Abstract: The invention provides derivatives of 5-arylsulfonyl indole and 5-arylsulfonyl indoline compounds which may be in the form of pharmaceutical acceptable salts or compositions that are useful in treating central nervous system diseases such as anxiety and depression. The invention also includes intermediates and processes to make the compounds, isotopically-labeled forms of the compounds and the use of the isotopically labeled forms of the compounds to perform nuclear magnetic resonance imaging and positron emission tomography.
Abstract: This invention relates to new macrocyclic chelants and metal chelates thereof, methods of preparing the chelants and metal chelates, and pharmaceutical compositions comprising the macrocyclic chelants and metal chelates. This invention relates particularly to the use of the new metal chelates as contrast agents in X-ray or CT, MRI imaging, and radiopharmaceuticals for the diagnosis of cardiovascular disorders, infectious disease and cancer. This invention also relates to new bifunctional chelants (BFCs) for attaching diagnostic metals and therapeutic isotopes to target-specific biomolecules such as proteins, peptides, peptidomimetics, and non-peptide receptor ligands. In addition, the macrocyclic chelants are useful for heavy metal detoxification.
Abstract: Radiolabeled epidermal growth factor receptor tyrosine kinase (EGFR-TK) irreversible inhibitors and their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) and as radiopharmaceuticals for radiotherapy are disclosed.
Type:
Grant
Filed:
March 12, 2001
Date of Patent:
May 13, 2003
Assignees:
Yissum Research Development Company of the Hebrew University
of Jerusalem, Hadasit Medical Research Services and Development Ltd.
Abstract: A novel means of pharmaceutical delivery for therapy or prophylaxis or to assist surgical or diagnostic operations on the living body is provided by agents which undergo neuronal endocytosis and axonal transport following pharmaceutical administration into vascularized, peripherally innervated tissue, e.g., intramuscular injections of a nerve adhesion molecule comprising a physiologically active substance or a diagnostic marker.
Abstract: A cosmetic composition having improved transfer resistance comprising:
a) from about 0.1-60% by weight of trimethylated silica,
b) from about 0.1-60% by weight of a volatile solvent having a viscosity of 0.5 to 100 centipoise at 25° C.,
c) 0.1-60% by weight of a nonvolatile oil having a viscosity of 200 to 1,000,000 centipoise at 25° C.
d) 0.1-80% of a cosmetically acceptable carrier.
Type:
Grant
Filed:
June 25, 2002
Date of Patent:
May 13, 2003
Assignee:
Revlon Consumer Products Corporation
Inventors:
Hernando Brieva, Julio Gans Russ, Ida Marie Sandewicz
Abstract: The present invention describes novel compounds of the formula:
(Q)d—Ln—Ch,
useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention further provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia and myocardial reperfusion injury. The present invention still further provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.
Type:
Grant
Filed:
December 17, 1999
Date of Patent:
May 6, 2003
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Edward H. Cheesman, Michael Sworin, Milind Rajopadhye
Abstract: The present invention is directed to methods for treating cancer wherein more than one therapeutic agent is used, with each of the therapeutic agents having different tumor-killing capabilities, and wherein the therapeutic agents are delivered to the tumor sites using combined targeting and pre-targeting methods. The methods of the present invention achieve good tumor to non-tumor ratios of the therapeutic agents, and are effective for cancer therapy.
Type:
Grant
Filed:
June 20, 2000
Date of Patent:
May 6, 2003
Assignee:
Immunomedics, Inc.
Inventors:
Gary L. Griffiths, Hans J. Hansen, David M. Goldenberg
Abstract: The invention features a method for treating obesity in a patient by administering to the patient a polymer that has been substituted with one or more groups that inhibit lipases, which are enzymes responsible for the hydrolysis of fat. The invention further relates to the polymers employed in the methods described herein as well as novel intermediates and methods for preparing the polymers.
Type:
Grant
Filed:
November 16, 2000
Date of Patent:
May 6, 2003
Assignee:
GelTex Pharmaceuticals, Inc.
Inventors:
W. Harry Mandeville, III, Molly Kate Boie, Venkata R. Garigapati
Abstract: A method for improving cellular gallium uptake (particularly of tumor cells) by exposing cells to a nifedipine photodegradation product, or an analog thereof. In particular embodiments, the gallium uptake enhancer is selected from the group of A-B and formula (I), wherein A is a pyridine and B is a nitrosophenyl, and n=1-10. In yet other embodiments, the uptake enhancer is formula (II), wherein R1-9 are independently selected from the group consisting of H, halogen, haloalkyl, NO2, NO, SO2, a C1-6 alkyl, a COOR10 wherein R10 is H or C1-6 alkyl, and an —OR11 wherein R11 is H or C1-6 alkyl; wherein at least one of R5 and R7 is NO. The uptake enhancers are particularly useful in imaging tumors, using such techniques as gallium scanning, in which the dose of the gallium isotope can be decreased or its imaging efficiency improved.
Type:
Grant
Filed:
October 6, 2000
Date of Patent:
May 6, 2003
Assignee:
Oregon Health and Science University
Inventors:
Kathryn A. Morton, Jean-Baptiste Roullet
Abstract: Tuftsin receptor-specific peptides, peptidomimetics and peptide-like constructs are provided, particularly for use in biological, pharmaceutical and radiopharmaceutical applications, in which the peptide, peptidomimetic or construct is conformationally fixed on complexation of the metal ion-binding portion thereof with a metal ion, resulting in a peptide, peptidomimetic or construct with increased affinity for the tuftsin receptor.
Abstract: Radiopharmaceutical compounds are disclosed. A tropane compound is linked through the N atom at the 8-position to a chelating ligand capable of complexing technetium or rhenium to produce a neutral labeled complex that selectively binds to the dopamine transporter over the serotonin transporter with a ratio of 10 or more. These compounds can be prepared as separate diastereoisomers as well as a mixture of diastereoisomers. Also disclosed are radiopharmaceutical kits for preparing the labeled radiopharmaceutical compounds.
Type:
Grant
Filed:
May 10, 2000
Date of Patent:
April 15, 2003
Assignees:
Organix, Inc., President and Fellow of Harvard College, The General Hospital Corporation
Inventors:
Peter C. Meltzer, Paul Blundell, Bertha K. Madras, Alan J. Fischman, Alun G. Jones, Ashfaq Mahmood
Abstract: The present invention relates to a method of contrast enhanced ultrasonic diagnostic imaging comprising administering to a subject a contrast enhancing amount of spherical particles comprising a matrix enclosing a gaseous contrast agent which reflects sound waves, said matrix being a biocompatible, biodegradable, non-immunogenic non-polyamino acid synthetic polymer; and generating an ultrasonic image of said subject. The polymer may be selected from the group consisting of carbohydrates, carbohydrate derivatives and non-polyamino acid synthetic polymers.
Abstract: There are provided compositions which include a retinoid and preferably retinol; a dermatologically active acid; and a volatile base, such as ammonium hydroxide. Another embodiment of the invention includes compositions comprising a retinoid and preferably retinol; a dermatologically active acid; a volatile base; and a second neutralizing agent. There are also provided compositions which include a retinoid, a neutralized ammonium salt of a dermatologically active acid, and optionally a neutralized salt, other than ammonium salt, of an acid. Further provided are methods for reducing fine lines, wrinkles, skin roughness, and pore size and for increasing the clarity of a skin surface, cellular turnover, skin radiance, skin smoothness, skin permeation or collagen synthesis in a mammal in need thereof. Compositions as described above are administered topically to the skin of the animal.
Type:
Grant
Filed:
November 9, 1999
Date of Patent:
April 8, 2003
Assignee:
Johnson & Johnson Products, Inc.
Inventors:
Curtis A. Cole, Laura E. Flack, Claudia Kaminski, Victoria Van Leeuwen
Abstract: Improved methods for detecting lesions in dense breast tissue are disclosed. The methods of the invention generally feature administration to a subject of an LHRH antagonist in an amount and for a period of time sufficient to reduce the density of breast tissue prior to generating an image of the breast tissue, for example by mammography, to detect a lesion in the breast tissue. Packaged formulations for reducing breast density in a subject prior to generating an image of the subject's breast tissue, comprising an LHRH antagonist packaged with instructions for using the LHRH antagonist to reduce breast density in a subject prior to imaging the breast tissue, are also disclosed.
Abstract: Kits for detecting and treating endometriosis are provided, which contain a targeting molecule comprising an eosinophil peroxidase-binding component. Methods of detecting and treating endometriosis using eosinophil peroxidase-specific targeting molecules are also provided Targeting molecules comprise an eosinophil peroxidase-binding component and an accessory component; the accessory component comprising an agent conferring detectability or a therapeutic effect.
Type:
Grant
Filed:
March 31, 2000
Date of Patent:
April 1, 2003
Assignee:
Center for Molecular Medicine and Immunology
Inventors:
Rosalyn D. Blumenthal, David M. Goldenberg, Michael Samoszuk
Abstract: Intestinal radiation injury (radiation enteropathy) is an important dose limiting factor during treatment of abdominal and pelvic tumors and a major determinant in the quality of life among cancer survivors. Inflammatory and fibrogenic mediators released by mucosal inflammatory cells are involved in the mechanisms of injury. Treatment with Orazipone decreases the toxicity following Gy radiation dose, as measured by histopathologic scoring, TGF-&bgr;, IL-1&agr;, and ED-2 macrophage antigen immunoreactivity.
Type:
Grant
Filed:
September 23, 1998
Date of Patent:
April 1, 2003
Assignee:
The Board of Trustees of the University of Arkansas
Abstract: The present invention relates to methods for identifying inhibitors of the bitter taste response, and by methods of using such inhibitors to either block the perception of bitterness and/or promote the perception of a sweet taste. The inhibitors of the invention may be used as flavor enhancers in foods and pharmaceuticals. The methods of the invention may further be used to characterize the gustatory perception of novel tastants.
Type:
Grant
Filed:
December 22, 1999
Date of Patent:
April 1, 2003
Assignee:
Mount Sinai School of Medicine of New York University
Abstract: The present invention describes novel compounds of the formula:
(Q)d—Ln—Ch,
useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.
Type:
Grant
Filed:
June 21, 2000
Date of Patent:
March 25, 2003
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Milind Rajopadhye, D. Scott Edwards, John A. Barrett, Alan P. Carpenter, Jr., Thomas D. Harris, Stuart J. Heminway, Shuang Liu, Prahlad R. Singh
Abstract: In a method for characterizing the angiogenesis status of a tumor in a living subject, timed magnetic resonance images of the subject into whom a reptating polymer contrast agent containing chelating diethylentriaminepentacetic acid dosed with gadolinum has been introduced are obtained. At least two images taken at different times are compared in order to determine the percentage image enhancement in a tumor region of interest. A contrast agent including a reptating polymer containing technetium-99 is used with a nuclear medicine version of this technique.