4-(肼基磺酰基)苯甲酸 | 6391-97-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 4-(肼基磺酰基)苯甲酸
• 英文名称: 4-hydrazinosulfonylbenzoic acid
• 英文别名: p-Carboxybenzolsulfonylhydrazid；4-Carboxy-phenylsulfonylhydrazid；(4-Carboxyphenylsulfonyl)hydrazin；p-H2NNHSO2C6H4COOH；4-(Hydrazinesulfonyl)benzoic acid
• CAS: 6391-97-5
• 化学式: C₇H₈N₂O₄S
• mdl: MFCD00025109
• 分子量: 216.218
• InChiKey: GDQXMMLQFVXPGA-UHFFFAOYSA-N

物化性质

• 熔点：
  235 °C (decomp)
• 沸点：
  461.1±47.0 °C(Predicted)
• 密度：
  1.547±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -2.6
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  118
• 氢给体数：
  3
• 氢受体数：
  6

安全信息

• 海关编码：
  2928000090

反应信息

• 作为反应物：
  描述：

  2-pyridinecarboxaldehyde N-oxide 、 4-(肼基磺酰基)苯甲酸 以 乙醇 为溶剂， 以70%的产率得到
  参考文献：
  名称：

  Synthesis and antineoplastic activity of phenyl-substituted phenylsulfonylhydrazones of 1-pyridinecarboxaldehyde 1-oxide

  摘要：

  A variety of derivatives of 2-pyridinecarboxaldehyde 1-oxide benzenesulfonylhydrazone, containing substituents on the benzene or pyridine rings as well as on the nitrogen atom which is bonded directly to the sulfonyl group, have been synthesized. The antineoplastic activity of these compounds has been assessed in mice bearing either leukemia L1210 or P388. The most potent agents in this series were 2,4-dimethoxy,3,4-dimethoxy-, and 2,4,6-trimethylbenzenesulfonylhydrazone of 2-pyridinecarboxyaldehyde 1-oxide, all causing disappearance of tumors in 20-80% of leukemia-bearing mice.

  DOI：

  10.1021/jm00180a010

文献信息

• Macromolecules
  申请人：Owen David

  公开号：US09744246B2

  公开（公告）日：2017-08-29

  The present invention relates to a macromolecule comprising a dendrimer having surface amino groups to which at least two different terminal groups are attached including a pharmaceutically active agent and a pharmacokinetic modifying agent, the pharmaceutically active agent comprising a hydroxyl group and being attached to the surface amino group of the dendrimer through a diacid linker. Pharmaceutical compositions comprising the macromolecules and methods of treatment using the macromolecules are also described.

  本发明涉及一种大分子，包括具有表面氨基团的树枝状聚合物，至少连接有两种不同末端基团，包括药用活性剂和药代动力学修饰剂，所述药用活性剂包括一个羟基，并通过二酸链连接剂连接到树枝状聚合物的表面氨基团上。还描述了包含这种大分子的药物组合物和使用这种大分子进行治疗的方法。
• [EN] PRO-DRUG FORMING COMPOUNDS<br/>[FR] COMPOSÉS POUR LA FORMATION DE PROMÉDICAMENTS
  申请人：EVESTRA INC

  公开号：WO2015006691A1

  公开（公告）日：2015-01-15

  Various prodrug compounds having the general structure: Active agent- (acid)-(linker) - SO2NR1R2 are described herein. Compounds having this general structure were shown to be more orally active than the unmodified parent molecule.

  本文描述了具有以下一般结构的各种前药化合物：活性药物-（酸）-（连接物）-SO2NR1R2。具有这种一般结构的化合物被证明比未经修改的母体分子更适合口服给药。
• [EN] PRO-DRUG FORM (P2PDOX) OF THE HIGHLY POTENT 2-PYRROLINODOXORUBICIN CONJUGATED TO ANTIBODIES FOR TARGETED THERAPY OF CANCER<br/>[FR] FORME DE PRO-MÉDICAMENT (P2PDOX) DE LA 2-PYRROLINODOXORUBICINE FORTEMENT PUISSANTE CONJUGUÉE À DES ANTICORPS POUR LA THÉRAPIE CIBLÉE DU CANCER
  申请人：IMMUNOMEDICS INC

  公开号：WO2014124227A1

  公开（公告）日：2014-08-14

  Disclosed are methods, compositions and uses of conjugates of prodrug forms of 2- pyrrolinodoxorubicin (P2PDox) with antibodies or antigen-binding fragments thereof (ADCs), with targetable construct peptides or with other targeting molecules that are capable of delivering the P2PDox to a targeted cell, tissue or pathogen. Once delivered to the target cell, the ADC or peptide conjugate is internalized, a highly toxic 2-pyrrolinodoxorubicin (2- PDox) is released intracellularly. The P2PDox-peptide or ADC conjugates are of use to treat a wide variety of diseases, such as cancer, autoimmune disease or infectious disease.

  本发明涉及2-吡咯烷基多柔比星（P2PDox）的前药形式与抗体或其抗原结合片段（ADC）、可靶向构建肽或其他靶向分子的结合物的共轭物的方法、组合物和用途，这些结合物能够将P2PDox递送到目标细胞、组织或病原体。一旦递送到目标细胞，ADC或肽共轭物被内吞，高毒性的2-吡咯烷基多柔比星（2-PDox）在细胞内释放。P2PDox-肽或ADC共轭物可用于治疗各种疾病，如癌症、自身免疫性疾病或传染病。
• Conjugates of disorazoles and their derivatives with cell-binding molecules, novel disorazole derivatives, processes of manufacturing and uses thereof
  申请人：AEterna Zentaris GmbH

  公开号：EP1900742A1

  公开（公告）日：2008-03-19

  The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.

  本发明提供了二氢异菊烯酮及其衍生物与细胞结合分子（如肽、蛋白质、激素、血液蛋白和抗体）结合的共轭物。本发明还提供了新的二氢异菊烯酮衍生物及制造这些共轭物和二氢异菊烯酮衍生物的方法。这些化合物可用作治疗哺乳动物的生理和/或病理状况，特别是治疗各种肿瘤的药物。
• NEOADJUVANT USE OF ANTIBODY-DRUG CONJUGATES
  申请人：Immunomedics, Inc.

  公开号：US20160095939A1

  公开（公告）日：2016-04-07

  The present invention concerns improved methods and compositions for neoadjuvant use of antibody-drug conjugates (ADCs) in cancer therapy, preferably ADCs comprising an anthracycline or camptothecin, more preferably SN-38 or pro-2-pyrrolinodoxorubicin (P2PDox). The ADC is administered as a neoadjuvant, prior to treatment with a standard anti-cancer therapy such as surgery, radiation therapy, chemotherapy, or immunotherapy. Neoadjuvant use of the ADC substantially improves the efficacy of standard anti-cancer therapy and may debulk a primary tumor or eliminate micrometasteses. In most preferred embodiments, neoadjuvant ADC in combination with a standard anti-cancer therapy is successful in treating cancers that are resistant to standard treatments, such as triple-negative breast cancer (TNBC).

  本发明涉及改进的方法和组合物，用于抗体药物联合物（ADC）在癌症治疗中的新辅助使用，优选包含蒽环类或喜树碱的ADC，更优选是SN-38或pro-2-pyrrolinodoxorubicin（P2PDox）的ADC。ADC作为新辅助治疗在标准抗癌疗法（如手术、放疗、化疗或免疫疗法）之前给予。ADC的新辅助使用显著提高了标准抗癌疗法的疗效，并可减少原发肿瘤或消除微小转移。在最优选实施例中，新辅助ADC与标准抗癌疗法结合治疗对标准治疗有抵抗的癌症，如三阴性乳腺癌（TNBC）具有成功的疗效。