Abstract: This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamass) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.
Type:
Grant
Filed:
July 2, 1991
Date of Patent:
July 19, 1994
Assignee:
Vertex Pharmaceuticals, Inc.
Inventors:
David M. Armistead, Joshua S. Boger, Harold V. Meyers, Jeffrey O. Saunders, Roger D. Tung
Abstract: Fatty acid sanitizer concentrates and diluted final solutions are provided which include individual amounts of germicidally effective fatty acid, hydrotrope, strong acid sufficient to lower the pH of the final solutions to about 1-5, and a concentrate stabilizing weak acid component selected from the group consisting of propionic, butyric and valeric acids and mixtures thereof. The concentrate stabilizing component enhances the room and low temperature phase stability of the concentrates, even when used at very low levels typically ranging from 2.5%-15% by weight. Preferably, the fatty acid is a mixture of nonanoic and decanoic acids, whereas the strong acid is selected from the group consisting of orthophosphoric, sulfuric and mixtures thereof.
Abstract: A biologically active preparation for human or veterinary use for the selective blockade of opioid binding sites of the brain responsible for respiratory depression containing in a biologically active quantity the codeinone derivative of general formula (I) or its saltR.sup.1 means amino--, hydroxyl--, --NH--phenyl or --NH--CO--NH.sub.2 groups,R.sup.2 means a hydrogen atom or a hydroxyl group.The invention also covers a process for selective blocking the opioid binding sites of the brain responsible for respiratory depression by administering to a patient in need of an analgetic a preparation containing a codeinone derivative of general formula (I) or its salt preferably three times per day in doses of 2,5-5 mg.
Type:
Grant
Filed:
October 2, 1992
Date of Patent:
May 31, 1994
Assignee:
Alkaloida Chemical Company Ltd.
Inventors:
Anna Borsodi, Zsuzsa Furst, Sandor Hosztafi, Schafferne E. Varga, BuzaBeata, Tamas Friedmann, Sandor Benyhe, Maria Szucs
Abstract: A method is provided for protecting against and/or treating ulcerative gastrointestinal conditions, including anti-inflammatory drug-induced gastrointestinal ulcers, using a thromboxane A.sub.2 receptor antagonist. In addition, a combination is provided which includes a thromboxane A.sub.2 receptor antagonist and an anti-inflammatory agent which combination may be used to treat inflammatory conditions, such as arthritis, while inhibiting formation of and/or treating gastrointestinal ulcers.
Type:
Grant
Filed:
December 23, 1992
Date of Patent:
May 17, 1994
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Bernard Rubin, Martin L. Ogletree, Eugene H. O'Keefe, A. K. Gunnar Aberg
Abstract: The present invention involves a method for prophylaxis or treatment of an animal for systemic hypotension induced by endotoxin and/or a biological response modifier such as the cytokines, IFN, TNF, IL-1 or IL-2 and the like. Said method involves administering, preferably intravascularly, a therapeutically effective amount of dobutamine and an inhibitor of nitric oxide formation from arginine. Although preferable administration is intravascular, it is contemplated that other parenteral administration routes such as intraperitoneal, intramuscular or subdermal injection, for example, may prove useful. Enteral or topical administration of arginine analogs may also prove beneficial under certain clinical conditions.
Type:
Grant
Filed:
May 29, 1992
Date of Patent:
May 17, 1994
Assignees:
Board of Regents, the University of Texas System, Cornell Research Foundation, Inc.
Inventors:
Robert G. Kilbourn, Steven S. Gross, Owen W. Griffith
Abstract: This invention provides new uses for the drugs of the thioureylene class and thiabendazole. These new uses include methods of treatment for a variety of conditions and diseases, including psoriasis, other atopic dermatoses and inflammatory conditions having an autoimmune basis, as well as other autoimmune diseases, including rheumatic disease, and transplant rejection.
Abstract: Acidic polysaccharide esters containing carboxylic groups are useful for protecting against and curing ulcers of the gastro-enteric system. These esters include choline esters with acidic polysaccharide selected from the group consisting of hyaluronic acid, alginic acid, gellan, oxidized cellulose, oxidized chitin, carboxy-hydrocarbyl-cellulose, carboxy-hydrocarbyl-starch and carboxy-hydrocarbyl-chitin, wherein the term hydrocarbyl means the residue of a hydrocarbon selected from the group consisting of by alkyl, aralkyl and cycloalkyl.
Abstract: Mycalamide compounds are derived from marine sponges of the genus Mycale or prepared by synthetic methods. These compounds, and pharmaceutical compositions containing them as active ingredients, are useful as immunomodulatory agents.
Type:
Grant
Filed:
December 14, 1992
Date of Patent:
March 29, 1994
Assignee:
Harbor Branch Oceanographic Institution, Inc.
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
Abstract: The present invention relates to the use of known substituted 2-cyclohexene derivatives in the control of diseases, in particular bacterial infections and mycoses.
Type:
Grant
Filed:
May 14, 1993
Date of Patent:
March 22, 1994
Assignee:
Bayer Aktiengesellschaft
Inventors:
Franz Kunisch, Peter Babczinski, Dieter Arlt, Manfred Plempel
Abstract: A process for preventing or ameliorating the myelosuppression which can occur in a mammal such as a human cancer patient being treated with a platinum-free antineoplastic drug is provided, comprising administering an effective dosage of a dithiocarbamate compound to said mammal, preferably subsequent to administration of the cytotoxic drug.
Type:
Grant
Filed:
July 30, 1992
Date of Patent:
March 15, 1994
Assignee:
University of Rochester
Inventors:
Richard F. Borch, Therese K. Schmalbach
Abstract: A method of decreasing the toxicity of chemical therapeutic agents administered in cancer chemotherapy including adminstration to a patient undergoing chemotherapy. This reduction in toxicity can be accomplished by administering an effective amount of S-3-(3-methylaminopropylamino)propyl dihydrogen phosphorothioate. Methods of inducing mucolytic activity and reducing toxicity of acetominophen overdose are also discussed. Such activities are induced through the administration of S-3-(3-methylaminopropylamino)propyl dihydrogen phosphorothioate.
Abstract: Disclosed herein is a method for preventing deterioration of an industrial material by using an azole derivative represented by the following formula ##STR1## wherein X means a halogen atom or a C.sub.1 -C.sub.5 alkyl, haloalkyl, phenyl, cyano or nitro group, n stands for 0 or an integer of 1-5, A denotes a nitrogen atom or CH, R.sub.1 and R.sub.2 mean individually a hydrogen atom or a C.sub.1 -C.sub.5 alkyl group, R.sub.3 denotes a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group, and when n is an integer of 2-5, Xs may be the same or different. A biocidal composition for the method is also disclosed.
Abstract: The invention herein is a method of protecting against renal damage in a patient receiving carboplatin, cyclosporine A or cisplatin comprising administering to said patient the following mixture of amino acids consisting of glycine, L-alanine, L-serine, L-threonine, L-valine, L-leucine, L-isoleucine and L-proline.
Abstract: A method of inhibiting tissue damage in warm blooded animals related to reperfusion of tissues after extended periods of ischemia is presented. The method comprises treatment prior to a planned ischemic event or up to six hours after an unplanned ischemic event with an effective amount of monophosphoryl lipid A or 3-deacylated monophosphoryl lipid A. Pharmaceutical compositions for the treatment are also disclosed.
Abstract: New organic nitrate compounds, formed by condensing a nitrato alkanoic acid with a sulfur-containing amino acid or peptide followed by the reaction of the resulting product with an amino acid, N-acylamino acid, peptide or an N-acyl peptide to produce a thio ester thereof, which prevent nitrate tolerance or overcome existing tolerance and which are useful for the treatment of cardiac diseases including circulatory diseases, coronary dilation, high blood pressure, cardiac insufficiency and for dilating the peripheral vessels.
Type:
Grant
Filed:
April 5, 1991
Date of Patent:
February 8, 1994
Assignee:
Schwarz Pharma AG
Inventors:
Klaus Sandrock, Eike Noack, Edgar Fritschi, Ralf Kanzler, Martin Feelisch
Abstract: Compounds of the general formula (2): ##STR1## wherein X is a hydrogen atom or a hydroxyl group, Y is a hydrogen atom or a hydroxyl group and R is an alkyl group of 1 to 4 carbon atoms, have anti-fungal activity, especially against organisms selected from Candida spp. and the athlete's foot organism Trichophyton mentagrophytes and the ringworm organism Microsporum audonii. Further, the compounds wherein X and R are hydrogen atoms and Y is a hydroxyl group (or its non-toxic salts) are useful against Microsporum audonii.
Abstract: The present invention provides a method for combatting damage to a body tissue contacted to an alkali. The method comprising administering CO.sub.2 to the subject in an amount sufficient to produce an acidotic state in the tissue, the acidotic state serving to prevent alkali damage to the tissue. In a preferred embodiment of the invention, a subject is caused to inhale a mixture of 95%O.sub.2 and 5%CO.sub.2 for brief periods of time, followed by periods of breathing room air. The invention is particularly useful for treating alkaline injury of the esophagus caused by ingestion of alkaline material.
Type:
Grant
Filed:
November 25, 1991
Date of Patent:
November 16, 1993
Assignee:
University of North Carolina at Chapel Hill