3-[6-(2-methoxyethoxy)-3-pyridinyl]-2-methyl-8-(4-pyridinyl)-imidazo[1,2-b]pyridazine hydrochloride | 1298031-90-9

• 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: 3-[6-(2-methoxyethoxy)-3-pyridinyl]-2-methyl-8-(4-pyridinyl)-imidazo[1,2-b]pyridazine hydrochloride
• 英文别名: 3-[6-(2-Methoxyethoxy)pyridin-3-yl]-2-methyl-8-pyridin-4-ylimidazo[1,2-b]pyridazine;hydrochloride
• CAS: 1298031-90-9
• 化学式: C₂₀H₁₉N₅O₂*ClH
• 分子量: 397.864
• InChiKey: QBXRUDVQFOBPAP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.61
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  74.4
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  3-[6-(2-methoxyethoxy)-3-pyridinyl]-2-methyl-8-(4-pyridinyl)-imidazo[1,2-b]pyridazine 在 盐酸 作用下， 以 乙醚 、 二氯甲烷 为溶剂， 反应 2.5h， 以91%的产率得到3-[6-(2-methoxyethoxy)-3-pyridinyl]-2-methyl-8-(4-pyridinyl)-imidazo[1,2-b]pyridazine hydrochloride
  参考文献：
  名称：

  IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS

  摘要：

  本发明涉及新型咪唑并[1,2-b]吡啶嗪衍生物，其为磷酸二酯酶10（PDE10）的抑制剂，并且适用于治疗或预防涉及PDE10酶的神经、精神和代谢紊乱。该发明还涉及包含这种化合物的药物组合物，用于制备这种化合物和组合物的方法，以及利用这种化合物或药物组合物预防或治疗神经、精神和代谢紊乱和疾病。

  公开号：

  US20110269752A1

文献信息

• [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。
• [EN] IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS<br/>[FR] DÉRIVÉS D'IMIDAZO[1,2-B]PYRIDAZINE ET LEUR UTILISATION COMME INHIBITEURS DE PDE10
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2011051342A8

  公开（公告）日：2011-07-07
• 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
• COMBINATIONS COMPRISING 4-METHYL-[1,2,4]TRIAZOLO[4,3-A]QUINOXALINE COMPOUNDS AS PDE 2 INHIBITORS AND PDE 10 INHIBITORS FOR USE IN THE TREATMENT OF NEUROLOGICAL OR METABOLIC DISORDERS
  申请人：Janssen Pharmaceutica N.V.

  公开号：EP2863909B1

  公开（公告）日：2020-11-04
• 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 OF METABOLIC DISORDERS
  申请人：Janssen Pharmaceutica NV

  公开号：US20150366873A1

  公开（公告）日：2015-12-24

  The present invention relates to combinations of phosphodiesterase 2 (PDE2) inhibitors with inhibitors of phosphodiesterase 10 (PDE10). 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 2011/051324 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.