Abstract: This invention provides novel radiopharmaceuticals which are useful as imaging agents for the diagnosis of cardiovascular disorders, infectious disease and cancer. The radiopharmaceuticals are comprised of phosphine or arsine ligated technetium-99m labeled hydrazino or diazino modified biologically active molecules that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy. This invention also provides methods for using the radiopharmaceuticals and kits comprising radiopharmaceutical precursors. The radiopharmaceuticals of this invention have the structure:?(Q).sub.d' L.sub.n --C.sub.h' !.sub.x --M.sub.t (A.sub.L1).sub.y (A.sub.L2).sub.z ;wherein the variables are as defined herein.
Type:
Grant
Filed:
April 3, 1995
Date of Patent:
April 28, 1998
Assignee:
The DuPont Merick Pharmaceutical Company
Abstract: As to reaction solutions in which the amount of each potassium ferricyanate, glucose oxidase and glucose substrate are set at a constant value while glucose concentrations are varied, intensity changes of peaks at a shift wavenumber of 2081 cm.sup.-1 in light scattering spectra are measured every 10 seconds, the maximum values of the intensity changes of the peaks at the respective glucose concentrations obtained, for obtaining a calibration curve from correlations between the maximum values of the reaction velocities and the glucose concentrations. The calibration curve is employed for carrying out quantitative measurement of an unknown sample.
Abstract: The present invention provides methods and compositions for the specific detection of Pseudomonas fluorescens and for the selective growth of this bacterium. In a preferred embodiment, selective growth of P. fluorescens is effected by the combination of Irgasan, carbenicillin and nitrofurantoin in a bacteriological medium comprising suitable nutrients for its growth. Also provided is a fast, reliable and economical method for the assessment of microbial quality of a fresh animal product, such as poultry, beef, fish, shellfish, milk or the like, using media selective for the growth of P. fluorescens and detection methods for microbial growth in the selective media.
Type:
Grant
Filed:
April 16, 1996
Date of Patent:
April 21, 1998
Assignee:
University of Georgia Research Foundation, Inc.
Abstract: A method for radiolabelling peptides using polyaminocarboxylate ligands having suitable protecting groups such that they can be added to peptides by standard solid phase or solution phase peptide synthetic chemistry and can be deproteced using standard cleavage/deprotection reagents and produce the peptide/chelate conjugate as a high purity monoaddition product is provided. The cleaved and deprotected ligand-peptide molecules can then be labeled with lanthanide or actinide radionuclides. The protected polyaminocarboxylate ligands form mono-anhydrides or mono-active esters under solid phase or solution phase conditions and permit only the desired monoaddition chelate-peptide conjugate to be formed.
Abstract: This invention relates to radiolabeled peptides and methods for producing such peptides. Specifically, the invention relates to specific binding peptides, methods and kits for making such peptides, and methods for using such peptides labeled with technetium-99m via a radiolabel-binding moiety covalently linked to the peptide to image thrombus sites in a mammalian body.
Abstract: The in vivo oxidation of lipids and lipid-containing molecules has been discovered to be initiated by the concurrent reaction of such lipid materials with reducing sugars such as glucose, advanced glycosylation endproducts such as AGE-peptides, or a compound which forms advanced glycosylation endproducts, to form materials or particles known as AGE-lipids. AGE-lipids have been implicated in the aging process, the abnormal formation of lipofuscin and in various disease states such as diabetes, atherosclerosis, and stroke. Methods of treating stroke, and especially inhibiting the infarct size of stroke, using agents which inhibit the formation of AGE-lipids are disclosed. Additionally, a method of screening for neuroprotective agents which can be used to reduce the size and severity of the infarct size is disclosed.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
March 31, 1998
Assignee:
The Picower Institute for Medical Research
Inventors:
Richard J. Bucala, Helen Vlassara, Anthony Cerami, Kevin J. Tracey
Abstract: New compounds endowed with a chelating property for paramagnetic bi- and trivalent metal ions, their chelates with said metal ions and their use as contrast agents in magnetic resonance imaging (MRI) are described. A method of obtaining images of organs and tissues of a human or animal body by means of nuclear magnetic resonance is also described.
Type:
Grant
Filed:
May 30, 1995
Date of Patent:
March 31, 1998
Assignee:
Dibra S.p.A.
Inventors:
Ernst Felder, Pier Lucio Anelli, Mario Virtuani, Andrea Beltrami, Marco Lolli
Abstract: A method of using cavitate- or clathrate-forming host/guest complexes for the preparation of contrast media in ultrasonic examination is provided. The host/guest complexes have a host which dissolves in a liquid carrier, releasing the guest (inert gas). With such contrast media, it is possible to diagnose blood and its flow conditions in the heart, and other organs, such as the myocardium, liver, spleen, and kidneys. Other internal systems such as the urinary ducts, the gastrointestinal tract, joints, and eyes can also be imaged.
Type:
Grant
Filed:
October 13, 1994
Date of Patent:
March 24, 1998
Assignee:
Schering Aktiengesellschaft
Inventors:
Celal Albayrak, Georg Rossling, Johannes Tack
Abstract: Herein described are radiolabeled compounds and their precursors useful to image D4 receptors in vivo, of the formula: ##STR1## wherein R is selected from iodo, tri(loweralkyl)tin and a radioisotopically labeled iodide and R.sup.1 is selected from H and alkoxycarbonyl, with the proviso that R is not iodo when R.sup.1 is H.The radiopharmaceutical compounds are useful particularly to image localization of D4 receptor in the human brain, and can therefore aid in the diagnosis of schizophrenia and other medical conditions in which the D4 receptor is implicated.
Type:
Grant
Filed:
November 12, 1996
Date of Patent:
March 10, 1998
Assignee:
Resolution Pharmaceuticals, Inc.
Inventors:
Alfred Pollak, Robert Dunn-Dufault, John Thornback
Abstract: The invention relates to a process for the preparation of an organ-specific substance labeled with technetium-99m, in which an organ-specific substance, or an organ-specific substance which has been pretreated or coupled to a complexing agent for technetium-99m, is mixed with ?99m!-pertechnetate and a complex-stabilized reducing agent.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
March 3, 1998
Assignee:
CIS Bio International
Inventors:
Karl-Heinz Bremer, Ludwig Kuhlmann, Alexander Schwarz, Axel Steinstrasser
Abstract: This invention provides compounds of the formula I ##STR1## wherein, R.sup.1, R.sup.2, and R.sup.3 are independently ?a first halogen atom,! fluorine, chlorine, bromine, iodine, alkyl, alkenyl, alkynyl, alkoxy, alkenoxy, or alkynoxy, wherein R.sup.2 and R.sup.3 can also independently be H, wherein at least one of R.sup.1, R.sup.2, and R.sup.3 is ?a second halogen atom! fluorine, bromine, iodine or is substituted with ?a second halogen atom,! fluorine, bromine or iodine and R.sup.4 is H or lower alkyl. The invention also provides precursors of formula I, radioactive analogs of formula I, and methods of using the compounds for the identification of 5-HT-3 receptors and the detection and treatment of abnormal conditions associated therewith.
Type:
Grant
Filed:
December 9, 1994
Date of Patent:
March 3, 1998
Assignee:
Vanderbilt University
Inventors:
Tomas de Paulis, Dennis E. Schmidt, William Hewlett, Michael H. Ebert
Abstract: This invention provides functional dyes of the general formula: ##STR1## wherein R.sup.1, R.sup.2, and R.sup.5 may be the same or different and are selected from the group consisting of hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyl, hydroxyl, C.sub.1 -C.sub.10 hydroxyalkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 aryl, carboxyl, C.sub.1 -C.sub.10 carboxylalkyl, halogen, nitro, C.sub.1 -C.sub.10 alkoxycarbonyl, mercapto, C.sub.1 -C.sub.10 mercaptoalkyl, C.sub.1 -C.sub.10 alkylthio, sulfonate, and --(CH.sub.2).sub.m --N(R.sup.6)(R.sup.7) wherein R.sup.6 and R.sup.7 are independently hydrogen or C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 acyl, and R.sup.6 and R.sup.7 are capable of forming 5, 6, or 7 membered rings which may optionally be substituted with --O--, --NR.sup.8, or --S--; R.sup.3 and R.sup.4 may be the same or different and are selected from the group consisting of C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 hydroxyalkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.
Abstract: This invention relates to radiolabel binding moieties for producing radiolabeled peptides and methods for making such peptides. Specifically, the invention relates to picolinic acid or picolinamine containing radiolabel binding moieties, peptides radiolabeled therewith and methods of making and using both the radiolabel binding moieties and peptides radiolabeled therewith.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
February 24, 1998
Assignee:
Diatide, Inc.
Inventors:
Richard T. Dean, Scott Buttram, William McBride, John Lister-James, Edgar R. Civitello
Abstract: A method of making a radiolabeled pyrimidine nucleoside or nucleotide is described. In the method, a stannylated pyrimidine nucleoside or nucleotide is contacted in an aqueous solution with a radioactive iodide, bromide, chlorine or astatine ion in the presence of an acidic hydrogen peroxide oxidizing solution comprising at least a 3:1 ratio of 30% hydrogen peroxide to 1N acid (v/v), whereby a water soluble pyrimidine nucleoside or nucleotide labeled with radioactive iodine, bromine, chlorine or astatine is formed. Kits suitable for practicing the method are also disclosed.
Type:
Grant
Filed:
June 9, 1995
Date of Patent:
February 24, 1998
Assignee:
President & Fellows of Harvard College
Inventors:
Amin I. Kassis, Catherine F. Foulon, S. James Adelstein
Abstract: The present invention is a method for assaying enzyme activity in a red blood sample. The method comprises these steps: (a) placing the following in a sample well: (1) a red blood sample containing an enzyme, (2) a substrate or substrates for the enzyme, (3) water, and (4) a buffer; (b) incubating the contents of the sample well for sufficient time and at sufficient temperature to allow for the formation of a fluorescent enzyme product should the enzyme be present in said red blood sample; (c) precipitating the hemoglobin; and (d) measuring the fluorescence of any fluorescent enzyme product formed in the sample well, directly from that sample well. The method of the invention may be used for assaying the activity of an enzyme, such as galactose-1-phosphate uridyl transferase (GALT) or biotinidase, in a red blood sample.
Type:
Grant
Filed:
May 6, 1996
Date of Patent:
February 17, 1998
Assignee:
Isolab, Inc.
Inventors:
Murray A. Rosenthal, Ronald A. Simkins, Ranjan Akhaury
Abstract: Peptides useful for lung imaging, and preferably containing a biological-function domain which includes the sequence Ile-Lys-Val-Ala-Val (IKVAV) (SEQ. ID NO.: 1) and a medically useful metal ion-binding domain are labeled with medically useful metal ions for use in a variety of diseases and pathologic conditions, and particularly diagnostic imaging of diseases and pathologic conditions of the lung.
Abstract: A method for revealing the presence or absence of a particular microorganism strain in a medium, wherein at least one strain enzyme substrate chromogen and at least one compound selected from a high-concentration carbohydrate are added to the culture medium so that a derived colour differing from the basic colour of the chromophore is obtained once the chromogen has been hydrolysed.
Abstract: This invention relates to radiolabeled peptides and methods for producing such peptides. Specifically, the invention relates to technetium-99m (Tc-99m) labeled leukocyte-binding peptides, methods and kits for making such peptides, and methods for using such peptides to image sites of infection and inflammation in a mammalian body.
Abstract: This invention provides functional dyes of the general formula: ##STR1## wherein R.sup.1, R.sup.2, and R.sup.5 may be the same or different and are selected from the group consisting of hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyl, hydroxyl, C.sub.1 -C.sub.10 hydroxyalkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 aryl, carboxyl, C.sub.1 -C.sub.10 carboxylalkyl, halogen, nitro, C.sub.1 -C.sub.10 alkoxycarbonyl, mercapto, C.sub.1 -C.sub.10 mercaptoalkyl, C.sub.1 -C.sub.10 alkylthio, sulfonate, and --(CH.sub.2).sub.m --N(R.sup.6)(R.sup.7) wherein R.sup.6 and R.sup.7 are independently hydrogen or C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 acyl, and R.sup.6 and R.sup.7 are capable of forming 5, 6, or 7 membered rings which may optionally be substituted with --O--, --NR.sup.8, or --S--; R.sup.3 and R.sup.4 may be the same or different and are selected from the group consisting of C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 hydroxyalkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1-C.sub.10 aryl, C.
Abstract: Liposomal compositions containing green porphyrins as photosensitizers are improved by enhancing the ratio of phospholipid to photosensitizer and by conducting the hydration an sizing of the liposomes in the composition at low temperature.