7,8-dimethylimidazo[1,2-a]pyridine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 英文名称: 7,8-dimethylimidazo[1,2-a]pyridine
• 化学式: C₉H₁₀N₂
• 分子量: 146.192
• InChiKey: ICSRJCBRZXLNKZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  17.3
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  7,8-dimethylimidazo[1,2-a]pyridine 在 N-碘代丁二酰亚胺 作用下， 以 氯仿 为溶剂， 反应 18.0h， 以19%的产率得到3-iodo-7,8-dimethylimidazo[1,2-a]pyridine
  参考文献：
  名称：

  HPK1 ANTAGONISTS AND USES THEREOF

  摘要：

  本发明提供了化合物、其组合物以及使用这些化合物用于抑制HPK1和治疗HPK1介导的疾病的方法。

  公开号：

  US20210078996A1
• 作为产物：
  描述：

  氯乙醛 、 2-氨基-3,4-二甲基吡啶 以 乙醇 、 水 为溶剂， 反应 18.0h， 以81%的产率得到7,8-dimethylimidazo[1,2-a]pyridine
  参考文献：
  名称：

  HPK1 ANTAGONISTS AND USES THEREOF

  摘要：

  本发明提供了化合物、其组合物以及使用这些化合物用于抑制HPK1和治疗HPK1介导的疾病的方法。

  公开号：

  US20210078996A1

文献信息

• [EN] NOVEL PHENYLIMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS<br/>[FR] NOUVEAU DÉRIVÉS DE PHÉNYLIMIDAZOLE CONVENANT COMME INHIBITEURS DE L'ENZYME PDE10A
  申请人：LUNDBECK & CO AS H

  公开号：WO2009152825A1

  公开（公告）日：2009-12-23

  This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective, amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula (I). The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I).

  该发明涉及一种PDE10A酶抑制剂的化合物。该发明提供了一种包含该发明化合物的治疗有效量和药用可接受载体的药物组合物。本发明还提供了一种制备公式（I）化合物的方法。本发明还提供了一种治疗患有神经退行性疾病的受试者的方法，包括向受试者投与公式（I）化合物的治疗有效量。本发明还提供了一种治疗患有药物成瘾的受试者的方法，包括向受试者投与公式（I）化合物的治疗有效量。本发明还提供了一种治疗患有精神障碍的受试者的方法，包括向受试者投与公式（I）化合物的治疗有效量。
• BICYCLIC HETEROCYCLIC COMPOUND
  申请人：Nakai Hisao

  公开号：US20090281120A1

  公开（公告）日：2009-11-12

  A compound represented by the formula (I), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof: wherein X, Y, and W each independently represent a carbon atom or a nitrogen atom; Z represents CH or a nitrogen atom; R 1 represents (1) C3-10 branched alkyl which may be substituted or (2) —(CH 2 ) m —NR 4 R 5 ; R 2 and R 3 each independently represent (1) a hydrogen atom, (2) C1-4 alkyl which may be substituted with a halogen atom, hydroxy which may be protected, amino which may be protected, or carboxyl which may be protected, (3) C2-4 alkenyl, (4) C2-4 alkynyl, (5) nitrile, (6) COOR 6 , (7) CONR 7 R 8 , (8) COR 101 , (9) S(O) n R 102 , or (10) a halogen atom, in which R 6 represents a hydrogen atom or C1-4 alkyl, R 7 and R 8 each independently represent a hydrogen atom or C1-4 alkyl, R 101 represents a hydrogen atom or C1-4 alkyl, R 102 represents C1-4 alkyl, n represents 1 or 2; and Ar represents an aromatic ring which may be substituted, is useful as a pharmacologically active ingredient having a CRF antagonist action in preventing and/or treating neuropsychiatric diseases, diseases of peripheral organs or the like.

  化合物的化学式为（I），其盐，N-氧化物，溶剂化合物或前药：其中X，Y和W各自独立地表示碳原子或氮原子；Z表示CH或氮原子；R1表示（1）C3-10支链烷基，可以被取代或（2）—（CH2）m—NR4R5；R2和R3各自独立地表示（1）氢原子，（2）C1-4烷基，可以用卤原子，羟基，氨基或羧基进行保护取代，（3）C2-4烯基，（4）C2-4炔基，（5）腈基，（6）COOR6，（7）CONR7R8，（8）COR101，（9）S（O）nR102或（10）卤原子，其中R6表示氢原子或C1-4烷基，R7和R8各自独立地表示氢原子或C1-4烷基，R101表示氢原子或C1-4烷基，R102表示C1-4烷基，n表示1或2；而Ar表示一个芳香环，可以被取代，是一种具有CRF拮抗剂作用的药理活性成分，可用于预防和/或治疗神经精神疾病，外周器官疾病等。
• COMPOUND AS ACC INHIBITOR AND USE THEREOF
  申请人：Nanjing Sanhome Pharmaceutical Co., Ltd.

  公开号：EP3660023A1

  公开（公告）日：2020-06-03

  Disclosed are a class of compounds which are inhibitors of acetyl-CoA carboxylase (ACC) and the use thereof. In particular, provided are compounds as shown in formula I or isomers, pharmaceutically acceptable salts, solvates, crystals or prodrugs thereof, and methods for preparing the same, and pharmaceutical compositions comprising the compounds and the use of the compounds or compositions for treating and/or preventing diseases associated with ACC expression, such as fibrotic diseases, metabolic diseases, cancers or tissue hyperplasia diseases. The compound has a good inhibitory activity against ACC and shows good promise to be a therapeutic drug for fibrotic diseases, metabolic diseases, cancers or tissue hyperplasia diseases.

  本发明公开了一类乙酰-CoA羧化酶（ACC）抑制剂化合物及其用途。特别是，提供了如式 I 所示的化合物或异构体、其药学上可接受的盐、溶液剂、晶体或原药，以及制备方法、包含该化合物的药物组合物和该化合物或组合物用于治疗和/或预防与 ACC 表达相关的疾病，如纤维化疾病、代谢性疾病、癌症或组织增生疾病。该化合物对 ACC 具有良好的抑制活性，很有希望成为纤维化疾病、代谢性疾病、癌症或组织增生疾病的治疗药物。
• Substituted isoindolin-1-ones and 2,3-dihydro-1H-pyrrol[3,4-c]pyridin-1-ones as HPK1 antagonists
  申请人：Nimbus Saturn, Inc.

  公开号：US11078201B2

  公开（公告）日：2021-08-03

  The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.

  本发明提供了用于抑制 HPK1 和治疗 HPK1 介导的疾病的化合物、其组合物和使用方法。
• Substituted isoindolin-1-ones and 2,3-dihydro-1h-pyrrolo[3,4-c]pyridin-1-ones as HPK1 antagonists
  申请人：Nimbus Saturn, Inc.

  公开号：US11021481B2

  公开（公告）日：2021-06-01

  The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.

  本发明提供了用于抑制 HPK1 和治疗 HPK1 介导的疾病的化合物、其组合物和使用方法。