N-(8-((R)-2-hydroxy-2-(4-methyl-1-oxo-1,3-dihydroisobenzofuran-5-yl)ethyl)-8-azabicyclo[3.2.1]octan-3-yl)-5-(1H-tetrazol-1-yl)picolinamide | 1612760-08-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异香豆素
• 英文名称: N-(8-((R)-2-hydroxy-2-(4-methyl-1-oxo-1,3-dihydroisobenzofuran-5-yl)ethyl)-8-azabicyclo[3.2.1]octan-3-yl)-5-(1H-tetrazol-1-yl)picolinamide
• 英文别名: N-[8-[(2R)-2-hydroxy-2-(4-methyl-1-oxo-3H-2-benzofuran-5-yl)ethyl]-8-azabicyclo[3.2.1]octan-3-yl]-5-(tetrazol-1-yl)pyridine-2-carboxamide
• CAS: 1612760-08-3
• 化学式: C₂₅H₂₇N₇O₄
• 分子量: 489.534
• InChiKey: LFXXPUPBDLBVET-WHZSGRLBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  36
• 可旋转键数：
  6
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  135
• 氢给体数：
  2
• 氢受体数：
  9

文献信息

• [EN] INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL<br/>[FR] INHIBITEURS DU CANAL POTASSIQUE MÉDULLAIRE EXTÉRIEUR RÉNAL
  申请人：MERCK SHARP & DOHME

  公开号：WO2014085210A1

  公开（公告）日：2014-06-05

  The present invention provides compounds of Formula (I), and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.

  本发明提供了式（I）的化合物及其药用可接受的盐，这些化合物是ROMK（Kir1.1）通道的抑制剂。这些化合物可用作利尿剂和/或钠利尿剂，并用于治疗和预防包括高血压、心力衰竭以及与过多盐分和水分潴留有关的疾病等医疗条件。
• CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTICS DELIVERY
  申请人：CERULEAN PHARMA INC.

  公开号：US20130156721A1

  公开（公告）日：2013-06-20

  The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.

  本发明涉及一种新型治疗环糊精含聚合物的组合物，设计为小分子治疗药物输送的载体以及其制药组合物。这些含环糊精的聚合物能够提高药物稳定性和溶解度，并在体内使用时减少小分子治疗药物的毒性。此外，通过从多种连接剂和靶向配体中选择聚合物，可以提供治疗剂的控制释放方法。本发明还涉及使用上述治疗组合物治疗受试者的方法。本发明还涉及制药业务的方法，包括制造、许可或分发包含或与上述聚合物相关的工具包。
• Inhibitors of the Renal Outer Medullary Potassium Channel
  申请人：WALSH Shawn P.

  公开号：US20150299198A1

  公开（公告）日：2015-10-22

  The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.

  本发明提供了I式化合物及其药学上可接受的盐，它们是ROMK（Kir1.1）通道的抑制剂。该化合物可用作利尿剂和/或钠利尿剂，以及用于治疗和预防包括高血压、心力衰竭和与过多盐和水潴留有关的医疗状况的药物。
• INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP2925322B1

  公开（公告）日：2018-10-24
• US9777002B2
  申请人：——

  公开号：US9777002B2

  公开（公告）日：2017-10-03