(2,2-Difluorocyclopropyl)(3-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone | 1883299-62-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: (2,2-Difluorocyclopropyl)(3-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone
• 英文别名: (2,2-difluorocyclopropyl)-[3-[2-[(1-methylpyrazol-4-yl)amino]pyrimidin-4-yl]-3,8-diazabicyclo[3.2.1]octan-8-yl]methanone
• CAS: 1883299-62-4
• 化学式: C₁₈H₂₁F₂N₇O
• 分子量: 389.4
• InChiKey: BUWBRTXGQRBBHG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  79.2
• 氢给体数：
  1
• 氢受体数：
  8

文献信息

• [EN] PREPARATION OF A PYRIMIDINYL-3,8-DIAZABICYCLO[3.2.1]OCTANYLMETHANONE DERIVATIVE AND SALT THEREOF<br/>[FR] PRÉPARATION D'UN DÉRIVÉ DE PYRIMIDINYL-3,8-DIAZABICYCLO[3.2.1]OCTANYLMÉTHANONE ET SEL DE CELUI-CI
  申请人：PFIZER

  公开号：WO2022003584A1

  公开（公告）日：2022-01-06

  Methods for preparing ((S)-2,2-difluorocyclopropyl)-((1R,5S)-3-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]-octan-8-yl)methanone and intermediates used in the processes of preparation thereof.

  制备（（S）-2,2-二氟环丙基）-（（1R,5S）-3-（2-（（1-甲基-1H-吡唑-4-基）氨基）嘧啶-4-基）-3,8-二氮杂双环[3.2.1]辛-8-基）甲酮及其制备过程中使用的中间体的方法。
• [EN] STABLE PHARMACEUTICAL TOPICAL FORMULATION CONTAINING IMMUNOSUPPRESSANT FOR TREATING DERMATOLOGICAL CONDITIONS<br/>[FR] FORMULATION TOPIQUE PHARMACEUTIQUE STABLE CONTENANT UN IMMUNOSUPPRESSEUR POUR LE TRAITEMENT D'AFFECTIONS DERMATOLOGIQUES
  申请人：PFIZER

  公开号：WO2022013708A1

  公开（公告）日：2022-01-20

  A topical formulation for use in the treatment of a dermatological condition comprising: a JAK inhibitor in an oil-in-water emulsion; white petrolatum in an amount of 10% by wt; less than 0.7 ppm butyl hydroxytoluene (BHT) by wt.; oleyl alcohol in an amount of 2% by wt.; and an antimicrobial agent. A topical formulation for use in the treatment of a dermatological condition comprising: a JAK inhibitor as an oil in purified water emulsion; white petrolatum in an amount of 10% by wt.; tocopherol in an amount of less than 6.5 ppm; oleyl alcohol in an amount of 2% by wt.; polyethylene glycol 400 in an amount of 10% by wt.; diethylene glycol monoethyl ether in an amount of 15% by wt.; mineral oil in an amount of 5% by wt.; an emulsifying wax in an amount of 10% by wt.; and an antimicrobial agent comprises 2-phenoxyethanol in an amount of 1 % by wt.; wherein the topical formulation is free of BHT and thereby maintains a yellowness index of less than 6 when stored at 40 degrees C for 16 weeks and not more than 10 when stored for 24 weeks at 40 degrees C. Said composition for use in treating or preventing a disease or condition selected from psoriasis, atopic dermatitis, atopic eczema, chronic hand eczema, uticaria, vitiligo, cutaneous lupus and alopecia areata.