N-[(2',6'-difluorobiphenyl-4-yl)methyl]-N'-(7-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)urea | 711015-88-2

• 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: N-[(2',6'-difluorobiphenyl-4-yl)methyl]-N'-(7-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)urea
• 英文别名: 1-[[4-(2,6-Difluorophenyl)phenyl]methyl]-3-(7-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)urea
• CAS: 711015-88-2
• 化学式: C₂₄H₂₂F₂N₂O₂
• 分子量: 408.448
• InChiKey: ZEHCCUBGRDGXNS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  30
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  61.4
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• [EN] TETRAHYDRO-NAPHTHALENE DERIVATIVES<br/>[FR] DERIVES DE TETRAHYDRO-NAPHTHALENE
  申请人：BAYER HEALTHCARE AG

  公开号：WO2004052846A1

  公开（公告）日：2004-06-24

  This invention relates to tetrahydro-naphthalene derivatives and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.

  这项发明涉及四氢萘衍生物及其盐，可用作药物制剂的活性成分。本发明的四氢萘衍生物具有出色的VR1拮抗活性，适用于预防和治疗与VR1活性相关的疾病，特别是用于治疗尿失禁、膀胱过度活跃、急迫性尿失禁、慢性疼痛、神经病痛、术后疼痛、类风湿性关节炎疼痛、神经痛、神经病、疼痛、神经损伤、缺血、神经退行性疾病、中风、炎症性疾病、哮喘和慢性阻塞性肺疾病的治疗。
• Tetrahydro-naphthalene derivatives
  申请人：Tajimi Masaomi

  公开号：US20060128704A1

  公开（公告）日：2006-06-15

  This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. They have the general formula (I) in which R 1 represents hydrogen or C 1-6 alkyl, and X represents —N(H)Y 1 , —N(H)—C 1-6 alkylene Y 1 , biphenyl or C 1-6 alkyl substituted by biphenyl, and the group Y 1 is an optionally substituted biphenyl. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.

  本发明涉及四氢萘衍生物及其盐，其可作为药物制剂的活性成分。它们具有通式（I），其中R1代表氢或C1-6烷基，X代表-N（H）Y1，-N（H）-C1-6烷基Y1，联苯或被联苯取代的C1-6烷基，而Y1是一个可选的取代联苯。本发明的四氢萘衍生物作为VR1拮抗剂具有出色的活性，并可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗尿失禁，过度活动的膀胱，急迫性尿失禁，慢性疼痛，神经性疼痛，术后疼痛，类风湿性关节炎疼痛，神经痛，神经病，疼痛，神经损伤，缺血，神经退行性疾病，中风，炎症性疾病，哮喘和COPD的治疗。
• TETRAHYDRO-NAPHTHALENE DERIVATIVES
  申请人：Tajimi Masaomi

  公开号：US20080275047A1

  公开（公告）日：2008-11-06

  This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tethrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontienence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.

  本发明涉及四氢萘衍生物及其盐，其作为药物制剂的活性成分具有优异的VR1拮抗活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗尿失禁、过度活动的膀胱、急迫性尿失禁、慢性疼痛、神经痛、术后疼痛、类风湿关节炎疼痛、神经痛、神经病、疼痛、神经损伤、缺血、神经退行性疾病、中风、炎症性疾病、哮喘和慢性阻塞性肺疾病的治疗。
• JP2006509018A
  申请人：——

  公开号：JP2006509018A

  公开（公告）日：2006-03-16
• US7381840B2
  申请人：——

  公开号：US7381840B2

  公开（公告）日：2008-06-03