哌丁茶碱 | 110390-84-6

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 哌丁茶碱
• 英文名称: 7-(4-(4-(p-fluorobenzoyl)-piperidino)-butyl)-theophylline
• 英文别名: perbufylline；7-[4-[4-(4-fluorobenzoyl)piperidin-1-yl]butyl]-1,3-dimethylpurine-2,6-dione
• CAS: 110390-84-6
• 化学式: C₂₃H₂₈FN₅O₃
• 分子量: 441.505
• InChiKey: RUELBIYEEYFIQA-UHFFFAOYSA-N

物化性质

• 沸点：
  647.3±65.0 °C(Predicted)
• 密度：
  1.34±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  32
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  78.8
• 氢给体数：
  0
• 氢受体数：
  6

文献信息

• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。
• Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
  申请人：Scaramuzzino, Giovanni

  公开号：EP1336602A1

  公开（公告）日：2003-08-20

  New pharmaceutical compounds of general formula (I): F-(X)q where q is an integer from 1 to 5, preferably 1; -F is chosen among drugs described in the text, -X is chosen among 4 groups -M, -T, -V and -Y as described in the text. The compounds of general formula (I) are nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without hypotensive side effects and for this reason they are useful for the preparation of medicines for prevention and treatment of inflammatory, ischemic, degenerative and proliferative diseases of musculoskeletal, tegumental, respiratory, gastrointestinal, genito-urinary and central nervous systems.

  通式（I）的新药物化合物：F-（X）q，其中q是1到5的整数，最好是1；-F是在文本中描述的药物中选择的，-X是在文本中描述的4个组-M，-T，-V和-Y中选择的。通式（I）的化合物是硝酸盐前药，可以在体内以受控和选择性的方式释放一氧化氮，而不会产生降压副作用，因此它们非常适用于制备用于预防和治疗肌肉骨骼，皮肤，呼吸，消化，泌尿和中枢神经系统的炎症，缺血，退行性和增生性疾病的药物。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Alpha1-adrenerg blockierende Theophyllinderivate
  申请人：SIEGFRIED AKTIENGESELLSCHAFT

  公开号：EP0229897A1

  公开（公告）日：1987-07-29

  Neue al-adrenerg blockierende Theophyllinderivate, zum Beispiel 7-(4-(4-(p-Fluorbenzoyl)piperidino)-butyltheophyllin, werden als blutdrucksenkende Arzneimittel beschrieben. Diese Stoffe können ausgehend von Theophyllin durch Alkylierung mit einem Dihalogenalkan und anschließender Umsetzung mit 4-(p-Fluorbenzoyl)piperidin synthetisiert werden.

  新的肾上腺素能阻断茶碱衍生物，例如 7-(4-(4-(对氟苯甲酰基)哌啶)-丁基茶碱，被描述为抗高血压药物。 这些物质可通过与二卤代烃烷基化，然后与 4-(对氟苯甲酰基)哌啶反应，从茶碱中合成。
• NOVEL COMPOUNDS AND METHODS FOR MODULATING UBIQUITINATION
  申请人：Johann Wolfgang Goethe-Universität Frankfurt am Main

  公开号：EP3299460A1

  公开（公告）日：2018-03-28

  The present invention pertains to the modification of the eukaryotic ubiquitin system by using the bacterial virulence factor SdeA and variants and mutants thereof. The invention is based on the phosphodiesterase activity of SdeA, which catalyzes a phospho-ribosylation (or simply "ribosylation") event of ubiquitin and ubiquitin-like proteins. The invention provides SdeA proteins and mutants without said phosphodiesterase activity, as well as medical applications of these recombinant proteins, their encoding nucleic acids, ribosylated ubiquitin proteins, and compounds which may act as selective or non-selective phosphodiesterase inhibitors.

  本发明涉及利用细菌毒力因子 SdeA 及其变体和突变体对真核生物泛素系统进行修饰。 本发明以 SdeA 的磷酸二酯酶活性为基础，SdeA 可催化泛素和泛素样蛋白的磷酸核糖化（或简称 "核糖化"）过程。 本发明提供了没有上述磷酸二酯酶活性的 SdeA 蛋白和突变体，以及这些重组蛋白、其编码核酸、核糖基化泛素蛋白和可作为选择性或非选择性磷酸二酯酶抑制剂的化合物的医学应用。