N-[[4-(dimethylamino)phenyl]methyl]-N'-hydroxy-2-(naphthalen-1-yloxymethyl)oct-2-enediamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: N-[[4-(dimethylamino)phenyl]methyl]-N'-hydroxy-2-(naphthalen-1-yloxymethyl)oct-2-enediamide
• 化学式: C₂₈H₃₃N₃O₄
• 分子量: 475.6
• InChiKey: NIFZMNPKVPWAMX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  35
• 可旋转键数：
  12
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  90.9
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• PHARMACEUTICALLY ACCEPTABLE SALT OF ALKYLCARBAMOYL NAPHTHALENYLOXY OCTENOYLHYDROXYAMIDE OR OF DERIVATIVE THEREOF AND METHOD FOR PREPARING SAME
  申请人：CRYSTALGENOMICS, INC.

  公开号：US20200283371A1

  公开（公告）日：2020-09-10

  The present invention relates to a pharmaceutically acceptable salt of alkylcarbamoyl naphthalenyloxy octenoylhydroxyamide or of a derivative thereof and a method for preparing same, and can improve moisture stability while maintaining the characteristics, such as the efficacy and effective dose, of a pharmaceutically acceptable salt of alkylcarbamoyl naphthalenyloxy octenoylhydroxyamide or of a derivative thereof. In addition, the present invention can simplify the production and manufacturing process of a formulation by improving hygroscopicity.

  本发明涉及一种药学上可接受的烷基氨基甲酰基萘氧基辛烯酰羟胺盐或其衍生物的制备方法，能够在保持药学上可接受的烷基氨基甲酰基萘氧基辛烯酰羟胺盐或其衍生物的功效和有效剂量等特性的同时，提高其湿度稳定性。此外，本发明还可以通过提高其吸湿性来简化配方的生产和制造过程。
• NAPHTHALENYLOXYPROPENYL DERIVATIVES HAVING INHIBITORY ACTIVITY AGAINST HISTONE DEACETYLASE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
  申请人：Lee Cheol Hae

  公开号：US20100069630A1

  公开（公告）日：2010-03-18

  The present invention discloses novel naphthalenyloxypropenyl derivatives useful for inhibiting the enzyme activity of histone deacetylase, leading effective suppression of cancer cell proliferation.

  本发明公开了一种新型萘氧基丙烯酰衍生物，用于抑制组蛋白去乙酰化酶的酶活性，从而有效抑制癌细胞增殖。
• Naphthalenyloxypropenyl derivatives having inhibitory activity against histone deacetylase and pharmaceutical composition comprising the same
  申请人：Korea Research Institute Of Chemical Technology

  公开号：EP2913322A2

  公开（公告）日：2015-09-02

  The present invention discloses novel naphthalenyloxypropenyl derivatives useful for inhibiting the enzyme activity of histone deacctylase, leading effective suppression of cancer cell proliferation.

  本发明公开了新型萘氧丙烯基衍生物，可用于抑制组蛋白脱切酶的酶活性，从而有效抑制癌细胞增殖。
• PHARMACEUTICAL COMPOSITION CONTAINING ALKYL CARBAMOYL NAPHTHALENYLOXY OCTENOYL HYDROXYAMIDE PHOSPHATE, TARTRATE OR COMBINATION THEREOF, AND PREPARATION METHOD THEREFOR
  申请人：Crystalgenomics, Inc.

  公开号：EP3875081A1

  公开（公告）日：2021-09-08

  The present invention relates to a pharmaceutical composition containing an alkyl carbamoyl naphthalenyloxy octenoyl hydroxyamide phosphate compound (hereinafter referred to as CG200745PPA) or a derivative thereof, and can provide a pharmaceutical composition in a tablet, granule, powder, capsule, dry syrup or injection form. By providing the composition in various forms, a suitable form can be selected and easily applied when oral administration is difficult.

  本发明涉及一种含有烷基氨基甲酰萘氧基辛烯酰羟酰胺磷酸酯化合物（以下简称 CG200745PPA）或其衍生物的药物组合物，可提供片剂、颗粒剂、粉剂、胶囊剂、干糖浆剂或注射剂形式的药物组合物。通过提供各种形式的组合物，可以选择合适的形式，并在口服给药困难时方便应用。
• PHARMACEUTICAL COMPOSITION COMPRISING HDAC INHIBITOR AND ANTI-PD1 ANTIBODY OR ANTI PD-L1 ANTIBODY
  申请人：Crystalgenomics, Inc.

  公开号：EP4026544A1

  公开（公告）日：2022-07-13

  The present invention relates to a method for killing cancer cells by using a combination of an HDAC inhibitor and an anti-PD1 antibody or an anti PD-L1 antibody. The present invention can have an effective influence on: extending the survival of animals with cancer, tumors, tumor-related disorders and neoplastic diseases; inhibiting the growth of proliferative cells associated with neoplasms; or neoplastic degeneration.

  本发明涉及一种通过使用 HDAC 抑制剂和抗 PD1 抗体或抗 PD-L1 抗体的组合来杀死癌细胞的方法。本发明可对以下方面产生有效影响：延长癌症、肿瘤、肿瘤相关疾病和肿瘤性疾病动物的生存期；抑制与肿瘤相关的增殖细胞的生长；或肿瘤变性。