8-[3-[4-(diethylcarbamoyl)piperazin-1-yl]propyl]-1,3,7-trimethylxanthine hydrochloride | 138472-18-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并嘧啶类
• 英文名称: 8-[3-[4-(diethylcarbamoyl)piperazin-1-yl]propyl]-1,3,7-trimethylxanthine hydrochloride
• 英文别名: N,N-diethyl-4-[3-(1,3,7-trimethyl-2,6-dioxopurin-8-yl)propyl]piperazine-1-carboxamide;hydron;chloride
• CAS: 138472-18-1
• 化学式: C₂₀H₃₃N₇O₃*ClH
• 分子量: 455.988
• InChiKey: GVHZRDKDUVIRNY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  31
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.7
• 拓扑面积：
  85.2
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Compositions for prevention and treatment of dementia
  申请人：——

  公开号：US20030144255A1

  公开（公告）日：2003-07-31

  4,4′-diaminodiphenylsulphone is a bactericide and anti-inflammatory agent. It is known to have therapeutic activity against leprosy, dermatitis herpetiformis, actinomycotic mycetoma, asthma, malaria, rheumatoid arthritis, Kaposiis sarcoma, pneumocystis carinii (pneumonia), subcorneal pustular dermatosis and cystic acne, in patients in need of such therapy. It is also known to have therapeutic activity against memory loss in patients in need of such therapy, including patients suffering from Alzheimer disease and related neurodegenerative disorders. Donepezil hydrochloride (donepezil) is an acetylcholinesterase inhibitor that is currently used for the symptomatic treatment of Alzheimer disease in patients in need of such therapy. It has now been found that combinations of 4,4′-diaminodiphenylsulphone and cholinesterase inhibitors unexpectedly show synergistic effects in the prevention and/or treatment of dementia. The present invention relates to novel compositions and methods of preventing and/or treating dementia using combinations of 4,4′-diaminodiphenylsulphone and a cholinesterase inhibitor (preferably donepezil). The method involves the administration to such individuals a drug composition of 4,4′-diaminodiphenylsulphone and a cholinesterase inhibitor. The invention also relates to a method of preventing and/or treating dementia including senile dementia, that involves the use of this combination of drugs.

  4,4′-二氨基二苯砜是一种杀菌剂和消炎剂。已知它对需要治疗的麻风病、疱疹性皮炎、放线菌霉菌瘤、哮喘、疟疾、类风湿性关节炎、卡波氏肉瘤、卡氏肺孢子菌（肺炎）、角膜下脓疱性皮肤病和囊肿性痤疮具有治疗活性。众所周知，它还对需要此类治疗的患者（包括阿尔茨海默病和相关神经退行性疾病患者）的记忆力减退具有治疗活性。盐酸多奈哌齐（多奈哌齐）是一种乙酰胆碱酯酶抑制剂，目前用于对需要治疗的阿尔茨海默病患者进行对症治疗。现在发现，4,4′-二氨基二苯砜和胆碱酯酶抑制剂的组合在预防和/或治疗痴呆症方面意外地显示出协同作用。本发明涉及使用 4,4′-二氨基二苯砜和胆碱酯酶抑制剂（最好是多奈哌齐）组合预防和/或治疗痴呆症的新型组合物和方法。该方法包括给这些人服用 4,4′-二氨基二苯砜和胆碱酯酶抑制剂的药物组合物。本发明还涉及一种预防和/或治疗包括老年性痴呆在内的痴呆症的方法，其中包括使用这种药物组合。
• Utilisation d'un dérivé de la triméthyl-1,3,7 xanthine pour le traitement des troubles de la mémoire, des troubles intellectuels de la sénescence et de la maladie d'Alzheimer
  申请人：ADIR ET COMPAGNIE

  公开号：EP0470317B1

  公开（公告）日：1994-05-11
• IDEBENONE CONTAINING COMBINATION AGENT FOR TREATING ALZHEIMER'S DISEASE
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP0952826A1

  公开（公告）日：1999-11-03
• DPP-IV INHIBITORS FOR TREATING NEURODEGENERATION AND COGNITIVE DISORDERS
  申请人：Novartis AG

  公开号：EP1732550A2

  公开（公告）日：2006-12-20
• Dpp-iv inhibitors for treating neurodegeneration and cognitive disorders
  申请人：Hughes Thomas Edward

  公开号：US20090017015A1

  公开（公告）日：2009-01-15

  The invention relates to the use of a Dipeptidyl peptidase IV inhibitor (DPP-IV inhibitor) or a pharmaceutically acceptable salt thereof for the prevention, delay of progression or the treatment of neurodegenerative disorders, cognitive disorders and for improving memory (both short term and long term) and learning ability.