公开(公告)号：EP3076975A1

公开(公告)日：2016-10-12

申请号：EP14867905.3

申请日：2014-12-02

申请人： Pharmacyclics, LLC ,  Regents Of The University Of Minnesota

发明人： BLAZAR, Bruce, R. ,  FLYNN, Ryan

IPC分类号： A61K31/519 ,  A61K31/506 ,  A61P37/00 ,  A61P43/00

CPC分类号： A61K31/519 ,  A61K35/28 ,  A61K45/06 ,  A61K2035/124

摘要： Described herein are methods for treating and preventing alloantibody driven chronic graft versus host disease (cGVHD). The methods include administering to an individual in need thereof ibrutinib for treating and preventing alloantibody driven graft versus host disease.

公开(公告)号：EP2650294B1

公开(公告)日：2016-07-20

申请号：EP13166272.8

申请日：2010-10-12

申请人： Pharmacyclics LLC

发明人： Chen, Wei ,  Loury, David J. ,  Mody, Tarak D. ,  Verner, Erik ,  Smyth, Mark Stephen ,  Luo, Wenchen

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P19/02 ,  A61P19/10

CPC分类号： C07D487/04 ,  C07D519/00

公开(公告)号：EP2139487B1

公开(公告)日：2015-11-11

申请号：EP08744513.6

申请日：2008-03-27

申请人： Pharmacyclics LLC

发明人： HONIGBERG, Lee ,  VERNER, Erik ,  BUGGY, Joseph, J. ,  LOURY, David ,  CHEN, Wei

IPC分类号： A61K31/52 ,  A61P29/00 ,  A61P35/00 ,  A61K31/519 ,  C07D253/06 ,  C07D487/04 ,  C07D473/34

CPC分类号： C07D487/04 ,  A61K31/52 ,  C07D471/04 ,  C12Q1/485 ,  G01N33/57426 ,  G01N2440/14 ,  G01N2500/00

公开(公告)号：EP4338738A3

公开(公告)日：2024-06-19

申请号：EP23211155.9

申请日：2016-03-02

申请人： Pharmacyclics LLC

发明人： ATLURI,, Harisha ,  CHONG,, Ching, Wah ,  KUEHL,, Robert ,  TAN,, Heow

IPC分类号： A61K31/436 ,  A61K31/519

CPC分类号： A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2095 ,  A61K31/519 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00

摘要： Described herein are pharmaceutical formulations of 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. Also disclosed are 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.

公开(公告)号：EP4338738A2

公开(公告)日：2024-03-20

申请号：EP23211155.9

申请日：2016-03-02

申请人： Pharmacyclics LLC

发明人： ATLURI,, Harisha ,  CHONG,, Ching, Wah ,  KUEHL,, Robert ,  TAN,, Heow

IPC分类号： A61K31/519

摘要： Described herein are pharmaceutical formulations of 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. Also disclosed are 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.

公开(公告)号：EP3265084A4

公开(公告)日：2018-08-01

申请号：EP16759417

申请日：2016-03-02

申请人： PHARMACYCLICS LLC

发明人： ATLURI HARISHA ,  CHONG CHING WAH ,  KUEHL ROBERT ,  TAN HEOW

IPC分类号： A61K31/436 ,  A61K31/519

CPC分类号： A61K9/2054 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2095 ,  A61K31/519

摘要： Described herein are pharmaceutical formulations of 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. Also disclosed are 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.

公开(公告)号：EP3311818A3

公开(公告)日：2018-07-18

申请号：EP17191704.0

申请日：2009-07-16

申请人： Pharmacyclics, LLC

发明人： HONIGBERG, Lee ,  VERNER, Erik ,  BUGGY, Joseph ,  LOURY, David ,  CHEN, Wei

IPC分类号： A61K31/52 ,  A61P35/00 ,  A61K31/519 ,  A61K31/00 ,  A61K31/675 ,  A61K31/704 ,  A61K33/24 ,  A61K31/19 ,  A61K31/337

CPC分类号： A61K31/519 ,  A61K31/00 ,  A61K31/337 ,  A61K31/52 ,  A61K31/675 ,  A61K31/704 ,  A61K33/24 ,  A61K39/3955 ,  A61K39/39558 ,  A61K45/06 ,  A61K2300/00 ,  A61K31/19

摘要： Described herein are irreversible Btk inhibitor compounds, and methods for using such irreversible inhibitors in the treatment of diseases and disorders characterized by the presence or development of solid tumors.

公开(公告)号：EP3226864A4

公开(公告)日：2018-04-04

申请号：EP15864946

申请日：2015-12-02

申请人： PHARMACYCLICS LLC

发明人： GONZALEZ TONI JAUSET ,  MASSO VALLES DANIEL ,  SOUCEK LAURA

IPC分类号： A61K31/445 ,  A61P35/00 ,  C07D487/04 ,  C09B31/147

CPC分类号： A61K31/519 ,  A61K31/7068 ,  C09B31/147 ,  A61K2300/00

摘要： Disclosed are methods of treating fibrosis in a patient, comprising administering to a patient in need thereof a therapeutically effective amount of an ACK inhibitor (e.g., a BTK inhibitor, such as for example an irreversible BTK inhibitor, such as for example, ibrutinib).

公开(公告)号：EP3177366A4

公开(公告)日：2018-04-04

申请号：EP15829601

申请日：2015-08-06

申请人： PHARMACYCLICS LLC ,  JANSSEN PHARMACEUTICA NV

发明人： BALASUBRAMANIAN SRIRAM ,  KUO HSU PING ,  HSIEH HSIN KANG ,  CHANG BETTY ,  XUE LING ,  CHEUNG LEO

IPC分类号： A61P35/02 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/426 ,  A61K31/454 ,  A61K31/519 ,  A61K31/69 ,  A61K38/00 ,  A61K38/19 ,  A61K38/20 ,  A61K38/21 ,  A61K38/31 ,  A61K45/06

CPC分类号： A61K31/519 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/426 ,  A61K31/454 ,  A61K31/69 ,  A61K38/005 ,  A61K38/191 ,  A61K38/2013 ,  A61K38/21 ,  A61K45/06 ,  A61K2300/00 ,  A61K38/31

摘要： Disclosed herein are methods, compositions, and kits for treating a B-cell malignancy comprising administering a combination of a BTK inhibitor (e.g. ibrutinib) and a PIM inhibitor. Also disclosed herein are methods, compositions, and kits for treating a BTK-resistant B-cell malignancy comprising administering a combination of a BTK inhibitor (e.g. ibrutinib) and a PIM inhibitor.

公开(公告)号：EP3119910A4

公开(公告)日：2018-02-21

申请号：EP15764524

申请日：2015-03-20

申请人： PHARMACYCLICS LLC

发明人： BYRD JOHN C ,  WOYACH JENNIFER A

IPC分类号： C12Q1/68

CPC分类号： C12Q1/6886 ,  A61K31/519 ,  C12Q2600/106 ,  C12Q2600/156 ,  G01N33/57426 ,  G01N2333/916 ,  G01N2800/52

摘要： Described herein is a mutation that confers resistance to the treatment with a BTK inhibitor. Described herein is a modified PLCγ2 polypeptide that is modified at amino acid position 742, 845, or 1140 and the modified PLCγ2 polypeptide exhibits decreased inhibition (e.g., resistance) to a covalent and/or irreversible BTK inhibitor. Described herein are diagnostic methods for detecting the modified polypeptide and nucleic acid encoding the modified polypeptide and applications of the methods thereof. Described herein are compositions, combinations, and kits containing the modified polypeptide and methods of using the modified polypeptide. Also described herein are methods of using the modified polypeptide as screening agents for the identification and design of inhibitors of PLCγ2.