Patents by Inventor Vern L. Schramm
Vern L. Schramm 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: 7211653Abstract: The present invention provides compounds having the formula: wherein A is CH or N; B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H, halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and X and Y are independently selected from H, OH or halogen except that when one of X and Y is hydroxy or halogen, the other is hydrogen; and Z is OH or, when X is hydroxy, Z is selected from hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof; and compounds having the formula: wherein A, X, Y, Z and R are defined for compounds of formula (I) where first shown above; E is chosen from CO2H or a corresponding salt form, CO2R, CN, CONH2, CONHR or CONR2; and G is chosen from NH2, NHCOR, NHCONHR or NHCSNHR; or a tautomer thereof, or a pharmaceutically acceptable salt thereof, or an ester thereof, or a prodrug theType: GrantFiled: September 2, 2004Date of Patent: May 1, 2007Assignees: Albert Einstein College of Medicine of Yeshiva University, Industrial Research LimitedInventors: Richard Hubert Furneaux, Peter Charles Tyler, Vern L. Schramm
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Patent number: 7109331Abstract: The present invention provides a compound of the formula (I): wherein A is selected from N, CH and CR, where R is selected from halogen, optionally substituted alkyl, aralkyl and aryl, OH, NH2, NHR1, NR1R2 and SR3, where R1, R2 and R3 are each optionally substituted alkyl, aralkyl or aryl groups; B is selected from OH, NH2, NHR4, H and halogen, where R4 is an optionally substituted alkyl, aralkyl or aryl group; D is selected from OH, NH2, NHR5, H, halogen and SCH3, where R5 is an optionally substituted alkyl, aralkyl or aryl group; X and Y are independendy selected from H, OH and halogen, with the proviso that when one of X and Y is hydroxy or halogen, the other is hydrogen; Z is OH, or, when X is hydroxy, Z is selected from hydrogen, halogen, hydroxy, SQ and OQ, where Q is an optionally substituted alkyl, aralkyl or aryl group; and W is OH or H, with the proviso that when W is OH, then A is CR where R is as defined above; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester tType: GrantFiled: August 24, 2001Date of Patent: September 19, 2006Assignees: Industrial Research Limited, Albert Einstein College of Medicine of Yeshiva UniversityInventors: Richard Hubert Furneaux, Peter Charles Tyler, Vern L. Schramm
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Patent number: 7098334Abstract: The invention provides a compound of the formula: wherein A is selected from N, CH and CR; R is selected from halogen, optionally substituted alkyl, aralkyl and aryl, OH, NH2, NHR1, NR1R2 and SR3; R1, R2 and R3 are each optionally substituted alkyl, aralkyl or aryl groups; B is selected from NH2 and NHR4; R4 is an optionally substituted alkyl, aralkyl or aryl group; X is selected from H, OH and halogen; Z is selected from H, Q, SQ and OQ; Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer, a pharmaceutically acceptable salt, an ester, or a prodrug thereof; with the proviso that the stereochemistry of the aza-sugar moiety is D-ribo or 2?-deoxy-D-erythro-; pharmaceutical compositions comprising said compound; and methods of treatment using said compound.Type: GrantFiled: March 24, 2003Date of Patent: August 29, 2006Assignees: Industrial Research Limited, Albert Einstein College of Medicine of Yeshiva UniversityInventors: Richard Hubert Furneaux, Peter Charles Tyler, Vern L. Schramm, Gary Brian Evans
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Patent number: 7056894Abstract: The present invention provides compounds having the formula: wherein A is chosen from a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group; both B and C are hydrogen, or either B or C is a halogen, amino, or thiol group and the other of B or C is hydrogen; and D is a primary alcohol, a hydrogen, or an oxygen, nitrogen, carbon, or sulfur linked to phosphate, a phosphoryl group, a pyrophosphoryl group, or adenosine monophosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted phosphodiester bridge, or to adenosine diphosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted pyrophosphodiester bridge. The present invention also provides pharmaceutical compositions containing the above compounds, methods of using the above compounds as pharmaceuticals, and processes for preparing the above compounds.Type: GrantFiled: January 4, 2002Date of Patent: June 6, 2006Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Anthony A. Sauve, Vern L. Schramm
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Patent number: 7022852Abstract: A process of preparing a compound of the formula (I) wherein B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and Z is selected from OH, hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof, which comprises reacting a compound of the formula (II) with an anion produced by abstraction of the bromine or iodine atom from a compound of formula (XIX), to form a compound of formula (XX) The compound of formula (LXX) is N- and O-deprotected to obtain the compound of formula (I).Type: GrantFiled: December 16, 2003Date of Patent: April 4, 2006Assignees: Industrial Research Limited, Albert Einstein College of Medicine of Yeshiva UniversityInventors: Richard Hubert Furneaux, Peter Charles Tyler, Vern L. Schramm
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Patent number: 7022680Abstract: The present invention provides compounds having the formula: wherein A is a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group, the group being further substituted with an electron contributing moiety; B is hydrogen, or a halogen, amino, or thiol group; C is hydrogen, or a halogen, amino, or thiol group; and D is a primary alcohol, a hydrogen, or an oxygen, nitrogen, carbon, or sulfur linked to phosphate, a phosphoryl group, a pyrophosphoryl group, or adenosine monophosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted phosphodiester bridge, or to adenosine diphosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted pyrophosphodiester bridge. The present invention also provides pharmaceutical compositions containing the above compounds, methods of using the above compounds as pharmaceuticals, and processes for preparing the above compounds.Type: GrantFiled: May 30, 2002Date of Patent: April 4, 2006Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Anthony A. Sauvé, Vern L. Schramm
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Patent number: 6987091Abstract: A novel compound, 2?/3?-O-acetyl-ADP-ribose, is provided. The compound is a mixture of the 2? and 3? regioisomers of O-acetyl-ADP ribose, and is formed nonenzymatically from 2?-O-acetyl-ADP-ribose, which is the newly discovered product of the reaction of Sir2 enzymes with acetylated peptides and NAD+. Analogs of 2?/3?-O-acetyl-ADP-ribose are also provided. Additionally, methods of preparing 2?/3?-O-acetyl-ADP-ribose, methods of determining whether a test compound is an inhibitor of a Sir2 enzyme, methods of detecting Sir2 activity in a composition, methods of deacetylating an acetylated peptide, and methods of inhibiting the deacetylation of an acetylated peptide are provided. Prodrugs of 2?/3?-O-acetyl-ADP-ribose are also provided.Type: GrantFiled: November 21, 2002Date of Patent: January 17, 2006Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Jef D. Boeke, Anthony Sauvé, Ivana Celic
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Patent number: 6895396Abstract: A new method to analyze and predict the binding energy for enzyme-transition state inhibitor interactions is presented. Computational neural networks are employed to discovery quantum mechanical features of transition states and putative inhibitors necessary for binding. The method is able to generate its own relationship between the quantum mechanical structure of the inhibitor and the strength of binding. Feed-forward neural networks with back propagation of error can be trained to recognize the quantum mechanical electrostatic potential at the entire van der Waals surface, rather than a collapsed representation, of a group of training inhibitors and to predict the strength of interactions between the enzyme and a group of novel inhibitors. The experimental results show that the neural networks can predict with quantitative accuracy the binding strength of new inhibitors.Type: GrantFiled: January 6, 2004Date of Patent: May 17, 2005Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Steven D. Schwartz, Vern L. Schramm, Benjamin B. Braunheim
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Patent number: 6803455Abstract: The present invention provides compounds having the formula: wherein A is CH or N; B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H, halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and X and Y are independently selected from H, OH or halogen except that when one of X and Y is hydroxy or halogen, the other is hydrogen; and Z is OH or, when X is hydroxy, Z is selected from hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof; and compounds having the formula: wherein A, X, Y, Z and R are defined for compounds of formula (I) where first shown above; E is chosen from CO2H or a corresponding salt form, CO2R, CN, CONH2, CONHR or CONR2; and G is chosen from NH2, NHCOR, NHCONHR or NHCSNHR; or a tautomer thereof, or a pharmaceutically acceptable salt thereof, or an esteType: GrantFiled: October 10, 2002Date of Patent: October 12, 2004Assignees: Albert Einstein College of Medicine of Yeshiva University, Industrial Research LimitedInventors: Richard Hubert Furneaux, Peter Charles Tyler, Vern L. Schramm
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Publication number: 20040181063Abstract: A process of preparing a compound of the formula (I) 1Type: ApplicationFiled: December 16, 2003Publication date: September 16, 2004Inventors: Richard Hubert Furneaux, Peter Charles Tyler, Vern L. Schramm
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Publication number: 20040148265Abstract: A new method to analyze and predict the binding energy for enzyme-transition state inhibitor interactions is presented. Computational neural networks are employed to discovery quantum mechanical features of transition states and putative inhibitors necessary for binding. The method is able to generate its own relationship between the quantum mechanical structure of the inhibitor and the strength of binding. Feed-forward neural networks with back propagation of error can be trained to recognize the quantum mechanical electrostatic potential at the entire van der Waals surface, rather than a collapsed representation, of a group of training inhibitors and to predict the strength of interactions between the enzyme and a group of novel inhibitors. The experimental results show that the neural networks can predict with quantitative accuracy the binding strength of new inhibitors.Type: ApplicationFiled: January 6, 2004Publication date: July 29, 2004Inventors: Steven D. Schwartz, Vern L. Schramm, Benjamin B. Braunheim
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Patent number: 6764829Abstract: The invention relates to a method of detecting and/or assaying nucleoside hydrolases or nucleoside phosphorylases using a chromogenic substrate. Preferred chromogenic substrates have formula (I) where X is OH, or H, and Y is the residue of Y—OH where Y—OH is a chromophore or a compound readily converted to a chromophore and the substrates are hydrolyzed by the nucleoside hydrolase to yield ribose or 2-deoxyribose plus Y—OH. Alternatively, those substrates may be phosphorylysed by nucleoside phosphorylase to yield ribose-1-phosphate plus Y—OH. The methods may be used to detect and/or assay parasites in biological samples.Type: GrantFiled: March 18, 2002Date of Patent: July 20, 2004Assignees: Albert Einstein College of Medicine of Yeshiva University, Industrial Research LimitedInventors: Vern L. Schramm, Richard Hubert Furneaux, Peter Charles Tyler, Keith Clinch
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Publication number: 20040110772Abstract: The invention provides a compound of the formula: 1Type: ApplicationFiled: March 24, 2003Publication date: June 10, 2004Inventors: Richard Hubert Furneaux, Peter Charles Tyler, Vern L. Schramm, Gary Brian Evans
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Publication number: 20040053944Abstract: The present invention provides a compound of formula (I), wherein: A is selected from N, CH and CR, where R is selected from halogen, optionally substituted alkyl, aralkyl and aryl, OH, NH2, NHR1, NR1R2 and SR3, where R1, R2 and R3 are each optionally substituted alkyl, aralkyl or aryl groups; B is selected from OH, NH2, NHR4, H and halogen, where R4 is an optionally substituted alkyl, aralkyl or aryl group; D is selected from OH, NH2, NHR5, H, halogen and SCH3, where R5 is an optionally substituted alkyl, aralkyl or aryl group; X and Y are independently selected from H, OH and halogen, with the proviso that when one of X and Y is hydroxy or halogen, the other is hydrogen; Z is OH, or, when X is hydroxy, Z is selected from hydrogen, halogen, hydroxy, SQ and OQ, where Q is an optionally substituted alkyl, aralkyl or aryl group; and W is OH or H, with the proviso that when W is OH, then A is CR where R is as defined above; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereofType: ApplicationFiled: October 3, 2003Publication date: March 18, 2004Inventors: Richard Hubert Furneaux, Peter Charles Tyler, Vern L. Schramm
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Patent number: 6693193Abstract: A process of preparing a compound of the formula (I) wherein B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and Z is selected from OH, hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted all, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof, which comprises reacting a compound of the formula (II) with an anion produced by abstraction of the bromine or iodine atom from a compound of formula (XIX), to form a compound of formula (XX) The compound of formula (XX) is N- and O-deprotected to obtain the compound of formula (I).Type: GrantFiled: April 18, 2002Date of Patent: February 17, 2004Assignees: Industrial Research Limited, Albert Einstein College of Medicine of Yesheva UniversityInventors: Richard Hubert Furneaux, Peter Charles Tyler, Vern L. Schramm
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Patent number: 6678618Abstract: A new method to analyze and predict the binding energy for enzyme-transition state inhibitor interactions is presented. Computational neural networks are employed to discovery quantum mechanical features of transition states and putative inhibitors necessary for binding. The method is able to generate its own relationship between the quantum mechanical structure of the inhibitor and the strength of binding. Feed-forward neural networks with back propagation of error can be trained to recognize the quantum mechanical electrostatic potential at the entire van der Waals surface, rather than a collapsed representation, of a group of training inhibitors and to predict the strength of interactions between the enzyme and a group of novel inhibitors. The experimental results show that the neural networks can predict with quantitative accuracy the binding strength of new inhibitors.Type: GrantFiled: November 13, 2000Date of Patent: January 13, 2004Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Steven D. Schwartz, Vern L. Schramm, Benjamin B. Braunheim
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Publication number: 20030229033Abstract: The present invention provides compounds having the formula: 1Type: ApplicationFiled: May 30, 2002Publication date: December 11, 2003Inventors: Anthony A. Sauve, Vern L. Schramm
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Publication number: 20030149261Abstract: A novel compound, 2′/3′-O-acetyl-ADP-ribose, is provided. The compound is a mixture of the 2′ and 3′ regioisomers of O-acetyl-ADP ribose, and is formed nonenzymatically from 2′-O-acetyl-ADP-ribose, which is the newly discovered product of the reaction of Sir2 enzymes with acetylated peptides and NAD+. Analogs of 2′/3′-O-acetyl-ADP-ribose are also provided. Additionally, methods of preparing 2′/3′-O-acetyl-ADP-ribose, methods of determining whether a test compound is an inhibitor of a Sir2 enzyme, methods of detecting Sir2 activity in a composition, methods of deacetylating an acetylated peptide, and methods of inhibiting the deacetylation of an acetylated peptide are provided. Prodrugs of 2′/3′-O-acetyl-ADP-ribose are also provided.Type: ApplicationFiled: November 21, 2002Publication date: August 7, 2003Inventors: Vern L. Schramm, Jef D. Boeke, Anthony Sauve, Ivana Celic
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Publication number: 20030096830Abstract: The present invention provides compounds having the formula: 1Type: ApplicationFiled: October 10, 2002Publication date: May 22, 2003Inventors: Richard Hubert Furneaux, Peter Charles Tyler, Vern L. Schramm
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Patent number: 6492347Abstract: The present invention provides novel nucleoside-analogue compounds that are effective inhibitors of purine nucleoside phosphorylase (PNP), purine phosphoribosyltransferases (PPRT), and/or nucleoside hydrolases. Also provided are tautomers, esters, prodrugs, and pharmaceutically-acceptable salts of the compounds disclosed herein. The present invention further provides the use of these compounds as pharmaceuticals. The present invention also discloses pharmaceutical compositions containing these compounds. Finally, the present invention provides processes for preparing these compounds.Type: GrantFiled: March 28, 2001Date of Patent: December 10, 2002Assignees: Albert Einstein College of Medicine of Yeshiva University, Industrial Research LimitedInventors: Richard Hubert Furneaux, Peter Charles Tyler, Vern L. Schramm