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).
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Publication number: 20210206791Abstract: 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: ApplicationFiled: March 2, 2017Publication date: July 8, 2021Inventors: Stephen L. Buchwald, Bradley L Pentelute, Chi Zhang
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Publication number: 20190055280Abstract: 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: ApplicationFiled: July 15, 2015Publication date: February 21, 2019Inventors: Stephen L. Buchwald, Brandley L. Pentelute, Alexander M. Spoloyny, Ekaterina V. Vinogradova, Chi Zhang
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Patent number: 10117948Abstract: 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: GrantFiled: June 20, 2016Date of Patent: November 6, 2018Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Bradley L. Pentelute, Daniel T. Cohen, Chi Zhang
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Patent number: 9972791Abstract: Disclosed are [2.2]paracyclophane-derivative compounds and related polymers that are useful as stable, efficient, blue-light emitting compounds for OLED applications.Type: GrantFiled: June 3, 2016Date of Patent: May 15, 2018Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Wenliang Huang
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Patent number: 9944607Abstract: 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: GrantFiled: October 16, 2013Date of Patent: April 17, 2018Assignees: 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
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Publication number: 20180028528Abstract: 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: ApplicationFiled: October 5, 2017Publication date: February 1, 2018Inventors: Jane Hirsh, Alexander M. Klibanov, Timothy M. Swager, Stephen L. Buchwald, Whe Yong Lo, Alison B. Fleming, Roman V. Rariy
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Patent number: 9790188Abstract: 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: GrantFiled: March 17, 2014Date of Patent: October 17, 2017Assignees: Whitehead Institute for Biomedical Research, Massachusetts Institute of TechnologyInventors: Susan L. Lindquist, Stephen L. Buchwald, Daniel Tardiff, Nathan Jui
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Patent number: 9738610Abstract: 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: GrantFiled: September 24, 2013Date of Patent: August 22, 2017Assignees: Whitehead Institute for Biomedical Research, The Broad Institute, Inc., Massachusetts Institute of TechnologyInventors: 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
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Patent number: 9595682Abstract: 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: GrantFiled: October 30, 2013Date of Patent: March 14, 2017Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Timothy M. Swager, Georgiy Teverovskiy, Mingjuan Su
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Publication number: 20160367693Abstract: 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: ApplicationFiled: June 20, 2016Publication date: December 22, 2016Inventors: Stephen L. Buchwald, Bradley L. Pentelute, Daniel T. Cohen, Chi Zhang
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Publication number: 20160359118Abstract: Disclosed are [2.2]paracyclophane-derivative compounds and related polymers that are useful as stable, efficient, blue-light emitting compounds for OLED applications.Type: ApplicationFiled: June 3, 2016Publication date: December 8, 2016Inventors: Stephen L. Buchwald, Wenliang Huang
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Publication number: 20160031824Abstract: 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: ApplicationFiled: March 17, 2014Publication date: February 4, 2016Applicants: Whitehead Institute for Biomedical Research, Massachusetts Institute of TechnologyInventors: Susan L. Lindquist, Stephen L. Buchwald, Daniel Tardiff, Nathan Jui
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Publication number: 20150353503Abstract: 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: ApplicationFiled: September 24, 2013Publication date: December 10, 2015Applicants: WHITEHEAD INSTITUTE FOR BIOMEDICAL RESEARCH, THE BROAD INSTITUTE, INC., MASSACHUSETTS INSTITUTE OF TECHNOLOGYInventors: 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
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Publication number: 20150265596Abstract: 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: ApplicationFiled: May 20, 2015Publication date: September 24, 2015Inventors: Jane Hirsh, Alexander M. Klibanov, Timothy M. Swager, Stephen L. Buchwald, Whe Yong Lo, Alison B. Fleming, Roman V. Rariy
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Publication number: 20150259298Abstract: 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: ApplicationFiled: October 16, 2013Publication date: September 17, 2015Applicants: 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
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Patent number: 9067955Abstract: 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 alkyType: GrantFiled: May 9, 2006Date of Patent: June 30, 2015Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Artis Klapars, Jon C. Antilla, Gabriel E. Job, Martina Uhlenbrock, Fuk Y. Kwong, Gero Nordmann, Edward J. Hennessy
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Patent number: 9044398Abstract: 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: GrantFiled: July 17, 2012Date of Patent: June 2, 2015Assignee: Collegium Pharmaceutical, Inc.Inventors: Jane Hirsh, Alexander M. Klibanov, Timothy M. Swager, Stephen L. Buchwald, Whe Yong Lo, Alison Fleming, Roman V. Rariy
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Patent number: 8981086Abstract: 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: GrantFiled: October 23, 2014Date of Patent: March 17, 2015Assignee: Massachusetts Institute of TechnologyInventors: Nicholas C. Bruno, Stephen L. Buchwald
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Publication number: 20150045570Abstract: 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: ApplicationFiled: October 23, 2014Publication date: February 12, 2015Inventors: Nicholas C. Bruno, Stephen L. Buchwald
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Patent number: 8889857Abstract: 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: GrantFiled: March 13, 2013Date of Patent: November 18, 2014Assignee: Massachusetts Institute of TechnologyInventors: Nicholas C. Bruno, Stephen L. Buchwald