4-[[4-Methyl-1,7-bis(methylamino)-1,7-dioxoheptan-4-yl]amino]-4-oxobutanoic acid

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 4-[[4-Methyl-1,7-bis(methylamino)-1,7-dioxoheptan-4-yl]amino]-4-oxobutanoic acid
• 英文别名: 4-[[4-methyl-1,7-bis(methylamino)-1,7-dioxoheptan-4-yl]amino]-4-oxobutanoic acid
• 化学式: C₁₄H₂₅N₃O₅
• 分子量: 315.37
• InChiKey: LBXRQJFBMGWHAY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.6
• 重原子数：
  22
• 可旋转键数：
  10
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  125
• 氢给体数：
  4
• 氢受体数：
  5

文献信息

• [EN] COMPOUNDS AND METHODS FOR INHIBITING NHE-MEDIATED ANTIPORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH FLUID RETENTION OR SALT OVERLOAD AND GASTROINTESTINAL TRACT DISORDERS<br/>[FR] COMPOSÉS ET PROCÉDÉS D'INHIBITION D'UN ANTIPORT À MÉDIATION PAR NHE DANS LE TRAITEMENT DE TROUBLES ASSOCIÉS À UNE RÉTENTION DE FLUIDE OU À UNE SURCHARGE DE SEL ET DE TROUBLES DU TRACTUS GASTRO-INTESTINAL
  申请人：ARDELYX INC

  公开号：WO2014029983A1

  公开（公告）日：2014-02-27

  The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.

  本公开涉及化合物和治疗液体潴留或盐过多相关疾病的方法，例如心力衰竭（特别是充血性心力衰竭）、慢性肾脏疾病、晚期肾脏疾病、肝脏疾病和过氧化物酶体增殖物激活受体（PPAR）γ激动剂诱导的液体潴留。本公开还涉及化合物和治疗高血压的方法。本公开还涉及化合物和治疗胃肠道疾病的方法，包括治疗或减轻与胃肠道疾病相关的疼痛。
• COMPOUNDS AND METHODS FOR INHIBITING NHE-MEDIATED ANTIPORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH FLUID RETENTION OR SALT OVERLOAD AND GASTROINTESTINAL TRACT DISORDERS
  申请人：ARDELYX, INC.

  公开号：US20150336892A1

  公开（公告）日：2015-11-26

  The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.

  本公开涉及化合物和方法，用于治疗与液体潴留或盐过量相关的疾病，例如心力衰竭（特别是充血性心力衰竭）、慢性肾脏疾病、晚期肾脏疾病、肝病和过氧化物酶体增殖物激活受体（PPAR）γ激动剂引起的液体潴留。本公开还涉及化合物和方法，用于治疗高血压。本公开还涉及化合物和方法，用于治疗胃肠道疾病，包括治疗或减轻与胃肠道疾病相关的疼痛。
• NHE3-BINDING COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT
  申请人：ARDELYX, INC

  公开号：US20160067242A1

  公开（公告）日：2016-03-10

  Provided are NHE3-binding and/or NHE3-modulating agents having activity as phosphate transport inhibitors, including inhibitors of phosphate transport in the gastrointestinal tract and the kidneys, and methods for their use as therapeutic or prophylactic agent.
• [EN] NHE3-BINDING COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT<br/>[FR] COMPOSÉS DE LIAISON À NHE3 ET PROCÉDÉS D'INHIBITION DU TRANSPORT DE PHOSPHATE
  申请人：ARDELYX INC

  公开号：WO2014169094A2

  公开（公告）日：2014-10-16

  Provided are NHE3-binding and/or NHE3 -modulating agents having activity as phosphate transport inhibitors, including inhibitors of phosphate transport in the gastrointestinal tract and the kidneys, and methods for their use as therapeutic or prophylactic agent.
• [EN] GLYCYRRHETINIC ACID DERIVATIVES FOR USE IN TREATING HYPERKALEMIA<br/>[FR] DÉRIVÉS D'ACIDE GLYCYRRHÉTINIQUE DESTINÉS À ÊTRE UTILISÉS DANS LE TRAITEMENT DE L'HYPERKALIÉMIE
  申请人：ARDELYX INC

  公开号：WO2020163642A1

  公开（公告）日：2020-08-13

  The present invention provides a compound of formula (I) or a salt thereof: (F ormula (I)) wherein X, L, V, R1, R2, R3 and R4, are as defined herein. The claimed compounds inhibit the enzyme 11-hydroxysteroid dehydrogenase type 2 (11-HSD2) and as a result are useful in the treatment of hyperkalemia by preventing cortisol from being oxidised to cortisone and thus allowing it to occupy the mineralocorticoid receptor, thus stimulating potassium excretion.