[1-(5-quinolinyl)-5-n-propyl-1H-pyrazole-4-carbonyl]guanidine | 241802-29-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: [1-(5-quinolinyl)-5-n-propyl-1H-pyrazole-4-carbonyl]guanidine
• 英文别名: N-carbamimidoyl-5-propyl-1-quinolin-5-ylpyrazole-4-carboxamide
• CAS: 241802-29-9
• 化学式: C₁₇H₁₈N₆O
• 分子量: 322.37
• InChiKey: SKXPKWWVCBZUIP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  112
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• Compounds for the treatment of ischemia
  申请人：——

  公开号：US20030055021A1

  公开（公告）日：2003-03-20

  A 3 agonists having Formula I are described herein as well as methods of using such A 3 agonists and pharmaceutical compositions containing such A 3 agonists. 1 The A 3 agonists are useful for the reduction of tissue damage resulting from tissue ischemia or hypoxia.

  本文描述了具有I式的A3受体激动剂，以及使用这种A3受体激动剂的方法和含有这种A3受体激动剂的药物组合物。这些A3受体激动剂对于减少由组织缺血或低氧引起的组织损伤是有用的。
• Sorbitol dehydrogenase inhibitors
  申请人：——

  公开号：US20040077671A1

  公开（公告）日：2004-04-22

  This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, 1 wherein R 1 , R 2 and R 3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an NHE-1 inhibitor and to methods of treating cardiomyopathy and other heart-related problems therewith. This invention is also directed to certain intermediates used in the synthesis of the compounds of formula I and to processes for preparing those intermediates.

  本发明涉及公式I的山梨醇脱氢酶抑制剂，其中R1、R2和R3如规范中所定义。本发明还涉及含有这些化合物的制药组合物以及通过向患有糖尿病且因此有发展这些并发症风险的哺乳动物投与这些化合物来治疗或预防糖尿病并发症，特别是糖尿病神经病、糖尿病肾病、糖尿病微血管病、糖尿病大血管病和糖尿病心肌病的方法。本发明还涉及一种公式I化合物与醛糖还原酶抑制剂的组合物制药组合物以及用于治疗或预防糖尿病并发症的方法。本发明还涉及一种公式I化合物与NHE-1抑制剂的组合物制药组合物以及用于治疗心肌病和其他心脏相关问题的方法。本发明还涉及用于合成公式I化合物的某些中间体以及制备这些中间体的方法。
• Pyridazinone aldose reductase inhibitors
  申请人：Mylari L. Banavara

  公开号：US20050113381A1

  公开（公告）日：2005-05-26

  The present invention relates to novel pyridazinone compounds, pharmaceutical compositions comprising those compounds and to methods of using such compounds and compositions to inhibit aldose reductase, lower sorbitol levels and, thus, lower fructose levels, and/or treat or prevent diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. This invention also relates to methods of affording cardioprotection to subjects not suffering from diabetes. This invention also relates to pharmaceutical compositions and kits comprising a combination of an aldose reductase inhibitor (ARI) of this invention and a sorbitol dehydrogenase inhibitor and to methods of using such compositions or kits to treat or prevent the above diabetic complications in mammals. This invention also relates to other combinations with the ARIs of this invention, including combinations with adenosine agonists; NHE-1 inhibitors; glycogen phosphorylase inhibitors; selective serotonin reuptake inhibitors; GABA agonists; antihypertensive agents; 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors; phosphodiesterase-5 inhibitors; and to glucose lowering agents.

  本发明涉及新型吡啶并咪唑酮化合物、包括这些化合物的制药组合物以及使用这些化合物和组合物的方法，以抑制醛固酮还原酶，降低山梨醇水平，从而降低果糖水平，并/或治疗或预防哺乳动物的糖尿病并发症，如糖尿病神经病变、糖尿病视网膜病变、糖尿病肾病、糖尿病心肌病、糖尿病微血管病和糖尿病大血管病。本发明还涉及在没有糖尿病的受试者中提供心脏保护的方法。本发明还涉及包含本发明的醛固酮还原酶抑制剂（ARI）和山梨醇脱氢酶抑制剂的组合的制药组合物和工具包，以及使用这些组合物或工具包治疗或预防哺乳动物的上述糖尿病并发症的方法。本发明还涉及与本发明的ARI的其他组合，包括与腺苷受体激动剂的组合；NHE-1抑制剂；糖原磷酸化酶抑制剂；选择性5-羟色胺再摄取抑制剂；GABA激动剂；降压药物；3-羟基-3-甲基谷氨酰辅酶A还原酶抑制剂；磷酸二酯酶-5抑制剂；以及降糖药物。
• 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。