Patents by Inventor Stephen L. Buchwald

Stephen L. Buchwald 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).

  • Publication number: 20210206791
    Abstract: Disclosed are methods of selective cysteine and selenocysteine modification on peptide/protein molecules under physiologically relevant conditions. The methods feature several advantages over existing methods of peptide modification, such as specificity towards thiols and selenols over other nucleophiles (e.g., amines, hydroxyls), excellent functional group tolerance, and mild reaction conditions, including completely aqueous reaction conditions. Also disclosed are methods of preparing palladium complexes in the presence of oxygen.
    Type: Application
    Filed: March 2, 2017
    Publication date: July 8, 2021
    Inventors: Stephen L. Buchwald, Bradley L Pentelute, Chi Zhang
  • Publication number: 20190055280
    Abstract: Disclosed are methods of selective cysteine and selenocysteine modification on peptide/protein molecules under physiologically relevant conditions. The methods feature several advantages over existing methods of peptide modification, such as specifically toward thiols and selenols over other nucleophiles (e.g., amines, hydroxyls), excellent functional group tolerance, and mild reaction conditions.
    Type: Application
    Filed: July 15, 2015
    Publication date: February 21, 2019
    Inventors: Stephen L. Buchwald, Brandley L. Pentelute, Alexander M. Spoloyny, Ekaterina V. Vinogradova, Chi Zhang
  • Patent number: 10117948
    Abstract: Disclosed are chemical transformations for the conjugation of unprotected peptide biomolecules. The disclosed chemical transformations relate to methods of selective cysteine and selenocysteine functionalization of unprotected peptide and protein molecules. The processes feature several significant advantages over existing methods of peptide modification, including specificity towards selenocysteine over other nucleophiles (e.g., amines, hydroxyls), excellent functional group tolerance, and mild reaction conditions. Also disclosed are syntheses of arylated cysteine and arylated selenocysteine peptide compounds.
    Type: Grant
    Filed: June 20, 2016
    Date of Patent: November 6, 2018
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, Bradley L. Pentelute, Daniel T. Cohen, Chi Zhang
  • Patent number: 9972791
    Abstract: Disclosed are [2.2]paracyclophane-derivative compounds and related polymers that are useful as stable, efficient, blue-light emitting compounds for OLED applications.
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: May 15, 2018
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, Wenliang Huang
  • Patent number: 9944607
    Abstract: The present invention provides novel compounds (e.g., compounds of Formula (I)), and pharmaceutically acceptable salts, solvates, hydrate, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits comprising the inventive Compounds, or compositions thereof, for treating and/or preventing a fungal or protozoan infection, inhibiting the activity of a fungal or protozoan enzyme, killing a fungus or protozoan, or inhibiting the growth of a fungus or protozoan. The fungus may be a Candida species, Sacchawmyces species, or other pathogenic fungal species. The compounds of the invention may inhibit the activity of fungal or protozoan mitochondrial phosphate carrier protein.
    Type: Grant
    Filed: October 16, 2013
    Date of Patent: April 17, 2018
    Assignees: Whitehead Institute for Biomedical Research, Massachusetts Institute of Technology, The Broad Institute, Inc.
    Inventors: Benjamin Vincent, Luke Whitesell, Susan L. Lindquist, Willmen Youngsaye, Stephen L. Buchwald, Jean-Baptiste Langlois, Jun Pu, Benito Munoz, Sivaraman Dandapani
  • Publication number: 20180028528
    Abstract: An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble, but enzymatically degradable by enzymes present in the human gastrointestinal tract. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed.
    Type: Application
    Filed: October 5, 2017
    Publication date: February 1, 2018
    Inventors: Jane Hirsh, Alexander M. Klibanov, Timothy M. Swager, Stephen L. Buchwald, Whe Yong Lo, Alison B. Fleming, Roman V. Rariy
  • Patent number: 9790188
    Abstract: 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 pharmaceutical compositions thereof. The present invention also provides methods and kits using the inventive compounds and pharmaceutical compositions for treating and/or preventing diseases associated with protein aggregation, such as amyloidoses (e.g., Parkinson's disease and Alzheimer's disease), treating and/or preventing neurodegenerative diseases, treating and/or preventing diseases associated with Tar DNA binding protein 43 kDa, reducing or preventing protein aggregation, and/or modulating E3 ubiquitin ligase in a subject in need thereof.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: October 17, 2017
    Assignees: Whitehead Institute for Biomedical Research, Massachusetts Institute of Technology
    Inventors: Susan L. Lindquist, Stephen L. Buchwald, Daniel Tardiff, Nathan Jui
  • Patent number: 9738610
    Abstract: The present invention provides novel compounds (e.g., 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 comprising the inventive compounds, or compositions thereof, for treating and/or preventing a fungal or protozoan infection, inhibiting the activity of a fungal or protozoan enzyme, killing a fungus or protozoon, or inhibiting the growth of a fungus or protozoon. The fungus may be a Candida species, Aspergillus species, or other pathogenic fungal species. The compounds of the invention may inhibit the activity of fungal or protozoan cytochrome b and/or fungal or protozoan Hsp90. The present invention also provides synthetic methods of the inventive compounds.
    Type: Grant
    Filed: September 24, 2013
    Date of Patent: August 22, 2017
    Assignees: Whitehead Institute for Biomedical Research, The Broad Institute, Inc., Massachusetts Institute of Technology
    Inventors: Benjamin Vincent, Luke Whitesell, Susan L. Lindquist, Willmen Youngsaye, Stephen L. Buchwald, Jean-Baptiste Langlois, Partha P. Nag, Amal Ting, Barbara J. Morgan, Benito Munoz, Sivaraman Dandapani, Bruce Tidor, Raja R. Srinivas
  • Patent number: 9595682
    Abstract: Embodiments described herein relate to compositions including iptycene-based structures and extended iptycene structures. In some embodiments, the compositions may be useful in organic light-emitting diodes (OLEDs), organic photovoltaics, and other devices.
    Type: Grant
    Filed: October 30, 2013
    Date of Patent: March 14, 2017
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, Timothy M. Swager, Georgiy Teverovskiy, Mingjuan Su
  • Publication number: 20160367693
    Abstract: Disclosed are chemical transformations for the conjugation of unprotected peptide biomolecules. The processes feature several significant advantages over existing methods of peptide modification, including specificity towards selenocysteine over other nucleophiles (e.g., amines, hydroxyls), excellent functional group tolerance, and mild reaction conditions.
    Type: Application
    Filed: June 20, 2016
    Publication date: December 22, 2016
    Inventors: Stephen L. Buchwald, Bradley L. Pentelute, Daniel T. Cohen, Chi Zhang
  • Publication number: 20160359118
    Abstract: Disclosed are [2.2]paracyclophane-derivative compounds and related polymers that are useful as stable, efficient, blue-light emitting compounds for OLED applications.
    Type: Application
    Filed: June 3, 2016
    Publication date: December 8, 2016
    Inventors: Stephen L. Buchwald, Wenliang Huang
  • Publication number: 20160031824
    Abstract: 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 pharmaceutical compositions thereof. The present invention also provides methods and kits using the inventive compounds and pharmaceutical compositions for treating and/or preventing diseases associated with protein aggregation, such as amyloidoses (e.g., Parkinson's disease and Alzheimer's disease), treating and/or preventing neurodegenerative diseases, treating and/or preventing diseases associated with Tar DNA binding protein 43 kDa, reducing or preventing protein aggregation, and/or modulating E3 ubiquitin ligase in a subject in need thereof.
    Type: Application
    Filed: March 17, 2014
    Publication date: February 4, 2016
    Applicants: Whitehead Institute for Biomedical Research, Massachusetts Institute of Technology
    Inventors: Susan L. Lindquist, Stephen L. Buchwald, Daniel Tardiff, Nathan Jui
  • Publication number: 20150353503
    Abstract: The present invention provides novel compounds (e.g., 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 comprising the inventive compounds, or compositions thereof, for treating and/or preventing a fungal or protozoan infection, inhibiting the activity of a fungal or protozoan enzyme, killing a fungus or protozoon, or inhibiting the growth of a fungus or protozoon. The fungus may be a Candida species, Aspergillus species, or other pathogenic fungal species. The compounds of the invention may inhibit the activity of fungal or protozoan cytochrome b and/or fungal or protozoan Hsp90. The present invention also provides synthetic methods of the inventive compounds.
    Type: Application
    Filed: September 24, 2013
    Publication date: December 10, 2015
    Applicants: WHITEHEAD INSTITUTE FOR BIOMEDICAL RESEARCH, THE BROAD INSTITUTE, INC., MASSACHUSETTS INSTITUTE OF TECHNOLOGY
    Inventors: Benjamin VINCENT, Luke WHITESELL, Susan L. LINQUIST, Willmen YOUNGSAYE, Stephen L. BUCHWALD, Jean-Baptiste LANGLOIS, Partha P. NAG, Amal TING, Barbara J. MORGAN, Benito MUNOZ, Sivaraman DANDAPANI, Bruce TIDOR, Raja R. SRINIVAS
  • Publication number: 20150265596
    Abstract: An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble, but enzymatically degradable by enzymes present in the human gastrointestinal tract. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed.
    Type: Application
    Filed: May 20, 2015
    Publication date: September 24, 2015
    Inventors: Jane Hirsh, Alexander M. Klibanov, Timothy M. Swager, Stephen L. Buchwald, Whe Yong Lo, Alison B. Fleming, Roman V. Rariy
  • Publication number: 20150259298
    Abstract: The present invention provides novel compounds (e.g., compounds of Formula (I)), and pharmaceutically acceptable salts, solvates, hydrate, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits comprising the inventive compounds, or compositions thereof, for treating and/or preventing a fungal or protozoan infection, inhibiting the activity of a fungal or protozoan enzyme, killing a fungus or protozoan, or inhibiting the growth of a fungus or protozoan. The fungus may be a Candida species, Sacchawmyces species, or other pathogenic fungal species. The compounds of the invention may inhibit the activity of fungal or protozoan mitochondrial phosphate carrier protein.
    Type: Application
    Filed: October 16, 2013
    Publication date: September 17, 2015
    Applicants: Whitehead Institute for biomedical Research, Massachusetts Institute of Technology, The Broad Institute, Inc.
    Inventors: Benjamin Vincent, Luke Whitesell, Susan L. Lindquist, Willmen Youngsaye, Stephen L. Buchwald, Jean-Baptiste Langlois, Jun Pu, Benito Munoz, Sivaraman Dandapani
  • Patent number: 9067955
    Abstract: The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods, such as the reaction of Z-X with C(L)(R)(R?)2 in the present of a catalyst and a base, thereby forming C(Z)(R)(R?)2; wherein X represents I, Cl, alkylsulfonate, or arylsulfonate; Z represents optionally substituted aryl, heteroaryl or alkenyl; L represents H or a negative charge; catalyst comprises a copper atom or ion, and a ligand, wherein the ligand is an optionally substituted aryl alcohol, alkyl amine, 1,2-diamine, 1,2-aminoalcohol, 1,2-diol, imidazolium carbene, pyridine, or 1,10-phenanthroline; the ligand is a chelating ligand; and the base represents a Bronsted base; R represents H, optionally substituted alkyl, cycloalkyl, aralkyl, aryl, or heteroaryl; R? represents independently for each occurrence H, alkyl, cycloalkyl, aralkyl, aryl, or heteroaryl, formyl, acyl, —CO2R?, —C(O)N(R)2, sulfonyl, —P(O)(OR?)2, —CN, or —NO2; R? represents independently for each occurrence optionally substituted alky
    Type: Grant
    Filed: May 9, 2006
    Date of Patent: June 30, 2015
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, Artis Klapars, Jon C. Antilla, Gabriel E. Job, Martina Uhlenbrock, Fuk Y. Kwong, Gero Nordmann, Edward J. Hennessy
  • Patent number: 9044398
    Abstract: An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the GI tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.
    Type: Grant
    Filed: July 17, 2012
    Date of Patent: June 2, 2015
    Assignee: Collegium Pharmaceutical, Inc.
    Inventors: Jane Hirsh, Alexander M. Klibanov, Timothy M. Swager, Stephen L. Buchwald, Whe Yong Lo, Alison Fleming, Roman V. Rariy
  • Patent number: 8981086
    Abstract: Described are palladium precatalysts, and methods of making and using them. The palladium precatalysts show improved stability and improved reactivity in comparison to previously-described palladium precatalysts.
    Type: Grant
    Filed: October 23, 2014
    Date of Patent: March 17, 2015
    Assignee: Massachusetts Institute of Technology
    Inventors: Nicholas C. Bruno, Stephen L. Buchwald
  • Publication number: 20150045570
    Abstract: Described are palladium precatalysts, and methods of making and using them. The palladium precatalysts show improved stability and improved reactivity in comparison to previously-described palladium precatalysts.
    Type: Application
    Filed: October 23, 2014
    Publication date: February 12, 2015
    Inventors: Nicholas C. Bruno, Stephen L. Buchwald
  • Patent number: 8889857
    Abstract: Described are palladium precatalysts, and methods of making and using them. The palladium precatalysts show improved stability and improved reactivity in comparison to previously-described palladium precatalysts.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: November 18, 2014
    Assignee: Massachusetts Institute of Technology
    Inventors: Nicholas C. Bruno, Stephen L. Buchwald