N-[(2R)-2-[(2S,3R)-2,3-bis(4-chlorophenyl)-5-oxomorpholin-4-yl]pentyl]-2-hydroxyacetamide

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: N-[(2R)-2-[(2S,3R)-2,3-bis(4-chlorophenyl)-5-oxomorpholin-4-yl]pentyl]-2-hydroxyacetamide
• 化学式: C₂₃H₂₆Cl₂N₂O₄
• 分子量: 465.4
• InChiKey: JWSQLILIBDUKBO-PTUXOGIPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  31
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  78.9
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• [EN] SPIRO[CYCLOBUTANE-1,3'-INDOLIN]-2'-ONE DERIVATIVES AS BROMODOMAIN INHIBITORS<br/>[FR] DÉRIVÉS SPIRO[CYCLOBUTANE-1,3'-INDOLIN]-2'-ONES EN TANT QU'INHIBITEURS DE BROMODOMAINE
  申请人：ORION CORP

  公开号：WO2015092118A1

  公开（公告）日：2015-06-25

  The present invention provides novel spiro[cyclobutane-1,3'-indolin]-2'- derivatives of formula (I) in which Cy, R1, R2, L and 'm' are have the meaning given in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful as bromodomain inhibitors in the treatment or prevention of diseases or disorders where bromodomain inhibition is desired.

  本发明提供了式(I)的新颖的螺[环丁烷-1,3'-吲哚]-2'-衍生物，其中Cy、R1、R2、L和'm'的含义如规范中所述，并且其药学上可接受的盐。式(I)的化合物在治疗或预防需要溴结构域抑制的疾病或紊乱中作为溴结构域抑制剂是有用的。
• [EN] BICYCLIC HETEROCYCLIC DERIVATIVES AS BROMODOMAIN INHIBITORS<br/>[FR] DÉRIVÉS BICYCLIQUES HÉTÉROCYCLIQUES COMME INHIBITEURS DE BROMODOMAINES
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2015104653A1

  公开（公告）日：2015-07-16

  The present invention provides bicyclic heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as bromodomain inhibitors; (I), in which R1, R2, R3, R4, L1, L2, Cy1, Cy2, X, n and dotted line are have the same meaning given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder associated as bromodomain inhibitors. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of bicyclic heterocyclic derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明提供了公式（I）的双环杂环衍生物，可能在治疗上有用，更具体地作为溴结构域抑制剂；其中R1、R2、R3、R4、L1、L2、Cy1、Cy2、X、n和虚线在说明书中具有相同的含义，并且其药学上可接受的盐或药学上可接受的立体异构体在治疗和预防疾病或紊乱方面有用，特别是它们在作为溴结构域抑制剂相关的疾病或紊乱中的使用。本发明还提供了该类化合物的制备以及包含至少一种公式（I）的双环杂环衍生物的药物配方，连同药学上可接受的载体、稀释剂或赋形剂。
• [EN] CIS-MORPHOLINONE AND OTHER COMPOUNDS AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER<br/>[FR] CIS-MORPHOLINONE ET AUTRES COMPOSÉS SERVANT D'INHIBITEURS DE MDM2 POUR LE TRAITEMENT DU CANCER
  申请人：AMGEN INC

  公开号：WO2014130470A1

  公开（公告）日：2014-08-28

  The present invention provides MDM2 inhibitor compounds of Formula (I), or the pharmaceutically acceptable salts thereof, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.

  本发明提供了式（I）的MDM2抑制剂化合物，或其药学上可接受的盐，其中变量如上所定义，这些化合物可用作治疗剂，特别用于治疗癌症。本发明还涉及含有MDM2抑制剂的药物组合物。
• [EN] SUBSTITUTED IMIDAZO[4,5-C]QUINOLINE DERIVATIVES AS BROMODOMAIN INHIBITORS<br/>[FR] DÉRIVÉS D'IMIDAZO[4,5-C]QUINOLÉINE SUBSTITUÉE UTILISÉS COMME INHIBITEURS DE BROMODOMAINES
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2014128655A1

  公开（公告）日：2014-08-28

  The present invention provides novel substituted imidazo[4,5-c]quinoline derivatives of formula (1), which may be therapeutically useful, more particularly as Bromodomain inhibitors; (1) in which Cyi, Cy2, R1, R2, R3, R4 and R5 have the same meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder associated as bromodomain inhibitors. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted imidazo[4,5-C]quinoline compounds of formula (1) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明提供了一种新颖的化合物，即式（1）的取代咪唑并[4,5-c]喹啉衍生物，其在治疗上可能有用，特别是作为Bromodomain抑制剂；其中Cyi，Cy2，R1，R2，R3，R4和R5具有规范中给定的相同含义，以及其药学上可接受的盐，可用于治疗和预防疾病或疾患，特别是作为Bromodomain抑制剂用于治疗相关疾病或疾患。本发明还提供了该化合物的制备方法和包括至少一种式（1）的取代咪唑并[4,5-c]喹啉化合物的制药配方，以及其药学上可接受的载体、稀释剂或赋形剂。
• CIS-MORPHOLINONE AND OTHER COMPOUNDS AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER
  申请人：AMGEN INC.

  公开号：US20160002185A1

  公开（公告）日：2016-01-07

  The present invention provides MDM2 inhibitor compounds of Formula (I), or the pharmaceutically acceptable salts thereof, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.

  本发明提供了公式（I）的MDM2抑制剂化合物或其药学上可接受的盐，其中变量如上所定义，这些化合物可用作治疗剂，特别是用于治疗癌症。本发明还涉及含有MDM2抑制剂的药物组合物。