ethyl 3-(2-amino-6-oxo-1H-purin-9-yl)propanoate

• 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: ethyl 3-(2-amino-6-oxo-1H-purin-9-yl)propanoate
• 化学式: C₁₀H₁₃N₅O₃
• 分子量: 251.24
• InChiKey: GGNXFQAJENHFIZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  18
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  112
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Methods for treatment of disease-induced peripheral neuropathy and related conditions
  申请人：Spectrum Pharmaceuticals, Inc.

  公开号：EP1790344A2

  公开（公告）日：2007-05-30

  The use of a compound of formula (I) in the manufacture of a medicament for the treatment of peripheral neuropathy. The compound can induce peripheral nerve sprouting through the action of a neurotrophic factor such as nerve growth factor (NGF) without the occurrence of hyperalgesia. The peripheral nerve sprouting can be nociceptive nerve sprouting.

  将式（I）化合物用于制造治疗周围神经病变的药物。该化合物可通过神经生长因子（NGF）等神经营养因子的作用诱导周围神经萌发，而不会出现痛觉减退。外周神经萌发可以是痛觉神经萌发。
• Methods for stimulation of synthesis of synaptophysin in the central nervous system
  申请人：——

  公开号：US20020040032A1

  公开（公告）日：2002-04-04

  A method of increasing the synthesis and/or secretion of synaptophysin comprises administering to a patient with a neurological disease or a patient at risk of developing a neurological disease an effective quantity of a purine derivative or analogue, a tetrahydroindolone derivative or analogue, or a pyrimidine derivative or analogue. If the compound is a purine derivative, the purine moiety can be guanine or hypoxanthine. The neurological disease can be a neurodegenerative disease such as Alzheimer's disease or a neurodevelopmental disorder such as Down's syndrome. Typically, the compound can pass through the blood-brain barrier. The purine moiety can be hypoxanthine or guanine. A particularly preferred purine derivative is N-4-carboxyphenyl-3-(6-oxohydropurin-9-yl) propanamide.

  一种增加突触素合成和/或分泌的方法包括向神经系统疾病患者或有患神经系统疾病风险的患者施用有效量的嘌呤衍生物或类似物、四氢吲哚酮衍生物或类似物或嘧啶衍生物或类似物。如果化合物是嘌呤衍生物，嘌呤分子可以是鸟嘌呤或次黄嘌呤。神经系统疾病可以是神经退行性疾病，如阿尔茨海默病，也可以是神经发育障碍，如唐氏综合征。通常情况下，化合物可以通过血脑屏障。嘌呤分子可以是次黄嘌呤或鸟嘌呤。一种特别优选的嘌呤衍生物是 N-4-羧基苯基-3-（6-氧代氢嘌呤-9-基）丙酰胺。
• Methods for prevention of accumulation of amyloid beta peptide in the central nervous system
  申请人：——

  公开号：US20020040031A1

  公开（公告）日：2002-04-04

  A method of either inhibiting the formation of A&bgr; or stimulating the formation of sAPP comprises administering to a patient with a neurological disease or a patient at risk of developing a neurological disease an effective quantity of a purine derivative or analogue, a tetrahydroindolone derivative or analogue, or a pyrimidine derivative or analogue. If the compound is a purine derivative, the purine moiety can be guanine or hypoxanthine. The neurological disease can be a neurodegenerative disease such as Alzheimer's disease or a neurodevelopmental disorder such as Down's syndrome. Typically, the compound can pass through the blood-brain barrier. The purine moiety can be hypoxanthine or guanine. A particularly preferred purine derivative is N-4-carboxyphenyl-3-(6-oxohydropurin-9-yl) propanamide.

  一种抑制 A&bgr 形成或刺激 sAPP 形成的方法包括向神经系统疾病患者或有患神经系统疾病风险的患者施用有效量的嘌呤衍生物或类似物、四氢吲哚酮衍生物或类似物或嘧啶衍生物或类似物。如果化合物是嘌呤衍生物，嘌呤分子可以是鸟嘌呤或次黄嘌呤。神经系统疾病可以是神经退行性疾病，如阿尔茨海默病，也可以是神经发育障碍，如唐氏综合征。通常情况下，化合物可以通过血脑屏障。嘌呤分子可以是次黄嘌呤或鸟嘌呤。一种特别优选的嘌呤衍生物是 N-4-羧基苯基-3-（6-氧代氢嘌呤-9-基）丙酰胺。
• Methods for treatment of drug-induced peripheral neuropathy and related conditions
  申请人：——

  公开号：US20020061899A1

  公开（公告）日：2002-05-23

  A method of treating drug-induced peripheral neuropathy comprises administering to a patient with drug-induced peripheral neuropathy an effective quantity of a purine derivative or analogue, a tetrahydroindolone derivative or analogue, or a pyrimidine derivative or analogue. If the compound is a purine derivative, the purine moiety can be guanine or hypoxanthine. The compound can induce peripheral nerve sprouting through the action of a neurotrophic factor such as nerve growth factor (NGF) without the occurrence of hyperalgesia. The peripheral nerve sprouting can be nociceptive nerve sprouting. The drug-induced peripheral neuropathy can be drug-induced peripheral neuropathy associated with the administration of oncolytic drugs, such as a vinca alkaloid, cisplatin, paclitaxel, suramin, altretamine, carboplatin, chlorambucil, cytarabine, dacarbazine, docetaxel, etoposide, fludarabine, ifosfamide with mesna, tamoxifen, teniposide, or thioguanine. Methods according to the present invention are particularly useful in treating peripheral neuropathy associated with the administration of vincristine, paclitaxel, or cisplatin.

  一种治疗药物性周围神经病变的方法包括向药物性周围神经病变患者施用有效量的嘌呤衍生物或类似物、四氢吲哚酮衍生物或类似物或嘧啶衍生物或类似物。如果化合物是嘌呤衍生物，嘌呤分子可以是鸟嘌呤或次黄嘌呤。该化合物可通过神经生长因子（NGF）等神经营养因子的作用诱导外周神经萌发，而不会出现痛觉减退。外周神经萌发可以是痛觉神经萌发。药物诱导的周围神经病变可以是与服用溶瘤药物相关的药物诱导的周围神经病变，如长春花生物碱、顺铂、紫杉醇、苏拉明、阿曲他胺、卡铂、氯霉素、阿糖胞苷、达卡巴嗪、多西他赛、依托泊苷、氟达拉滨、伊福法胺与美司那、他莫昔芬、替尼泊苷或硫鸟嘌呤。根据本发明的方法尤其适用于治疗与长春新碱、紫杉醇或顺铂用药相关的周围神经病变。
• Methods for treatment of conditions affected by activity of multidrug transporters
  申请人：——

  公开号：US20020128264A1

  公开（公告）日：2002-09-12

  One aspect of the present invention is a method of treating a condition or disease associated with the activity of a multidrug transporter protein comprising administering to a mammal with a condition or disease associated with the activity of a multidrug transporter protein an effective quantity of a purine derivative or analogue, a tetrahydroindolone derivative or analogue, or a pyrimidine derivative or analogue. If the compound is a purine derivative, the purine moiety can be guanine or hypoxanthine. A particularly preferred bifunctional purine derivative is N-4-carboxyphenyl-3-(6-oxohydropurin-9-yl) propanamide. Methods according to the present invention can be used to treat cancer, a microbial or parasitic infection, HIV, infection, or a condition associated with inflammation such as asthma or rheumatic disease.

  本发明的一个方面是一种治疗与多药转运蛋白活性相关的病症或疾病的方法，包括向患有与多药转运蛋白活性相关的病症或疾病的哺乳动物施用有效量的嘌呤衍生物或类似物、四氢吲哚酮衍生物或类似物或嘧啶衍生物或类似物。如果化合物是嘌呤衍生物，嘌呤分子可以是鸟嘌呤或次黄嘌呤。一种特别优选的双功能嘌呤衍生物是 N-4-羧基苯基-3-（6-氧代氢嘌呤-9-基）丙酰胺。根据本发明的方法可用于治疗癌症、微生物或寄生虫感染、HIV、感染或与炎症有关的疾病，如哮喘或风湿病。