1-{5-[2-(3,5-dichloro-pyridin-4-yl)-acetyl]-8-methoxy-[1,2,4]triazolo[1,5-a]pyridin-2-yl}-cyclopropanecarboxylic acid (pyridin-2-ylmethyl)-amide | 1072077-80-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并三嗪类
• 英文名称: 1-{5-[2-(3,5-dichloro-pyridin-4-yl)-acetyl]-8-methoxy-[1,2,4]triazolo[1,5-a]pyridin-2-yl}-cyclopropanecarboxylic acid (pyridin-2-ylmethyl)-amide
• 英文别名: 1-[5-[2-(3,5-dichloropyridin-4-yl)acetyl]-8-methoxy-[1,2,4]triazolo[1,5-a]pyridin-2-yl]-N-(pyridin-2-ylmethyl)cyclopropane-1-carboxamide
• CAS: 1072077-80-5
• 化学式: C₂₄H₂₀Cl₂N₆O₃
• 分子量: 511.367
• InChiKey: RSUNKVROVYIJRB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  35
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  111
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• TRIAZOLOPYRIDINES AS PHOSPHODIESTERASE INHIBITORS FOR TREATMENT OF DERMAL DISEASES
  申请人：Felding Jakob

  公开号：US20100113442A1

  公开（公告）日：2010-05-06

  The present invention relates to a compound according to formula (I), wherein X and Y are either C and N or N and C; Z is CH 2 , CH 2 —CH 2 , CH 2 —NH, or NH; R 1 is halogen, or R 1 is alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, cycloalkyl, alkoxycarbonyl, aryl, all of which are optionally substituted; R 2 is hydrogen, or R 2 is alkyl, cycloalkyl, alkoxy, heterocycloalkyl, aryl, heteroaryl, alkoxycarbonyl, aminocarbonyl, amino, all of which are optionally substituted; A is aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocycloalkyl or heterocycloalkenyl, all of which are optionally substituted; and pharmaceutically acceptable salts, hydrates, or solvates hereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments, in particular for the treatment of dermal diseases.

  本发明涉及一种化合物，其化学式为（I），其中X和Y分别为C和N或N和C；Z为CH2， - ， -NH或NH；R1为卤素，或R1为烷基，烯基，炔基，卤代烷基，烷氧基，环烷基，烷氧羰基，芳基，所有这些均可选择性地被取代；R2为氢，或R2为烷基，环烷基，烷氧基，杂环烷基，芳基，杂芳基，烷氧羰基，氨基羰基，氨基，所有这些均可选择性地被取代；A为芳基，环烷基，环烯基，杂芳基，杂环烷基或杂环烯基，所有这些均可选择性地被取代；以及其药学上可接受的盐，水合物或溶剂化物。本发明进一步涉及所述化合物在治疗中的应用，包括含有该化合物的制药组合物，使用该化合物治疗疾病的方法，例如皮肤疾病，并且涉及使用该化合物制造药物，特别是用于治疗皮肤疾病。
• US8829190B2
  申请人：——

  公开号：US8829190B2

  公开（公告）日：2014-09-09