Pulrodemstat | 1821307-10-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: Pulrodemstat
• 英文别名: 4-[2-(4-aminopiperidin-1-yl)-5-(3-fluoro-4-methoxyphenyl)-1-methyl-6-oxopyrimidin-4-yl]-2-fluorobenzonitrile
• CAS: 1821307-10-1
• 化学式: C₂₄H₂₃F₂N₅O₂
• 分子量: 451.5
• InChiKey: NBAIXBAUHIQQGF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  33
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  95
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• [EN] TREATMENT OF RELAPSED AND/OR REFRACTORY SOLID TUMORS AND NON-HODGKIN'S LYMPHOMAS<br/>[FR] TRAITEMENT DE TUMEURS SOLIDES RÉCIDIVANTES ET/OU RÉFRACTAIRES ET DE LYMPHOMES NON HODGKINIENS.
  申请人：CELGENE CORP

  公开号：WO2018031658A1

  公开（公告）日：2018-02-15

  Methods are provided for the treatment of relapsed and/or refractory solid tumors (including neuroendocrine carcinomas (NEC) and non-Hodgkin's lymphomas (NHLs) and the like, using substituted heterocyclic derivative compounds and pharmaceutical compositions comprising compounds useful for the inhibition of lysine specific demethylase-1 (LSD-1).

  提供了一种治疗复发和/或难治性实体肿瘤（包括神经内分泌癌（NEC）和非霍奇金淋巴瘤（NHL）等）的方法，使用替代杂环衍生物化合物和包含用于抑制赖氨酸特异性去甲基化酶-1（LSD-1）的化合物的药物组合物。
• ANTIPROLIFERATIVE COMPOUNDS AND METHODS OF USE THEREOF
  申请人：Celgene Corporation

  公开号：US20190008852A1

  公开（公告）日：2019-01-10

  Provided herein is 4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-1-yl)-3-fluorobenzonitrile, or an enantiomer, a mixture of enantiomers, a tautomer, or a pharmaceutically acceptable salt thereof, and methods for treating, preventing or managing multiple myeloma using such compounds. Also provided are pharmaceutical compositions comprising the compounds, and methods of use of the compositions.

  提供的是4-(4-(4-(((2-(2,6-二氧杂哌啶-3-基)-1-氧代异吲哚啉-4-基)氧基)甲基)苯甲基)哌嗪-1-基)-3-氟苯甲腈，或其对应体，对应体的混合物，互变异构体，或其药物可接受的盐，以及使用这些化合物治疗、预防或管理多发性骨髓瘤的方法。还提供了包含该化合物的药物组合物，以及这些组合物的使用方法。
• PHARMACEUTICAL COMPOSITIONS COMPRISING (S)-4-(4-(4-(((2-(2,6-DIOXOPIPERIDIN-3-YL)-1-OXOISOINDOLIN-4-YL)OXY)METHYL)BENZYL)PIPERAZIN-1-YL)-3-FLUOROBENZONITRILE AND METHODS OF USING THE SAME
  申请人：Celgene Corporation

  公开号：US20200215061A1

  公开（公告）日：2020-07-09

  Provided herein are pharmaceutical compositions (e.g., oral dosage formulations) comprising (S)-4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-1-yl)-3-fluorobenzonitrile, or an enantiomer, mixture of enantiomers, tautomer, isotopolog, or pharmaceutically acceptable salt thereof, and a carrier or diluent. Also provided herein are methods of preparing and methods of using the pharmaceutical compositions.

  本文提供了包含(S)-4-(4-(4-(((2-(2,6-二氧代哌啶-3-基)-1-氧代异吲哚-4-基)氧甲基)苄基)哌嗪-1-基)-3-氟苯甲腈，或其对映体、对映体混合物、互变异构体、同位素替代物或其药用可接受盐，以及载体或稀释剂的药物组合物（例如口服剂型）。本文还提供了制备方法和使用药物组合物的方法。
• SOLID FORMS COMPRISING (S)-4-(4-(4-(((2-(2,6-DIOXOPIPERIDIN-3-YL)-1-OXOISOINDOLIN-4-YL)OXY)METHYL)BENZYL)PIPERAZIN-1-YL)-3-FLUOROBENZONITRILE AND SALTS THEREOF, AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME
  申请人：Celgene Corporation

  公开号：US20200216418A1

  公开（公告）日：2020-07-09

  Provided herein are formulations, processes, solid forms and methods of use relating to salts of and solid forms comprising free base or salts of (S)-4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-1-yl)-3-fluorobenzonitrile.

  本文提供了与(S)-4-(4-(4-(((2-(2,6-二氧代哌啶-3-基)-1-氧基异吲哚-4-基)氧甲基)苄基)哌嗪-1-基)-3-氟苯甲腈的盐或固体形式相关的配方、工艺、固体形式和使用方法。
• INHIBITORS OF LYSINE SPECIFIC DEMETHYLASE-1
  申请人：Quanticel Pharmaceuticals, Inc.

  公开号：US20160130247A1

  公开（公告）日：2016-05-12

  The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.

  本发明涉及治疗癌症和肿瘤性疾病的组合物和方法。提供了取代杂环衍生物化合物和包含该化合物的制药组合物。所述化合物和组合物对于抑制赖氨酸特异性去甲基化酶-1具有用途。此外，所述化合物和组合物对于治疗癌症具有用途。