Benzene Ring Containing Patents (Class 514/576)
  • Patent number: 6706290
    Abstract: Nanobacteria contribute to pathological calcification in the human and animal body, including diseases such as kidney stones, salivary gland stones, dental pulp stones and atherosclerosis. The present invention provides methods for sterilizing articles contaminated with nanobacteria. The present invention also provides methods of treating patients infected with nanobacteria. In particular, the present invention provides a method for preventing the recurrence of kidney stones in a patient that has suffered from kidney stones, comprising administration of an antibiotic, a bisphosphonate, or a calcium chelator, either alone or in combination, in an amount effective to inhibit or prevent the growth and development of nanobacteria.
    Type: Grant
    Filed: July 2, 1999
    Date of Patent: March 16, 2004
    Inventors: Olvai E. Kajander, Neva Ciftcioglu
  • Patent number: 6699510
    Abstract: The mastitis control teat dip composition having a visible indicator aspect of the invention provides a softening, soothing, smoothing, relaxing property, a rapid initial kill, a useful highly pseudoplastic rheology, a barrier/film-forming capacity, a unique antimicrobial composition that is stable over an extended period of time, and unexpected long term microbial control when compared to the prior art materials disclosed in patents and used in the marketplace. The indicator aspect provides ease of visually detecting the material on the animal skin and can indicate efficacy of the material. The compositions of the invention are made by combining an aqueous liquid composition containing the visual indicator combined with the organic components which can be combined with a simple aqueous solution of a salt of chlorous acid, preferably an alkali metal chlorite.
    Type: Grant
    Filed: August 19, 2002
    Date of Patent: March 2, 2004
    Assignee: Ecolab Inc.
    Inventors: David D. McSherry, Francis L. Richter
  • Patent number: 6683069
    Abstract: Exposure of human skin to ultraviolet (UV) radiation from the sun not only induces the production of enzymes (matrix metalloproteinases) that degrade collagen, but also inhibits the synthesis of new collagen by inhibiting the synthesis of procollagen. This UV-induced inhibition of the synthesis of collagen can be prevented by the topical application of a retinoid or c-JUN inhibitor to the skin prior to its exposure to UV radiation.
    Type: Grant
    Filed: April 2, 1999
    Date of Patent: January 27, 2004
    Assignee: Regents of the University of Michigan
    Inventors: Gary J. Fisher, John J. Voorhees
  • Patent number: 6656967
    Abstract: The invention provides fungicidal compounds of formula I and salts thereof: wherein the various radicals and substituents are as defined in the description, fungicidal compositions containing them and method for combating fungi which comprises applying these.
    Type: Grant
    Filed: August 6, 2001
    Date of Patent: December 2, 2003
    Assignee: Bayer Cropscience SA
    Inventors: Vincent Gerusz, Darren James Mansfield, Joseph Perez, Jean-Pierre Vors
  • Patent number: 6653321
    Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.
    Type: Grant
    Filed: July 28, 2000
    Date of Patent: November 25, 2003
    Assignee: Telik, Inc.
    Inventors: Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum, Louise Robinson, Jeong Weon Park
  • Patent number: 6642260
    Abstract: The present invention provides a compound containing at least one sulfhydryl group and at least one NO donor group, wherein said compound contains one or more protected sulfhydryl groups linked to at least one aromatic ring or a heteroaromatic ring with a nitrogen in the ring structure, which ring is substituted by one or more substitutes bearing at least one terminal —ONO2 group. The present invention further provides pharmaceutical compositions comprising one or more of said compounds as an active ingredient.
    Type: Grant
    Filed: January 9, 2002
    Date of Patent: November 4, 2003
    Assignee: Yissum Research Development Company of The Hebrew University of Jerusalem
    Inventor: Abdullah Haj-Yehia
  • Patent number: 6635678
    Abstract: Fecal incontinence and anal itch can be treated by administration, more particularly by local application to the anus, of an a adrenergic blocker, nitric oxide synthase inhibitor, prostaglandin F2&agr;, dopamine, morphine, &bgr;-blockers, and 5-Hydroxytryptamine. The patients who benefit most from the invention are those who have a normal or low maximum anal resting pressure and a structurally intact internal anal sphincter muscle, and patients who have had major bowel resection and reanastomisis.
    Type: Grant
    Filed: August 24, 1999
    Date of Patent: October 21, 2003
    Assignee: S.L.A. Pharma AG
    Inventors: Michael A. Kamm, Robin K. S. Phillips
  • Patent number: 6630516
    Abstract: The deleterious effects of the passage of time on human skin (i.e., chronological aging of human skin) can be prevented and treated with the topical application of a retinoid, preferably retinol. We have found that some of the same pathways (namely the stress-activated pathways, SAPs) activated in photoaging of human skin (i.e., sun-induced premature skin aging) are similarly elevated in the skin of elderly people. We have also found that other pathways (namely the mitogen-activated ERK pathway) is depressed in the same skin. Treatment of chronologically-aged skin with a non-retinoid MMP inhibitor and optionally a retinoid both inhibits degradation of dermal collagen and promotes procollagen synthesis. Biopsied sections from skin of elderly (80+ years old) show that a single treatment can increase epidermal thickness, improve the dermal collagen density, and promote the formation of rete pegs and dermal papillae (see FIG.
    Type: Grant
    Filed: February 24, 1998
    Date of Patent: October 7, 2003
    Assignee: The Regents of the University of Michigan
    Inventors: James Varani, Gary J. Fisher, John J. Voorhees, Sewon Kang
  • Patent number: 6599941
    Abstract: A non-toxic, environmentally safe and easily employable insecticide and insect repellent is achieved by providing an aqueous composition incorporating ethanolamine based compounds, either independently or in combination with the ethanolamine based compounds being selected from both simple compounds and conjugated compounds. In one preferred embodiment, a highly effective composition is attained for safe, effective, direct topical application to humans and animals by employing between about 10% and 70% by volume of the entire composition of the ethanolamine-based compound. In alternate preferred embodiments, the insecticide is formulated for application to plants, trees, crops, and other vegetation to provide a composition which effectively controls bothersome insects, while being completely safe and non-injurious to the plant, tree, or crop, as well as to the flowers or fruit thereof.
    Type: Grant
    Filed: July 17, 2000
    Date of Patent: July 29, 2003
    Inventors: Lynn Sue James, Michael A. Siedman
  • Patent number: 6552085
    Abstract: The use of isolated or purified stilbenoid compounds including longistyline A-2-carboxylic acid as hypoglycemic agents or to lower serum glucose levels is described. The invention also relates to the use of such stibenoid compounds in combination with other hypoglycemic agents.
    Type: Grant
    Filed: August 2, 2001
    Date of Patent: April 22, 2003
    Assignee: Insmed Incorporated
    Inventors: Wayne D. Inman, David C. Hopp
  • Patent number: 6545050
    Abstract: The present invention relates to novel amino acid esters of arylsulphonamides and analogues, to processes for their preparation and to their use for the prophylaxis and treatment of neurodegenerative disorders, in particular for the treatment of cerebral apoplexy, craniocerebral trauma, pain and spasticity.
    Type: Grant
    Filed: February 16, 2001
    Date of Patent: April 8, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Joachim Mittendorf, Jürgen Dressel, Michael Matzke, Jörg Keldenich, Frank Mauler, Jean-Marie-Viktor de Vry, Jürgen Franz, Peter Spreyer, Verena Vöhringer, Joachim Schumacher, Michael-Harold Rock, Ervin Horvàth, Arno Friedl
  • Patent number: 6541522
    Abstract: The use of isolated or purified stilbenoid compounds including longistyline A-2-carboxylic acid as a dietary supplement to mammals suffering from elevated triglyceride levels is described. The invention also relates to the use of such stibenoid compounds in combination with other hypotriglyceridemic agents.
    Type: Grant
    Filed: August 2, 2001
    Date of Patent: April 1, 2003
    Assignee: Insmed Incorporated
    Inventors: Wayne D. Inman, David C. Hopp
  • Patent number: 6537991
    Abstract: The invention provides methods for treating and preventing neuropathic pain which comprise the administration of an effective amount of an antagonist of the pain-enhancing effects of E-type prostaglandins, for example, EP1-typo prostaglandin receptor antagonists, to warm-blooded animals including humans in need of such treatment. The invention also provides pharmaceutical compositions for such prevention and treatment of neuropathic pain.
    Type: Grant
    Filed: November 15, 2001
    Date of Patent: March 25, 2003
    Assignee: AstraZeneca AB
    Inventors: John S Shaw, William Bastain
  • Patent number: 6524624
    Abstract: A two-part disinfecting systems, as well as disinfecting compositions and methods for making and using the same. The two-part disinfecting system contains a first part and a second part adapted to be mixed to yield an aqueous disinfecting composition, wherein the first part comprises a chlorite and the second part comprises an acid and an optional oxidizable colorant, and wherein the first part, the second part, or both the first and second parts comprise an alpha olefin sulfonate.
    Type: Grant
    Filed: May 16, 2001
    Date of Patent: February 25, 2003
    Assignee: Alcide Corporation
    Inventors: Joseph Morelli, C. Cayce Warf, Jr., Maura Aldrich, Cecilia Moser Morse, Jean Wiley
  • Patent number: 6521666
    Abstract: The present invention relates to a pharmaceutical composition comprising as an active ingredient a compound of formula (I), wherein Ring A is an aromatic or a heterocyclic ring; Q is a bond, carbonyl, lower alkylene, lower alkenylene, —O-(lower alkylene)-, etc.; n is 0, 1 or 2; Z is oxygen or sulfur, W is oxygen, sulfur, —CH═CH—, —NH— or —N═CH—; R1, R2 and R3 are the same or different and are hydrogen, halogen, hydroxyl, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, etc.; R4 is tetrazolyl, carboxyl group, amide or ester; R5 is hydrogen, nitro, amino, hydroxyl, lower alkanoyl, lower alkyl etc.; R6 is selected from (a) a substituted or unsubstituted phenyl group, (b) a substituted or unsubstituted pyridyl group, (c) a substituted or unsubstituted thienyl group, (d) a substituted or unsubstituted benzofuranyl group, etc.
    Type: Grant
    Filed: July 19, 2000
    Date of Patent: February 18, 2003
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Ila Sircar, Kristjan S. Gudmundsson, Richard Martin
  • Patent number: 6492424
    Abstract: Novel glucocorticoid and thyroid receptor ligands as provided which have the general formula (I): in which R1 is an aliphatic hydrocarbon, an aromatic hydrocarbon, carboxylic acid or ester thereof, alkenyl carboxylic acid or ester thereof, hydroxy, halogen, or cyano, or a pharmaceutically acceptable salt thereof. R2 and R3 are the same or different, and are hydrogen, halogen, alkyl of 1 to 4 carbons, or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen. X is carbonyl or methylene. R4 is an aliphatic, aromatic or heteroaromatic. Y is hydroxyl, methoxy, amino, or alkyl amino. n is an integer from 0 to 4. A method for treating diseases associated with metabolism dysfunction or which are dependent on the expression of a glucocorticoid or thyroid receptor gene such as diabetes, hypercholesterolemia, or obesity using these compounds is also disclosed.
    Type: Grant
    Filed: April 9, 2001
    Date of Patent: December 10, 2002
    Assignee: Karo Bio AB
    Inventors: Theresa Apelqvist, Patrick Goede, Erik Holmgren
  • Patent number: 6482860
    Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents.
    Type: Grant
    Filed: July 18, 1997
    Date of Patent: November 19, 2002
    Assignee: Tularik Inc.
    Inventors: John A. Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
  • Patent number: 6479551
    Abstract: The invention is directed to pharmaceutical compositions useful in the treatment of migraine. The compositions contain metoclopramide and one or more NSAIDs in unit dosage form. By selecting NSAIDs that are non-acidic or segregating the metoclopramide and NSAID, the storage life of the compositions has been increased. Also disclosed are coordinated dosage forms for the sequential release of drugs. The invention encompasses methods of treating migraine using any of these dosage forms.
    Type: Grant
    Filed: March 3, 2000
    Date of Patent: November 12, 2002
    Assignee: Pozen Inc.
    Inventors: John R. Plachetka, Zakauddin T. Chowhan
  • Patent number: 6478946
    Abstract: A method of preparing organic acids (fulvic, humic, and ulmic) for use as an electrolyte for producing high ionizations of precious metals (such as silver) which entails leaching out the organic acid from its source, stabilizing the organic acid first with ascorbic acid followed by sodium benzoate, removing cations, and using the organic acid as an electrolyte. A precious metal (such as silver) is used as a sacrificial electrode in this electrolyte. A non-sacrificial electrode could either be the same precious metal or an inert non-precious metal (titanium or graphite carbons). If the same material is used for the non-sacrificial electrode as for the sacrificial electrode, the size of each electrode may be about the same. If different material is used for the non-sacrificial electrode, its size should be larger that of the sacrificial electrode. Current at about 2 or more volts is applied to the electrodes and the ionization process begins yielding high concentrations of ionized precious metals.
    Type: Grant
    Filed: March 7, 2001
    Date of Patent: November 12, 2002
    Assignee: The Chemins Company, Inc.
    Inventor: Kenneth D. Westwood
  • Patent number: 6455582
    Abstract: Sulfohydroxamic acid diarylamines of formula (I), in which the variables are as defined in the claims, are inhibitors of MEK and are effective in the treatment of proliferative diseases, cancer, stroke, heart failure, xenograft rejection, arthritis, cystic fibrosis, hepatomegaly, cardiomegaly, Alzheimer's disease, complications of diabetes, septic shock, and viral infection.
    Type: Grant
    Filed: July 11, 2001
    Date of Patent: September 24, 2002
    Assignee: Warner-Lambert Company
    Inventor: Haile Tecle
  • Patent number: 6436444
    Abstract: The mastitis control teat dip composition of the invention provides rapid initial kill, a useful highly pseudoplastic rheology, a barrier/film-forming capacity, a unique antimicrobial composition that is stable over an extended period of time, and unexpected long term microbial control when compared to the prior art materials disclosed in patents and used in the marketplace. The compositions of the invention are made by combining an aqueous thickened liquid composition containing the organic components which can be combined with a simple aqueous solution of a salt of chlorous acid, preferably an alkali metal chlorite. The materials can be combined, blended into a smooth viscous material and can be immediately contacted with the target animals. The .compositions of the invention provide rapid initial kill, consistent long term kill and chemical and rheological stability.
    Type: Grant
    Filed: September 26, 1997
    Date of Patent: August 20, 2002
    Assignee: Ecolab Inc.
    Inventors: Francis L. Richter, Cathy M. Paquette, Richard K. Staub
  • Patent number: 6428772
    Abstract: A composition for topical aerosol application contains, by weight, a) about 20 to 90% of an active mixture in the form of a solution, gel or lotion with salicylic acid or benzoyl peroxide as active ingredient, and optionally, a polymeric thickening agent for a gel or lotion, and b) about 10 to 80% of a propellant system which includes dimethyl ether. The composition has a temperature in the range of 3 to 25° C. when dispensed.
    Type: Grant
    Filed: June 25, 2001
    Date of Patent: August 6, 2002
    Assignee: Blistex Inc.
    Inventors: Mohinder Singh, Michael A. Wojcik
  • Patent number: 6420394
    Abstract: The present invention relates to a novel pharmaceutical formulation for the topical application of drugs, particularly non-steroidal anti-inflammatory drugs (NSAID's), comprising a therapeutically effective amount of a drug, sodium phosphate buffer, and, optionally, an alcoholic solvent. It has been found that by the addition of sodium phosphate buffer to such formulations, the permeation of the NSAID can be significantly improved.
    Type: Grant
    Filed: April 8, 1998
    Date of Patent: July 16, 2002
    Assignee: Roche Consumer Health (Worldwide) SA
    Inventor: Andreas Supersaxo
  • Patent number: 6410596
    Abstract: The use of isolated or purified stilbenoid compounds including longistyline A-2-carboxylic acid as hypoglycemic agents or to lower serum glucose levels is described. The invention also relates to the use of such stibenoid compounds in combination with other hypoglycemic agents.
    Type: Grant
    Filed: August 2, 2001
    Date of Patent: June 25, 2002
    Assignee: Insmed Incorporated
    Inventors: David C. Hopp, Wayne D. Inman
  • Patent number: 6410602
    Abstract: A method of increasing the volume, the total sperm count and the reproductive performance of semen from human and animal males, is described. The method comprises administration of an effective dosage of a human or veterinary preparation containing at least one type of xanthoplylls, such as astaxanthin, to said males. Preferably, the astaxanthin exists in a form esterified with fatty acids, e.g. in the form of algal meal produced by culturing of the alga Haematococcus sp. Further, the use of at least one type of xanthophylls, such as astaxanthin, for the preparation of a human or veterinary preparation for increasing the volume, the total sperm count and the reproductive performance of semen from human and animal males, is disclosed.
    Type: Grant
    Filed: June 6, 2000
    Date of Patent: June 25, 2002
    Assignee: Astacarotene AB
    Inventors: Ake Lignell, John Inborr, Curt Nicolin
  • Patent number: 6403627
    Abstract: Spin trapping compositions in general have now been discovered to be effective in treating a variety of disorders, including disorders such as those arising from ischemia, infection, inflammation, exposure to radiation or cytotoxic compounds, not just of the central and peripheral nervous systems but of peripheral organ disease having a wide variety of etiologies. In the preferred embodiment, the compositions for treating tissue damage from ischemia contain PBN, or active derivatives thereof, in a suitable pharmaceutical carrier for intravenous, oral, topical, or nasal/pulmonary administration. Other preferred spin-trapping agents include 5,5-dimethyl pyrroline N-oxide (DMPO), &agr;-(4-pyridyl-1-oxide)-N-tert-butylnitrone (POBN), and (TEMPO) and spin-trapping derivatives thereof. Examples of derivatives of PBN include halogenated derivatives, bifunctional derivatives, conjugates with drugs or targeting molecules, dimers and cyclodextran polymers of PBN.
    Type: Grant
    Filed: July 20, 1999
    Date of Patent: June 11, 2002
    Assignees: Oklahoma Medical Research Foundation, University of Kentucky Foundation
    Inventors: John M. Carney, Robert A. Floyd
  • Patent number: 6403647
    Abstract: The invention relates to novel compositions and to methods for the pulsed administration of compositions to a patient or to cells in vitro for the treatment of human blood disorders. Compositions contain chemical compounds that stimulate the expression of fetal hemoglobin and/or stimulate the proliferation of red blood cells, white blood cells and platelets in patients and ex vivo for reconstitution of hematopoiesis in vivo. These methods are useful to treat or prevent the symptoms associated with anemia, sickle cell disease, thalassemia and other blood disorders. The, invention also relates to methods for the pulsed administration of compositions to patients for the treatment and prevention of cell proliferative disorders including deficiencies such as cytopenia and malignancies such as viral-induced tumors, other forms of neoplasia and for expansion of cells for hematopoietic transplantation. Pulsed administration has been shown to be more effective than continuous therapy in patients tested.
    Type: Grant
    Filed: April 25, 2000
    Date of Patent: June 11, 2002
    Inventor: Susan P. Perrine
  • Patent number: 6387959
    Abstract: The invention relates to the field of antiviral agents, and more specifically to antiviral therapy. The invention provides use of at least one compound or mixture of compounds of the general formula or a functional equivalent or pharmaceutically acceptable salt, ester or hydrate thereof for the treatment of a viral infection.
    Type: Grant
    Filed: June 30, 2000
    Date of Patent: May 14, 2002
    Assignees: Universiteit Utrecht, Universitair Medisch Centrum Utrecht
    Inventor: Johannes Servatius Leonardus Maria Nottet
  • Patent number: 6383527
    Abstract: Preparations and extracts of valerian, as well as isovaleramide, isovaleric acid, and its pharmaceutically acceptable salts, esters, and substituted amides, and other valerian-related compounds, in combination with NSAIDs exhibit clinically significant pharmacological properties which implicate a treatment for acute muscular aches, strains, and sprains which occur from a localized, external insult to a particular muscle or muscle group outside of, or peripheral to, the CNS. The compositions in question generally are non-cytotoxic and do not elicit weakness or sedative activity at doses that are effective for the symptomatic treatment of such pathological conditions.
    Type: Grant
    Filed: February 22, 2001
    Date of Patent: May 7, 2002
    Assignee: NPS Pharmaceuticals, Inc.
    Inventors: Linda D. Artman, Manuel F. Balandrin
  • Patent number: 6369105
    Abstract: When used in admixture with mancozeb, chlorothalonil, a copper salt, folpet, fluazinam or cymoxanil (it being possible for the latter to be used also together with one of the other five components), metalaxyl having a high R-enantiomer content of more than 70% by weight, or pure R-metalaxyl, exhibits a markedly increased fungicidal action against plant diseases as compared with a similar mixture in which metalaxyl is used in the form of the racemate.
    Type: Grant
    Filed: August 29, 2000
    Date of Patent: April 9, 2002
    Assignee: Syngenta Investment Corporation
    Inventors: Cosima Nuninger, John Edward Nicholas Goggin, Dino Sozzi
  • Patent number: 6365625
    Abstract: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalenesulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.
    Type: Grant
    Filed: September 17, 1999
    Date of Patent: April 2, 2002
    Assignee: Procept, Inc.
    Inventors: Shyam K. Singh, Raymond J. Patch, Peter V. Pallai, Edith A. Neidhardt, Gerard P. Palace, Kevin J. Willis, Theresa M. Sampo, Kevin W. McDonald, Zhan Shi
  • Patent number: 6346279
    Abstract: An acidic aqueous hydrogen peroxid solution is provided, with improved disinfectant activity. Concentrated solutions preferably contain up to about 8% and as-used concentrations contain about 0.5% peroxide. The solution also contains from 0.1 to 5.0% of at least one acid compound, e.g. phosphoric and/or a phosphonate with from 1 to 5 phosphonic acid groups, and from 0.02 to 5% of at least one anionic surfactant. The surfactant is selected from C8 to C16-alkyl aryl sulphonic acids, sulphonated C12 to C22 carboxylic acids, C8 to C22-alkyl diphenyl oxide sulphonic acids, naphthalene sulphonic acids, C8 to C22 alkyl sulphonic acids, and alkali metal and ammonium salts thereof, and alkali metal C8 to C18 alkyl sulphates, and mixtures thereof. Most preferably the solution has an emulsifier, e.g. a salt of an alkylated diphenyl oxide. The solution may also contain corrosion inhibitors and/or lower alcohols.
    Type: Grant
    Filed: July 19, 1999
    Date of Patent: February 12, 2002
    Assignee: Virox Technologies, Inc.
    Inventor: Michael J. Rochon
  • Patent number: 6331555
    Abstract: The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity other members of the PDGF-R super family and are selective for members of the PDGF-R super family. The PDGF-R super family includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see FIG. 1a), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.
    Type: Grant
    Filed: July 27, 1999
    Date of Patent: December 18, 2001
    Assignees: University of California, Yissum Research Development Company of the Hebrew University of Jerusalem, Biosignal LTD, Sugen, Inc., Max-Planck-Gesellschaft zur Forderung der Wissenschaften E.V.
    Inventors: Klaus P. Hirth, Elaina Mann, Laura K. Shawyer, Axel Ullrich, Istvan Szekely, Tamas Bajor, Janis Haimichael, Laszlo Orfi, Alex Levitzki, Aviv Gazit, Peng Cho Tang, Reiner Lammers
  • Patent number: 6306900
    Abstract: This invention provides a pharmaceutical composition comprising a mycophenolate salt, the composition being adapted to release mycophenolate in the upper part of the intestinal tract.
    Type: Grant
    Filed: October 23, 2000
    Date of Patent: October 23, 2001
    Assignee: Novartis AG
    Inventors: Barbara Haeberlin, Ching-Pong Mak, Armin Meinzer, Jacky Vonderscher
  • Patent number: 6303145
    Abstract: A method and composition are disclosed utilizing the pure (S,R) isomer of formoterol, which is a bronchodilator with reduced adverse effects. (S,R)-Formoterol may be conveniently and safely formulated for aerosol administration.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: October 16, 2001
    Assignee: Sepracor Inc.
    Inventors: Thomas P. Jerussi, Chris Hugh Senanayake
  • Patent number: 6296881
    Abstract: Pathogenic bacteria have long posed a threat to mankind, and it has been a goal in the food industry and the medical profession to develop a bactericide that would have a high degree of practicality which included spores in its scope, that would exhibit a pronounced effect on pathogenic bacteria, that would be safe for humans and the earth, and that would be composed of metal ions having affinity with the body, that is, those which are essential structural components for the body, and compounds that are used in food additives. Provided are a bactericide containing ferric ions (Fe3+) and one or more members of the group consisting of sorbic acid, benzoic acid, and para-hydroxybenzoic acid esters; a bactericide containing ferric ions (Fe3+), L-ascorbic acid, and one or more members of the group consisting of sorbic acid, benzoic acid, and para-hydroxybenzoic acid esters; and a bactericide containing ferric ions (Fe3+), sorbic acid, benzoic acid, and L-ascorbic acid.
    Type: Grant
    Filed: August 3, 1999
    Date of Patent: October 2, 2001
    Assignee: Kenkohyakunijussai Co., Ltd.
    Inventors: Tadayo Hata, Toshiyuki Maruoka
  • Patent number: 6277874
    Abstract: Methods for treating diseases associated with toxicity of Apolipoprotein E (“apoE”). Specifically, the present invention relates to new methods for treating a mammal having a condition associated with toxicity of apolipoprotein E cleavage fragments containing residues 130-169, comprising administering to said mammal a pharmacologically effective amount of compound or a pharmaceutically acceptable sale, derivative or fragment thereof to interfere with the receptor-binding site associated with residues 130-169 of the apolipoprotein E molecule in said mammal.
    Type: Grant
    Filed: February 22, 1999
    Date of Patent: August 21, 2001
    Assignee: University of Cincinnati and Apologic, Incorporated
    Inventors: Keith A. Crutcher, Judith A. K. Harmony
  • Patent number: 6271245
    Abstract: The present invention relates to hydroxamic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.
    Type: Grant
    Filed: June 1, 1999
    Date of Patent: August 7, 2001
    Assignee: Guilford Pharmaceuticals, Inc.
    Inventors: Paul F. Jackson, Kevin L. Tays, Keith M. MacLin, Barbara S. Slusher
  • Patent number: 6265437
    Abstract: Derivatives of sulphonic aminoalkane acids, corresponding to formula (I) where X is  R1, R2 and R3 are selected from hydrogen and a C1-C7 alkyl radical, and A is a group of the formula (e) where v and w are 0, 1, 2 or a group of formula (f) where R5 and R6 are selected independently of each other from hydrogen, a C1-C7 alkyl radical, an aryl radical having between 6 and 14 carbon atoms and a heteroaryl radical; t is 1-3; R4 is selected from hydrogen, a C1-C7 alkyl radical, a CF3 radical, an aryl radical having between 6 and 14 carbon atoms and a heteroaryl radical; M is a monovalent metal (Na, K, Li) or a divalent metal (Ca, Mg, Sr, Zn); m is 1 or 2; p is 1-2 and q is 1-2; and where p and q are such that the electrical neutrality of the salt is ensured. The compounds can be used for the treatment of alcohol dependence.
    Type: Grant
    Filed: October 12, 2000
    Date of Patent: July 24, 2001
    Assignee: LIPHA
    Inventors: Jean-Jacques Berthelon, Philippe Durbin
  • Patent number: 6265613
    Abstract: Phenylacetic acid derivatives of the formula I where the substituents and the indexes have the meanings given in the specification, their salts, their preparation and their use.
    Type: Grant
    Filed: February 24, 1998
    Date of Patent: July 24, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Müller, Hubert Sauter, Herbert Bayer, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Klaus Oberdorf, Franz Röhl, Norbert Götz, Michael Rack, Ruth Müller, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Volker Harries
  • Patent number: 6251942
    Abstract: Composition and methods of alleviating impaired mental function and memory loss in mammals and reducing the recovery time from anaesthesia in age mammals, comprising treating the mammal with a non-toxic, enhancing effective amount of a cell membrane permeant calcium buffer. The buffer is preferably a calcium ion chelating agent having a KD selected from the range 1×10−4 to 1×10−8 Molar and being essentially calcium ion-selective over other metal ions. A most preferred buffer is BAPTA-AM.
    Type: Grant
    Filed: May 21, 1999
    Date of Patent: June 26, 2001
    Inventors: Peter Louis Carlen, Christopher George Janus, Hossam El-Beheiry
  • Patent number: 6248782
    Abstract: A therapeutic process for treating disease in mammals caused by retroviruses in which the infected mammal is treated with a ribonucleotide reductase inhibitor such as a polyhydroxy benzoic, mandelic or phenylacetic acid derivative, such as N,3,4-trihydroxybenzamide, a hlydroxyurea, a thiosemicarbazone or other ribonucleotide reductase inhibitor. The polyhydroxybenzoic acid derivatives are also useful in the treatment of diseases in mammals caused by DNA viruses.
    Type: Grant
    Filed: January 18, 1994
    Date of Patent: June 19, 2001
    Inventors: Howard L. Elford, Bartholomeus van't Riet
  • Patent number: 6217914
    Abstract: An ascorbic acid-based composition and related method for the treatment of aging or photo-damaged skin is disclosed. The composition includes water and ascorbic acid, at least a portion of which has generally been pretreated by being dissolved under relatively high temperature and concentration conditions. The composition typically includes at least about 5.0% (w/v) ascorbic acid and may advantageously be formulated to have a pH above 3.5. Generally, the composition also includes non-toxic zinc salt, tyrosine compound, and/or pharmaceutically acceptable carrier. In addition, the composition may include an anti-inflammatory compound, such as aminosugar and/or sulfur-containing anti-inflammatory compound. The topical composition may be in the form of a serum, a hydrophilic lotion, an ointment, a cream, or a gel.
    Type: Grant
    Filed: July 19, 1999
    Date of Patent: April 17, 2001
    Assignee: Bioderm, Inc.
    Inventor: Lorraine Faxon Meisner
  • Patent number: 6214879
    Abstract: Chemical structures have been identified which allosterically modify pyrvate kinase and either inhibit or activate enzymatic activity. These compounds can be used as pharmaceuticals in the treatment of a wide variety of diseases and disorders where influencing metabolic processes is beneficial, such as the glycolytic pathway, all pathways which use ATP as an energy source, and all pathways which involve 2,3-diphosphoglycerate.
    Type: Grant
    Filed: March 24, 1998
    Date of Patent: April 10, 2001
    Assignee: Virginia Commonwealth University
    Inventors: Donald J. Abraham, Richmond E. Danso-Danquah, Telih Boyiri, Changquing Wang, Michael J. Gerber, Stephen J. Hoffman, Gajanan Joshi
  • Patent number: 6211197
    Abstract: Compounds and methods for treating prostaglandin mediated diseases, and certain pharmaceutical compositions thereof are disclosed. The compounds are represented by formula II: Ar1—W—Ar2—X—Q  II The compounds of the invention are structurally different from NSAIDs and opiates, and are antagonists of the pain and inflammatory effects of E-type prostaglandins.
    Type: Grant
    Filed: October 4, 1999
    Date of Patent: April 3, 2001
    Assignee: Merck Frosst Canada & Co.
    Inventors: Michel Belley, Marc Labelle, Nicholas Lachance, Michel Gallant, Nathalie Chauret, Laird A. Trimble, Chun Li
  • Patent number: 6210686
    Abstract: Yeast-derived fiber has been demonstrated, as described herein, to effectively improve the serum lipid profile in humans, when provided as a dietary supplement, without some of the disadvantages known to accompany dietary supplementation with oat fiber or psyllium fiber. Described herein are dietary supplements comprising yeast fiber, e.g., &bgr;-glucan or glucomannan, and further comprising folic acid or a salt thereof, vitamin B6, vitamin B12, and vitamin E. The dietary supplements of the invention can further comprise fats, carbohydrates and proteins, for example, and other ingredients added to formulate a food product. Such food products can be in the form, for example, of solid or semi-solid foods, such as food bars, pudding, or spreads. By including folate and vitamin B6, the dietary supplement provides a second benefit of suppressing the level of homocysteine in the blood.
    Type: Grant
    Filed: December 18, 1998
    Date of Patent: April 3, 2001
    Assignee: Beth Israel Deaconess Medical Center
    Inventors: Stacey J. Bell, R. Armour Forse, Bruce R. Bistrian
  • Patent number: 6191165
    Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 30, 1997
    Date of Patent: February 20, 2001
    Assignee: Allelix Neuroscience Inc.
    Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
  • Patent number: 6180601
    Abstract: The invention relates to freeze-dried soft, flexible and continous matrix of low-molecular weight hyaluronic acid or salt thereof, in which the molecular weight of the hyaluronic acid is preferably between 50 000 and 200 000 Da, containing at least one peptide or protein. It also relates to a pharmaceutical composition in the form of a layer which is characterised by this freeze-dried low-molecular weight hyaluronic acid containing at least one peptide or protein. The drug is preferably chosen from at least one of GH, IGF-I, IGF-II and/or EGF and could be mixtured with an antibiotic agent. The process for the manufacture of this matrix and the use of the pharmaceutical composition for the manufacturing of a drug for wound healing is claimed. The invention discloses a method for accurately obtaining a predetermined dosage of a topically administerable drug which is characterised by freeze-drying a water solution of low-molecular weight hyaluronic acid and the peptide or protein to form a layer.
    Type: Grant
    Filed: June 18, 1996
    Date of Patent: January 30, 2001
    Assignee: Pharmacia AB
    Inventor: Gustaf Jederström
  • Patent number: 6172107
    Abstract: This invention provides a pharmaceutical composition comprising a mycophenolate salt, the composition being adapted to release mycophenolate in the upper part of the intestinal tract.
    Type: Grant
    Filed: December 22, 1999
    Date of Patent: January 9, 2001
    Assignee: Novartis AG
    Inventors: Barbara Haeberlin, Ching-Pong Mak, Armin Meinzer, Jacky Vonderscher
  • Patent number: 6130254
    Abstract: Methods are provided for ameliorating various effects of UVA and UVB radiation from the sun, comprising administering compositions including an ingredient that prevents photoaging from MED and subMED radiation, such as a retinoid, certain other compounds (such as N-acetylcysteine, 2-furildioxime, and vitamin C) and optionally other MMP inhibitors such as tetracyclines and/or compounds that inhibit the P-450-mediated metabolism of retinoids such as ketoconazole and other azole compounds. In the method, the composition is applied prior to exposure to the sun; depending upon the ingredients used in the composition, application should be from 7 to 48 hours prior to exposure. Compounds that prevent erythema (skin reddening, sunburn) do not necessarily protect against UV-mediated elevation of MMP levels and activity, and similarly compounds that prevent UV-mediated elevation of MMP levels and activity are not necessarily effective against UV-induced erythema.
    Type: Grant
    Filed: June 3, 1998
    Date of Patent: October 10, 2000
    Assignee: Regents of the University of Michigan
    Inventors: Gary J. Fisher, John J. Voorhees, Sewon Kang