Rutgers Inventor:
Leslie Jimenez, Ph.D.
Department of Chemistry & Chemical Biology
Invention Summary:
Scientists at Rutgers University have developed a novel method to regioselectively introduce functional groups onto arenes by using aryl bromides as easily removable blocking groups. This novel method addresses the difficulty of functional group placement for a variety of aromatic ring structures and enables the synthesis of compounds in far fewer steps. The methodology has been exploited in over 12 distinct substrates demonstrating broad utility. This method may be useful for a variety of chemical synthesis strategies employed by chemical and drug manufacturers.
Market Applications:
Chemical synthesis, organic synthesis, process development, pharmaceuticals.
Advantages:
High yield synthesis, easily removable by-products, reduced number of steps for synthesis.
Intellectual Property & Development Status: A Provisional patent application has been filed.
Wednesday, September 16, 2009
Friday, September 11, 2009
Novel Synthetic Route for c-di-GMP and Analogs
Rutgers Inventor:
Roger Jones, Ph.D.
Department of Chemistry & Chemical Biology
Invention Summary:
Investigators at Rutgers have developed a procedure for the synthesis of cyclic diguanosine monophosphate (c-di-GMP) that can be carried out in one day starting from commercially available material. A number of other routes to this molecule have been reported, though all require more time to synthesize the molecule, and employ starting materials that are not commercially available. Further, this novel route lends itself to preparation of a variety of analogs, including especially the thiophosphates, gives crystalline material, and is scalable. There is intense current interest in c-di-GMP, and analogs, because of its role as a bacterial signaling molecule and its importance in bacterial virulence, pathogenesis, and biofilm formation.
Market Applications:
Chemical synthesis, c-di-GMP, bacterial virulence, pathogenesis, biofilm.
Advantages:
Rapid, scalable, one-flask, gram quantity.
Intellectual Property & Development Status:
A Provisional patent application has been filed.
Roger Jones, Ph.D.
Department of Chemistry & Chemical Biology
Invention Summary:
Investigators at Rutgers have developed a procedure for the synthesis of cyclic diguanosine monophosphate (c-di-GMP) that can be carried out in one day starting from commercially available material. A number of other routes to this molecule have been reported, though all require more time to synthesize the molecule, and employ starting materials that are not commercially available. Further, this novel route lends itself to preparation of a variety of analogs, including especially the thiophosphates, gives crystalline material, and is scalable. There is intense current interest in c-di-GMP, and analogs, because of its role as a bacterial signaling molecule and its importance in bacterial virulence, pathogenesis, and biofilm formation.
Market Applications:
Chemical synthesis, c-di-GMP, bacterial virulence, pathogenesis, biofilm.
Advantages:
Rapid, scalable, one-flask, gram quantity.
Intellectual Property & Development Status:
A Provisional patent application has been filed.
Total Synthesis of Microcin C Analogues with Altered Intracellular Targets
Rutgers Inventor:
Konstantin Severinov, PhD
Chemistry and Chemical Biology
Invention Summary:
Scientists have recently developed a novel, total synthesis for analogues of Microcin C (McC), a potent antibacterial agent. McC is a Trojan horse inhibitor that is actively taken into sensitive cells and processed to a non-hydrolyzable form that inhibits translation by preventing aminoacylation of tRNAAsp by aspartyl-tRNA synthetase (AspRS). The new synthetic approach results in analogues lacking proplyamine and N-terminal formyl groups, and the phosphoramide normally found in McC is substituted by a sulfamoyl bond. These analogues are taken up by a unique mechanism of action and inhibit aaRS, found in both gram-negative and gram-positive bacteria. These compounds may also be used as coupling agents for other drugs to enhance uptake. Further, synthesis allows for the generation of inhibitors of all 20 aminoacyl-tRNA synthetases and may be widely applicable to creating novel antibiotics.
Market Applications:
Therapeutics, Antibacterial, Antiobiotic, Food preservative, gram-positive, gram-negative.
Advantages:
Total synthesis, broad spectrum antibiotic activity.
Intellectual Property & Development Status: A provisional patent application has been filed. Note: Rutgers also has an IP estate on the compounds and analogues.
Konstantin Severinov, PhD
Chemistry and Chemical Biology
Invention Summary:
Scientists have recently developed a novel, total synthesis for analogues of Microcin C (McC), a potent antibacterial agent. McC is a Trojan horse inhibitor that is actively taken into sensitive cells and processed to a non-hydrolyzable form that inhibits translation by preventing aminoacylation of tRNAAsp by aspartyl-tRNA synthetase (AspRS). The new synthetic approach results in analogues lacking proplyamine and N-terminal formyl groups, and the phosphoramide normally found in McC is substituted by a sulfamoyl bond. These analogues are taken up by a unique mechanism of action and inhibit aaRS, found in both gram-negative and gram-positive bacteria. These compounds may also be used as coupling agents for other drugs to enhance uptake. Further, synthesis allows for the generation of inhibitors of all 20 aminoacyl-tRNA synthetases and may be widely applicable to creating novel antibiotics.
Market Applications:
Therapeutics, Antibacterial, Antiobiotic, Food preservative, gram-positive, gram-negative.
Advantages:
Total synthesis, broad spectrum antibiotic activity.
Intellectual Property & Development Status: A provisional patent application has been filed. Note: Rutgers also has an IP estate on the compounds and analogues.
Automated, Self-Contained Venipuncture Device
Rutgers Inventors:
Martin L. Yarmush, MD, PhD
Stanley Dunn, PhD
Department of Biomedical Engineering
Invention Summary:
Rutgers scientists have developed a device design for autonomous venipuncture. It combines a subcutaneous imaging system with a robotically driven needle in a compact form that allows for portable application. The device uses near-infrared imaging to create a 3-D vector coordinate system in real-time to visualize subcutaneous veins. The device also provides critical depth representations of the target vein and utilizes robotics for optimal needle placement. The introduction of an automated venipuncture device will find utility in numerous clinical care and out-patient settings and will enable improved blood collection methods for a wide range of patient populations.
Market Applications: Automated venipuncture, robotics, blood vessel imaging, phlebotomy.
Advantages: Safe and accurate venipuncture, elimination of human error, improved patient comfort, rapid phlebotomy
Intellectual Property & Development Status: A provisional patent application has been filed.
Martin L. Yarmush, MD, PhD
Stanley Dunn, PhD
Department of Biomedical Engineering
Invention Summary:
Rutgers scientists have developed a device design for autonomous venipuncture. It combines a subcutaneous imaging system with a robotically driven needle in a compact form that allows for portable application. The device uses near-infrared imaging to create a 3-D vector coordinate system in real-time to visualize subcutaneous veins. The device also provides critical depth representations of the target vein and utilizes robotics for optimal needle placement. The introduction of an automated venipuncture device will find utility in numerous clinical care and out-patient settings and will enable improved blood collection methods for a wide range of patient populations.
Market Applications: Automated venipuncture, robotics, blood vessel imaging, phlebotomy.
Advantages: Safe and accurate venipuncture, elimination of human error, improved patient comfort, rapid phlebotomy
Intellectual Property & Development Status: A provisional patent application has been filed.
Biodegradable, Antimicrobial PolymerActives as Films/Particles
Rutgers Inventor:
Kathryn Uhrich Ph.D.
Department of Chemistry & Chemical Biology
Kathryn Uhrich Ph.D.
Department of Chemistry & Chemical Biology
Summary:
Biodegradable, bioactive-based polymers (PolymerActives) (i.e., plastics) are patented materials that can be used for a variety of applications from food safety to personal care products. The bioactive molecules are chemically incorporated into the polymers, so that a very high bioactive loading is achieved. Furthermore, the polymers are fully biodegradable (i.e., hydrolytically degradable), and upon degradation release the bioactive molecules in a controlled, sustained manner. The polymer degradation rate can be easily manipulated, and degradation times can be controlled to release the bioactive from hours to days or weeks to months, depending on the specific application.
For traditional food packaging, bioactives (e.g., antimicrobials, preservatives, antioxidants) are physically incorporated into a polymer “carrier”. In this technology, the polymer is both the carrier and the bioactive. The bioactive is only released when the polymer is in contact with water. Additional bioactive molecules can be “loaded” into the PolymerActive to give a dual or triple release system.
Relevant for food products, PolymerActives can easily be formulated into films or wraps: PolymerActives have already been proven effective for prevention of biofilm formation on both Gram negative and Gram positive bacteria including E. coli, Salmonella enterica, Pseudomonas aeruginosa, Staph. epidermis and Staph. Aureus. There are a variety of patented synthetic approaches for the incorporation of the bioactives depending on the specific application and polymer properties desired.
Advantages:
· Bioactives (e.g., antimicrobial, antioxidants) are naturally occurring with proven track record of safety (GRAS and EAFUS status)
· Bioactives are chemically (not physically) incorporated into the polymers to give a controlled release
· High weight percentage of bioactive incorporated means high activity per mass
· Polymer degradation rate to release bioactive is controlled by changing polymer composition
· Ease of manipulation into different geometries (e.g., particles, films, fibers)
· Food-based polymers are dual release systems – release two compounds (i.e., an antimicrobial agent and food preservative such as EDTA); ability to physically admix other bioactive compounds
· Proven effective for prevention of biofilms (i.e., microbial contamination)
Market Applications:
· Biodegradable, antimicrobial food packaging (i.e., edible packaging and active plastic wrap)
· Mixing with foods as particles (i.e., replacement for antibiotics sprinkled onto food surfaces)
IP Protection and Development Status:
Numerous U.S. patents and U.S. patent provisional applications support this invention. The IP associated with PolymerActives is available for licensing. Additional research and development support is available from Dr. Kathryn Uhrich’s group in the Chemistry and Chemical Biology Department at Rutgers University. Complete synthesis and characterization of these biodegradable, bioactive-based polymers were published in scientific journals (see http://rutchem.rutgers.edu/content_dynamic/faculty/kathryn_uhrich.shtml).
Monday, July 13, 2009
Uses of Kombo Better Extract and Derivatives
Rutgers Inventor:
James E. Simon, Ph.D.
Department of Plant Biology & Pathology
Invention Summary: Rutgers scientists have developed novel methods to treat a variety of neurological disorders including ischemic stroke. The methods center on the use of novel neuroprotectants isolated from Kombo butter, an African nutmeg. The scientists additionally developed methods to produce and purify the Kombo butter, its extracts and derivatives. These compounds may find utility in treat CNS and neurodegenerative diseases and for uses in aiding cognition.
Market Applications: CNS, Stroke, Parkinson’s, Alzheimer’s, Neuroprotection, Kombo butter.
Advantages: Complementary and alternative medicine.
Intellectual Property & Development Status: Provisional patent application filed.
James E. Simon, Ph.D.
Department of Plant Biology & Pathology
Invention Summary: Rutgers scientists have developed novel methods to treat a variety of neurological disorders including ischemic stroke. The methods center on the use of novel neuroprotectants isolated from Kombo butter, an African nutmeg. The scientists additionally developed methods to produce and purify the Kombo butter, its extracts and derivatives. These compounds may find utility in treat CNS and neurodegenerative diseases and for uses in aiding cognition.
Market Applications: CNS, Stroke, Parkinson’s, Alzheimer’s, Neuroprotection, Kombo butter.
Advantages: Complementary and alternative medicine.
Intellectual Property & Development Status: Provisional patent application filed.
Functional Neuronal Cell Lines
Rutgers Inventor:
Martin Grumet, PhD
Department of Cell Biology and Neuroscience
Invention Summary: Rutgers scientists have developed a novel cell line that gives rise to GABAergic neurons, currently lacking in the research field. The cells express markers characteristic of GABAergic-like neurons such as calretinin, calbindin, neuropeptide Y and somatostatin, and are electrically excitable in culture. These cells may be important for developing models of CNS diseases or for drug screening and transplantation, and may be useful for indications such as Alzheimer’s and Parkinson’s diseases.
Market Applications: Drug Discovery, Drug Screening, Cell Transplantation, Neuron.
Advantages: The cells show restricted neuronal differentiation in vitro, giving rise exclusively to neuron-like cells (b-III tubulin+) but not to astrocytes or oligodendrocytes. Further, they express significantly higher levels of mRNAs for a variety of enzymes, transcription factors and markers associated with functional neurons.
Intellectual Property & Development Status: A provisional patent application has been filed.
Martin Grumet, PhD
Department of Cell Biology and Neuroscience
Invention Summary: Rutgers scientists have developed a novel cell line that gives rise to GABAergic neurons, currently lacking in the research field. The cells express markers characteristic of GABAergic-like neurons such as calretinin, calbindin, neuropeptide Y and somatostatin, and are electrically excitable in culture. These cells may be important for developing models of CNS diseases or for drug screening and transplantation, and may be useful for indications such as Alzheimer’s and Parkinson’s diseases.
Market Applications: Drug Discovery, Drug Screening, Cell Transplantation, Neuron.
Advantages: The cells show restricted neuronal differentiation in vitro, giving rise exclusively to neuron-like cells (b-III tubulin+) but not to astrocytes or oligodendrocytes. Further, they express significantly higher levels of mRNAs for a variety of enzymes, transcription factors and markers associated with functional neurons.
Intellectual Property & Development Status: A provisional patent application has been filed.
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