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公开(公告)号：US10806712B2
公开(公告)日：2020-10-20
申请号：US16297986
申请日：2019-03-11
申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC. , UNIVERSITY OF SOUTH FLORIDA , UNIVERSITY OF CENTRAL FLORIDA RESEARCH FOUNDATION, INC.
发明人： James Turkson , Said M. Sebti , Wayne Guida , Man Lun Yip , Nicholas Lawrence , Harshani Rithma Lawrence , Benjamin Greedy
IPC分类号： A61K31/192 , A61K31/015 , A61K31/196 , A61K31/00 , A61K31/18 , A61K45/06 , G01N33/50 , G01N33/574 , C07C235/84 , C07C309/73 , C07C311/19
摘要： The present invention concerns compounds, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of Stat3 signaling, Stat3 dimerization, Stat3-DNA binding, Stat5-DNA binding, and/or aberrant cell growth in vitro or in vivo, e.g., as anti-cancer agents for treatment of cancer, such as breast cancer. The compounds of the invention include, but are not limited to, NSC 74859 (S3I-201), NSC 42067, NSC 59263, NSC 75912, NSC 11421, NSC 91529, NSC 263435, and pharmaceutically acceptable salts and analogs of the foregoing. Other non-malignant diseases characterized by proliferation of cells that may be treated using the compounds of the invention, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis. The invention further includes an in-vitro screening test for the presence of malignant cells in a mammalian tissue; a method of identifying inhibitors of constitutive Stat3 activation, Stat3-DNA binding, Stat5-DNA binding, and/or Stat3 dimerization; and a method of identifying anti-cancer agents.
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公开(公告)号：US11987568B2
公开(公告)日：2024-05-21
申请号：US17265649
申请日：2019-08-02
发明人： Nupam Mahajan , Nicholas Lawrence
IPC分类号： C07D333/38
CPC分类号： C07D333/38
摘要： Disclosed is a method for selecting a cancer therapeutic for a patient that involves assaying a tumor biopsy sample from the subject to detect PAXIP1 expression, and selecting a WEE1 inhibitor as the cancer therapeutic if PAXIP1 is detected in the tumor biopsy sample.
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公开(公告)号：US10226439B2
公开(公告)日：2019-03-12
申请号：US15468460
申请日：2017-03-24
申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC. , UNIVERSITY OF SOUTH FLORIDA , UNIVERSITY OF CENTRAL FLORIDA RESEARCH FOUNDATION, INC.
发明人： James Turkson , Said M. Sebti , Wayne Guida , Man Lun Yip , Nicholas Lawrence , Harshani Rithma Lawrence , Benjamin Greedy
IPC分类号： A61K31/196 , A61K31/00 , A61K31/18 , A61K45/06 , G01N33/50 , G01N33/574 , C07C235/84 , C07C309/73 , C07C311/19
摘要： The present invention concerns compounds, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of Stat3 signaling, Stat3 dimerization, Stat3-DNA binding, Stat5-DNA binding, and/or aberrant cell growth in vitro or in vivo, e.g., as anti-cancer agents for treatment of cancer, such as breast cancer. The compounds of the invention include, but are not limited to, NSC 74859 (S3I-201), NSC 42067, NSC 59263, NSC 75912, NSC 11421, NSC 91529, NSC 263435, and pharmaceutically acceptable salts and analogs of the foregoing. Other non-malignant diseases characterized by proliferation of cells that may be treated using the compounds of the invention, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis. The invention further includes an in-vitro screening test for the presence of malignant cells in a mammalian tissue; a method of identifying inhibitors of constitutive Stat3 activation, Stat3-DNA binding, Stat5-DNA binding, and/or Stat3 dimerization; and a method of identifying anti-cancer agents.
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公开(公告)号：US12060332B2
公开(公告)日：2024-08-13
申请号：US18098990
申请日：2023-01-19
发明人： Brian Betts , Said M. Sebti , Harshani Lawrence , Nicholas Lawrence , Claudio Anasetti , Joseph Pidala
IPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61K45/06 , A61P35/00 , C07D401/12 , C07D403/12
CPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61K45/06 , A61P35/00 , C07D401/12 , C07D403/12
摘要： Disclosed herein are compounds and methods for reducing the risk of developing, preventing, or treating graft versus host disease (GVHD) in a subject. The compounds can concurrently block Aurora kinase A and JAK2 signal transduction which synergistically suppresses alloreactive human T-cells in vitro, prevents xenogeneic graft-versus-host disease without impairing anti-tumor responses, and promotes the development and suppressive potency of CD39+ inducible Treg. In certain aspects, disclosed are compounds of Formula I-V.
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公开(公告)号：US11203576B2
公开(公告)日：2021-12-21
申请号：US16083681
申请日：2017-03-13
发明人： Brian Betts , Said M. Sebti , Harshani Lawrence , Nicholas Lawrence , Claudio Anasetti , Joseph Pidala
IPC分类号： A61K31/505 , C07D239/48 , C07D401/12 , C07D403/12 , A61P35/00 , A61K31/506 , A61K45/06
摘要： Disclosed herein are compounds and methods for reducing the risk of developing, preventing, or treating graft versus host disease (GVHD) in a subject. The compounds can concurrently block Aurora kinase A and JAK2 signal transduction which synergistically suppresses alloreactive human T-cells in vitro, prevents xenogeneic graft-versus-host disease without impairing anti-tumor responses, and promotes the development and suppressive potency of CD39+ inducible Treg. In certain aspects, disclosed are compounds of Formula I-V.
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公开(公告)号：US20190127335A1
公开(公告)日：2019-05-02
申请号：US16083681
申请日：2017-03-13
发明人： Brian Betts , Said Sebti , Harshani Lawrence , Nicholas Lawrence , Claudio Anasetti , Joseph Pidala
IPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , A61P35/00
摘要： Disclosed herein are compounds and methods for reducing the risk of developing, preventing, or treating graft versus host disease (GVHD) in a subject. The compounds can concurrently block Aurora kinase A and JAK2 signal transduction which synergistically suppresses alloreactive human T-cells in vitro, prevents xenogeneic graft-versus-host disease without impairing anti-tumor responses, and promotes the development and suppressive potency of CD39+ inducible Treg. In certain aspects, disclosed are compounds of Formula I-V.
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公开(公告)号：US20220281828A1
公开(公告)日：2022-09-08
申请号：US17555786
申请日：2021-12-20
发明人： Brian Betts , Said M. Sebti , Harshani Lawrence , Nicholas Lawrence , Claudio Anasetti , Joseph Pidala
IPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , A61P35/00 , A61K31/506 , A61K31/505 , A61K45/06
摘要： Disclosed herein are compounds and methods for reducing the risk of developing, preventing, or treating graft versus host disease (GVHD) in a subject. The compounds can concurrently block Aurora kinase A and JAK2 signal transduction which synergistically suppresses alloreactive human T-cells in vitro, prevents xenogeneic graft-versus-host disease without impairing anti-tumor responses, and promotes the development and suppressive potency of CD39+ inducible Treg. In certain aspects, disclosed are compounds of Formula I-V.
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公开(公告)号：US09604923B2
公开(公告)日：2017-03-28
申请号：US14246522
申请日：2014-04-07
申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC. , UNIVERSITY OF SOUTH FLORIDA , UNIVERSITY OF CENTRAL FLORIDA
发明人： James Turkson , Said M. Sebti , Wayne Guida , Man Lun Yip , Nicholas Lawrence , Harshani Rithma Lawrence , Benjamin Greedy
IPC分类号： C07C309/73 , C07C311/19 , A61K31/00 , A61K31/18 , A61K45/06 , G01N33/50 , G01N33/574 , C07C235/84
CPC分类号： A61K31/196 , A61K31/00 , A61K31/18 , A61K45/06 , C07C235/84 , C07C309/73 , C07C311/19 , G01N33/5011 , G01N33/5088 , G01N33/574 , G01N33/57407 , G01N33/57484 , A61K2300/00
摘要： The present invention concerns compounds, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of Stat3 signaling, Stat3 dimerization, Stat3-DNA binding, Stat5-DNA binding, and/or aberrant cell growth in vitro or in vivo, e.g., as anti-cancer agents for treatment of cancer, such as breast cancer. The compounds of the invention include, but are not limited to, NSC 74859 (S31-201), NSC 42067, NSC 59263, NSC 75912, NSC 11421, NSC 91529, NSC 263435, and pharmaceutically acceptable salts and analogs of the foregoing. Other non-malignant diseases characterized by proliferation of cells that may be treated using the compounds of the invention, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis. The invention further includes an in-vitro screening test for the presence of malignant cells in a mammalian tissue; a method of identifying inhibitors of constitutive Stat3 activation, Stat3-DNA binding, Stat5-DNA binding, and/or Stat3 dimerization; and a method of identifying anti-cancer agents.
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公开(公告)号：US20170044127A1
公开(公告)日：2017-02-16
申请号：US15113500
申请日：2015-01-23
发明人： Sheng Wei , Alan List , Nicholas Lawrence
IPC分类号： C07D311/30 , C07H17/07 , C07D239/91
CPC分类号： C07D311/30 , C07D239/91 , C07D311/62 , C07H17/07
摘要： Disclosed are derivatives of icariin. Disclosed are compounds having Formula I-VIII as defined herein. Methods of using these compounds for the treatment of cancer and inflammation are also disclosed.
摘要翻译： 披露的是淫羊藿苷的衍生物。 公开了具有本文定义的式I-VIII的化合物。 还公开了使用这些化合物治疗癌症和炎症的方法。
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