Patents by Inventor Matthew D. Shair
Matthew D. Shair 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: 20180135134Abstract: A method for the targeted selection and treatment of patients with a tumor or cancer, comprising (i) determining whether the patient has a RUNX1 pathway impairment; and if so (ii) administering an effective amount of a cortistatin or its pharmaceutically acceptable salt or oxide, optionally in a pharmaceutically acceptable composition.Type: ApplicationFiled: November 8, 2017Publication date: May 17, 2018Applicant: President and Fellows of Harvard CollegeInventors: Matthew D. Shair, Henry Efrem Pelish, Ioana IIinca Nitulescu
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Publication number: 20180118778Abstract: Compounds of Formula (A?), (B?), (C?), (D?), (E?), (A?), (B?), (C?), (D?), (E?), (G1), and (G2) are useful as therapeutics for treating a wide variety of conditions in a host such as a human, e.g., including but not limited to, conditions associated with angiogenesis and/or which are mediated by CDK8 and/or CDK19 kinase activity. Also provided are methods of modulating the ?-catenin pathway, methods of modulating STAT1 activity, methods of modulating the TGF?/BMP pathway, methods of modulating HIF-1-alpha activity in a cell, and methods of increasing BIM expression to induce apoptosis, using an effective amount of a compound of Formula (A?), (B?), (C?), (D?), (E?), (A?), (B?), (C?), (D?), (E?), (G1), or (G2).Type: ApplicationFiled: December 22, 2017Publication date: May 3, 2018Applicant: President and Fellows of Harvard CollegeInventors: Matthew D. Shair, Henry Efrem Pelish
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Publication number: 20170320886Abstract: The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: and salts thereof, wherein R1, R2, R3, R4, n, and m are as defined herein; processes for preparing such compounds and intermediates thereto; pharmaceutical compositions comprising such compounds; methods for treating a proliferative disease; methods for treating a disease associated with aberrant angiogenesis; methods for inhibiting angiogenesis; and processes for preparing cortistatin A, J, K, and L, and analogs thereof.Type: ApplicationFiled: July 24, 2017Publication date: November 9, 2017Applicant: President and Fellows of Harvard CollegeInventors: Alec Nathanson Flyer, Hong Myung Lee, Andrew G. Myers, Cristina Montserrat Nieto-Oberhuber, Matthew D. Shair, Chong Si Allston
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Patent number: 9790253Abstract: Provided are a number of compounds structurally related to OSW-1, a natural compound that binds OSBPs. Also provided are pharmaceutical compositions comprising the OSW-1 analogs, as well as methods for use of these OSW-1 analogs, or pharmaceutically acceptable salts, enantiomers, or stereoisomers thereof in the treatment of atherosclerosis. Alzheimer's disease, and cancer, including p21-deficient cancer. Conjugates of OSW-1 analogs with monoclonal antibodies, including monoclonal antibodies targeted to cancer cells, are also provided. Also provided are pharmaceutical compositions comprising the conjugates, as well as methods for use of these conjugates, in the treatment of cancer, including p21-deficient cancer.Type: GrantFiled: May 18, 2012Date of Patent: October 17, 2017Assignee: President and Fellows of Harvard CollegeInventors: Matthew D. Shair, Anthony William George Burgett
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Patent number: 9714255Abstract: The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: and salts thereof, wherein R1, R2, R3, R4, n, and m are as defined herein; processes for preparing such compounds and intermediates thereto; pharmaceutical compositions comprising such compounds; methods for treating a proliferative disease; methods for treating a disease associated with aberrant angiogenesis; methods for inhibiting angiogenesis; and processes for preparing cortistatin A, J, K, and L, and analogs thereof.Type: GrantFiled: September 8, 2015Date of Patent: July 25, 2017Assignee: President and Fellows of Harvard CollegeInventors: Alec Nathanson Flyer, Hong Myung Lee, Andrew G. Myers, Cristina Montserrat Nieto-Oberhuber, Matthew D. Shair, Chong Si
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Publication number: 20170029435Abstract: Provided herein are compounds of Formula (A), (B), (C), (D) and (E), pharmaceutically acceptable salts, quaternary amine salts, and N-oxides thereof, and pharmaceutical compositions thereof. Compounds of Formula (A), (B), (C), (D), and (E) are contemplated useful as therapeutics for treating a wide variety of conditions, e.g., including but not limited to, conditions associated with angiogenesis and with CDK8 and/or CDK19 kinase activity. Further provided are methods of inhibiting CDK8 and/or CDK19 kinase activity, methods of modulating the ?-catenin pathway, methods of modulating STAT1 activity, methods of modulating the TGF?/BMP pathway, methods of modulating HIF-1-alpha activity in a cell, and methods of increasing BIM expression to induce apoptosis, using a compound of Formula (A), (B), (C), (D), or (E). Further provided are CDK8 and CDK19 point mutants and methods of use thereof.Type: ApplicationFiled: June 24, 2016Publication date: February 2, 2017Inventors: Matthew D. Shair, Juergen Ramharter, Henry Efrem Pelish, Brian Bor-Jen Liau, Jae Young Ahn
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Patent number: 9321713Abstract: The present invention provides a novel 11-step enantioselective approach to the natural product hyperforin, which enables access to a wide variety of hyperforin analogs. The present invention also provides pharmaceutical compositions comprising inventive hyperforin analogs. Hyperforin analogs synthesized using the present synthetic method are envisioned useful in the treatment of various conditions, including, but not limited to, depression and conditions characterized by depression, inflammatory skin conditions, diabetes, asthma, chronic obstructive pulmonary disease (COPD), kidney disorders, and ischemic brain damage.Type: GrantFiled: June 1, 2012Date of Patent: April 26, 2016Assignee: President and Fellows of Harvard CollegeInventors: Matthew D. Shair, Brian A. Sparling, David Moebius
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Publication number: 20150376201Abstract: The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: and salts thereof, wherein R1, R2, R3, R4, n, and m are as defined herein; processes for preparing such compounds and intermediates thereto; pharmaceutical compositions comprising such compounds; methods for treating a proliferative disease; methods for treating a disease associated with aberrant angiogenesis; methods for inhibiting angiogenesis; and processes for preparing cortistatin A, J, K, and L, and analogs thereof.Type: ApplicationFiled: September 8, 2015Publication date: December 31, 2015Applicant: President and Fellows of Harvard CollegeInventors: Alec Nathanson Flyer, Hong Myung Lee, Andrew G. Myers, Cristina Montserrat Nieto-Oberhuber, Matthew D. Shair, Chong Si
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Patent number: 9193989Abstract: The present invention provides methods of identifying an agent that modulates PRPK, TPRKB, OSGEP, LAGE3 and its homologs, PRPK/TPRKB complex, and/or KEOPS complex. The present invention also provides compositions of such agents and methods of treating a disease, disorder, or condition associated with PRPK, TPRKB, OSGEP, LAGE3 and its homologs family (CT antigens), PRPK/TPRKB complex, and/or KEOPS complex using such an agent or composition.Type: GrantFiled: June 17, 2011Date of Patent: November 24, 2015Assignee: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Eun Sun Park, Henry E. Pelish, Astrid S. Clarke, Grace L. Williams, Maria Paola Castaldi, Alexander Arefolov, Jennifer E. Ring, Matthew D. Shair, Randall W. King
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Patent number: 9127019Abstract: The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: I and salts thereof, wherein R1, R2, R3, R4, n, and m are as defined herein; processes for preparing such compounds and intermediates thereto; pharmaceutical compositions comprising such compounds; methods for treating a proliferative disease; methods for treating a disease associated with aberrant angiogenesis; methods for inhibiting angiogenesis; and processes for preparing cortistatin A, J, K, and L, and analogs thereof.Type: GrantFiled: June 2, 2014Date of Patent: September 8, 2015Assignee: President and Fellows of Harvard CollegeInventors: Alec Nathanson Flyer, Hong Myung Lee, Andrew G. Myers, Cristina Montserrat Nieto-Oberhuber, Matthew D. Shair, Chong Si
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Publication number: 20150111921Abstract: The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: I and salts thereof, wherein R1, R2, R3, R4, n, and m are as defined herein; processes for preparing such compounds and intermediates thereto; pharmaceutical compositions comprising such compounds; methods for treating a proliferative disease; methods for treating a disease associated with aberrant angiogenesis; methods for inhibiting angiogenesis; and processes for preparing cortistatin A, J, K, and L, and analogs thereof.Type: ApplicationFiled: June 2, 2014Publication date: April 23, 2015Applicant: President and Fellows of Harvard CollegeInventors: Alec Nathanson Flyer, Hong Myung Lee, Andrew G. Myers, Cristina Montserrat Nieto-Oberhuber, Matthew D. Shair, Chong Si
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Publication number: 20140135287Abstract: The present invention provides a novel 11-step enantioselective approach to the natural product hyperforin, which enables access to a wide variety of hyperforin analogs. The present invention also provides pharmaceutical compositions comprising inventive hyperforin analogs. Hyperforin analogs synthesized using the present synthetic method are envisioned useful in the treatment of various conditions, including, but not limited to, depression and conditions characterized by depression, inflammatory skin conditions, diabetes, asthma, chronic obstructive pulmonary disease (COPD), kidney disorders, and ischemic brain damage.Type: ApplicationFiled: June 1, 2012Publication date: May 15, 2014Applicant: President and Fellows of Harvard CollegeInventors: Matthew D. Shair, Brian A. Sparling, David Moebius
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Publication number: 20140135279Abstract: Provided are a number of compounds structurally related to OSW-1, a natural compound that binds OSBPs. Also provided are pharmaceutical compositions comprising the OSW-1 analogs, as well as methods for use of these OSW-1 analogs, or pharmaceutically acceptable salts, enantiomers, or stereoisomers thereof in the treatment of atherosclerosis. Alzheimer's disease, and cancer, including p21-deficient cancer. Conjugates of OSW-1 analogs with monoclonal antibodies, including monoclonal antibodies targeted to cancer cells, are also provided. Also provided are pharmaceutical compositions comprising the conjugates, as well as methods for use of these conjugates, in the treatment of cancer, including p21-deficient cancer.Type: ApplicationFiled: May 18, 2012Publication date: May 15, 2014Applicant: President and Fellows of Harvard CollegeInventor: Matthew D. Shair
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Publication number: 20110319277Abstract: The present invention provides methods of identifying an agent that modulates PRPK, TPRKB, OSGEP, LAGE3 and its homologs, PRPK/TPRKB complex, and/or KEOPS complex. The present invention also provides compositions of such agents and methods of treating a disease, disorder, or condition associated with PRPK, TPRKB, OSGEP, LAGE3 and its homologs family (CT antigens), PRPK/TPRKB complex, and/or KEOPS complex using such an agent or composition.Type: ApplicationFiled: June 17, 2011Publication date: December 29, 2011Inventors: Eun Sun Park, Henry E. Pelish, Astrid S. Clarke, Grace L. Williams, Maria Paola Castaldi, Alexander Arefolov, Jennifer E. Ring, Matthew D. Shair, Randall W. King
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Publication number: 20110319352Abstract: The invention relates in part to the discovery that certain CRAMs, such as schweinfurthin A, target OSBPs (a family of oxysterol binding proteins). Because OSBPs have been shown to be integral to atherosclerosis and Alzheimer's disease (AD), one aspect of the invention relates to the use of CRAMs, or a pharmaceutically acceptable salt, biologically active metabolite, solvate, hydrate, prodrug, enantiomer or stereoisomer thereof, in the treatment and/or prevention of atherosclerosis, Alzheimer's disease and related disorders. Another aspect of the invention relates to novel derivatives of CRAMs, or a pharmaceutically acceptable salt, biologically active metabolite, solvate, hydrate, prodrug, enantiomer or stereoisomer thereof, for the treatment and/or prevention of atherosclerosis, Alzheimer's disease and related disorders. Another aspect of the invention relates to the use of an immobilized CRAMs, such as OSW-I, to aid in screening of compounds to identify additional OSBP binders.Type: ApplicationFiled: December 11, 2009Publication date: December 29, 2011Applicant: President and Fellows of Harvard CollegeInventors: Matthew D. Shair, Anthony Burgett, D. Ryan Anderson
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Publication number: 20110190323Abstract: The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: I and salts thereof, wherein R1, R2, R3, R4, n, and m are as defined herein; processes for preparing such compounds and intermediates thereto; pharmaceutical compositions comprising such compounds; methods for treating a proliferative disease; methods for treating a disease associated with aberrant angiogenesis; methods for inhibiting angiogenesis; and processes for preparing cortistatin A, J, K, and L, and analogs thereof.Type: ApplicationFiled: August 28, 2009Publication date: August 4, 2011Applicant: President and Fellows of Harvard CollegeInventors: Alec Nathanson Flyer, Hong Myung Lee, Andrew G. Myers, Cristina Montserrat Nieto-Oberhuber, Matthew D. Shair, Chong Si
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Patent number: 7109377Abstract: The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis.Type: GrantFiled: June 27, 2002Date of Patent: September 19, 2006Assignee: President and Fellows of Harvard CollegeInventors: Stuart L. Schreiber, Matthew D. Shair, Derek S. Tan, Michael A. Foley, Brent R. Stockwell
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Patent number: 7045360Abstract: The present invention provides methods, compounds, and kits useful in the analysis of reaction products and components of reaction mixtures, and in certain embodiments for the rapid and simultaneous determination of enantiomeric ratios, percent conversions, and absolute configurations.Type: GrantFiled: February 7, 2001Date of Patent: May 16, 2006Assignee: President and Fellows of Harvard CollegeInventors: Matthew D. Shair, Gregory A. Korbel, Gojko Lalic
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Publication number: 20030082830Abstract: The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis.Type: ApplicationFiled: June 27, 2002Publication date: May 1, 2003Inventors: Stuart L. Schreiber, Matthew D. Shair, Derek S. Tan, Michael A. Foley, Brent R. Stockwell
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Patent number: 6448443Abstract: The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis.Type: GrantFiled: July 25, 1998Date of Patent: September 10, 2002Assignee: President and Fellows of Harvard CollegeInventors: Stuart L. Schreiber, Matthew D. Shair, Derek S. Tan, Michael A. Foley, Brent R. Stockwell