6-(5-bromo-2-fluoro-phenyl)-3-fluoro-2,6-dimethyl-6,7-dihydro-5H-pyrazolo[1,5-a]pyrazine-4-thione
• 英文别名: (6R)-6-(5-bromo-2-fluorophenyl)-3-fluoro-2,6-dimethyl-5,7-dihydropyrazolo[1,5-a]pyrazine-4-thione
• CAS: 1397683-89-4
• 化学式: C₁₄H₁₂BrF₂N₃S
• 分子量: 372.236
• InChiKey: IITQXLLUHIONGH-AWEZNQCLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  21
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  61.9
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (R)-6-(5-bromo-2-fluoro-phenyl)-3-fluoro-2,6-dimethyl-6,7-dihydro-5H-pyrazolo[1,5-a]pyrazine-4-thione 在 氨 、 氯化铵 作用下， 以 乙醇 为溶剂， 反应 144.0h， 以42%的产率得到(R)-6-(5-bromo-2-fluoro-phenyl)-3-fluoro-2,6-dimethyl-6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-ylamine
  参考文献：
  名称：

  [EN] 6,7-DIHYDRO-PYRAZOLO[1,5-A]PYRAZIN-4-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
  [FR] DÉRIVÉS DE 6,7-DIHYDRO-PYRAZOLO[1,5-A]PYRAZIN-4-YLAMINE UTILES EN TANT QU'INHIBITEURS DE BÊTA-SÉCRÉTASE (BACE)

  摘要：

  本发明涉及作为β-分泌酶抑制剂的新型6,7-二氢吡唑并[1,5-a]吡嗪-4-基胺衍生物，该酶也称为β-位点淀粉样蛋白裂解酶、BACE、BACEl、Asp2或memapsin2。该发明还涉及包含这些化合物的药物组合物，制备这些化合物和组合物的方法，以及利用这些化合物和组合物预防和治疗涉及β-分泌酶的疾病的用途，如阿尔茨海默病（AD）、轻度认知障碍、老年痴呆、带有Lewy小体的痴呆、唐氏综合征、与中风相关的痴呆、与帕金森病相关的痴呆或与β-淀粉样蛋白相关的痴呆。

  公开号：

  WO2012117027A1

文献信息

• 6,7-DIHYDRO-PYRAZOLO[1,5-a]PYRAZIN-4-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
  申请人：Trabanco-Suárez Andrés Avelino

  公开号：US20140005200A1

  公开（公告）日：2014-01-02

  The present invention relates to novel 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-yl-amine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.

  本发明涉及一种新型的6,7-二氢-吡唑并[1,5-a]吡嗪-4-基胺衍生物，作为β-分泌酶抑制剂，也被称为β-淀粉样蛋白裂解酶、BACE、BACE1、Asp2或memapsin2。本发明还涉及包含这些化合物的制药组合物，制备这些化合物和组合物的方法，以及使用这些化合物和组合物预防和治疗β-分泌酶参与的疾病，如阿尔茨海默病（AD）、轻度认知障碍、老年痴呆、帕金森病相关痴呆、Lewy小体痴呆、唐氏综合症、中风相关痴呆或β-淀粉样蛋白相关的痴呆。
• 6,7-DIHYDRO-PYRAZOLO[1,5-A]PYRAZIN-4-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
  申请人：Janssen Pharmaceutica, N.V.

  公开号：EP2681219B1

  公开（公告）日：2015-10-28
• FUSED RING DERIVATIVE HAVING MGAT-2 INHIBITORY ACTIVITY
  申请人：Shionogi & Co., Ltd.

  公开号：US20220073518A1

  公开（公告）日：2022-03-10

  The present invention provides the compound represented by the following formula (I): wherein a moiety represented by formula: or the like. The symbols are defined in the specification. The compounds of the present invention have MGAT2 inhibitory activity, and are useful as a medicine for treatment of MGAT2-associated diseases including obesity, metabolic syndrome, hyperlipidemia, hypertriglyceridemia, hyper-VLDL-triglyceridemia, hyperfattyacidemia, diabetes mellitus, and arteriosclerosis.
• US9346811B2
  申请人：——

  公开号：US9346811B2

  公开（公告）日：2016-05-24