Patents by Inventor Tinghu Zhang
Tinghu Zhang 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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Publication number: 20190092768Abstract: The present application provides bifunctional compounds of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 4 (CDK4) and/or cyclin-dependent kinase 6 (CDK6). The present application also relates to methods for the targeted degradation of CDK4 and/or CDK6 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK4 and/or CDK6 which can be utilized in the treatment of disorders modulated by CDK4 and/or CDK6.Type: ApplicationFiled: April 21, 2017Publication date: March 28, 2019Inventors: Nathanael S. GRAY, Tinghu ZHANG, Calla M. OLSON, Yanke LIANG, Nicholas 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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Publication number: 20190031642Abstract: 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 a cyclin-dependent kinase (CDK) (e.g.Type: ApplicationFiled: August 1, 2018Publication date: January 31, 2019Inventors: Nathanael Gray, Tinghu Zhang, Stephane Ciblat, Melissa Leblanc, Jason J. Marineau, Joel Moore, Kevin Sprott, M. Arshad Siddiqui, Anzhelika Kabro, Tom Miller, Stephanie Roy, Darby Schmidt, Dana K. Winter, Michael Bradley
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Publication number: 20180369243Abstract: 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., lung cancer, breast cancer, leukemia, lymphoma, melanoma, multiple myeloma, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma), 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 (e.g. a protein kinase (e.g. a cyclin-dependent kinase (CDK) (e.g. CDK7, CDK12, or CDK13) or a lipid kinase such as a phosphatidylinositol-5-phosphate 4-kinase (PIP4K) (e.g.Type: ApplicationFiled: June 24, 2016Publication date: December 27, 2018Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Tinghu Zhang
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Publication number: 20180344733Abstract: 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., lung cancer, breast cancer, leukemia, lymphoma, melanoma, multiple myeloma, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma), 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 (e.g. a protein kinase (e.g. a cyclin-dependent kinase (CDK) (e.g. CDK7, CDKl2, or CDKl3) or a lipid kinase such as a phosphatidylinositol-5-phosphate 4-kinase (PIP4K) (e.g.Type: ApplicationFiled: June 24, 2016Publication date: December 6, 2018Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Tinghu Zhang
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Patent number: 10144730Abstract: The present invention provides novel compounds according to Formula (I): where Ring A, Ring B, X, L1, L2, RA, RC, RD, RE, m, n, and p are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of human diseases associated with kinase activity, for example, proliferative diseases, neurodegenerative diseases, metabolic disorders, inflammatory diseases, and cardiovascular diseases.Type: GrantFiled: June 21, 2016Date of Patent: December 4, 2018Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael Gray, Tinghu Zhang
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Publication number: 20180319801Abstract: 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: November 8, 2018Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Tinghu Zhang, Nicholas Paul Kwiatkkowski
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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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Publication number: 20180258040Abstract: The application relates to a compound of Formula (I): which modulates the activity of ALK or SRPK, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which ALK or SRPK plays a role.Type: ApplicationFiled: September 23, 2016Publication date: September 13, 2018Applicant: Dana-Farber Cancer Institute, Inc.Inventors: John HATCHER, Nathanael S. GRAY, Hwan Geun CHOI, Pasi JANNE, Tinghu ZHANG
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Patent number: 10047070Abstract: 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 a cyclin-dependent kinase (CDK) (e.g.Type: GrantFiled: October 17, 2014Date of Patent: August 14, 2018Assignee: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael Gray, Tinghu Zhang, Stephane Ciblat, Melissa Leblanc, Jason J. Marineau, Joel Moore, Kevin Sprott, M. Arshad Siddiqui, Anzhelika Kabro, Tom Miller, Stephanie Roy, Darby Schmidt, Dana K. Winter, Michael Bradley
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Publication number: 20180170912Abstract: Provided herein are small molecule inhibitors of maternal embryonic leucine zipper kinase (MELK) having the structure of formula (I), wherein X and R1-R3 are defined in the specification. The compounds are useful for treating cancer and other conditions or diseases associated with aberrant MELK expression. Also provided herein are pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. The invention also provides methods of treating cancers associated with over-expression of MELK.Type: ApplicationFiled: March 4, 2016Publication date: June 21, 2018Inventors: Nathanael Gray, Tinghu Zhang, Hai-Tsang Huang, Yubao Wang, Jean Zhao, Hwan Geun Choi
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Publication number: 20180110778Abstract: 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., lung cancer, breast cancer, leukemia, lymphoma, melanoma, multiple myeloma, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma), 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 (e.g. a protein kinase (e.g. a cyclin-dependent kinase (CDK) (e.g. CDK7, CDKl2, or CDKl3) or a lipid kinase such as a phosphatidylinositol-5-phosphate 4-kinase (PIP4K) (e.g.Type: ApplicationFiled: June 24, 2016Publication date: April 26, 2018Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Tinghu Zhang
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Publication number: 20160368910Abstract: The present invention provides novel compounds according to Formula (I): where Ring A, Ring B, X, L1, L2, RA, RC, RD, RE, m, n, and p are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of human diseases associated with kinase activity, for example, proliferative diseases, neurodegenerative diseases, metabolic disorders, inflammatory diseases, and cardiovascular diseases.Type: ApplicationFiled: June 21, 2016Publication date: December 22, 2016Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Tinghu Zhang
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Publication number: 20160264554Abstract: 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 a cyclin-dependent kinase (CDK) (e.g.Type: ApplicationFiled: October 17, 2014Publication date: September 15, 2016Inventors: Nathanael Gray, Tinghu Zhang, Stephane Ciblat, Melissa Leblanc, Jason J. Marineau, Joel Moore, Kevin Sprott, M. Arshad Siddiqui, Anzhelika Kabro, Tom Miller, Stephanie Roy, Darby Schmidt, Dana K. Winter, Michael Bradley
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Publication number: 20160264551Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), 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 a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, in duce cellular apoptosis and/or inhibit transcription in the subject.Type: ApplicationFiled: October 17, 2014Publication date: September 15, 2016Applicants: SYROS PHARMACEUTICALS, INC., DANA-FARBER CANCER INSTITUTE, INC., DANA-FARBER CANCER INSTITUTE, INC.Inventors: Stephane Ciblat, Patrick Deroy, Nathanael Gray, Melissa Leblanc, Jason J. Marineau, Joel Moore, Kevin Sprott, Tinghu Zhang, M. Arshad Siddiqui, Anzhelika Kabro, Serge Leger, Tom Miller, Stephanie Roy, Darby Schmidt, Dana K. Winter, Michael Bradley
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Patent number: 9382239Abstract: The present invention provides novel compounds according to Formula (I): where Ring A, Ring B, X, L1, L2, RA, RC, RD, RE, m, n, and p are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of human diseases associated with kinase activity, for example, proliferative diseases, neurodegenerative diseases, metabolic disorders, inflammatory diseases, and cardiovascular diseases.Type: GrantFiled: November 16, 2012Date of Patent: July 5, 2016Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael Gray, Tinghu Zhang
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Publication number: 20160122323Abstract: 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: October 18, 2013Publication date: May 5, 2016Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael Gray, Tinghu ZHANG, Nicholas Paul KWIATKOWSKI
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Publication number: 20140309249Abstract: The present invention provides novel compounds according to Formula (I): where Ring A, Ring B, X, L1, L2, RA, RC, RD, RE, m, n, and p are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of human diseases associated with kinase activity, for example, proliferative diseases, neurodegenerative diseases, metabolic disorders, inflammatory diseases, and cardiovascular diseases.Type: ApplicationFiled: November 16, 2012Publication date: October 16, 2014Applicant: Dana-Farber Cancer Intitute, Inc.Inventors: Nathanael Gray, Tinghu Zhang
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Publication number: 20120219613Abstract: Provided herein are a series of arylmethylidene rhodanine derivatives having broad-spectrum antiviral activity against enveloped viruses, including but not limited to filoviruses, poxviruses, arenaviruses, bunyaviruses, paramyxoviruses, flaviviruses, influenza A, and HIV-1. The compounds act via a novel mechanism to disrupt viral membranes and inhibit viral attachment, fusion, and/or entry into host cells. The membrane disrupting activity of the compounds is selective for viral membranes relative to other biological membranes, making the compounds non-toxic to cells and host subjects.Type: ApplicationFiled: June 18, 2009Publication date: August 30, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Benhur Lee, Michael E. Jung, Michael C. Wolf, Tinghu Zhang