N-heptyl-2-propan-2-yloxyacetamide

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: N-heptyl-2-propan-2-yloxyacetamide
• 化学式: C₁₂H₂₅NO₂
• 分子量: 215.33
• InChiKey: DXZGTOQCXZOAQA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  15
• 可旋转键数：
  9
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.92
• 拓扑面积：
  38.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• TARGET PROTEIN EED DEGRADATION-INDUCING DEGRADUCER, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING DISEASES RELATED TO EED, EZH2, OR PRC2, COMPRISING SAME AS ACTIVE INGREDIENT
  申请人：Korea Research Institute of Chemical Technology

  公开号：EP3922632A1

  公开（公告）日：2021-12-15

  The present invention relates to a target protein degradation-inducing Degraducer, a preparation method thereof, and a pharmaceutical composition for preventing or treating diseases related to EED, EZH2, or PRC2 comprising same as an active ingredient. A novel compound represented by formula 1, according to the present invention is a Degraducer compound that induces degradation of a target protein, i.e., embryonic ectoderm development (EED) or polycomb repressive complex 2 (PRC2), utilizing cereblon E3 ubiquitin ligase, von Hippel-Lindau tumor suppressor (VHL) E3 ubiquitin ligase, mouse double minute 2 homolog (MDM2) E3 ubiquitin ligase, and cellular inhibitor of apoptosis protein 1 (cIAP) E3 ubiquitin ligase, wherein the compound has an aspect of remarkably achieving target protein degradation-inducing activity through a ubiquitin proteasome system (UPS), and therefore there is a useful effect in that it is possible to provide a pharmaceutical composition for preventing or treating diseases or conditions related to a target protein, and a functional health food composition for preventing or improving same, comprising said compound as an active ingredient.

  本发明涉及一种靶蛋白降解诱导剂Degraducer，其制备方法以及包含其作为活性成分的用于预防或治疗与EED、EZH2或PRC2相关疾病的药物组合物。根据本发明，由式1表示的一种新化合物是一种Degraducer化合物，通过利用cereblon E3泛素连接酶、von Hippel-Lindau肿瘤抑制因子（VHL）E3泛素连接酶、鼠双分钟2同源物（MDM2）E3泛素连接酶和细胞凋亡抑制蛋白1（cIAP）E3泛素连接酶诱导靶蛋白，即胚胎外胚层发育（EED）或多能复合体抑制2（PRC2）的降解，其中该化合物通过泛素蛋白酶体系统（UPS）显著实现靶蛋白降解诱导活性的方面，因此可以提供一种用于预防或治疗与靶蛋白相关疾病或症状的药物组合物，以及包含所述化合物作为活性成分的功能性保健食品组合物，具有有益效果。
• [EN] HCK DEGRADERS AND USES THEREOF<br/>[FR] AGENTS DE DÉGRADATION DE HCK ET LEURS UTILISATIONS
  申请人：DANA FARBER CANCER INST INC

  公开号：WO2020263935A1

  公开（公告）日：2020-12-30

  Provided herein are bifunctional compounds with a moiety (e.g., lenalidomide, thalidomide) that is a binder of an E3 ubiquitin ligase (e.g., Cereblon) and another moiety that is a binder of a kinase (e.g., HCK, BTK) to induce degradation of the kinase (e.g., HCK, BTK). Also provided are pharmaceutical compositions comprising the bifunctional compounds, and methods of treating and/or preventing diseases (e.g., proliferative diseases (e.g., non-Hodgkin's lymphoma, Burkitt's lymphoma, Waldenstrom macroglobulinemia, MYD88-mutated Waldenstrom macroglobulinemia, activated B-cell diffuse large B-cell lymphoma, leukemia)), inflammatory disease, or other diseases associated with MYD88 mutations). Provided also are methods of inducing the degradation of a kinase (e.g., HCK, BTK) in a cell in a biological sample or subject by administering the bifunctional compound or composition described herein.

  本文提供了一种双功能化合物，其具有一种基团（例如，来那度胺，沙利度胺），该基团是E3泛素连接酶的结合物（例如，Cereblon），以及另一种基团，该基团是激酶的结合物（例如，HCK，BTK），以诱导激酶（例如，HCK，BTK）的降解。还提供了包含双功能化合物的制药组合物，并提供了治疗和/或预防疾病（例如，增生性疾病（例如，非何杰金淋巴瘤，Burkitt淋巴瘤，Waldenstrom巨球蛋白血症，MYD88突变Waldenstrom巨球蛋白血症，激活B细胞弥漫性大B细胞淋巴瘤，白血病），炎症性疾病或其他与MYD88突变相关的疾病）的方法。还提供了通过给予本文所述的双功能化合物或组合物在生物样品或受试者中诱导细胞中激酶（例如，HCK，BTK）的降解的方法。
• COMPOUNDS AND METHODS FOR PURIFICATION OF SERINE PROTEASES
  申请人：Portola Pharmaceuticals, Inc.

  公开号：US20140186923A1

  公开（公告）日：2014-07-03

  Disclosed herein are compounds, compositions, methods and kits for purifying a serine protease and serine proteases purified with the compounds, compositions and methods.
• US9200268B2
  申请人：——

  公开号：US9200268B2

  公开（公告）日：2015-12-01
• US9644195B2
  申请人：——

  公开号：US9644195B2

  公开（公告）日：2017-05-09