公开(公告)号：US20150158871A1

公开(公告)日：2015-06-11

申请号：US14405317

申请日：2013-06-03

Applicant: PHARMACYCLICS, INC.

Inventor： Norbert Purro ,  Mark Smyth ,  Erick Goldman ,  David D. Wirth

IPC: C07D487/04 ,  A61K45/06 ,  A61K31/519

CPC classification number: C07D487/04 ,  A61J1/035 ,  A61K9/0053 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/4825 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/519 ,  A61K45/06 ,  B65D75/36 ,  C07B2200/13 ,  A61K2300/00

Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Abstract translation: 本文描述了Bruton的酪氨酸激酶（Btk）抑制剂1 - （（R）-3-（4-氨基-3-（4-苯氧基苯基）-1H-吡唑并[3,4-d]嘧啶-1-基）哌啶 -1-基）丙-2-烯-1-酮，包括结晶形式，溶剂化物和药学上可接受的盐。 还公开了包括Btk抑制剂的药物组合物，以及使用Btk抑制剂单独或与其它治疗剂组合用于治疗自身免疫疾病或病症，异种免疫疾病或病症，癌症（包括淋巴瘤）和 炎性疾病或病症。