N-methyl-N-(4-methyl-5-sulfamoyl-1,3-thiazol-2-yl)-2-(3-pyridin-2-ylphenyl)acetamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: N-methyl-N-(4-methyl-5-sulfamoyl-1,3-thiazol-2-yl)-2-(3-pyridin-2-ylphenyl)acetamide
• 化学式: C₁₈H₁₈N₄O₃S₂
• 分子量: 402.5
• InChiKey: PONWBCCKDDAHGA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  27
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  143
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• [EN] A MALEATE SALT OF THE FREE BASE OF N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)-PHENYL]-ACETAMIDE, PHARMACEUTICAL FORMULATIONS, METHODS OF MANUFACTURE AND USES THEREOF FOR THE TREATMENT OF HERPES VIRUSES<br/>[FR] SEL DE MALÉATE DE LA BASE LIBRE DE N- [5- (AMINOSULFONYL)-4-MÉTHYL -1,3-THIAZOL-2-YL]-N-MÉTHYL-2-[4- (2-PYRIDINYL)-PHÉNYL]-ACÉTAMIDE, FORMULATIONS PHARMACEUTIQUES, PROCÉDÉS DE FABRICATION ET UTILISATIONS DE CEUX-CI POUR LE TRAITEMENT DU VIRUS DE L'HERPÈS
  申请人：AICURIS ANTI INFECTIVE CURES GMBH

  公开号：WO2018096177A1

  公开（公告）日：2018-05-31

  The present invention relates to the field of anti-viral active agents, particularly to salts, more particularly to a maleate salt of the free base of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2- yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]-acetamide, to pharmaceutical formulations thereof as well as to methods for the production of these salts. The present invention also relates to the use of theses salts and of respective pharmaceutical formulations thereof in methods of treatment and/or prevention of human herpes simplex virus infections, particulary infections caused by HSV-1 and HSV-2.

  本发明涉及抗病毒活性剂领域，特别涉及盐，更具体地涉及一种N-[5-(氨基磺酰基)-4-甲基-1,3-噻唑-2-基]-N-甲基-2-[4-(2-吡啶基)-苯基]-乙酰胺的游离碱的马来酸盐，以及其药物制剂和制备这些盐的方法。本发明还涉及这些盐及其相应药物制剂在治疗和/或预防人类单纯疱疹病毒感染，特别是HSV-1和HSV-2感染的方法中的使用。
• EP2956134A2
  申请人：——

  公开号：EP2956134A2

  公开（公告）日：2015-12-23
• A MALEATE SALT OF THE FREE BASE OF N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)-PHENYL]-ACETAMIDE, PHARMACEUTICAL FORMULATIONS, METHODS OF MANUFACTURE AND USES THEREOF FOR THE TREATMENT OF HERPES VIRUSES
  申请人：AiCuris Anti-infective Cures GmbH

  公开号：EP3544977A1

  公开（公告）日：2019-10-02
• [EN] HELICASE-PRIMASE INHIBITORS FOR USE IN A METHOD OF TREATING ALZHEIMER'S DISEASE<br/>[FR] INHIBITEURS DE L'HÉLICASE-PRIMASE DESTINÉS À ÊTRE UTILISÉS DANS UNE MÉTHODE DE TRAITEMENT DE LA MALADIE D'ALZHEIMER
  申请人：AICURIS GMBH & CO KG

  公开号：WO2014124978A2

  公开（公告）日：2014-08-21

  The present invention relates to the use of helicase-primase inhibitors in a method of treating Alzheimer's Disease (AD). Particularly, the present invention relates to the use of helicase-primase inhibitors in a method of treating AD in a subject that is having HSV-1 infection and is having AD or is having HSV-1 infection and is suspected of having AD. The provided antiviral helicase-primase inhibitors affect the accumulation of the key AD proteins amyloid beta and abnormally phosphorylated tau that occur during HSV-1 infection.
• [EN] TOPICAL PHARMACEUTICAL FORMULATION COMPRISING N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)-PHENYL]-ACETAMIDE<br/>[FR] FORMULATION PHARMACEUTIQUE TOPIQUE COMPRENANT DU N-[5-(AMINOSULFONYLE)-4-MÉTHYL-1,3-THIAZOL-2-YL]-N-MÉTHYL-2-[4-(2-PYRIDINYL)-PHÉNYL]-ACÉTAMIDE
  申请人：AICURIS ANTI INFECTIVE CURES GMBH

  公开号：WO2018095576A1

  公开（公告）日：2018-05-31

  The present invention relates to pharmaceutical formulations of anti-viral active agents for the use in topical application, particularly for the use of these in the treatment of human herpes virus infections, wherein the anti-viral active agents may be selected from the group comprising the N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]-acetamide free base hemihydrate, the maleate salt of N-[5-(amino-sulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide, the mesylate salt of N-[5-(amino-sulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide, and the free base of N-[5-(amino-sulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide. Specifically, the present invention provides said pharmaceutical formulations for the use in topical application, wherein said formulations comprise an anti-viral agent as described above in dissolved state or in solubilized form, butylated hydroxyl toluene (BHT) and Super Refined™ PEG 400 at an apparent pH of 4.0 to 5.0, preferably at an apparent pH of 4.0 to 4.5.