Abstract: The invention relates to the use of an AT1 receptor antagonist or or an AT2 receptor modulator, respectively, or a pharmaceutically acceptable salt thereof, for producing a pharmaceutical preparation for the treatment of conditions or diseases associated with the increase of AT1 receptors in the sub-epithelial area or increase of AT2 receptors in the epithelia.
Type:
Grant
Filed:
December 21, 1999
Date of Patent:
October 15, 2002
Assignee:
Novartis AG
Inventors:
Gillian Rosemary Bullock, Marc De Gasparo, Sabina Maria Ganter
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
Abstract: This invention is related with the obtention of a new natural mixture composed by higher primary aliphatic alcohols, eventually in an extended range of 22 to 38 carbon atoms, specially those between 24 and 34 carbon atoms and more specially those of 24, 26, 28, 30, 32 and 34 carbon atoms. This mixture shows a relative composition of each alcohol that is highly reproducible from batch to batch and is obtained from bee wax.
This natural mixture has been used, with efficacy, as an active principle, in different pharmaceutical formulations used against ulcer, and/or protector of the gastric and duodenal mucose, and shows antiinflamatory activity administered by topical, oral or parenteral route.
Type:
Grant
Filed:
September 22, 2000
Date of Patent:
October 15, 2002
Assignee:
Laboratories Dalmer SA
Inventors:
Juan Magraner Hernandez, Abilio Laguna Granja, Rosa Mas Ferreiro, Maria de Lourdes Arruzazabala Valmaña, Daysi Carvajal Quintana, Vivian Molina Sánchez, Suria Valdés García, Maritza Díaz Gómez
Abstract: The use of orally administered L-arginine in conjunction with a topical preparation for producing enhanced blood flow in tissue thus causing beneficial effects such as warming cold tissue of the hands and feet, promoting hair growth on bald scalp tissue, promoting healing of superficial Ilcers such as leg ulcers in persons with diabetes, and overcoming male erectile failure (impotence) is disclosed. Specifically, use of orally administered L-arginine in conjunction with this is topical preparation provides local delivery of the amino acid L-arginine, an important biological precursor to the main substance which is responsible for relaxation of blood vessels permitting enhancement of blood flow. In the preferred embodiments, the L-arginine is provided so that it can be topically applied to the cold tissue. The preparation also contains an agent which aids in the transfer of L-arginine into the tissue.
Abstract: An article and method for reducing somnolence in a patient receiving tizanidine therapy. Tizanidine may be administered in the form of an immediate release multiparticulate composition at or around the time food is consumed. The composition may be packaged in a container for distribution.
Abstract: The present invention focuses upon a method for inhibiting bone resorption. This method involves administering a 5-lipoxygenase inhibitor to a subject in an amount inhibiting the effects of an osteoclast-stimulating factor. When the production of the osteoclast-stimulating factors such as PTH, PTHrp, IL-1, TNF, LT, 1,25(OH)2D3 or other factors which may stimulate the production of 5-LO metabolites via the 5-lipoxygenase pathway is inhibited, bone resorption markedly declines. The direct osteoclast-stimulating factors include leukotriene, peptidoleukotriene and 5-hydroxyeicosatetraenoic acid. Other factors yet to be identified or previously known may also be 5-lipoxygenase metabolites that stimulate bone resorption. While 5-lipoxygenase inhibitors may be substrate analogs or allosteric inhibitors, a substance which inhibits the activity of this enzyme may utilize other mechanisms (e.g., inhibition of 5-LO biosynthesis) and nevertheless function to inhibit bone resorption.
Type:
Grant
Filed:
May 8, 2000
Date of Patent:
September 24, 2002
Assignee:
Board of Regents, The University of Texas System
Inventors:
Lynda F. Bonewald, G. R. Mundy, Wolf E. Gallwitz
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
Abstract: This invention provides a method of contraception which comprises administering to a female of child beating age for a combination of a progestin at a daily dosage of 40-500 &mgr;g trimegestone, 250 &mgr;g-4 mg dienogest, or 250 &mgr;g-4 mg drospirenone, and an estrogen at a daily dosage equivalent in estrogenic activity to 10-20 &mgr;g ethinyl estradiol for 23-25 days beginning on day 1 of the menstrual cycle, and wherein the same dosage of the progestin and estrogen combination is administered in each of the 23-25 days.
Abstract: The present invention relates to a method of feeding carnitine supplemented diets to sows during the period of gestation or during both gestation and lactation periods. The method enhances pork productivity by increasing litter and pig birth and weaning weights, reducing the number of stillborn pigs and increasing the number of pigs born alive in the subsequent reproductive cycle. Sow diets of this invention include carnitine, such as L-carnitine or L-carnitine salts. Carnitine is generally added to the swine feed formulation in the amount of from about 5 to about 5,000 ppm.
Type:
Grant
Filed:
July 18, 2000
Date of Patent:
September 17, 2002
Assignees:
Lonza Inc., Kansas State University Research Foundation
Inventors:
Stephen A. Blum, Kevin Q. Owen, Jim L. Nelssen, Robert D. Goodband, Michael D. Tokach, Rene A. Blum, Robert E. Musser
Abstract: The present invention relates to methods of using peptide-like compounds, e.g., aminocarboxylic acid amide derivatives, to bias the immune system toward producing, enhancing, or maintaining a polarized Th1 response, and to methods for treating diseases that improve by creating a Th1 response. The invention also relates to a method of treating diseases associated with elevated soluble TNF alpha levels by administering beta-alethine together with NAC to reduce soluble TNF alpha, and to a pharmaceutical composition comprising same. The present compounds can be used to modulate cytokines including IFN-gamma and IL-10.
Abstract: Chemical compounds that are derivatives of indeno[1,2-c]-, naphtho[1,2-c]- and benzo[6,7]cyclohepta[1,2-c]pyrazole are inhibitors of tyrosine kinase activity. Several of the tyrosine kinases, whose activity is inhibited by these chemical compounds, are involved in hyperproliferative, angiogenic or in vascular hyperpermeability processes. Thus, these chemical compounds can ameliorate disease states where tumor formation, metastasis, angiogenesis, vascular hyperpermeability or endothelial cell proliferation is a factor.
Type:
Grant
Filed:
April 3, 2000
Date of Patent:
September 17, 2002
Assignee:
BASF Aktiengesellschaft
Inventors:
Lee D. Arnold, Yajun Xu, Teresa Barlozzari
Abstract: A controlled release microcapsulate pharmaceutical formulation for burst-free, sustained, programmable release of hydrophocib bioactive agent over a duration from 24 hours to 100 days comprising: and a blend of end-capped uncapped biocompatible, biodegradable poly(lactide/glycolide).
Type:
Grant
Filed:
August 21, 1997
Date of Patent:
September 10, 2002
Assignee:
The United States of America as represented by the Secretary
of the Army
Inventors:
Noelle Christine Vook, Elliott Jacob, Jean A. Setterstrom, John van Hamont, William Vaughan, Ha Duong
Abstract: The invention provides a method for treating vaginal dryness by increasing hydration and lubrication of vaginal and cervical tissues in a subject in need of such treatment. The method comprises administering to the subject a nicotinic acetylcholine receptor agonist such as nicotine and its analogs, transmetanicotine and its analogs, epibatidine and it analogs, lobeline and its analogs, pyridol derivatives, para-alkylthiophenol derivatives, and imidacloprid and its analogs, in an amount effective to stimulate cervical and vaginal secretions. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the formulation include: topical administration via a liquid, gel, cream, ointment, foam, pessary, or tablet; systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, suppository form, or transdermal form. The invention is useful for treating vaginal dryness and vulvar pain.
Abstract: This invention relates to the use of angiotensin II antagonists in treating or preventing the development of disease conditions associated with impaired neuronal conduction velocity, such as diabetic neuropathy, as well as their use in the manufacture of a medicament for use in such treatment. The invention also concerns pharmaceutical compositions containing an angiotensin II antagonist together with one or more other agents known to be of value in treating or preventing the development of disease conditions associated with impaired neuronal conduction velocity.
Type:
Grant
Filed:
January 5, 1995
Date of Patent:
September 10, 2002
Assignee:
Zeneca Limited
Inventors:
Frank Carey, Alexander Anthony Oldham, Norman Eugene Cameron, Mary Anne Cotter
Abstract: 8,8a-Dihydroindeno[1,2-d]thiazole derivatives which carry in the 2-position a substituent having a sulfonamide structure or sulfone structure; processes for their preparation and their use as medicaments
The invention relates to polycyclic dihydrothiazoles and to their physiologically acceptable salts and physiologically functional derivatives.
Compounds of formula I,
in which the radicals are as defined above, and their physiologically acceptable salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.
Type:
Grant
Filed:
January 17, 2002
Date of Patent:
September 3, 2002
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Gerhard Jaehne, Hans Jochen Lang, Matthias Gossel, Martin Bickel
Abstract: This invention provides a method of treating obesity, generalized anxiety disorder, post-traumatic stress disorder, late luteal phase disphoric disorder (premenstrual syndrome), attention deficit disorder, with and without hyperactivity, Gilles de la Tourette syndrome, bulimia nervosa or Shy Drager Syndrome in a mammal by administering to the mammal an effective amount of a hydroxycycloalkanephenethyl amine of the following structural formula:
in which A is a moiety of the formula
where
the dotted line represents optional unsaturation;
R1 is hydrogen or alkyl;
R2 is alkyl;
R4 is hydrogen, alkyl, formyl, or alkanol;
R5 and R6 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, cyano, nitro, alkylmercapto, amino, alkylamino, dialkylamino, alkanamido, halo, trifluoromethyl, or taken together, methylene dioxy;
R7 is hydrogen or alkyl; and
n is 0, 1, 2, 3, or 4;
or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
January 25, 2001
Date of Patent:
September 3, 2002
Assignee:
Wyeth
Inventors:
Richard L. Rudolph, Albert T. Derivan, G. Virginia Upton
Abstract: A compound which is an antagonist of platelet activating factor (PAF-antagonist) or a structurally related compound thereof not having PAF-antagonistic activity can be used for decreasing the plasma level of lipoprotein(a) and/or increasing the plasma level of high-density lipoprotein. The compound may be an azepine derivative, especially a benzo- or thienotriazolo-diazepine derivative, a diphenyl-tetrahydrofuran or diphenyldioxolane derivative or a tetrahydrofuran phospholipid analogue.
Type:
Grant
Filed:
April 17, 1998
Date of Patent:
September 3, 2002
Assignee:
Nederlandse Organisatie voor Toegepast - Natuurweten
Schappelijk Onderzoek (TNO)
Inventors:
Johannes Marinus Gerardus Princen, Take Kooistra
Abstract: Novel uses of biologically active bis-heterocyclic e.g. bis-indole alkaloid compounds which have improved activity are disclosed. Pharmaceutical compositions containing the compounds are also disclosed. Specifically, the novel Utility pertains to the anti-immunogenic and neurogenic inflammatory properties exhibited by the bis-indole compounds and their analogs.
Type:
Grant
Filed:
July 27, 2001
Date of Patent:
September 3, 2002
Assignees:
Harbor Branch Oceanographic Instutition, Inc., Regents of the University of California
Inventors:
Amy E. Wright, Ralph-Heiko Mattern, Robert S. Jacobs
Abstract: Blood cholesterol levels are correlated with production of amyloid &bgr; protein (A&bgr;), and are predictors of populations at risk of developing AD. Methods for lowering blood cholesterol levels can be used to decrease production of A&bgr;, thereby decreasing the risk of developing AD. The same methods and compositions can also be used for treating individuals diagnosed with AD. Methods include administration of compounds which increase uptake of cholesterol by the liver, such as the administration of HMG CoA reductase inhibitors, administration of compounds which block endogenous cholesterol production, such as administration of HMG CoA reductase inhibitors, administration of compositions which prevent uptake of dietary cholesterol, and administration of combinations of any of these which are effective to lower blood cholesterol levels. Methods have also been developed to predict populations at risk, based on the role of cholesterol in production of A&bgr;.
Abstract: Combinations of a GABAA alpha 5 inverse agonist and a COX-2 inhibitor, NSAID, estrogen or vitamin E are disclosed for treating neurodegenerative conditions such as Alzheimer's Disease.