Abstract: The present invention relates to certain novel dinucleotides and formulations thereof which are highly selective agonists of the P2Y2 and/or P2Y4 purinergic receptor. They are useful in the treatment of chronic obstructive pulmonary diseases such as chronic bronchitis, PCD, cystic fibrosis, as well as prevention of pneumonia due to immobility. Furthermore, because of their general ability to clear retained mucus secretions and stimulate ciliary beat frequency, the compounds of the present invention are also useful in the treatment of sinusitis, otitis media and nasolacrimal duct obstruction. They are also useful for treatment of dry eye disease and retinal detachment.
Type:
Grant
Filed:
July 10, 1998
Date of Patent:
February 19, 2002
Assignee:
Inspire Pharmaceuticals, Inc.
Inventors:
William Pendergast, Benjamin R. Yerxa, Janet L. Rideout, Suhaib M. Siddiqi
Abstract: A method for reducing evaporation of a liquid reagent solution during solid phase, micro-scale chemical synthesis of a molecule comprising sub-units on an open environment solid support surface. The method includes the steps of providing an open solid support surface including at least one binding site which is functionalized with a reactive chemical moiety; and depositing a substantially controlled and minute volume of liquid reagent solution onto the support surface, and in contact with the binding site. The reagent solution includes reactants contained in at least one relatively high boiling point solvent, in contrast to standard organic solvents for such reagents. Application of a high boiling point solvent substantially reduces evaporation of the reagent solution in the open environment during synthesis on the solid support while enabling the maintenance of a substantially high reaction yield.
Type:
Grant
Filed:
September 14, 2000
Date of Patent:
January 8, 2002
Assignee:
Protogene Laboratories, Inc.
Inventors:
Thomas M. Brennan, Albrecht W. Frauendorf
Abstract: A method and preparation for the stimulation of mucosal hydration in a subject in need of such treatment is disclosed. The method comprises administering to the mucosal surfaces of the subject a purinergic receptor agonist such as uridine 5′-diphosphate (UDP), dinucleotides, cytidine 5′-diphosphate (CDP), adenosine 5′-diphosphate (ADP), or their therapeutically useful analogs and derivatives, in an amount effective to stimulate mucin secretion. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include: topical administration via a liquid, gel, cream, or as part of a contact lens or selective release membrane; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.
Type:
Grant
Filed:
February 25, 2000
Date of Patent:
December 18, 2001
Assignee:
Inspire Pharmaceuticals, Inc.
Inventors:
Benjamin R. Yerxa, Janet L. Rideout, Arthur C. Jones
Abstract: This invention provides a DNA polymerase that is a mutant form of a naturally occurring DNA polymerase, of which one or more amino acids in the active site are mutated. The DNA polymerase mutant of this invention is characterized by altered fidelity or altered enzymatic activity in comparison with the naturally occurring DNA polymerase. For example, the DNA polymerase mutant provides increased enzymatic activity, altered dNTP/rNTP specificity, or enhanced fidelity. In one aspect of the invention, the naturally occurring DNA polymerase comprises an amino acid sequence motif: AspTyrSerGlnIleGluLeuArg in the active site. In another aspect of the invention, the naturally occurring DNA polymerase comprises an amino acid sequence motif: LeuLeuVa1AlaLeuAspTyrSerGlnIleGluLeuArg in the active site.
Abstract: A method and media for producing bacterial cellulose under agitated culture conditions resulting in sustained production over an average of 70 hours of at least 0.1 g/liter per hour are achieved. A unique reticulated cellulose product is produced using the methods and conditions claimed, and may be converted to of a sheet characterized by substantial resistance to densification and great tensile strength when produced by sheet forming means. Acetobacter strains are identified as stable under agitated culture conditions and exhibit substantially reduced gluconic and keto-gluconic acids production.
Type:
Grant
Filed:
June 1, 1993
Date of Patent:
December 11, 2001
Assignee:
CP Kelco U.S., Inc.
Inventors:
Arie Ben-Bassat, Robert Bruner, Sharon Shoemaker, Yehoshua Aloni, Harry Wong, Donald C. Johnson, Amar N. Neogi
Abstract: A system and method for rating the performance of competing antennas under various environmental conditions is herein disclosed. The present invention provides a method to statistically characterize antenna performance, relating actual operating conditions to the likelihood of completing a reliable wireless communication link within a desired confidence level. The invention provides a system and method to predict antenna performance based upon actual usage condition factors, such as power needed for transmitting, and radiation absorption by a user, relative to the angle of orientation between the antenna under test and a corresponding antenna on the opposite side of a wireless communication link.
Abstract: The present invention is directed to a method for inhibiting viral replication and treating viral infections by administering a pharmaceutically effective amount of a compound capable of binding a microtubule such as a diiodo thyronine analogue having no significant hormonal activity. The present invention also features novel pharmaceutical compositions comprising the same.
Abstract: The present invention relates to P1-(cytidine 5′-)-P-(uridine 5′-)tetraphosphates and its salts, esters and amides, and formulations thereof which are highly stable and selective agonists of the P2Y2 and/or P2Y4 purinergic receptor. The compounds of the invention are useful in the treatment of chronic obstructive pulmonary diseases such as chronic bronchitis, primary ciliary dyskinesia, cystic fibrosis, as well as prevention of pneumonia due to immobility, and the induction of sputum and its expectoration. Furthermore, because of their general ability to clear retained mucus secretions and stimulate ciliary beat frequency, the compounds of the present invention are also useful in the treatment of sinusitis and otitis media.
Type:
Grant
Filed:
May 21, 1999
Date of Patent:
November 27, 2001
Assignees:
Inspire Pharmaceuticals, Inc., University of North Carolina at Chapel Hill
Inventors:
Benjamin R. Yerxa, William Pendergast, Janet L. Rideout, Maryse Picher, Richard C. Boucher, Jr., M. Jackson Stutts
Abstract: The present invention provides new methods for the synthesis of the therapeutic dinucleotide, P1,P4-di(uridine 5′-tetraphosphate), and demonstrates applicability to the production of large quantities. The methods of the present invention substantially reduce the time period required to synthesize diuridine tetraphosphate, preferably to three days or less. The novel tetrammonium and tetrasodium salts of P1,P4-di(uridine 5′-tetraphosphate) (Formula I) prepared by these methods are stable, soluble, nontoxic, and easy to handle during manufacture,
wherein:
X is Na, NH4 or H, provided that all X groups are not H.
Abstract: A method for inhibition of retroviral replication by manipulation of enzyme adenosine diphosphoribosyl transferase which endogenously inhibits retroviral reverse transcriptase. The method is useful for prevention and treatment of retroviral infections, including HIV. The inhibition of the viral replication is achieved by administration to a mammal susceptible to or infected with a retrovirus drugs which specifically inhibit poly-ADP-ribosylation of adenosine diphosphoribosyl transferase.
Abstract: The present invention relates to conjugates comprising a compound capable of emitting fluorescence, a linker and a protein. The present invention also concerns the preparation of such conjugates as well as their use.
Type:
Grant
Filed:
November 19, 1998
Date of Patent:
October 23, 2001
Assignee:
Deutsches Krebsforschungszentrum Stiftung des offentlichen
Rechts
Inventors:
Hansjörg Sinn, Wolfgang Maier-Borst, Gerd Stehle, Michael Kaus, Andreas Wunder, Hans-Hermann Schrenk
Abstract: The present invention is directed to a method for treating cancers by administering a pharmaceutically effective amount of a diiodo thyronine analogue having no significant hormonal activity and a vinca alkaloid or biologically active analog thereof. The present invention also features novel pharmaceutical compositions comprising the same.
Abstract: The present invention relates to a method for conferring herbicide, pest, and disease resistance in plant hosts. Specifically, the present invention employs transient viral expression vectors to express proteins or enzymes conferring resistance in plant hosts. In addition, a library of nucleotide sequence variants in a sense or antisene orientation may be used to determine the targets of an herbicide or pathogen and to screen suitable viral nucleic acids for herbicide, pest, and disease resistance.
Abstract: The present invention is directed to a method for treating inflammation or inflammatory disease, bacterial infection, arthritis and stroke in an animal or mammal, which comprises the steps of administering an effective amount of a pADPRT inhibitory compound to said animal or mammal.
Abstract: The present invention features a method for isolating and purifying vitamins and sugars from a plant host which is applicable on a large scale. Moreover, the present invention provides a more efficient method for isolating vitamins and sugars than those methods described in the prior art. In general, the present method of isolating vitamins and sugars comprises the steps of homogenizing a plant to produce a green juice, adjusting the pH of and heating the green juice, separating the target species, either vitamins or sugars, from other components of the green juice by one or more cycles of centrifugation, resuspension, and ultrafiltration, and finally purifying vitamins or sugars by such procedure as PEG-precipitation, chromatography and/or salt precipitation.
Type:
Grant
Filed:
December 17, 1999
Date of Patent:
October 16, 2001
Assignee:
Large Scale Biology Corporation
Inventors:
Stephen J. Garger, R. Barry Holtz, Michael J. McCulloch, Thomas H. Turpen
Abstract: The present invention relates to an expression vector having a foreign DNA. Said DNA at its 3′ end has a sequence which prevents the replication of the expression vector from occurring in the opposite direction to the transcription thereof. The invention also relates to a preparation containing such an expression vector and to the use of both in the permanent expression of foreign DNA in cells.
Abstract: This invention is directed to a plus strand RNA viral vector for transformation of a host organism with a foreign RNA, and expression of said foreign RNA. The foreign RNA is inserted into an infective RNA viral segment containing cis-acting viral replication elements, and allowed to infect the host organism. The RNA vector is modified to obtain infectivity by not incorporating a cap at the 5′ end of the genome. The modified RNA is able to tolerate the exogenous RNA segment without disrupting the replication of the modified RNA, in the absence of a trans-acting viral replication element in a single component plant virus host cell.
Type:
Grant
Filed:
February 11, 2000
Date of Patent:
October 9, 2001
Assignee:
Large Scale Biology Corporation
Inventors:
John A. Lindbo, Gregory P. Pogue, Thomas H. Turpen
Abstract: This invention is directed to a plus strand RNA viral vector for transformation of a host organism with a foreign RNA, and expression of said foreign RNA. The foreign RNA is inserted into an infective RNA viral segment containing cis-acting viral replication elements, and allowed to infect the host organism. The RNA vector is modified to obtain infectivity by including an intervening sequence between the cap and the 5′ end. The modified RNA is able to tolerate the exogeneous RNA segment without disrupting the replication of the modified RNA, in the absence of a trans-acting viral replication element in a single component plant virus host cell.
Type:
Grant
Filed:
February 11, 2000
Date of Patent:
October 9, 2001
Assignee:
Large Scale Biology Corporation
Inventors:
John A. Lindbo, Gregory P. Pogue, Thomas H. Turpen
Abstract: Novel enzymatically produced melanins are described that are useful in the treatment of HIV infection. The novel remanins are optionally modified to contain chemical moieties such as halogens, sulfates, or sulfonyl groups. Additionally, the novel enzymatically synthesized melanins may be modified, or further modified, by chemical oxidation.
Abstract: The present invention relates to a method for isolating from the immunological gene repertoire a gene coding for a receptor having the ability to bind a preselected ligand. Receptors produced by the gene isolated by the method, particularly catalytic receptors, are also contemplated.
Type:
Grant
Filed:
August 21, 1992
Date of Patent:
September 18, 2001
Assignees:
Scripps Research Institute, Medical Research Council, Stratagene
Inventors:
Gregory P. Winter, Lutz Riechmann, William D. Huse, Joseph A. Sorge, Richard A. Lerner