7-(1-butanesulfonylcarbamoyl)-1-(2,4-dichlorobenzyl)-2-methylbenzimidazole

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 英文名称: 7-(1-butanesulfonylcarbamoyl)-1-(2,4-dichlorobenzyl)-2-methylbenzimidazole
• 英文别名: N-butylsulfonyl-3-[(2,4-dichlorophenyl)methyl]-2-methylbenzimidazole-4-carboxamide
• 化学式: C₂₀H₂₁Cl₂N₃O₃S
• 分子量: 454.377
• InChiKey: BBYKXXFGGJUBDU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  29
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  89.4
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  7-carboxy-1-(2,4-dichlorobenzyl)-2-methylbenzimidazole 、 1-丁烷磺酰胺 在 1,8-二氮杂双环[5.4.0]十一碳-7-烯 、 N,N'-羰基二咪唑 作用下， 生成 7-(1-butanesulfonylcarbamoyl)-1-(2,4-dichlorobenzyl)-2-methylbenzimidazole
  参考文献：
  名称：

  Benzimidazole compounds

  摘要：

  一种由公式（I）表示的苯并咪唑化合物：其中R3是一个羧基、酯化羧基、酰胺化羧基、氨基、酰胺基或磺酰基，或其药学上可接受的盐。由于它们具有降低血糖作用或PDE5抑制作用，这些化合物或其盐可用作治疗糖耐量受损、糖尿病、糖尿病并发症、胰岛素抵抗综合征、高脂血症、动脉粥样硬化、心血管疾病、高血糖或高血压的药物；或心绞痛、高血压、肺动脉高压、充血性心力衰竭、肾小球病、肾小管间质疾病、肾功能衰竭、动脉粥样硬化、血管狭窄、远端血管病、脑卒中、慢性可逆性梗阻、过敏性鼻炎、荨麻疹、青光眼、以肠蠕动障碍为特征的疾病、阳痿、糖尿病并发症、肾炎、癌性消瘦或PTCA后再狭窄的药物。

  公开号：

  US06352985B1

文献信息

• Benzimidazole compounds
  申请人：Fujisawa Pharmaceutical Co., Ltd.

  公开号：US06352985B1

  公开（公告）日：2002-03-05

  A benzimidazole compound represented by the formula (I): wherein R3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable salts. Because of their blood sugar-depressing effect or PDE5 inhibitory effect, these compounds or salts thereof are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin resistance, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, or hypertension; or stenocardia, hypertension, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, atherosclerosis, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, diabetic complications, nephritis, cancerous cachexia, or restenosis after PTCA.

  一种由公式（I）表示的苯并咪唑化合物：其中R3是一个羧基、酯化羧基、酰胺化羧基、氨基、酰胺基或磺酰基，或其药学上可接受的盐。由于它们具有降低血糖作用或PDE5抑制作用，这些化合物或其盐可用作治疗糖耐量受损、糖尿病、糖尿病并发症、胰岛素抵抗综合征、高脂血症、动脉粥样硬化、心血管疾病、高血糖或高血压的药物；或心绞痛、高血压、肺动脉高压、充血性心力衰竭、肾小球病、肾小管间质疾病、肾功能衰竭、动脉粥样硬化、血管狭窄、远端血管病、脑卒中、慢性可逆性梗阻、过敏性鼻炎、荨麻疹、青光眼、以肠蠕动障碍为特征的疾病、阳痿、糖尿病并发症、肾炎、癌性消瘦或PTCA后再狭窄的药物。
• Benzimidazole derivatives
  申请人：Fujisawa Pharmaceutical Co., Ltd.

  公开号：US06166219A1

  公开（公告）日：2000-12-26

  Novel benzimidazole derivatives represented by the formula (I): ##STR1## wherein R.sub.3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable salts. Because of their blood sugar-depressing effect or PDE5 inhibitory effect, these compounds or salts thereof are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin resistance, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, or hypertension; or stenocardia, hypertension, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, atherosclerosis, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, diabetic complications, nephritis, cancerous cachexia, or restenosis after PTCA.

  新型苯并咪唑衍生物的化学式（I）表示如下：##STR1##其中R.sub.3是一个羧基、酯化羧基、酰胺化羧基、氨基、酰胺基或磺酰基，或它们的药学上可接受的盐。由于它们具有降低血糖作用或PDE5抑制作用，这些化合物或其盐可用作治疗糖耐量受损、糖尿病、糖尿病并发症、胰岛素抵抗综合征、高脂血症、动脉粥样硬化、心血管疾病、高血糖或高血压的药物；或心绞痛、高血压、肺动脉高压、充血性心力衰竭、肾小球病、肾小管间质疾病、肾功能衰竭、动脉粥样硬化、血管狭窄、远端血管病变、脑卒中、慢性可逆性梗阻、过敏性鼻炎、荨麻疹、青光眼、以肠动力障碍为特征的疾病、阳痿、糖尿病并发症、肾炎、癌性消瘦或PTCA后再狭窄的药物。
• BENZIMIDAZOLE DERIVATIVES
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP0882718A1

  公开（公告）日：1998-12-09

  Novel benzimidazole derivatives represented by the formula (I): wherein R3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable salts. Because of their blood sugar-depressing effect or PDE5 inhibitory effect, these compounds or salts thereof are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin resistance, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, or hypertension; or stenocardia, hypertension, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, atherosclerosis, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, diabetic complications, nephritis, cancerous cachexia, or restenosis after PTCA.

  由式(I)代表的新型苯并咪唑衍生物： 其中 R3 是羧基、酯化羧基、酰胺化羧基、氨基、酰胺基或磺酰基，或它们的药学上可接受的盐。由于具有降低血糖的作用或抑制 PDE5 的作用，这些化合物或其盐类可用作治疗糖耐量受损、糖尿病、糖尿病并发症、胰岛素抵抗综合征、高脂血症、动脉粥样硬化、心血管疾病、高血糖或高血压的药物；或狭窄性心肌病、高血压、肺动脉高压、充血性心力衰竭、肾小球病变、肾小管间质病变、肾功能衰竭、动脉粥样硬化、血管狭窄、远端血管病变、脑中风、慢性可逆性阻塞、过敏性鼻炎、荨麻疹、青光眼、以肠蠕动障碍为特征的疾病、阳痿、糖尿病并发症、肾炎、癌症恶病质或 PTCA 后再狭窄。
• Methods of Treating Neuropathic Pain with Benzimidazole Derivative Agonists of PPARgamma
  申请人：Chiang Lillian W.

  公开号：US20110028527A1

  公开（公告）日：2011-02-03

  Embodiments of the invention relate to the treatment of neuropathic pain in mammals. Embodiments of the invention include methods for treating neuropathic pain with benzimidazole derivatives with PPARgamma agonist activity, as well as methods for preparing medicaments used in such treatments of mammalian pain.
• US6166219A
  申请人：——

  公开号：US6166219A

  公开（公告）日：2000-12-26