methyl (8S)-8-(bromomethyl)-2-methyl-4-(4-methylpiperazine-1-carbonyl)oxy-6-(5,6,7-trimethoxy-3a,7a-dihydro-1H-indole-2-carbonyl)-7,8-dihydro-3H-pyrrolo[3,2-e]indole-1-carboxylate

• 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: methyl (8S)-8-(bromomethyl)-2-methyl-4-(4-methylpiperazine-1-carbonyl)oxy-6-(5,6,7-trimethoxy-3a,7a-dihydro-1H-indole-2-carbonyl)-7,8-dihydro-3H-pyrrolo[3,2-e]indole-1-carboxylate
• 化学式: C₃₂H₃₈BrN₅O₈
• 分子量: 700.6
• InChiKey: GCOXYLIQHZXACO-WYVJCVMXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  46
• 可旋转键数：
  9
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  135
• 氢给体数：
  2
• 氢受体数：
  10

文献信息

• [EN] PYRAZOLO[3,4-B]PYRAZINE SHP2 PHOSPHATASE INHIBITORS<br/>[FR] INHIBITEURS DE PYRAZOLO[3,4-B]PYRAZINE SHP2 PHOSPHATASE
  申请人：OTSUKA PHARMA CO LTD

  公开号：WO2021033153A1

  公开（公告）日：2021-02-25

  The invention provides new pyrazine derivatives of formula (I): or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein. The invention also provides pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

  该发明提供了式(I)的新吡嗪衍生物：或其互变异构体或溶剂化物或药学上可接受的盐，其中取代基如本文所定义。该发明还提供了包括所述化合物的药物组合物，并且用于治疗疾病，例如癌症的所述化合物的用途。
• [EN] CONJUGATES OF AN ELECTRON-DONATING NITROGEN OR TERTIARY AMINE COMPRISING COMPOUNDS<br/>[FR] CONJUGUÉS D'AZOTE DONNEUR D'ÉLECTRONS OU DE COMPOSÉS COMPRENANT UNE AMINE TERTIAIRE
  申请人：ASCENDIS PHARMA AS

  公开号：WO2020254602A1

  公开（公告）日：2020-12-24

  The present invention relates to conjugates of an electron-donating heteroaromatic nitrogen or tertiary amine comprising drugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said conjugates and the use of said conjugates as medicaments.

  本发明涉及包含药物和其药用盐的电子给体杂环氮或三级胺的共轭物，包括含有该共轭物的药物组合物以及将该共轭物用作药物的用途。
• 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。
• Method of using a COX-2 inhibitor and an alkylating-type antineoplastic agent as a combination therapy in the treatment of neoplasia
  申请人：Pharmacia Corporation

  公开号：US20040072889A1

  公开（公告）日：2004-04-15

  The present invention provides compositions and methods to treat, prevent or inhibit a neoplasia or a neoplasia-related disorder in a mammal using a combination of a COX-2 inhibitor and an alkylating-type antineoplastic agent.

  本发明提供了一种使用COX-2抑制剂和烷基化类抗肿瘤药物的组合来治疗、预防或抑制哺乳动物中的肿瘤或与肿瘤相关的疾病的组合物和方法。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。