4-methyl-5-(5-nitropyridin-2-yl)oxazole | 1239719-59-5

• 分子结构分类: 有机化合物 - 有机1,3-偶极化合物 - 烯丙基型1,3-偶极有机化合物
• 英文名称: 4-methyl-5-(5-nitropyridin-2-yl)oxazole
• 英文别名: 2-(4-Methyl-5-oxazolyl)-5-nitropyridine；4-methyl-5-(5-nitropyridin-2-yl)-1,3-oxazole
• CAS: 1239719-59-5
• 化学式: C₉H₇N₃O₃
• 分子量: 205.173
• InChiKey: OFSKJWGNAPHBLY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  84.7
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  4-methyl-5-(5-nitropyridin-2-yl)oxazole 在 铁粉 、 氯化铵 作用下， 以 四氢呋喃 、 水 为溶剂， 反应 4.0h， 以71%的产率得到6-(4-methyloxazol-5-yl)pyridin-3-amine
  参考文献：
  名称：

  [EN] NOVEL SUBSTITUTED INDAZOLE AND AZA-INDAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS
  [FR] NOUVEAUX DÉRIVÉS SUBSTITUÉS D'INDAZOLE ET D'AZA-INDAZOLE UTILISÉS COMME MODULATEURS DE LA GAMMA SÉCRÉTASE

  摘要：

  本发明涉及具有公式（I）中定义的R1、R2、R3、R4、Y、A1、A2、A3、A4、X1、X2、X3和Het1含义的新型取代的吲唑和氮杂吲唑衍生物。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过程，包含该化合物作为活性成分的药物组合物以及将该化合物用作药物的用途。

  公开号：

  WO2010145883A1
• 作为产物：
  描述：

  3-硝基-6-吡啶甲醛 、 1-甲基-对甲苯磺酰甲基异腈 以 甲醇 为溶剂， 反应 12.0h， 生成 4-methyl-5-(5-nitropyridin-2-yl)oxazole
  参考文献：
  名称：

  PYRROLO[1,2-b]PYRIDAZINE DERIVATIVES

  摘要：

  提供的是化合物的化学式（I），其中变量基团在此处被定义。

  公开号：

  US20180230157A1

文献信息

• [EN] NOVEL SUBSTITUTED BICYCLIC HETEROCYCLIC COMPOUNDS AS GAMMA SECRETASE MODULATORS<br/>[FR] NOUVEAUX COMPOSÉS HÉTÉROCYCLIQUES BICYCLIQUES SUBSTITUÉS EN TANT QUE MODULATEURS DE LA GAMMA-SÉCRÉTASE
  申请人：ORTHO MCNEIL JANSSEN PHARM

  公开号：WO2010089292A1

  公开（公告）日：2010-08-12

  The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 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.

  本发明涉及式（I）的取代双环杂环化合物，其中Het1、Het2、A1、A2、A3和A4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。本发明还涉及制备这种新化合物的方法，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。
• [EN] NOVEL SUBSTITUTED INDAZOLE AND AZA-INDAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS<br/>[FR] NOUVEAUX DÉRIVÉS SUBSTITUÉS D'INDAZOLE ET D'AZA-INDAZOLE UTILISÉS COMME MODULATEURS DE LA GAMMA SÉCRÉTASE
  申请人：ORTHO MCNEIL JANSSEN PHARM

  公开号：WO2010145883A1

  公开（公告）日：2010-12-23

  The present invention is concerned with novel substituted indazole and aza-indazole derivatives of Formula (I), wherein R1, R2, R3, R4, Y, A1, A2, A3, A4, X1, X2, X3 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.

  本发明涉及具有公式（I）中定义的R1、R2、R3、R4、Y、A1、A2、A3、A4、X1、X2、X3和Het1含义的新型取代的吲唑和氮杂吲唑衍生物。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过程，包含该化合物作为活性成分的药物组合物以及将该化合物用作药物的用途。
• Pyrrolo[1,2-b]pyridazine derivatives
  申请人：Gilead Sciences, Inc.

  公开号：US10336762B2

  公开（公告）日：2019-07-02

  Provided is a compound of Formula (I) wherein the variable groups are defined herein.

  提供的是式 (I) 化合物 其中变量组在此定义。
• NOVEL SUBSTITUTED BICYCLIC HETEROCYCLIC COMPOUNDS AS GAMMA SECRETASE MODULATORS
  申请人：Gijsen Henricus, Jacobus, Maria

  公开号：US20110281881A1

  公开（公告）日：2011-11-17

  The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het 1 , Het 2 , A 1 , A 2 , A 3 and A 4 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.
• NOVEL SUBSTITUTED INDAZOLE AND AZA-INDAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS
  申请人：Bischoff François Paul

  公开号：US20120095036A1

  公开（公告）日：2012-04-19

  The present invention is concerned with novel substituted indazole and aza-indazole derivatives of Formula (I) wherein R 1 , R 2 , R 3 , R 4 , Y, A 1 , A 2 , A 3 , A 4 , X 1 , X 2 , X 3 and Het 1 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.