Bvt-3498 | 376641-49-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: Bvt-3498
• 英文别名: 3-chloro-2-methyl-N-[4-[2-(3-oxomorpholin-4-yl)ethyl]-1,3-thiazol-2-yl]benzenesulfonamide
• CAS: 376641-49-5
• 化学式: C₁₆H₁₈ClN₃O₄S₂
• 分子量: 415.9
• InChiKey: WZFZJEPHYDDFCT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  26
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  125
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• [EN] INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1<br/>[FR] INHIBITEURS DE 11-BETA-HYDROXY-STEROIDE-DESHYDROGENASE DE TYPE 1
  申请人：BIOVITRUM AB

  公开号：WO2001090090A1

  公开（公告）日：2001-11-29

  The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of thecompounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

  本发明涉及式（II）的化合物，以及包含该化合物的药物组合物，以及其制备过程，以及化合物在医学上的应用以及用于制备对人类11-β-羟基类固醇脱氢酶1型酶有作用的药物。
• Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
  申请人：——

  公开号：US20040224996A1

  公开（公告）日：2004-11-11

  The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-&bgr;-hydroxysteroid dehydrogenase type 1 enzyme. 1

  本发明涉及式（II）的化合物，以及包含该化合物的制药组合物，其制备过程，以及在医学上使用该化合物以及用于制备对人体11-β-羟基类固醇脱氢酶1型酶起作用的药物。
• INHIBITORS OF 11-BETA-HYDROXY STERIOD DEHYDROGENASE TYPE 1
  申请人：BARF Tjeerd

  公开号：US20100113435A1

  公开（公告）日：2010-05-06

  The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

  本发明涉及公式（II）的化合物，以及包含这些化合物的制药组合物，它们的制备过程，以及这些化合物在医学上的使用和用于制备对人类11-β-羟基类固醇脱氢酶1型酶起作用的药物。
• Methods and compositions for treating alcohol use disorders
  申请人：Sanna Pietro Paolo

  公开号：US10039772B2

  公开（公告）日：2018-08-07

  Disclosed are methods and compositions for treating alcohol dependence by administration to a patient of an inhibitor of 11β-hydroxysteroid dehydrogenases (11β-HSD) to modulate glucocorticoid effects. One such compound is the 11β-HSD inhibitor carbenoxolone (18β-glycyrrhetinic acid 3β-O-hemisuccinate), which has been extensively employed in the clinic for the treatment of gastritis and peptic ulcer. Carbenoxolone is active on both 11β-HSD1 and 2 isoforms. Here, carbenoxolone is surprisingly shown to reduce both baseline and excessive drinking in rats and mice. The carbenoxolone diastereomer 18α-glycyrrhetinic acid 3β-O-hemisuccinate (αCBX), which the applicants discovered to be selective for 11β-HSD2, was also effective in reducing alcohol drinking in mice. Thus, 11β-HSD inhibitors are a new class of candidate alcohol abuse medications and existing 11β-HSD inhibitor drugs may be re-purposed for alcohol abuse treatment.

  本发明公开了通过向患者施用 11β-羟基类固醇脱氢酶（11β-HSD）抑制剂以调节糖皮质激素作用来治疗酒精依赖症的方法和组合物。其中一种化合物是 11β-HSD 抑制剂卡本诺酮（18β-甘草次酸 3β-O-hemisuccinate ），临床上已广泛用于治疗胃炎和消化性溃疡。卡贝诺酮对 11β-HSD1 和 2 同工酶均有活性。令人惊讶的是，羧甲诺龙在大鼠和小鼠体内可减少基线饮酒量和过量饮酒量。申请人发现，羧诺龙的非对映异构体 18α-甘草次酸 3β-O-hemisuccinate (αCBX)对 11β-HSD2 具有选择性，也能有效减少小鼠的饮酒量。因此，11β-HSD 抑制剂是一类新的候选酗酒药物，现有的 11β-HSD 抑制剂药物可重新用于酗酒治疗。
• FXR agonist compositions for combination therapy
  申请人：Intercept Pharmaceuticals, Inc.

  公开号：US10894054B2

  公开（公告）日：2021-01-19

  The present application relates to a pharmaceutical composition comprising a combination of an FXR agonist and at least one additional therapeutic agent that lowers the glucose level in the blood, stimulates insulin secretion, and/or increases insulin sensitivity. The present application relates to use of the pharmaceutical composition for the treatment or prevention of a FXR mediated disease or condition, such as NAFLD and NASH, a disease or condition related to an elevated level of glucose in the blood, decreased secretion of insulin, and/or decreased insulin sensitivity such as hyperglycemia, diabetes, obesity, and insulin resistance, or for lowering the glucose level in the blood, stimulating insulin secretion, and/or increasing insulin sensitivity.

  本申请涉及一种药物组合物，其包含一种FXR激动剂和至少一种额外治疗剂的组合，该治疗剂可降低血液中的葡萄糖水平、刺激胰岛素分泌和/或增加胰岛素敏感性。本申请涉及该药物组合物用于治疗或预防FXR介导的疾病或病症，如非酒精性脂肪肝和NASH，与血液中葡萄糖水平升高、胰岛素分泌减少和/或胰岛素敏感性降低有关的疾病或病症，如高血糖、糖尿病、肥胖和胰岛素抵抗，或用于降低血液中葡萄糖水平、刺激胰岛素分泌和/或增加胰岛素敏感性。