(1-isobutyl-1H-imidazo[4,5-c]quinolin-4-yl)-carbamic acid ethyl ester | 847453-15-0

• 英文名称: (1-isobutyl-1H-imidazo[4,5-c]quinolin-4-yl)-carbamic acid ethyl ester
• 英文别名: ethyl N-[1-(2-methylpropyl)imidazo[4,5-c]quinolin-4-yl]carbamate
• CAS: 847453-15-0
• 化学式: C₁₇H₂₀N₄O₂
• 分子量: 312.371
• InChiKey: BLBCKNPLCZACOW-UHFFFAOYSA-N

物化性质

• 密度：
  1.26±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  23
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  69
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Administration of TLR7 ligands and prodrugs thereof for treatment of infection by hepatitis C virus
  申请人：Averett R. Devron

  公开号：US20050054590A1

  公开（公告）日：2005-03-10

  This invention relates to methods for treating or preventing hepatitis C virus infections in mammals using Toll-Like Receptor (TLR)7 ligands and prodrugs thereof. More particularly, this invention relates to methods of orally administering a therapeutically effective amount of one or more prodrugs of TLR7 ligands for the treatment or prevention of hepatitis C viral infection. Oral administration of these TLR7 immunomodulating ligands and prodrugs thereof to a mammal provides therapeutically effective amounts and reduced undesirable side effects.

  这项发明涉及使用Toll样受体（TLR）7配体及其前药治疗或预防哺乳动物体内的丙型肝炎病毒感染的方法。更具体地，这项发明涉及口服给予一种或多种TLR7配体前药的治疗有效量，用于治疗或预防丙型肝炎病毒感染。将这些TLR7免疫调节配体及其前药口服给哺乳动物可提供治疗有效量并减少不良副作用。
• [EN] NOVEL N- (ALKOXYALKYL) CARBAMOYL - SUBSTITUTED 6-PHENYL-BENZONAPHTHYRIDINE DERIVATIVES AND THEIR USE AS PDE3/4 INHIBITORS<br/>[FR] NOUVEAUX DERIVES DE 6-PHENYL-BENZONAPHTYRIDINES A SUBSTITUTION N-(ALCOXYALKYL) CARBAMOYLE ET LEUR UTILISATION COMME INHIBITEURS DE PDE3/4
  申请人：ALTANA PHARMA AG

  公开号：WO2005090345A1

  公开（公告）日：2005-09-29

  Compounds of formula (1), in which R1 is 1-4C-alkyl, R2 is hydroxyl, 1-4C-alkoxy. 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, R3 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, or in which R2 and R3 together are a 1-2C-alkylenedioxy group, R4 is hydrogen, halogen, nitro, 1-4C-alkyl, trifluoromethyl or 1-4C-alkoxy, R5 is hydrogen, 1-8C-alkyl, 3-7C-cycloalkyl or phenyl-1-4C-alkyl, R6 is 1-4C-alkyl, phenyl-1-4C-alkyl, or Aryl-1-4C-alkyl, in which Aryl is R61 - and/or R62-substituted phenyl, in which R61 is 1-4C-alkoxy, trifluoromethyl or cyano, R62 is 1-4C-alkoxy, and in which either R7 is 1-4C-alkyl, and n is 1 or 2, or R7 is hydrogen, and n is 1, 2 or 3, the salts, the N-oxides of these compounds and the salts of the latter are novel effective PDE3/4 inhibitors.

  化学式为（1）的化合物，其中R1是1-4C-烷基，R2是羟基，1-4C-氧烷基，3-7C-环氧基，3-7C-环烷基甲氧基，或者完全或主要被氟取代的1-4C-氧烷基，R3是羟基，1-4C-氧烷基，3-7C-环氧基，3-7C-环烷基甲氧基，或者完全或主要被氟取代的1-4C-氧烷基，或者R2和R3一起是1-2C-烷基二氧基基团，R4是氢，卤素，硝基，1-4C-烷基，三氟甲基或1-4C-氧烷基，R5是氢，1-8C-烷基，3-7C-环烷基或苯基-1-4C-烷基，R6是1-4C-烷基，苯基-1-4C-烷基或芳基-1-4C-烷基，其中芳基是R61-和/或R62-取代的苯基，其中R61是1-4C-氧烷基，三氟甲基或氰基，R62是1-4C-氧烷基，并且R7是1-4C-烷基，n为1或2，或者R7是氢，n为1,2或3，这些化合物的盐，N-氧化物以及后者的盐是新颖的有效PDE3/4抑制剂。
• ADMINISTRATION OF TLR7 LIGANDS AND PRODRUGS THEREOF FOR TREATMENT OF INFECTION BY HEPATITIS C VIRUS
  申请人：Averett Devron R.

  公开号：US20090298863A1

  公开（公告）日：2009-12-03

  This invention relates to methods for treating or preventing hepatitis C virus infections in mammals using Toll-Like Receptor (TLR)7 ligands and prodrugs thereof. More particularly, this invention relates to methods of orally administering a therapeutically effective amount of one or more prodrugs of TLR7 ligands for the treatment or prevention of hepatitis C viral infection. Oral administration of these TLR7 immunomodulating ligands and prodrugs thereof to a mammal provides therapeutically effective amounts and reduced undesirable side effects.

  本发明涉及使用Toll样受体(TLR)7配体及其前药治疗或预防哺乳动物的丙型肝炎病毒感染的方法。更具体地说，本发明涉及口服治疗丙型肝炎病毒感染的一种或多种TLR7配体前药的治疗剂量的方法。将这些TLR7免疫调节配体及其前药口服给哺乳动物，可提供治疗有效量和减少不良副作用。
• TLR7 LIGANDS FOR THE TREATMENT OF HEPATITIS C
  申请人：Anadys Pharmaceuticals, Inc.

  公开号：EP1667694B1

  公开（公告）日：2010-04-28
• NOVEL N-(ALKOXYALKYL)CARBAMOYL- SUBSTITUTED 6-PHENYL-BENZONAPHTHYRIDINE DERIVATIVES AND THEIR USE AS PDE3/4 INHIBITORS
  申请人：Altana Pharma AG

  公开号：EP1732925A1

  公开（公告）日：2006-12-20