3-(2-Methoxypyridin-4-yl)-6-(trifluoromethyl)pyridazine | 1173155-65-1

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 3-(2-Methoxypyridin-4-yl)-6-(trifluoromethyl)pyridazine
• CAS: 1173155-65-1
• 化学式: C₁₁H₈F₃N₃O
• 分子量: 255.199
• InChiKey: PWENPURWDBJDIM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  47.9
• 氢给体数：
  0
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  3-(2-Methoxypyridin-4-yl)-6-(trifluoromethyl)pyridazine 在 水 作用下， 以 盐酸 为溶剂， 反应 18.0h， 以to provide the title compound (120 mg, quant) as a white solid的产率得到4-(6-(trifluoromethyl)pyridazin-3-yl)pyridin-2(1H)-one
  参考文献：
  名称：

  Azinone-substituted azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine MCH-1 antagonists, methods of making, and use thereof

  摘要：

  本发明披露了小说MCH-1受体拮抗剂。这些化合物用于治疗各种疾病，包括肥胖症、焦虑、抑郁症、非酒精性脂肪肝病和精神障碍。本发明还描述了制备这些化合物的方法。

  公开号：

  US09073925B2
• 作为产物：
  描述：

  3-氯-6-三氟甲基哒嗪 、 2-甲氧基吡啶-4-戊酰硼酸 以to provide the title compound (115 mg, 60%) as a white solid的产率得到3-(2-Methoxypyridin-4-yl)-6-(trifluoromethyl)pyridazine
  参考文献：
  名称：

  (1-AZINONE)-SUBSTITUTED PYRIDOINDOLES

  摘要：

  用于治疗各种疾病的制药组合物中的取代吡啶并吲哚对应于式(I)，其中R1为H或可选取代的烷基；R2、R3、R4各自独立地选自H、—O-烷基、—S-烷基、烷基、卤素、—CF3和—CN；G为—CR12R13—NR5—或—NR5—CR12R13；R5为H、可选取代的烷基、可选取代的杂环、—C(═O)—R6、—C(═O)—O—R7或—C(═O)—NR19R20；R6和R7各自可选取代的烷基或可选取代的杂环；R8、R9、R10、R11、R12、R13、R19和R20各自独立地选自H或可选取代的烷基；R14和R15各自独立地为H或卤素；L为—CH2—O—、—CH2CH2—、—CH═CH—或键；B为芳基或杂芳基或环烷基；但当L为直接键时，B不能为未取代的杂芳基或单取代氟的杂芳基。

  公开号：

  US20160159798A1

文献信息

• [EN] (1-AZINONE) -SUBSTITUTED PYRIDOINDOLES AS MCH ANTAGONISTS<br/>[FR] PYRIDOINDOLES (1-AZINONE)-SUBSTITUÉS EN TANT QU'ANTAGONISTES MCH
  申请人：ALBANY MOLECULAR RES INC

  公开号：WO2009089482A1

  公开（公告）日：2009-07-16

  Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein R1 is H or optionally substituted alkyl; R2, R3, R4 are each independently selected from H, -O-alkyl, -S-alkyl, alkyl, halo, -CF3, and -CN; G is -CR12R13-NR5- or -NR5-CR12R13; R5 is H, optionally substituted alkyl, optionally substituted heterocycle, -C(=O)-R6, -C(=O)-O-R7, or -C(=O)-NR19R20; R6 and R7 are each optionally substituted alkyl or optionally substituted heterocycle; R8, R9, R10, R11, R12, R13, R19 and R20 are each independently selected from H or optionally substituted alkyl; R14 and R15 are each independently H or halogen; L is -CH2-O-, -CH2CH2-, -CH=CH- or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.

  将吡啶吲哚替代物用于制药组合物中，用于治疗各种疾病，对应于式（I），其中R1为H或可选择的取代烷基；R2、R3、R4分别独立选择自H、-O-烷基、-S-烷基、烷基、卤素、-CF3和-CN；G为-CR12R13-NR5-或-NR5-CR12R13；R5为H、可选择的取代烷基、可选择的取代杂环、-C(=O)-R6、-C(=O)-O-R7或-C(=O)-NR19R20；R6和R7分别为可选择的取代烷基或可选择的取代杂环；R8、R9、R10、R11、R12、R13、R19和R20分别独立选择自H或可选择的取代烷基；R14和R15分别独立为H或卤素；L为-CH2-O-、-CH2CH2-、-CH=CH-或一个键；B为芳基或杂芳基或环烷基；但条件是，当L为直接键时，B不能是未取代的杂芳基或单取代氟的杂芳基。
• AZINONE-SUBSTITUTED AZEPINO[b]INDOLE AND PYRIDO-PYRROLO-AZEPINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF
  申请人：Guzzo Peter R.

  公开号：US20110003793A1

  公开（公告）日：2011-01-06

  Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.

  揭示了新型MCH-1受体拮抗剂。这些化合物用于治疗各种疾病，包括肥胖、焦虑、抑郁、非酒精性脂肪肝病和精神疾病。本发明还描述了制备这些化合物的方法。
• AZABICYCLOALKANE-INDOLE AND AZABICYCLOALKANE-PYRROLO-PYRIDINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF
  申请人：GUZZO Peter R.

  公开号：US20110003737A1

  公开（公告）日：2011-01-06

  Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.

  揭示了新型MCH-1受体拮抗剂。这些化合物用于治疗各种疾病，包括肥胖、焦虑、抑郁、非酒精性脂肪肝病和精神障碍。本发明还描述了制备这些化合物的方法。
• TETRAHYDRO-AZACARBOLINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USES THEREOF
  申请人：SURMAN Matthew D.

  公开号：US20120157460A1

  公开（公告）日：2012-06-21

  The present invention relates to tetrahydro-azacarboline derivatives of formula (I): having the substituents as described herein which are melanin-concentrating hormone (MCH-1) receptor antagonists. The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof.

  本发明涉及式(I)的四氢-吖啶咔啉衍生物，其具有如本文所述的取代基，这些取代基是黑素浓缩激素（MCH-1）受体拮抗剂。本发明还涉及包括这些化合物的药物组合物，以及其制备和使用方法。
• AZINONE-SUBSTITUTED AZABICYCLOALKANE-INDOLE AND AZABICYCLOALKANE-PYRROLO-PYRIDINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF
  申请人：GUZZO Peter R.

  公开号：US20110003739A1

  公开（公告）日：2011-01-06

  Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.

  揭示了新型MCH-1受体拮抗剂。这些化合物用于治疗各种疾病，包括肥胖、焦虑、抑郁、非酒精性脂肪肝病和精神障碍。本发明还描述了制备这些化合物的方法。