Acyclic And Contains At Least One Carbon Atom Between The Phosphorus Atoms Patents (Class 514/108)
  • Patent number: 7138388
    Abstract: This invention provides methods for treating inflammatory or autoimmune diseases by contacting the affected cell or tissue with a therapeutic compound as described herein. Such pathologies include, but are not limited to rheumatoid arthritis, systemic lupus erythmatosus, psoriatic arthritis, reactive arthritis, Crohn's disease, ulcerative colitis and scleroderma. Therapeutic compounds useful in the methods of this invention are selected from the group consisting of a 1,5-substituted pyrimidine derivative or analog and substituted furano-pyrimidone analog.
    Type: Grant
    Filed: January 18, 2002
    Date of Patent: November 21, 2006
    Assignee: Celmed Oncology (USA), Inc.
    Inventor: H. Michael Shepard
  • Patent number: 7084126
    Abstract: Methods and composisions for enhancing cellular function through protection of a tissue components such receptors, proteins, lipids, nucleic acids, carbohydrates, hormones, vitamins, and cofactors, by administering pyrophosphate analogs or related compounds.
    Type: Grant
    Filed: April 27, 2001
    Date of Patent: August 1, 2006
    Assignee: HealthPartners Research Foundation
    Inventors: William H. Frey, II, John Randall Fawcett
  • Patent number: 7078059
    Abstract: The invention provides a method for enhancing bone formation, inhibiting osteoclastic differentiation and/or activating osteoblastic differentiation whereby to manage, treat or achieve prophylaxis of bone disease which comprises administering to a human or animal subject suffering from, or susceptible to bone disease a therapeutically or prophylactically effective amount of a lanthanum compound.
    Type: Grant
    Filed: June 26, 2001
    Date of Patent: July 18, 2006
    Assignee: Shire Holdings AG
    Inventors: Nigel D. Atherton, Joseph William Totten, Michael David Gaitonde
  • Patent number: 7018982
    Abstract: The invention relates to a combined pharmaceutical preparation comprising parathyroid hormone and a bone resorption inhibitor, said preparation being adapted for (a) the administration of parathyroid hormone during a period of approximately 6 to 24 months; (b) after the administration of parathyroid hormone has been terminated, the administration of a bone resorption inhibitor during a period of approximately 12 to 36 months.
    Type: Grant
    Filed: March 18, 2003
    Date of Patent: March 28, 2006
    Assignee: NPS Allelix Corp.
    Inventors: John Dietrich, Sverker Ljunghall, Sven Sjögren
  • Patent number: 6896871
    Abstract: The present invention is directed to particular bisphosphonate compounds, and in particular, to bisphosphonate conjugates that are useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis.
    Type: Grant
    Filed: April 10, 2001
    Date of Patent: May 24, 2005
    Assignee: MBC Research, Inc.
    Inventors: Alexander Karpeisky, Nelly Padioukova, Sergey Mikhailov, H.B.F. Dixon, Grigorii Tzeitline, Marat Karpeisky
  • Patent number: 6864228
    Abstract: This procedure consists in the first stage, of the administration of enough quantity of bisphosphonate preparation during the necessary period of time to acquire a degree of volumetric mineral density of the cortical tissue of application, within the normal range (average IDS). Then the administration of the bisphosphonate preparation is interruption in order to enable the development of the sectional momentum of inertia. The length of the second stage can be determined by means of a tomography. That is to say, that the periods of administration or non-administration of the mineralizing agent are defined or controlled by precise osteologic variables and therefore are not fixed. If during the second stage the cortical mineral density drops by 6-10% of the maximum value previously obtained, administration of bisphosphonate preparation should be resumed until the corresponding maximum adjusted value is reached again.
    Type: Grant
    Filed: May 12, 2000
    Date of Patent: March 8, 2005
    Assignee: Gador, S.A.
    Inventors: Emilio J. A. Roldan, Anibal Perez Lloret
  • Patent number: 6844320
    Abstract: Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in further combination with one or more of a cyclooxygenase inhibitor, a PGI2-mimetic, a thromboxane (TXA2) inhibitor, a compound possessing TXA2-agonistic and TXA2-inhibiting properties, a compound possessing TXA2-antagonistic and PGI2-memetic activities, and a TXA2 antagonist.
    Type: Grant
    Filed: July 24, 1998
    Date of Patent: January 18, 2005
    Assignees: Board of Regents, The University of Texas System, Schering Aktiengesellschaft
    Inventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampalli
  • Patent number: 6835722
    Abstract: The present invention relates to a pharmaceutical composition for the treatment of metabolic bone disease and the method of preparation thereof, and more particularly, to an improved pharmaceutical composition for the therapeutic treatment of metabolic disease and the method of preparation thereof, wherein said composition is prepared as a composite pharmaceutical agent which comprises calcitriol; which reduces the rate of spine fractures and increases bone density; alendronate, a bone resorption inhibitor, as two main active ingredients in an optimal mixing ratio to exert the greatest synergistic therapeutic effect; and adequate amount of other additives such as a resorption fortifier of alendronate.
    Type: Grant
    Filed: April 19, 2002
    Date of Patent: December 28, 2004
    Assignee: Yuyu Industrial Co., Ltd.
    Inventors: Sung An Kang, Kyung Hee Lee, Chung Shil Kwak, Chang Jong Kim, Yong Oh Lee
  • Patent number: 6824794
    Abstract: A water treatment agent and method of treating water to inhibit, reduce, or prevent the formation of algae and bacteria in a water body. The water treatment agent may include copper sulfate penta-hydrate and/or silver, di-sodium ethylene di-amine tetra-acetic acid dihydrate, a scale inhibitor, a shocking agent and a buffer agent. For instance, the treatment agent may include a composition of copper sulfate pentahydrate, di-sodium ethylene di-amine tetra-acetic acid, monopotassium phosphate or sulfuric acid, and potassium monopersulfate and 1-hydroxyethylidene-1,1-diphosphonic acid.
    Type: Grant
    Filed: May 31, 2002
    Date of Patent: November 30, 2004
    Assignee: Innovative Water Technologies, Inc.
    Inventors: Terry A. Ring, Tom Smolkov, M. Anthony Gamarra
  • Patent number: 6812214
    Abstract: In the present invention, it is discovered that a compound of formula (I) has a potent effect for treatment of osteoporosis, arthritis and ruptured disc: in which R1 represents hydrogen atom or alkyl group and R2 represents hydrogen atom r cinnamoyl group. Therefore, the compound of formula (I) can be used for prevention and treatment of osteoporosis, arthritis and ruptured disc. Thus, the present invention provides a pharmaceutical preparation containing as an effective component a compound of formula (I) in combination with a pharmaceutically acceptable auxiliary, diluent, isotonic agent, preservative, lubricant and solubilizing aid, which is formulated in the form of a pharmaceutically acceptable preparation and has a potent effect for osteoporosis, arthritis and ruptured disc.
    Type: Grant
    Filed: November 29, 2001
    Date of Patent: November 2, 2004
    Inventors: Joon Shik Shin, Sang Tae Kim, Yong Nam Han
  • Patent number: 6803057
    Abstract: An acidic aqueous hydrogen peroxide solution is provided with improved disinfectant activity. Concentrated solutions preferably contain up to about 8 wt./wt. % H2O2 and as-used concentrations contain about 0.5% wt./wt. % H2O2. The solution also contains from 0.05 to 8.0 wt./wt. % of at least one phosphorous-based acid, e.g. phosphoric acid and/or a phosphonic acid with from 1 to 5 phosphonic acid groups, and from 0.02 to 5 wt./wt. % of at least one anionic surfactant. The surfactant is selected from C8 to C16 alkyl aryl sulfonic acids, sulfonated C12 to C22 carboxylic acids, C8 to C22 alkyl diphenyl oxide sulfonic acids, naphthalene sulfonic acids, C8 to C22 alkyl sulfonic acids, and alkali metal and ammonium salts thereof, and alkali metal C8 to C18 alkyl sulfates, and mixtures thereof. Most preferably the solution has an emulsifier and/or hydrotrope, e.g. an alkylated sulfonated diphenyl oxide salt, an alkyl aryl polyoxyethylene surfactant, and/or a polyoxyethylene surfactant.
    Type: Grant
    Filed: December 28, 2001
    Date of Patent: October 12, 2004
    Assignee: Virox Technologies Inc.
    Inventors: Jose A. Ramirez, Michael J. Rochon
  • Patent number: 6794371
    Abstract: A method for preventing loss of bone mineral in mammals which method comprises administering to a mammal an amount of an aminoalkylenephosphonate which is effective to prevent or minimize loss of bone material density. The aminoalkylenephophonates of the present invention should have at least one R-N(Alk-PO3H2)2 group or at least two RRN-Alk-PO3H2 groups wherein R and R can be, same or different, aliphatic or cyclic moiety, and Alk is an alkylene group having from 1 to 4 carbon atoms.
    Type: Grant
    Filed: March 21, 2002
    Date of Patent: September 21, 2004
    Assignee: The Dow Chemical Company
    Inventor: R. Keith Frank
  • Patent number: 6784168
    Abstract: A synergistic biocide comprises a tris(hydroxymethyl)phosphine or a tetrakis (hydroxymethyl)phosphonium salt and at least one non-surfactant biopenetrant, such as a polymer or copolymer having a plurality of quaternary ammonium groups, a hydrotrope or a syntan, together optionally with a surfactant.
    Type: Grant
    Filed: September 5, 2000
    Date of Patent: August 31, 2004
    Assignee: Rhodia Consumer Specialties Limited
    Inventors: Christopher Raymond Jones, Robert Eric Talbot
  • Patent number: 6770620
    Abstract: The present invention relates to methods for prevention and treatment of bone-related or nutrition-related disorders using a GLP molecule or GLP activator either alone or in combination with another therapeutic. The present invention also encompasses methods of diagnosing or monitoring the progression of a disorder. The invention also encompasses methods of monitoring the effectiveness of treatment of the invention.
    Type: Grant
    Filed: September 17, 2001
    Date of Patent: August 3, 2004
    Assignee: Sanos Bioscience A/S
    Inventor: Dennis Bang Henriksen
  • Patent number: 6750340
    Abstract: The present invention is directed to particular bisphosphonate compounds, and in particular, to bisphosphonate conjugates that are useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis.
    Type: Grant
    Filed: December 7, 2000
    Date of Patent: June 15, 2004
    Assignee: MBC Research, Inc.
    Inventors: Nelly Padioukova, Sergey Mikhailov, H. B. F. Dixon, Grigorii Tzeitline
  • Patent number: 6699850
    Abstract: The present invention relates to oral compositions and methods for inhibiting bone resoprtion in a mammal while counteracting the occurrence of potentially adverse gastrointestinal effects. The compositions useful herein comprise the combination of a pharmaceutically effective amount of a nitrogen-containing bisphosphonate or a pharmaceutically-acceptable salt thereof and a pharmaceutically effective amount of an isoprenoid compound.
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: March 2, 2004
    Assignee: Merck & Co., Inc.
    Inventors: Alfred A. Reszka, Edward S. Scolnick
  • Patent number: 6696429
    Abstract: The invention relates to a process for treating lameness with an osseous, articular or osteoarticular component, comprising the administration, to a human or to an animal not suffering from arthritis or from fractures, of an effective amount of a bisphosphonic acid derivative of formula: in which: R1 represents a hydrogen atom, a halogen atom, a hydroxyl, an amino, a mono(C1-C4)alkylamino or a di(C1-C4) alkylamino; R2 represents a halogen atom, a linear alkyl comprising from 1 to 5 carbon atoms which is unsubstituted or substituted with a group chosen from a chlorine atom, a hydroxyl, an amino, a mono (C1-C4) alkylamino or a di(C1-C4) alkylamino; a (C3-C7) cycloalkylamino, or R2 represents a phenoxy, a phenyl, a thiol, a phenylthio, a chlorophenylthio, a pyridyl, a pyridyl-methyl, a 1-pyridyl-1-hydroxymethyl, an imidazolyl-methyl or a 4-thiomorpholinyl, of one of its pharmaceutically acceptable salts or of one of its hydrates.
    Type: Grant
    Filed: September 5, 2002
    Date of Patent: February 24, 2004
    Assignee: Ceva Sante Animale
    Inventors: Philippe Du Mesnil, Thierry Bardon, Dominique Thibaud
  • Patent number: 6692764
    Abstract: Pharmaceutical compositions of bisphosphonic acids, and salts thereof, are prepared by wet granulation tablet formulation. These pharmaceutical compositions are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease. These compositions are prepared without the addition of binder; instead, the drug itself acts as a binder.
    Type: Grant
    Filed: September 23, 2002
    Date of Patent: February 17, 2004
    Assignee: Merck & Co., Inc.
    Inventors: Ashok V. Katdare, Kenneth A. Kramer
  • Patent number: 6682718
    Abstract: The invention relates to an alveolar bone resorption inhibitor for use in topical injection by an alveolar mucosa injection method, which comprises a bisphosphonic acid derivative or a salt thereof as an active ingredient and to an alveolar bone resorption inhibitor for human periodontal tissue topical injection, which comprises a bisphosphonic acid derivative or a salt thereof in a concentration small enough so that local irritation to human periodontal tissues as the administrating site is acceptable but sufficient enough for expressing alveolar bone resorption inhibitory action by topical injection.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: January 27, 2004
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Naoto O'Uchi, Takaya Iwai, Taiji Yoshino, Hiroyuki Kanoh, Hiroyuki Motoie
  • Patent number: 6680307
    Abstract: The invention relates to use of ibandronic acid (1-hydroxy-3-(N-methyl-N-pentyl)aminopropyl-1,1-diphosphonic acid) or physiologically compatible salts or esters thereof for improving the osseointegration of cement-free anchored endoprostheses. Ibandronate or salts thereof is applied for a short time immediately after insertion of an endoprosthesis, with the surprising result that secondary stability of the implant is obtained in only 5 weeks or less after the operation.
    Type: Grant
    Filed: May 31, 2001
    Date of Patent: January 20, 2004
    Assignee: Roche Diagnostics GmbH
    Inventors: Frieder Bauss, Andreas A. Kurth
  • Patent number: 6677320
    Abstract: The present invention relates to a parenteral composition comprising a bisphosphonic acid or a pharmaceutically acceptable salt thereof (bisphosphonate) as active component and a pharmaceutically acceptable chelating agent, processes of the preparation of this composition, and methods of their use in the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, hypercalcemia of malignancy, and metabolic bone disease. The compositions are especially useful for improving the local tolerance of the active component when administered parenterally.
    Type: Grant
    Filed: January 11, 2001
    Date of Patent: January 13, 2004
    Assignee: Hoffmann-La Roches Inc.
    Inventors: Anke Diederich, Pierre Goldbach, Thomas Pfister
  • Patent number: 6670343
    Abstract: An agent for periodontal disease includes, as an active component, a methanebisphosphonic acid derivative or a hydrate thereof represented by the general formula (I): [wherein X, Y, m, n, The methanebisphosphonic acid derivative represented by the general formula (I) or a hydrate thereof according to the present invention has activities such as inhibitory effect on cell infiltration to the affected part associated with periodontal disease, and is useful for the prophylaxis or treatment of periodontal disease.
    Type: Grant
    Filed: May 29, 2001
    Date of Patent: December 30, 2003
    Assignee: Toray Industries, Inc.
    Inventors: Masatoshi Ito, Seiji Okazaki, Yuriko Kawai, Norio Kawabe
  • Patent number: 6649601
    Abstract: The present invention relates to a process for increasing the egg production and strengthening the eggshells of poultry, which comprises the administration to the animal of at least one bisphosphonic compound chosen from a bisphosphonic acid, a physiologically acceptable salt thereof, hydrates thereof and mixtures thereof.
    Type: Grant
    Filed: February 17, 2000
    Date of Patent: November 18, 2003
    Assignee: Ceva Sante Animale
    Inventors: Thierry Bardon, Dominique Thibaud
  • Patent number: 6638920
    Abstract: The present invention relates to compositions and methods of preventing or reducing the risk or incidence of skeletal injuries in horses. The present invention further relates to compositions and methods for alleviating pain associated with skeletal injuries in horses and to treating skeletal injuries in horses.
    Type: Grant
    Filed: July 11, 2001
    Date of Patent: October 28, 2003
    Assignee: Merck & Co., Inc.
    Inventor: Donald R. Thompson
  • Patent number: 6627221
    Abstract: The invention relates to a solid pharmaceutical form of administration containing a diphosphonic acid or a physiologically compatible salt thereof as the active substance, wherein the active substance is present in granulate form, optionally together with pharmaceutical adjuvants in the inner phase, and the outer phase contains a lubricant in the form of less than 5% by weight of stearic acid relative to the total weight of the form of administration.
    Type: Grant
    Filed: July 20, 2001
    Date of Patent: September 30, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rolf-Dieter Gabel, Walter Preis, Heinrich Woog
  • Patent number: 6624151
    Abstract: The invention concerns compounds CH3—R1—(CH1)2—R2 wherein: R1 is selected among a tertiary alcohol; a 1,2-diol; a halohydrine; an apoxide; an alkene; an aldehyde or an &agr;-hydroxyaldehyde; and R2 is selected among a methylenediphosphonate; a difluoromethylenediphosphonate; or a monofluoromethylenediphosphoneate. The invention also concerns the uses of said compounds as selective inhibitors of T&ggr;9&dgr;2 lymphocytes, and their uses, in particular for therapeutic purposes.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: September 23, 2003
    Assignees: Institut National de la Sante et de la Recherche Medicale, Sangstat Medical Corporation
    Inventors: Christian Belmant, Marc Bonneville, Marc Alix Peyrat, Jean-Jacques Fournie, Alan P. Kozikowski
  • Patent number: 6610682
    Abstract: A pharmaceutical composition comprising as its active ingredients one or more drugs selected from the group consisting of angiotensin II receptor antagonists and angiotensin converting enzyme inhibitors, and one or more insulin resistance improving agents exhibits excellent arteriosclerotic progress inhibitory effects, and is useful as a drug, particularly as a drug for the prevention or treatment of arteriosclerosis. The invention also provides a method for the treatment or prophylaxis of arteriosclerosis by administering in combination (i) at least one of said angiotensin II receptor antagonists or angiotensin converting enzyme inhibitors and (ii) one or more insulin resistance improving agents to a mammal suffering from or susceptible to arteriosclerosis.
    Type: Grant
    Filed: August 21, 2001
    Date of Patent: August 26, 2003
    Assignee: Sankyo Company, Limited
    Inventors: Yoshio Tsujita, Toshihiko Fujiwara, Toshio Sada, Naoyuki Maeda
  • Patent number: 6596710
    Abstract: The present invention is directed to a novel enteric-coated oral dosage form of a risedronate active ingredient comprised of a safe and effective amount of a pharmaceutical compostion which is comprised of a risedronate active ingredient and pharmaceutically-acceptable excipients. Said dosage forms prohibit the exposure of the risedronate active ingredient to the epithelial and mucosal tissues of the buccal cavity, pharynx, esophagus, and stomach and thereby protects said tissues from erosion, ulceration or other like irritation. Accordingly, the said dosage forms effect the delivery to the lower intestinal tract of said human or other mammal of a safe and effective amount of the risedronate active ingredient, and substantially alleviate the esophagitis or esophageal irritation which sometimes accompanies the oral administration of risedronate active ingredients.
    Type: Grant
    Filed: June 9, 2000
    Date of Patent: July 22, 2003
    Assignee: The Procter & Gamble Company
    Inventors: Richard John Dansereau, Russell Youker Mosher, Douglas Wayne Axelrod, William Kendall Sietsema
  • Patent number: 6593313
    Abstract: Methods and formulations for treating female sexual dysfunction are provided. A pharmaceutical composition formulated so as to contain a selected vasoactive agent is administered to the vagina, vulvar area or urethra of the individual undergoing treatment. Suitable vasoactive agents are vasodilators, including naturally occurring prostaglandins, synthetic prostaglandin derivatives, endothelial-derived relaxation factors, vasoactive intestinal polypeptide agonists, smooth muscle relaxants, leukotriene inhibitors, and others. The formulations are also useful for preventing the occurrence of yeast infections, improving vaginal muscle tone and tissue health, enhancing vaginal lubrication, and minimizing excess collagen deposition. A clitoral drug delivery device is also provided.
    Type: Grant
    Filed: July 13, 2001
    Date of Patent: July 15, 2003
    Assignee: Vivus, Inc.
    Inventors: Virgil A. Place, Leland F. Wilson, Paul C. Doherty, Jr., Mark S. Hanamoto, Alfred P. Spivack, Neil Gesundheit, Sean R. Bennett
  • Patent number: 6573252
    Abstract: The present invention relates to nitrate salts of compounds having therapeutic activity in bony disorders, such compounds being characterized in that they contain at least a reactive group capable of being salified with nitric acid.
    Type: Grant
    Filed: January 19, 2001
    Date of Patent: June 3, 2003
    Assignee: Nicox, S.A.
    Inventor: Piero Del Soldato
  • Patent number: 6558702
    Abstract: The present invention relates to a method for the sustained release in vivo of a biologically active agent comprising administering to a subject in need of treatment an effective amount of a sustained release composition comprising a biocompatible polymer having the biologically active agent incorporated therein, and a bisphosphonate wherein the bisphosphonate compound is present in an amount sufficient to modify the release profile of the biologically active agent from the sustained release composition. Pharmaceutical compositions suitable for use in the method of the invention are also disclosed.
    Type: Grant
    Filed: April 13, 2001
    Date of Patent: May 6, 2003
    Assignee: Alkermes Controlled Therapeutics, Inc.
    Inventors: James R. Dasch, M. Gary I. Riley
  • Patent number: 6555529
    Abstract: The present invention has the objective of offering drug for treating abnormalities in bone marrow which corrects the biological balance in the bone marrow, in particular which has the effect of suppressing inflammatory cell infiltration and suppressing cell growth-differentiation factor increase. The present invention relates to drug for treating abnormalities in bone marrow which has, as an effective component, a methanebisphosphonic acid derivative, ester thereof, medicinally acceptable salt thereof, or a hydrate of these. The methanebisphosphonic acid derivatives of the present invention show an outstanding bone marrow abnormality therapeutic effect, so efficacy can be expected in the prevention and treatment of rheumatoid arthritis, multiple myeloma, osteomyelitis and other bone marrow abnormalities. Furthermore, application can also be expected in the prevention and treatment of hypoplastic anaemia, myelocytic leukaemia and other such haematopoietic disorders.
    Type: Grant
    Filed: August 25, 1999
    Date of Patent: April 29, 2003
    Assignee: Toray Industries, Inc.
    Inventors: Yuriko Funaba, Junzo Koike, Masahiko Tanahashi, Seiji Okazaki, Masatoshi Ito
  • Patent number: 6555138
    Abstract: A drug delivery system for oral administration in solid dry form of greasy/oily/sticky substance(s) and pharmaceutically active substance(s) or pharmaceutically active substance(s) which itself/themselves is/are greasy/oily/sticky) characterized by having a plurality of solid, polymeric matrix beads comprising considerable amounts of greasy/oily/sticky substances and having fast release characteristics and a process for the preparation of such solid, polymeric matrix beads comprising greasy/oily/sticky substances.
    Type: Grant
    Filed: January 4, 1999
    Date of Patent: April 29, 2003
    Assignee: AstraZeneca AB
    Inventors: Christer Karlsson, Per Johan Lundberg, Adam Rosinski, Malin Söderbom
  • Patent number: 6544967
    Abstract: Disclosed are methods for inhibiting bone resorption in mammals while minimizing the occurrence of or potential for adverse gastrointestinal effects. Also disclosed are pharmaceutical compositions and kits for carrying out the therapeutic methods disclosed herein.
    Type: Grant
    Filed: January 8, 2001
    Date of Patent: April 8, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Anastasia G. Daifotis, Arthur C. Santora, II, A. John Yates
  • Patent number: 6541454
    Abstract: A method for treating patients having calcium related disorders includes using di- or tripeptide derivatives of bisphosphonates to enhance oral bioavailability of such compounds.
    Type: Grant
    Filed: December 31, 1997
    Date of Patent: April 1, 2003
    Assignee: Yissum Research Development Company of the Hebrew University Jerusalem
    Inventors: Eli Breuer, Gershon Golomb, Gordon L. Amidon, Ivan Sergeievitch Alferiev, Naama El-Hanany Rozen, Aviva Friedman-Ezra
  • Patent number: 6506733
    Abstract: Compounds of the formula: are provided, and are useful as cysteine protease inhibitors, particularly in the treatment of diseases such as osteoporosis or autoimmune disorders in which cathepsins K or S contribute to the pathology or symptomatolgy of the disease.
    Type: Grant
    Filed: March 15, 2000
    Date of Patent: January 14, 2003
    Assignee: Axys Pharmaceuticals, Inc.
    Inventors: Ann M. Buysse, Rohan V. Mendonca, James T. Palmer, Zong-Qiang Tian, Shankar Venkatraman
  • Patent number: 6482809
    Abstract: The present invention relates to the use of an active substance selected from the group consisting of tiludronic acid, one of its pharmaceutically acceptable salts, one of its hydrates and mixtures thereof, in the preparation of a medicinal product for preventing and treating osteoporosis in poultry.
    Type: Grant
    Filed: February 17, 2000
    Date of Patent: November 19, 2002
    Assignee: Ceva Sante Animale
    Inventors: Thierry Bardon, Dominique Thibaud
  • Patent number: 6476008
    Abstract: The invention relates to use of diphosphonic acids or physiologically compatible salts or esters thereof for preventive treatment of disturbances to ossary mineralization which may occur after operative extension of the urine bladder by augmentation plasties or replacement of the urine bladder by replacement plasties but often do not appear until years after the operation.
    Type: Grant
    Filed: December 27, 1999
    Date of Patent: November 5, 2002
    Assignee: Roche Diagnostics GmbH
    Inventors: Frieder Bauss, Drasko Brkovic
  • Patent number: 6468559
    Abstract: Oral dosage forms are provided for the administration of a bisphosphonic acid compound in the prevention and treatment of conditions involving calcium or phosphate metabolism, i.e., conditions associated with bone resorption such as osteoporosis, Paget's disease, periprosthetic bone loss, osteolysis, malignant hypercalcemia, metastatic bone disease, multiple myeloma, and periodontal disease. The dosage forms are either enterically coated capsules housing the drug in a liquid or semi-solid carrier, or enterically coated osmotically activated drug delivery devices.
    Type: Grant
    Filed: April 28, 2000
    Date of Patent: October 22, 2002
    Assignee: Lipocine, Inc.
    Inventors: Feng-Jing Chen, Mahesh V. Patel
  • Patent number: 6468963
    Abstract: Formulations and methods for reducing the unwanted toxicity and complications associated with treatments for diabetes mellitus. The formulations include co-formulations of an anti-diabetic agent and a toxicity reducing agent of the formula described in the specification. The methods include administration of effective amounts of the anti-diabetic agent and the toxicity reducing agent to safely treat the diabetic patient.
    Type: Grant
    Filed: May 1, 2000
    Date of Patent: October 22, 2002
    Assignee: BioNumerik Pharmaceuticals, Inc.
    Inventors: Frederick H. Hausheer, Aulma Parker, Susan E. Hamilton
  • Patent number: 6465443
    Abstract: Disclosed are methods for inhibiting bone resorption in mammals while minimizing the occurrence of or potential for adverse gastrointestinal effects. Also disclosed are pharmaceutical compositions and kits for carrying out the therapeutic methods disclosed herein.
    Type: Grant
    Filed: March 20, 2001
    Date of Patent: October 15, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Anastasia G. Daifotis, Arthur C. Santora, II, A. John Yates
  • Patent number: 6455514
    Abstract: The invention relates to a process for treating lameness with an osseous, articular or osteoarticular component, comprising the administration, to a human or to an animal not suffering from arthritis or from fractures, of an effective amount of a bisphosphonic acid derivative of formula: in which: R1 represents a hydrogen atom, a halogen atom, a hydroxyl, an amino, a mono(C1-C4)alkylamino or a di(C1-C4)alkylamino; R2 represents a halogen atom, a linear alkyl comprising from 1 to 5 carbon atoms which is unsubstituted or substituted with a group chosen from a chlorine atom, a hydroxyl, an amino, a mono(C1-C4)alkylamino or a di(C1-C4)alkylamino; a (C3-C7) cycloalkylamino, or R2 represents a phenoxy, a phenyl, a thiol, a phenylthio, a chlorophenylthio, a pyridyl, a pyridyl-methyl, a 1-pyridyl-1-hydroxymethyl, an imidazolyl-methyl or a 4-thiomorpholinyl, of one of its pharmaceutically acceptable salts or of one of its hydrates.
    Type: Grant
    Filed: November 16, 1998
    Date of Patent: September 24, 2002
    Assignee: Ceva Sante Animale
    Inventors: Philippe Du Mesnil, Thierry Bardon, Dominique Thibaud
  • Patent number: 6436913
    Abstract: Estramustine phosphate is shown to act as an inhibitor of bone resorption and can thus be used to treat, prevent or alleviate the symptoms of bone metastasis which arise due to said bone resorption.
    Type: Grant
    Filed: July 25, 2000
    Date of Patent: August 20, 2002
    Assignee: Pharmacia & Upjohn Company
    Inventor: Beryl Asp
  • Patent number: 6432931
    Abstract: The present invention relates to oral compositions and methods for inhibiting bone resoprtion in a mammal while counteracting the occurrence of potentially adverse gastrointestinal effects. The compositions useful herein comprise the combination of a pharmaceutically effective amount of a nitrogen-containing bisphosphonate or a pharmaceutically-acceptable salt thereof and a pharmaceutically effective amount of an isoprenoid compound.
    Type: Grant
    Filed: June 21, 1999
    Date of Patent: August 13, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Alfred A. Reszka, Edward S. Scolnick
  • Patent number: 6432932
    Abstract: Disclosed are methods for inhibiting bone resorption in mammals while minimizing the occurrence of or potential for adverse gastrointestinal effects. Also disclosed are pharmaceutical compositions and kits for carrying out the therapeutic methods disclosed herein.
    Type: Grant
    Filed: September 2, 1999
    Date of Patent: August 13, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Anastasia G. Daifotis, Arthur C. Santora, II, A. John Yates
  • Patent number: 6376477
    Abstract: The inhibition of natural bone formation experienced in the prophylaxis and/or treatment of bone resorption disease with a bisphosphonic acid or a pharmaceutically acceptable salt thereof is overcome by the concommitant administration of an agent that binds to the androgen receptor.
    Type: Grant
    Filed: December 19, 2000
    Date of Patent: April 23, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Azriel Schmidt, Shun-Ichi Harada, Gideon Rodan
  • Patent number: 6352970
    Abstract: This invention relates to methods for treating bone loss in a mammal by administering to the mammal a therapeutically effective amount of leptin or a leptin mimetic. This invention also relates to methods for treating bone fracture, enhancing bone healing following facial reconstruction, maxillary reconstruction or madibular reconstruction, enhancing long bone extension, enhancing the healing rate of a bone graft, enhancing prosthetic growth and inducing vertebral synostosis by administering a therapeutically effective amount of leptin or a leptin mimetic. This invention further relates to methods and compositions comprising leptin or a leptin mimetic and estrogen, a selective estrogen receptor modulator or a bisphonate for treating the above-recited diseases and conditions.
    Type: Grant
    Filed: February 19, 1999
    Date of Patent: March 5, 2002
    Assignee: Pfizer Inc.
    Inventors: HuaZhu Ke, Claire M. Steppan, Andrew Gordon Swick
  • Publication number: 20020010161
    Abstract: Disclosed are methods for inhibiting bone resorption in mammals while minimizing the occurrence of or potential for adverse gastrointestinal effects. Also disclosed are pharmaceutical compositions and kits for carrying out the therapeutic methods disclosed herein.
    Type: Application
    Filed: August 18, 1999
    Publication date: January 24, 2002
    Inventors: ANASTASIA G. DAIFOTIS, ARTHUR C. SANTORA, II, A. JOHN YATES
  • Patent number: 6333316
    Abstract: Disclosed are methods for inhibiting bone resorption in mammals while minimizing the occurrence of or potential for adverse gastrointestinal effects. Also disclosed are pharmaceutical compositions and kits for carrying out the therapeutic methods disclosed herein.
    Type: Grant
    Filed: August 18, 1999
    Date of Patent: December 25, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Anastasia G. Daifotis, Arthur C. Santora, II, A. John Yates
  • Patent number: 6331293
    Abstract: The present invention relates to compounds and, more particularly, to a class of compounds having specific quaternized amine based upon a dimer acid amido amine linked to specific phosphate esters. Dimer acid is a C-36 diacid having a cyclic structure and two amine groups that allow for the synthesis of a high molecular weight material phospholipid composition which is extremely substantitive to human skin and are well tolerated by human tissue making them suitable for use preparation of barrier products for personal care applications.
    Type: Grant
    Filed: June 4, 2001
    Date of Patent: December 18, 2001
    Assignee: Colonial Chemical INC
    Inventors: Scott Smith, Dean Smith, Anthony J. O'Lenick, Jr.