Patents by Inventor Angela N. Koehler
Angela N. Koehler 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: 20230303512Abstract: Provided herein are compounds that inhibit the function of MYB. In particular, provided are compounds that can inhibit MYB and/or disrupt the interaction between MYB and a protein associated with MYB, a protein whose dysregulation is implicated in cancer. Also provided are pharmaceutical compositions comprising the compounds, methods of inhibiting MYB function, and methods of treating cancer in a subject by administering a compound or composition described herein.Type: ApplicationFiled: August 26, 2021Publication date: September 28, 2023Applicant: Massachusetts Institute of TechnologyInventors: Angela N. Koehler, Becky Leifer, Florian Kabinger, Brice Curtin, Jasmin Kruell
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Publication number: 20230158159Abstract: Provided herein are bifunctional compounds that bind cyclin-dependent kinase 9 (CDK9) and/or promote targeted ubiquitination for the degradation of CDK9. In particular, provided are compounds that can bind CDK9, a protein whose dysregulation is implicated in a variety of cancers, and can promote CDK9?s degradation by recruiting an E3 ubiquitin ligase (e.g., Cereblon, VHL). The E3 ubiquitin ligase can ubiquitinate CDK9, marking it for proteasomal degradation. Also provided are pharmaceutical compositions comprising the bifunctional compounds. Also provided are methods of treating cancer, and methods of promoting the degradation of CDK9 protein by E3 ubiquitin ligase activity in a subject or biological sample by administering a compound or composition described herein.Type: ApplicationFiled: April 22, 2021Publication date: May 25, 2023Applicant: Massachusetts Institute of TechnologyInventors: Angela N. Koehler, Andre Richters, Julie Urgiles, Florian Kabinger, Mohammed Abraham Toure
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Publication number: 20220089537Abstract: Organic compounds for target identification, drug discovery, chemical library production, high-throughput screening, fluorophore conjugation, chemiluminescent compound conjugation, creation of proximity induced modulators (e.g., protein degraders)/chimeric molecules, or a combination thereof are described. The compounds can contain small molecule moieties for identification of their potential targets; an isocyanate, photoactivatable groups; chemical moieties for enrichment and detection of target-small molecule moiety interactions; proximity induced modulator element; fluorophores; chemiluminescent groups; or combinations thereof.Type: ApplicationFiled: July 12, 2021Publication date: March 24, 2022Inventors: Angela N. Koehler, Christina Woo, Catherine Henry, Chia-Fu Chang, Sebastian Pomplun, Jasmin Kruell, Brice Curtin
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Patent number: 10961216Abstract: Provided herein are compounds useful for modulating the activity of an androgen receptor, or a variant thereof, and related compositions and methods. Compounds of the invention are useful for antagonizing the androgen receptor splice variant AR-v7, and for the treatment of castration-resistant prostate cancer.Type: GrantFiled: November 21, 2018Date of Patent: March 30, 2021Assignee: Massachusetts Institute of TechnologyInventors: David Freeman, Nicholas B. Struntz, Shelby K. Doyle, Andre Richters, Angela N. Koehler
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Patent number: 10865213Abstract: The present disclosure provides compounds of Formula (I?), Formula (I), Formula (II), Formula (II-A), Formula (III), and Formula (IV). The compounds described herein are MAX binders and/or modulators of Myc, Mad, or Mxi1 (e.g., inhibitors of Myc, Mad, or Mxi1), and may be useful in treating a subject with a disease associated with Myc, such as proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions and kits including the compounds described herein, as well as methods of using and uses of the compounds, compositions, and kits.Type: GrantFiled: October 22, 2018Date of Patent: December 15, 2020Assignee: Massachusetts Institute of TechnologyInventors: Angela N. Koehler, Eric Stefan, Francisco Caballero, Dylan Vijith Neel, Nicholas B. Struntz, Helen L. Evans, Andrew Chen
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Publication number: 20200048276Abstract: The present disclosure provides compounds of Formula (I-a), Formula (I), and Formula (II). The compounds described herein may be Myc modulators (e.g., Myc inhibitors) and may be useful in treating in a subject in need thereof diseases associated with Myc and proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including a compound described herein.Type: ApplicationFiled: June 11, 2018Publication date: February 13, 2020Applicant: Massachusetts Institute of TechnologyInventors: Angela N. Koehler, Eric Stefan, Francisco Caballero
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Publication number: 20190202800Abstract: Provided herein are compounds useful for modulating the activity of an androgen receptor, or a variant thereof, and related compositions and methods. Compounds of the invention are useful for antagonizing the androgen receptor splice variant AR-v7, and for the treatment of castration-resistant prostate cancer.Type: ApplicationFiled: November 21, 2018Publication date: July 4, 2019Inventors: David Freeman, Nicholas B. Struntz, Shelby K. Doyle, Andre Richters, Angela N. Koehler
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Publication number: 20190144466Abstract: The present disclosure provides compounds of Formula (I?), Formula (I), Formula (II), Formula (II-A), Formula (III), and Formula (IV). The compounds described herein are MAX binders and/or modulators of Myc, Mad, or Mxi1 (e.g., inhibitors of Myc, Mad, or Mxi1), and may be useful in treating a subject with a disease associated with Myc, such as proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions and kits including the compounds described herein, as well as methods of using and uses of the compounds, compositions, and kits.Type: ApplicationFiled: October 22, 2018Publication date: May 16, 2019Applicant: Massachusetts Institute of TechnologyInventors: Angela N. Koehler, Eric Stefan, Francisco Caballero, Dylan Vijith Neel, Nicholas B. Struntz, Helen L. Evans, Andrew Chen
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Publication number: 20190060296Abstract: Provided herein are methods useful for identifying compounds that modulate the activity of an androgen receptor, or variant thereof. In particular, this invention encompasses reagents and strategies for identifying compounds that target specific androgen receptor splice variants, for example, AR-v7, that are important for prostate cancer progression and metastasis, for example in the development of castration-resistant prostate cancer. Also provided herein are specific compounds that modulate the activity of an androgen receptor, or variant thereof, pharmaceutical compositions, and methods of using these compounds and pharmaceutical compositions for modulating the activity of an androgen receptor, or variant thereof in vitro and in vivo.Type: ApplicationFiled: July 27, 2018Publication date: February 28, 2019Inventors: Angela N. Koehler, Marius S. Pop
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Patent number: 10106555Abstract: The present disclosure provides compounds of Formula (I?), Formula (I), Formula (II), Formula (II-A), Formula (III), and Formula (IV). The compounds described herein are MAX binders and/or modulators of Myc, Mad, or Mxi1 (e.g., inhibitors of Myc, Mad, or Mxi1), and may be useful in treating a subject with a disease associated with Myc, such as proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions and kits including the compounds described herein, as well as methods of using and uses of the compounds, compositions, and kits.Type: GrantFiled: February 16, 2017Date of Patent: October 23, 2018Assignee: Massachusetts Institute of TechnologyInventors: Angela N. Koehler, Eric Stefan, Francisco Caballero, Dylan Vijith Neel, Nicholas B. Struntz, Helen L. Evans, Andrew Chen
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Publication number: 20180291035Abstract: The present disclosure provides compounds of Formula (I-a), Formula (I), and Formula (II). The compounds described herein may be Myc modulators (e.g., Myc inhibitors) and may be useful in treating in a subject in need thereof diseases associated with Myc and proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including a compound described herein.Type: ApplicationFiled: June 11, 2018Publication date: October 11, 2018Applicant: Massachusetts Institute of TechnologyInventors: Angela N. Koehler, Eric Stefan, Francisco Caballero
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Patent number: 10017520Abstract: The present disclosure provides compounds of Formula (I-a), Formula (I), and Formula (II). The compounds described herein may be Myc modulators (e.g., Myc inhibitors) and may be useful in treating in a subject in need thereof diseases associated with Myc and proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including a compound described herein.Type: GrantFiled: December 10, 2015Date of Patent: July 10, 2018Assignee: Massachusetts Institute of TechnologyInventors: Angela N. Koehler, Eric Stefan, Francisco Caballero
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Publication number: 20170233405Abstract: The present disclosure provides compounds of Formula (I?), Formula (I), Formula (II), Formula (II-A), Formula (III), and Formula (IV). The compounds described herein are MAX binders and/or modulators of Myc, Mad, or Mxi1 (e.g., inhibitors of Myc, Mad, or Mxi1), and may be useful in treating a subject with a disease associated with Myc, such as proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions and kits including the compounds described herein, as well as methods of using and uses of the compounds, compositions, and kits.Type: ApplicationFiled: February 16, 2017Publication date: August 17, 2017Inventors: Angela N. Koehler, Eric Stefan, Francisco Caballero, Dylan Vijith Neel, Nicholas B. Struntz, Helen L. Evans, Andrew Chen
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Publication number: 20160168165Abstract: The present disclosure provides compounds of Formula (I-a), Formula (I), and Formula (II). The compounds described herein may be Myc modulators (e.g., Myc inhibitors) and may be useful in treating in a subject in need thereof diseases associated with Myc and proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including a compound described herein.Type: ApplicationFiled: December 10, 2015Publication date: June 16, 2016Inventors: Angela N. Koehler, Eric Stefan, Francisco Caballero
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Publication number: 20130261023Abstract: The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support using isocyanate or isothiocyanate chemistry, wherein the density of the array of compounds is at least 1000 spots per cm2.Type: ApplicationFiled: October 10, 2012Publication date: October 3, 2013Applicants: Dana-Farber Cancer Institute, Inc., President and Fellows of Harvard CollegeInventors: David W. Barnes, Angela N. Koehler, James Elliot Bradner, Ralph Mazitschek, Stuart L. Schreiber
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Publication number: 20120021933Abstract: The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support, wherein the density of the array of compounds is at least 1000 spots per cm2. In particularly preferred embodiments, these compounds are attached to the solid support through a covalent interaction.Type: ApplicationFiled: April 26, 2011Publication date: January 26, 2012Inventors: Seung Bum Park, David Barnes-Seeman, Angela N. Koehler, Stuart L. Schreiber
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Patent number: 7932213Abstract: The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. A composition is provided that comprises an array of chemical compounds attached to a solid support, wherein the density of the array of compounds is at least 1000 spots per cm2. The inventive arrays are generated by: providing a solid support functionalized with a selected chemical moiety capable of interacting with a chemical compound to form an attachment and delivering compounds to the solid support having a density of at least 1000 spots per cm2. The present invention also provides methods for utilizing these arrays to identify small molecule partners for biological macromolecules of interest.Type: GrantFiled: February 20, 2003Date of Patent: April 26, 2011Assignee: President and Fellows of Harvard CollegeInventors: Seung Bum Park, David Barnes-Seeman, Angela N. Koehler, Stuart L. Schreiber
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Publication number: 20100093716Abstract: The present invention provides, inter alia, compositions and methods for treating various diseases and disorders in a mammal by administering to a mammal in need an effective amount of a composition comprising a non-DNA small molecule that binds WRN, such as members of the spirooxindole (SPOX) class.Type: ApplicationFiled: August 29, 2007Publication date: April 15, 2010Applicant: TRUSTEES OF BOSTON UNIVERSITY AND PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: Barbara A. Gilchrest, Mark S. Eller, Angela N. Koehler, Olivia M. McPherson, Christopher S. Neumann, Timothy A. Lewis
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Publication number: 20090221433Abstract: The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support using isocyanate or isothiocyanate chemistry, wherein the density of the array of compounds is at least 1000 spots per cm2.Type: ApplicationFiled: January 3, 2007Publication date: September 3, 2009Inventors: David W. Barnes, Angela N. Koehler, James E. Bradner, Ralph Mazitschek, Stuart L. Schreiber
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Patent number: 6824987Abstract: The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support, wherein the density of the array of compounds is at least 1000 spots per cm2. In particularly preferred embodiments, these compounds are attached to the solid support through a covalent interaction.Type: GrantFiled: May 10, 2000Date of Patent: November 30, 2004Assignee: President and Fellows of Harvard CollegeInventors: Stuart L. Schreiber, Gavin MacBeath, Angela N. Koehler, Paul Hergenrother, Kristopher M. Depew