(R)-5-cyano-N-(1-(2-hydroxy-2-(4-methyl-1-oxo-1,3-dihydroisobenzofuran-5-yl)ethyl)piperidin-4-yl)-4-methylpicolinamide | 1612247-84-3

• 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: (R)-5-cyano-N-(1-(2-hydroxy-2-(4-methyl-1-oxo-1,3-dihydroisobenzofuran-5-yl)ethyl)piperidin-4-yl)-4-methylpicolinamide
• 英文别名: 5-cyano-N-[1-[(2R)-2-hydroxy-2-(4-methyl-1-oxo-3H-2-benzofuran-5-yl)ethyl]piperidin-4-yl]-4-methylpyridine-2-carboxamide
• CAS: 1612247-84-3
• 化学式: C₂₄H₂₆N₄O₄
• 分子量: 434.495
• InChiKey: UKDYURZFDKBMSD-QFIPXVFZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  32
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  116
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  5-cyano-4-methyl-N-(piperidin-4-yl)picolinamide hydrochloride 、 (R)-4-甲基-5-(环氧乙烷-2-基)异苯并呋喃-1(3H)-酮 生成 (R)-5-cyano-N-(1-(2-hydroxy-2-(4-methyl-1-oxo-1,3-dihydroisobenzofuran-5-yl)ethyl)piperidin-4-yl)-4-methylpicolinamide
  参考文献：
  名称：

  Inhibitors of the Renal Outer Medullary Potassium Channel

  摘要：

  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。

  公开号：

  US20150299198A1

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。
• PYRIDINECARBOXAMIDE DERIVATIVES, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USES THEREOF
  申请人：Jiangsu Hengrui Medicine Co., Ltd.

  公开号：EP3231802A1

  公开（公告）日：2017-10-18

  The present invention relates to pyridinecarboxamide derivatives, a preparation method thereof and a pharmaceutical use thereof. Specifically, the present invention relates to pyridinecarboxamide derivatives represented by general formula (I), wherein the substituents of the formula (I) are defined as the same as in the specification, a preparation method therefor, a pharmaceutical composition comprising the derivaties, and the uses as therapeutic agents, especially as inhibitors of the Renal Outer Medullary Potassium channel (ROMK) and in the preparation of medicaments for treating and/or preventing hypertension and heart failure.

  本发明涉及吡啶甲酰胺衍生物、其制备方法及其药物用途。具体地说，本发明涉及由通式（I）代表的吡啶甲酰胺衍生物（其中式（I）的取代基定义与说明书中相同）、其制备方法、包含该衍生物的药物组合物，以及其作为治疗剂的用途，特别是作为肾外髓钾通道（ROMK）的抑制剂和在制备治疗和/或预防高血压和心力衰竭的药物中的用途。
• Pyridinecarboxamide derivatives, preparation method thereof and pharmaceutical uses thereof
  申请人：Jiangsu Hengrui Medicine Co., Ltd.

  公开号：US10364234B2

  公开（公告）日：2019-07-30

  Pyridinecarboxamide derivatives, preparation methods, and a pharmaceutical uses thereof are provided. In particular, pyridinecarboxamide derivatives represented by general formula (I), wherein the substituents of the formula (I) are defined in the specification are provided. Also provided are a preparation method for the pyridinecarboxamide derivatives of formula (I), a pharmaceutical composition containing the pyridinecarboxamide derivatives, and uses of the pyridinecarboxamide derivatives as therapeutic agents, especially as inhibitors of the Renal Outer Medullary Potassium channel (ROMK) and in the preparation of medicaments for treating and/or preventing hypertension and heart failure.

  本发明提供了吡啶甲酰胺衍生物、制备方法及其制药用途。特别是提供了由通式（I）代表的吡啶甲酰胺衍生物，其中式（I）的取代基在说明书中定义。还提供了式(I)吡啶甲酰胺衍生物的制备方法、含有该吡啶甲酰胺衍生物的药物组合物，以及该吡啶甲酰胺衍生物作为治疗剂的用途，特别是作为肾外髓钾通道(ROMK)的抑制剂和在制备治疗和/或预防高血压和心力衰竭的药物中的用途。
• Processes for preparing pyridine carboxamide derivatives
  申请人：Jiangsu Hengrui Medicine Co., Ltd.

  公开号：US10442794B2

  公开（公告）日：2019-10-15

  Processes for preparing pyridinecarboxamide derivatives are provided. In particular, process for preparing pyridinecarboxamide derivatives represented by general formula (I) are provided, wherein the substituents of the formula (I) are defined in the specification.

  本发明提供了制备吡啶甲酰胺衍生物的工艺。特别是提供了以通式（I）为代表的吡啶甲酰胺衍生物的制备工艺，其中式（I）的取代基在说明书中定义。
• INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP2925322A1

  公开（公告）日：2015-10-07