1-(4-hydroxyphenyl)-3-phenyl-1H-pyrazolo[3,4-b]pyridine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 1-(4-hydroxyphenyl)-3-phenyl-1H-pyrazolo[3,4-b]pyridine
• 英文别名: 4-(3-phenylpyrazolo[3,4-b]pyridin-1-yl)phenol
• 化学式: C₁₈H₁₃N₃O
• 分子量: 287.321
• InChiKey: LJAZEBCLHPGEFO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  50.9
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-(4-hydroxyphenyl)-3-phenyl-1H-pyrazolo[3,4-b]pyridine 、 3-氯-1-丙醇 生成 ethyl acetate diisopropyl ether
  参考文献：
  名称：

  Fused pyrazole compounds and pharmaceutical use thereof

  摘要：

  一种新型融合吡唑化合物，其一般式为##STR1##其中所有符号均如规范中所定义或其药学上可接受的盐，具有刺激白细胞吞噬作用、刺激巨噬细胞吞噬作用、恢复白细胞减少症、刺激非特异性抗感染能力、抗肿瘤作用、激活免疫反应等作用，因此可用于药物。

  公开号：

  US05006520A1

文献信息

• FUSED PYRAZOLE COMPOUNDS, PROCESS FOR THEIR PREPARATION, AND THEIR MEDICINAL USE
  申请人：Yoshitomi Pharmaceutical Industries, Ltd.

  公开号：EP0338087A1

  公开（公告）日：1989-10-25

  Novel fused pyrazole compounds represented by general formula (I) (wherein X represents =N- or =CH-, R repre­sents H, alkyl, alkoxy or halogen, Y¹ represents α, phenyl or phenyl substituted by halogen, alkyl or alkoxy, Y² represents β, -A²-B², H, alkyl, substituted alkyl, phenyl or phenyl substituted by a substituent selected from the group consisting of halogen, alkyl and alkoxy, provided that at least one of Y¹ and Y² represents α or β, Z¹ and Z² each represents -O-, -S- or -NR³ (wherein R³ represents H or alkyl), A¹ and A² each represents alkylene, B¹ and B² each represents carboxyl, alkoxy­carbonyl or phenylalkoxycarbonyl wherein the phenyl group may optionally be substituted by a substituent selected from the group consisting of halogen, alkyl and alkoxy, acyl, -OH, acyloxy, γ or λ (wherein R¹ and R² represents H, alkyl, dial­kylaminoalkyl, hydroxyalkyl or, when taken together, R¹ and R² represent a group forming a heterocyclic ring together with the adjacent nitrogen atom), and L¹ and L² each represents halogen, alkyl or alkoxy) and salts thereof, a process for their preparation and a medicinal composition containing same are disclosed. The compounds have the action of increa­sing phagocytosis of leucocytes, that of increasing phagocytosis of macrophage, that of restoring the number of leucocytes, that of activating infection protective function, that of improving immunological competence, an antitumor action, etc. ABSTRACT Novel fused pyrazole compounds of the general formula wherein all the symbols are as defined in the specification or its pharmaceutically acceptable salt which possesses a stimulating action on phagocytosis of leukocytes, a stimulating action on phagocytosis of macrophages, a restorative action on leukopenia, a stimulating action on non-specific resistance to infection, an antitumour action, an activating action on immune responses and the like, and therefore is of use as a pharmaceutical.

  通式(I)代表的新型融合吡唑化合物（其中X代表＝N-或＝CH-，R代表H、烷基、烷氧基或卤素，Y¹代表α、苯基或被卤素、烷基或烷氧基取代的苯基，Y²代表β、-A²-B²、H、烷基、取代的烷基、苯基或被选自卤素、烷基和烷氧基的取代基取代的苯基，条件是 Y¹ 和 Y² 中至少有一个代表 α 或 β，Z¹ 和 Z² 各自代表 -O-、-S- 或 -NR³（其中 R³ 代表 H 或烷基），A¹ 和 A² 各自代表亚烷基，B¹ 和 B² 各自代表羧基、烷氧基羰基或苯基烷氧基羰基，其中苯基可任选被选自卤素、烷基和烷氧基、酰基、-OH、酰氧基、γ 或 λ （其中 R¹ 和 R² 代表 H、烷基、二烷基氨基烷基、羟基烷基或）的取代基取代、公开了 R¹ 和 R² 代表与相邻氮原子一起形成杂环的基团，L¹ 和 L² 各自代表卤素、烷基或烷氧基）及其盐、制备方法和含有这些化合物的药物组合物。这些化合物具有增加白细胞吞噬功能、增加巨噬细胞吞噬功能、恢复白细胞数量、激活感染保护功能、提高免疫能力、抗肿瘤等作用。 摘要 通式如下的新型融合吡唑化合物 其中所有符号如说明书中所定义，或其药学上可接受的盐，具有刺激白细胞吞噬作用、刺激巨噬细胞吞噬作用、恢复白细胞减少作用、刺激非特异性抗感染作用、抗肿瘤作用、激活免疫反应作用等，因此可用作药物。
• OEH, TAKANORI;MASUOKA, XIROYUKI;KURU, MASAO;YAMAKAMI, KEHJDZI
  作者：OEH, TAKANORI、MASUOKA, XIROYUKI、KURU, MASAO、YAMAKAMI, KEHJDZI

  DOI：——

  日期：——
• US5006520A
  申请人：——

  公开号：US5006520A

  公开（公告）日：1991-04-09
• Fused pyrazole compounds and pharmaceutical use thereof
  申请人：Yoshitomi Pharmaceutical Industries, Ltd.

  公开号：US05006520A1

  公开（公告）日：1991-04-09

  Novel fused pyrazole compounds of the general formula ##STR1## wherein all the symbols are as defined in the specification or its pharmaceutically acceptable salt which possesses a stimulating action on phagocytosis of leukocytes, a stimulating action on phagocytosis of macrophages, a restorative action on leukopenia, a stimulating action on non-specific resistance to infection, an antitumour action, an activating action on immune responses and the like, and thereof is of use as a pharmaceutical.

  一种新型融合吡唑化合物，其一般式为##STR1##其中所有符号均如规范中所定义或其药学上可接受的盐，具有刺激白细胞吞噬作用、刺激巨噬细胞吞噬作用、恢复白细胞减少症、刺激非特异性抗感染能力、抗肿瘤作用、激活免疫反应等作用，因此可用于药物。