6-氯-1H-苯并三唑-1-基氧三吡咯烷基六氟磷酸盐 | 893413-42-8

• 物质功能分类: 生物 - 细胞培养 - 添加剂
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并三唑类
• 中文名称: 6-氯-1H-苯并三唑-1-基氧三吡咯烷基六氟磷酸盐
• 中文别名: 1-(2,4,6-三异丙基苯基磺酰)咪唑
• 英文名称: Pyclock
• 英文别名: (6-chlorobenzotriazol-1-yl)oxy-tripyrrolidin-1-ylphosphanium;hexafluorophosphate
• CAS: 893413-42-8
• 化学式: C18H27ClF6N6OP2
• 分子量: 554.8
• InChiKey: QJZCQEPNBRAYQL-UHFFFAOYSA-N

物化性质

• 熔点：
  174-180°C

计算性质

• 辛醇/水分配系数(LogP)：
  6.86
• 重原子数：
  34
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  49.7
• 氢给体数：
  0
• 氢受体数：
  13

安全信息

• 安全说明：
  S23
• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H315,H319,H335

文献信息

• [EN] TRICYCLIC HETEROCYCLE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES TRICYCLIQUES UTILES EN TANT QU'INHIBITEURS DE L'INTÉGRASE DU VIH
  申请人：MERCK SHARP & DOHME

  公开号：WO2018102634A1

  公开（公告）日：2018-06-07

  The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein A, X, Y, Z, R1, R7A, R7B and R8 are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.

  本发明涉及式(I)的三环杂环化合物及其药学上可接受的盐或前药，其中A、X、Y、Z、R1、R7A、R7B和R8如本文所定义。本发明还涉及包含至少一种三环杂环化合物的组合物，以及使用这些三环杂环化合物治疗或预防受试者的HIV感染的方法。
• [EN] PROCESS FOR PREPARING A GIP/GLP1 DUAL AGONIST<br/>[FR] PROCÉDÉ DE PRÉPARATION D'UN AGONISTE DOUBLE GIP/GLP1
  申请人：LILLY CO ELI

  公开号：WO2020159949A1

  公开（公告）日：2020-08-06

  The present invention provides novel intermediates and processes useful in the manufacture of tirzepatide, or a pharmaceutically acceptable salt thereof.

  本发明提供了在制备替瑞普肽或其药用可接受盐时有用的新型中间体和工艺。
• [EN] CRF RECEPTOR ANTAGONISTS AND METHODS OF USE<br/>[FR] ANTAGONISTES DU RÉCEPTEUR CRF ET PROCÉDÉS D'UTILISATION
  申请人：NEUROCRINE BIOSCIENCES INC

  公开号：WO2021113263A1

  公开（公告）日：2021-06-10

  Compounds are provided herein that antagonize corticotropin-releasing factor (CRF) receptors, in particular CRF receptor 1 (CRF1), as well as related preparations, compositions and methods for treating diseases and/or disorders that would benefit from the same such as congenital adrenal hyperplasia (CAH).

  本文提供了一些拮抗促肾上腺皮质激素释放因子（CRF）受体的化合物，特别是CRF受体1（CRF1），以及相关的制剂、组合物和治疗疾病和/或疾病的方法，这些疾病和/或疾病可以从中受益，如先天性肾上腺皮质增生症（CAH）。
• [EN] PEPTIDE COMPOUNDS<br/>[FR] COMPOSÉS PEPTIDIQUES
  申请人：ULTUPHARMA AB

  公开号：WO2020046190A1

  公开（公告）日：2020-03-05

  The present invention relates to novel compounds, which presents a peptide structure and an unexpected antibacterial effect even against certain multiresistant bacteria. The compounds may becyclic peptides, sometimes depsipeptides, ornon-ring-closed peptides, asdefined by Formula (I). Further, the invention relates to the medical use of the herein claimed compounds, a method for the production of the compounds as well as a method of treatment including the compounds. In addition, the invention relates to a pharmaceutical preparation comprising one or more of the herein described and claimed compounds combined with suitable carrier(s) and/or adjuvant(s). Finally, the invention is the use of one or more of the claimed compounds in a method for decolonization of a surface of Gram-positive and/or Gram-negative bacteria.

  本发明涉及一种新型化合物，其具有肽结构并且具有出乎意料的抗菌效果，甚至对某些多重耐药细菌也有效。这些化合物可能是环肽，有时是脱氨肽，或者是非环闭合肽，如公式（I）所定义。此外，本发明涉及所述化合物的医药用途，一种生产该化合物的方法以及包括该化合物的治疗方法。此外，本发明还涉及一种制药制剂，其中包括一种或多种所述化合物，结合适当的载体和/或辅料。最后，本发明是利用一种或多种所述化合物在去除革兰氏阳性和/或阴性细菌表面的方法中的应用。
• HALOGENATED-HETEROARYL AND OTHER HETEROCYCLIC KINASE INHIBITORS, AND USES THEREOF
  申请人：iOmx Therapeutics AG

  公开号：EP3901151A1

  公开（公告）日：2021-10-27

  The invention relates to kinase inhibitors, in particular inhibitors of protein kinases including the SIK-family CSF1R, ABL/BCR-ABL, SRC, HCK, PDGFR, KIT and/or their mutants. Although structurally similar to dasatinib, the kinase inhibitors of the invention are distinctive; possessing a particular class of halogenated heteroaryls. Such kinase inhibitors can display one or more certain properties distinct to dasatinib and other structurally similar kinase inhibitors. The kinase inhibitors of the invention or pharmaceutical compositions comprising them may be used in the treatment of a disorder or condition, such as a proliferative disorder, for example, a leukaemia or solid tumour. In particular, these and other structurally similar kinase inhibitors may be used in the treatment of a proliferative disorder - such as a mixed phenotype acute leukaemia (MPAL) - characterised by (inter-alia) the presence of MEF2C protein, a human chromosomal translocation at 11q23, and/or a KMT2A fusion oncoprotein. The kinase inhibitors or pharmaceutical compositions disclosed herein may be used topically to modulate skin pigmentation in a subject, for example to impart UV protection and reduce skin cancer risk.

  该发明涉及激酶抑制剂，特别是蛋白激酶的抑制剂，包括SIK家族CSF1R，ABL/BCR-ABL，SRC，HCK，PDGFR，KIT和/或它们的突变体。尽管在结构上类似于达沙替尼，但该发明的激酶抑制剂具有独特之处；具有一类特殊的卤代杂环芳基。这种激酶抑制剂可能表现出与达沙替尼和其他在结构上相似的激酶抑制剂不同的某些性质。该发明的激酶抑制剂或包含它们的药物组合物可用于治疗某种疾病或病况，例如增生性疾病，例如白血病或实体肿瘤。特别是，这些和其他在结构上相似的激酶抑制剂可用于治疗增生性疾病 - 例如混合表型急性白血病（MPAL）- 其特征包括MEF2C蛋白的存在，11q23处的人类染色体易位，和/或KMT2A融合致癌蛋白。本文披露的激酶抑制剂或药物组合物可用于局部调节受试者的皮肤色素沉着，例如赋予UV保护并降低皮肤癌风险。