1-benzoyl-4-(4-pyridylcarbamoyl)piperidine | 110105-34-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-benzoyl-4-(4-pyridylcarbamoyl)piperidine
• 英文别名: 1-(phenylcarbonyl)-N-(pyridin-4-yl)piperidine-4-carboxamide；1-benzoyl-N-pyridin-4-ylpiperidine-4-carboxamide
• CAS: 110105-34-5
• 化学式: C₁₈H₁₉N₃O₂
• mdl: MFCD09874956
• 分子量: 309.368
• InChiKey: QQYHEZPCISSJEX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  62.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-benzoyl-4-(4-pyridylcarbamoyl)piperidine 、 1-propyl-4-(4-pyridylcarbamoyl)piperidine 、 1-[3-(2-(2-thienylmethyl)phenoxy)-2-hydroxypropyl]-4-(4-pyridylcarbamoyl)piperidine 生成 glycolic acid-lactic acid
  参考文献：
  名称：

  Visual function disorder improving agents

  摘要：

  本发明提供了一种含有具有Rho激酶抑制活性的化合物的视觉功能障碍改善剂，特别是(R)-(+)-N-(1H-吡咯[2,3-b]吡啶-4-基)-4-(1-氨基乙基)苯甲酰胺作为有效成分。该剂具有促进视网膜神经节细胞轴突延伸和视神经细胞再生的作用，可用于治疗与视网膜或视神经的损伤、缺陷、退化等引起的各种眼部疾病相关的视觉功能障碍。

  公开号：

  US20040106646A1

文献信息

• Preventives/remedies for kidney diseases
  申请人：——

  公开号：US20030096843A1

  公开（公告）日：2003-05-22

  A compound having a Rho kinase inhibitory activity, such as (+)-trans-4-(1-aminoethyl)-1-(4-pyridylcarbamoyl)-cyclohexane, has a renal interstitial fibrosis inhibitory action in renal interstitial fibrosis model mice and various other actions, and therefore, is useful as an agent for the prophylaxis or treatment of renal diseases.

  具有Rho激酶抑制活性的化合物，例如（+）-trans-4-(1-氨乙基)-1-(4-吡啶基氨甲酰基)-环己烷，对于肾间质纤维化模型小鼠具有肾间质纤维化抑制作用和其他各种作用，因此，可用作预防或治疗肾脏疾病的药物。
• Agent for prophylaxis and treatment of glaucoma
  申请人：——

  公开号：US20030125351A1

  公开（公告）日：2003-07-03

  An agent for the prophylaxis and treatment of glaucoma, which contains a compound having a Rho kinase inhibitory activity, particularly an agent for the prophylaxis and treatment of glaucoma, which contains a compound of the formula (I) 1 wherein each symbol is as defined in the specification, as the compound having a Rho kinase inhibitory activity, is provided. The agent for the prophylaxis and treatment of glaucoma of the present invention is a novel agent for the prophylaxis and treatment of glaucoma and has intraocular pressure lowering action, optic disc blood flow improving action and aqueous humor outflow promoting action.

  一种预防和治疗青光眼的药剂，其中包含一种具有Rho激酶抑制活性的化合物，特别是一种预防和治疗青光眼的药剂，其中包含式（I）1的化合物，其中每个符号如规范中所定义，作为具有Rho激酶抑制活性的化合物。本发明的预防和治疗青光眼的药剂是一种新型的预防和治疗青光眼的药剂，具有降低眼内压、改善视盘血流和促进房水排出的作用。
• Antitumor effect potentiators
  申请人：——

  公开号：US20030165576A1

  公开（公告）日：2003-09-04

  When used concurrently with an antitumor agent, a compound having a Rho kinase inhibitory activity, such as (R)-(+)-N-(4-pyridyl)-4-(1-aminoethyl)benzamide, reinforces an antitumor effect of the antitumor agent and is useful as an antitumor effect potentiator. Particularly, a compound having a Rho kinase inhibitory activity used with an antitumor agent in combination can reduce the dose of the antitumor agent, which in turn affords provision of a sufficient effect and/or reduction of side effects.

  当与抗肿瘤药物同时使用时，具有Rho激酶抑制活性的化合物，如(R)-(+)-N-(4-吡啶基)-4-(1-氨乙基)苯甲酰胺，可以增强抗肿瘤药物的抗肿瘤效果，并且可用作抗肿瘤效应增强剂。特别是，与抗肿瘤药物联合使用具有Rho激酶抑制活性的化合物可以降低抗肿瘤药物的剂量，从而提供足够的疗效和/或减少副作用。
• Pharmaceutical agent containing Rho kinase inhibitor
  申请人：——

  公开号：US20020032148A1

  公开（公告）日：2002-03-14

  A Rho kinase inhibitor is provided as a novel pharmaceutical agent, particularly as a therapeutic agent of hypertension, a therapeutic agent of angina pectoris, a suppressive agent of cerebrovascular contraction, a therapeutic agent of asthma, a therapeutic agent of peripheral circulation disorder, a prophylactic agent of immature birth, a therapeutic agent of arteriosclerosis, an anti-cancer drug, an anti-inflammatory agent, an immunosuppressant, a therapeutic agent of autoimmune disease, an anti-AIDS drug, a contraceptive, a prophylactic agent of digestive tract infection, a therapeutic agent of osteoporosis, a therapeutic agent of retinopathy and a brain function improving drug. In addition, the Rho kinase inhibitor is provided as a reagent and a diagnostic.

  提供了一种新型药物代理——Rho激酶抑制剂，特别用于治疗高血压、心绞痛、脑血管收缩抑制剂、哮喘、周围循环障碍的治疗剂、早产预防剂、动脉硬化的治疗剂、抗癌药物、抗炎剂、免疫抑制剂、自身免疫疾病的治疗剂、抗艾滋病药物、避孕药、消化道感染预防剂、骨质疏松症的治疗剂、视网膜病的治疗剂和脑功能改善药物。此外，Rho激酶抑制剂还可作为试剂和诊断工具。
• PREVENTIVES/REMEDIES FOR GLAUCOMA
  申请人：Senju Pharmaceutical Co., Ltd.

  公开号：EP1034793A1

  公开（公告）日：2000-09-13

  An agent for the prophylaxis and treatment of glaucoma, which contains a compound having a Rho kinase inhibitory activity, particularly an agent for the prophylaxis and treatment of glaucoma, which contains a compound of the formula (I) wherein each symbol is as defined in the specification, as the compound having a Rho kinase inhibitory activity, is provided. The agent for the prophylaxis and treatment of glaucoma of the present invention is a novel agent for the prophylaxis and treatment of glaucoma and has intraocular pressure lowering action, optic disc blood flow improving action and aqueous humor outflow promoting action.

  一种用于预防和治疗青光眼的制剂，其中含有一种具有 Rho 激酶抑制活性的化合物，特别是一种用于预防和治疗青光眼的制剂，其中含有式（I）化合物 其中各符号如本说明书中所定义，作为具有 Rho 激酶抑制活性的化合物。本发明的青光眼预防和治疗剂是一种新型的青光眼预防和治疗剂，具有降低眼压、改善视盘血流和促进房水外流的作用。