Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/393)
  • Patent number: 6482846
    Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: November 19, 2002
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
  • Publication number: 20020169328
    Abstract: Novel antimicrobial compositions and strategy to combat bacterial resistance in a variety of bacterial strains are disclosed. The antimicrobial compositions comprise a combination of mitomycin C, or other reductively activated compounds, and ABPI and/or imino-ABPI. The unique strategy involves exposing microorganisms to a first antimicrobial agent, such as mitomycin C, which can induce the expression of at least one protein which confers resistance to mitomycin C, i.e., inactivates mitomycin C. Simultaneously or soon thereafter, the microorganisms are exposed to a second antimicrobial agent, such as ABPI and/or imino-APBI, which is activated by the same protein which inactivates the first antimicrobial agent.
    Type: Application
    Filed: May 23, 2002
    Publication date: November 14, 2002
    Inventor: Thomas C. Goodman
  • Patent number: 6479527
    Abstract: A pharmaceutical composition comprising a compound of formula (I): or a pharmaceutically acceptable salt, ester or amide thereof, which is an inhibitor of monocyte chemoattractant protein-1 and wherein A and B together form an optionally substituted 5-member aromatic ring which includes at least one heteroatom; R1 is an optionally substituted aryl or heteroaryl ring; R2 is selected from a range of organic groups including carboxy, and R3 is hydrogen, or a range of organic groups; in combination with a pharmaceutically acceptable carrier. Certain compounds of formula (I) are novel and these form a further aspect of the invention.
    Type: Grant
    Filed: July 26, 2000
    Date of Patent: November 12, 2002
    Assignee: AstraZeneca UK Limited
    Inventors: Andrew J. Barker, Alan W Faull, Jason G. Kettle
  • Patent number: 6479063
    Abstract: A method of decreasing atherosclerosis and its complications involving administering to a human or animal various combinations of medications with Finasteride, Bicalutamide, Flutamide and Nilutamide.
    Type: Grant
    Filed: December 26, 2000
    Date of Patent: November 12, 2002
    Inventors: Kenneth Weisman, Michael E. Goldberg
  • Publication number: 20020150632
    Abstract: A method for reducing or eliminating cravings associated with habitual substance abuse by administering to a human a synergistic composition containing an effective amount of each of Glutamine, gamma aminobutyric acid, tyrosine, taurine, theanine, 5-hydroxtryptamine, phenylethylamine, phosphatidyl serine, phosphatidyl choline, inositol, thiamin, riboflavin, niacin, pyridoxin, folic acid, biotin, pantothenic acid, cyanocobalamin, chromium polynicotinate magnesium, and decosahexaenoic acid. The pharmaceutical composition can be administered after complete cessation of a given habit forming substance, or to nullify cravings and to reduce abuse of a given habit forming substance, without total and complete remittance prior to administration of the composition. Worthy of note, all constituents found in this composition may be derived by synthetic means, or from natural sources.
    Type: Application
    Filed: March 12, 2002
    Publication date: October 17, 2002
    Inventor: Nick Scott
  • Publication number: 20020151575
    Abstract: The invention provides compounds of formula I: 1
    Type: Application
    Filed: June 13, 2001
    Publication date: October 17, 2002
    Inventors: Edmond J. LaVoie, Jung Sun Kim, Leroy Fong Liu
  • Publication number: 20020146463
    Abstract: The present invention discloses compositions useful as food additives or in medicaments to improve health by treating, preventing, or curing diseases and medical disorders. In particular, the compositions are formulated to provide the nutrients necessary for maintaining optimal free radical defenses in the body.
    Type: Application
    Filed: December 14, 2001
    Publication date: October 10, 2002
    Inventor: Paul Clayton
  • Patent number: 6462036
    Abstract: This invention relates to certain 3-aryl or 3-heteroaryl pyrazoles with 4,5(3,4)-bicyclic ring fusion which are inhibitors of protein kinase activity, of which some are novel compounds, to pharmaceutical compositions containing these pyrazoles and to processes for preparing these pyrazoles.
    Type: Grant
    Filed: May 17, 2000
    Date of Patent: October 8, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Kevin J. Doyle, Paul Rafferty, Robert W. Steele, David J. Wilkins, Lee D. Arnold, Michael Hockley, Anna M. Ericsson, Nobuhiko Iwasaki, Nobuo Ogawa
  • Patent number: 6462041
    Abstract: The present invention is directed to gambogic acid, analogs and derivatives thereof, represented by the general Formulae I-III: wherein R1-R5 are defined herein. The present invention also relates to the discovery that compounds having Formula I-III are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled cell growth and spread of abnormal cells occurs.
    Type: Grant
    Filed: February 1, 2000
    Date of Patent: October 8, 2002
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, Han-Zhong Zhang, Yan Wang, Ben Tseng, Shailaja Kasibhatla, John A. Drewe
  • Publication number: 20020143035
    Abstract: Compounds having the formula (I): 1
    Type: Application
    Filed: November 30, 2001
    Publication date: October 3, 2002
    Inventors: Michele Launay, Dominique Potin, Magali Jeannine Blandine Maillet, Eric Antoine Nicolai, T.G. Murali Dhar, Edwin J. Iwanowicz
  • Publication number: 20020132800
    Abstract: A dietary supplement composition for promoting healthy skin comprised of lycopene and other carotenoids, selenium, chromium and biotin.
    Type: Application
    Filed: October 30, 2001
    Publication date: September 19, 2002
    Inventors: Karl F. Popp, Samuel J. Alioto
  • Patent number: 6441017
    Abstract: The present invention is directed to macrocyclic compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemothera-peutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: September 7, 2000
    Date of Patent: August 27, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Ian M. Bell, Douglas C. Beshore, Steven N. Gallicchio, C. Blair Zartman
  • Patent number: 6432356
    Abstract: The subject matter of the present invention is the adamantane 5,7-diphenyl-1,3-diazoadamantan-6-one derivative per se and the aqueous disinfectant compositions, characterized in that they contain this molecule, and/or the molecule of at least another adamantane derivative, associated in particular with peracetic acid. The disinfectant compositions according to the invention can be utilized as such or water-diluted at the time of use. The disinfectant compositions according to the invention are sporicidal, bactericidal, fungicidal and virucidal for very short contact times.
    Type: Grant
    Filed: March 28, 2000
    Date of Patent: August 13, 2002
    Assignee: IMS S.R.L.
    Inventors: Pietro Affaitati, Giancarlo Folchitto
  • Publication number: 20020102313
    Abstract: A composition for the relief of heat stress, particularly for restoration of electrolyte balance due to passive exposure to heat resulting in excessive transpiration/perspiration, without strenuous physical activity, comprises predetermined levels of selected electrolytes including, in part by weight, sodium ion not exceeding 250 parts, at least 100 parts of potassium ion, at least 100 parts of magnesium ion, and carbohydrates not exceeding 2.5% by weight, as needed for organoleptic purposes only. The composition can further include up to 30 parts of zinc, up to 10 parts of manganese, and from 65 to 400 parts of calcium. Furthermore, the composition can comprise oligoelements, dermoprotective vitamins and anti-oxidants so as to compensate for the chemical changes which might occur in the skin of a person passively exposed to heat.
    Type: Application
    Filed: February 13, 2002
    Publication date: August 1, 2002
    Applicant: ALL SUN HSF COMPANY LIMITED
    Inventors: Fausto Armonti, Donato Mitola, Jacobus C. Samson
  • Publication number: 20020099074
    Abstract: The invention relates to a novel anilide compound and a pharmaceutical composition comprising the same.
    Type: Application
    Filed: December 19, 2001
    Publication date: July 25, 2002
    Applicant: Kowa Company, Ltd.,Japan
    Inventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Mitsuteru Hirata, Chiyoka Ozaki
  • Patent number: 6420395
    Abstract: The present invention discloses compounds of formula (1) or (2), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalky-alkyl, aryl or aralkyl; and R1 is aryl which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cyloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group a monocyclic 5 to 6-membered heteroaryl group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3.
    Type: Grant
    Filed: November 29, 1999
    Date of Patent: July 16, 2002
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet O. Nielsen
  • Publication number: 20020091115
    Abstract: The invention is directed to aza-bridged-bicyclic compounds having Formula (I): 1
    Type: Application
    Filed: June 26, 2001
    Publication date: July 11, 2002
    Inventors: Alexey B. Dyatkin, Bruce E. Maryanoff, William J. Hoekstra, Wei He, William A. Kinney
  • Patent number: 6403616
    Abstract: Process for the manufacturing of slightly soluble or less soluble alkaline salts of substituted sulphinyl heterocycles containing an imidazole moiety with formula I preferably alkaline salts of a proton pump inhibitor compound, wherein the process comprises the step of reacting the substituted sulphinyl heterocycle of Formula I with a source of the cation in the presence of a base, characterized by a washing step in which the prepared alkaline salt of the substituted sulphinyl compound is washed with a basic aqueous solvent mixture. The obtained bulk drug substance resulting in a bulk product that in an aqueous suspension of the substituted sulphinyl heterocycle having a pH not significantly lower than that of a saturated water solution of the pure compound prepared. Alternatively, the process for manufacturing a pharmaceutical dosage form comprising the active substance could be adjusted.
    Type: Grant
    Filed: February 17, 2000
    Date of Patent: June 11, 2002
    Assignee: AstraZeneca AB
    Inventors: Magnus Erickson, Anders Gustavsson, Lars Josefsson
  • Publication number: 20020068747
    Abstract: The present invention is directed to peptidomimetic macrocyclic compounds that inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Application
    Filed: April 6, 2001
    Publication date: June 6, 2002
    Inventors: Craig A. Stump, Theresa M. Williams
  • Publication number: 20020065306
    Abstract: Methods for preventing ulcers, such as gastric ulcers, as well as for improving oxygen consumption and/or time to fatigue involving administering a proton pump inhibitor (PPI) are disclosed and claimed.
    Type: Application
    Filed: May 29, 2001
    Publication date: May 30, 2002
    Inventor: Frank Pipers
  • Publication number: 20020064560
    Abstract: This invention relates to compositions and methods for enhancing the penetration of topical skin agents into the skin wherein said compositions contain at least one active ingredient, a skin conditioner and a polymeric emulsifier.
    Type: Application
    Filed: December 7, 2001
    Publication date: May 30, 2002
    Inventors: John Kung, Jue-Chen Liu, Susan Niemiec
  • Publication number: 20020061913
    Abstract: The present invention provides compounds of formula (I): 1
    Type: Application
    Filed: June 22, 2001
    Publication date: May 23, 2002
    Inventors: Christopher John Urch, Terence Lewis, Raymond Leo Sunley, Roger Salmon, Christopher Richard Ayles Godfrey, Christopher Ian Brightwell, Matthew Brian Hotson
  • Patent number: 6380228
    Abstract: The present invention is directed to peptidomimetic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: April 6, 2001
    Date of Patent: April 30, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Craig A. Stump, Theresa M. Williams
  • Publication number: 20020049238
    Abstract: Compounds with heterocyclic-hydroxyimino-fluorene nuclei that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
    Type: Application
    Filed: August 16, 2001
    Publication date: April 25, 2002
    Inventors: Wesley Kwon Mung Chong, Rohit Kumar Duvadie
  • Patent number: 6369235
    Abstract: The present invention provides compositions and methods for the treatment of HIV infection. In particular, the present invention provides non-nucleoside inhibitors of reverse transcriptase (RT), as well as methods to treat HIV infection using these non-nucleoside inhibitors of RT. In preferred embodiments, the present invention provides a novel class of substituted benzimidazoles, effective in the inhibition of human immunodeficiency virus (HIV) RT.
    Type: Grant
    Filed: February 1, 2000
    Date of Patent: April 9, 2002
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Christopher J. Michejda, Marshall Morningstar, Thomas Roth
  • Patent number: 6362202
    Abstract: The invention relates to methods and compositions for the prevention, treatment, or management of gastrointestinal disorders or symptoms thereof, employing two or more agents or compounds to provide a triple site action on 5-HT3 receptors, 5-HT4 receptors, and at least one of H2 receptors and proton pumps.
    Type: Grant
    Filed: February 22, 2000
    Date of Patent: March 26, 2002
    Assignee: Sepracor Inc.
    Inventors: Paul D. Rubin, Timothy J. Barberich
  • Publication number: 20020034511
    Abstract: Methods, compounds, compositions and kits that relate to pretargeted delivery of diagnostic and therapeutic agents are disclosed. In particular, methods for radiometal labeling of biotin and for improved radiohalogenation of biotin, as well as related compounds, are described. Also, clearing agents, anti-ligand-targeting moiety conjugates, target cell retention enhancing moieties and additional methods are discussed.
    Type: Application
    Filed: August 1, 2001
    Publication date: March 21, 2002
    Inventors: John M. Reno, Louis J. Theodore, Linda M. Gustavson
  • Patent number: 6358985
    Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 29, 1999
    Date of Patent: March 19, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Ian M. Bell, Douglas C. Beshore, Terrence M. Ciccarone, S. Jane de Solms, Christopher J. Dinsmore, Gerald E. Stokker
  • Patent number: 6359144
    Abstract: The invention provides a rapid approach for combinatorial synthesis and screening of combinatorial libraries of bicyclic guanidine compounds. The present invention further provides the compounds made by the combinatorial synthesis and individually as well as methods of using the same.
    Type: Grant
    Filed: February 3, 1998
    Date of Patent: March 19, 2002
    Assignee: Lion Bioscience AG
    Inventors: John M. Ostresh, Jean-Philippe Meyer, Colette T. Dooley, Sylvie E. Blondelle, Christa C. Schoner, Richard A. Houghten
  • Patent number: 6353005
    Abstract: The invention relates to methods and compositions for the prevention, treatment, or management of gastrointestinal disorders or symptoms thereof, employing two or more agents or compounds to provide a triple site action on 5-HT3 receptors, 5-HT4 receptors, and at least one of H2 receptors and proton pumps.
    Type: Grant
    Filed: February 22, 2000
    Date of Patent: March 5, 2002
    Assignee: Sepracor, Inc.
    Inventors: Paul D. Rubin, Timothy J. Barberich
  • Patent number: 6350909
    Abstract: The invention relates to new imides, to a plurality of processes for their preparation and to their use as fungicides.
    Type: Grant
    Filed: January 2, 2001
    Date of Patent: February 26, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Herbert Gayer, Peter Gerdes, Martin Vaupel, Astrid Mauler-Machnik, Gerd Hänssler, Klaus Stenzel, Martin Kugler, Thomas Jaetsch, Peter Wachtler
  • Publication number: 20020019425
    Abstract: The therapeutic use of temporary p53 inhibitors in the treatment of p53-mediated diseases, conditions, and injuries is disclosed.
    Type: Application
    Filed: September 6, 2001
    Publication date: February 14, 2002
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Andrei V. Gudkov, Pavel G. Komarov, Elena A. Komarova
  • Patent number: 6344570
    Abstract: Compounds of formula (II) where R1 is in the para or meta position and is (A); R2 and R3 are each independently selected from hydrogen, nitro, C1-6alkyl, C3-6cycloalkyl, C2-6alkenyl, C2-6alkynyl, C1-4alkoxyl, C1-6alkylamino, C1-6dialkylamino, C1-6akylC1-4alkoxyl, C1-6alkylaminoC1-6alkyl, amino, cyano, halogeno, trifluoromethyl, —CO2R12 and —CONR12R13, where R12 and R13 are independently selected from hydrogen or C1-6alkyl, or R2 and R3 together with the phenyl to which they are attached form a 9 or 10 membered bicyclic ring system; R4 is C1-4alkyl; R5 is selected from hydrogen and C1-4alkyl; R6 is selected from C1-6alkyl, C1-4alkyl(C4-6)cycloalkyl, C1-6alkyl(C1-6)alkoxyl, C1-6alkylS(C1-6)alkyl, C1-4alkylsulphonyl(C1-4)alkyl; (B) where q is an integer from 1 to 6 and R14 is halogeno; R7 is selected from C1-6alkyl, C1-8alkoxylcarbonyl, C2-6alkenyl, 1,3-benzodioxol-5-yl and aryl each optionally substituted by one or more substituents selected from C1-4alkoxy, C1-6alkyl, cyano, halog
    Type: Grant
    Filed: July 11, 2000
    Date of Patent: February 5, 2002
    Assignee: AstraZeneca UK Limited
    Inventors: David R Brittain, Craig Johnstone
  • Publication number: 20020013354
    Abstract: The present invention relates to compounds of Formula (I) 1
    Type: Application
    Filed: April 19, 2001
    Publication date: January 31, 2002
    Inventors: Soan Cheng, David Michael Goldstein, Teresa Alejandra Trejo Martin, Eric Brian Sjogren
  • Publication number: 20020010142
    Abstract: A parasiticidal formulation is provided. This formulation includes a pyrrolidone solvent, a bridging solvent, and an parasiticidal agent. One or more parasiticidal agents may be included in the formulation. Preferably, the formulation contains both closantel and ivermectin. Another aspect of the present invention is a method of making this parasiticidal formulation. This method includes mixing a pyrrolidone solvent and a bridging solvent to form a solvent solution and adding one or more parasiticidal agents to the solvent solution. A further aspect of the present invention is a method for administering the parasiticidal formulation of the present invention to an animal. This method of administration includes providing the parasiticidal formulation described above and applying this formulation to the skin of an animal, wherein the formulation is absorbed through the animal's skin.
    Type: Application
    Filed: September 26, 2001
    Publication date: January 24, 2002
    Inventor: Richard Mihalik
  • Patent number: 6340672
    Abstract: A parasiticidal formulation is provided. This formulation includes a pyrrolidone solvent, a bridging solvent, and an parasiticidal agent. One or more parasiticidal agents may be included in the formulation. Preferably, the formulation contains both closantel and ivermectin. Another aspect of the present invention is a method of making this parasiticidal formulation. This method includes mixing a pyrrolidone solvent and a bridging solvent to form a solvent solution and adding one or more parasiticidal agents to the solvent solution. A further aspect of the present invention is a method for administering the parasiticidal formulation of the present invention to an animal. This method of administration includes providing the parasiticidal formulation described above and applying this formulation to the skin of an animal, wherein the formulation is absorbed through the animal's skin.
    Type: Grant
    Filed: February 16, 2000
    Date of Patent: January 22, 2002
    Assignee: Phoenix Scientific, Inc.
    Inventor: Richard Mihalik
  • Publication number: 20020007071
    Abstract: This invention provides a series of substituted benzimidazoles which are useful in treating or preventing a condition associated with an excess of neuropeptide Y. This invention also provides methods employing these substituted benzimidazoles as well as pharmaceutical formulations with comprise as an active ingredient one or more of these compounds.
    Type: Application
    Filed: November 30, 2000
    Publication date: January 17, 2002
    Inventors: Thomas Charles Britton, Robert Frederick Bruns, Buddy Eugene Cantrell, Philip Arthur Hipskind, Karen Lynn Lobb, James Arthur Nixon, Paul Leslie Ornstein, Edward C. R. Smith, Hamideh Zarrinmayeh, Dennis Michael Zimmerman, Anne Marie Nunes, James Jeffry Howbert
  • Patent number: 6339082
    Abstract: A compound selected from the group consisting of a compound of the formula wherein the substituents are defined as set forth in the specification and its salts with non-toxic pharmaceutically acceptable acids and bases useful for treating loss of bone matrix.
    Type: Grant
    Filed: June 29, 2000
    Date of Patent: January 15, 2002
    Assignees: Aventis Pharma S.A., Genetech, Inc.
    Inventors: Denis Carniato, Thomas R. Gadek, Jean-Francois Gourvest, Jochen Knolle, Robert S. McDowell, Anurschirwan Peyman
  • Publication number: 20020001622
    Abstract: The present invention relates in general to a method of producing a dry, free-flowing mixture of liquid tocopherols. The present invention also relates to a dry free-flowing vitamin powder.
    Type: Application
    Filed: August 22, 2001
    Publication date: January 3, 2002
    Inventors: Charles A. Morris, Francis W. Calhoon, Huey L. Willis
  • Patent number: 6323234
    Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; composition comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.
    Type: Grant
    Filed: March 3, 2000
    Date of Patent: November 27, 2001
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
  • Patent number: 6316481
    Abstract: The present invention is concerned with an oral pharmaceutical formulation containing a proton pump inhibitor (PPI) which is suitable for the treatment of gastric acid related diseases in man and animals. More specifically, the composition is a paste, and is particularly suitable for delivery of a proton pump inhibitor to horses.
    Type: Grant
    Filed: February 22, 2000
    Date of Patent: November 13, 2001
    Assignee: Merck & Co. Inc.
    Inventor: Keith Freehauf
  • Patent number: 6310080
    Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically inhibiting retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: December 1, 1999
    Date of Patent: October 30, 2001
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
  • Publication number: 20010031779
    Abstract: The invention involves methods and materials for treating and preventing non-invasive fungus-induced mucositis. Specifically, the invention involves administrating an antifungal agent such that it contact mucus in an amount, at a frequency, and for a duration effective to prevent, reduce, or eliminate non-invasive fungus-induced rhinosinusitis. This invention also provides methods and materials for diagnosing non-invasive fungus-induced rhinosinusitis and culturing non-invasive fungus from a mammalian mucus sample as well as specific antifungal formulations and medical devices for treating and preventing non-invasive fungus-induced rhinosinusitis. In addition, the invention provides methods and materials for treating and preventing other non-invasive fungus-induced mucositis conditions such as chronic otitis media, chronic colitis, and Crohn's disease. Further, the invention involves methods and materials for treating and preventing chronic asthma symptoms.
    Type: Application
    Filed: May 25, 2001
    Publication date: October 18, 2001
    Inventor: Jens Ponikau
  • Patent number: 6303644
    Abstract: The invention relates to the use of proton pump inhibitors as combination therapeutics in the treatment of bacterial diseases which do not affect the gastrointestinal track using antibacterially active compounds.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: October 16, 2001
    Assignee: Byk Gulden Lomberg Chemische Fabrik GmbH
    Inventor: Klaus Tuch
  • Patent number: 6300358
    Abstract: Use of benzydamine and physiologically acceptable acid addition salts thereof for preparing a medicament for the treatment of pathological conditions caused by TNF.
    Type: Grant
    Filed: May 6, 1996
    Date of Patent: October 9, 2001
    Assignee: Angelini Ricerche S.p.A. Societa'Consortile
    Inventor: Valerio Cioli
  • Patent number: 6297260
    Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.
    Type: Grant
    Filed: October 29, 1999
    Date of Patent: October 2, 2001
    Assignee: NitroMed, Inc.
    Inventors: Upul K. Bandarage, Qing Dong, Xinqin Fang, David S. Garvey, Gregory J. Mercer, Stewart K. Richardson, Joseph D. Schroeder, Tiansheng Wang
  • Patent number: 6291533
    Abstract: Dietary supplement compositions designed to be responsive to specific blood types, and thus most beneficial for people with specific antigenic blood types.
    Type: Grant
    Filed: December 22, 1999
    Date of Patent: September 18, 2001
    Assignee: Vitamerica, Inc.
    Inventor: Albert M. Fleischner
  • Patent number: 6291447
    Abstract: Novel granulatimide compounds and pharmaceutical formulations thereof are provided.
    Type: Grant
    Filed: February 26, 1999
    Date of Patent: September 18, 2001
    Assignees: The University of British Columbia, Kinetek Pharmaceuticals, Inc.
    Inventors: Raymond Andersen, Michel Roberge, Jasbinder Sanghera, Daniel Leung, Edward Piers, Roberto GS Berlinck, Robert Britton
  • Patent number: 6291500
    Abstract: The invention involves methods and materials for treating and preventing non-invasive fungus-induced mucositis. Specifically, the invention involves administrating an antifungal agent such that it contact mucus in an amount, at a frequency, and for a duration effective to prevent, reduce, or eliminate non-invasive fungus-induced rhinosinusitis. This invention also provides methods and materials for diagnosing non-invasive fungus-induced rhinosinusitis and culturing non-invasive fungus from a mammalian mucus sample as well as specific antifungal formulations and medical devices for treating and preventing non-invasive fungus-induced rhinosinusitis. In addition, the invention provides methods and materials for treating and preventing other non-invasive fungus-induced mucositis conditions such as chronic otitis media, chronic colitis, and Crohn's disease. Further, the invention involves methods and materials for treating and preventing chronic asthma symptoms.
    Type: Grant
    Filed: October 22, 1998
    Date of Patent: September 18, 2001
    Inventor: Jens Ponikau
  • Publication number: 20010016343
    Abstract: An efficient synthesis for the selective and efficient 1′-N derivatization of biotin is reported. The derivatized biotin acts as a stable analog of the carboxyphosphate intermediate in naturally-occurring biotin-mediated CO2 transfer. The synthesis may readily be scaled up to perform large-scale, selective acylations of biotin. The stable analog of the intermediate can inhibit the activity of the biotin carboxylase enzymes such as acetyl CoA carboxylase, and HIV protease. The functionalization at the 1′-N of biotin results in the attachment of an electrophilic “handle” amenable to reaction with a wide variety of nucleophiles to generate a new family of biotin analogs.
    Type: Application
    Filed: April 6, 2001
    Publication date: August 23, 2001
    Inventors: Robert M. Strongin, Marcelo C. Saraiva, Grover L. Waldrop, David R. Amspacher