N-(4-acetylphenyl)-3-methylbutanamide

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: N-(4-acetylphenyl)-3-methylbutanamide
• 化学式: C₁₃H₁₇NO₂
• mdl: MFCD01336638
• 分子量: 219.28
• InChiKey: VCCOOXHDDPOVCX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  16
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.384
• 拓扑面积：
  46.2
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] CYTOTOXIC BIS-BENZODIAZEPINE DERIVATIVES AND CONJUGATES THEREOF WITH CELL-BINDING AGENTS FOR INHIBITING ABNORMAL CELL GROWTH OR FOR TREATING PROLIFERATIVE DISEASES<br/>[FR] DÉRIVÉS DE BIS-BENZODIAZÉPINE CYTOTOXIQUES ET LEURS CONJUGUÉS AVEC DES AGENTS DE LIAISON À UNE CELLULE POUR INHIBER LA CROISSANCE CELLULAIRE ANORMALE OU POUR TRAITER DES MALADIES PROLIFÉRATIVES
  申请人：IMMUNOGEN INC

  公开号：WO2020205564A1

  公开（公告）日：2020-10-08

  The invention relates to benzodiazepine derivatives with antiproliferative activity and more specifically to benzodiazepine compounds of formulae (I), (II), (TI) and (T2). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

  这项发明涉及具有抗增殖活性的苯二氮䓬啶衍生物，更具体地涉及具有式(I)、(II)、(TI)和(T2)的苯二氮䓬啶化合物。该发明还提供了与细胞结合剂连接的苯二氮䓬啶化合物的结合物。该发明还提供了使用该发明的化合物或结合物抑制异常细胞生长或治疗哺乳动物增殖性疾病的组合物和方法。
• CYTOTOXIC BENZODIAZEPINE DERIVATIVES
  申请人：IMMUNOGEN, INC.

  公开号：US20160082114A1

  公开（公告）日：2016-03-24

  The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VI). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

  该发明涉及具有抗增殖活性的新型苯二氮䓬类衍生物，更具体地涉及具有式(I)-(VI)的新型苯二氮䓬类化合物。该发明还提供了将苯二氮䓬类化合物与细胞结合剂连接的结合物。该发明还提供了使用该发明的化合物或结合物抑制异常细胞生长或治疗哺乳动物增生性疾病的有效组合物和方法。
• Inhibitors of interleukin-1beta converting enzyme
  申请人：Batchelor James Mark

  公开号：US20080039449A1

  公开（公告）日：2008-02-14

  The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-γ-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-γ-mediated diseases and decreasing IGIF and IFN-γ production using the compounds and compositions of this invention. This invention also relates to methods for preparing-N-acylamino compounds.

  本发明涉及一种新型的化合物类别，其为白细胞介素-1β转化酶的抑制剂。本发明的ICE抑制剂具有特定的结构和物理化学特征。本发明还涉及包含这些化合物的制药组合物。本发明的化合物和制药组合物特别适用于抑制ICE活性，因此可以作为抗IL-1、凋亡、IGIF、IFN-γ介导的疾病、炎症性疾病、自身免疫性疾病、破坏性骨病、增生性疾病、感染性疾病、退行性疾病和坏死性疾病的药物。本发明还涉及使用这些化合物和组合物抑制ICE活性、治疗白细胞介素-1、凋亡、IGIF和IFN-γ介导的疾病、降低IGIF和IFN-γ的产生的方法。本发明还涉及制备N-酰基氨基化合物的方法。
• INHIBITORS OF INTERLEUKIN-1 BETA CONVERTING ENZYME
  申请人：Batchelor Mark James

  公开号：US20110178069A1

  公开（公告）日：2011-07-21

  The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-γ-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-γ-mediated diseases and decreasing IGIF and IFN-γ production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds.

  本发明涉及一种新型化合物类别，其为白细胞介素-1β转化酶抑制剂。本发明的ICE抑制剂具有特定的结构和物理化学特征。本发明还涉及包含这些化合物的制药组合物。本发明的化合物和制药组合物特别适用于抑制ICE活性，因此可以优势地用作对抗IL-1、凋亡、IGIF和IFN-γ介导的疾病、炎症性疾病、自身免疫性疾病、破坏性骨病、增生性疾病、传染性疾病、退行性疾病和坏死性疾病的药剂。本发明还涉及使用本发明的化合物和组合物抑制ICE活性、治疗白细胞介素-1、凋亡、IGIF和IFN-γ介导的疾病、减少IGIF和IFN-γ产生的方法。本发明还涉及制备N-酰基氨基化合物的方法。
• Inhibitors of interleukin-1ß converting enzyme
  申请人：Vertex Pharmceuticals Incorporated

  公开号：EP2083014A2

  公开（公告）日：2009-07-29

  The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physiochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-γ-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF-, and IFN-γ-mediated diseases and decreasing IGIF, and IFN-γ production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds.

  本发明涉及一类新型化合物，它们是白细胞介素-1β转换酶的抑制剂。本发明的 ICE 抑制剂具有特定的结构和理化特征。本发明还涉及包含这些化合物的药物组合物。本发明的化合物和药物组合物特别适用于抑制 ICE 的活性，因此可作为抗 IL-1、细胞凋亡、IGIF 和 IFN-γ 介导的疾病、炎症性疾病、自身免疫性疾病、破坏性骨疾病、增殖性疾病、感染性疾病、退行性疾病和坏死性疾病的药物。本发明还涉及使用本发明化合物和组合物抑制 ICE 活性、治疗白细胞介素-1、细胞凋亡、IGIF 和 IFN-γ 介导的疾病以及减少 IGIF 和 IFN-γ 生成的方法。本发明还涉及制备 N-酰氨基化合物的方法。