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公开(公告)号：US20240293408A1
公开(公告)日：2024-09-05
申请号：US18372398
申请日：2023-09-25
申请人： Pharmacyclics LLC
IPC分类号： A61K31/519 , A61K31/5377 , A61K31/56 , A61K35/17 , A61K35/28 , A61K38/13 , A61K45/06 , A61P35/00 , A61P35/02 , A61P43/00
CPC分类号： A61K31/519 , A61K31/5377 , A61K31/56 , A61K35/17 , A61K38/13 , A61K45/06 , A61P35/00 , A61P35/02 , A61P43/00 , A61K35/28
摘要： Described herein are methods for treating and preventing graft versus host disease using ACK inhibitors. The methods include administering to an individual in need thereof an ACK inhibitor such as ibrutinib for treating and preventing graft versus host disease.
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公开(公告)号：US20240065971A1
公开(公告)日：2024-02-29
申请号：US17881302
申请日：2023-08-04
申请人： Pharmacyclics LLC
IPC分类号： A61K9/00 , A61K31/519 , C12Q1/6886
CPC分类号： A61K9/0053 , A61K31/519 , C12Q1/6886
摘要： 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).
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公开(公告)号：US20220098200A1
公开(公告)日：2022-03-31
申请号：US17177852
申请日：2021-02-17
发明人： Cyril Ben Haim , Wei Chen , Erick Goldman , Andras Horvath , Philip Pye , Mark S. Smyth , Erik J. Verner
IPC分类号： C07D487/04
摘要： 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.
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公开(公告)号：US20210070748A1
公开(公告)日：2021-03-11
申请号：US16514544
申请日：2019-07-17
申请人： Pharmacyclics LLC
发明人： Gordana B. Atallah , Wei Chen , Zhaozhong J. Jia , Alfonso Pozzan , Luca F. Raveglia , Riccardo Zanaletti
IPC分类号： 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
摘要： 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.
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公开(公告)号：US20200368235A1
公开(公告)日：2020-11-26
申请号：US16529467
申请日：2019-08-01
发明人： 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分类号： 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
摘要： 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.
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公开(公告)号：US10751342B2
公开(公告)日：2020-08-25
申请号：US16748142
申请日：2020-01-21
申请人： Pharmacyclics LLC
发明人： Joseph J. Buggy , Gwen Fyfe , Lee Honigberg , David J. Loury
IPC分类号： 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
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.
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公开(公告)号：US20200223856A1
公开(公告)日：2020-07-16
申请号：US16837665
申请日：2020-04-01
申请人： Pharmacyclics LLC
发明人： Norbert Purro , Mark S. Smyth , Erick Goldman , David D. Wirth
IPC分类号： C07D487/04 , A61K31/519 , A61K45/06 , A61K9/20 , A61K9/48 , A61J1/03 , A61K9/00 , B65D75/36
摘要： 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.
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公开(公告)号：US20180311153A1
公开(公告)日：2018-11-01
申请号：US15828939
申请日：2017-12-01
申请人： Pharmacyclics LLC
IPC分类号： A61K9/00 , C12Q1/6886 , A61K31/519
CPC分类号： A61K9/0053 , A61K31/519 , C12Q1/6886
摘要： 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).
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公开(公告)号：US10010507B1
公开(公告)日：2018-07-03
申请号：US15909779
申请日：2018-03-01
申请人： Pharmacyclics LLC
发明人： Ching W. Chong , Robert Kuehl , Heow Tan , Harisha Atluri
IPC分类号： A61K31/52 , A61K9/20 , 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.
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公开(公告)号：US20180170940A1
公开(公告)日：2018-06-21
申请号：US15887712
申请日：2018-02-02
申请人： Pharmacyclics LLC
发明人： Norbert Purro , Mark S. Smyth , Erick Goldman , David D. Wirth
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： 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
摘要： 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.
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