2-甲基-1,2,3,4-四氢吡嗪并[1,2-a]苯并咪唑 | 115213-55-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 中文名称: 2-甲基-1,2,3,4-四氢吡嗪并[1,2-a]苯并咪唑
• 英文名称: 2-methyl-1,2,3,4-tetrahydro-benz[4,5]imidazo[1,2-a]pyrazine
• 英文别名: 2-Methyl-1,2,3,4-tetrahydro-benz[4,5]imidazo[1,2-a]pyrazin；2-Methyl-1,2,3,4-tetrahydropyrazino[1,2-a]benzimidazole；2-methyl-3,4-dihydro-1H-pyrazino[1,2-a]benzimidazole
• CAS: 115213-55-3
• 化学式: C₁₁H₁₃N₃
• mdl: MFCD11844488
• 分子量: 187.244
• InChiKey: IYOLRZWFJQGDNY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  21.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-甲基-1,2,3,4-四氢吡嗪并[1,2-a]苯并咪唑 、 碘甲烷 生成 2,2-dimethyl-1,2,3,4-tetrahydro-benz[4,5]imidazo[1,2-a]pyrazinium; iodide
  参考文献：
  名称：

  Piperazino-1'，2'：1,2-苯并咪唑

  摘要：

  合成哌嗪子-1'，2'：1,2-苯并达唑-环系统的反应：（b）杜林（Ringschluss）eines geeignet替代Piperazins zum Benzimidazol-Derivat nach der Methode von Saunders 2。

  DOI：

  10.1002/hlca.19560390416
• 作为产物：
  描述：

  1-乙酰基-4-(2-硝基-苯基)-哌嗪 在 盐酸 、 palladium on activated charcoal 、 sodium azide 、 乙醇 、 sodium acetate 、 丙酮 、 sodium nitrite 作用下， 生成 2-甲基-1,2,3,4-四氢吡嗪并[1,2-a]苯并咪唑
  参考文献：
  名称：

  Piperazino-1'，2'：1,2-苯并咪唑

  摘要：

  合成哌嗪子-1'，2'：1,2-苯并达唑-环系统的反应：（b）杜林（Ringschluss）eines geeignet替代Piperazins zum Benzimidazol-Derivat nach der Methode von Saunders 2。

  DOI：

  10.1002/hlca.19560390416

文献信息

• T-TYPE CALCIUM CHANNEL INHIBITOR
  申请人：NISSAN CHEMICAL INDUSTRIES, LTD.

  公开号：US20160237071A1

  公开（公告）日：2016-08-18

  A novel compound that has an excellent T-type calcium channel inhibitory activity and is specifically useful for prevention or treatment of pain, chronic kidney disease and atrial fibrillation. The novel triazinone compound of Formula (I): where each substituent in the formula is defined in detail in the description, and R 1 could be a hydrogen atom, or a C 1-6 alkyl group, etc., E could be a 7 to 14-membered non-aromatic fused heterocyclic group, L 3 could be a C 1-6 alkylene group, etc., D could be a C 6-14 aryl group or a 5 to 10-membered heteroaryl group each of which is optionally substituted, etc., a tautomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof.

  一种新型化合物，具有出色的T型钙通道抑制活性，特别适用于预防或治疗疼痛、慢性肾脏疾病和心房颤动。该新型三嗪酮化合物的化学式为（I），其中公式中的每个取代基在描述中都有详细定义，R1可以是氢原子或C1-6烷基等，E可以是7-14个成员的非芳香融合杂环基，L3可以是C1-6亚烷基等，D可以是C6-14芳基或5-10个成员的杂环芳基，每个基团都可以有选择性地取代等，该化合物的互变异构体或药学上可接受的盐或溶剂化物。
• Inhibitors of ADAMTS4 or ADAMTS5 for use in preventing or treating cardiac remodeling and chronic heart failure
  申请人：Universitetet i Oslo

  公开号：US10322143B2

  公开（公告）日：2019-06-18

  The present invention provides an inhibitor of an ADAMTS proteoglycanase for use in treating or preventing cardiac remodeling or for use in treating or preventing heart failure in a subject. In particular, the present invention provides an inhibitor of ADAMTS4 or ADAMTS5 for use in treating or preventing cardiac remodeling or chronic heart failure in a subject with cardiac remodeling or with chronic heart failure, or with a condition that may lead to cardiac remodeling and/or chronic heart failure. Also provided is a method of treating or preventing cardiac remodeling or treating or preventing heart failure which method comprises administering to a subject in need thereof a therapeutically effective amount of an inhibitor of an ADAMTS proteoglycanase. Also provided is the use of an inhibitor of an ADAMTS proteoglycanase in the manufacture of a medicament for treating or preventing cardiac remodeling or treating or preventing heart failure.

  本发明提供了一种ADAMTS蛋白聚糖酶抑制剂，用于治疗或预防心脏重塑或用于治疗或预防受试者的心力衰竭。特别是，本发明提供了一种ADAMTS4或ADAMTS5的抑制剂，用于治疗或预防患有心脏重塑或慢性心力衰竭或可能导致心脏重塑和/或慢性心力衰竭的病症的受试者的心脏重塑或慢性心力衰竭。还提供了一种治疗或预防心脏重塑或治疗或预防心衰的方法，该方法包括向有需要的受试者施用治疗有效量的 ADAMTS 蛋白聚糖酶抑制剂。还提供了一种ADAMTS蛋白聚糖酶抑制剂在制造治疗或预防心脏重塑或治疗或预防心衰的药物中的用途。
• Ferroportin inhibitors
  申请人：Vifor (International) AG

  公开号：US11001579B2

  公开（公告）日：2021-05-11

  The invention relates to novel compounds of the general formula (I), with Het-2 being an optionally substituted bicyclic heteroaryl of the formula pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for the use as ferroportin inhibitors, more particularly for the use in the prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, such as particularly iron overload states such as in particular thalassemia and hemochromatosis.

  本发明涉及通式 (I) 的新型化合物、 式中 Het-2 为任选取代的双环杂芳基 由它们组成的药物组合物及其作为药物的用途，特别是作为铁蛋白抑制剂的用途，尤其是用于预防和/或治疗因缺乏肝素或铁代谢紊乱引起的疾病，如特别是铁过载状态，如地中海贫血症和血色病。
• TRICYCLIC COMPOUNDS FOR USE IN TREATMENT OF PROLIFERATIVE DISORDERS.
  申请人：Argonaut Therapeutics Limited

  公开号：EP3596073B1

  公开（公告）日：2022-05-11
• INHIBITORS OF ADAMTS4 OR ADAMTS5 FOR USE IN PREVENTING OR TREATING CARDIAC REMODELING AND CHRONIC HEART FAILURE
  申请人：UNIVERSITETET I OSLO

  公开号：US20160158271A1

  公开（公告）日：2016-06-09

  The present invention provides an inhibitor of an ADAMTS proteoglycanase for use in treating or preventing cardiac remodeling or for use in treating or preventing heart failure in a subject. In particular, the present invention provides an inhibitor of ADAMTS4 or ADAMTS5 for use in treating or preventing cardiac remodeling or chronic heart failure in a subject with cardiac remodeling or with chronic heart failure, or with a condition that may lead to cardiac remodeling and/or chronic heart failure. Also provided is a method of treating or preventing cardiac remodeling or treating or preventing heart failure which method comprises administering to a subject in need thereof a therapeutically effective amount of an inhibitor of an ADAMTS proteoglycanase. Also provided is the use of an inhibitor of an ADAMTS proteoglycanase in the manufacture of a medicament for treating or preventing cardiac remodeling or treating or preventing heart failure.