2-methyl-8-morpholin-4-yl-3-[6-(tetrahydro-pyran-4-yl)-pyridin-3-yl]-imidazo [1,2-q]pyrazine | 1334168-37-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡嗪类
• 英文名称: 2-methyl-8-morpholin-4-yl-3-[6-(tetrahydro-pyran-4-yl)-pyridin-3-yl]-imidazo [1,2-q]pyrazine
• 英文别名: 2-methyl-8-(4-morpholinyl)-3-[6-(tetrahydro-2H-pyran-4-yl)-3-pyridinyl]-imidazo[1,2-a]pyrazine；2-methyl-8-morpholin-4-yl-3-[6-(tetrahydro-pyran-4-yl)-pyridin-3-yl]-imidazo[1,2-a]pyrazine；4-[2-Methyl-3-[6-(oxan-4-yl)pyridin-3-yl]imidazo[1,2-a]pyrazin-8-yl]morpholine
• CAS: 1334168-37-4
• 化学式: C₂₁H₂₅N₅O₂
• 分子量: 379.462
• InChiKey: CRVVISKTRMHANS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  64.8
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  2-氯-5-吡啶硼酸 在 四(三苯基膦)钯 、 palladium 10% on activated carbon 甲酸铵 、 碳酸氢钠 、 sodium carbonate 作用下， 以 1,4-二氧六环 、 甲醇 、 水 为溶剂， 反应 41.0h， 生成 2-methyl-8-morpholin-4-yl-3-[6-(tetrahydro-pyran-4-yl)-pyridin-3-yl]-imidazo [1,2-q]pyrazine
  参考文献：
  名称：

  [EN] IMIDAZO [1, 2 -A] PYRAZINE DERIVATIVES AND THEIR USE FOR THE PREVENTION OR TREATMENT OF NEUROLOGICAL, PSYCHIATRIC AND METABOLIC DISORDERS AND DISEASES
  [FR] DÉRIVÉS D'IMIDAZO[1,2-A]PYRAZINE ET LEUR UTILISATION POUR LA PRÉVENTION OU LE TRAITEMENT DE TROUBLES ET MALADIES NEUROLOGIQUES, PSYCHIATRIQUES ET MÉTABOLIQUES.

  摘要：

  本发明涉及新型咪唑并[1,2-a]吡嗪衍生物，它们是磷酸二酯酶10（PDE10）的抑制剂，并且对涉及PDE10酶的神经、精神和代谢性疾病的治疗或预防具有用处。该发明还涉及包含这类化合物的药物组合物，用于制备这类化合物和组合物的方法，以及利用这类化合物或药物组合物预防或治疗神经、精神和代谢性疾病和疾病。

  公开号：

  WO2011110545A1

文献信息

• [EN] IMIDAZO [1, 2 -A] PYRAZINE DERIVATIVES AND THEIR USE FOR THE PREVENTION OR TREATMENT OF NEUROLOGICAL, PSYCHIATRIC AND METABOLIC DISORDERS AND DISEASES<br/>[FR] DÉRIVÉS D'IMIDAZO[1,2-A]PYRAZINE ET LEUR UTILISATION POUR LA PRÉVENTION OU LE TRAITEMENT DE TROUBLES ET MALADIES NEUROLOGIQUES, PSYCHIATRIQUES ET MÉTABOLIQUES.
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2011110545A1

  公开（公告）日：2011-09-15

  The present invention relates to novel imidazo[1,2-a]pyrazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.

  本发明涉及新型咪唑并[1,2-a]吡嗪衍生物，它们是磷酸二酯酶10（PDE10）的抑制剂，并且对涉及PDE10酶的神经、精神和代谢性疾病的治疗或预防具有用处。该发明还涉及包含这类化合物的药物组合物，用于制备这类化合物和组合物的方法，以及利用这类化合物或药物组合物预防或治疗神经、精神和代谢性疾病和疾病。
• [EN] COMBINATIONS COMPRISING PDE 2 INHIBITORS SUCH AS 1-ARYL-4-METHYL- [1,2,4] TRIAZOLO [4,3-A] QUINOXALINE COMPOUNDS AND PDE 10 INHIBITORS FOR USE IN THE TREATMENT OF NEUROLOGICAL OR METABOLIC DISORDERS<br/>[FR] COMBINAISONS COMPRENANT DES INHIBITEURS DE LA PDE 2 TELS QUE DES COMPOSÉS 1-ARYL-4-MÉTHYL-[1, 2, 4] TRIAZOLO [4, 3-A]-QUINOXALINE ET DES INHIBITEURS DE LA PDE 10 POUR UTILISATION DANS LE TRAITEMENT DE TROUBLES NEUROLOGIQUES OU MÉTABOLIQUES
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2014001314A1

  公开（公告）日：2014-01-03

  The present invention relates to combinations of phosphodiesterase 2 (PDE2) inhibitors with inhibitors of phosphodiesterase 10 (PDE 10). In particular, the invention relates to combinations of 1-aryl-4- methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives which have been found to inhibit phosphodiesterase 2 (PDE2), with inhibitors of phosphodiesterase 10 (PDE10). Particular PDE10 inhibitors are selected from the group of MP-10, PQ-10, TP-10, papaverine, and the compounds disclosed in WO 2011/051342 and in WO 2011/110545. The invention is also directed to pharmaceutical compositions comprising such combinations, to processes for preparing such compositions, to the use of PDE2 inhibitors, in particular of 1- aryl-4-methyl- [1,2,4]triazolo[4,3-a]-quinoxaline derivatives for the potentiation of said PDE10 inhibitors, and to the use of said PDE10 inhibitors for the potentiation of the effect of said PDE2 inhibitors, in particular, 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives, and to the use of such combinations and compositions for the prevention and treatment of disorders in which PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases.

  本发明涉及磷酸二酯酶2（PDE2）抑制剂与磷酸二酯酶10（PDE 10）抑制剂的组合物。具体地，本发明涉及已被发现能够抑制磷酸二酯酶2（PDE2）的1-芳基-4-甲基-[1,2,4]三唑并[4,3-a]-喹喔啉衍生物与磷酸二酯酶10（PDE10）抑制剂的组合物。特定的PDE10抑制剂选自MP-10、PQ-10、TP-10、罂粟碱以及WO 2011/051342和WO 2011/110545中披露的化合物。本发明还涉及包含这种组合物的药物组合物、制备这种组合物的工艺、使用PDE2抑制剂，特别是1-芳基-4-甲基-[1,2,4]三唑并[4,3-a]-喹喔啉衍生物来增强所述PDE10抑制剂的作用，以及使用所述PDE10抑制剂来增强所述PDE2抑制剂的作用，特别是1-芳基-4-甲基-[1,2,4]三唑并[4,3-a]-喹喔啉衍生物，以及使用这种组合物和组合物预防和治疗涉及PDE2和PDE10的疾病，如神经和精神疾病以及内分泌或代谢性疾病。
• EP2545055B1
  申请人：——

  公开号：EP2545055B1

  公开（公告）日：2017-08-09
• IMIDAZO [1, 2 -A]PYRAZINE DERIVATIVES AND THEIR USE FOR THE PREVENTION OR TREATMENT OF NEUROLOGICAL, PSYCHIATRIC AND METABOLIC DISORDERS AND DISEASES
  申请人：Janssen Pharmaceutica, N.V.

  公开号：EP2545055A1

  公开（公告）日：2013-01-16
• COMBINATIONS COMPRISING PDE 2 INHIBITORS SUCH AS 1-ARYL-4-METHYL- [1,2,4]TRIAZOLO [4,3-A]QUINOXALINE COMPOUNDS AND PDE 10 INHIBITORS FOR USE IN THE TREATMENT OF NEUROLOGICAL OR METABOLIC DISORDERS
  申请人：Janssen Pharmaceutica N.V.

  公开号：EP2863909A1

  公开（公告）日：2015-04-29