Polycarboxylic Acid Patents (Class 514/566)
  • Patent number: 5362754
    Abstract: Disclosed are pharmaceutical compositions of a mixture of minocycline and EDTA (M-EDTA) and methods of using the compositions in maintaining the patency of a catheter port. Methods for inhibiting the formation of polysaccharide-rich glycocalyx (such as the glycocalyx of staphylococcal organisms) are also provided using an M-EDTA solution. The M-EDTA solution may also be used to pretreat a medical device to prevent adherence of infectious organisms, such as S. epidermidis and S. aureus. The compositions destroy and prevent the formation of polysaccharide-rich glycocalyx. Methods for treating infections of S. epidermidis and S. aureus where glycocalyx formation are provided with an M-EDTA solution. The minocycline and EDTA solutions are included together within a pharmacologically acceptable carrier solution, such as saline.
    Type: Grant
    Filed: November 12, 1992
    Date of Patent: November 8, 1994
    Assignee: Univ. of TX MD Anderson Cancer Center
    Inventors: Issam Raad, Robert J. Sherertz
  • Patent number: 5332579
    Abstract: A nutritional supplement, functioning as a food for special dietary use, enhances diets and assists persons recovering from addiction to health damaging substances. Since cellular damage and deficiencies occur and continue to exist even after the person has stopped abusing the substances, use of the nutritional supplement, which contains a variety of minerals, vitamins, herbs, amino acids, and other substances and nutrients, should be continuous. The nutritional supplement consists of a mixture of nutrients which cooperate synergistically in enhancing cellular metabolic pathways and assists in normalization of cellular functions and optimization of cellular health.
    Type: Grant
    Filed: November 20, 1992
    Date of Patent: July 26, 1994
    Inventor: Anthony J. Umbdenstock
  • Patent number: 5324747
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, n, m, o, p and q are as hereinafter set forth, and, when R.sub.2 is hydrogen, pharmaceutically acceptable salts thereof with bases, are described. The compounds of formula 1 are potent inhibitors of phospholipases A.sub.2 (PLA.sub.2 's) and are therefore useful in the treatment of inflammatory diseases, such as psosiasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia/reperfusion, and trauma induced inflammation, such as spinal cord injury.
    Type: Grant
    Filed: July 15, 1992
    Date of Patent: June 28, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Mathew Carson, Ru-Jen L. Han, Ronald A. LeMahieu, Vincent S. Madison
  • Patent number: 5312831
    Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.
    Type: Grant
    Filed: May 12, 1993
    Date of Patent: May 17, 1994
    Assignee: American Cyanamid Company
    Inventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
  • Patent number: 5308627
    Abstract: A nutritional supplement, functioning as a food for special dietary use, enhances diets and assists persons recovering from addiction to health damaging substance(s). Since cellular damage and deficiencies occur and continue to exist even after the person has stopped abusing the substance(s), use of the nutritional supplement, which contains at least one enzyme activating substance and at least one enzyme cofactor, should be continuous. The nutritional supplement consists of a mixture of nutrients which cooperate synergistically in enhancing cellular metabolic pathways and assists in normalization of cellular functions and optimization of cellular health.
    Type: Grant
    Filed: November 19, 1992
    Date of Patent: May 3, 1994
    Inventor: Anthony J. Umbdenstock, Jr.
  • Patent number: 5296501
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein the dotted lines indicate an optionally endo or exo double bond, Y is selected from the group consisting of alkyl, alkenyl and alkynyl of 2 to 18 carbon atoms and alkyl of 1 to 18 carbon atoms substituted with at least one halogen, X, X' and X.sub.1 are individually selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, aryl of 6 to 14 carbon atoms, aralkyl of 7 to 18 carbon atoms, acyl of a fatty acid and acyl of an .alpha. or .omega.-amino acid, n and/or n.sub.1 is 1 and R and/or R.sub.1 is the remainder of an amine or an .alpha. or .omega.-amino acid or n and/or n.sub.1 is 2 and R and R.sub.1 are selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, aryl of 6 to 14 carbon atoms, aralkyl of 7 to 18 carbon atoms and ##STR2## R.sub.
    Type: Grant
    Filed: April 27, 1993
    Date of Patent: March 22, 1994
    Assignee: Roussel Uclaf
    Inventors: Constantin Agouridas, Nicole Tessot, Annie Martel
  • Patent number: 5154903
    Abstract: This invention pertains to an improved method of inhibiting peroxide-reduction catalytic activity and concomitant toxicity of asbestos and nonasbestos iron-containing silicates. These undesirable reactions can be substantially reduced or essentially eliminated by contacting these potentially harmful materials with an aqueous solution comprising a non-mutagenic non-toxic iron chelating agent, such as phytic acid, diethylenetriamine pentaacetic acid (DTPA) or derivatives of these.
    Type: Grant
    Filed: September 13, 1990
    Date of Patent: October 13, 1992
    Assignees: Massachusetts General Hospital, Boston Biomedical Research Institute
    Inventors: Philip J. Graceffa, Sigmund A. Weitzman
  • Patent number: 5143732
    Abstract: An orally administered pharmaceutical agent that is particularly suited for iron and magnesium substitutive therapy is disclosed. This drug consists of a combination of one or more pharmaceutically and physiologically compatible iron compounds, one or more pharmaceutically and physiologically compatible magnesium compounds, and, if the magnesium compounds do not contain any chlorine atoms dissociable in aqueous media and saturating the available magnesium valences, the drug further consists of one or more pharmaceutically and physiologically compatible compounds providing chlorine ions in aqueous media. The iron compounds, magnesium compounds and chlorine ion supplying compounds may be mixed with the conventional pharmaceutical solvents and/or thinners and/or auxiliary matter. Unexpectedly, this drug makes it possible to simultaneously administer magnesium or calcium compounds with iron compounds, without thereby causing reduced iron resorption.
    Type: Grant
    Filed: March 15, 1989
    Date of Patent: September 1, 1992
    Assignee: Verla-Pharm Arzneimittelfabrik Apotheker H.J. V. Ehrlich GmbH & Co.
    Inventors: Joachim Helbig, Hans G. Classen
  • Patent number: 5122369
    Abstract: An orally acceptable nutrient and mineral supplement for reducing hair loss wherein the composition contains divalent iron and pantothenic acid in a weight to weight ratio of approximately 1-3 and racemic d, 1-methionine. A particularly preferred composition contains 11.25 mg. of divalent iron as ferrous fumarate and 35 mg. of pantothenic acid as calcium pantothenate and 200 mg. of d,1-methionine.
    Type: Grant
    Filed: April 16, 1991
    Date of Patent: June 16, 1992
    Assignee: Harmony Health Products, Inc.
    Inventor: R. Harvey Dye
  • Patent number: 5114974
    Abstract: The treatment of atherosclerosis by administration of pure MgNa.sub.2 EDTA to a patient to favorably influence one or more of the multiple stages in the complex pathophysiology of the disease.
    Type: Grant
    Filed: January 30, 1991
    Date of Patent: May 19, 1992
    Inventor: Martin Rubin
  • Patent number: 5108733
    Abstract: Spontaneous aspecific coloration in so-called Trinder reagents which can alter subsequent colorimetric determinations is inhibited by adding compounds of the chelating agent class to the solution. The resultant compositions contain a peroxidase enzyme, a phenylpyrazone derivative, a compound of phenolic or aromatic amine structure and a stabilizer. Preferred stabilizers are ethylenediaminetetraacetic acid (EDTA) and diethylenetriaminepentaacetic acid (DTPA).
    Type: Grant
    Filed: August 30, 1990
    Date of Patent: April 28, 1992
    Assignees: Instrumentation Laboratory S.p.A., 501 Instrumentation Laboratory S.p.A.
    Inventors: Dario Frontini, Maurizio D'Alterio
  • Patent number: 5106873
    Abstract: This invention relates to novel compounds which are ACAT inhibitors rendering them useful in lowering blood cholesterol levels. The compounds contain two urea or thiourea, amide, or amine moieties or combinations of said moieties and have the following general formula: ##STR1## wherein m and n are zero or one, W and YNH and ##STR2## form the urea, thiourea, amide or amine moieties; and R.sub.1 and R .sub.2 are hydrogen or a hydrocarbon radical.
    Type: Grant
    Filed: June 26, 1990
    Date of Patent: April 21, 1992
    Assignee: Warner-Lambert Company
    Inventors: Patrick M. O'Brien, Drago R. Sliskovic, Michael W. Wilson
  • Patent number: 5047425
    Abstract: Compounds of the formula ##STR1## wherein Ar, R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X and n have the meanings mentioned in the description, processes and intermediates for their preparation, pharmaceutical compositions which contain them and their use in therapy in the treatment of cardiovascular diseases.
    Type: Grant
    Filed: November 30, 1988
    Date of Patent: September 10, 1991
    Assignee: Simes Societa Italiana Medicinali & Sintetici SpA
    Inventors: Cesare Casagrande, Francesco Santangelo, Luisa Calabi
  • Patent number: 5036052
    Abstract: There are herein disclosed stablized and/or dense L-amino acid nutrient compositions, i.e., amino acid infusion solutions, which contain at least one oligopeptide having at least one residue of L-Tryptophan, L-Tyrosine, L-Leucine, L-Isoleucine and L-Valine.
    Type: Grant
    Filed: June 21, 1989
    Date of Patent: July 30, 1991
    Assignees: Morishita Pharmaceutical Co., Ltd., Ajinomoto Co., Inc.
    Inventors: Kohji Ozeki, Yoshitsugu Tsukamoto, Hideya Yaginuma, Makoto Sato
  • Patent number: 5030658
    Abstract: Disclosed are arthropodicidal solutions for application to plants comprising, as an active ingredient, arthropodicidally active mono alpha carboxylic acids, of hydrocarbons having 8 to 20 carbon atoms, and/or monovalent metal salts thereof. The arthropodicidal activity of these fatty acids is potentiated by including in the solution an agent capable of sequestering metal ions such as one or a mixture of chelateing agents, sequestering agents, and surfactants.
    Type: Grant
    Filed: November 17, 1989
    Date of Patent: July 9, 1991
    Assignee: Safer, Inc.
    Inventors: Greg Salloum, George Puritch, Michelle Gorman, Roderick Bradbury
  • Patent number: 4988724
    Abstract: Disclosed are total parenteral nutrition formulations which include essential amino acids in combination with either arginine or ornithine, for use in the detection of recurrent malignant disease in patients. Such formulations stimulate tumor-specific polyamine production to a greater extent than non-tumor related polyamine production. Additionally, such formulations were found to specifically promote an increase in red blood cell putrescine levels of tumor-bearing rats. Nontumor-bearing rats were not found to be similarly reactive to these formulations. Methods for making and administering these formulations as well as their use in preventing DFMO-induced toxicity are also disclosed.Also disclosed are parenteral nutritional formulations which include both citrulline and ornithine which have an arginine concentration of less than about 0.10% by weight final concentration. These formulations inhibit tumor growth and are particularly suited to provide nutritional support for patients with malignant disease.
    Type: Grant
    Filed: December 9, 1988
    Date of Patent: January 29, 1991
    Assignee: Board of Regents, The University of Texas System
    Inventors: Jaffer Ajani, Bruce Grossie, Jr., Kenji Nishioka, David M. Ota
  • Patent number: 4975281
    Abstract: In accordance with the present invention a novel oral composition and method of using same for the treatment of ulcers and other gastrointestinal disorders is disclosed. The composition comprises an agent capable of forming an ulcer-adherent protective complex in an acid environment combined with one or more alkaline materials in a total amount sufficient to substantially prevent the formation of such a complex in the mouth and adherence of such a complex to the buccal mucosa.
    Type: Grant
    Filed: January 30, 1989
    Date of Patent: December 4, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Richard J. Harwood, Edward V. Henry, Joseph S. Sonk, Luke T. H. Foo, Jay L. Rheingold, Robert C. deGroof
  • Patent number: 4891356
    Abstract: A method of treating gastrointgestinal ulcer disease is provided which involves administration of a proteinase inhibitor or analogue to patients suffering from same. Of particular interest is the use of inhibitors of serine, cysteine, carboxyl, and metallo proteinases.
    Type: Grant
    Filed: July 15, 1987
    Date of Patent: January 2, 1990
    Assignee: Brigham & Women's Hospital
    Inventor: Sandor Szabo
  • Patent number: 4859653
    Abstract: This invention relates to new compositions of matter for use in treating wrinkling of the human skin. The compositions comprise, as an essential ingredient therein, at least one N-acylate, by butyric acid, of an alpha-amino acid or a salt of said acylate with an inorganic, organic or biologic base or with a metal.
    Type: Grant
    Filed: December 9, 1986
    Date of Patent: August 22, 1989
    Inventors: Jean V. Morelle, Eliane M. T. Lauzanne-Morelle
  • Patent number: 4845125
    Abstract: An improved composition for dissolution of renal calculi is disclosed. The composition includes citric acid, preferably at about 10 to about 15% by weight, and an effective amount of a pharmacologically acceptable chelating agent such as EDTA in a sterile aqueous solution having a pH between about 3 and about 4.5. In vivo irrigation with the improved formulation, optionally in combination with incident ultrasound therapy promotes rapid stone dissolution with minimal complications for the patient.
    Type: Grant
    Filed: November 10, 1987
    Date of Patent: July 4, 1989
    Assignee: Indianapolis Center for Advanced Research, Inc.
    Inventor: George E. Geier
  • Patent number: 4814351
    Abstract: A scalp treatment for reducing average daily hair loss periodically applies to the scalp a composition containing an active chelating agent sufficient to chelate at least 0.3 milligrams of divalent calcium ion per milliliter of the composition and leaving the chelating agent in contact with the scalp for at least eight hours. Particularly preferred chelating agents comprise ethylene diamine tetraacetic acid, citric acid, and soluble salts thereof.
    Type: Grant
    Filed: June 26, 1987
    Date of Patent: March 21, 1989
    Assignee: Redken Laboratories, Inc.
    Inventors: Roger A. Mathews, David W. Cannell
  • Patent number: 4721726
    Abstract: A method for inhibiting the action of enkephalinases in a mammal to thereby elicit an analgesic effect in said mammal is described.Novel compound and compositions useful for accomplishing the method of the invention are also described.
    Type: Grant
    Filed: July 25, 1986
    Date of Patent: January 26, 1988
    Assignee: Schering Corporation
    Inventor: Joel G. Berger
  • Patent number: 4695588
    Abstract: Novel substituted .alpha.-fluoromethyl-.alpha.-amino alkanoic acids and esters thereof are disclosed. The novel compounds have biological activity including decarboxylase inhibition.
    Type: Grant
    Filed: March 16, 1978
    Date of Patent: September 22, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Janos Kollonitsch, Arthur A. Patchett
  • Patent number: 4689347
    Abstract: A new pharmaceutical composition is disclosed useful in the treatment of neuroviruses and formulated as an injectable solution. The pharmaceutical composition is composed of the calcium and sodium double salt of ethylene diamine tetracetic acid, associated with calcium gluconate as a source of Ca.sup.2+ ions, and cysteine or its HC1 salt, wherein the weight ratio of the ingredients ranges from 8-12 g to 0.3 to 1 g to 0.05 to 0.2 g respectively per 100 ml of water.
    Type: Grant
    Filed: October 10, 1985
    Date of Patent: August 25, 1987
    Assignee: Centrala Industriala de Medicamente Cosmetice Coloranti Si Lacuri
    Inventors: Romulus C. Dinu, Illeana D. Dinu
  • Patent number: 4668665
    Abstract: A storage-stable sucralfate-containing preparation which maintains its ability, even after extended periods of time, to form a viscous, sticky, paste-like material in the presence of gastric secretions is disclosed as well as the method of making same.
    Type: Grant
    Filed: September 10, 1985
    Date of Patent: May 26, 1987
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Kouji Ishihara, Kazuo Igusa, Toshichika Ogasawara
  • Patent number: 4661510
    Abstract: Novel .alpha.-allenic-.alpha.-amino acids which are enzyme inhibitors of the suicide or k.sub.cat type are disclosed herein.
    Type: Grant
    Filed: October 21, 1985
    Date of Patent: April 28, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Alexander Krantz, Arlindo L. Castelhano
  • Patent number: 4584404
    Abstract: Selective biogenic amine uptake inhibitors, 3-substituted phenyloxy-3-phenylpropyldimethylamines.
    Type: Grant
    Filed: October 24, 1983
    Date of Patent: April 22, 1986
    Assignee: Eli Lilly and Company
    Inventors: Bryan B. Molloy, Klaus K. Schmiegel
  • Patent number: 4496588
    Abstract: A novel method of treating psoriasis which comprises administering a halomethyl derivative of .alpha.-amino acids of the following general structure: ##STR1## wherein Y is FCH.sub.2 --, F.sub.2 CH--, F.sub.3 C--, ClCH.sub.2 --, Cl.sub.2 CH--; Z is .gamma.-guanidinopropyl or R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4; each of R.sub.a and R.sub.b can be the same or different and is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.1 is hydroxy; a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms, or ##STR3## wherein R.sub.
    Type: Grant
    Filed: April 28, 1983
    Date of Patent: January 29, 1985
    Assignee: Merrell Toraude et Compagnie
    Inventors: Philippe Bey, Michel Jung