卡立泊来德甲磺酸盐

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 异戊烯醇脂质
• 中文名称: 卡立泊来德甲磺酸盐
• 英文名称: HOE642
• 英文别名: 4-isopropyl-3-methylsulphonylbenzoyl-guanidine methanesulphonate；cariporide mesylate；cariporide；(4-isopropyl-3-methylsulfonyl-benzoyl)-guanidine methanesulfonate；(4-isopropyl-3-methanesulfonylbenzoyl)guanidine methanesulfonate；N-carbamimidoyl-3-methylsulfonyl-4-propan-2-ylbenzamide;methanesulfonic acid
• 化学式: CH₄O₃S*C₁₂H₁₇N₃O₃S
• 分子量: 379.458
• InChiKey: FNDLQABGYJQJPH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.13
• 重原子数：
  24
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  187
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  4-异丙基苯甲酸 在 氯磺酸 、 sodium hydroxide 、 氯化亚砜 、 sodium sulfite 作用下， 以 四氢呋喃 、 水 、 N,N-二甲基甲酰胺 、 甲苯 为溶剂， 反应 11.0h， 生成 卡立泊来德甲磺酸盐
  参考文献：
  名称：

  [EN] COMPOUNDS FOR TREATMENT OF CARDIOVASCULAR DISEASES
  [FR] COMPOSES POUR TRAITEMENT DES MALADIES CARDIO-VASCULAIRES

  摘要：

  含有钠-氢交换型1（NHE-1）抑制剂与Ca2+超载抑制剂的药物组合，以及利用这种组合抑制剂治疗心血管疾病（如缺血），特别是哺乳动物（包括人类）中的围手术期心肌缺血性损伤的用途被披露。

  公开号：

  WO2005079803A1

文献信息

• Benzoylguanidines, pharmaceutical composition containing them and
  申请人：Hoechst Aktiengesellschaft

  公开号：US05591754A1

  公开（公告）日：1997-01-07

  Benzoylguanidines, process for their preparation, their use as a medicament and medicament containing them. The invention relates to benzoylguanidines of the formula I ##STR1## where R(1) or R(2) is R(3)-S(O).sub.n -- or R(4)R(5)N--O.sub.2 S-- and the other substituent R(1) or R(2) in each case is H, OH, F, Cl, Br, I, alkyl, alkoxy, benzyloxy or phenoxy, R(3)-S(O).sub.n or R(4)R(5)N-- or 3,4-dehydropiperidine and R(3) is alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl, R(4) and R(5) are alkyl or phenylalkyl or phenyl, and in which R (4) and R (5) can also together be a C.sub.4 -C.sub.7 -chain, and in which R(4) and R(5), together with the nitrogen atom to which they are bonded, can be a dihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system, and where n is zero, 1 or 2 and their pharmaceutically tolerable salts are excellent antiarrhythmics.

  苯甲酰基胍，其制备方法，其作为药物的用途以及含有它们的药物。本发明涉及公式I的苯甲酰基胍##STR1## 其中R（1）或R（2）为R（3）-S（O）.sub.n--或R（4）R（5）N--O.sub.2 S--，而另一个取代基R（1）或R（2）在每种情况下为H，OH，F，Cl，Br，I，烷基，烷氧基，苄氧基或苯氧基，R（3）-S（O）.sub.n或R（4）R（5）N--或3,4-脱氢哌啶和R（3）为烷基，环烷基，环戊基甲基，环己基甲基或苯基，R（4）和R（5）为烷基或苯基烷基或苯基，其中R（4）和R（5）也可以共同成为C.sub.4-C.sub.7-链，在其中R（4）和R（5），连同它们所连接的氮原子，可以是二氢吲哚，四氢喹啉或四氢异喹啉系统，其中n为0,1或2，它们的药物耐受性盐是优秀的抗心律失常药物。
• Pharmaceutical compositions for the treatment of ischemic brain damage
  申请人：Sumitomo Pharmaceuticals Company, Limited

  公开号：EP0937459A2

  公开（公告）日：1999-08-25

  The use of a compound which has Na+/H+ exchange system inhibition activity, in particular a substituted guanidine derivative, or a pharmaceutically acceptable acid addition salt thereof, in the manufacture of a pharmaceutical composition for the treatment of ischemic brain damage such as cerebral infarction, cerebral embolism and cerebral thrombus.

  将具有Na+/H+交换系统抑制活性的化合物，特别是取代的胍衍生物或其药学上可接受的酸加成盐，用于制造治疗缺血性脑损伤（如脑梗塞、脑栓塞和脑血栓）的药物组合物。
• REMEDY FOR URINARY FREQUENCY AND URINARY INCONTINENCE
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP1532978A1

  公开（公告）日：2005-05-25

  A composition for treating frequent urination and/or urinary incontinence comprising a compound having an activity to inhibit Na+/H+ exchange transporter or its pharmaceutically acceptable salt as an active ingredient.

  一种用于治疗尿频和/或尿失禁的组合物，其活性成分包括一种具有抑制 Na+/H+ 交换转运体活性的化合物或其药学上可接受的盐。
• Compositions and methods for treating disorders associated with salt or fluid retention
  申请人：Ironwood Pharmaceuticals, Inc.

  公开号：EP2671584A2

  公开（公告）日：2013-12-11

  Methods for reducing the risk of or treating a disorder associated with fluid and/or salt retention in a patient are described. The methods include administering to the patient an agent selected from: a) an agent that reduces sodium absorption in the intestine; b) an agent that increases anion secretion in the intestine; or c) an agent that both reduces sodium absorption in the intestine and increases anion secretion in the intestine.

  本文描述了降低患者发生与体液和/或盐潴留有关的疾病的风险或治疗这种疾病的方法。这些方法包括向患者施用选自以下几种的制剂：a) 减少肠道钠吸收的制剂；b) 增加肠道阴离子分泌的制剂；或 c) 既减少肠道钠吸收又增加肠道阴离子分泌的制剂。
• Pharmaceutical composition comprising a sodium hydrogen exchange inhibitor and an angiotensin converting enzyme inhibitor
  申请人：——

  公开号：US20030158247A1

  公开（公告）日：2003-08-21

  This invention is directed to a pharmaceutical composition comprising the sodium-hydrogen exchanger (NHE) inhibitor cariporide and an angiotensin converting enzyme (ACE) inhibitor which exhibits unexpectedly efficacious properties for preventing heart failure and other age-related organ dysfunctions, age-related disorders and for prolonging life, and to methods of preventing heart failure and other age-related organ dysfunctions, age-related disorders and for prolonging life comprising administering pharmaceutically effective amounts of the sodium-hydrogen exchange inhibitor cariporide and an ACE inhibitor.

  本发明涉及一种药物组合物，该组合物包含钠-氢交换机（NHE）抑制剂卡利波利和血管紧张素转换酶（ACE）抑制剂，在预防心力衰竭和其他与年龄相关的器官功能障碍方面具有意想不到的功效、以及预防心力衰竭和其他与年龄有关的器官功能障碍、与年龄有关的疾病和延长寿命的方法，包括给药有效量的钠-氢交换抑制剂卡利波利和血管紧张素转换酶抑制剂。