公开(公告)号：EP2755648A1

公开(公告)日：2014-07-23

申请号：EP11872389.9

申请日：2011-09-13

申请人： Pharmacyclics, Inc. ,  Les Laboratoires Servier SAS

发明人： LOURY, David, J. ,  BUGGY, Joseph, J. ,  MODY, Tarak, D. ,  VERNER, Erik, J. ,  PURRO, Norbert ,  BALASUBRAMANIAN, Sriram ,  KLOOS, Ioana ,  DEPIL, Stéphane

IPC分类号： A61K31/343 ,  A61K31/166 ,  A61K31/16 ,  A61P35/00

CPC分类号： A61K31/343 ,  A61K9/14 ,  A61K9/28 ,  A61K9/70 ,  A61K31/4184 ,  A61K2300/00

摘要： Dosing regimens, methods of treatment, controlled release formulations, and combination therapies that include bendamustine, or a pharmaceutically acceptable salt thereof and an HDAC inhibitor, or a pharmaceutically acceptable salt thereof, are described.

公开(公告)号：EP2920180A1

公开(公告)日：2015-09-23

申请号：EP13854424.2

申请日：2013-11-14

申请人： Pharmacyclics, Inc.

发明人： CHEN, Wei ,  LOURY, David, J. ,  WANG, Longcheng

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P37/00 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07D487/04 ,  A61K31/519

摘要： Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, 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.

摘要翻译： 本文公开了与布鲁顿酪氨酸激酶（Btk）形成共价键的化合物。 还描述了Btk的不可逆抑制剂。 另外，还描述了Btk的可逆抑制剂。 还公开了包含该化合物的药物组合物。 单独或与其他治疗剂组合使用Btk抑制剂的方法用于治疗自身免疫疾病或病症，异质性免疫疾病或病症，癌症（包括淋巴瘤）和炎性疾病或病症。

公开(公告)号：EP2731612A2

公开(公告)日：2014-05-21

申请号：EP12811600.1

申请日：2012-07-13

申请人： Pharmacyclics, Inc.

发明人： CHEN, Wei ,  LOURY, David, J. ,  MODY, Tarak, D. ,  WANG, Longcheng

IPC分类号： A61K31/52 ,  A61K31/433 ,  C07D473/34 ,  C07D473/32 ,  A61P17/00 ,  A61P29/00

CPC分类号： C07D487/04 ,  A61K31/52 ,  C07D473/34

摘要： Described herein are kinase inhibitor compounds, methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate inhibitor of a protein, including a kinase.

公开(公告)号：EP2809672A1

公开(公告)日：2014-12-10

申请号：EP13743025.2

申请日：2013-01-30

申请人： Pharmacyclics, Inc.

发明人： YAN, Shunqi ,  WANG, Longcheng ,  FRYE, Leah, Lynn ,  CHEN, Wei ,  LOURY, David, J.

IPC分类号： C07D473/32 ,  A61K31/52 ,  A61P37/00 ,  A61P35/00

CPC分类号： C07D473/34

摘要： Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, 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.

公开(公告)号：EP2575818A2

公开(公告)日：2013-04-10

申请号：EP11790524.0

申请日：2011-06-03

申请人： Pharmacyclics, Inc.

发明人： BUGGY, Joseph, J. ,  ELIAS, Laurence ,  FYFE, Gwen ,  HEDRICK, Eric ,  LOURY, David, J. ,  MODY, Tarak, D.

IPC分类号： A61K31/519 ,  A61K31/505 ,  A61P35/02 ,  A61P35/00

CPC分类号： A61K31/519 ,  A61K9/0014 ,  A61K9/0031 ,  A61K9/0048 ,  A61K9/0056 ,  A61K9/007 ,  A61K9/06 ,  A61K31/195 ,  A61K31/337 ,  A61K31/4184 ,  A61K31/436 ,  A61K31/437 ,  A61K31/454 ,  A61K31/4745 ,  A61K31/475 ,  A61K31/573 ,  A61K31/606 ,  A61K31/664 ,  A61K31/675 ,  A61K31/69 ,  A61K31/7032 ,  A61K31/704 ,  A61K31/7076 ,  A61K39/395 ,  A61K39/39533 ,  A61K39/3955 ,  A61K45/06 ,  C07D487/04 ,  A61K2300/00

摘要： Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.