4-(9-Ethoxy-8-methoxy-2-methyl-1,2,3,4,4a,10b-hexahydrobenzo[c][1,6]naphthyridin-6-yl)-N,N-di(propan-2-yl)benzamide

• 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: 4-(9-Ethoxy-8-methoxy-2-methyl-1,2,3,4,4a,10b-hexahydrobenzo[c][1,6]naphthyridin-6-yl)-N,N-di(propan-2-yl)benzamide
• 英文别名: 4-(9-ethoxy-8-methoxy-2-methyl-3,4,4a,10b-tetrahydro-1H-benzo[c][1,6]naphthyridin-6-yl)-N,N-di(propan-2-yl)benzamide
• 化学式: C₂₉H₃₉N₃O₃
• 分子量: 477.6
• InChiKey: CVDXFPBVOIERBH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  35
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  54.4
• 氢给体数：
  0
• 氢受体数：
  5

文献信息

• [EN] QUINUCLIDINE DERIVATIVES AND THEIR USE AS MUSCARINIC RECEPTOR ANTAGONISTS FOR THE TREATMENT OF ASTHMA AND CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)<br/>[FR] DÉRIVÉS DE QUINUCLIDINE ET LEUR UTILISATION COMME ANTAGONISTES DES RÉCEPTEURS MUSCARINIQUES POUR LE TRAITEMENT DE L'ASTHME ET DE LA BRONCHOPNEUMOPATHIE CHRONIQUE OBSTRUCTIVE (BPCO)
  申请人：ASTRAZENECA AB

  公开号：WO2009139709A1

  公开（公告）日：2009-11-19

  The invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, Het1, n, Y and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions, their use in therapy and intermediates of use in their preparation.

  本发明提供式(I)化合物，其中R1、R2、R3、R4、R5、Het1、n、Y和X如说明书中所定义，制备这些化合物的方法，含有这些化合物的药物组合物，制备药物组合物的方法，它们在治疗中的用途，以及用于制备它们的中间体。
• [EN] QUINUCLIDINE DERIVATIVES AND THEIR USE AS MUSCARINIC RECEPTOR ANTAGONISTS<br/>[FR] DÉRIVÉS DE QUINUCLIDINE ET LEUR UTILISATION COMME ANTAGONISTES DES RÉCEPTEURS MUSCARINIQUES
  申请人：ASTRAZENECA AB

  公开号：WO2009139710A1

  公开（公告）日：2009-11-19

  The invention provides compounds of formula (I) wherein R1, R2, R3, Het1, n, Y and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions, their use in therapy and intermediates of use in their preparation

  本发明提供了公式(I)的化合物，其中R1、R2、R3、Het1、n、Y和X如说明书中所定义，一种制备它们的方法，包含它们的药物组合物，制备药物组合物的过程，它们在治疗中的用途以及用于它们制备的中间体。
• [EN] ANTI-INFLAMMATORY GLUCOCORTICOIDS<br/>[FR] GLUCOCORTICOÏDES ANTI-INFLAMMATOIRES
  申请人：GLAXO GROUP LTD

  公开号：WO2005028495A1

  公开（公告）日：2005-03-31

  A compound of formula (I) wherein R1 and R2 are the same or different and each represents hydrogen, halogen or a methyl group; R3 represents H, Cl, F, OH OR OC(O)R6; R4 represents hydrogen or methyl, R5 represents -(CH2)n-CH=CH)m-Cycl or -(CH2)n-(CH=CH)m-Ar or cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; n represents 0, 1 or 2; m represents 0 or 1; R6 represents H, C1-8alkyl; and formula (b) represents a single or a double bond; including pharmaceutically acceptable esters, amides and carbamates thereof, salts thereof, solvates thereof, and solvates of such pharmaceutically acceptable esters, amides, carbamates and salts.

  一种具有式（I）的化合物，其中R1和R2相同或不同，每个代表氢、卤素或甲基；R3代表H、Cl、F、OH或OC（O）R6；R4代表氢或甲基，R5代表-(CH2)n-CH=CH)m-Cycl或-(CH2)n-(CH=CH)m-Ar或环丙基、环丁基、环戊基、环己基、环庚基或环辛基；n代表0、1或2；m代表0或1；R6代表H、C1-8烷基；和式（b）代表单键或双键；包括其药学上可接受的酯、酰胺和氨基甲酸酯，其盐，其溶剂合物，以及这种药学上可接受的酯、酰胺、氨基甲酸酯和盐的溶剂合物。
• QUINUCLIDINE DERIVATIVES AS MUSCARINIC M3 RECEPTOR ANTAGONISTS
  申请人：Bull Richard James

  公开号：US20110172237A1

  公开（公告）日：2011-07-14

  The invention provides named compounds of formula (I), wherein R4 is a N-substituted quinuclidine (I) pharmaceutical compositions containing them and a process for preparing the pharmaceutical compositions. Their use in therapy for’ the treatment of conditions mediated by M3 muscarinic receptors, such as chronic obstructive pulmonary disease is also disclosed.

  这项发明提供了式(I)的命名化合物，其中R4是N-取代的喹啉啶(I)药物组合物以及制备药物组合物的方法。还披露了它们在治疗由M3胆碱能受体介导的疾病，如慢性阻塞性肺病中的用途。
• [EN] 2,3-BENZOXAZIN DERIVATIVES AS NON-STEROIDAL GLUCOCORTICOID RECEPTOR MODULATORS<br/>[FR] DERIVES DE 2,3-BENZOXAZINE UTILISES EN TANT QUE MODULATEURS NON STEROIDIENS DU RECEPTEUR GLUCOCORTICOIDE
  申请人：GLAXO GROUP LTD

  公开号：WO2006000398A1

  公开（公告）日：2006-01-05

  The present invention provides compounds of formula (I), wherein R1 represents 1-ethylpropyl, 1-methylethyl or 2-methylpropyl; or a physiologically functional derivative thereof; pharmaceutical compositions comprising the compounds, the use of the compounds for the manufacture of medicaments particularly for the treatment of inflammatory and/or allergic conditions, processes for the preparation of the compounds, and chemical intermediates in the processes for the manufacture of the compounds.

  本发明提供了式(I)的化合物，其中R1代表1-乙基丙基、1-甲基乙基或2-甲基丙基；或其生理功能衍生物；包括这些化合物的药物组合物，这些化合物用于制造药物，特别用于治疗炎症和/或过敏症状，以及用于制备这些化合物的过程和制造这些化合物的化学中间体。