U.S. patents available from 1976 to present.
U.S. patent applications available from 2005 to present.

Modified cellular substrates used as linkers for increased cell retention of diagnostic and therapeutic agents

Patent 5057301 Issued on October 15, 1991. Estimated Expiration Date: Icon_subject October 15, 2008. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Patent References

3817978

3852413

Diagnostic agent
Patent #: 4126669
Issued on: 11/21/1978
Inventor: Rothman ,   et al.

Monoradioiodinated derivatives and precursors for production thereon
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Issued on: 05/13/1980
Inventor: Akerkar ,   et al.

Physiological preparation containing loaded cells in suspension and a magnetic agent for local concentration thereof in a living body
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Peptide macromolecular complexes
Patent #: 4275000
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Inventor: Ross

Radiopharmaceutical method for monitoring kidneys
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Inventor: Frank ,   et al.

Biocidal triazolylmercapto substituted haloacrylonitrile compounds
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Inventor: Felix

ଲ-Galactosyl-umbelliferone-labeled protein and polypeptide conjugates
Patent #: 4331590
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Inventor: Bocuslaski ,   et al.

Immunogenic polysaccharide-protein conjugates
Patent #: 4356170
Issued on: 10/26/1982
Inventor: Jennings ,   et al.

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Inventors

Assignee

Application

No. 178418 filed on 04/06/1988

US Classes:

530/363, Serum albumin, e.g., BSA, HSA, etc.424/179.1, Conjugated via claimed linking group, bond, chelating agent, or coupling agent (e.g., conjugated to proteinaceous toxin via claimed linking group, bond, coupling agent, etc.)424/181.1, Conjugated to nonproteinaceous bioaffecting compound (e.g., conjugated to cancer-treating drug, etc.)514/8, Glycoprotein (carbohydrate containing)530/386, Globulins530/391.5, Conjugated via a specifically-identified linking group, chelating group, coordination complex, coupling agent, or conjugation agent530/391.9, Conjugated via a specifically-identified linking group, coupling agent, or conjugation agent530/395, Glycoprotein, e.g., mucins proteoglycans, etc.530/399, Hormones, e.g., prolactin, thymosin, growth factors, etc.536/18.4Halogen containing

Examiners

Primary: Maples, John S.

Attorney, Agent or Firm

Foreign Patent References

  • 094844 EP. 11/21/1983
  • 289187 EP. 11/21/1988
  • 336364 EP. 10/21/1989

International Classes

A61K 039/395
A61K 037/10
A61K 043/00
C07H 015/00

Abstract

Modified cellular substrates are used as linking groups that are recognized as cellular substrates by intracellular metabolic enzymes. The linking groups function to attach a ligand, such as a drug or radionuclide, to a targeting protein, such as an antibody or antibody fragment. The false substrate structure of the linking groups causes increased cellular retention of the linking group/ligand conjugate because the enzymes used for catabolism of the substrate are inhibited by the false substrate structure of the linking group.

Other References

  • European Search Report for Application No. EP/89105876
  • Goodman et al., "New Myocardial Imaging Agents: Preparation of 15-(p-[123 I]-Iodophenyl)-7-Tellurapontadecanoic Acid from Na[123 I] by a Triazene Decomposition Reaction", in Paras and Thiessen (eds.), The Developing Role of Short-Lived Radio-nuclides in Nuclear Medical Practice, Office of Science and Technical Information, U.S. Dept. of Energy, 1985 [Goodman et al., I]
  • Liefhold et al., "Synthesis, Labeling, and Pharmacokinetics of 131 I Labeled Phenylene-Iodophenyl-Fatty Acids (PHIPA)", in Sixth Int. Symposium on Radiopharmaceutical Chemistry, pp. 212-14, 1986
  • Knapp, Jr. et al., "Development of Radioiodinated Fatty Acids for Applications in Nuclear Cardiology", in Paras and Thiessen (eds.), The Developing Role of Short-Lived Radionuclides in Nuclear Medical Practice, Office of Science and Technical Information, U.S. Dept. of Energy, [Knapp, Jr. et al. I]
  • Gallagher et al., "Radiopharmaceuticals XXVII. 18 F-Labeled 2-Deoxy-2-Fluoro-D-Glucose as a Radiopharmaceutical for Measuring Regional Myocardial glucose Metabolism in Vivo: Tissue Distribution and Imaging Studies in Animals", J. Nucl. Med. 18:990-996, 1977 [Gallagher et al., I]
  • Knapp, Jr. et al., "Effect of Tellurium Position on the Myocardial Uptake of Radioiodinated 18-Iodotellura-17-Octadecanoic Acid Analogues", J. Med. Chem. 27:57-63, 1984, [Knapp, Jr. et al., II]
  • Livni et al., "Beta-methyl[1-11 C] heptadecanoic Acid: A New Myocardial Metabolic Tracer for Position Emission Tomography", J. Nucl. Med. 23:169-175, 1982
  • Elmaleh et al., "Myocardial Imaging with 9-[Te-123m]Telluraheptadecanoic Acid", J. Nucl. Med. 22:994-999, 1981 [Elmleh et al. 1]
  • Goodman et al., "Synthesis and Evaluation of Radioiodinated Terminal p-Iodophenyl-Substituted ଱-and ଲ-Methyl-Branched Fatty Aciods", J. Med. Chem. 27:340-397, 1984 [Goodman et al. II]
  • Goodman et al., "New Myocardial Imaging Agents: Synthesis of 15-(p-Iodophenyl)-3(R,S)-methylpentadecanoic Acid by Decomposition of a 3,3-(1,5-Pentarediyl)triazene Precursor", J. Org. Chem. 49:2322-2325, 1984 [Goodman et al. III]
  • Gallagher et al., "Metabolic Trapping as a Principle of Radio-pharmaceutical Design: Some Factors Responsible for the Biodistribution of [18 F]2-Deoxy-2-Fluoro-D-Glucose", J. Nucl. Med. 19:1154-1161, 1978 [Gallagher et al. II]
  • Elmaleh et al., "Comparison of 11 C and 14 C-Labeled Fatty Acids and Their ଲ-Methyl Analogs", Int. J. Med. Biol. 10:181-187, 1983 [Elmaleh et al. II]
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  • Goodman et al., "Synthesis and Biological Evaluation of 17-[131 I]Iodo-9-Telluraheptadecanoic Acid, a Potential Myocardial Imaging Agent", J. Med. Chem. 25:613-618, 1982[Goodman et al. IV]
  • Goodman et al., "A New, Well-Retained Myocardial Imaging Agent: Radioiodinated 15-(p-Iodophenyl)-6-Tollurapntadecanoic Acid", J. Nucl. Med. 23:904-908, 1982 [Goodman et al. V]
  • Knapp, Jr. et al., "New Myocardial Imaging Agents: Stabilization of Radioiodine as a Terminal Vinyl Iodide Moiety on Tellurium Fatty Acids", J. Med. Chem. 26:1293-300, 1983 [Knapp, Jr. et al. III]
  • Otto et al., "Radioiodinated Branched-Chain Fatty Acids: Substrates for Beta Oxidation? Concise Communication", J. Nucl. Med. 25:75-80, 1985
  • Knapp, Jr. et al., "Effects of Chain Length and Tellurium Position on the Myocardial Uptake of Te-123m Fatty Acids", J. Nucl. Med. 22:988-993, 1981 [Knapp, Jr. et al. IV]
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