公开(公告)号：US20220098200A1

公开(公告)日：2022-03-31

申请号：US17177852

申请日：2021-02-17

Applicant: Pharmacyclics LLC ,  Janssen Pharmaceutica NV

Inventor： Cyril Ben Haim ,  Wei Chen ,  Erick Goldman ,  Andras Horvath ,  Philip Pye ,  Mark S. Smyth ,  Erik J. Verner

IPC: C07D487/04

Abstract: Described herein is the synthesis 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.

公开(公告)号：US20210070748A1

公开(公告)日：2021-03-11

申请号：US16514544

申请日：2019-07-17

Applicant: Pharmacyclics LLC

Inventor： Gordana B. Atallah ,  Wei Chen ,  Zhaozhong J. Jia ,  Alfonso Pozzan ,  Luca F. Raveglia ,  Riccardo Zanaletti

IPC: C07D417/14 ,  C07D403/04 ,  A61P19/10 ,  A61P29/00 ,  A61P35/02 ,  A61P19/02 ,  A61P37/02 ,  C07D471/08 ,  C07D471/04 ,  C07D409/14 ,  C07D401/04 ,  C07D413/14 ,  C07D405/14 ,  C07D401/14

Abstract: Disclosed herein are reversible and irreversible inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are described, 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：US20200368235A1

公开(公告)日：2020-11-26

申请号：US16529467

申请日：2019-08-01

Applicant: Pharmacyclics LLC ,  Janssen Pharmaceutica NV

Inventor： Betty Chang ,  Sriram Balasubramanian ,  Richard Crowley ,  Hsu-Ping Kuo ,  Brett Hall ,  Kate A. Sasser ,  Tineke Casneuf ,  Michael Schaffer ,  Matthias Versele ,  Willem Ligtenberg ,  Cue Davis

IPC: A61K31/519 ,  A61K45/06 ,  A61K31/454 ,  A61K31/496 ,  A61K31/282 ,  A61K31/395 ,  A61K31/4439 ,  A61K31/4745 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/573 ,  A61K31/664 ,  A61K31/704 ,  A61K31/7048 ,  A61K31/7068 ,  A61K39/395

Abstract: Combinations of Bruton's tyrosine kinase (Btk) inhibitors, e.g., 1-((R)-3-(4-amino-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, with a second anticancer agent are provided. Also provided are methods of treating cancers, and autoimmune disorders by administering combinations of Bruton's tyrosine kinase (Btk) inhibitors, e.g., 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, and second anticancer agents.

公开(公告)号：US10751342B2

公开(公告)日：2020-08-25

申请号：US16748142

申请日：2020-01-21

Applicant: Pharmacyclics LLC

Inventor： Joseph J. Buggy ,  Gwen Fyfe ,  Lee Honigberg ,  David J. Loury

IPC: A61K31/519 ,  A61K9/48 ,  A61K9/00 ,  A61K39/395 ,  A61K31/664 ,  A61K31/437 ,  A61K31/337 ,  C07D487/04 ,  A61K31/7032 ,  A61K31/4745 ,  A61K31/4184 ,  A61K45/06 ,  A61K31/7076 ,  A61K31/704 ,  A61K31/69 ,  A61K31/675 ,  A61K31/606 ,  A61K31/573 ,  A61K31/475 ,  A61K31/454 ,  A61K31/436 ,  A61K31/195 ,  A61K47/26 ,  A61K47/38 ,  A61K47/14 ,  A61K47/36 ,  A61K47/20 ,  A61K47/10 ,  A61K47/12 ,  A61K9/06

Abstract: 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.

公开(公告)号：US20200223856A1

公开(公告)日：2020-07-16

申请号：US16837665

申请日：2020-04-01

Applicant: Pharmacyclics LLC

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

IPC: C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61K9/20 ,  A61K9/48 ,  A61J1/03 ,  A61K9/00 ,  B65D75/36

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.

公开(公告)号：US20180311153A1

公开(公告)日：2018-11-01

申请号：US15828939

申请日：2017-12-01

Applicant: Pharmacyclics LLC

Inventor： Joseph J. Buggy ,  Louis M. Staudt ,  Wyndham H. Wilson

IPC: A61K9/00 ,  C12Q1/6886 ,  A61K31/519

CPC classification number: A61K9/0053 ,  A61K31/519 ,  C12Q1/6886

Abstract: Disclosed herein are methods for treating an individual diagnosed with ABC-DLBCL. The methods include administering to the individual an inhibitor of Bruton's tyrosine kinase (Btk).

公开(公告)号：US10010507B1

公开(公告)日：2018-07-03

申请号：US15909779

申请日：2018-03-01

Applicant: Pharmacyclics LLC

Inventor： Ching W. Chong ,  Robert Kuehl ,  Heow Tan ,  Harisha Atluri

IPC: A61K31/52 ,  A61K9/20 ,  A61K31/519

CPC classification number: A61K9/2054 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2095 ,  A61K31/519

Abstract: 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：US20180170940A1

公开(公告)日：2018-06-21

申请号：US15887712

申请日：2018-02-02

Applicant: Pharmacyclics LLC

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

IPC: C07D487/04 ,  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.

公开(公告)号：US20180071293A1

公开(公告)日：2018-03-15

申请号：US15650830

申请日：2017-07-14

Applicant: Pharmacyclics LLC

Inventor： Joseph J. Buggy ,  Tarak D. Mody ,  Richard B. Love ,  John C. Byrd ,  Betty Y. Chang ,  Jason A. Dubovsky ,  Natarajan Muthusamy ,  Amy J. Johnson

IPC: A61K31/519 ,  A61K45/06

CPC classification number: A61K31/519 ,  A61K45/06 ,  A61K2300/00

Abstract: Described herein are methods and compositions comprising a covalent TEC family kinase inhibitor for use in adjuvant therapy, including adjuvant cancer therapy, vaccination and treatment of immune disorders and pathogenic infections.

公开(公告)号：US20180037583A1

公开(公告)日：2018-02-08

申请号：US15466472

申请日：2017-03-22

Applicant: Pharmacyclics LLC

Inventor： Wei Chen ,  Zhaozhong J. Jia ,  David J. Loury

IPC: C07D473/34 ,  A61K31/52

CPC classification number: C07D473/34 ,  A61K31/52

Abstract: 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.