4-[8-氨基-3-[(2R)-1-(1-氧代-2-丁炔-1-基)-2-吡咯烷基]咪唑并[1,5-A]吡嗪-1-基]-N-2-吡啶基苯甲酰胺 | 1952316-43-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: 4-[8-氨基-3-[(2R)-1-(1-氧代-2-丁炔-1-基)-2-吡咯烷基]咪唑并[1,5-A]吡嗪-1-基]-N-2-吡啶基苯甲酰胺
• 中文别名: 4-[8-氨基-3-[(2R)-1-(1-氧代-2-丁炔-1-基)-2-吡咯烷基]咪唑并[1,5-a]吡嗪-1-基]-N-2-吡啶基苯甲酰胺
• 英文名称: Acalabrutinib enantiomer
• 英文别名: 4-[8-amino-3-[(2R)-1-but-2-ynoylpyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-N-pyridin-2-ylbenzamide
• CAS: 1952316-43-6
• 化学式: C₂₆H₂₃N₇O₂
• 分子量: 465.5
• InChiKey: WDENQIQQYWYTPO-LJQANCHMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  35
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  119
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• Treatment of pemphigus
  申请人：Principia Biopharma Inc.

  公开号：US10485797B2

  公开（公告）日：2019-11-26

  The present disclosure provides methods of treating with a BTK inhibitor a blistering disease, in particular pemphigus vulgaris or pemphigus folliaceous in a mammal, use of a BTK inhibitor as a replacement therapy for corticosteroid therapy for diseases treatable with a corticosteroid, such as autoimmune or inflammatory disease and in particular where corticosteroids are used as first or second line therapy, and pharmaceutical formulations comprising the same.

  本公开提供了用BTK抑制剂治疗哺乳动物的大疱性疾病，特别是寻常天疱疮或花斑丘疹性天疱疮的方法，用BTK抑制剂作为皮质类固醇疗法的替代疗法治疗可使用皮质类固醇治疗的疾病，如自身免疫性或炎症性疾病，特别是在皮质类固醇被用作一线或二线疗法的情况下，以及包含BTK抑制剂的药物制剂。
• TREATMENT OF PEMPHIGUS
  申请人：PRINCIPIA BIOPHARMA, INC.

  公开号：EP3233103A1

  公开（公告）日：2017-10-25
• COMPOSITIONS FOR ILEO-JEJUNAL DRUG DELIVERY
  申请人：PRINCIPIA BIOPHARMA INC.

  公开号：EP3236943A1

  公开（公告）日：2017-11-01
• [EN] TREATMENT OF PEMPHIGUS<br/>[FR] TRAITEMENT DU PEMPHIGUS
  申请人：GOURLAY STEVEN

  公开号：WO2016100914A1

  公开（公告）日：2016-06-23

  The present disclosure provides methods of treating with a BTK inhibitor a blistering disease, in particular pemphigus vulgaris or pemphigus folliaceous in a mammal, use of a BTK inhibitor as a replacement therapy for corticosteroid therapy for diseases treatable with a corticosteroid, such as autoimmune or inflammatory disease and in particular where corticosteroids are used as first or second line therapy, and pharmaceutical formulations comprising the same.
• [EN] COMPOSITIONS FOR ILEO-JEJUNAL DRUG DELIVERY<br/>[FR] COMPOSITIONS POUR ADMINISTRATION DE MÉDICAMENTS ILÉO-JÉJUNAL.
  申请人：NUNN PHILIP A

  公开号：WO2016105582A1

  公开（公告）日：2016-06-30

  The current invention affords new formulations which deliver reversible and irreversible covalent kinase inhibitors, in particular BTK inhibitors, into the small intestine and specifically into the ileum and jejunum of the small intestine.