L-erythro-5,6,7,8-tetrahydrobiopterin

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 蝶啶及其衍生物
• 英文名称: L-erythro-5,6,7,8-tetrahydrobiopterin
• 英文别名: 2-amino-6-[(1R,2S)-1,2-dihydroxypropyl]-5,6,7,8-tetrahydro-3H-pteridin-4-one
• 化学式: C₉H₁₅N₅O₃
• 分子量: 241.25
• InChiKey: FNKQXYHWGSIFBK-BYAPIUGTSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.9
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  132
• 氢给体数：
  6
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  L-erythro-5,6,7,8-tetrahydrobiopterin 生成 2-amino-6-[(1R,2S)-1,2-dihydroxypropyl]-4a-hydroxy-3,7,8,8a-tetrahydropteridin-4-one
  参考文献：
  名称：

  HAAVIK, J.;ANDERSSON, K. K.;PETERSSON, L.;FLATMARK, T., BIOL. CHEM. HOPPE-SEYLER., 369,(1988) N 7, 528

  摘要：

  DOI：

文献信息

• COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC DISEASES
  申请人：CELLIXBIO PRIVATE LIMITED

  公开号：US20150291590A1

  公开（公告）日：2015-10-15

  The invention relates to the compounds of formula I, formula II and formula III or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II or formula III; and methods for treating or preventing metabolic diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of phenylketonuria, cardiovascular disease, autism, ADHD, hypertension, endothelial dysfunction and chronic kidney disease.

  该发明涉及公式I、公式II和公式III的化合物或其药用可接受的盐，以及其多晶型、溶剂合物、对映体、立体异构体和水合物。包括公式I、公式II或公式III化合物的有效量的药物组合物；以及用于治疗或预防代谢性疾病的方法可以制备成口服、颊内、直肠、局部、经皮、经粘膜、静脉、肠道、糖浆或注射剂。这些组合物可用于治疗苯丙酮尿症、心血管疾病、自闭症、注意力缺陷多动障碍、高血压、内皮功能障碍和慢性肾脏疾病。
• PROCESS FOR PRODUCING CARBON-DIMINISHED ALDOSE COMPOUND
  申请人：Asubio Pharma Co., Ltd.

  公开号：EP1849793A1

  公开（公告）日：2007-10-31

  The present invention provides a process capable of industrially producing 5-deoxy-L-arabinose, important as a raw material for the production of sapropterin useful as a therapeutic agent for atypical hyperphenylalaninemia, satisfactorily efficiently even with a simple production apparatus. Provided is the process for producing 5-deoxy-L-arabinose characterized by including: reacting L-rhamnose with a C11-16 straight chain alkyl mercaptan compound in the presence of an acid catalyst to prepare L-rhamnose dialkylmercaptal; subjecting then the obtained compound to an oxidation reaction to prepare a sulfonyl derivative; and subjecting then the sulfonyl derivative to a carbon-reduction reaction to prepare 5-deoxy-L-arabinose. The present production process can also be applied to a process for producing compounds obtained by removing one carbon atom from other aldol compounds, and thus the present invention provides a general process for producing compounds obtained by reducing the number of carbon atoms from aldose compounds.

  本发明提供了一种工业生产5-去氧-L-阿拉伯糖的方法，该方法是生产治疗非典型高苯丙氨酸血症的治疗剂Sapropterin的原材料，即使使用简单的生产设备也能高效地生产。该生产方法包括以下步骤：在酸催化剂的存在下，将L-鼠李糖与C11-16直链烷基巯基化合物反应，制备L-鼠李糖二烷基硫代缩醛；然后将所得化合物进行氧化反应，制备磺酰基衍生物；最后将磺酰基衍生物进行碳还原反应，制备5-去氧-L-阿拉伯糖。该生产方法也可以应用于从其他醛糖化合物中去除一个碳原子得到的化合物的生产过程，因此本发明提供了一种从醛糖化合物中减少碳原子数量得到化合物的通用生产方法。
• PTERIN ANALOGS
  申请人：KAKKIS Emil D.

  公开号：US20100016328A1

  公开（公告）日：2010-01-21

  Disclosed herein are analogs of tetrahydrobiopterin, compositions containing the same, and methods of treating an individual suffering from a condition responsive to tetrahydrobiopterin by administration of the analog. These analogs are contemplated for use wherever tetrahydrobiopterin is currently used to treat conditions responsive to tetrahydrobiopterin therapies.

  本文披露了四氢生物黄素的类似物、包含类似物的组合物以及通过给予类似物治疗对四氢生物黄素敏感的病症的个体的方法。这些类似物可在目前使用四氢生物黄素治疗对四氢生物黄素疗法敏感的病症的任何地方使用。
• METHOD FOR PREPARING L-ERYTHROBIOPTERIN COMPOUND
  申请人：Shanghai Forefront Pharma Co., Ltd.

  公开号：EP4019523A1

  公开（公告）日：2022-06-29

  The invention relates to a preparation method of L-erythro biopterin compound. Among them, the L-erythro biopterin compound is of a structure as shown in formula (I), and the L-erythro biopterin compound represented by formula (I) is mainly obtained by a dihydroxylation reaction of the compound with a structure as shown in formula (II) or formula (III); The preparation method of L-erythro biopterin compound is of high production efficiency, low cost, is environment-friendly, and suitable for industrial production.

  本发明涉及一种L-赤式生物蝶呤化合物的制备方法。其中，L-赤式生物蝶呤化合物的结构如式（I）所示，式（I）代表的 L-赤式生物蝶呤化合物主要由结构如式（II）或式（III）所示的化合物通过二羟基化反应得到； 该 L-赤式生物蝶呤化合物的制备方法生产效率高、成本低、环境友好，适合工业化生产。
• Modulation of the nitric oxide synthase pathway for oral health
  申请人：Meharry Medical College

  公开号：US10688098B2

  公开（公告）日：2020-06-23

  Pharmaceutical compositions and methods of treatment or prevention of diseases and conditions associated with or characterized by at least one of xerostomia and periodontal disease by modulation of the nitric oxide synthase pathway are provided, as are animal models and drug screening methods. Such modulation may be achieved by the administration of tetrahydrobiopterin (BH4) or its prodrugs and/or salts. Treating and preventing xerostomia can have the downstream effect of also preventing periodontitis, dental caries, parotid gland enlargement, inflammation and fissuring of the lips (chelitis), inflammation or ulcers of the tongue and buccal mucosa, oral candidiasis, salivary gland infection (sialadenitis), halitosis, and cracking and fissuring of oral mucosa.

  本研究提供了通过调节一氧化氮合酶途径治疗或预防与口腔干燥症和牙周病中至少一种相关或以其为特征的疾病和病症的药物组合物和方法，以及动物模型和药物筛选方法。这种调节可通过服用四氢生物蝶呤（BH4）或其原药和/或盐来实现。治疗和预防口腔干燥症的下游效果还包括预防牙周炎、龋齿、腮腺肿大、嘴唇发炎和裂开（唇炎）、舌头和口腔粘膜发炎或溃疡、口腔念珠菌病、唾液腺感染（唾液腺炎）、口臭以及口腔粘膜开裂和裂开。