N-benzyl-8-hydroxy-1,6-naphthyridine-7-carboxamide | 410542-93-7

• 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: N-benzyl-8-hydroxy-1,6-naphthyridine-7-carboxamide
• CAS: 410542-93-7
• 化学式: C₁₆H₁₃N₃O₂
• 分子量: 279.298
• InChiKey: JJCRDRIRTLRLLP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  75.1
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors
  申请人：——

  公开号：US20030055071A1

  公开（公告）日：2003-03-20

  Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

  描述了包括某些喹啉羧酰胺和萘啉羧酰胺衍生物在内的氮杂萘基羧酰胺衍生物。这些化合物是HIV整合酶的抑制剂和HIV复制的抑制剂，可用于预防或治疗HIV感染和治疗艾滋病，作为化合物或药学上可接受的盐，或作为药物组合物中的成分，可选择与其他抗病毒药物、免疫调节剂、抗生素或疫苗组合使用。还描述了预防、治疗或延缓艾滋病发作的方法，以及预防或治疗HIV感染的方法。
• Pharmaceutical compositions containing an hiv integrase inhibitor and a nonionic surfactant
  申请人：Robertson K. Sandra

  公开号：US20050165000A1

  公开（公告）日：2005-07-28

  Pharmaceutical compositions comprise a therapeutically effective amount of an 8-hydroxy-1,6-naphthyridine-7-carboxamide of Formula (I), or a pharmaceutically acceptable salt thereof: and a nonionic surfactant; wherein R 1 , R 2 , R 3 and Q 1 are defined herein. Compounds of Formula (I) are HIV integrase inhibitors, and the pharmaceutical compositions are useful for preventing or treating HIV infection or for preventing, treating, or delaying the onset of AIDS. The pharmaceutical compositions are typically administered orally, for example, in the form of capsules or tablets, and can provide good oral bioavailability. Methods for preparing encapsulated and tabletted forms of the pharmaceutical compositions are described.

  药物组成物包括以下成分：治疗有效量的式（I）的8-羟基-1,6-萘啶并[2,3-d]嘧啶-7-羧酰胺或其药学上可接受的盐；以及一种非离子表面活性剂。其中，R1、R2、R3和Q1的定义如本文所述。式（I）的化合物是HIV整合酶抑制剂，药物组成物可用于预防或治疗HIV感染，或用于预防、治疗或延缓艾滋病的发作。这些药物组成物通常口服给药，例如以胶囊或片剂的形式，并且可以提供良好的口服生物利用度。还描述了制备药物组成物的胶囊和片剂形式的方法。
• AZA- AND POLYAZA-NAPHTHALENYL CARBOXAMIDES USEFUL AS HIV INTEGRASE INHIBITORS
  申请人：Merck & Co., Inc.

  公开号：EP1326865A2

  公开（公告）日：2003-07-16
• PHARMACEUTICAL COMPOSITIONS CONTAINING AN HIV INTEGRASE INHIBITOR AND A NONIONIC SURFACTANT
  申请人：Merck & Co., Inc.

  公开号：EP1499391A2

  公开（公告）日：2005-01-26
• US6921759B2
  申请人：——

  公开号：US6921759B2

  公开（公告）日：2005-07-26