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Radioiodinated diacylglycerol analogues and methods of use
NW/. Med. Viol. Vol. 17, No. 8, pp. iii-vi, 1990 In/. J. Radiat. Appl. Instrum. Part E Pergamon Press plc. Printed in Great Britain
NEW PATENTS This Section contains abstracts and, where appropriate, illustrations of recently issued United States patents and
published patent applications filed from over 30 countries under the Patent Cooperation Treaty. This information was obtained from recent additions to the Pergamon PATSEARCH’* online database in accordance with interest profiles developed by the Editors. Further information about Pergamon PATSEARCH” can be obtained from Pergamon Orbit InfoLine Inc., 8000 Westpark Drive, McLean, Virginia 22102, U.S.A. Copies of complete patents announced in this Section are available from Pergamon Orbit InfoLine Inc. for $8 per copy. Payment with order is required. Orders outside North America add $2 for air postage. Order by patent number for Pergamon Orbit InfoLine only.
4917878
4923969
NOVEL USE OF A RADIOLABELLED ANTIBODY AGAINST STAGE SPECIFIC EMBRYONIC ANTIGEN FOR THE DETECTION OF OCCULT ABSCESSES IN MAMMALS
PREPARATION OF 99M TC RADIOPHARMACEUTICALS Bonnyman, John Baldas, Nunawading, Australia assigned to The Commonwealth of Australia
John
Compounds of the formula I: See Patent for Tubular Presentation PS wherein R + represents a cation and X represents a halo group, are prepared by reaction with an azide compound in the presence of a hydrohalic acid. The compounds are useful in production of 99mTc-labelled radio-pharmaceuticals by reaction with ligands and monoclonal antibodies or antibody fractions.
Madhukar L Thakur assigned to Thomas Jefferson University The invention discloses improved reagents containing antibodies against stage specific embryonic antigen-l antibodies and improved methods for detection of occult abscess and inflammation using the improved reagents.
4921963
4925649
PLATINUM COMPLEXES WITH ONE RADIOSENSITIZING LIGAND
RADIOIODINATED DIACYLGLYCEROL ANALOGUES AND METHODS OF USE
Kirsten Skov, Nicholas P Farrell, David J Chaplin, Vancouver, VT, Canada assigned to British Columbia Cancer Foundation
Raymond E Counsell, Laurie Strawn assigned to The University of Michigan Novel iodinated and radioiodinated I ,2diacylglycerol analogues are biological reagents for studying the effect of diacylglycerols in the activation of protein kinase C. This calciumrequiring enzyme may be involved in tumor promotion by phorbol diesters and related compounds, Iodinated and radioiodinated 1,2diacylglycerol analogues, in accordance with the
Complexes of platinum II containing a single radiosensitizer ligand and an amino or ammine substituent shows superior binding to DNA and are useful in chemotherapy and sensitization of hypoxic tumors to radiation. The chemotherapeutic value of these compounds is enhanced by administration of vasoactive agents. ..,
111
New Patents
iv
invention, are useful as imaging agents, such as radiopaques and radiopharmaceuticals, and have the general formula: See Patent for Chemical Structure
4925650 TECHNETIUM -99M COMPLEX FOR EXAMINING THE RENAL FUNCTION
in particular fluorine- 18, bromine-75 or iodine123, and R denotes hydrogen or methyl, in of 2-fluoro( 18)-tyrosine and particular methyltyrosine (II) for emission-tomographic measurement of protein synthesis in vivo, in particular for the purposes of cerebral diagnosis, by means of SPECT and, in particular, by means of PET, provides, in view of the particularly high incorporation rate, especially of II, the possibility of quantitative kinetic evaluation and is thus of great interest, specifically in the framework of tumor diagnosis.
Dennis Nosco, Alfons M Verbruggen assigned to Mallinckrodt Inc The invention relates to a technetium-99m complex of the general formula See Patentfor Chemical Structure (I) wherein Z is a sulphur atom or an amino group of the general formula R 17-N(Rl8)k, in which k is 0 or 1 and R17 and RI8 have the same meanings as the symbols R 1-R 16; each of the symbols RI-R16 is individually selected from the group consisting of hydrogen, straight or branched, unsubstituted or substituted alkyl having l-4 carbon atoms, and ACOOH, wherein A is a straight or branched, unsubstituted or substituted alkly group having O-4 carbon atoms; and R5 together with R6 or R9 together with R 10 additionally may form an oxygen atom; Tc represents technetium-99m; t is 0 or 1; and n is 0 or 1; with the provisos that (a) if R15, R 16, R17 and/or R18 are/is ACOOH, A is a straight or branched, unsubstituted or substituted alkyl group having l-4 carbon atoms; (b) at least one of the symbols RI-R18 is ACOOH; and (c) if t is 1, at least two of the symbols RlRI8 are ACOOH; or a pharmaceutically acceptable salt of this compound, The invention further relates to a radiopharmaceutical composition comprising said complex, to the use of this composition for examining the renal function, and to a kit for preparing such a composition.
4925651 RADIOFLUORO-TYROSINE DERIVATIVES, THE PREPARATION AND USE THEREOF Heinz H Coenen, Peer Kling, Gerhard Stoecklin, Grevenbroich, Federal Republic Of Germany assigned to Kernforschungsanlage Juelich Gesellschaft mit beschrankter Haftung The use of 2-radiohalogenotyrosine derivatives of the formula I See Patent for Chemical Structure (I) in which X denotes a radioactive halogen,
4925925 RADIOACTIVE RHENIUM LIGATED TO 2-HYDROXY ISOBUTYRIC ACID AND METHOD OF USE Edward A Deutsch assigned to University of Cincinnati A composition of matter having the following general formula See Patent for Chemical Structure wherein L represents 2-hydroxy isobutyric acid. This composition of matter is useful in improving the reaction efficiency or yield when bonding rhenium to a chelating ligand preferably a polydentate sulfur, selenium, phosphorous or nitrogen ligand. This provides a method to bond radioactive rhenium to various chelating ligands for a radiopharmaceutical. Further, this also provides a method to bond a radioactive rhenium to a protein such as a monoclonal antibody. This in turn provides a method to provide beta emitting radiation to cancer cells.
4931270 METHOD FOR DETECTING DOPAMINERGIC DISEASES USING FLUORINE-18 RADIOLABELLED D2 DOPAMINE RECEPTOR LIGANDS Alan S Horn, Paul A Jerabek, James Peck, Groningen, CA, Netherlands assigned to Nelson Research & Development Abnormalitites in the distribution of a dopamine D2 receptors in humans and other mammals are detected by (1) administering to a human or other mammal an amount of a 18Fradiolabelled compound sufficient to be detected by a positron emission sensitive means for im-
NEW PATENTS This Section contains abstracts and, where appropriate, illustrations of recently issued United States patents and
published patent applications filed from over 30 countries under the Patent Cooperation Treaty. This information was obtained from recent additions to the Pergamon PATSEARCH’* online database in accordance with interest profiles developed by the Editors. Further information about Pergamon PATSEARCH” can be obtained from Pergamon Orbit InfoLine Inc., 8000 Westpark Drive, McLean, Virginia 22102, U.S.A. Copies of complete patents announced in this Section are available from Pergamon Orbit InfoLine Inc. for $8 per copy. Payment with order is required. Orders outside North America add $2 for air postage. Order by patent number for Pergamon Orbit InfoLine only.
4917878
4923969
NOVEL USE OF A RADIOLABELLED ANTIBODY AGAINST STAGE SPECIFIC EMBRYONIC ANTIGEN FOR THE DETECTION OF OCCULT ABSCESSES IN MAMMALS
PREPARATION OF 99M TC RADIOPHARMACEUTICALS Bonnyman, John Baldas, Nunawading, Australia assigned to The Commonwealth of Australia
John
Compounds of the formula I: See Patent for Tubular Presentation PS wherein R + represents a cation and X represents a halo group, are prepared by reaction with an azide compound in the presence of a hydrohalic acid. The compounds are useful in production of 99mTc-labelled radio-pharmaceuticals by reaction with ligands and monoclonal antibodies or antibody fractions.
Madhukar L Thakur assigned to Thomas Jefferson University The invention discloses improved reagents containing antibodies against stage specific embryonic antigen-l antibodies and improved methods for detection of occult abscess and inflammation using the improved reagents.
4921963
4925649
PLATINUM COMPLEXES WITH ONE RADIOSENSITIZING LIGAND
RADIOIODINATED DIACYLGLYCEROL ANALOGUES AND METHODS OF USE
Kirsten Skov, Nicholas P Farrell, David J Chaplin, Vancouver, VT, Canada assigned to British Columbia Cancer Foundation
Raymond E Counsell, Laurie Strawn assigned to The University of Michigan Novel iodinated and radioiodinated I ,2diacylglycerol analogues are biological reagents for studying the effect of diacylglycerols in the activation of protein kinase C. This calciumrequiring enzyme may be involved in tumor promotion by phorbol diesters and related compounds, Iodinated and radioiodinated 1,2diacylglycerol analogues, in accordance with the
Complexes of platinum II containing a single radiosensitizer ligand and an amino or ammine substituent shows superior binding to DNA and are useful in chemotherapy and sensitization of hypoxic tumors to radiation. The chemotherapeutic value of these compounds is enhanced by administration of vasoactive agents. ..,
111
New Patents
iv
invention, are useful as imaging agents, such as radiopaques and radiopharmaceuticals, and have the general formula: See Patent for Chemical Structure
4925650 TECHNETIUM -99M COMPLEX FOR EXAMINING THE RENAL FUNCTION
in particular fluorine- 18, bromine-75 or iodine123, and R denotes hydrogen or methyl, in of 2-fluoro( 18)-tyrosine and particular methyltyrosine (II) for emission-tomographic measurement of protein synthesis in vivo, in particular for the purposes of cerebral diagnosis, by means of SPECT and, in particular, by means of PET, provides, in view of the particularly high incorporation rate, especially of II, the possibility of quantitative kinetic evaluation and is thus of great interest, specifically in the framework of tumor diagnosis.
Dennis Nosco, Alfons M Verbruggen assigned to Mallinckrodt Inc The invention relates to a technetium-99m complex of the general formula See Patentfor Chemical Structure (I) wherein Z is a sulphur atom or an amino group of the general formula R 17-N(Rl8)k, in which k is 0 or 1 and R17 and RI8 have the same meanings as the symbols R 1-R 16; each of the symbols RI-R16 is individually selected from the group consisting of hydrogen, straight or branched, unsubstituted or substituted alkyl having l-4 carbon atoms, and ACOOH, wherein A is a straight or branched, unsubstituted or substituted alkly group having O-4 carbon atoms; and R5 together with R6 or R9 together with R 10 additionally may form an oxygen atom; Tc represents technetium-99m; t is 0 or 1; and n is 0 or 1; with the provisos that (a) if R15, R 16, R17 and/or R18 are/is ACOOH, A is a straight or branched, unsubstituted or substituted alkyl group having l-4 carbon atoms; (b) at least one of the symbols RI-R18 is ACOOH; and (c) if t is 1, at least two of the symbols RlRI8 are ACOOH; or a pharmaceutically acceptable salt of this compound, The invention further relates to a radiopharmaceutical composition comprising said complex, to the use of this composition for examining the renal function, and to a kit for preparing such a composition.
4925651 RADIOFLUORO-TYROSINE DERIVATIVES, THE PREPARATION AND USE THEREOF Heinz H Coenen, Peer Kling, Gerhard Stoecklin, Grevenbroich, Federal Republic Of Germany assigned to Kernforschungsanlage Juelich Gesellschaft mit beschrankter Haftung The use of 2-radiohalogenotyrosine derivatives of the formula I See Patent for Chemical Structure (I) in which X denotes a radioactive halogen,
4925925 RADIOACTIVE RHENIUM LIGATED TO 2-HYDROXY ISOBUTYRIC ACID AND METHOD OF USE Edward A Deutsch assigned to University of Cincinnati A composition of matter having the following general formula See Patent for Chemical Structure wherein L represents 2-hydroxy isobutyric acid. This composition of matter is useful in improving the reaction efficiency or yield when bonding rhenium to a chelating ligand preferably a polydentate sulfur, selenium, phosphorous or nitrogen ligand. This provides a method to bond radioactive rhenium to various chelating ligands for a radiopharmaceutical. Further, this also provides a method to bond a radioactive rhenium to a protein such as a monoclonal antibody. This in turn provides a method to provide beta emitting radiation to cancer cells.
4931270 METHOD FOR DETECTING DOPAMINERGIC DISEASES USING FLUORINE-18 RADIOLABELLED D2 DOPAMINE RECEPTOR LIGANDS Alan S Horn, Paul A Jerabek, James Peck, Groningen, CA, Netherlands assigned to Nelson Research & Development Abnormalitites in the distribution of a dopamine D2 receptors in humans and other mammals are detected by (1) administering to a human or other mammal an amount of a 18Fradiolabelled compound sufficient to be detected by a positron emission sensitive means for im-