Patents by Inventor Gerald Koelsch
Gerald Koelsch 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: 7829669Abstract: Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogues including isosteres at the sites of the critical amino acid residues were developed and the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1).Type: GrantFiled: August 3, 2007Date of Patent: November 9, 2010Assignees: Oklahoma Medical Research Foundation, The Board of Trustees of the University of IllinoisInventors: Gerald Koelsch, Jordan J. N. Tang, Lin Hong, Arun K. Ghosh, Xinli Lin
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Publication number: 20080112946Abstract: Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogues including isosteres at the sites of the critical amino acid residues were developed and the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1).Type: ApplicationFiled: August 3, 2007Publication date: May 15, 2008Inventors: Gerald Koelsch, Jordan J. N. Tang, Lin Hong, Arun K. Ghosh, Xinli Lin
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Publication number: 20060234944Abstract: Compounds inhibit memapsin 2 ?-secretase activity and selectively inhibit memapsin 2 ?-secretase activity relative to memapsin 1 ?-secretase activity. The compounds are employed in methods to inhibit memapsin 2 ?-secretase activity, in the treatment of Alzheimer's disease, in the inhibition of hydrolysis of a ?-secretase site of a ?-amyloid precursor protein and to decrease ?-amyloid protein in in vitro samples and in mammals. Proteins of memapsin 2 associated with compounds of the invention are crystallized.Type: ApplicationFiled: October 23, 2002Publication date: October 19, 2006Applicants: Oklahoma Medical Reseach Foundation, The Board of Trustees of the University of IllinoisInventors: Arun Ghosh, Jordan Tang, Geoffrey Bilcer, Wanpin Chang, Lin Hong, Gerald Koelsch, Jeff Loy, Robert Turner III
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Publication number: 20040220079Abstract: Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogues including isosteres at the sites of the critical amino acid residues were developed and the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1).Type: ApplicationFiled: February 6, 2004Publication date: November 4, 2004Applicants: Oklahoma Medical Research Foundation, The Board of Trustees of the University of IllinoisInventors: Gerald Koelsch, Jordan J.N. Tang, Lin Hong, Arun K. Ghosh
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Publication number: 20030092629Abstract: Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed-, The substrate and subsite specificity of the catalytically active enzyme have been determined by a method which determines the initial hydrolysis rate of the substrates by using MALDI-TOF/MS. Alternatively, the subsite specificity of memapsin can be determined by probing a library of inhibitors with memapsin 2 and subsequently detecting the bound memapsin 2 with an antibody raised to memapsin 2 and an alkaline phosphatase conjugated secondary antibody. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2.Type: ApplicationFiled: December 28, 2001Publication date: May 15, 2003Applicant: Oklahoma Medical Research FoundationInventors: Jordan J. N. Tang, Gerald Koelsch, Arun K. Ghosh
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Patent number: 6545127Abstract: Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogues including isosteres at the sites of the critical amino acid residues were developed and the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1).Type: GrantFiled: June 27, 2000Date of Patent: April 8, 2003Assignee: Oklahoma Medical Research FoundationInventors: Jordan J. N. Tang, Xinli Lin, Gerald Koelsch, Lin Hong
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Publication number: 20020164760Abstract: Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogues including isosteres at the sites of the critical amino acid residues were developed and the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1).Type: ApplicationFiled: February 28, 2001Publication date: November 7, 2002Applicant: Oklahoma Medical Research FoundationInventors: Xinli Lin, Gerald Koelsch, Jordan J.N. Tang
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Publication number: 20020115600Abstract: Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogues including isosteres at the sites of the critical amino acid residues were developed and the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1).Type: ApplicationFiled: April 30, 2001Publication date: August 22, 2002Applicant: Oklahoma Medical Research FoundationInventors: Gerald Koelsch, Jordan J.N. Tang, Lin Hong, Arun K. Ghosh
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Publication number: 20020049303Abstract: Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogs including isosteres at the sites of the critical amino acid residues were developed and the substrate analogs, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1).Type: ApplicationFiled: February 28, 2001Publication date: April 25, 2002Inventors: Jordan J. N. Tang, Xinli Lin, Gerald Koelsch, Lin Hong