Patents by Inventor Helen Blackwell
Helen Blackwell 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: 20230094587Abstract: Compounds that regulate quorum sensing in Staphylococcal bacteria and in particular in Staphylococcus aureus are provided. Compounds provided are racemic, non-racemic or substantially enantiomerically pure cyclic peptides of formula I: or salts or solvates thereof, where variables R, W, X1, X2, and Z and are as described in the specification and L1 is a divalent linker which contains 1-12 carbon atoms, optionally 1-4 oxygen atoms, optionally one or two carbon-carbon double bonds, and hydrogen atoms to satisfy valency. Certain dimers of the cyclic peptides are also provided. One or more cylic peptides or dimers thereof herein can be employed to inhibit QS and to thus inhibit virulence in Staphylococcus bacteria. Compounds herein and pharmaceutical compositions containing one or more of these compounds are useful in treating infections of Staphylococcus bacteria. Methods for treating such bacterial infections are also provided.Type: ApplicationFiled: August 29, 2022Publication date: March 30, 2023Inventors: Helen BLACKWELL, Joseph VASQUEZ, Yiftah TAL GAN
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Patent number: 11560361Abstract: Compounds that regulate quorum sensing in Staphylococcal bacteria and in particular in Staphylococcus aureus are provided. Compounds provided are racemic, non-racemic or substantially enantiomerically pure cyclic peptides of formula I: or salts or solvates thereof, where variables R, W, X1, X2, and Z and are as described in the specification and L1 is a divalent linker which contains 1-12 carbon atoms, optionally 1-4 oxygen atoms, optionally one or two carbon-carbon double bonds, and hydrogen atoms to satisfy valency. Certain dimers of the cyclic peptides are also provided. One or more cylic peptides or dimers thereof herein can be employed to inhibit QS and to thus inhibit virulence in Staphylococcus bacteria. Compounds herein and pharmaceutical compositions containing one or more of these compounds are useful in treating infections of Staphylococcus bacteria. Methods for treating such bacterial infections are also provided.Type: GrantFiled: March 24, 2020Date of Patent: January 24, 2023Assignee: Wisconsin Alumni Research FoundationInventors: Helen Blackwell, Joseph Vasquez, Yiftah Tal Gan
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Patent number: 11247976Abstract: RhlR modulators including agonist and antagonists which are useful for modulating QS phenotypes in Gram-negative bacteria. Certain compounds of general formula A-W-HG having various carbocyclic ad heterocyclic head groups (HG) and various tail groups (A), where —W— is —CO—NH—, —SO2—NH—, —CO—NH—CH2—, or —SO2—NH—CH2— are RhlR agonists or antagonists. The compounds are useful in methods of modulating quorum sensing in Gram-negative bacteria, particularly in Pseudomonas. Compositions including certain RhlR modulators are useful for decreasing the virulence of Gram-negative bacteria. Pharmaceutical compositions comprising certain RhlR modulators are useful for treatment of infections of Gram-negative bacteria.Type: GrantFiled: April 30, 2017Date of Patent: February 15, 2022Assignee: Wisconsin Alumni Research FoundationInventors: Helen Blackwell, Michelle E. Boursier, Joseph D. Moore
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Publication number: 20210024476Abstract: Compounds that regulate quorum sensing in Staphylococcal bacteria and in particular in Staphylococcus aureus are provided. Compounds are described in formulas I, II, III, IV, V and VI herein. One or more compounds herein can be employed to inhibit QS and to thus inhibit virulence in Staphylococcus bacteria and in particular in Staphylococcus aureus. Compounds herein and pharmaceutical compositions containing one or more of these compounds are useful, for example, in treating infections of Staphylococcus bacteria and in particular of Staphylococcus aureus. Methods for treating such bacterial infections are provided.Type: ApplicationFiled: March 24, 2020Publication date: January 28, 2021Inventors: Helen BLACKWELL, Joseph VASQUEZ, Yiftah TAL GAN
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Publication number: 20200140489Abstract: Compounds that affect quorum sensing (QS) in Staphylococcus aureus and related Staphylococcus species (e.g., S. epidermidis). Compounds which modulate one or more of the four AgrC receptors of Staphylococcus species, particularly of Staphylococcus aureus. Modulation includes inhibition or activation of one or more of these four AgrC receptors. These compounds are useful for bacterial interference and are useful for treating bacterial infections, particularly staphylococcal infection. Treatment can include combination of one or more of the compounds of the invention in combination with one or more antibiotics.Type: ApplicationFiled: January 8, 2020Publication date: May 7, 2020Applicant: Wisconsin Alumni Research FoundationInventors: Helen BLACKWELL, Yftah TAL-GAN, Danielle STACY
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Patent number: 10597372Abstract: Compounds that regulate quorum sensing in Staphylococcal bacteria and in particular in Staphylococcus aureus are provided. Compounds are described in formulas I, II, III, IV, V and VI herein. One or more compounds herein can be employed to inhibit QS and to thus inhibit virulence in Staphylococcus bacteria and in particular in Staphylococcus aureus. Compounds herein and pharmaceutical compositions containing one or more of these compounds are useful, for example, in treating infections of Staphylococcus bacteria and in particular of Staphylococcus aureus. Methods for treating such bacterial infections are provided.Type: GrantFiled: December 21, 2017Date of Patent: March 24, 2020Assignee: Wisconsin Alumni Research FoundationInventors: Helen Blackwell, Joseph Vasquez, Yiftah Tal Gan
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Publication number: 20200087249Abstract: Modulation of quorum sensing in Gram-negative bacteria, particularly strains of Pseudomonas which form biofilms, by compounds including those of formula I and formula II: where: AR is optionally substituted phenyl, cycloalkyl or cycloalkenyl or heterocyclic, and R1 is optionally substituted alkyl, alkenyl, alkoxyalkyl, or alkylthioalkyl or alkyl substituted at the omega position with optionally substituted phenyl, cyclohexyl or cyclohexenyl. In particular compounds inhibit quorum sensing and biofilm formation.Type: ApplicationFiled: November 21, 2019Publication date: March 19, 2020Applicant: Wisconsin Alumni Research FoundationInventors: Helen BLACKWELL, Daniel MANSON
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Patent number: 10526278Abstract: Modulation of quorum sensing in Gram-negative bacteria, particularly strains of Pseudomonas which form biofilms, by compounds including those of formula I and formula II: where: AR is optionally substituted phenyl, cycloalkyl or cycloalkenyl or heterocyclic, and R1 is optionally substituted alkyl, alkenyl, alkoxyalkyl, or alkylthioalkyl or alkyl substituted at the omega position with optionally substituted phenyl, cyclohexyl or cyclohexenyl. In particular compounds inhibit quorum sensing and biofilm formation. Pharmaceutical compositions for treatment of bacterial infections and methods of treatment of such infections are provided.Type: GrantFiled: October 11, 2018Date of Patent: January 7, 2020Assignee: Wisconsin Alumni Research FoundationInventors: Helen Blackwell, Daniel Manson
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Patent number: 10322112Abstract: Methods for modulating quorum sensing in certain Gram-negative bacteria having multiple QS systems including Las, Rhl, and Pqs with associated receptors (LasR, RhlR and PqsR) which are modulated by small molecule modulators, particularly non-native modulators. Certain combinations of modulators of Las, Rhl and Pqs exhibit improved inhibition of virulence in comparison to the respective individual modulators. In particular, certain combinations of modulators exhibit improved inhibition in nutritionally depleted environments. More specifically, certain combinations of modulators exhibit improved inhibition in environments depleted in phosphate and/or environments depleted in iron. Nutrient depleted environments can mimic environments associated with bacterial infection in humans and non-human animals. The methods are useful in particular for modulating QS in Pseudomonas and Burkholderia.Type: GrantFiled: February 13, 2017Date of Patent: June 18, 2019Assignee: Wisconsin Alumni Research FoundationInventors: Helen Blackwell, Michael Welsh
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Patent number: 10292390Abstract: Compounds described herein inhibit biofilm formation or disperse pre-formed biofilms of Gram-negative bacteria. Biofilm-inhibitory compounds can be encapsulated or contained in a polymer matrix for controlled release. Coatings, films, multilayer films, hydrogels, microspheres and nanospheres as well as pharmaceutical compositions and disinfecting compositions containing biofilm-inhibitory compounds are also provided. Methods for inhibiting formation of biofilms or dispersing already formed biofilms are provided. Methods for treating infections of gram-negative bacteria which form biofilms, particularly those of Pseudomonas and more particularly P. aeruginosa.Type: GrantFiled: November 5, 2012Date of Patent: May 21, 2019Assignee: Wisconsin Alumni Research FoundationInventors: Helen Blackwell, Reto Frei, Anthony Breitbach, David M. Lynn, Adam H. Broderick
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Publication number: 20190144407Abstract: RhlR modulators including agonist and antagonists which are useful for modulating QS phenotypes in Gram-negative bacteria. Certain compounds of general formula A-W-HG having various carbocyclic ad heterocyclic head groups (HG) and various tail groups (A), where —W— is —CO—NH—, —SO2—NH—, —CO—NH—CH2—, or —SO2—NH—CH2— are RhlR agonists or antagonists. The compounds are useful in methods of modulating quorum sensing in Gram-negative bacteria, particularly in Pseudomonas. Compositions including certain RhlR modulators are useful for decreasing the virulence of Gram-negative bacteria. Pharmaceutical compositions comprising certain RhlR modulators are useful for treatment of infections of Gram-negative bacteria.Type: ApplicationFiled: April 30, 2017Publication date: May 16, 2019Inventors: Helen BLACKWELL, Michelle E. BOURSIER, Joseph D. MOORE
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Publication number: 20190119201Abstract: Modulation of quorum sensing in Gram-negative bacteria, particularly strains of Pseudomonas which form biofilms, by compounds including those of formula I and formula II: where: AR is optionally substituted phenyl, cycloalkyl or cycloalkenyl or heterocyclic, and R1 is optionally substituted alkyl, alkenyl, alkoxyalkyl, or alkylthioalkyl or alkyl substituted at the omega position with optionally substituted phenyl, cyclohexyl or cyclohexenyl. In particular compounds inhibit quorum sensing and biofilm formation.Type: ApplicationFiled: October 11, 2018Publication date: April 25, 2019Inventors: Helen BLACKWELL, Daniel MANSON
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Publication number: 20180170889Abstract: Compounds that regulate quorum sensing in Staphylococcal bacteria and in particular in Staphylococcus aureus are provided. Compounds are described in formulas I, II, III, IV, V and VI herein. One or more compounds herein can be employed to inhibit QS and to thus inhibit virulence in Staphylococcus bacteria and in particular in Staphylococcus aureus. Compounds herein and pharmaceutical compositions containing one or more of these compounds are useful, for example, in treating infections of Staphylococcus bacteria and in particular of Staphylococcus aureus. Methods for treating such bacterial infections are provided.Type: ApplicationFiled: December 21, 2017Publication date: June 21, 2018Inventors: Helen BLACKWELL, Joseph VASQUEZ, Yftah TAL-GAN
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Publication number: 20170231962Abstract: Methods for modulating quorum sensing in certain Gram-negative bacteria having multiple QS systems including Las, Rhl, and Pqs with associated receptors (LasR, RhlR and PqsR) which are modulated by small molecule modulators, particularly non-native modulators. Certain combinations of modulators of Las, Rhl and Pqs exhibit improved inhibition of virulence in comparison to the respective individual modulators. In particular, certain combinations of modulators exhibit improved inhibition in nutritionally depleted environments. More specifically, certain combinations of modulators exhibit improved inhibition in environments depleted in phosphate and/or environments depleted in iron. Nutrient depleted environments can mimic environments associated with bacterial infection in humans and non-human animals. The methods are useful in particular for modulating QS in Pseudomonas and Buckholderia.Type: ApplicationFiled: February 13, 2017Publication date: August 17, 2017Inventors: Helen BLACKWELL, Michael Welsh
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Publication number: 20160194360Abstract: Compounds that affect quorum sensing (QS) in Staphylococcus aureus and related Staphylococcus species (e.g., S. epidermidis). Compounds which modulate one or more of the four AgrC receptors of Staphylococcus species, particularly of Staphylococcus aureus. Modulation includes inhibition or activation of one or more of these four AgrC receptors. These compounds are useful for bacterial interference and are useful for treating bacterial infections, particularly staphylococcal infection. Treatment can include combination of one or more of the compounds of the invention in combination with one or more antibiotics.Type: ApplicationFiled: January 4, 2016Publication date: July 7, 2016Inventors: Helen BLACKWELL, Yftah TAL-GAN, Danielle STACY
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Patent number: 9227996Abstract: Compounds that affect quorum sensing (QS) in Staphylococcus aureus and related Staphylococcus species (e.g., S. epidermidis). Compounds which modulate one or more of the four AgrC receptors of Staphylococcus species, particularly of Staphylococcus aureus. Modulation includes inhibition or activation of one or more of these four AgrC receptors. These compounds are useful for bacterial interference and are useful for treating bacterial infections, particularly staphylococcal infection. Treatment can include combination of one or more of the compounds of the invention in combination with one or more antibiotics.Type: GrantFiled: December 17, 2013Date of Patent: January 5, 2016Assignee: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Helen Blackwell, Yftah Tal-Gan, Danielle Stacy
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Publication number: 20140256615Abstract: Compounds that affect quorum sensing (QS) in Staphylococcus aureus and related Staphylococcus species (e.g., S. epidermidis). Compounds which modulate one or more of the four AgrC receptors of Staphylococcus species, particularly of Staphylococcus aureus. Modulation includes inhibition or activation of one or more of these four AgrC receptors. These compounds are useful for bacterial interference and are useful for treating bacterial infections, particularly staphylococcal infection. Treatment can include combination of one or more of the compounds of the invention in combination with one or more antibiotics.Type: ApplicationFiled: December 17, 2013Publication date: September 11, 2014Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Helen BLACKWELL, Yftah TAL-GAN, Danielle STACY
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Publication number: 20130136782Abstract: Compounds described herein inhibit biofilm formation or disperse pre-formed biofilms of Gram-negative bacteria. Biofilm-inhibitory compounds can be encapsulated or contained in a polymer matrix for controlled release. Coatings, films, multilayer films, hydrogels, microspheres and nanospheres as well as pharmaceutical compositions and disinfecting compositions containing biofilm-inhibitory compounds are also provided. Methods for inhibiting formation of biofilms or dispersing already formed biofilms are provided. Methods for treating infections of gram-negative bacteria which form biofilms, particularly those of Pseudomonas and more particularly P. aeruginosa.Type: ApplicationFiled: November 5, 2012Publication date: May 30, 2013Inventors: Helen BLACKWELL, Reto Frei, Anthony Breitbach, David M. Lynn, Adam H. Broderick
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Publication number: 20080009528Abstract: The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use. For example, the present invention provides chalcone and cyanopyridine compounds, and derivatives thereof, exhibiting high antibacterial activities having multiple electron withdrawing group substituents, such as halogens and fluorinated alky groups, and optionally having hydroxyl and/or alkoxyl groups substituents.Type: ApplicationFiled: May 16, 2007Publication date: January 10, 2008Inventors: Helen Blackwell, Matthew Bowman, Jennifer O'Neill, Joseph Stringer
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Publication number: 20070128658Abstract: The present invention provides a method for identifying and characterizing candidate fluorescent molecules. This method involves the generation of spatially addressed arrays of heterocyclic compounds which are candidate fluorescent molecules. The spatially addressed array can be used to identify fluorescent molecules among the candidate molecules. The spatially addressed array can be used to determine the optical characteristics of one more candidate molecules. The invention also provides methods for making such arrays of heterocyclic compounds. In a specific embodiment, synthetic methods are provided for synthesis of triarylpyridines, particularly unsymmetric triarylpyridines. n preferred embodiments, the present invention provides novel heterocyclic fluorescent compounds having deazalumazine, cyanopyridine or pyrimidine cores. Heterocyclic fluorescent compounds of this invention are useful as dyes to label molecules such as nucleic acids, peptides and proteins, and particularly antibodies.Type: ApplicationFiled: November 14, 2006Publication date: June 7, 2007Inventors: Helen Blackwell, Matthew Bowman