Patents by Inventor Yanke Liang
Yanke Liang 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: 10905768Abstract: This invention provides heterocyclic compounds that bind to E3 Ubiquitin Ligase (typically through cereblon) (“Degrons”), which can be used as is or linked to a Targeting Ligand for a selected Target Protein for therapeutic purposes and methods of use and compositions thereof as well as methods for their preparation.Type: GrantFiled: May 11, 2020Date of Patent: February 2, 2021Assignee: C4 Therapeutics, Inc.Inventors: Andrew J. Phillips, Chris G. Nasveschuk, James A. Henderson, Yanke Liang, Mark E. Fitzgerald, Minsheng He, Ryan E. Michael
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Patent number: 10882848Abstract: The present invention provides compounds which are selective allosteric inhibitors of T790M and C797S containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.Type: GrantFiled: June 21, 2019Date of Patent: January 5, 2021Assignee: Hoffmann-La Roche, Inc.Inventors: Martin Duplessis, Georg Jaeschke, Bernd Kuhn, Kiel Lazarski, Yanke Liang, Yvonne Alice Nagel, Antonio Ricci, Daniel Rueher, Sandra Steiner
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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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Patent number: 10865205Abstract: The present application provides bifunctional compounds of Formula (Ia) or (Ib): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 8 (CDK8). The present application also relates to methods for the targeted degradation of CDK8 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK8 which can be utilized in the treatment of disorders modulated by CDK8.Type: GrantFiled: April 21, 2017Date of Patent: December 15, 2020Assignee: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael S. Gray, Tinghu Zhang, Calla M. Olson, Yanke Liang, Nicholas Kwiatkowski
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Patent number: 10865204Abstract: 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: GrantFiled: April 21, 2017Date of Patent: December 15, 2020Assignee: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael S. Gray, Tinghu Zhang, Calla M. Olson, Yanke Liang, Nicholas Kwiatkowski, Baishan Jiang, Eric Wang
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Patent number: 10849982Abstract: This invention provides Degronimers that have carbon-linked E3 Ubiquitin Ligase targeting moieties (Degrons), which can be linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.Type: GrantFiled: November 9, 2018Date of Patent: December 1, 2020Assignee: C4 Therapeutics, Inc.Inventors: Andrew J. Phillips, Chris G. Nasveschuk, James A. Henderson, Yanke Liang, Minsheng He, Kiel Lazarski, Gesine Kerstin Veits, Harit U. Vora
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Publication number: 20200361930Abstract: The present invention provides compounds that cause specifically the degradation of EGFR via the targeted ubiquitination of EGFR protein and subsequent proteasomal degradation. The present compounds are useful for the treatment of various cancers.Type: ApplicationFiled: August 4, 2020Publication date: November 19, 2020Applicants: Hoffmann-La Roche Inc., C4 Therapeutics, Inc.Inventors: Martin Duplessis, Georg Jaeschke, Bernd Kuhn, Kiel Lazarski, Yanke Liang, Yvonne Alice Nagel, Antonio Ricci, Daniel Rueher, Sandra Steiner
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Publication number: 20200338087Abstract: 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 STK inhibitors of Formula (III)).Type: ApplicationFiled: April 19, 2019Publication date: October 29, 2020Applicants: 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 S. Gray, Ramnik Xavier, Stuart L. Schreiber, Hwan Geun Choi, Yanke Liang
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Publication number: 20200317675Abstract: The present disclosure provides compounds of Formula (I), (II), and (III). The provided compounds are able to bind protein kinases (e.g., SIK) and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase (e.g., SIK, (e.g., SIK1, SIK2, or SIK3)) in a subject or cell. The provided compounds may be useful in treating or preventing a disease (e.g., proliferative disease, musculoskeletal disease, genetic disease, hematological disease, neurological disease, painful condition, psychiatric disorder, or metabolic disorder) in a subject in need thereof. Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound described herein.Type: ApplicationFiled: July 5, 2017Publication date: October 8, 2020Applicants: The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc., The General Hospital CorporationInventors: Nathanael S. GRAY, Yanke LIANG, Hwan Geun CHOI, Thomas SUNDBERG, Alykhan SHAMJI, Ramnik XAVIER, David E. FISHER, Nisma MUJAHID
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Publication number: 20200308171Abstract: Present invention provides bifunctional compounds that comprise an E3 Ubiquitin Ligase moiety that is linked to a moiety that inhibit EGFR, where the target protein can be proximate to the ubiquitin ligase to effect degradation of said protein. Present compounds are useful for the treatment of various cancers.Type: ApplicationFiled: June 16, 2020Publication date: October 1, 2020Applicants: Hoffmann-La Roche Inc., C4 Therapeutics, Inc.Inventors: Georg Jaeschke, Bernd Kuhn, Antonio Ricci, Daniel Rueher, Sandra Steiner, Yvonne Alice Nagel, Martin Duplessis, Kiel Lazarski, Yanke Liang
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Publication number: 20200253981Abstract: The present disclosure provides methods of increasing skin pigmentation in a subject in need thereof using salt-inducible kinase (SIK) inhibitors, such as macrocyclic compounds of Formula (I), bicyclic urea compounds of Formula (II), (III), and (IV), and compounds of Formula (V), (VI), (VI-A), or (VII). Also provided are pharmaceutical compositions, methods, and uses that include or involve a compound described herein.Type: ApplicationFiled: February 28, 2018Publication date: August 13, 2020Applicants: The General Hospital Corporation, Dana-Farber Cancer Institute, Inc.Inventors: David E. Fisher, Nisma Mujahid, Ryo Murakami, Nathanael S. Gray, Yanke Liang, Hwan Geun Choi
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Publication number: 20200179387Abstract: The present disclosure provides methods of treating and/or preventing osteoporosis using salt-inducible kinase (SIK) inhibitors. Also provided are methods of using SIK inhibitors for increasing the function of osteocytes, increasing the number of osteoblasts, increasing the activity of osteoblasts, inhibiting the resorption of a bone, decreasing the number of osteoclasts, inhibiting the activity of osteoclasts, increasing the mass of a bone, down-regulating the expression of the gene SOST, and/or inhibiting the activity of sclerostin. The SIK inhibitors may be combined with Src inhibitors or CSF I R inhibitors. Exemplary SIK inhibitors include the compounds of the formula: (I), (II), (III), (IV), (V) or (VI).Type: ApplicationFiled: September 16, 2017Publication date: June 11, 2020Applicants: The General Hospital Corporation, The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc.Inventors: Marc Wein, Henry Kronenberg, Thomas Sundberg, Ramnik Xavier, Nathanael S. Gray, Yanke Liang, Hwan Geun Choi, Alykhan Shamji
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Patent number: 10660968Abstract: This invention provides compounds that have spirocyclic E3 Ubiquitin Ligase targeting moieties (Degrons), which can be used as is or linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.Type: GrantFiled: November 9, 2018Date of Patent: May 26, 2020Assignee: C4 Therapeutics, Inc.Inventors: Andrew J. Phillips, Chris G. Nasveschuk, James A. Henderson, Yanke Liang, Kiel Lazarski, Ryan E. Michael
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Patent number: 10646575Abstract: This invention provides heterocyclic compounds that bind to E3 Ubiquitin Ligase (typically through cereblon) (“Degrons”), which can be used as is or linked to a Targeting Ligand for a selected Target Protein for therapeutic purposes and methods of use and compositions thereof as well as methods for their preparation.Type: GrantFiled: November 9, 2018Date of Patent: May 12, 2020Assignee: C4 Therapeutics, Inc.Inventors: Andrew J. Phillips, Chris G. Nasveschuk, James A. Henderson, Yanke Liang, Mark E. Fitzgerald, Minsheng He, Ryan E. Michael
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Publication number: 20200140456Abstract: This invention provides Degronimers that have E3 Ubiquitin Ligase targeting moieties (Degrons) that can be linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation. The invention also provides Degrons that can be used to treat disorders mediated by cereblon or an Ikaros family protein, and methods of use and compositions thereof as well as methods for their preparation.Type: ApplicationFiled: December 19, 2019Publication date: May 7, 2020Applicant: C4 Therapeutics, Inc.Inventors: Andrew J. Phillips, Christopher G. Nasveschuk, James A. Henderson, Yanke Liang, Minsheng He, Martin Duplessis, Chi-Li Chen
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Patent number: 10532103Abstract: 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 9 (CDK9), the present application also relates to methods for the targeted degradation of CDK9 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK9 which can be utilized in the treatment of disorders modulated by CDK9.Type: GrantFiled: April 21, 2017Date of Patent: January 14, 2020Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Tinghu Zhang, Calla M. Olson, Yanke Liang, Nicholas Kwiatkowski
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Publication number: 20190367487Abstract: The present disclosure provides imidazolyl compounds of Formula (I) and methods of preparing the compounds. The provided compounds are able to bind protein kinases and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase in a subject or cell and/or in treating or preventing a disease (e.g., proliferative disease, genetic disease, hematological disease, neurological disease, painful condition, psychiatric disorder, or metabolic disorder) in a subject in need thereof. Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound described herein.Type: ApplicationFiled: May 13, 2019Publication date: December 5, 2019Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Hwan Geun Choi, Yanke Liang
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Publication number: 20190343842Abstract: 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 STK inhibitors of Formula (III)).Type: ApplicationFiled: April 19, 2019Publication date: November 14, 2019Applicants: 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 S. Gray, Ramnik Xavier, Stuart L. Schreiber, Hwan Geun Choi, Yanke Liang
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Patent number: 10457691Abstract: The present disclosure provides macrocyclic compounds of Formula (I). The provided compounds are able to bind protein kinases and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase in a subject or cell and/or in treating or preventing a disease (e.g., proliferative disease, genetic disease, hematological disease, neurological disease, painful condition, psychiatric disorder, or metabolic disorder) in a subject in need thereof. Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound described herein.Type: GrantFiled: July 21, 2015Date of Patent: October 29, 2019Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Hwan Geun Choi, Yanke Liang
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Publication number: 20190315752Abstract: The present disclosure provides compounds of Formula (I), (II), and (III). The provided compounds are able to bind protein kinases (e.g., SIK) and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase (e.g., SIK, (e.g., SIK1, SIK2, or SIK3)) in a subject or cell. The provided compounds may be useful in treating or preventing a disease (e.g., proliferative disease, musculoskeletal disease, genetic disease, hematological disease, neurological disease, painful condition, psychiatric disorder, or metabolic disorder) in a subject in need thereof. Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound described herein.Type: ApplicationFiled: July 5, 2017Publication date: October 17, 2019Applicants: The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc., The General Hospital CorporationInventors: Nathanael S. GRAY, Yanke LIANG, Hwan Geun CHOI, Thomas SUNDBERG, Alykhan SHAMJI, Ramnik XAVIER, David E. FISHER, Nisma MUJAHID