1-(环丙基甲基)-4-羟基吡啶-2-酮 | 1127499-04-0

• 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
• 中文名称: 1-(环丙基甲基)-4-羟基吡啶-2-酮
• 中文别名: 1-(环丙基甲基)-4-羟基吡啶-2(1H)-酮
• 英文名称: 1-(cyclopropylmethyl)-4-hydroxypyridin-2-one
• 英文别名: 1-cyclopropylmethyl-4-hydroxy-1H-pyridin-2-one；1-(Cyclopropylmethyl)-4-hydroxypyridin-2(1H)-one
• CAS: 1127499-04-0
• 化学式: C₉H₁₁NO₂
• 分子量: 165.192
• InChiKey: VNJQMLBHELLWTR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  40.5
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 海关编码：
  2933399090

反应信息

• 作为反应物：
  描述：

  1-(环丙基甲基)-4-羟基吡啶-2-酮 在 palladium on activated charcoal 、 氢气 、 三甲基铝 、 potassium carbonate 、 溶剂黄146 作用下， 以 四氢呋喃 、 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 29.0h， 生成 3-cyclopropyl-N-[4-[(4-[[1-(cyclopropylmethyl)-2-oxopyridin-4-yl]oxy]-3-methylphenyl)amino]quinazolin-6-yl]prop-2-ynamide
  参考文献：
  名称：

  [EN] ALKYNE QUINAZOLINE DERIVATIVES AS INHIBITORS OF ERBB2
  [FR] DÉRIVÉS DE QUINAZOLINE ALCYNE SERVANT D'INHIBITEURS D'ERBB2

  摘要：

  本公开涉及一般用于抑制ErbB2的化合物及其组合物，包括ErbB2的突变形式，特别是那些携带Exon 20突变的形式，制备这些化合物和组合物的方法，以及它们在治疗或预防各种癌症中的应用，如肺癌、胶质瘤、皮肤癌、头颈癌、唾液腺癌、乳腺癌、食道癌、肝癌、胃癌、子宫癌、宫颈癌、胆道癌、胰腺癌、结直肠癌、肾癌、膀胱癌或前列腺癌。

  公开号：

  WO2022006386A1
• 作为产物：
  描述：

  4-苄氧基-2(1H)-吡啶酮 在 palladium 10% on activated carbon 氢气 、 potassium carbonate 作用下， 以 乙醇 、 乙腈 为溶剂， 反应 18.0h， 生成 1-(环丙基甲基)-4-羟基吡啶-2-酮
  参考文献：
  名称：

  3-AZABICYCLO[3.1.0]HEXYL DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS

  摘要：

  本发明涉及新颖化合物，特别是根据式（I）中定义的新型吡啶酮衍生物，其中所有基团均如申请和权利要求中所定义。根据本发明的化合物是代谢型受体亚型2（“mGluR2”）的正向变构调节剂，用于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍，以及涉及代谢型受体亚型mGluR2的疾病。特别是，这些疾病是来自焦虑、精神分裂症、偏头痛、抑郁症和癫痫等中枢神经系统障碍的疾病。该发明还涉及制备这种化合物和组合物的药物组合物和工艺，以及利用这种化合物预防和治疗涉及mGluR2的这种疾病。

  公开号：

  US20110306642A1

文献信息

• [EN] 1,3-DISUBSTITUTED 4-(ARYL-X-PHENYL)-1H-PYRIDIN-2-ONES<br/>[FR] 4-(ARYL-X-PHÉNYL)-1H-PYRIDINE-2-ONES 1,3-DISUBSTITUÉES
  申请人：ORTHO MCNEIL JANSSEN PHARM

  公开号：WO2009033702A1

  公开（公告）日：2009-03-19

  The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I), wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors - subtype 2 ('mGluR2') which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及新化合物，特别是根据式（I）的新吡啶酮衍生物，其中所有基团如申请和索赔中所定义。根据本发明的化合物是代谢型受体-亚型2（'mGluR2'）的阳性别构调节剂，对与谷氨酸功能障碍相关的神经系统和精神障碍以及涉及代谢型受体亚型mGluR2的疾病的治疗或预防是有用的。具体来说，这些疾病是从焦虑、精神分裂症、偏头痛、抑郁症和癫痫等疾病组中选择的中枢神经系统疾病。该发明还涉及制备这种化合物和组合物的药物组合物和方法，以及利用这种化合物预防和治疗涉及mGluR2的这些疾病。
• [EN] 1',3'-DISUBSTITUTED-4-PHENYL-3,4,5,6-TETRAHYDRO-2H, 1'H-[1, 4'] BIPYRIDINYL-2'-ONES<br/>[FR] 4-PHÉNYL-3,4,5,6-TÉTRAHYDRO-2H,1'H-[1, 4'] BIPYRIDINYL-2'-ONES 1', 3'-DISUSBSTITUÉES
  申请人：ORTHO MCNEIL JANSSEN PHARM

  公开号：WO2009033704A1

  公开（公告）日：2009-03-19

  The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors - subtype 2 ('mGluR2') which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及新型化合物，特别是根据式（I）中定义的新型吡啶酮衍生物，其中所有基团均如申请和权利要求中所定义。根据本发明的化合物是代谢型受体亚型2（'mGluR2'）的阳性变构调节剂，用于治疗或预防与谷氨酸功能障碍相关的神经系统和精神疾病，以及mGluR2代谢型受体亚型涉及的疾病。具体来说，这些疾病是来自焦虑、精神分裂症、偏头痛、抑郁症和癫痫等中枢神经系统疾病的选择性疾病。本发明还涉及制备这种化合物和组合物的药物组合物和方法，以及利用这种化合物预防和治疗mGluR2涉及的疾病。
• 3-AZABICYCLO[3.1.0]HEXYL DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
  申请人：Cid-Nunez Jose Maria

  公开号：US20110306642A1

  公开（公告）日：2011-12-15

  The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及新颖化合物，特别是根据式（I）中定义的新型吡啶酮衍生物，其中所有基团均如申请和权利要求中所定义。根据本发明的化合物是代谢型受体亚型2（“mGluR2”）的正向变构调节剂，用于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍，以及涉及代谢型受体亚型mGluR2的疾病。特别是，这些疾病是来自焦虑、精神分裂症、偏头痛、抑郁症和癫痫等中枢神经系统障碍的疾病。该发明还涉及制备这种化合物和组合物的药物组合物和工艺，以及利用这种化合物预防和治疗涉及mGluR2的这种疾病。
• INDOLE AND BENZOMORPHOLINE DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
  申请人：Cid-Nunez Jose Maria

  公开号：US20110275624A1

  公开（公告）日：2011-11-10

  The present invention relates to novel compounds, in particular novel indole and benzomorpholine derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及一种新型化合物，特别是根据公式（I）中定义的所有基团的新型吲哚和苯并吗啡衍生物。本发明的化合物是代谢型受体亚型2（“mGluR2”）的正向变构调节剂，可用于治疗或预防与谷氨酸功能障碍有关的神经和精神障碍以及涉及代谢型受体亚型2的疾病。特别是，这些疾病是从焦虑、精神分裂症、偏头痛、抑郁症和癫痫等中枢神经系统疾病中选择的。本发明还涉及制备这种化合物和组合物的制药组合物和制备过程，以及使用这种化合物预防和治疗涉及mGluR2的这些疾病。
• 1,3-DISUBSTITUTED-4-PHENYL-3,4,5,6-TETRAHYDRO-2H,1 H-1,4 BIPYRIDINYL-2-ONES
  申请人：Cid-Nunez Jose Maria

  公开号：US20100240688A1

  公开（公告）日：2010-09-23

  The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及一种新型化合物，特别是公式（I）中所示的新型吡啶酮衍生物，其中所有基团均如申请和权利要求中所定义。本发明的化合物是代谢型受体亚型2（“mGluR2”）的正向变构调节剂，可用于治疗或预防与谷氨酸功能障碍有关的神经和精神障碍以及涉及代谢型受体mGluR2亚型的疾病。特别是，这些疾病是从焦虑、精神分裂症、偏头痛、抑郁症和癫痫等中枢神经系统疾病中选择的。本发明还涉及制备这种化合物和组合物的制药组合物和制备过程，以及利用这种化合物预防和治疗涉及mGluR2的这些疾病的用途。