cis-2,3,6,7,12,12a-hexahydro-6-(2,3-dihydrobenzo[b]furan-5-yl)-2-methyl-pyrazino[2',1':6,1]pyrido[3,4-b]indole-1,4-dione

• 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: cis-2,3,6,7,12,12a-hexahydro-6-(2,3-dihydrobenzo[b]furan-5-yl)-2-methyl-pyrazino[2',1':6,1]pyrido[3,4-b]indole-1,4-dione
• 英文别名: cis-2,3,6,7,12,12-hexahydro-6-(2,3-dihydrobenzo[b]furan-5-yl)-2-methyl-pyrazino[2',1':6,1]pyrido[3,4-b]indole-1,4-dione；6-(2,3-Dihydro-benzofuran-5-yl)-2-methyl-2,3,6,7,12,12a-hexahydro pyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione；2-(2,3-dihydro-1-benzofuran-5-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dione
• 化学式: C₂₃H₂₁N₃O₃
• 分子量: 387.438
• InChiKey: GLNOKAPGTIWNRI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  29
• 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：
  65.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  cis-2,3,6,7,12,12a-hexahydro-6-(2,3-dihydrobenzo[b]furan-5-yl)-2-methyl-pyrazino[2',1':6,1]pyrido[3,4-b]indole-1,4-dione 在 盐酸 、 N,N-二异丙基乙胺 、 bromo-tris(1-pyrrolidinyl)phosphonium hexafluorophosphate 作用下， 以 四氢呋喃 、 N,N-二甲基甲酰胺 为溶剂， 以1%的产率得到11-(2,3-Dihydro-benzofuran-5-yl)-3-methyl-2,3,4a,11-tetrahydro-10H-3 10,11a-triaza-benzo[b]fluorene-1,4,5-trione
  参考文献：
  名称：

  US2003/144268

  摘要：

  公开号：

文献信息

• Methods and compositions for nucleic acid delivery
  申请人：Johns Hopkins University

  公开号：US20020094326A1

  公开（公告）日：2002-07-18

  The present provides methods and compositions that enable effective delivery of nucleic acids to desired cells, including to a solid organ such as a mammalian heart. The methods and compositions enable effective gene transfer and subsequent expression to a majority of cells throughout a solid organ such as the heart. Methods and compositions of the invention preferably provide enhanced vascular permeability that enables increased gene transfer to targeted cells, but without significant degradation or injury to endothelial cell layers.

  本文提供了一种方法和组合物，可以有效地将核酸传递到所需的细胞，包括哺乳动物心脏等固体器官。这些方法和组合物可以实现有效的基因转移，并随后在固体器官（如心脏）的大多数细胞中表达。本发明的方法和组合物最好提供增强的血管通透性，从而使基因转移到靶向细胞的数量增加，但不会对内皮细胞层造成显著的降解或损伤。
• 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。
• Tetracyclic derivatives, process of preparation and use
  申请人：ICOS Corporation

  公开号：US20020119976A1

  公开（公告）日：2002-08-29

  A compound of formula (I) 1 and salts and solvates thereof, in which: R o represents hydrogen, halogen or C 1-6 alkyl; R 1 represents hydrogen, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, halo C 1-6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl C 1-3 alkyl, arylC 1-3 alkyl or heteroaryl C 1-3 alkyl; R 2 represents an optionally substituted monocyclic aromatic ring selected from benzene, thiophene, furan and pyridine or an optionally substituted bicyclic ring 2 attached to the rest of the molecule via one of the benzene ring carbon atoms and wherein the fused ring A is a 5- or 6-membered ring which may be saturated or partially or fully unsaturated and comprises carbon atoms and optionally one or two heteroatoms selected from oxygen, sulphur and nitrogen; and R 3 represents hydrogen or C 1-3 alkyl, or R 1 and R 3 together represent a 3- or 4-membered alkyl or alkenyl chain. A compound of formula (I) is a potent and'selective inhibitor of cyclic guanosine 3′, 5′-monophosphate specific phosphodiesterase (CGMP specific PDE) having a utility in a variety of therapeutic areas where such inhibition is beneficial, including the treatment of cardiovascular disorders.

  式(I)1的化合物及其盐和溶剂化物，其中：R代表氢，卤素或C1-6烷基；R1代表氢，C1-6烷基，C2-6烯基，C2-6炔基，卤代C1-6烷基，C3-8环烷基，C3-8环烷基C1-3烷基，芳基C1-3烷基或杂环芳基C1-3烷基；R2代表一个可选的取代的单环芳香环，选择自苯，噻吩，呋喃和吡啶或一个可选的取代的二环2，通过苯环碳原子之一连接到分子的其余部分，其中融合的环A是一个5-或6-成员环，可以是饱和的或部分或完全不饱和的，并包括碳原子和可选的一个或两个异原子，选择自氧，硫和氮；R3代表氢或C1-3烷基，或R1和R3一起代表一个3-或4-成员烷基或烯基链。式(I)的化合物是环鸟苷3'，5'-单磷酸特异性磷酸二酯酶（CGMP特异性PDE）的有效和选择性抑制剂，具有在多种治疗领域中抑制有益的功效，包括心血管疾病的治疗。
• Method of inhibiting neoplastic cells with tetracyclic pyrido[3,4-B] indole derivatives
  申请人：——

  公开号：US20020035111A1

  公开（公告）日：2002-03-21

  A method for inhibiting neoplasia, particularly cancerous and precancerous lesions by exposing the affected cells to pyrido[3,4b]indoles.

  一种通过将受影响的细胞暴露于吡啶并［3,4b］吲哚来抑制肿瘤，特别是癌症和癌前病变的方法。
• Pyrrolidine derivatives as prostaglandin modulators
  申请人：Liao Yihua

  公开号：US20050176800A1

  公开（公告）日：2005-08-11

  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, osteporosis 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.

  本发明提供了替代吡咯烷化合物，并提供了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多种疗法，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、先兆子痫或子痫前期、嗜酸性粒细胞异常、性功能障碍、骨质疏松和其他破坏性骨疾病或疾病，以及与前列腺素家族化合物相关的其他疾病和疾病。在优选方面，替代吡咯烷化合物与磷酸二酯酶抑制剂化合物协同给予病人。