(3S,6R,12aR)-2,3,6,7,12,12a-hexahydro-2,3-dimethyl-6-(3,4-methylenedioxyphenyl)-pyrazino[2',1':6,1]pyrido[3,4-b]indole-1,4-dione | 171596-40-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: (3S,6R,12aR)-2,3,6,7,12,12a-hexahydro-2,3-dimethyl-6-(3,4-methylenedioxyphenyl)-pyrazino[2',1':6,1]pyrido[3,4-b]indole-1,4-dione
• 英文别名: (3S,6R,12aR)-2,3,6,7,12,12a-hexahydro-2,3-dimethyl-6-(3,4-methylenedioxyphenyl)-pyrazino[2',1':6,1]pyrido[3,4-b]indol-1,4-dione；(2R,5S,8R)-2-(1,3-benzodioxol-5-yl)-5,6-dimethyl-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dione
• CAS: 171596-40-0
• 化学式: C₂₃H₂₁N₃O₄
• 分子量: 403.437
• InChiKey: XZCSUPWHWMDLEC-LKNMKHRSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  30
• 可旋转键数：
  1
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  74.9
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Methods for prevention and treatment of gastrointestinal disorders
  申请人：——

  公开号：US20020128171A1

  公开（公告）日：2002-09-12

  Disclosed are methods for preventing or treating a gastrointestinal (GI) disorder in a mammal such as a human patient. In one embodiment, the methods include administering to the mammal a therapeutically effective amount of a compound that modulates a nitric oxide (NO) signaling pathway, particularly in GI neurons. Methods of the invention are particularly useful for the treatment (including prophylactic treatment) of diabetic gastropathies and other GI disorders.

  本发明涉及一种预防或治疗哺乳动物（例如人类患者）胃肠道（GI）疾病的方法。在一种实施例中，该方法包括向哺乳动物（特别是GI神经元）中投与治疗效果的化合物，该化合物调节一氧化氮（NO）信号通路的数量。本发明的方法对于治疗（包括预防性治疗）糖尿病性胃病和其他GI疾病特别有用。
• PYRROLIDINE DERIVATIVES AS PROSTAGLANDIN MODULATORS
  申请人：LIAO Yihua

  公开号：US20080114051A1

  公开（公告）日：2008-05-15

  Substituted pyrrolidine compounds are provided, and methods of treatment and pharmaceutical composition that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteoporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin family of compounds. In a preferred aspect, a substituted pyrrolidine compound is administered to a subject in coordination with a phosphodiesterase inhibitor compound.

  本发明提供了取代吡咯烷化合物，以及利用或包含一种或多种这样的化合物的治疗方法和制药组合物。本发明的化合物可用于各种疗法，包括治疗或预防早产、痛经、哮喘、高血压、不孕症或生育障碍、不良血凝、妊娠高血压综合症或子痫前期、嗜酸性粒细胞异常、性功能障碍、骨质疏松症和其他破坏性骨疾病或障碍，以及与前列腺素家族化合物相关的其他疾病和障碍。在首选方面，取代吡咯烷化合物与磷酸二酯酶抑制剂化合物协同给予给受试者。
• COMPOSITION AND USE FOR PHOSPHODIESTERASE INHIBITORS
  申请人：Chervinsky Alex

  公开号：US20120157467A1

  公开（公告）日：2012-06-21

  Compositions and methods for enhancing the aesthetic appearance of the lip or lips of a human achieved by applying to the surface of the lip a composition containing a phosphodiesterase inhibitor, preferably a pyrazolopyrimidinone such as sildenafil or its citrate salt.

  本发明提供了一种用于增强人类唇部或唇部的美观外观的组合物和方法，其通过将含有磷酸二酯酶抑制剂的组合物（最好是吡唑啉并嘧啶酮，例如西地那非或其柠檬酸盐）涂抹于唇部表面来实现。
• Pharmaceutical compositions for treating nitrate-induced tolerance
  申请人：Pfizer Limited

  公开号：EP1022026A2

  公开（公告）日：2000-07-26

  The present invention relates to methods for treating nitrate-induced tolerance in a mammal by administering a nitrate-induced tolerance treating amount of a compound of formulae (I), (II), (III) (IV), (V), (VI), (VII), (VIII), (IX), (XA) or (XB) as defined herein, or the pharmaceutically acceptable salts, prodrugs, polymorphs, hydrates, solvates, active metabolites or stereoisomers thereof. The invention also relates to pharmaceutical compositions for the treatment of nitrate-induced tolerance in a mammal comprising a nitrate-induced tolerance treating amount of a compound of formulae (I), (II), (III) (lV), (V), (VI), (VII), (VIII), (IX), (XA) or (XB) as defined herein, or the pharmaceutically acceptable salts, prodrugs, polymorphs, hydrates, solvates, active metabolites or stereoisomers thereof, and a pharmaceutically acceptable vehicle, diluent or carrier. The invention further relates to methods of preventing nitrate-induced tolerance in a mammal comprising administering a nitrate-induced tolerance preventing amount of a cGMP PDE inhibitor.

  本发明涉及通过施用本文定义的式(I)、(II)、(III)(IV)、(V)、(VI)、(VII)、(VIII)、(IX)、(XA)或(XB)化合物或其药学上可接受的盐、原药、多晶型物、水合物、溶解物、活性代谢物或立体异构体的硝酸盐诱导的耐受性治疗量来治疗哺乳动物的硝酸盐诱导的耐受性的方法。本发明还涉及用于治疗哺乳动物硝酸盐诱导耐受性的药物组合物，其包含硝酸盐诱导耐受性治疗量的式(I)、(II)、(III)(lV)、(V)、(VI)、(VII)、(VIII)、(IX)、(XA)或(XB)，或其药学上可接受的盐、原药、多晶型物、水合物、溶解物、活性代谢物或立体异构体，以及药学上可接受的载体、稀释剂或载体。本发明还涉及防止哺乳动物产生硝酸盐耐受性的方法，包括施用一定量的 cGMP PDE 抑制剂，以防止产生硝酸盐耐受性。
• TABLETS IMMEDIATELY DISINTEGRATING IN THE ORAL CAVITY
  申请人：Eisai Co., Ltd.

  公开号：EP1120120A1

  公开（公告）日：2001-08-01

  The present invention provides an intraoral quickly disintegrating tablet containing a phosphodiesterase inhibitor having an effect of improving the erectile dysfunction and a method for manufacturing the tablet. The present invention also provides an intraoral quickly disintegrating tablet containing a slightly soluble pharmaceutical agent having an improved solubility and a method for manufacturing the tablet. That is, it is an intraoral quickly disintegrating tablet containing a cyclic GMP phosphodiesterase inhibitor and a saccharide, and a method for manufacturing the tablet. Further, it is a method for manufacturing an intraoral quickly disintegrating tablet, which comprises dissolving a slightly soluble pharmaceutical agent in an organic solvent or an aqueous organic solvent together with a surfactant and/or a water-soluble polymer, coating the solution on a filler or granulating it with a filler to obtain molded products, mixing a saccharide with them, adding an organic solvent, water or an aqueous organic solvent thereto, followed by kneading, and subjecting it to a compression-molding.

  本发明提供了一种含有具有改善勃起功能障碍效果的磷酸二酯酶抑制剂的口腔内快速崩解片剂以及该片剂的制造方法。本发明还提供了一种含有具有改善溶解度的微溶性药剂的口腔内快速崩解片剂及其制造方法。也就是说，本发明是一种含有环 GMP 磷酸二酯酶抑制剂和糖类的口腔内快速崩解片剂，以及该片剂的制造方法。此外，这是一种口腔内快速崩解片剂的制造方法，包括将微溶性药剂与表面活性剂和/或水溶性聚合物一起溶解在有机溶剂或水性有机溶剂中，将溶液涂覆在填料上或与填料一起制粒以获得模制产品，将糖类与它们混合，向其中添加有机溶剂、水或水性有机溶剂，然后进行捏合，并进行压缩成型。