Pharmacy and Pharmaceutical Sciences Commons^™

Synthases, Joseph Chappell, Kathleen R. Manna, Joseph P. Noel, Courtney M. Starks

Pharmaceutical Sciences Faculty Patents

Novel synthases and the corresponding nucleic acids encoding such synthases are disclosed herein. Such synthases possess an active site pocket that includes key amino acid residues that are modified to generate desired terpenoid reaction intermediates and products. Synthase modifications are designed based on, e.g., the three-dimensional coordinates of tobacco 5-epi-aristolochene synthase, with or without a substrate bound in the active site.

Pathogen- Or Elicitor-Inducible Transcription Regulatory Element From The Tobacco 5-Epi-Aristolochene Synthase Gene And Plants Transformed Therewith, Joseph Chappell, Shaohui Yin, Catherine Cornett

Pharmaceutical Sciences Faculty Patents

A tobacco epi-5-aristolochene synthase transcriptional regulatory element functional in plants, plant tissue and in plant cells for pathogen inducible gene expression and a method for increasing the transcriptional expression of downstream genetic information in plants, plant tissue and plant cells are disclosed.

Synthases, Joe Chappell, Kathleen R. Manna, Joseph P. Noel, Courtney M. Starks

Pharmaceutical Sciences Faculty Patents

Novel synthases and the corresponding nucleic acids encoding such synthases are disclosed herein. Such synthases possess an active site pocket that includes key amino acid residues that are modified to generate desired terpenoid reaction intermediates and products. Synthase modifications are designed based on, e.g., the three-dimensional coordinates of tobacco 5-epi-aristolochene synthase, with or without a substrate bound in the active site.

Transdemal Delivery Of Opioid Antagonist Prodrugs, Audra L. Stinchcomb, Peter W. Swaan

Pharmaceutical Sciences Faculty Patents

A composition, a method and an apparatus for transdermally delivering an effective amount of opioid antagonists derived from prodrugs for treatment of eating disorders, narcotic dependence and alcoholism. In addition, the present invention relates to a composition, a method and an apparatus for transdermally delivering an effective amount of an opioid and opioid antagonist derived from an opioid agonist and one of an opioid antagonist and a prodrug for treatment of pain.

Synthases, Joe Chappell, Kathleen R. Manna, Joseph P. Noel, Courtney M. Starks

Pharmaceutical Sciences Faculty Patents

Novel synthases and the corresponding nucleic acids encoding such synthases are disclosed herein. Such synthases possess an active site pocket that includes key amino acid residues that are modified to generate desired terpenoid reaction intermediates and products. Synthase modifications are designed based on, e.g., the three-dimensional coordinates of tobacco 5-epi-aristolochene synthase, with or without a substrate bound in the active site.

Bridged Nicotine Compounds For Use In The Treatment Of Cns Pathologies, Peter A. Crooks, Linda P. Dwoskin, Rui Xu, Vladimir P. Grinevich

Pharmaceutical Sciences Faculty Patents

Pharmaceutical compounds comprising bridged nicotine analogs of N-octylnicotinium iodide (NONI) having selective antagonist properties at α3β2-containing nicotinic receptor subtypes, and compositions containing these compounds. The compounds and compositions are used to treat central nervous system pathologies.

Synthases, Joseph Chappell, Kathleen R. Manna, Joseph P. Noel, Courtney M. Starks

Pharmaceutical Sciences Faculty Patents

Novel synthases and the corresponding nucleic acids encoding such synthases are disclosed herein. Such synthases possess an active site pocket that includes key amino acid residues that are modified to generate desired terpenoid reaction intermediates and products. Synthase modifications are designed based on, e.g., the three-dimensional coordinates of tobacco 5-epi-aristolochene synthase with or without a substrate bound in the active site.

Methods Of Making Modified Polypeptides, Joseph Chappell, Kathleen R. Manna, Joseph P. Noel, Courtney M. Starks

Pharmaceutical Sciences Faculty Patents

Novel polypeptides and the corresponding nucleic acids encoding such polypeptides are disclosed herein. The invention provides methods of making modified polypeptides by altering one or more amino acid residues involved in the active site of a preselected polypeptide.

Cis-2,6-Disubstituted Piperidines For The Treatment Of Psychostimulant Abuse And Withdrawal, Eating Disorders, And Central Nervous System Diseases And Pathologies, Linda P. Dwoskin, Peter A. Crooks, Marlon D. Jones

Pharmaceutical Sciences Faculty Patents

Cis-2,6-disubstituted piperdine analogs, or lobeline analogs, having the general formula:

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Water Soluble Amine Esters Of Testosterone For Intranasal Administration, Anwar A. Hussain

Pharmaceutical Sciences Faculty Patents

The present invention provides novel water soluble testosterone analogs. These testosterone analogs are suitable for intranasal administration to patients requiring increased plasma testosterone levels. The present invention also provides pharmaceutical compositions containing the testosterone analogs of the present invention. The present invention further provides a method of increasing plasma testosterone levels in patients in need of such treatment comprising the intranasal administration of the water-soluble testosterone analogs and pharmaceutical compositions of the present invention.

Camptothecin Analogs And Methods Of Preparation Thereof, Dennis P. Curran, Bom David, Thomas Burke

Pharmaceutical Sciences Faculty Patents

To see this abstract, please download this patent.

Morphine-6-Sulfate Analogues And Their Use For The Treatment Of Pain, Peter A. Crooks, Abdulghani A. Houdi, Santosh G. Kottayil, D. Allan Butterfield

Pharmaceutical Sciences Faculty Patents

3-O-Acetylmorphine-6-sulfate analogues are potent, centrally-acting morphine derivatives. The compounds are useful for the treatment of pain.

Drug Delivery System Involving Interaction Between Protein Or Polypeptide And Hydrophobic Biodegradable Polymer, Patrick P. Deluca

Pharmaceutical Sciences Faculty Patents

A drug delivery system for controlled release of a protein or polypeptide comprising a hydrophobic biodegradable polymer and a protein or polypeptide. A physical interaction is present between the polymer and the protein or polypeptide, thus, allowing protection and controlled release of the protein or polypeptide in-vivo. The drug delivery system may be prepared by a polymer precipitation technique or a microsphere technique.

Water Soluble Derivatives Of Camptothecin/Homocamptothecin, Thomas Burke, Ayhan Demir, Cihangir Tanyeli, Ashok J. Chavan, Tie-Lin Wang, Yves Pommier

Pharmaceutical Sciences Faculty Patents

Camptothecin and homocamptothecin analogs and derivatives are provided incorporating alkylamine and polyalkylamine moieties.

Iodo-Nonoxynol-9-Derivatives And Methods For Their Use, George Digenis, Philip Fowler, Kazuya Matsumoto, Gustavo Doncel

Pharmaceutical Sciences Faculty Patents

Mono- and di-iodinated nonoxynol-9-derivatives and methods for their use are disclosed.

Use Of The Naturally-Occuring Quinones Thymoquinone And Dithymoquinone As Antineoplastic And Cytotoxic Agents, Peter A. Crooks, David R. Worthen, Omar A. Ghosheh

Pharmaceutical Sciences Faculty Patents

Nigella sativa derivatives, thymoquinone (TM) and dithymoquinone (DIM) are used in treatment of parental and multi-drug resistant human cancers.

Pathogen-Inducible Regulatory Element, Joseph Chappell, Catherine A. G. Cornett, Shauhui Yui

Pharmaceutical Sciences Faculty Patents

Qualitative transcriptional regulatory sequences functional in plants, plant tissue and in plant cells for inducible gene expression and quantitative transcriptional regulatory sequences for increasing the transcriptional expression of downstream genetic information in plants, plant tissue and plant cells are disclosed. Also disclosed are methods and recombinant DNA molecules for improving the disease resistance of transgenic plants, especially wherein an inducible promoter controls the expression of a protein capable of evoking the hypersensitive response in a plant.

Use Of Lobeline Compounds In The Treatment Of Central Nervous System Diseases And Pathologies, Peter A. Crooks, Linda P. Dwoskin

Pharmaceutical Sciences Faculty Patents

Lobeline and nicotine evoke [³H]overflow from rat striatal slices preloaded with [³H]dopamine ([³H]DA). The lobeline-evoked overflow is calcium-independent and not antagonized by mecamylamine, suggesting a mechanism of action other than the stimulation of nicotinic receptors. Whereas nicotine stimulates nicotinic receptors, lobeline inhibits [³H]DA uptake into synaptic vesicles and striatal synaptosomes. The results suggest that different mechanisms are responsible for the increase in striatal DA release evoked by lobeline and nicotine. [³H]-Dihydrotetrabenazine [³H]DTBZ), used routinely to probe a high-affinity binding site-on the vesicular monoamine transporter (VMAT2) binds to vesicle …

Formulations For Sustained-Release Of Topical Anesthetics And Methods Of Making And Using Same, Michael Joseph Jay, G. Thomas Kluemper, Sang Hun Kim

Pharmaceutical Sciences Faculty Patents

The present invention provides, inter alia, formulations useful to ameliorate symptoms associated with mucosal abrasions, specifically those due to dental orthodontic brackets; oral surgery; periodontal surgery or other procedures. For instance, there is a formulation comprising: 65 to 75% microcrystalline wax; 5 to 15% non-ionic polymer; 15 to 25% topical anesthetic; and 1 to 5% surfactant, wherein the ratio of non-ionic polymer to microcrystalline wax is no greater than 0.2. Preferably, for solid topical anesthetics, the particle size is less than the apertures of a 100-mesh screen. However, the topical anesthetic may also be a liquid. Formulations wherein the mixture …

Chemical Isoprenoid Synthases And Uses Thereof, Joseph Chappell, Kyoungwhan Back

Pharmaceutical Sciences Faculty Patents

Disclosed is a chimeric isoprenoid synthase polypeptide including a first domain from a first isoprenoid synthase joined to a second domain from a second, heterologous isoprenoid synthase, whereby the chimeric isoprenoid synthase is capable of catalyzing the production of isoprenoid reaction products that are not produced in the absence of the second domain of the second, heterologous isoprenoid synthase. Also disclosed is a chimeric isoprenoid synthase polypeptide including an asymmetrically positioned homologous domain, whereby the chimeric isoprenoid synthase is capable of catalyzing the production of isoprenoid reaction products that are not produced when the domain is positioned at its naturally-occurring …

Host-Derived Signals For Inducing Isoprenoid Gene Expression And Uses Thereof, Joseph Chappell, Marcos Lusso

Pharmaceutical Sciences Faculty Patents

Disclosed is a method for preparing a composition that is capable of activating the expression of a gene involved in the synthesis of an isoprenoid, the method involving: (a) contacting a plant cell with an elicitor under conditions that allow an elicitor-induced release of a compound that activates the synthesis of an isoprenoid; and (b) recovering a composition including the compound, wherein the compound is diffusible and has a molecular weight less than or equal to 10,000 daltons. Also disclosed is a substantially pure elicitor-induced composition, the composition being capable of activating a gene involved in the synthesis of a …

Transcriptional Silencing Elements And Their Binding Factors, Joseph Chappell, Jeffrey D. Newman, Shaohui Yin

Pharmaceutical Sciences Faculty Patents

The invention features an isolated gene silencing regulatory element that includes 5' TACNNTAC 3'. Vectors, transgenic plants and seeds thereof that include such a gene silencing regulatory element are also disclosed. The invention further provides methods of decreasing the transcription of a DNA sequence in a transgenic plant using the isolated gene silencing regulatory element.

Derivatives Of N-Chloro-N-Methyl Glucamine And N-Chloro-N-Methyl Glucamine Esters, Anwar A. Hussain, Bassam Tashtoush, Lewis W. Dittert

Pharmaceutical Sciences Faculty Patents

The present invention relates to N-chloro-N-methyl glucamine and N-chloro-N-methyl glucamine esters, and their use as agents for water disinfection and as mild oxidizing agents for the radiolabeling of oxidation-sensitive biomolecules.

Elicitin-Mediated Plant Resistance, Joseph Chappell, Shaohui Yin, Catherine Cornett

Pharmaceutical Sciences Faculty Patents

Qualitative transcriptional regulatory sequences functional in plants, plant tissue and in plant cells for inducible gene expression and quantitative transcriptional regulatory sequences for increasing the transcriptional expression of downstream genetic information in plants, plant tissue and plant cells are disclosed. Also disclosed are methods and recombinant DNA molecules for improving the disease resistance of transgenic plants, especially wherein an inducible promoter controls the expression of a protein capable of evoking the hypersensitive response in a plant.

Methods Of Treating Eye Conditions With Human Leukocyte Elastase (Hle) Inhibitory Agents, George A. Digenis, Charles Khouri

Pharmaceutical Sciences Faculty Patents

A method of reducing corneal scarring or fibroblast proliferation comprises applying to an area of a subject's eye afflicted with the condition a corneal scar-fibroblast proliferation-reducing amount of a free or polymer-bound HLE inhibitory agent under conditions and for a period of time effective to attain the desired effect. A method of reducing neovascularization of corneal scar tissue comprises applying to an area of a subject's eye afflicted with the condition a neovascularization-inhibitory amount of a free or polymer-bound HLE inhibitory agent under conditions and for a period of time effective to attain the desired effect.

Canavanine Analogs And Their Use As Chemotherapeutic Agents, Peter A. Crooks, Gerald A. Rosenthal

Pharmaceutical Sciences Faculty Patents

This invention relates to canvanine analogs, their pharmaceutical compositions, and a method for treatment of cancer, particularly pancreatic cancer.

Lobeline Compounds As A Treatment For Psychostimulant Abuse And Withdrawal, And For Eating Disorders, Peter A. Crooks, Linda P. Dwoskin

Pharmaceutical Sciences Faculty Patents

Methods are disclosed that suggest the use of lobeline and analogs thereof in treating individuals for drug dependence and withdrawal and for eating disorders.

Chimeric Isoprenoid Synthases And Uses Thereof, Joseph Chappell, Kyoungwhan Back

Pharmaceutical Sciences Faculty Patents

Disclosed is a chimeric isoprenoid synthase polypeptide including a first domain from a first isoprenoid synthase joined to a second domain from a second, heterologous isoprenoid synthase, whereby the chimeric isoprenoid synthase is capable of catalyzing the production of isoprenoid reaction products that are not produced in the absence of the second domain of the second, heterologous isoprenoid synthase. Also disclosed is a chimeric isoprenoid synthase polypeptide including an assymetrically positioned homologous domain, whereby the chimeric isoprenoid synthase is capable of catalyzing the production of isoprenoid reaction products that are not produced when the domain is positioned at its naturally-occurring …

Nornicotine Enantiomers For Use As A Treatment For Dopamine Related Conditions And Disease States, Peter A. Crooks, Linda Phyliss Dwoskin, Michael Thomas Bardo

Pharmaceutical Sciences Faculty Patents

Optically active nornicotine compounds as a treatment for dopamine-related conditions and disease states. Such disease states include the treatment of myasthenia gravis, Parkinson's disease, Alzheimer's disease, schizophrenia, eating disorders, ulcers, drug addiction and as a substitute for psycho-stimulant self-administration.

N-Chloro-N-Methyl Glucamine And N-Chloro-N-Methyl Glucamine Esters As Novel Safe Agents For Water Disinfetion, Anwar A. Hussain, Bassam Tashtoush, Lewis W. Dittert

Pharmaceutical Sciences Faculty Patents

The present invention relates to N-chloro-N-methyl glucamine and N-chloro-N-methyl glucamine esters, and their use as agents for water disinfection and as mild oxidizing agents for the radiolabeling of oxidation-sensitive biomolecules.