2-diphenylphosphoryl-N-ethyl-4-methylbenzamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-diphenylphosphoryl-N-ethyl-4-methylbenzamide
• 化学式: C₂₂H₂₂NO₂P
• 分子量: 363.4
• InChiKey: XNQDRGRKJFGPCJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  46.2
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• CELL PROLIFERATION INHIBITORS AND CONJUGATES THEREOF
  申请人：Barsanti Paul A.

  公开号：US20140322247A1

  公开（公告）日：2014-10-30

  Disclosed herein are immunoconjugates comprising an inhibitor of Eg5 linked to an antigen binding moiety such as an antibody, that are useful for treating cell proliferative disorders. Also disclosed are novel inhibitors of Eg5 that can be used either alone or as part of an immunoconjugate to treat cell proliferation disorders. The Eg5 inhibitors include compounds of this formula as described herein: The invention further provides pharmaceutical compositions comprising these compounds and immunoconjugates, and compositions comprising the immunoconjugates or compounds with a therapeutic co-agent, and methods to use these compounds, conjugates and compositions for treating cell proliferation disorders.

  本文披露了一种包含Eg5抑制剂和抗原结合部分（如抗体）的免疫结合物，用于治疗细胞增殖性疾病。还披露了新型的Eg5抑制剂，可单独使用或作为免疫结合物的一部分用于治疗细胞增殖性疾病。Eg5抑制剂包括本文所述的这种化合物：进一步提供了包含这些化合物和免疫结合物的药物组合物，以及包含免疫结合物或化合物与治疗协同剂的组合物，以及使用这些化合物、结合物和组合物治疗细胞增殖性疾病的方法。
• TUBULYSIN COMPOUNDS AND CONJUGATES THEREOF
  申请人：Mersana Therapeutics, Inc.

  公开号：US20160022829A1

  公开（公告）日：2016-01-28

  A tubulysin compound conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -L D -D, the protein based recognition-molecule being connected to the polymeric carrier by L P . Each occurrence of D is independently a tubulysin compound having a molecular weight≦5 kDa. L D and L P are distinct linkers connecting the tubulysin compound and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-tubulysin compound-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

  本文提供了一种管芽菌素化合物结合物。该结合物包括一种基于蛋白质的识别分子（PBRM）和一种聚合物载体，该聚合物载体被取代了一个或多个-LD-D，其中，基于蛋白质的识别分子通过LP连接到聚合物载体上。每个D的出现独立地是分子量≦5 kDa的管芽菌素化合物。LD和LP是连接管芽菌素化合物和PBRM分别到聚合物载体的不同连接物。还公开了用于与PBRM结合形成聚合物-管芽菌素化合物-PBRM结合物的聚合物支架，包括结合物的组合物，其制备方法以及使用结合物或其组合物治疗各种疾病的方法。
• HYDROXYL-POLYMER-DRUG-PROTEIN CONJUGATES
  申请人：MERSANA THERAPEUTICS, INC.

  公开号：US20150306240A1

  公开（公告）日：2015-10-29

  A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric scaffold having one or more -L D -D, the PBRM being connected to the polymeric scaffold by L p , wherein the polymeric scaffold comprises a linear, branched or cyclic polymer having four or more —OH groups. Each occurrence of D is independently a therapeutic agent having a molecular weight <5 kDa. L D and L p are linkers connecting the therapeutic agent and PBRM to the polymeric scaffold respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

  本文提供了一种药物结合物。该结合物包括一种基于蛋白质的识别分子（PBRM）和一个具有一个或多个-LD-D的聚合物支架，其中PBRM通过Lp连接到聚合物支架上，聚合物支架包括具有四个或更多—OH基团的线性、分支或环状聚合物。每个D的出现都是独立的，具有分子量<5 kDa的治疗剂。LD和Lp是连接治疗剂和PBRM到聚合物支架的连接剂。还公开了用于与PBRM结合形成聚合物-药物-PBRM结合物的聚合物支架，包括结合物的组成，其制备方法以及使用结合物或其组成物治疗各种疾病的方法。
• PROTEIN-POLYMER-DRUG CONJUGATES
  申请人：Mersana Therapeutics, Inc.

  公开号：US20160067353A1

  公开（公告）日：2016-03-10

  A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -L D -D, the protein based recognition-molecule being connected to the polymeric carrier by L P . Each occurrence of D is independently a therapeutic agent having a molecular weight ≦5 kDa. L D and L P are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

  本文提供了一种药物偶联物。该偶联物包括基于蛋白质的识别分子（PBRM）和多聚载体，该多聚载体被取代了一个或多个-LD-D，基于蛋白质的识别分子通过LP与多聚载体连接。每个D的出现都是具有分子量≦5 kDa的治疗剂。LD和LP是将治疗剂和PBRM分别连接到多聚载体的连接剂。还揭示了用于与PBRM共轭形成聚合物-药物-PBRM偶联物的多聚支架，包括偶联物的组成，制备它们的方法以及使用偶联物或其组成治疗各种疾病的方法。
• CYTOTOXIC PEPTIDES AND CONJUGATES THEREOF
  申请人：Novartis AG

  公开号：EP3753578A1

  公开（公告）日：2020-12-23

  Disclosed herein are novel cytotoxic peptides of formula (I) as described herein: and the use of such peptides in making immunoconjugates (i.e Antibody Drug Conjugates) Also described herein are immunoconjugates (i.e Antibody Drug Conjugates) comprising such novel cytotoxic peptide linked to an antigen binding moiety, such as an antibody; where such immunoconjugates are useful for treating cell proliferative disorders. The invention further provides pharmaceutical compositions comprising these immunoconjugates, compositions comprising the immunoconjugates with a therapeutic co-agent, and methods to use these immunoconjugates and compositions for treating cell proliferation disorders.

  本文公开了如本文所述的式 (I) 的新型细胞毒性肽： 以及使用这种肽制造免疫结合剂（即抗体药物结合剂）的方法 本发明还描述了免疫结合剂（即抗体药物结合剂），其包含与抗原结合分子（如抗体）连接的这种新型细胞毒性肽；其中这种免疫结合剂可用于治疗细胞增殖性疾病。本发明进一步提供了包含这些免疫共轭物的药物组合物、包含这些免疫共轭物与治疗共用试剂的组合物，以及使用这些免疫共轭物和组合物治疗细胞增殖障碍的方法。