Patents Examined by Lara E. Chapman
  • Patent number: 5690906
    Abstract: Tetralin derivatives, such as 7-hydroxy-2-(N-n-propyl-N-3 '-iodo-2'-propenyl)-amino!tetralin and 8-hydroxy-2-(N-n-propyl-N-3 '-iodo-2'-propenyl)amino-tetralin, are disclosed which have affinity and specificity for dopamine D-3 and/or serotonin 5-HT.sub.1A receptors.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: November 25, 1997
    Assignee: The Trustees of the University of Pennsylvania
    Inventor: Hank F. Kung
  • Patent number: 5684137
    Abstract: Novel chelating compounds and the corresponding radionuclide metal chelates are useful for radiolabeling proteins such as antibodies, ligands such as biotin and anti-ligands such as streptavidin with radionuclide metals such as .sup.99m Tc, .sup.186 Re, and .sup.188 Re. The radiolabeled proteins, ligands and anti-ligands have diagnostic or therapeutic use, depending on the radionuclide metal chosen.
    Type: Grant
    Filed: February 22, 1995
    Date of Patent: November 4, 1997
    Assignee: NeoRx Corporation
    Inventors: Sudhakar Kasina, Linda M. Gustavson
  • Patent number: 5679318
    Abstract: Stable therapeutic radionuclide compositions comprising, for example, .sup.186 Re, .sup.188 Re and .sup.131 I stably bound to a proteinaceous targeting moiety and suitable for human in vivo administration are disclosed. Stabilizing agents preferably comprise antioxidants and challenging agents, and combination of HSA with an antioxidant and/or challenging agent provides enhanced long term stability. Ascorbic acid is an especially preferred stabilizing agent, which provides stability of therapeutic radionuclide compositions at levels of at least about 90% for several hours up to several days.
    Type: Grant
    Filed: November 21, 1994
    Date of Patent: October 21, 1997
    Assignee: NeoRx Corporation
    Inventors: Jean-Luc Vanderheyden, Alan R. Fritzberg, Joseph E. Bugaj, Fu-Min Su, Prasanna Venkatesan
  • Patent number: 5667764
    Abstract: Compounds are provided having the capability of binding therapeutically active substances to lipid containing bio-compatible particles, such as cells or viruses. These compounds include a bio-affecting moiety, comprising a therapeutically active substance, which is linked via a linking moiety to at least one hydrocarbon substituent selected so that the compounds is sufficiently non-polar to impart lipid binding capability to the compound. Thus, compounds of the invention are useful for site-selective delivery of therapeutic agents, and retention thereof at the selected site.Methods are provided for using various compounds of the invention in treatment of diseases or other pathological conditions. For example, methods are provided for treatment of: (1) post-angioplasty restenosis; (2) rheumatoid arthritis; (3) tumor cell proliferation, particularly tumor cells associated with ovarian cancer; and (4) psoriasis.
    Type: Grant
    Filed: May 15, 1992
    Date of Patent: September 16, 1997
    Assignee: Zynaxis, Inc.
    Inventors: Gregory A. Kopia, Paul K. Horan, Brian D. Gray, David E. Troutner, Katharine A. Muirhead, Kamleshkumar A. Sheth, Chia-En Lin, Zhizhou Yu, Bruce D. Jensen, Sue Ellen Slezak
  • Patent number: 5662882
    Abstract: The present invention relates to novel radiopharmaceutical imaging agents having non-stannous reductants. The present invention further relates to kits for forming radiopharmaceutical imaging agents, such kits including non-stannous reducing agents.
    Type: Grant
    Filed: March 23, 1995
    Date of Patent: September 2, 1997
    Assignee: Mallinckrodt Medical, Inc.
    Inventors: James W. Brodack, Mark A. DeRosch, Edward A. Deutsch, Mary Marmion Dyszlewski
  • Patent number: 5648344
    Abstract: Ligands that bind to human selectin receptors are disclosed. The ligands are formulated with excipient carriers to form compositions which are administered to treated condition such as inflammation. The ligands have the structural formula III ##STR1## or molecules which have hydrogen bond donor groups equivalent to the circled groups with respect to their ability to form hydrogen bonds with a selectin under physiological conditions.
    Type: Grant
    Filed: July 30, 1992
    Date of Patent: July 15, 1997
    Assignee: Glycomed Incorporated
    Inventors: Brian K. Brandley, Michael Tiemeyer, Stuart J. Swiedler, Margaret Moreland, Hans Schweingruber, Narasinga Rao
  • Patent number: 5643884
    Abstract: This invention relates generally to the field of medicinal chemistry, and more specifically to derivatives of a subclass of triterpenoid acids that have multi-medicament properties, that is derivatives of the lupane, betulinic acid, formulations containing such, and their use to prevent or treat certain diseases, and preferably to derivatives or analogues of betulinic acid, that have the following structural formula (1): ##STR1## wherein: Y is OR.sup.1, NR.sup.1.sub.2, O.sup.- M.sup.1 ;R.sup.1 is H, LOWER ALKYL,M.sup.1 is Na.sup.+, K.sup.+, Mg.sup.++, Ca.sup.++ ions;each R.sup.2 is independently CH.sub.2 OR.sub.1 or CH.sub.3 ;each R.sup.3 is independently H, CH.sub.3, lower alkyl, COY, CH.sub.2 OH, CH.sub.2 OCH.sub.2 CH=CH.sub.2, CH.sub.2 OSO.sub.3.sup.- M.sup.1 ;each Z is independently NHR.sup.1.sub.2, NR.sup.1 Ac, NR.sup.1 Bz, H, OCH.sub.3, lower alkyl, OH, OSO.sub.3.sup.- M.sup.1, OCH.sub.2 CH=CH.sub.2, OCH.sub.2 CO.sub.2 H or O-glucoside;each X is independently O, S, NR.sup.1 or NR.sub.2.sup.
    Type: Grant
    Filed: August 9, 1993
    Date of Patent: July 1, 1997
    Assignee: Glycomed Incorporated
    Inventors: Mark Brian Anderson, John Henry Musser
  • Patent number: 5635156
    Abstract: The present invention relates to non-lethal methods of conditioning a recipient for bone marrow transplantation. In particular, it relates to the use of nonlethal doses of total body irradiation, total lymphoid irradiation cell type-specific antibodies, especially antibodies directed to bone marrow stromal cell markers, cytotoxic drugs, or a combination thereof. The methods of the invention have a wide range of applications, including, but not limited to, the conditioning of an individual for hematopoietic reconstitution by bone marrow transplantation for the treatment of hematologic malignancies, hematologic disorders, autoimmunity, infectious diseases such as acquired immunodeficiency syndrome, and the engraftment of bone marrow cells to induce tolerance for solid organ, tissue and cellular transplantation.
    Type: Grant
    Filed: November 14, 1994
    Date of Patent: June 3, 1997
    Assignee: University of Pittsburgh
    Inventor: Suzanne T. Ildstad
  • Patent number: 5632968
    Abstract: This invention relates to reagents and methods for detecting and imaging cardiovascular lesions such as atherosclerotic plaques, vascular clots including thrombi and emboli, myocardial infarction, and other organ infarcts. Monospecific antibody imaging agent conjugates specific for one type of leukocyte, as well as multispecific antibody imaging agent conjugates specific for at least one type of leukocyte and for antigens associated with fibrin, myosin or platelets, are used in the present invention. Multispecific antibody imaging agent conjugates specific for at least two different antigens selected from the group consisting of fibrin-, myosin- and platelet associated antigens are also provided.
    Type: Grant
    Filed: November 9, 1994
    Date of Patent: May 27, 1997
    Assignee: Immunomedics, Inc.
    Inventor: David M. Goldenberg
  • Patent number: 5625075
    Abstract: The present invention provides metal chelating compounds, to chelates and chelate-targeting agent conjugates formed from the chelating compounds, and to methods for making and using these compositions. The chelating compounds incorporate two nitrogen atoms and three sulfur atoms ("N.sub.2 S.sub.3 "), two nitrogen atoms and four sulfur atoms ("N.sub.2 S.sub.4 "), or three nitrogen atoms and three sulfur atoms ("N.sub.3 S.sub.3 "). Metals, and metal oxides, capable of being chelated by the compounds include those that are radionuclides, such as .sup.99m Tc and .sup.186/188 Re.The targeting agent portion of the chelate-targeting agent conjugates provided includes antibodies, peptides, hormones, enzymes and biological response modifiers. Methods for making the conjugates are provided and encompass the addition of a metal, or metal oxide, to a chelating compound prior to attachment to a targeting agent as well as subsequent to the attachment.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: April 29, 1997
    Assignee: NeoRx Corporation
    Inventors: Ananthachari Srinivasan, Alan R. Fritzberg, David S. Jones
  • Patent number: 5622685
    Abstract: Tumor-active or tumor-diagnostic substances having preferred accumulation in the tumor, which are characterized in that they haveat least two phenolic hydroxyl and/or amino groups,at least one aliphatic amino group, orat least one phenolic hydroxyl and/or amino group andat least one aliphatic amino groupand that these groups are substituted with polyethylene glycol chains whose polymerization degree n is 5 to 250 and whose terminal hydroxyl group is substituted by C.sub.1 -C.sub.12 alkyl ester or ether, each of the substances being substituted by at least two such polyethylene glycol chains.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 22, 1997
    Assignee: Deutches Krebsforchunszentrum Stiftung des Offentlichen Rechts
    Inventors: Hans J. Sinn, Hans-Hermann Schrenk, Wolfgang Maier-Borst, Eckhard Friedrich, Georgi Graschew, Dieter Wohrle, Thomas Klenner
  • Patent number: 5612016
    Abstract: Provided are conjugates useful in cancer, cardiovascular or infectious disease detection and/or therapy. The conjugate is of a ligand and protein. The ligand has a moiety capable of binding to mercapto groups and is capable of chelating a metal useful for detection or therapy. The protein reacts with a substance associated with a targeted cell, pathologic lesion or pathogen. The protein prior to conjugation has at least one mercapto group which becomes a site for conjugation to the ligand. Also provided are metal chelates of the conjugate, methods of detection and therapy, methods for producing the conjugate and pharmaceuticals compositions of the conjugates.
    Type: Grant
    Filed: March 29, 1993
    Date of Patent: March 18, 1997
    Assignee: Immunomedics, Inc.
    Inventors: Gary L. Griffiths, Habibe Diril, Hans J. Hansen
  • Patent number: 5612017
    Abstract: A method for performing boron neutron capture therapy for the treatment of tumors is disclosed. The method includes administering to a patient an iodinated sulfidohydroborane, a boron-10-containing compound. The site of the tumor is localized by visualizing the increased concentration of the iodine labelled compound at the tumor. The targeted tumor is then irradiated with a beam of neutrons having an energy distribution effective for neutron capture. Destruction of the tumor occurs due to high LET particle irradiation of the tissue secondary to the incident neutrons being captured by the boron-10 nuclei. Iodinated sulfidohydroboranes are disclosed which are especially suitable for the method of the invention. In a preferred embodiment, a compound having the formula Na.sub.4 B.sub.12 I.sub.11 SSB.sub.12 I.sub.11, or another pharmaceutically acceptable salt of the compound, may be administered to a cancer patient for boron neutron capture therapy.
    Type: Grant
    Filed: April 24, 1995
    Date of Patent: March 18, 1997
    Assignee: Associated Universities, Inc.
    Inventors: Michiko Miura, Daniel N. Slatkin
  • Patent number: 5609848
    Abstract: Haloaryl compounds are lithiated and thereafter metalated with one of the following organometallic groups: Sn(n--Bu).sub.3 or SnMe.sub.3. The resulting aryltin compound can be transmetalated in site-specific reaction with one of the following organometallic groups: HgX, Hg(OAc).sub.2, BX.sub.3, or BZ.sub.2, wherein X is Cl, Br, or I, and Z is alkyl or alkoxy. The metalated compounds are subsequently radiohalogenated via a demetalation reaction. A functional group suitable for conjugation to protein can be added subsequent or preferably prior to the radiohalogenation.Also compounds of the formula: R.sub.1 --Ar--R.sub.2, wherein R.sub.1 is either a radiohalogen or any one of the organometallic groups stated above, Ar is aromatic or heteroaromatic ring, and R.sub.2 is a short-chain substituent that does not activate the aromatic ring and that bears a functional group, or a precursor thereof, suitable for conjugation to protein under conditions that preserve the biological activity of the protein.
    Type: Grant
    Filed: September 23, 1991
    Date of Patent: March 11, 1997
    Assignee: NeoRx Corporation
    Inventors: D. Scott Wilbur, Alan R. Fritzberg
  • Patent number: 5609846
    Abstract: Anticancer, antimicrobial and autoimmune disease, and anti-organ rejection therapy using cytotoxic agents is improved using cytokines to prevent, mitigate or reverse adverse radiation-induced or drug-induced toxicity, especially to hematopoietic cells. Cytotoxic agents can include radioisotopes, drugs, toxins and even unconjugated cytotoxic antibodies. A preferred cytokine is IL-1. Higher doses of cytotoxic agents can be administered and tolerated by the patient and dose-limiting marrow toxicity can be prevented, palliated or reversed using adjunct cytokine therapy.
    Type: Grant
    Filed: March 27, 1995
    Date of Patent: March 11, 1997
    Assignee: Immunomedics, Inc.
    Inventor: Milton D. Goldenberg
  • Patent number: 5609849
    Abstract: Compounds such as 4-(s'-methoxy)phenyl-[2'-N-2"-pyridinyl)-p-iodobenzamido]ethylpiperazine have affinity and specificity for serotonin 5-HT.sub.1A receptors.
    Type: Grant
    Filed: March 11, 1994
    Date of Patent: March 11, 1997
    Assignee: The Trustees of the University of Pennsylvania
    Inventor: Hank F. Kung
  • Patent number: 5607659
    Abstract: The present invention provides methods for directing the biodistribution of molecules that are not generally specifically excreted via the renal pathway to renal excretion. The methods employ conjugates or complexes containing a directed biodistribution molecule (DBM) and one or more bound molecules, wherein the biodistribution of the conjugate or complex is directed to renal excretion in vivo by the DBM component thereof.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 4, 1997
    Assignee: NeoRx Corporation
    Inventors: Linda M. Gustavson, Alan R. Fritzberg
  • Patent number: 5602236
    Abstract: Metal-containing steroid mimic complexes are provided. Compositions containing a metal ion incorporated into a steroid skeleton structure and ligands useful in the preparation of such compositions are also provided. The metal ion is preferably a radionuclide, such as technetium, rhenium or gallium. Methods for using the metal complexes for diagnostic and therapeutic purposes are further provided.
    Type: Grant
    Filed: April 8, 1994
    Date of Patent: February 11, 1997
    Assignee: Mallinckrodt Medical, Inc.
    Inventor: Raghavan Rajagopalan
  • Patent number: 5595721
    Abstract: Methods for the treatment of lymphoma by adminstration of a B cell-specific antibody are described. The invention encompasses providing to a patient both unlabeled antibodies and antibodies labeled with a radioisotope. A principal advantage of the method is that tumor responses can be obtained in a radiometric dose range that does not require hematopoietic stem cell replacement as an adjunct therapy.
    Type: Grant
    Filed: September 16, 1993
    Date of Patent: January 21, 1997
    Assignee: Coulter Pharmaceutical, Inc.
    Inventors: Mark S. Kaminski, Gregory M. Butchko, Stephan D. Glenn, Richard L. Wahl
  • Patent number: 5589576
    Abstract: Novel complexes of technetium (.sup.99 Tc or .sup.99m Tc) which contain the moiety Tc.dbd.NR, Tc--N.dbd.NY or Tc(--N.dbd.NY).sub.2, and a ligand which confers biological target-seeking properties on the complex, wherein R represents an aryl group, a substituted or unsubstituted alkyl group, or the grouping .dbd.NR.sup.1 R.sup.2 ; Y represents an aryl group or a substituted or unsubstituted alkyl group; and R.sup.1 and R.sup.2 are hydrogen, aryl groups or substituted or unsubstituted aliphatic or cyclic alkyl groups, and may be both the same or different, provided that both are not hydrogen. The complexes are suitable for use in radiopharmaceuticals for a variety of clinical applications. Methods for the preparation of these technetium complexes are also described.
    Type: Grant
    Filed: August 12, 1994
    Date of Patent: December 31, 1996
    Assignee: Amersham International plc
    Inventors: Colin M. Archer, Jonathan R. Dilworth, Panna Jobanputra, Ian A. Latham, Russell M. Thompson