[(19S)-10,19-diethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaen-7-yl] 4-piperidin-1-ylpiperidine-1-carboxylate;5-fluoro-1H-pyrimidine-2,4-dione

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 喜树碱
• 英文名称: [(19S)-10,19-diethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaen-7-yl] 4-piperidin-1-ylpiperidine-1-carboxylate;5-fluoro-1H-pyrimidine-2,4-dione
• 化学式: C37H41FN6O8
• 分子量: 716.8
• InChiKey: OVNCRSSUMDRBAF-WAQYZQTGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.29
• 重原子数：
  52
• 可旋转键数：
  5
• 环数：
  8.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  171
• 氢给体数：
  3
• 氢受体数：
  11

文献信息

• Intrathecal and intratumoral superantigens to treat malignant disease
  申请人：TERMAN, David S.

  公开号：EP2386312A2

  公开（公告）日：2011-11-16

  The presence of tumor nodules in organs often results in serious clinical manifestations and the permeation by cancer cells of sheaths surrounding organs often produces clinical manifestations of pleural effusion, ascites or cerebral edema. The present invention addresses this problem by providing a method for treating tumors comprising (a) intratumoral administration of a superantigen and/or (b) intrathecal or intracavitary administration of a superantigen directly into the sheath. Intratumoral superantigen results in significant and sustained reduction of the tumor size. Intrathecal administration produces significant sustained reduction of the fluid accumulation associated with clinical improvement and prolonged survival.; Useful superantigen compositions for intrathecal and intratumoral injection include tumoricidally effective homologues, fragments and fusion proteins of native superantigens. Also disclosed is combined therapy that includes intratumoral or intrathecal superantigen compositions in combination with (i) intratumoral low, non-toxic doses of one or more chemotherapeutic drugs or (ii) systemic chemotherapy at reduced and non-toxic doses of chemotherapeutic drugs.

  器官中出现肿瘤结节往往会导致严重的临床表现，而癌细胞对器官周围鞘的渗透往往会产生胸腔积液、腹水或脑水肿等临床表现。本发明通过提供一种治疗肿瘤的方法解决了这一问题，该方法包括(a)瘤内超抗原给药和/或(b)鞘内或腔内超抗原直接给药。瘤内超抗原可显著、持续地缩小肿瘤体积。用于鞘内和瘤内注射的有用超抗原组合物包括对肿瘤有效的原生超抗原的同源物、片段和融合蛋白。还公开了联合疗法，包括瘤内或鞘内超抗原组合物与(i)瘤内低无毒剂量的一种或多种化疗药物或(ii)降低化疗药物无毒剂量的全身化疗联合使用。
• Mesoporous silica nanoparticles with a lipid bilayer coating for cargo delivery
  申请人：The Regents of the University of California

  公开号：US10765636B2

  公开（公告）日：2020-09-08

  A nanocarrier including a silica body having a surface and defining a plurality of pores that are suitable to receive molecules therein is described. The nanocarrier also includes a lipid bilayer coating the surface, and a cargo-trapping agent within the phospholipid bilayer. The phospholipid bilayer stably seals the plurality of pores. The cargo-trapping reagent can be selected to interact with a desired cargo, such as a drug.

  本文描述了一种纳米载体，它包括一个具有表面的硅体，硅体上有多个适合接收分子的孔隙。该纳米载体还包括包裹表面的磷脂双分子层和磷脂双分子层内的货物捕获剂。磷脂双分子层可稳定地密封多个孔。货物捕获试剂可以选择与所需货物（如药物）相互作用。
• INTRATHECAL AND INTRATUMORAL SUPERANTIGENS TO TREAT MALIGNANT DISEASE
  申请人：TERMAN, David S.

  公开号：EP1534312A2

  公开（公告）日：2005-06-01
• Staphylococcal superantigens for combination treatment of lung tumors
  申请人：Terman, David S.

  公开号：EP1534312B1

  公开（公告）日：2012-08-15
• EP1534312A4
  申请人：——

  公开号：EP1534312A4

  公开（公告）日：2007-02-28