1-(6-bromo-2-methoxy-quinolin-3-yl)-4-dimethylamino-2-naphthalen-1-yl-1-p-tolyl-butan-2-ol

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: 1-(6-bromo-2-methoxy-quinolin-3-yl)-4-dimethylamino-2-naphthalen-1-yl-1-p-tolyl-butan-2-ol
• 英文别名: 1-(6-Bromo-2-methoxy-3-quinolyl)-4-(dimethylamino)-2-(1-naphthyl)-1-(p-tolyl)butan-2-ol；1-(6-bromo-2-methoxyquinolin-3-yl)-4-(dimethylamino)-1-(4-methylphenyl)-2-naphthalen-1-ylbutan-2-ol
• 化学式: C₃₃H₃₃BrN₂O₂
• 分子量: 569.541
• InChiKey: CFPPFXNAPDMERR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.6
• 重原子数：
  38
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  45.6
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] QUINOLINE DERIVATIVES AND THEIR USE AS MYCOBACTERIAL INHIBITORS<br/>[FR] DERIVES DE QUINOLEINE ET LEUR UTILISATION EN TANT QU'INHIBITEURS MYCOBACTERIENS
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2004011436A1

  公开（公告）日：2004-02-05

  The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or the general Formula (Ib), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of mycobacterial diseases, particularly those diseases caused by pathogenic mycobacteria such as Mycobacterium tuberculosis, M. bovis, M. avium and M. marinum. In particular, compounds are claimed in which, independently from each other, R1 is bromo, p=1, R2 is alkyloxy, R3 is optionally substituted naphthyl or phenyl, q=1, R4 and R5 each independently are hydrogen, methyl or ethyl, R6 is hydrogen, r is equal to 0 or 1 and R7 is hydrogen. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of mycobacterial diseases and a process for preparing the claimed compounds.

  本发明涉及根据通式(Ia)或通式(Ib)的新型取代喹啉衍生物，其药学上可接受的酸盐或碱盐，其立体化学异构体形式，其互变异构体形式和其N-氧化物形式。所述化合物对治疗结核分枝杆菌病等由病原性分枝杆菌引起的疾病有用，特别是对治疗结核分枝杆菌、博维氏分枝杆菌、埃维分枝杆菌和海洋分枝杆菌等疾病有用。特别地，所述化合物中，独立于彼此，R1为溴，p=1，R2为烷氧基，R3为可选择取代的萘基或苯基，q=1，R4和R5各自独立为氢、甲基或乙基，R6为氢，r等于0或1，R7为氢。还声明了一种包含药学上可接受载体和作为活性成分的所述化合物的治疗有效量的组合物，所述化合物或组合物用于制备治疗结核分枝杆菌病的药物以及制备所述化合物的方法。
• [EN] USE OF SUBSTITUTED QUINOLINE DERIVATIVES FOR THE TREATMENT OF DRUG RESISTANT MYCOBACTERIAL DISEASES<br/>[FR] UTILISATION DE DERIVES QUINOLINE SUBSTITUES DESTINES AUX TRAITEMENTS DE MALADIES MYCOBACTERIENNES RESISTANT AUX MEDICAMENTS
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2005117875A1

  公开（公告）日：2005-12-15

  The present invention relates to the use of a substituted quinoline derivative for the preparation of a medicament for the treatment of an infection with a drug resistant Mycobacterium strain wherein the substituted quinoline derivative is a compound according to Formula (Ia) or Formula (Ib) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the above compounds and one or more other antimycobacterial agents.

  本发明涉及使用一种取代喹啉衍生物制备治疗对药物耐药分枝杆菌菌株感染的药物，其中所述取代喹啉衍生物是符合式(Ia)或式(Ib)的化合物，其药学上可接受的酸或碱盐，其立体化学异构体形式，其互变异构体形式和其N-氧化物形式。还声明了一种包含药学上可接受的载体和作为活性成分的上述化合物的治疗有效量以及一种或多种其他抗分枝杆菌药物的组合物。
• Novel mycobacterial inhibitors
  申请人：Van Gestel Frans Elisabetha Jozef

  公开号：US20050148581A1

  公开（公告）日：2005-07-07

  The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or the general Formula (Ib) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of mycobacterial diseases, particularly those diseases caused by pathogenic mycobacteria such as Mycobacterium tuberculosis, M. bovis, M. avium and M. marinum . In particular, compounds are claimed in which, independently from each other, R 1 is bromo, p=1, R 2 is alkyloxy, R 3 is optionally substituted naphthyl or phenyl, q=1, R 4 and R 5 each independently are hydrogen, methyl or ethyl, R 6 is hydrogen, r is equal to 0 or 1 and R 7 is hydrogen. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of mycobacterial diseases and a process for preparing the claimed compounds.

  本发明涉及符合通式（Ia）或通式（Ib）的新型取代喹啉衍生物 其药学上可接受的酸或碱加成盐、其立体化学异构体形式、其同分异构体形式和其 N-氧化物形式。所要求的化合物可用于治疗分枝杆菌疾病，特别是由致病分枝杆菌引起的疾病，如 结核分枝杆菌、牛分枝杆菌、禽分枝杆菌 和 M. marinum .具体而言，本发明要求的化合物中，R 1 是溴，p=1，R 2 是烷氧基，R 3 是任选取代的萘基或苯基，q=1，R 4 和 R 5 各自独立地为氢、甲基或乙基，R 6 是氢，r 等于 0 或 1，R 7 是氢。本发明还要求一种组合物，该组合物包含药学上可接受的载体和作为活性成分的治疗有效量的所称化合物，使用所称化合物或组合物制造治疗霉菌病的药物，以及制备所称化合物的工艺。
• QUINOLINE DERIVATIVES AND THEIR USE AS MYCOBACTERIAL INHIBITORS
  申请人：Janssen Pharmaceutica NV

  公开号：EP1527050B1

  公开（公告）日：2010-04-07
• USE OF SUBSTITUTED QUINOLINE DERIVATIVES FOR THE TREATMENT OF DRUG RESISTANT MYCOBACTERIAL DISEASES
  申请人：Janssen Pharmaceutica NV

  公开号：EP1753427B1

  公开（公告）日：2008-04-02