[5-methyl-2-phenyl-2H-1,2,3-triazole-4-carbonyl]guanidine | 209538-43-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: [5-methyl-2-phenyl-2H-1,2,3-triazole-4-carbonyl]guanidine
• 英文别名: N-carbamimidoyl-5-methyl-2-phenyltriazole-4-carboxamide
• CAS: 209538-43-2
• 化学式: C₁₁H₁₂N₆O
• 分子量: 244.256
• InChiKey: URFUKELOUPOPNT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  112
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• [EN] COMPOUNDS FOR TREATMENT OF CARDIOVASCULAR DISEASES<br/>[FR] COMPOSES POUR TRAITEMENT DES MALADIES CARDIO-VASCULAIRES
  申请人：PFIZER PROD INC

  公开号：WO2005079803A1

  公开（公告）日：2005-09-01

  Pharmaceutical compositions containing sodium-hydrogen exchanger type 1 (NHE-1) inhibitors in combination with Ca 2+ overload inhibitors, and the use of such combination inhibitors to treat, for example, cardiovascular disease, such as ischemia, particularly, perioperative myocardial ischemic injury in mammals, including humans, are disclosed.

  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。
• [EN] N-[(SUBSTITUTED FIVE-MEMBERED DI- OR TRIAZA DIUNSATURATED RING)CARBONYL] GUANIDINE DERIVATIVES FOR THE TREATMENT OF ISCHEMIA<br/>[FR] DERIVES DE LA N-[(A CYCLE DI OU TRIAZA DIINSATURE SUBSTITUE) CARBONYLE] GUANIDINE UTILISES POUR LE TRAITEMENT DE L'ISCHEMIE
  申请人：PFIZER PRODUCTS INC.

  公开号：WO1999043663A1

  公开（公告）日：1999-09-02

  (EN) NHE-1 inhibitors, methods of using such NHE-1 inhibitors and pharmaceutical compositions containing such NHE-1 inhibitors. The NHE-1 inhibitors are useful for the reduction of tissue damage resulting from tissue ischemia.(FR) L'invention porte sur des inhibiteurs du NHE-1, sur leurs procédés d'utilisation, et sur des préparations pharmaceutiques les contenant. Lesdits inhibiteurs servent à réduire les dommages tissulaires résultant de l'ischémie des tissus.

  NHE-1抑制剂，使用这种NHE-1抑制剂的方法以及含有这种NHE-1抑制剂的药物组合物。这些NHE-1抑制剂有助于减少组织缺血引起的组织损伤。
• Treatment of diabetes and diabetic complications with NHE-1 inhibitors
  申请人：Pfizer Inc.

  公开号：US20030212104A1

  公开（公告）日：2003-11-13

  This invention relates to methods of treating or preventing type 2 diabetes, diabetic neuropathy, diabetic cardiomyopathy, cataracts, diabetic retinopathy, foot ulcers, diabetic microangiopathy, diabetic macroangiopathy, diabetic ischemia reperfusion injury, diabetic cardiac ischemia reperfusion injury and/or insulin resistance syndrome (IRS) in mammals, particularly in humans, by administering a sodium-hydrogen exchanger type 1 (NHE-1) inhibitor or a pharmaceutical composition containing such an inhibitor. This invention also relates to combinations comprising NHE-1 inhibitors and a second pharmaceutical agent, said combinations being useful in treating type 2 diabetes, IRS, diabetic neuropathy, diabetic cardiomyopathy, cataracts, diabetic retinopathy, foot ulcers, diabetic ischemia reperfusion injury, diabetic cardiac ischemia reperfusion injury, diabetic microangiopathy and/or diabetic macroangiopathy.

  本发明涉及一种治疗或预防哺乳动物中的2型糖尿病、糖尿病神经病、糖尿病心肌病、白内障、糖尿病视网膜病变、足部溃疡、糖尿病微血管病、糖尿病大血管病、糖尿病缺血再灌注损伤、糖尿病心脏缺血再灌注损伤及/或胰岛素抵抗综合症（IRS）的方法，尤其是在人类中，通过给哺乳动物或人类注射一种钠-氢交换酶类型1（NHE-1）抑制剂或含有这种抑制剂的药物组合物。本发明还涉及包含NHE-1抑制剂和第二种药物剂量的组合物，该组合物在治疗2型糖尿病、IRS、糖尿病神经病、糖尿病心肌病、白内障、糖尿病视网膜病变、足部溃疡、糖尿病缺血再灌注损伤、糖尿病心脏缺血再灌注损伤、糖尿病微血管病和/或糖尿病大血管病方面有用。
• N-[(substituted five-membered di-or triaza diunsaturated ring)carbonyl] guanidine derivatives for the treatment of ischemia
  申请人：Pfizer Inc.

  公开号：US20030149043A1

  公开（公告）日：2003-08-07

  NHE-1 inhibitors, methods of using such NHE-1 inhibitors and pharmaceutical compositions containing such NHE-1 inhibitors. The NHE-1 inhibitors are useful for the reduction of tissue damage resulting from tissue ischemia.

  NHE-1抑制剂，使用这种NHE-1抑制剂的方法以及含有这种NHE-1抑制剂的制药组合物。NHE-1抑制剂对于减少组织缺血引起的组织损伤是有用的。
• Combination therapy involving a sodium-hydrogen exchanger type 1 or NHE-1 inhibitor for use in treatment of ischemia
  申请人：Pfizer Products Inc.

  公开号：EP1226830A2

  公开（公告）日：2002-07-31

  The invention provdes methods of reducing tissue damage resulting from ischemia which comprise administering to a mammal in need of such reduction an effective amount of a combination, or a pharmaceutical composition comprising such combination, of an NHE-1 inhibitor and a second compound selected from the group consisting of: (a) a complement modulator, (b) a metabolic modulator, (c) an anti-apoptotic agent, (d) a nitric oxide synthase-related agent, and (e) an enzyme/protein modulator. The invention further provides pharmaceutical compositions comprising an amount of an NHE-1 inhibitor; an amount of a second compound selected from the group consisting of (a) a complement modulator, (b) a metabolic modulator, (c) an anti-apoptotic agent, (d) a nitric oxide synthase-related agent, and an enzyme/protein modulator selected from the group consisting of a protein kinase C activator, an endothelin converting enzyme inhibitor, a thrombin-activatable fibrinolysis inhibitor (TAFI) inhibitor, an activated thrombin-activatable fibrinolysis inhibitor (TAFIa) inhibitor, a Na+/Ca+2 exchanger isoform-1 (NCX-1) inhibitor, and a poly (ADP ribose) synthetase (PARS/PARP) inhibitor; and, preferably, a pharmaceutically acceptable pharmaceutically acceptable carrier, vehicle, or diluent. The invention further provides kits comprising an amount of a sodium-hydrogen exchanger type-1 inhibitor, and a pharmaceutically acceptable carrier, vehicle, or diluent in a first unit dosage form; an amount of a second compound selected from the group consisting of (a) a complement modulator, (b) a metabolic modulator, (c) an anti-apoptotic agent, (d) a nitric oxide synthase-related agent, and (e) an enzyme/protein modulator selected from the group consisting of a protein kinase C activator, an endothelin converting enzyme inhibitor, a thrombin-activatable fibrinolysis inhibitor (TAFI) inhibitor, an activated thrombin-activatable fibrinolysis inhibitor (TAFIa) inhibitor, a Na+/Ca+2 exchanger isoform-1 (NCX-1) inhibitor, and a poly (ADP ribose) synthetase (PARS/PARP) inhibitor, and a pharmaceutically acceptable carrier, vehicle, or diluent in a second unit dosage form; and a container.

  本发明提供了减少缺血导致的组织损伤的方法，该方法包括向需要减少损伤的哺乳动物施用有效量的 NHE-1 抑制剂和选自以下组别的第二种化合物的组合或包含这种组合的药物组合物：(a) 补体调节剂，(b) 代谢调节剂，(c) 抗凋亡剂，(d) 一氧化氮合酶相关剂，和 (e) 酶/蛋白调节剂。本发明进一步提供了药物组合物，其中包含一定量的 NHE-1 抑制剂；一定量的选自以下组别的第二种化合物：(a) 补体调节剂；(b) 代谢调节剂；(c) 抗凋亡剂；(d) 一氧化氮合酶相关剂；以及选自以下组别的酶/蛋白调节剂：蛋白激酶 C 激活剂、内皮素转换酶抑制剂、凝血酶活化性纤维蛋白溶解抑制剂（TAFI）抑制剂、活化的凝血酶活化性纤维蛋白溶解抑制剂（TAFIa）抑制剂、Na+/Ca+2 交换异构体-1（NCX-1）抑制剂和多（ADP 核糖）合成酶（PARS/PARP）抑制剂；以及，优选药学上可接受的载体、载体或稀释剂。本发明进一步提供了包含一定量的钠-氢交换剂型-1 抑制剂和药学上可接受的载体、载体或稀释剂的试剂盒，试剂盒为第一单位剂型；一定量的选自以下组别的第二种化合物：(a) 补体调节剂；(b) 代谢调节剂；(c) 抗细胞凋亡剂；(d) 一氧化氮合酶相关剂；(e) 酶/蛋白调节剂，选自以下组别：蛋白激酶 C 激活剂；内皮素转换酶抑制剂；凝血酶激活的可凝血酶抑制剂、凝血酶活化性纤维蛋白溶解抑制剂（TAFI）抑制剂、活化的凝血酶活化性纤维蛋白溶解抑制剂（TAFIa）抑制剂、Na+/Ca+2 交换异构体-1（NCX-1）抑制剂和聚（ADP 核糖）合成酶（PARS/PARP）抑制剂，以及药学上可接受的载体、载体或稀释剂组成的组；以及一个容器。