Patents by Inventor Paul Kwiatkowski
Paul Kwiatkowski has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 10870651Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g.Type: GrantFiled: December 23, 2015Date of Patent: December 22, 2020Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Yanke Liang, Tinghu Zhang, Nicholas Paul Kwiatkowski
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Publication number: 20200361906Abstract: The present invention provides novel compounds of Formulae (I?) and (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g.Type: ApplicationFiled: November 22, 2017Publication date: November 19, 2020Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Tinghu Zhang, Baishan Jiang, Nicholas Paul Kwiatkowski
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Publication number: 20200360381Abstract: The present disclosure provides antiviral (e.g., anti-Dengue virus) agents, such as compounds of Formula (I). Also provided are pharmaceutical compositions and kits of the compounds of Formula (I). Further provided are methods and uses of the antiviral agents (e.g., the compounds of Formula (I); and compounds K786-9739, S4105, C200-5340, G199-0398, C200-9144, S7337, S1633, and C066-4182, and derivatives thereof) for treating or preventing a viral infection (e.g., Dengue fever). The antiviral agents may inhibit the entry of a virus into a cell by, e.g., inhibiting the fusion between the envelope of the virus and the membrane of the cell.Type: ApplicationFiled: May 15, 2018Publication date: November 19, 2020Applicants: Dana-Farber Cancer Institute, Inc., President and Fellows of Harvard CollegeInventors: Priscilla L. Yang, Wenlong Lian, Nathanael S. Gray, Nicholas Paul Kwiatkowski, Jinhua Wang, Jaebong Jang
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Patent number: 10787436Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma, lung cancer), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.Type: GrantFiled: September 13, 2018Date of Patent: September 29, 2020Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael Gray, Tinghu Zhang, Nicholas Paul Kwiatkowski
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Publication number: 20200277292Abstract: The present invention provides novel compounds of Formula (I), (II), or (III), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g.Type: ApplicationFiled: February 3, 2020Publication date: September 3, 2020Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Tinghu Zhang, Nicholas Paul Kwiatkowski
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Patent number: 10684829Abstract: A system and method for combining text editing and tree encoding for computer programs and related software. Source code for programs and the like are stored using a maintaining a structured tree representation comprising a plurality of nodes, including nodes associated with respective identifiers, operands, operators, variables, and flow control elements in the source code, and nodes associated with formatting aspects of a text-based representation of the source code.Type: GrantFiled: June 12, 2017Date of Patent: June 16, 2020Assignee: INTENTIONAL SOFTWARE CORPORATIONInventors: David Waggoner, Melanie A. Jensenworth, Paul Kwiatkowski, Charles Simonyi
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Publication number: 20200172499Abstract: The present invention provides novel compounds of Formulae (I?), (I), (II?), and (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g.Type: ApplicationFiled: September 9, 2016Publication date: June 4, 2020Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Tinghu Zhandg, Nicholas Paul Kwiatkowski, Mingfeng Hao
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Patent number: 10570154Abstract: The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), polo kinase 1, 2, 3, or 4, Ack1, Ack2, Abl, DCAMKL1, ABL1, Abl mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.Type: GrantFiled: August 22, 2018Date of Patent: February 25, 2020Assignee: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael S. Gray, Xianming Deng, Nicholas Paul Kwiatkowski
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Patent number: 10550121Abstract: The present invention provides novel compounds of Formula (I), (II), or (III), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g.Type: GrantFiled: March 25, 2016Date of Patent: February 4, 2020Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Tinghu Zhang, Nicholas Paul Kwiatkowski
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Publication number: 20200017475Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma, lung cancer), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.Type: ApplicationFiled: September 13, 2018Publication date: January 16, 2020Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael Gray, Tinghu Zhang, Nicholas Paul Kwiatkowski
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Publication number: 20190315747Abstract: The present invention provides novel compounds of Formula (I), (II), or (III), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g.Type: ApplicationFiled: March 25, 2016Publication date: October 17, 2019Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Tinghu Zhang, Nicholas Paul Kwiatkowski
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Publication number: 20190100511Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma, lung cancer), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.Type: ApplicationFiled: September 13, 2018Publication date: April 4, 2019Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael Gray, Tinghu Zhang, Nicholas Paul Kwiatkowski
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Publication number: 20190055248Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g.Type: ApplicationFiled: December 23, 2015Publication date: February 21, 2019Inventors: Nathanael S. Gray, Yanke Liang, Tinghu Zhang, Nicholas Paul Kwiatkowski
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Patent number: 10172905Abstract: The invention relates to methods of treating protein degradation disorders, such cellular proliferative disorders (e.g., cancer) and protein deposition disorders (e.g., neurodegenerative disorders). The invention provides methods and pharmaceutical compositions for treating these diseases using aggresome inhibitors or combinations of aggresome inhibitors and proteasome inhibitors. The invention further relates to methods and pharmaceutical compositions for treating multiple myeloma. New HDAC/TDAC inhibitors and aggresome inhibitors are also provided as well as synthetic methodologies for preparing these compounds.Type: GrantFiled: January 9, 2017Date of Patent: January 8, 2019Assignees: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.Inventors: Kenneth C. Anderson, James E. Bradner, Edward Franklin Greenberg, Teru Hideshima, Nicholas Paul Kwiatkowski, Ralph Mazitschek, Stuart L. Schreiber, Jared Shaw, Stephen J. Haggarty
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Publication number: 20180362545Abstract: The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), polo kinase 1, 2, 3, or 4, Ack1, Ack2, Abl, DCAMKL1, ABL1, Abl mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.Type: ApplicationFiled: August 22, 2018Publication date: December 20, 2018Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Xianming Deng, Nicholas Paul Kwiatkowski
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Publication number: 20180362483Abstract: The present invention provides novel compounds of Formulae (I?), (I), (II?), and (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g.Type: ApplicationFiled: September 9, 2016Publication date: December 20, 2018Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Tinghu Zhandg, Nicholas Paul Kwiatkowski, Mingfeng Hao
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Patent number: 10112927Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma, lung cancer), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.Type: GrantFiled: October 18, 2013Date of Patent: October 30, 2018Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael Gray, Tinghu Zhang, Nicholas Paul Kwiatkowski
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Patent number: 10081639Abstract: The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), polo kinase 1, 2, 3, or 4, Ack1, Ack2, Abl, DCAMKL1, ABL1, Abl mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.Type: GrantFiled: May 25, 2017Date of Patent: September 25, 2018Assignee: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael S. Gray, Xianming Deng, Nicholas Paul Kwiatkowski
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Publication number: 20170315787Abstract: A system and method for combining text editing and tree encoding for computer programs and related software. Source code for programs and the like are stored using a maintaining a structured tree representation comprising a plurality of nodes, including nodes associated with respective identifiers, operands, operators, variables, and flow control elements in the source code, and nodes associated with formatting aspects of a text-based representation of the source code.Type: ApplicationFiled: June 12, 2017Publication date: November 2, 2017Applicant: Intentional Software CorporationInventors: David Waggoner, Melanie A. Jensenworth, Paul Kwiatkowski, Charles Simonyi
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Publication number: 20170260208Abstract: The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), polo kinase 1, 2, 3, or 4, Ack1, Ack2, Abl, DCAMKL1, ABL1, Abl mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.Type: ApplicationFiled: May 25, 2017Publication date: September 14, 2017Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Xianming Deng, Nicholas Paul Kwiatkowski