N-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]-7-oxo-4H-thieno[3,2-b]pyridine-6-carboxamide;hydron;chloride

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩并吡啶类
• 英文名称: N-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]-7-oxo-4H-thieno[3,2-b]pyridine-6-carboxamide;hydron;chloride
• 化学式: C15H18ClN3O2S
• 分子量: 339.8
• InChiKey: XGVADZZDFADEOO-YDALLXLXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.84
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  89.7
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• [EN] CONJUGATES OF HETEROAROMATIC NITROGEN-COMPRISING COMPOUNDS<br/>[FR] CONJUGUÉS DE COMPOSÉS HÉTÉROAROMATIQUES CONTENANT DE L'AZOTE
  申请人：ASCENDIS PHARMA AS

  公开号：WO2020254606A1

  公开（公告）日：2020-12-24

  The present invention relates to conjugates of ΤΓ-electron-pair-donating heteroaromatic nitrogen-comprising drugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said conjugates and the use of said conjugates as medicaments.

  本发明涉及ΤΓ-电子对供体杂芳氮含药物及其药用盐的结合物，包括所述结合物的药物组合物以及将所述结合物用作药物的用途。
• PREVENTIVE OR THERAPEUTIC AGENTS FOR GASTRIC OR ESOPHAGEAL REGURGITATION
  申请人：Mitsubishi Pharma Corporation

  公开号：EP1256581A1

  公开（公告）日：2002-11-13

  The compound of the following formula: wherein R1 and R2 independently represent a hydrogen atom or a lower alkyl group; A represents a group selected from the group consisting of 1-azabicyclo[3.2.2]nonyl group, 1-azabicyclo[2.2.2]octyl group, or an N-oxide thereof, or a pharmaceutically acceptable salt thereof or a hydrate thereof has both improving effect on enterokinetic functions and suppressing effect on acid secretion, and also is highly safe. Accordingly, the substance is useful as preventive or therapeutic medicament for a gastroesophageal reflux disease.

  下式的化合物： 其中 R1 和 R2 分别代表氢原子或低级烷基；A 代表选自 1-氮杂双环[3.2.2]壬基、1-氮杂双环[2.2.2]辛基或其 N-氧化物组成的组，或其药学上可接受的盐或其水合物，具有改善肠动力功能和抑制胃酸分泌的作用，而且安全性高。因此，该物质可用作胃食管反流病的预防或治疗药物。
• Preventive or therapeutic agents for gastric or esophageal regurgitation
  申请人：——

  公开号：US20030130304A1

  公开（公告）日：2003-07-10

  The compound of the following formula: 1 wherein R 1 and R 2 independently represent a hydrogen atom or a lower alkyl group; A represents a group selected from the group consisting of 1-azabicyclo[3.2.2]nonyl group, 1-azabicyclo[2.2.2]octyl group, or an N-oxide thereof, or a pharmaceutically acceptable salt thereof or a hydrate thereof has both improving effect on enterokinetic functions and suppressing effect on acid secretion, and also is highly safe. Accordingly, the substance is useful as preventive or therapeutic medicament for a gastroesophageal reflux disease.

  下式化合物 1 其中 R 1 和 R 2 A 代表选自 1-氮杂双环[3.2.2]壬基、1-氮杂双环[2.2.2]辛基、或其 N-氧化物、或其药学上可接受的盐或其水合物组成的组。因此，该物质可用作胃食管反流病的预防或治疗药物。
• Preventive agent/remedial agent for constipation predominant ibs
  申请人：——

  公开号：US20040248927A1

  公开（公告）日：2004-12-09

  A novel preventive and/or therapeutic medicament for a constipation predominant IBS which contains as the active ingredient a thieno[3,2-b]pyridinecarboxamide derivative represented by the formula (I): 1 wherein R 1 and R 2 each independently represents hydrogen atom or a lower alkyl group and A represents a substituent selected from the group consisting of 1-azabicyclo[3.2.2]nonyl group 1-azabicyclo[2.2.2]octyl group, and the N.oxides thereof, a pharmaceutically acceptable salt thereof, or a solvate or hydrate thereof

  一种新型的预防和/或治疗以便秘为主的肠易激综合征的药物，其活性成分是由式 (I) 所代表的噻吩[3,2-b]吡啶甲酰胺衍生物： 1 其中 R 1 和 R 2 各自独立地代表氢原子或低级烷基，且 A 代表选自以下组别的取代基：1-氮杂双环[3.2.2]壬基 1-氮杂双环[2.2.2]辛基，及其 N.氧化物，其药学上可接受的盐，或其溶液或水合物
• Compositions useful for treating gastrointestinal motility disorders
  申请人：Landau B. Steven

  公开号：US20050059704A1

  公开（公告）日：2005-03-17

  The present invention relates to method of treating a gastrointestinal motility disorder in a subject in need of treatment comprising coadministering to said subject a first amount of a compound having 5-HT 3 receptor agonist activity or a pharmaceutically acceptable salt, hydrate or solvate thereof; and a second amount of at least one gastric acid suppressing agent (e.g., a proton pump inhibitor, an H 2 receptor antagonist or a pharmaceutically acceptable salt, hydrate or solvate thereof; or an acid pump antagonist or pharmaceutically acceptable salt, hydrate or solvate thereof) wherein the first and second amounts together comprise a therapeutically effective amount. In particular, the method is for treating GERD, including nocturnal GERD. The invention further relates to a method of treating nocturnal GERD comprising administering to a subject in need thereof a therapeutically effective amount of a compound having 5-HT 3 receptor agonist activity or a pharmaceutically acceptable salt, hydrate or solvate thereof. The invention further relates to a method of increasing esophageal motility in a subject in need thereof. The method of increasing esophageal motility can be achieved by administration of a compound having 5-HT 3 receptor agonist activity or a pharmaceutically acceptable salt, hydrate or solvate thereof. The coadministration can also be used to increase esophageal motility.

  本发明涉及治疗需要治疗的受试者胃肠道运动紊乱的方法，包括向所述受试者联合施用第一种量的具有 5-HT 3 受体激动剂活性的化合物或其药学上可接受的盐、水合物或溶液；以及第二种量的至少一种胃酸抑制剂（如质子泵抑制剂、H 2 受体拮抗剂或其药学上可接受的盐、水合物或溶液；或酸泵拮抗剂或其药学上可接受的盐、水合物或溶液），其中第一和第二量共同构成治疗有效量。特别是，该方法用于治疗胃食管反流病，包括夜间胃食管反流病。本发明进一步涉及一种治疗夜间胃食管反流病的方法，该方法包括向有需要的受试者施用治疗有效量的具有 5-HT 3 受体激动剂活性的化合物或其药学上可接受的盐、水合物或溶液。本发明进一步涉及一种增加需要者食管蠕动的方法。增加食管蠕动的方法可通过给予具有 5-HT 3 受体激动剂活性的化合物或其药学上可接受的盐、水合物或溶液。联合给药也可用于增加食管运动。