US9572811, Example 139A

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: US9572811, Example 139A
• 英文别名: (E)-2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-3-[1-(diethylaminomethyl)cyclopentyl]prop-2-enenitrile
• 化学式: C₃₆H₄₁FN₈O₂
• 分子量: 636.8
• InChiKey: BTWNIXPKIHIIBT-ZQBMCQTHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.9
• 重原子数：
  47
• 可旋转键数：
  10
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  126
• 氢给体数：
  1
• 氢受体数：
  9

文献信息

• [EN] TREATMENT OF DRY EYE<br/>[FR] TRAITEMENT DE LA SÉCHERESSE OCULAIRE
  申请人：PRINCIPIA BIOPHARMA INC

  公开号：WO2014022569A1

  公开（公告）日：2014-02-06

  The present disclosure provides a method of treating dry eye by inhibition of Bruton's tyrosine kinase (hereinafter "BTK") inhibitors, pharmaceutical formulations comprising the same, and processes for preparing such compounds.

  本公开提供了一种通过抑制Bruton酪氨酸激酶（以下简称“BTK”）抑制剂来治疗干眼症的方法，包括含有该抑制剂的药物配方，以及制备这些化合物的过程。
• TYROSINE KINASE INHIBITORS
  申请人：Principia Biopharma, Inc.

  公开号：US20140303161A1

  公开（公告）日：2014-10-09

  The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.

  本公开提供的化合物及其药学上可接受的盐是酪氨酸激酶抑制剂，特别是BLK、BMX、EGFR、HER2、HER4、ITK、TEC、BTK和TXK，因此可用于治疗通过抑制酪氨酸激酶的疾病，如癌症和炎症性疾病，如关节炎等。还提供了包含这些化合物及其药学上可接受的盐的制药组合物以及制备这些化合物及其药学上可接受的盐的过程。
• TREATMENT OF DRY EYE
  申请人：PRINCIPIA BIOPHARMA INC.

  公开号：US20150182530A1

  公开（公告）日：2015-07-02

  The present disclosure provides a method of treating dry eye by inhibition of Bruton's tyrosine kinase (hereinafter “BTK”) inhibitors, pharmaceutical formulations comprising the same, and processes for preparing such compounds.

  本公开提供一种通过抑制布鲁顿酪氨酸激酶（以下简称“BTK”）抑制剂治疗干眼症的方法，包括该抑制剂的制药配方以及制备这些化合物的过程。
• FORMULATIONS CONTAINING REVERSIBLE COVALENT COMPOUNDS
  申请人：PRINCIPIA BIOPHARMA INC.

  公开号：US20160045503A1

  公开（公告）日：2016-02-18

  Oral pharmaceutical formulations comprising reversible covalent compounds having a Michael acceptor moiety, a process of their production and use of these formulations for the treatment of diseases treatable by such compounds such as cancer and autoimmune diseases.

  口服药物制剂包括具有Michael受体基团的可逆共价化合物，其生产过程以及利用这些制剂治疗可通过此类化合物治疗的疾病，例如癌症和自身免疫性疾病。
• 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。