Patents by Inventor Nathanael Gray
Nathanael Gray 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: 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: 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: 20180221379Abstract: The present disclosure provides methods of treating and/or preventing inflammatory bowel disease (IBD) and graft-versus-host disease (GVHD) using salt-inducible kinase (SIK) inhibitors, such as macrocyclic SIK inhibitors of Formula (I), imidazolyl SIK inhibitors of Formula (II), and urea and carbamate SIK inhibitors of Formula (III-A) (e.g., urea and carbamate SIK inhibitors of Formula (III)).Type: ApplicationFiled: December 19, 2017Publication date: August 9, 2018Applicants: Dana-Farber Cancer Institute, Inc., The Broad Institute, Inc., President and Fellows of Harvard College, The General Hospital Corporation d/b/a Massachusetts General HospitalInventors: Alykhan Shamji, Thomas Sundberg, Nathanael Gray, Ramnik Xavier, Stuart L. Schreiber, Hwan Geun Choi, Yanke Liang
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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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Patent number: 10000483Abstract: 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 compounds of Formula (I) or (II), or compositions thereof, for treating or preventing a wide range of diseases (e.g., proliferative diseases (e.g., cancers, benign neoplasms, angiogenesis, inflammatory diseases, autoimmune diseases) and metabolic diseases (e.g., diabetes (e.g., type 2 diabetes, gestational diabetes)) in a subject. Treatment of a subject with a disease using a compound of Formula (I) or (II), or compositions thereof, may downregulate the expression and/or inhibit the activity of a kinase (e.g., a tyrosine kinase, such as a Tec kinase, in particular, bone marrow on X chromosome kinase (BMX)), and therefore, suppress tyrosine kinase singling in the subject.Type: GrantFiled: October 18, 2013Date of Patent: June 19, 2018Assignees: Dana-Farber Cancer Institute, Inc., Beth Israel Deaconess Medical Center, Inc.Inventors: Nathanael Gray, Steven Balk, Qingsong Liu, Sen Chen
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Patent number: 9879003Abstract: Novel antiviral compounds of Formulae (I)-(III) are provided: (I) (II) (III) The inventive compounds, pharmaceutical compositions thereof, and kits including the inventive compounds are useful for the prevention and treatment of infectious diseases caused by viruses, for example, by Flaviviridae virus (e.g., Dengue virus (DENY)), Kunjin virus, Japanese encephalitis virus, vesicular stomatitis virus (VSV), herpes simplex virus 1 (HSV-1), human cytomegalovirus (HCMV), poliovirus, Junin virus, Ebola virus, Marburg virus (MARV), Lassa fever virus (LASV), Venezuelan equine encephalitis virus (VEEV), or Rift Valley Fever virus (RVFV).Type: GrantFiled: March 15, 2013Date of Patent: January 30, 2018Assignees: Dana-Farber Cancer Institute, Inc., President and Fellows of Harvard CollegeInventors: Nathanael Gray, Priscilla Yang, Qingsong Liu, Mélissanne de Wispelaere
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Publication number: 20170369449Abstract: The invention relates to compounds and their use in the treatment of disease. Novel irreversible inhibitors of wild-type and mutant forms of EGFR, FGFR, ALK, ROS, JAK, BTK, BLK, ITK, TEC, and/or TXK and their use for the treatment of cell proliferation disorders are described.Type: ApplicationFiled: September 6, 2017Publication date: December 28, 2017Inventors: Nathanael GRAY, Hwan Geun CHOI, Li TAN
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Patent number: 9783504Abstract: The invention relates to compounds and their use in the treatment of disease. Novel irreversible inhibitors of wild-type and mutant forms of EGFR, FGFR, ALK, ROS, JAK, BTK, BLK, ITK, TEC, and/or TXK and their use for the treatment of cell proliferation disorders are described.Type: GrantFiled: July 9, 2014Date of Patent: October 10, 2017Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael Gray, Hwan Geun Choi, Li Tan
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Patent number: 9758522Abstract: Provided are bifunctional small molecules of Formula (I): or pharmaceutically acceptable salts thereof, wherein M represents a small organic molecule which binds, covalently or non-covalently, a kinase, such as Her3 protein kinase; L1 represents a linker; and RH represents a hydrophobic group. An example of a compound of Formula (I) is a compound of Formula (II): Also provided are pharmaceutical compositions comprising a compound of Formula (I) or (II) and methods of using such compounds for treating proliferative diseases.Type: GrantFiled: October 18, 2013Date of Patent: September 12, 2017Assignees: Dana-Farber Cancer Institute, Inc., Yale UniversityInventors: Nathanael Gray, Ting Xie, Sang Min Lim, Pasi A. Janne, Craig M. Crews
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Patent number: 9725425Abstract: Provided are small molecule inhibitors of ubiquitin specific protease 2, 8 and 12 (USP2 and USP8 and USP12) activity and methods for their use in treating cancers. The small molecule inhibitors of the invention are particularly useful in the treatment of non-small cell lung cancers that are resistant to tyrosine kinase inhibitors and in the treatment of prostate cancer that is resistant to AR inhibitor therapy.Type: GrantFiled: February 25, 2015Date of Patent: August 8, 2017Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Alan D. D'Andrea, Nathanael Gray, Sara Jean Buhrlage, Kalindi Parmar
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Patent number: 9670165Abstract: The present invention relates to the discovery that salt inducible kinases (SIKs) suppress the formation of anti-inflammatory molecules such as IL-10, which are important for the resolution of inflammation and identifies SIK inhibitors that may be used to treat disorders associated with undesirable inflammation, such as inflammatory bowel disease and/or autoimmune disorders.Type: GrantFiled: March 13, 2013Date of Patent: June 6, 2017Assignees: Dana-Farber Cancer Institute, Inc., University Court of the University of DundeeInventors: Philip Cohen, Kristopher Clark, Hwan Geun Choi, Nathanael Gray
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Patent number: 9505784Abstract: The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.Type: GrantFiled: July 1, 2014Date of Patent: November 29, 2016Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Hwan Geun Choi, Taebo Sim, Nathanael Gray, Wenjun Zhou, Jae Won Chang, Jianming Zhang, Ellen Weisberg
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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: 20160176825Abstract: The invention relates to compounds and their use in the treatment of disease. Novel irreversible inhibitors of wild-type and mutant forms of EGFR, FGFR, ALK, ROS, JAK, BTK, BLK, ITK, TEC, and/or TXK and their use for the treatment of cell proliferation disorders are described.Type: ApplicationFiled: July 9, 2014Publication date: June 23, 2016Inventors: Nathanael Gray, Hwan Geun Choi, Li Tan
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Patent number: 9358231Abstract: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.Type: GrantFiled: November 24, 2014Date of Patent: June 7, 2016Assignees: Dana-Farber Cancer Institute, Inc., University of MiamiInventors: Nathanael Gray, Hwan Geun Choi, Xianming Deng, Jianming Zhang, Izidore Lossos
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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: 20160046661Abstract: Described herein are compounds of Formulae (I)-(II), and pharmaceutically acceptable salts, and pharmaceutical compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases such as cancers (e.g., lung cancer, large bowel cancer, pancreas cancer, biliary tract cancer, or endometrial cancer), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases in a subject.Type: ApplicationFiled: March 13, 2014Publication date: February 18, 2016Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael Gray, Sang Min Lim, Hwan Geun Choi, Kenneth Dale Westover
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Publication number: 20150274738Abstract: Provided are bifunctional small molecules of Formula (I): or pharmaceutically acceptable salts thereof, wherein M represents a small organic molecule which binds, covalently or non-covalently, a kinase, such as Her3 protein kinase; L1 represents a linker; and RH represents a hydrophobic group. An example of a compound of Formula (I) is a compound of Formula (II): Also provided are pharmaceutical compositions comprising a compound of Formula (I) or (II) and methods of using such compounds for treating proliferative diseases.Type: ApplicationFiled: October 18, 2013Publication date: October 1, 2015Applicants: Dana-Farber Cancer, Institute, Inc., Yale UniversityInventors: Nathanael Gray, Ting Xie, Sang Min Lim, Pasi A. Janne, Craig M. Crews