噁丙烯并[f]异喹啉(9CI) | 72238-04-1

• 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
• 中文名称: 噁丙烯并[f]异喹啉(9CI)
• 中文别名: 1-((3-(二乙基氨基)丙基)氨基)-5-甲基-6H-吡啶并(4,3-b)咔唑-9-醇
• 英文名称: 1-<<3-(diethylamino)propyl>amino>-9-hydroxy-5-methyl-6H-pyrido<4,3-b>carbazole
• 英文别名: 1-(3-diethylamino-propylamino)-5-methyl-6H-pyrido[4,3-b]carbazol-9-ol；6H-Pyrido(4,3-b)carbazol-9-ol, 1-((3-(diethylamino)propyl)amino)-5-methyl-；1-[3-(diethylamino)propylamino]-5-methyl-6H-pyrido[4,3-b]carbazol-9-ol
• CAS: 72238-04-1
• 化学式: C₂₃H₂₈N₄O
• 分子量: 376.502
• InChiKey: JOTXWZGCPJPKOO-UHFFFAOYSA-N

物化性质

• 沸点：
  641.8±55.0 °C(Predicted)
• 密度：
  1.239±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  28
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  64.2
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  1-chloro-9-(benzoyloxy)-5-methyl-5H-pyrido<4,3-b>carbazole 生成 噁丙烯并[f]异喹啉(9CI)
  参考文献：
  名称：

  RIVALLE, C.;WENDLING, F.;TAMBOURIN, P.;LHOSTE, J. -M.;BISAGNI, E.;CHERMAN+, J. MED. CHEM., 1983, 26, N 2, 181-185

  摘要：

  DOI：

文献信息

• Antitumor amino-substituted pyrido[3',4':4,5]pyrrolo[2,3-g]isoquinolines and pyrido[4,3-b]carbazole derivatives: synthesis and evaluation of compounds resulting from new side chain and heterocycle modifications
  作者：Christian Rivalle、Francoise Wendling、Pierre Tambourin、Jean Marc Lhoste、Emile Bisagni、Jean Claude Chermann

  DOI：10.1021/jm00356a012

  日期：1983.2

  11-dimethyl-6H-pyrido[4,3-b]carba zole (4b), which display important antitumor properties, were performed either on the side chain or on the intercalating heterocycle. Side chains were introduced by direct substitution of the corresponding chloro derivatives and 6-N-methyl-9-hydroxypyrido[4,3-b]carbazoles analogues were prepared via 9-O-benzoyl-1-chloroellipticines. Evaluation of all new compounds shows no significant

  10-[[[3-（二乙基氨基）丙基]氨基] -6-甲基-5H-吡啶基[3'，4'：4,5]吡咯并[2,3-g] i异喹啉（1b）和1的新修饰对[[[3-（二乙基氨基）丙基]氨基] -9-甲氧基-5,11-二甲基-6H-吡啶基[4,3-b]卡巴唑（4b）进行了重要的抗肿瘤研究，侧链或插入杂环上。通过直接取代相应的氯衍生物引入侧链，并通过9-O-苯甲酰基-1-氯玫瑰树碱制备6-N-甲基-9-羟基吡啶并[4,3-b]咔唑类似物。与模型化合物1b和4b相比，对所有新化合物的评估均显示L1210白血病系统的体外细胞毒性和ILS百分比没有显着增加。
• Use of indole-derived compounds for the preparation of a medicament that can be used to treat diseases related to the splicing process
  申请人：Tazi Jamal

  公开号：US20070054905A1

  公开（公告）日：2007-03-08

  The invention relates to indole-derived compounds and to the use of said compounds for the preparation of a medicament that can be used to treat diseases related to the process of splicing pre-messenger RNAs in the cell, such as Frasier syndrome, frontotemporal dementia linked to chromonsoem 17 (a form of Parkinson's disease), Leigh syndrome (a type of encephalopathy), atypical cystic fibrosis, certain neuropathologies including Alzheimer's disease linked to a mutation in the Tau protein, muscle atorphy which affects the SMN (survival of Motor Neuron) gene, depression linked to a serotonin splicing impairment, and certain cancers in which the global splicing process is affected (e.g. breast cancer, colon cancer and certain lymphomas), as well as viral diseases such as AIDS.

  该发明涉及吲哚衍生物化合物及其用于制备药物的用途，该药物可用于治疗与细胞内预信使RNA剪接过程相关的疾病，如弗雷泽综合征、与染色体17相关的额颞叶痴呆症（一种帕金森病形式）、利综合征（一种脑病类型）、非典型囊性纤维化、某些神经病理学疾病，包括与Tau蛋白突变相关的阿尔茨海默病、影响SMN（运动神经元存活）基因的肌肉萎缩、与血清素剪接障碍相关的抑郁症，以及全局剪接过程受影响的某些癌症（例如乳腺癌、结肠癌和某些淋巴瘤），以及病毒性疾病，如艾滋病。
• NOVEL COMPOUNDS DERIVED FROM INDOLE AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
  申请人：Lejeune Fabrice

  公开号：US20110003843A1

  公开（公告）日：2011-01-06

  The present invention relates to a compound derived from indole corresponding to the following formula II: wherein X represents N, CR8 or N + R8, wherein R8 represents a hydrogen atom, a hydroxyl or alkyl or methoxy group optionally substituted with a phenyl group; R2, R3 and R4 independently represent a hydrogen atom or a halogen atom or an optionally substituted alkyl, amine, alkene, ester, sulfonamide, ether or benzyl group; R5 represents a hydrogen atom or an optionally substituted, saturated or unsaturated alkyl group, amine, benzyl group; R6 represents an optionally substituted C1-C3 alkyl group; R7 represents a hydrogen atom or an optionally substituted C1-C3 alkyl group and R7 is absent when the ring A is in the b position, and A represents a ring; R9 and R10 represent together a carbon bond or independently represent an R11 OR11, SR11 group; wherein R11 represents a hydrogen atom, an optionally substituted, saturated or unsaturated, C1-C3 alkyl group, which may contain one or more sulfur, oxygen or nitrogen atoms; pharmaceutically acceptable salts of said compounds, their isomers and/or a mixture thereof; pharmaceutical composition comprising such a compound; the use of such a compound for preparing a drug intended to treat a genetic disease resulting from at least one mutation causing the occurrence of an early termination codon.

  本发明涉及一种从吲哚衍生的化合物，对应于以下公式II： 其中，X表示N，CR8或N+R8，其中R8表示氢原子，羟基或烷基或甲氧基，可选地取代为苯基；R2、R3和R4分别表示氢原子或卤素原子或可选地取代的烷基、胺基、烯烃、酯、磺酰胺、醚或苄基；R5表示氢原子或可选地取代的饱和或不饱和烷基、胺基、苄基；R6表示可选地取代的C1-C3烷基；R7表示氢原子或可选地取代的C1-C3烷基，当环A在b位置时，R7不存在；A表示一个环；R9和R10共同表示碳键，或分别表示R11 OR11、SR11基团；其中，R11表示氢原子、可选地取代的饱和或不饱和的C1-C3烷基，可以含有一个或多个硫、氧或氮原子；该化合物的药学可接受盐、其异构体和/或混合物；包括这种化合物的药物组合物；使用这种化合物制备用于治疗由至少一个突变引起的早期终止密码子出现的遗传疾病的药物。
• DERIVES D'INDOLE POUR LE TRAITEMENT DE MALADIES LIEES AU PROCESSUS D'EPISSAGE
  申请人：CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)

  公开号：EP1663219B1

  公开（公告）日：2010-05-12
• NOUVEAUX COMPOSÉS DÉRIVÉS D'INDOLE ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
  申请人：Centre National de la Recherche Scientifique (CNRS)

  公开号：EP2121685B1

  公开（公告）日：2016-02-17