Patents by Inventor Timothy L. Macdonald
Timothy L. Macdonald 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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Patent number: 10369120Abstract: The present invention provides novel T type calcium channel inhibitors of formula (I), the use thereof in the treatment of a disease or condition in a mammal associated with influx of extracellular calcium via T type calcium channels, wherein R1 is C1-C4 alkyl, hydroxy, or C1-C4 alkoxy; Z is NH, NCH3, O, S, or CH2; Y is NH, O, or CH2 with the proviso that Y and Z are not the same; R2 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy; m and n are independently selected from integers ranging from 1-5 with the proviso that m+n=an integer ranging from 2-9; and R3 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy.Type: GrantFiled: November 5, 2015Date of Patent: August 6, 2019Assignee: University of Virginia Patent FoundationInventors: Lloyd S. Gray, Timothy L. Macdonald, Doris M. Haverstick, Jaclyn R. Patterson, William F. McCalmont
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Patent number: 9908849Abstract: Imidamide (amidine) analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumors.Type: GrantFiled: August 19, 2016Date of Patent: March 6, 2018Assignee: University of Virginia Patent FoundationInventors: Kevin R. Lynch, Timothy L. Macdonald, Thomas P. Mathews, Andrew Kennedy, Yugesh Kharel
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Patent number: 9688668Abstract: The invention relates to inhibitors of Sphingosine Kinase enzymatic activity, and methods of treating diseases and disorders by administering inhibitors of Sphingosine Kinase enzymatic activity.Type: GrantFiled: February 8, 2013Date of Patent: June 27, 2017Assignee: University of Virginia Patent FoundationInventors: Webster L. Santos, Kevin R. Lynch, Timothy L. Macdonald, Andrew Kennedy, Yugesh Kharel, Mithun Rajendra Raje, Joseph Houck
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Publication number: 20170166525Abstract: Imidamide (amidine) analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumors.Type: ApplicationFiled: August 19, 2016Publication date: June 15, 2017Inventors: Kevin R. Lynch, Timothy L. Macdonald, Thomas P. Mathews, Andrew Kennedy, Yugesh Kharel
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Patent number: 9421177Abstract: Imidamide (amidine) analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumors.Type: GrantFiled: August 16, 2010Date of Patent: August 23, 2016Assignee: University of Virginia Patent FoundationInventors: Kevin R. Lynch, Timothy L. Macdonald, Thomas P. Mathews, Andrew Kennedy, Yugesh Kharel
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Patent number: 9376430Abstract: The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.Type: GrantFiled: July 30, 2014Date of Patent: June 28, 2016Assignee: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. Macdonald, Thomas Eric Ballard, Jr.
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Publication number: 20160136115Abstract: The present invention provides novel T type calcium channel inhibitors of formula (I), the use thereof in the treatment of a disease or condition in a mammal associated with influx of extracellular calcium via T type calcium channels, wherein R1 is C1-C4 alkyl, hydroxy, or C1-C4 alkoxy; Z is NH, NCH3, O, S, or CH2; Y is NH, O, or CH2 with the proviso that Y and Z are not the same; R2 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy; m and n are independently selected from integers ranging from 1-5 with the proviso that m+n=an integer ranging from 2-9; and R3 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy.Type: ApplicationFiled: November 5, 2015Publication date: May 19, 2016Inventors: Lloyd S. Gray, Timothy L. Macdonald, Doris M. Haverstick, Jaclyn R. Patterson, William F. McCalmont
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Patent number: 9333193Abstract: The invention provides for the use of antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit anti-mycobacteria activity, including the mycobacterium causing tuberculosis. Multiple compounds were synthesized and screened for anti-tuberculosis activity. Disclosed herein are a series of compounds with anti-tuberculosis activity, including six leads that completely inhibited bacterial growth at 5 micrograms per ml or less. Three of these compounds were tested to determine MIC and these ranged between 1 and 4 micrograms per ml against both drug susceptible Mycobacterium tuberculosis strains and strains that are multi-drug resistant (MDR) including XDR strains. The compounds developed are derived from parent compound nitazoxanide, which had no inhibitory activity in the stringent testing format used herein.Type: GrantFiled: September 20, 2011Date of Patent: May 10, 2016Assignee: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Paul S. Hoffman, Timothy L. MacDonald, Eric R. Houpt, Thomas E. Ballard, Jr.
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Patent number: 9278098Abstract: Phthalazine analogs of a Lisofylline (LSF) and synthetic methods for preparation of such analogs are provided. Compounds of the invention have structural formula III: wherein 1) R3a is hydrogen and R3b is selected from C5-22alkyl, C2-22alkenyl, or C2-22alkynyl; or a pharmaceutically acceptable salt thereof; or 2) R3b is hydrogen and R3a is selected from C9alkyl, C15-22alkyl, C9-22alkenyl, or C2-22alkynyl; or a pharmaceutically acceptable salt thereof; or 3) R3a and R3b are the same or different and are selected from C9alkyl, C15-22alkyl, C4-22alkenyl, or C2-22alkynyl; or a pharmaceutically acceptable salt thereof. The analogs of LSF provided have the ability to protect cell viability, particularly the ability to protect pancreatic ?-cells, to induce insulin secretion.Type: GrantFiled: October 27, 2014Date of Patent: March 8, 2016Assignee: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
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Patent number: 9212127Abstract: The present invention provides novel T type calcium channel inhibitors of formula (I), the use thereof in the treatment of a disease or condition in a mammal associated with influx of extracellular calcium via T type calcium channels, wherein R1 is C1-C4 alkyl, hydroxy, or C1-C4 alkoxy; Z is NH, NCH3, O, S, or CH2; Y is NH, O, or CH2 with the proviso that Y and Z are not the same; R2 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy; m and n are independently selected from integers ranging from 1-5 with the proviso that m+n=an integer ranging from 2-9; and R3 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy.Type: GrantFiled: August 22, 2005Date of Patent: December 15, 2015Assignee: University of Virginia Patent FoundationInventors: Lloyd S. Gray, Timothy L. MacDonald, Doris M. Haverstick, Jaclyn R. Patterson, William F. McCalmont
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Publication number: 20150210675Abstract: The invention relates to inhibitors of Sphingosine Kinase enzymatic activity, and methods of treating diseases and disorders by administering inhibitors of Sphingosine Kinase enzymatic activity.Type: ApplicationFiled: February 8, 2013Publication date: July 30, 2015Inventors: Santos L. Webster, Kevin R. Lynch, Timothy L. Macdonald, Andrew Kennedy, Yugesh Kharel, Mithun Rajendra Raje, Joseph Houck
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Publication number: 20150164892Abstract: Analogs of a Lisofylline (LSF), and synthetic methods for preparation of such analogs are provided. The analogs of LSF provided have the ability to protect cell viability, particularly the ability to protect pancreatic ?-cells.Type: ApplicationFiled: October 27, 2014Publication date: June 18, 2015Inventors: Timothy L. MACDONALD, Jerry L. NADLER, Peng CUI
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Patent number: 8987321Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.Type: GrantFiled: June 27, 2013Date of Patent: March 24, 2015Assignee: University of Virginia Patent FoundationInventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
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Publication number: 20150018330Abstract: The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.Type: ApplicationFiled: July 30, 2014Publication date: January 15, 2015Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. MacDonald, Thomas Eric Ballard, JR.
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Patent number: 8871764Abstract: Analogs of a Lisofylline (LSF), and synthetic methods for the preparation of such analogs are provided. The analogs of LSF provided have the ability to protect cell viability, particularly the ability to protect pancreatic ?-cells.Type: GrantFiled: May 22, 2012Date of Patent: October 28, 2014Assignee: University of Virginia Patent FoundationInventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
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Patent number: 8835644Abstract: The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.Type: GrantFiled: March 16, 2010Date of Patent: September 16, 2014Assignee: University of Virginia Patent FoundationInventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. Macdonald, Thomas Eric Ballard, Jr.
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Patent number: 8686046Abstract: Amidine analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumor cells.Type: GrantFiled: October 2, 2010Date of Patent: April 1, 2014Assignee: University of Virginia Patent FoundationInventors: Kevin R. Lynch, Timothy L. Macdonald, Yugesh Kharel, Thomas P. Mathews, Brian R. Wamhoff
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Publication number: 20140018355Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.Type: ApplicationFiled: June 27, 2013Publication date: January 16, 2014Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Timothy L. MACDONALD, Jerry L. NADLER, Peng CUI
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Publication number: 20130317070Abstract: The invention provides for the use of antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit anti-mycobacteria activity, including the mycobacterium causing tuberculosis. Multiple compounds were synthesized and screened for anti-tuberculosis activity. Disclosed herein are a series of compounds with anti-tuberculosis activity, including six leads that completely inhibited bacterial growth at 5 micrograms per ml or less. Three of these compounds were tested to determine MIC and these ranged between 1 and 4 micrograms per ml against both drug susceptible Mycobacterium tuberculosis strains and strains that are multi-drug resistant (MDR) including XDR strains. The compounds developed are derived from parent compound nitazoxanide, which had no inhibitory activity in the stringent testing format used herein.Type: ApplicationFiled: September 20, 2011Publication date: November 28, 2013Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATION D/B/A UNIVERSITY OF VIRGINIA LICENSING & VENTURES GROUPInventors: Paul S. Hoffman, Timothy L. MacDonald, Eric R. Houpt, Thomas E. Ballard
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Patent number: 8481580Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.Type: GrantFiled: February 25, 2008Date of Patent: July 9, 2013Assignee: University of Virginia Patent FoundationInventors: Timothy L. Macdonald, Jerry L. Nadler, Peng Cui