Pyrazolo<1.5-c>chinazolin | 234-65-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: Pyrazolo<1.5-c>chinazolin
• 英文别名: Pyrazolo[1,5-c]quinazoline
• CAS: 234-65-1
• 化学式: C₁₀H₇N₃
• 分子量: 169.186
• InChiKey: ONCMJWSDNCJMLL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  30.2
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] TRIAZOLO- AND PYRAZOLOQUINAZOLINE DERIVATIVES AS PDE10A ENZYME INHIBITOR<br/>[FR] DÉRIVÉS DE TRIAZOLO- ET DE PYRAZOLOQUINAZOLINE EN TANT QU'INHIBITEURS D'ENZYME PDE10A
  申请人：LUNDBECK & CO AS H

  公开号：WO2012007006A1

  公开（公告）日：2012-01-19

  The invention relates to compounds of the formula (I) and their use as pharmaceutical ingredients, in particular for the treatment of CNS related diseases.

  本发明涉及式(I)化合物的用途，以及它们作为药物成分的应用，特别是用于治疗与中枢神经系统相关的疾病。
• Process for preparing pyrazolo(1,5-c)-quinazoline derivatives and novel intermediates
  申请人：E.R. Squibb & Sons, Inc.

  公开号：EP0023773A1

  公开（公告）日：1981-02-11

  A process is provided for preparing pyrazolo[1,5-c]-quinazoline derivatives of the structure wherein X is 0 or S; R' is hydrogen, lower alkyl, hydroxymethyl, phenyl-lower alkyl, phenyl or phenyl substituted with halogen, lower alkyl, lower alkoxy, or trifluoromethyl; R2 is lower alkoxy, phenyl-lower alkoxy, phenoxy, or phenoxy substituted with lower alkyl or lower alkoxy; and R3 and R4 are the same or different and are selected from the group consisting of hydrogen, alkyl of 1 to 4 carbons, alkoxy of 1 to 4 carbons, lower alkanoyloxy of 1 to 4 carbons, nitro, benzyloxy, benzyloxy having a single mono- lower alkoxy substituent, halogen, hydroxy, and trifluoromethyl, wherein quinolone compounds of the structure which are new intermediates, are reacted with a hydrazine compound to form a 5-(2-aminophenyl)-pyrazole which is then cyclized to the product. In addition, the above product may be reacted with a halogen acid to form the corresponding hydroxymethyl compound.

  本发明提供了一种制备吡唑并[1,5-c]-喹唑啉衍生物的方法，其结构如下： 其中，X为0或S；R'为氢、低碳基、羟甲基、苯基-低碳基、苯基或卤素、低碳基、低碳氧基或三氟甲基取代的苯基；R2为低碳氧基、苯基-低碳氧基、苯氧基或低碳基或低碳氧基取代的苯氧基；R3和R4相同或不同，选自氢、1至4碳的烷基、1至4碳的烷氧基、1至4碳的低烷酰氧基、硝基、苄氧基、带有单一单一低烷氧基取代基的苄氧基、卤素、羟基和三氟甲基的群，其中新的中间体结构的喹啉化合物如下： 与肼化合物反应形成5-(2-氨基苯基)-吡唑，然后环化成产物。此外，上述产物可以与卤素酸反应形成相应的羟甲基化合物。
• METHODS FOR USE OF SMALL MOLECULE ACTIVATORS OF HEM-Y / PROTOPORPHYRINOGEN OXIDASE (PPO)
  申请人：Vanderbilt University

  公开号：US20160213780A1

  公开（公告）日：2016-07-28

  A method for treating a microbial infection involves administering an effective amount of a compound of the formula: wherein R 1 is H, alkyl, aryl, heteroaryl, R 2 is H, halogen, alkyl, aryl, heteroaryl, R 3 is H, hydroxyl, alkoxy, alkyl, aryl, heteroaryl, amino, amino sulfonyl, acetamide, R 4 is H, hydroxyl, alkoxy, alkyl, aryl, heteroaryl, amino, amino sulfonyl, acetamide, R 5 is H, hydroxyl, alkoxy, alkyl, aryl, heteroaryl, amino, amino sulfonyl, acetamide, R 6 is H, hydroxyl, alkoxy, alkyl, aryl, heteroaryl, amino, amino sulfonyl, acetamide, R 7 is H, hydroxyl, alkoxy, alkyl, aryl, heteroaryl, amino, amino sulfonyl, acetamide, R 8 is —CR 3 , O, S, wherein R 5 and R 6 , R 7 and R 6 , R 5 and R 4 , R 4 and R 3 can cyclize forming a 3-10 member ring comprising C, O, S, and/or N optionally substituted with one or more R 3 ; and administering light therapy, such as a photodynamic therapy (PDT) light source.

  一种治疗微生物感染的方法包括给予一定量的化合物，其化学式为：其中R1为H，烷基，芳基，杂环芳基，R2为H，卤素，烷基，芳基，杂环芳基，R3为H，羟基，烷氧基，烷基，芳基，杂环芳基，氨基，氨基磺酰基，乙酰胺基，R4为H，羟基，烷氧基，烷基，芳基，杂环芳基，氨基，氨基磺酰基，乙酰胺基，R5为H，羟基，烷氧基，烷基，芳基，杂环芳基，氨基，氨基磺酰基，乙酰胺基，R6为H，羟基，烷氧基，烷基，芳基，杂环芳基，氨基，氨基磺酰基，乙酰胺基，R7为H，羟基，烷氧基，烷基，芳基，杂环芳基，氨基，氨基磺酰基，乙酰胺基，R8为—CR3，O，S，其中R5和R6，R7和R6，R5和R4，R4和R3可以环化形成一个由C，O，S和/或N组成的3-10成员环，可选地取代一个或多个R3；并且给予光疗法，例如光动力疗法（PDT）光源。
• NITROGEN-CONTAINING FUSED TRICYCLIC COMPOUND AND USE THEREOF AS AGROFORESTRY INSECTICIDE
  申请人：South China Agricultural University

  公开号：EP3689877A1

  公开（公告）日：2020-08-05

  Disclosed are a nitrogen-containing fused tricyclic compound, an optical isomer, cis and trans isomers or an agromedically acceptable salt thereof, and the insecticidal use thereof in agroforestry. The delayed working effect of the compound on pests such as red imported fire ants can make the pests carry the drug to a nest, thereby having a better killing effect on the whole red imported fire ants nest and the queen ant.

  本发明公开了一种含氮融合三环化合物、一种光学异构体、顺式和反式异构体或其农用可接受盐及其在农林业中的杀虫用途。该化合物对红火蚁等害虫的延时作用可使害虫将药物带至蚁巢，从而对整个红火蚁蚁巢和蚁后产生更好的杀灭效果。
• FUSED HETEROCYCLIC COMPOUND, PYRAZOLE-RING-CONTAINING FUSED HETEROCYCLIC COMPOUND, AGRICULTURAL COMPOSITION CONTAINING THEREOF, AND METHOD OF USING THE COMPOSITION
  申请人：SOUTH CHINA AGRICULTURAL UNIVERSITY

  公开号：US20210188853A1

  公开（公告）日：2021-06-24

  A fused tricyclic compound, an optical isomer, cis and trans isomers or an agromedically acceptable salt thereof, and insecticidal use thereof in agroforestry. A pyrazole-ring-contained fused heterocyclic compound, an agricultural composition, and a method of using the agricultural composition are also provided.