Patents by Inventor Webster L. Santos
Webster L. Santos 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: 11896591Abstract: This disclosure provides compounds of Formula I, II, and III and pharmaceutically acceptable salts thereof for use as mitochondrial uncouplers, where the variables, e.g. R1-R9, X1, X2, and Y1 are defined in the specification. The disclosure also provides pharmaceutical compositions comprising a compound or pharmaceutically acceptable salt of Formula I, II, or III, alone or in combination with another active compound. Compounds and compositions of Formula I, II, and III are useful for treating or preventing certain conditions such as obesity, type II diabetes, fatty liver disease, insulin resistance, Parkinson's disease, ischemia reperfusion injury, heart failure, non-alcoholic fatty liver disease (NALFD), and non-alcoholic steatohepatitis (NASH). Compounds of Formula I, II, and III are also useful for regulating glucose homeostatis and insulin action.Type: GrantFiled: May 22, 2018Date of Patent: February 13, 2024Assignee: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Kyle Hoehn, Webster L. Santos, Elizabeth S. Childress, Yumin Dai, Jacob Murray, Jose Santiago-Rivera
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Publication number: 20230373937Abstract: The present disclosure provides SPNS2 inhibitor compounds according to Formula (I) and their pharmaceutically acceptable salts, and/or tautomers as described in the disclosure, and the disclosure provides their pharmaceutical compositions and methods of use in therapy.Type: ApplicationFiled: September 8, 2021Publication date: November 23, 2023Inventors: Kevin R. Lynch, Yugesh Kharel, Webster L. Santos, Russell G. Fritzemeier, Ashley N. Peralta
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Publication number: 20230331683Abstract: The present disclosure provides SPNS2 inhibitor compounds according to Formula (IA) and Formula (I), and their pharmaceutically acceptable salts, and/or tautomers as described in the disclosure, and the disclosure provides their pharmaceutical compositions and methods of use in therapy.Type: ApplicationFiled: September 8, 2021Publication date: October 19, 2023Inventors: Kevin R. Lynch, Yugesh Kharel, Webster L. Santos, Russell G. Fritzemeier, Ariel Louise Burgio, Christopher Shrader, Daniel Foster
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Patent number: 11708376Abstract: The disclosure provides compounds of Formula (I-A) and (I-B) and the pharmaceutically acceptable salts thereof. The variables, R, R2, R3, X1, X2, X3, Y1, Y, and Z are defined herein. Certain compounds of Formula (I-A) and (I-B) act as selective mitochondrial protonophore uncouplers that do not affect plasma membrane potential. These compounds are useful for treating or decreasing the risk of conditions responsive to mitochondrial uncoupling, such as cancer, obesity, type II diabetes, fatty liver disease, insulin resistance, Parkinson's disease, ischemia reperfusion injury, heart failure, non-alcoholic fatty liver disease (NALFD), and non-alcoholic steatohepatitis (NASH), Because mitochondrial uncouplers decrease the production of reactive oxygen species (ROS), which are known to contribute to age-related cell damage, the compounds are useful for increasing lifespan. Compounds and salts of Formulae (I-A) and (I-B) are also useful for regulating glucose homeostasis or insulin action in a patient.Type: GrantFiled: April 22, 2019Date of Patent: July 25, 2023Assignee: VIRGINIA TECH INTELLECTUAL PROPERTIES, INC.Inventors: Webster L. Santos, Yumin Dai, Jose A. Santiago-Rivera, Jacob H. Murray
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Publication number: 20230050649Abstract: Sphingosine kinases are enzymes that catalyze the biosynthesis of sphingosine-1-phosphate. The invention provides prodrugs of compounds that are effective for inhibition of sphingosine kinase type 1, sphingosine kinase type 2, or both, according to formula (I) as described herein. Formula I compounds are useful in the treatment of a range of diseases wherein increasing the level of sphingosine-1-phosphate in blood is medically indicated. The invention also provides pharmaceutical compositions of Formula I compounds.Type: ApplicationFiled: July 14, 2021Publication date: February 16, 2023Inventors: Steven Brandon Thorpe, Webster L. Santos, Kevin R. Lynch
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Publication number: 20220089581Abstract: The present disclosure provides SPNS2 inhibitor compounds according to Formula I and their pharmaceutically acceptable salts, and/or tautomers as described in the disclosure, and the disclosure provides their pharmaceutical compositions and methods of use in therapy.Type: ApplicationFiled: January 22, 2020Publication date: March 24, 2022Inventors: Kevin R. Lynch, Yugesh Kharel, Webster L. Santos, Ashley Peralta, Russell G. Fritzemeier, Daniel Foster
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Patent number: 11180489Abstract: Sphingosine kinases are enzymes that catalyze the biosynthesis of sphingosine-1-phosphate. The invention provides prodrugs of compounds that are effective for inhibition of sphingosine kinase type 1, sphingosine kinase type 2, or both, according to formula (I) as described herein. Formula I compounds are useful in the treatment of a range of diseases wherein increasing the level of sphingosine-1-phosphate in blood is medically indicated. The invention also provides pharmaceutical compositions of Formula I compounds.Type: GrantFiled: March 29, 2017Date of Patent: November 23, 2021Assignees: U niversity of Virginia Patent Foundation, Virginia Tech Entellectuzal Properties, Inc.Inventors: Steven Brandon Thorpe, Webster L. Santos, Kevin R. Lynch
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Publication number: 20210253594Abstract: The disclosure provide compounds of Formula I and the pharmaceutically acceptable salts thereof. The variables, R1, R2, R3, X1, X2, and Z are defined herein. Certain compounds of Formula I act as selective mitochondrial protonophore uncouplers that do not affect the plasma membrane potential. Compounds and salts of Formula I are useful for treating or decreasing the risk of conditions responsive to mitochondrial uncoupling, such as cancer, obesity, type II diabetes, fatty liver disease, insulin resistance, Parkinson's disease, ischemia reperfusion injury, heart failure, non-alcoholic fatty liver disease (NALFD), and non-alcoholic steatohepatitis (NASH). Because mitochondrial uncouplers decrease the production of reactive oxygen species (ROS), which are known to contribute to age-related cell damage, compounds of Formula I are useful for increasing lifespan. Compounds and salts of Formula I are also useful for regulating glucose homeostasis or insulin action in a patient.Type: ApplicationFiled: April 22, 2019Publication date: August 19, 2021Inventors: Webster L. Santos, Loseph Michael Salamoun, Christopher J. Garcia, Jacob H. Murray
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Publication number: 20210253538Abstract: The disclosure provides compounds of Formula I and the pharmaceutically acceptable salts thereof. The variables, R1, R2, R3, R4, R5, X1, X2, and Z are defined herein. Certain compounds of Formula I act as selective mitochondrial protonophore uncouplers that do not affect the plasma membrane potential. The disclosure includes pharmaceutical composition comprising a compound or salt Formula I, and a pharmaceutically acceptable carrier. Compounds and salts of Formula I are useful for treating or decreasing the risk of conditions responsive to mitochondrial uncoupling, such as obesity, cancer, type II diabetes, fatty liver disease, insulin resistance, Parkinson's disease, ischemia reperfusion injury, heart failure, non-alcoholic fatty liver disease (NALFD), and non-alcoholic steatohepatitis (NASH). Because mitochondrial uncouplers decrease the production of reactive oxygen species (ROS), which are known to contribute to age-related cell damage, compounds of Formula I are useful for increasing lifespan.Type: ApplicationFiled: April 22, 2019Publication date: August 19, 2021Inventors: Webster L. SANTOS, Jacob H. MURRAY, Jan NEKVINDA, Ariel BURGIO
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Publication number: 20210238181Abstract: The disclosure provides compounds of Formula (I-A) and (I-B) and the pharmaceutically acceptable salts thereof. The variables, R, R2, R3, X1, X2, X3, Y1, Y, and Z are defined herein. Certain compounds of Formula (I-A) and (I-B) act as selective mitochondrial protonophore uncouplers that do not affect plasma membrane potential. These compounds are useful for treating or decreasing the risk of conditions responsive to mitochondrial uncoupling, such as cancer, obesity, type II diabetes, fatty liver disease, insulin resistance, Parkinson's disease, ischemia reperfusion injury, heart failure, non-alcoholic fatty liver disease (NALFD), and non-alcoholic steatohepatitis (NASH), Because mitochondrial uncouplers decrease the production of reactive oxygen species (ROS), which are known to contribute to age-related cell damage, the compounds are useful for increasing lifespan. Compounds and salts of Formulae (I-A) and (I-B) are also useful for regulating glucose homeostasis or insulin action in a patient.Type: ApplicationFiled: April 22, 2019Publication date: August 5, 2021Applicant: Virginia Tech Intellectual Properties, Inc.Inventors: Webster L. SANTOS, Yumin DAI, Jose A. SANTIAGO-RIVERA, Jacob H. MURRAY
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Publication number: 20200323846Abstract: This disclosure provides compounds of Formula I, II, and III and pharmaceutically acceptable salts thereof for use as mitochondrial uncouplers, where the variables, e.g. R1-R9, X1, X2, and Y1 are defined in the specification. The disclosure also provides pharmaceutical compositions comprising a compound or pharmaceutically acceptable salt of Formula I, II, or III, alone or in combination with another active compound. Compounds and compositions of Formula I, II, and III are useful for treating or preventing certain conditions such as obesity, type II diabetes, fatty liver disease, insulin resistance, Parkinson's disease, ischemia reperfusion injury, heart failure, non-alcoholic fatty liver disease (NALFD), and non-alcoholic steatohepatitis (NASH). Compounds of Formula I, II, and III are also useful for regulating glucose homeostatis and insulin action.Type: ApplicationFiled: May 22, 2018Publication date: October 15, 2020Applicants: University of Virgina Patent Foundation, Virginia Tech Intellectual Properties, Inc., NewSouth Innovations Pty LimitedInventors: Kyle HOEHN, Webster L. SANTOS, Elizabeth S. CHILDRESS, Yumin DAI, Jacob MURRAY, Jose SANTIAGO-RIVERA
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Publication number: 20200308159Abstract: Sphingosine kinases are enzymes that catalyze the biosynthesis of sphingosine-1-phosphate. The invention provides prodrugs of compounds that are effective for inhibition of sphingosine kinase type 1, sphingosine kinase type 2, or both, according to formula (I) as described herein. Formula I compounds are useful in the treatment of a range of diseases wherein increasing the level of sphingosine-1-phosphate in blood is medically indicated. The invention also provides pharmaceutical compositions of Formula I compounds.Type: ApplicationFiled: March 29, 2017Publication date: October 1, 2020Inventors: Steven Brandon Thorpe, Webster L. Santos, Kevin R. Lynch
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Patent number: 10100022Abstract: Sphingosine kinases are enzymes that catalyze the biosynthesis of sphingosine-1-phosphate. The invention provides compounds that are effective for inhibition of sphingosine kinase type 1, sphingosine kinase type 2, or both. Certain compounds are selective for sphingosine kinase type 2 relative to sphingosine kinase type 1. Compounds of the invention can be used in treatment of a range of diseases wherein increasing the level of sphingosine-1-phosphate in blood is medically indicated. Diseases that can be treated by administration of an effective dose of a compound of the invention include a neoplastic disease that involves excess vascular growth; macular degeneration or diabetic retinopathy; an allergic disease such as asthma, an inflammatory disease of the eye such as uveitis, scleritis, or vitritis; an inflammatory disease of the kidney; a fibrotic disease; atherosclerosis; or pulmonary arterial hypertension.Type: GrantFiled: September 30, 2015Date of Patent: October 16, 2018Assignees: University of Virginia Patent Foundation, Virginia Tech Intellectual Properties, Inc.Inventors: Kevin R. Lynch, Webster L. Santos
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Publication number: 20170298032Abstract: Sphingosine kinases are enzymes that catalyze the biosynthesis of sphingosine-1-phosphate. The invention provides compounds that are effective for inhibition of sphingosine kinase type 1, sphingosine kinase type 2, or both. Certain compounds are selective for sphingosine kinase type 2 relative to sphingosine kinase type 1. Compounds of the invention can be used in treatment of a range of diseases wherein increasing the level of sphingosine-1-phosphate in blood is medically indicated. Diseases that can be treated by administration of an effective dose of a compound of the invention include a neoplastic disease that involves excess vascular growth; macular degeneration or diabetic retinopathy; an allergic disease such as asthma, an inflammatory disease of the eye such as uveitis, scleritis, or vitritis; an inflammatory disease of the kidney; a fibrotic disease; atherosclerosis; or pulmonary arterial hypertension.Type: ApplicationFiled: September 30, 2015Publication date: October 19, 2017Inventors: Kevin R. Lynch, Webster L. Santos
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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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Patent number: 7169818Abstract: The present invention is directed to compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom.Type: GrantFiled: October 3, 2001Date of Patent: January 30, 2007Assignee: University of Virginia Patent FoundationInventors: Kevin R. Lynch, Timothy L. Macdonald, Christopher E. Heise, Webster L. Santos, Mark D. Okusa
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Publication number: 20040122236Abstract: The present invention is directed to compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom.Type: ApplicationFiled: October 15, 2003Publication date: June 24, 2004Inventors: Kevin R. Lynch, Timothy L Macdonald, Christopher E Heise, Webster L Santos, Mark D Okusa