8-(4-fluorophenyl)-5,6,7,8-tetrahydro-2-[6-methoxy-5-(4-methyl-1H-imidazol-1-yl)-2-pyridinyl]-[1,2,4]triazolo[1,5-a]pyridine | 1242309-44-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 8-(4-fluorophenyl)-5,6,7,8-tetrahydro-2-[6-methoxy-5-(4-methyl-1H-imidazol-1-yl)-2-pyridinyl]-[1,2,4]triazolo[1,5-a]pyridine
• 英文别名: 8-(4-Fluorophenyl)-2-[6-methoxy-5-(4-methylimidazol-1-yl)pyridin-2-yl]-5,6,7,8-tetrahydro-[1,2,4]triazolo[1,5-a]pyridine
• CAS: 1242309-44-9
• 化学式: C₂₂H₂₁FN₆O
• 分子量: 404.447
• InChiKey: GFWSSGUZGVQIDX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  30
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  70.6
• 氢给体数：
  0
• 氢受体数：
  6

文献信息

• [EN] SUBSTITUTED TRIAZOLE AND IMIDAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS<br/>[FR] DÉRIVÉS DE TRIAZOLE ET D'IMIDAZOLE SUBSTITUÉS EN TANT QUE MODULATEURS DE GAMMA SECRÉTASE
  申请人：ORTHO MCNEIL JANSSEN PHARM

  公开号：WO2011006903A1

  公开（公告）日：2011-01-20

  The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

  本发明涉及具有以下式（I）的新型取代三唑和咪唑衍生物，其中R1、R2、A1、A2、A3、A4、X和Het1的含义如权利要求中所定义。根据本发明的化合物可用作γ-分泌酶调节剂。该发明还涉及制备这种新型化合物的方法，包含所述化合物作为活性成分的药物组合物，以及将所述化合物用作药物的用途。
• Nitrogen-Containing Fused Heterocyclic Compounds and Their use as Beta Amyloid Production Inhibitors
  申请人：Kitazawa Noritaka

  公开号：US20120053171A1

  公开（公告）日：2012-03-01

  A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a five-membered aromatic heterocyclic group or the like fused with a non-aromatic ring group, which may be substituted, Ring B represents a phenyl group or the like which may be substituted, X1 represents a single bond or the like, R1 and R2 each represent a C1-6 alkyl group or the like, m represents an integer of 0 to 3, and n represents an integer of 0 to 2, is effective as a therapeutic agent for a disease caused by Aβ.

  化合物的化学式为[I]，或其药理学上可接受的盐或酯，其中环A代表一个五元芳香杂环基团或类似物，与非芳香环基团融合，可以被取代，环B代表苯基或类似物，可以被取代，X1代表单键或类似物，R1和R2各代表C1-6烷基或类似物，m代表0至3的整数，n代表0至2的整数，该化合物对由Aβ引起的疾病具有治疗作用。
• Nitrogen-containing fused heterocyclic compounds and their use as beta amyloid production inhibitors
  申请人：Eisai R&D Management Co., Ltd.

  公开号：EP2615090A1

  公开（公告）日：2013-07-17

  A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a five-membered aromatic heterocyclic group or the like fused with a non-aromatic ring group, which may be substituted, Ring B represents a phenyl group or the like which may be substituted, X1 represents a single bond or the like, R1 and R2 each represent a C1-6 alkyl group or the like, m represents an integer of 0 to 3, and n represents an integer of 0 to 2, is effective as a therapeutic agent for a disease caused by Aβ.

  由式 [I] 代表的化合物： 或其药理学上可接受的盐或酯，其中环 A 代表五元芳香杂环基团或类似基团，与非芳香环基团融合，可被取代；环 B 代表苯基或类似基团，可被取代；X1 代表单键或类似键；R1 和 R2 各代表 C1-6 烷基或类似基团；m 代表 0 至 3 的整数；n 代表 0 至 2 的整数。
• NITROGEN-CONTAINING FUSED HETEROCYCLIC COMPOUNDS AND THEIR USE AS BETA AMYLOID PRODUCTION INHIBITORS
  申请人：Eisai R&D Management Co., Ltd.

  公开号：EP2401276B1

  公开（公告）日：2013-06-05
• SUBSTITUTED TRIAZOLE AND IMIDAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS
  申请人：Janssen Pharmaceuticals Inc.

  公开号：EP2454239A1

  公开（公告）日：2012-05-23