(2R,3R)-2,3-dihydroxybutanedioate;(2R,3R)-2,3-dihydroxybutanedioic acid;1-methyl-1-[5-(1-methylpyrrolidin-1-ium-1-yl)pentyl]pyrrolidin-1-ium

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (2R,3R)-2,3-dihydroxybutanedioate;(2R,3R)-2,3-dihydroxybutanedioic acid;1-methyl-1-[5-(1-methylpyrrolidin-1-ium-1-yl)pentyl]pyrrolidin-1-ium
• 化学式: C23H42N2O12
• 分子量: 538.6
• InChiKey: HSMKTIKKPMTUQH-WBPXWQEISA-L

计算性质

• 辛醇/水分配系数(LogP)：
  -4.28
• 重原子数：
  37
• 可旋转键数：
  10
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  236
• 氢给体数：
  6
• 氢受体数：
  12

文献信息

• Method for treating resistant hypertension
  申请人：Gerber Michael J.

  公开号：US20070196510A1

  公开（公告）日：2007-08-23

  A method is provided for lowering blood pressure in a patient having clinically diagnosed resistant hypertension. The method comprises administering darusentan to the patient adjunctively with a baseline antihypertensive regimen that comprises administration of at least one diuretic and at least two antihypertensive drugs selected from at least two of (a) ACE inhibitors and angiotensin II receptor blockers, (b) beta-adrenergic receptor blockers and (c) calcium channel blockers. The darusentan is orally administered at a dose and frequency effective, in combination with the baseline regimen, to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.

  提供了一种降低临床诊断为顽固性高血压患者血压的方法。该方法包括将达卢生坦作为辅助药物与基础抗高血压治疗方案联合给药，该基础方案包括至少一种利尿剂和至少两种抗高血压药物，这些药物选自至少两类：(a) ACE抑制剂和血管紧张素II受体阻滞剂，(b) β-肾上腺素能受体阻滞剂，以及(c) 钙通道阻滞剂。达卢生坦以有效剂量和频率口服给药，与基础治疗方案结合，能够使选自谷值坐位收缩压、谷值坐位舒张压、24小时动态收缩压、24小时动态舒张压、日间最高收缩压和日间最高舒张压的一个或多个血压参数至少降低约3 mmHg。
• THERAPY FOR COMPLICATIONS OF DIABETES
  申请人：Roden Robert L.

  公开号：US20090054473A1

  公开（公告）日：2009-02-26

  A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ET A ) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ET A receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ET A receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ET A receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ET A receptor antagonist.

  一种增强患有糖尿病肾病和/或代谢综合征的人类受试者的血糖控制和/或胰岛素敏感性的方法，包括向该受试者施用一种选择性内皮素A（ETA）受体拮抗剂，其剂量足以增强血糖控制和/或胰岛素敏感性。一种治疗老年糖尿病人类受试者中复合共病的方法，包括向该受试者施用一种选择性ETA受体拮抗剂，与至少一种其他药物联合或作为辅助治疗，该其他药物（i）不是选择性ETA受体拮抗剂，且（ii）在治疗糖尿病和/或至少一种除高血压外的上述共病中有效。适用于此类方法的治疗组合包括一种选择性ETA受体拮抗剂和至少一种非选择性ETA受体拮抗剂的抗糖尿病、抗肥胖或抗血脂异常药物。
• ANTIHYPERTENSIVE THERAPY
  申请人：Gerber Michael J.

  公开号：US20090221549A1

  公开（公告）日：2009-09-03

  A new use of darusentan is provided in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy with one or more drugs. The composition comprises darusentan in an amount providing a therapeutically effective daily dose; wherein (a) the composition is orally deliverable and/or (b) the daily dose of darusentan is effective to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures. Further provided is a new use of darusentan in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy, wherein the composition is administered adjunctively with at least one diuretic and at least one antihypertensive drug selected from ACE inhibitors, angiotensin II receptor blockers, beta-adrenergic receptor blockers and calcium channel blockers.

  提供了一种新的达卢生坦用途，用于制备一种药用组合物，旨在降低对一种或多种药物的基础抗高血压治疗表现出抵抗性的患者的血压。该组合物包含达卢生坦，其剂量提供了治疗上有效的每日剂量；其中（a）该组合物可通过口服给药，和/或（b）达卢生坦的每日剂量有效，能在一项或多项选自谷底坐位收缩压、谷底坐位舒张压、24小时动态收缩压、24小时动态舒张压、日间最高收缩压和日间最高舒张压的血压参数中至少降低约3mmHg。还提供了一种新的达卢生坦用途，用于制备一种药用组合物，旨在降低对基础抗高血压治疗表现出抵抗性的患者的血压，其中该组合物与至少一种利尿剂和至少一种选自ACE抑制剂、血管紧张素II受体阻滞剂、β-肾上腺素能受体阻滞剂和钙通道阻滞剂的抗高血压药物联合给药。
• [EN] INHIBITORS OF GLUCOSE-6-PHOSPHATE DEHYDROGENASE FOR TREATING CARDIOVASCULAR AND PULMONARY CONDITIONS<br/>[FR] INHIBITEURS DE LA GLUCOSE-6-PHOSPHATE DÉSHYDROGÉNASE PERMETTANT DE TRAITER DES AFFECTIONS CARDIOVASCULAIRES ET PULMONAIRES
  申请人：GUPTE SACHIN A

  公开号：WO2018093856A1

  公开（公告）日：2018-05-24

  The present disclosure provides for methods of treating or preventing a cardiovascular disorder and/or a related pulmonary disorder in a subject. In certain embodiments, the method comprises administering a therapeutically effective amount of an inhibitor of Glucose-6-phosphate dehydrogenase (G6PD), or a pharmaceutically acceptable salt, non-salt amorphous form, solvate, poly-morph, tautomer or prodrug thereof.

  本公开提供了用于治疗或预防受试者的心血管疾病和/或相关肺部疾病的方法。在某些实施例中，该方法包括向受试者投予治疗有效量的葡萄糖-6-磷酸脱氢酶（G6PD）抑制剂，或其药用可接受的盐、非盐非晶形态、溶剂合物、多形态、互变异构体或前药。
• METHODS AND COMPOSITIONS FOR TREATING INFECTION
  申请人：UNIVERSITY OF ROCHESTER

  公开号：US20150238473A1

  公开（公告）日：2015-08-27

  Provided herein are compositions and methods for treating or preventing infection.

  本文提供了用于治疗或预防感染的组合物和方法。