Pregna-4,9(11)-diene-3,20-dione, 6-fluoro-17,21-dihydroxy-16-methyl-, (6alpha,16alpha)- | 378-61-0

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: Pregna-4,9(11)-diene-3,20-dione, 6-fluoro-17,21-dihydroxy-16-methyl-, (6alpha,16alpha)-
• 英文别名: (6S,8S,10R,13S,14S,16R,17R)-6-fluoro-17-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-2,6,7,8,12,14,15,16-octahydro-1H-cyclopenta[a]phenanthren-3-one
• CAS: 378-61-0
• 化学式: C₂₂H₂₉FO₄
• 分子量: 376.5
• InChiKey: MUEOUHRWNRABSW-XUOSUNSOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  27
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.73
• 拓扑面积：
  74.6
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• CRYSTALLINE FORMS OF C21H22Cl2N4O2
  申请人：BIOMED VALLEY DISCOVERIES, INC.

  公开号：US20170320851A1

  公开（公告）日：2017-11-09

  The present invention provides crystalline forms of a compound of formula (I): Also provided are pharmaceutical compositions that include the provided crystalline forms and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.

  本发明提供了公式（I）化合物的晶体形式。还提供包含所提供晶体形式的药物组合物以及使用所提供的晶体形式和药物组合物治疗癌症的方法。
• CRYSTALLINE C21H22Cl2N4O2 MALONATE
  申请人：BIOMED VALLEY DISCOVERIES, INC.

  公开号：US20160221988A1

  公开（公告）日：2016-08-04

  The present invention provides a malonate salt of a compound of formula (I): which is a crystalline salt. Also provided are pharmaceutical compositions that include the provided malonate salt and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.

  本发明提供了公式（I）化合物的马隆酸盐，该盐为晶体盐。还提供了包含所提供的马隆酸盐的药物组合物以及使用所提供的晶体形式和药物组合物治疗癌症的方法。
• Crystalline forms of C21H22Cl2N4O2
  申请人：BIOMED VALLEY DISCOVERIES, INC.

  公开号：US10183927B2

  公开（公告）日：2019-01-22

  The present invention provides crystalline forms of a compound of formula (I): Also provided are pharmaceutical compositions that include the provided crystalline forms and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.

  本发明提供了式 (I) 化合物的结晶形式： 还提供了包括所提供晶体形式的药物组合物，以及使用所提供晶体形式和药物组合物治疗癌症的方法。
• C. novyi for the treatment of solid tumors in humans
  申请人：BIOMED VALLEY DISCOVERIES, INC.

  公开号：US10617723B2

  公开（公告）日：2020-04-14

  The present invention provides, inter alia, methods for treating or ameliorating an effect of a solid tumor present in a human. These methods include administering intratumorally to the human a unit dose of C. novyi, preferably C. novyi NT, colony forming units (CFUs), which contains about 1×103-1×107 CFUs suspended in a pharmaceutically acceptable carrier or solution. Methods for debulking a solid tumor present in a human, methods for ablating a solid tumor present in a human, a method for microscopically precise excision of tumor cells in a human, methods for treating or ameliorating an effect of a solid tumor that has metastasized to one or more sites in a human, unit doses of C. novyi, preferably C. novyi NT, CFUs, and kits for treating or ameliorating an effect of a solid tumor present in a human are also provided.

  本发明特别提供了治疗或改善人体内实体瘤影响的方法。这些方法包括向人体瘤内注射单位剂量的C. novyi，最好是C. novyi NT，菌落形成单位（CFUs），其中包含悬浮在药学上可接受的载体或溶液中的约1×103-1×107 CFUs。此外，还提供了用于清除人体内存在的实体瘤的方法、消融人体内存在的实体瘤的方法、在显微镜下精确切除人体内肿瘤细胞的方法、治疗或改善转移到人体内一个或多个部位的实体瘤的效果的方法、单位剂量的C.
• Combination therapies targeting tumor-associated stroma or tumor cells
  申请人：BIOMED VALLEY DISCOVERIES, INC.

  公开号：US11033621B2

  公开（公告）日：2021-06-15

  The present invention provides, inter alia, methods for treating or ameliorating the effects of a disease, such as cancer, in a subject. The methods include: administering to a subject in need thereof (a) a therapeutically effective amount of an agent selected from the group consisting of an anti-angiogenic agent, a vascular disrupting agent (VDA), and combinations thereof; and (b) a therapeutically effective amount of a monoclonal antibody or antigen binding fragment thereof, wherein the monoclonal antibody contains: (i) a heavy chain variable region (VH), which includes an amino acid sequence selected from SEQ ID NO:1, SEQ ID NO:3, SEQ ID NO:5, and SEQ ID NO:7; and (ii) a light chain variable region (VL), which includes an amino acid sequence selected from SEQ ID NO:2, SEQ ID NO:4, SEQ ID NO:6, and SEQ ID NO:8. Compositions, including pharmaceutical compositions, and kits for treating diseases, such as cancer, are also provided.

  本发明除其他外，提供了用于治疗或改善疾病（如癌症）对受试者的影响的方法。这些方法包括：向有需要的受试者施用(a)治疗有效量的药剂，该药剂选自由抗血管生成剂、血管破坏剂（VDA）及其组合组成的组；和(b)治疗有效量的单克隆抗体或其抗原结合片段，其中单克隆抗体包含：(i) 重链可变区（VH），其包括选自 SEQ ID NO:1、SEQ ID NO:3、SEQ ID NO:5 和 SEQ ID NO:7 的氨基酸序列；以及 (ii) 轻链可变区（VL），其包括选自 SEQ ID NO:2、SEQ ID NO:4、SEQ ID NO:6 和 SEQ ID NO:8 的氨基酸序列。还提供了用于治疗癌症等疾病的组合物（包括药物组合物）和试剂盒。