N-(2-hydroxy-1,3-dimethoxy-10-methylsulfanyl-9-oxo-6,7-dihydro-5H-benzo[a]heptalen-7-yl)acetamide | 87424-26-8

• 分子结构分类: 有机化合物 - 碳氢化合物衍生物 - 环庚三烯酮
• 英文名称: N-(2-hydroxy-1,3-dimethoxy-10-methylsulfanyl-9-oxo-6,7-dihydro-5H-benzo[a]heptalen-7-yl)acetamide
• CAS: 87424-26-8
• 化学式: C₂₁H₂₃NO₅S
• 分子量: 401.5
• InChiKey: OMQLBXIHBJAOIO-UHFFFAOYSA-N

物化性质

• 熔点：
  218-220°C
• 沸点：
  766.8±60.0 °C(Predicted)
• 密度：
  1.33±0.1 g/cm3(Predicted)
• 溶解度：
  溶于氯仿

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  110
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• [EN] PROCESS FOR THE CONVERSION OF COLCHICINOIDS TO THEIR 3-GLYCOSYLATED DERIVATIVES VIA THEIR RESPECTIVE 3-DEMETHYL ANALOGUES<br/>[FR] PROCÉDÉ POUR LA CONVERSION DE COLCHICINOÏDES EN LEURS DÉRIVÉS 3-GLYCOSYLÉS PAR LEUR ANALOGUES 3-DÉMÉTHYL CORRESPONDANTS
  申请人：ALKALOIDS CORP

  公开号：WO2015097567A1

  公开（公告）日：2015-07-02

  The present invention relates to a bioprocess for the preparation of glycosylated Colchicine, its analogs and derivatives of formula (I) wherein X represents O or S, and R1 represents C1-C6 alkyl, R2 is a glycoside residue, R represents hydrogen, C1-C6 alkyl, formyl or acetyl.

  本发明涉及一种生物工艺，用于制备糖基化的秋水仙碱、其类似物和衍生物，其化学式为（I），其中X代表O或S，R1代表C1-C6烷基，R2为糖苷残基，R代表氢、C1-C6烷基、甲酰基或乙酰基。
• Carbonates of 3-demethylthiocolchicine and N-acyl analogs
  申请人：Advance Biofactures Corporation

  公开号：EP0356137A2

  公开（公告）日：1990-02-28

  The present invention relates to esters of 3-demethylthiocolchicine and N-acyl analogs thereof having the following formula: wherein R is O-CO-alkyl, O-CO-CH₂Oalkyl, O-CO-Phenyl, O-COOalkyl; the alkyl group having from 1 to 4 carbon atoms and the Ac group representing acetyl and its higher homologs, benzoyl, alkoxyacetyl, or haloacetyl. The invention further relates to processes for preparing these ester compounds, pharmaceutical compositions thereof and methods for treating diseases such as gout, Mediterranean fever and liver disorders.

  本发明涉及具有下式的 3-去甲基硫代小儿钦碱的酯及其 N-酰基类似物： 其中R是O-CO-烷基、O-CO-CH₂-烷基、O-CO-苯基、O-COO烷基；烷基具有1至4个碳原子，Ac基团代表乙酰基及其高级同系物、苯甲酰基、烷氧基乙酰基或卤代乙酰基。 本发明进一步涉及制备这些酯类化合物的工艺、其药物组合物以及治疗痛风、地中海热和肝脏疾病等疾病的方法。
• Thiocolchicine derivatives with antiinflammatory and muscle relaxant activities
  申请人：INDENA S.p.A.

  公开号：EP0870761A1

  公开（公告）日：1998-10-14

  The present invention relates to 3-demethyl-thiocolchicine derivatives of general formula (I) in which R can be HOCH2-CHOH-CH2-, H2NCH2CHOHCH2-, HOOCCH2-, OH-CH2-CHCl-CH2-, to a process for the preparation thereof, to pharmaceutical compositions containing them and to the use thereof for the preparation of medicaments with muscle relaxant and antiinflammatory activities.

  本发明涉及通式(I)的 3-去甲基-硫代小儿喹啉衍生物 其中 R 可以是 HOCH2-CHOH-CH2-、H2NCH2CHOHCH2-、HOOCCH2-、OH-CH2-CHCl-CH2-；本发明涉及其制备方法、含有它们的药物组合物，以及使用它们制备具有肌肉松弛剂和抗炎活性的药物。
• Anti-CS1 antibodies and antibody drug conjugates
  申请人：AbbVie Biotherapeutics Inc.

  公开号：US10011657B2

  公开（公告）日：2018-07-03

  The present disclosure provides antibodies and antibody drug conjugates that bind human CS1 and their uses to treat subjects diagnosed with a plasma cell neoplasm, for example, multiple myeloma.

  本公开提供了与人类 CS1 结合的抗体和抗体药物共轭物，以及它们在治疗确诊为浆细胞肿瘤（例如多发性骨髓瘤）患者中的用途。
• Anti-glyco-MUC1 antibodies and their uses
  申请人：GO Therapeutics, Inc.

  公开号：US11161911B2

  公开（公告）日：2021-11-02

  The present disclosure relates to anti-glyco-MUC1 antibodies and antigen binding fragments thereof that specifically bind to a cancer-specific glycosylation variant of MUC1 and related fusion proteins and antibody-drug conjugates, as well as nucleic acids encoding such biomolecules. The present disclosure further relates to use of the antibodies, antigen-binding fragments, fusion proteins, antibody-drug conjugates and nucleic acids for cancer therapy.

  本公开涉及抗糖基化 MUC1 抗体及其抗原结合片段，它们能特异性地与癌症特异性糖基化变体 MUC1 和相关融合蛋白及抗体-药物共轭物结合，以及编码此类生物大分子的核酸。本公开进一步涉及这些抗体、抗原结合片段、融合蛋白、抗体-药物共轭物和核酸在癌症治疗中的应用。