(3S)-2-[2-[(1-ethoxy-1-oxo-4-phenylbutan-2-yl)amino]propanoyl]-3,4-dihydro-1H-isoquinoline-3-carboxylic 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: (3S)-2-[2-[(1-ethoxy-1-oxo-4-phenylbutan-2-yl)amino]propanoyl]-3,4-dihydro-1H-isoquinoline-3-carboxylic acid
• 化学式: C₂₅H₃₀N₂O₅
• 分子量: 438.5
• InChiKey: JSDRRTOADPPCHY-IVXJCAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  32
• 可旋转键数：
  10
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  95.9
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• PREPARATION OF QUINAPRIL HYDROCHLORIDE
  申请人：——

  公开号：US20040192613A1

  公开（公告）日：2004-09-30

  Methods and materials for preparing quinapril, its pharmaceutically acceptable salts, including quinapril hydrochloride, are disclosed. The method includes reacting (2S,4S)-2-(4-methyl-2,5-dioxo-oxazolidin-3-yl)-4-phenyl-butyric acid ethyl ester with (3S)-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid tert-butyl ester to yield quinapril tert-butyl ester, which is subsequently reacted with an acid to yield quinapril or an acid addition salt of quinapril.

  制备喹那普利及其可药用盐的方法和材料被公开，包括喹那普利盐酸盐。该方法包括将(2S,4S)-2-(4-甲基-2,5-二氧代恶唑烷-3-基)-4-苯基丁酸乙酯与(3S)-1,2,3,4-四氢异喹啉-3-羧酸叔丁酯反应，得到喹那普利叔丁酯，随后与酸反应，得到喹那普利或喹那普利的酸加成盐。
• COMBINATION THERAPY FOR PATIENTS HAVING ACUTE AND/OR PERSISTENT DYSPNEA
  申请人：S-Form Pharma

  公开号：EP4023218A1

  公开（公告）日：2022-07-06

  Subject matter of the present invention is a combination medication for use in the treatment of a patient having acute and/or persistent dyspnea comprising at least two of the following components: a beta blocker, and one agent of the group consisting of an angiotensin-converting enzyme (ACE) inhibitor, an angiotensin II inhibitor and a combination of angiotensin II inhibitor or an angiotensin receptor-neprilysin inhibitor (ARNi), and mineralo receptor antagonist (MRA), gliflozine, a loop-acting diuretic, wherein a sample of bodily fluid of said patient has a level of BNP > 200 pg/mL and/or has a level NT-proBNP > 600 pg/mL, and wherein said sample of bodily fluid is selected from the group comprising blood, plasma and serum, and wherein said patient is either a patient with heart failure with left ventricular ejection fraction (LVEF) greater and equal to 40 %, preferably 50 %, or a patient with no heart failure.

  本发明的主题是一种用于治疗急性和/或持续性呼吸困难患者的复方药物，至少包含以下两种成分：血管紧张素转换酶（ACE）抑制剂、血管紧张素 II 抑制剂、血管紧张素 II 抑制剂或血管紧张素受体-肾素抑制剂（ARNi）和矿物质受体拮抗剂（MRA）的组合、格列酮类、环状作用利尿剂、其中，所述患者的体液样本的 BNP 水平大于 200 pg/mL，和/或 NT-proBNP 水平大于 600 pg/mL，且所述体液样本选自包括血液、血浆和血清的组，且所述患者为左室射血分数（LVEF）大于等于 40%（最好为 50%）的心衰患者或无心衰的患者。
• PROCESS FOR OBTAINING QUINAPRYL HYDROCHLORIDE AND SOLVATES USEFUL FOR ISOLATING AND PURIFYING QUINAPRYL HYDROCHLORIDE
  申请人：ESTEVE QUIMICA, S.A.

  公开号：EP0992495B1

  公开（公告）日：2004-02-04
• SIGMA-1 RECEPTOR AGONIST SYSTOLIC BLOOD PRESSURE THERAPY
  申请人：Anavex Life Sciences Corp.

  公开号：EP3716968A1

  公开（公告）日：2020-10-07
• STROMA-TARGETING TREATMENT FOR PATIENTS WITH ELEVATED ADAM12 LEVELS
  申请人：Academisch Medisch Centrum

  公开号：US20210145964A1

  公开（公告）日：2021-05-20

  The invention relates to a method for treating a human patient having a cancer characterized by at least one stroma-rich tumor, said human patient having increased disintegrin and metalloproteinase domain-containing protein 12 (ADAM12) levels in a bodily fluid, when compared to ADAM12 levels in a bodily fluid of a control person, the method comprising treating the human patient with a stroma-targeting agent. The invention further relates to a composition comprising a stroma-targeting agent for treating a human patient diagnosed with cancer characterized with at least one stroma-rich tumor, and one or more pharmaceutically acceptable excipients.