BIP抑制剂(HA15) | 1609402-14-3

• 中文名称: BIP抑制剂(HA15)
• 英文名称: HA15
• 英文别名: N-[4-[3-[[5-(dimethylamino)naphthalen-1-yl]sulfonylamino]phenyl]-1,3-thiazol-2-yl]acetamide
• CAS: 1609402-14-3
• 化学式: C₂₃H₂₂N₄O₃S₂
• 分子量: 466.585
• InChiKey: LBSMEKVVMYSTIH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  32
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  128
• 氢给体数：
  2
• 氢受体数：
  7

安全信息

• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335

文献信息

• [EN] NEW BENZENE SULFONAMIDE THIAZOLE COMPOUNDS<br/>[FR] NOUVEAUX COMPOSÉS DE BENZÈNESULFONAMIDE-THIAZOLE
  申请人：INSERM INST NAT DE LA SANTÉ ET DE LA RECH MÉDICALE

  公开号：WO2014072486A1

  公开（公告）日：2014-05-15

  The present invention relates to compound of general formula (1) wherein R1 represents C6-C10 aryl comprising one or two fused rings, wherein from 2 to 5 carbon atoms may be replaced with a heteroatom selected from O, S and NR6, and eventually substituted with from 5 to 11 substituants selected from R6, halo, CN, NO2, CF3, OCF3, COOR6, OCOR6, SO2NR6R7, CONR6R7, NR6R7, NR6COR7, (CH2)P- NR6R7, (CH2)P- OR6 and (CH2)PSR6, as well as, if appropriate, their pharmaceutically acceptable salts and/or isomers, tautomers, solvates or isotopic variations thereof. The compounds are useful for the treatment of cancers.

  本发明涉及一般式（1）的化合物，其中R1代表含有一个或两个融合环的C6-C10芳基，其中2至5个碳原子可以被从O、S和NR6中选择的杂原子取代，最终可以被从R6、卤素、CN、NO2、CF3、O 、COOR6、OCOR6、SO2NR6R7、CONR6R7、NR6R7、NR6COR7、（CH2）P-NR6R7、（ ）P-OR6和（ ）PSR6中选择的5至11个取代基取代，以及在适当情况下，它们的药学上可接受的盐和/或异构体、互变异构体、溶剂合物或同位素变体。这些化合物对于治疗癌症很有用。
• NEW BENZENE SULFONAMIDE THIAZOLE COMPOUNDS
  申请人：Institut National de la Santé et de la Recherche Médicale (INSERM)

  公开号：EP2917190B1

  公开（公告）日：2017-07-19
• US9567310B2
  申请人：——

  公开号：US9567310B2

  公开（公告）日：2017-02-14
• [EN] PHARMACY PREPARATION FOR MALIGNANT MELANOMA TREATMENT<br/>[FR] PRÉPARATION PHARMACEUTIQUE POUR TRAITEMENT D'UN MÉLANOME MALIN
  申请人：UNIV KARLOVA

  公开号：WO2019196965A2

  公开（公告）日：2019-10-17

  The invention relates to a pharmacy preparation for malignant melanoma treatment containing combination of active ingredients, being GANT61, Obatoclax with the advantage of its mesylate salt, and agent selected from the group comprising (+)-JQ1, SGI-7079, GSK343, GSK126, HA15, wherein concentration of active ingredients in the specific triple-combination necessary to eradicate tumor cells is as follows: a) GANT61 from 10 to 20 μmol/l; b) Obatoclax from 150 to 300 nmol/l; cl) (+)-JQ1 from 125 to 500 nmol/l; c2) SGI-7079 from 125 to 500 nmol/l; c3) GSK343 from 0.25 to 1,0 μmol/l; c4) GSK126 from 25 to 100 nmol/l; and c5) HA15 from 2.5 to 10 μmol/l. All triple-combinations are highly effective in the experiments carried-out on cell cultures of human melanoma cells, when all tumor cells were eradicated not later than 7th day after application.