Ether Oxygen Single Bonded To Carboxylic Acid, Percarboxylic Acid Or Salt Thereof Through An Acyclic Carbon Or Acyclic Carbon Chain Patents (Class 514/571)
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Patent number: 5506226Abstract: Compounds structurally related to ethacrynic acid are described. The compounds are useful for controlling intraocular pressure. Unlike ethacrynic acid, the compounds of the present invention are capable of effectively penetrating the cornea. Methods of controlling intraocular pressure via topical application of one or more of the compounds to the eye and topical ophthalmic compositions useful in the treatment of glaucoma are also described.Type: GrantFiled: April 19, 1993Date of Patent: April 9, 1996Assignee: Alcon Laboratories, Inc.Inventor: Jesse A. May
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Patent number: 5490992Abstract: The present invention is generally related to a product and a process to reduce the microbial contamination of processed meat and is particularly related to a product and a process to disinfect poultry carcasses using a disinfectant composition containing a fatty acid monoester, an acid or chelating agent, and a food grade surfactant. These components may be combined in either an aqueous or nonaqueous vehicle as desired. The present combination is effective against pathogenic and undesired bacteria. Advantageously, the present composition does not detrimentally alter the taste, texture, color, odor or appearance of the processed meat.Type: GrantFiled: March 22, 1995Date of Patent: February 13, 1996Assignee: Minnesota Mining and Manufacturing CompanyInventors: Jeffrey F. Andrews, Janet F. Munson
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Patent number: 5478857Abstract: This invention provides methods for the treatment or prevention of Alzheimer's disease in a mammal which comprises administering to a mammal in need thereof an effective amount of an inhibitor of phospholipase A.sub.2. This invention also provides a series of compounds which are useful as inhibitors of phospholipases A.sub.2, especially cytosolic phospholipase A.sub.2.Type: GrantFiled: December 23, 1993Date of Patent: December 26, 1995Assignee: Eli Lilly and CompanyInventors: James A. Clemens, Michael J. Sofia, Diane T. Stephenson
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Patent number: 5460833Abstract: The present invention is generally related to a product and a process to reduce the microbial contamination of processed meat and is particularly related to a product and a process to disinfect poultry carcasses using a disinfectant composition containing a fatty acid monoester, an acid or chelating agent, and a food grade surfactant. These components may be combined in either an aqueous or nonaqueous vehicle as desired. The present combination is effective against pathogenic and undesired bacteria. Advantageously, the present composition does not detrimentally alter the taste, texture, color, odor or appearance of the processed meat.Type: GrantFiled: March 22, 1995Date of Patent: October 24, 1995Assignee: Minnesota Mining and Manufacturing CompanyInventors: Jeffrey F. Andrews, Janet F. Munson
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Patent number: 5453443Abstract: Compounds having the formula I: ##STR1## are inhibitors of the PLA.sub.2 s enzymes. These compounds are useful as anti-allergic, anti-asthmatic, they are also useful in treating various inflammatory diseases such as rheumatoid arthritis, osteoarthritis, bursitis, psoriasis; immunoinflammatory disorders such as contact dermatitis, irritable bowel disease and the like.Type: GrantFiled: July 20, 1994Date of Patent: September 26, 1995Assignee: Merck Frosst Canada, Inc.Inventors: Helene Perrier, Petpiboon Prasit, Ian Street, Zhaoyin Wang
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Patent number: 5444090Abstract: The rate and character of mammalian hair growth is altered by the topical application to the skin of a composition containing an organic inhibitor of the enzyme L-asparagine synthetase.Type: GrantFiled: March 11, 1994Date of Patent: August 22, 1995Inventor: Gurpreet S. Ahluwalia
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Patent number: 5434186Abstract: Compounds of the formula ##STR1## wherein X is O or CH.sub.2 ; Y is O, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, or --OCH.sub.2 C.sub.6 H.sub.4 --;Z is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--;f, h, k, m and t, independently, are 0 or 1;n is an integer from 1 to 12;R.sup.1 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, or aralkyl; and A is B or --O--B, wherein B is a mono-, di- or tricyclic aromatic or heteroaromatic moiety substituted by the group --COR.sup.2, --(O).sub.t --(W).sub.s --COR.sup.2 or --(CH.dbd.CH).sub.p COR.sup.2 and which may also contain up to 4 additional substituents selected, independently, from the group consisting of halogen, cyano, lower alkyl, lower alkoxy, sulfonamido, alkanoyl, aroyl, --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, provided that no more than one of said substituents is --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, and wherein E is COR.sup.Type: GrantFiled: September 28, 1993Date of Patent: July 18, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Noal Cohen, Ferdinand K. Lee, Keith A. Yagaloff
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Patent number: 5422372Abstract: This invention provides an improved therapeutic method which comprises administering to a mammal a therapeutic agent and 5-(2,5-dimethylphenoxy)-2,2-dimethyl-pentanoic acid, or a structural analog thereof, in an amount effective to improve the efficacy of the therapeutic agent. Also provided by this invention is an improved therapeutic method which comprises administering to a mammal a therapeutic agent and 5-(2,5-dimethylphenoxy)-2,2-dimethyl-pentanoic acid, or a structural analog thereof, in an amount effective to improve the efficacy of the therapeutic agent. Further provided by this invention is a method of treating an intracellular bacterial infection which comprises contacting the infected cell with an effective amount of a therapeutic agent and with an effective amount of 5-(2,5-dimethylphenoxy)-2,2-dimethyl-pentanoic acid, or a structural analog therof, effective to treat an intracellular bacterial infection.Type: GrantFiled: June 15, 1993Date of Patent: June 6, 1995Assignee: The Trustees of Columbia University in the City of New YorkInventors: Samuel C. Silverstein, Harold C. Neu, Charles Cao
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Patent number: 5352702Abstract: A method for treating glaucoma in an eye of a human patient is disclosed. The method comprises the step of chronically, orally administering to the patient an unsaturated ketone derivative of an aryloxyacetic acid in an amount sufficient to safely and effectively lower intraocular pressure in the human eye. The unsaturated ketone derivative is selected from the group consisting of ethacrynic acid, an analog of ethacrynic acid, an ester derivative of ethacrynic acid, an ester derivative of an ethacrynic acid analog, an amide derivative of ethacrynic acid, an amide derivative of an ethacrynic acid analog, a pharmaceutically acceptable salt of ethacrynic acid, a pharmaceutically acceptable salt of an ethacrynic acid analog, a pharmaceutically acceptable salt of the ester derivative, a pharmaceutically acceptable salt of the amide derivative, and mixtures thereof. The amount administered is preferably between about 50 mg and about 75 mg two times per day.Type: GrantFiled: February 4, 1993Date of Patent: October 4, 1994Inventor: Marshall N. Cyrlin
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Patent number: 5344843Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.2 ' X, Y, Z, A, B, Q and n are as described herein. Their pharmaceutically acceptable salts, and when appropriate, enantiomers, racemates, diastereomers or mixtures thereof or geometric isomer or mixtures thereof, and pharmaceutically acceptable salts thereof. The compounds of formula I inhibit enzyme carnitine acyltransferase 1 (CAT-1) and are therefore useful in the prevention of injury to ischemic tissue, and can limit infarct size, improve cardiac function and prevent arrhythmias during and following a myocardial infarction.Type: GrantFiled: March 13, 1992Date of Patent: September 6, 1994Assignee: Hoffman-La Roche Inc.Inventors: Robert W. Guthrie, John G. Mullin, Jr., David F. Kachensky, Richard W. Kierstead, Jefferson W. Tilley, Guy P. Heathers, Alan J. Higgins, Ronald A. LeMahieu
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Patent number: 5306731Abstract: This invention is directed to improved treatment for glaucoma. It involves delivering to the eye molecules which increase the outflow of aqueous humor, in conjunction with masking agents. The masking agents reduce the side effects of the therapeutically active molecules by masking the sulfhydryl reactive groups on the molecules. The masking agents can be delivered separately from the molecules, or as adducts of the molecules.Type: GrantFiled: March 14, 1991Date of Patent: April 26, 1994Assignee: Massachusetts Eye and Ear InfirmaryInventor: David L. Epstein
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Patent number: 5302635Abstract: The invention is directed to a method and an arrangement continuously producing a rubber base compound and a rubber end compound in a single stage for vehicle tires, drive belts, conveyor belts as well as for industrial rubber products. The rubber base compound and the rubber end compound are produced continuously in one and the same mixing arrangement which includes a twin-screw extruder.Type: GrantFiled: December 13, 1991Date of Patent: April 12, 1994Assignee: Hermann Berstorff Maschinenbau GmbHInventors: Heinz Brinkmann, Gerd Capelle
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Patent number: 5298506Abstract: The invention relates to the administration of guanylate cyclase inhibitors, such as methylene blue, for the treatment of septic shock, cardiogenic shock, hypovolemic shock, obstructive shock, neuropathic shock and hypotension caused by excessive doses of nitrovasodilators. The invention also relates to the use of other redox dyes, such as toluidine blue, neutral red, tetrazolium salts, chloranil and dichlorophenolindophenol for the treatment of shock.Type: GrantFiled: May 8, 1992Date of Patent: March 29, 1994Assignee: Brigham and Women's HospitalInventors: Jonathan Stamler, Joseph Loscalzo
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Patent number: 5290812Abstract: Phenoxyalkylcarboxylic acid derivatives represented by the following formula (I) ##STR1## having a strong and selective leukotriene antagonistic action and useful for prophylaxis and therapy of allergic diseases as asthma and processes of preparing the same.Type: GrantFiled: December 30, 1991Date of Patent: March 1, 1994Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Mitsuo Ohashi, Toshio Tanaka, Norihisa Ishikawa, Tetsuya Kishi
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Patent number: 5272178Abstract: The present invention relates to compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl, phenyl, or hydrogen; R.sup.3 represents hydrogen or alkyl; X represents O, S or (CH.sub.2).sub.m wherein m is 1 or 2; A represents O or S(O).sub.n wherein n is 0, 1, or 2; p is an integer from 0 to 4; and R represents alkyl; OH; OR.sup.4 wherein R.sup.4 is alkyl; or NR.sup.5 R.sup.6 wherein R.sup.5 is hydrogen or alkyl, and R.sup.6 is hydrogen, alkyl, heterocyclealkyl, substituted heterocyclealkyl, cycloalkyl, substituted cycloalkyl, phenyl, substituted phenyl, phenylalkyl, or substituted phenylalkyl, or NR.sup.5 R.sup.6 together form a heterocyclic ring which may optionally be substituted; or (CH.sub.2).sub.t COOR.sup.7 wherein t is an integer from 1 to 4 and R.sup.7 is hydrogen or alkyl; and the pharmaceutically acceptable salts thereof. The compounds are inhibitors or stimulators of superoxide generation.Type: GrantFiled: April 8, 1993Date of Patent: December 21, 1993Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis
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Patent number: 5238832Abstract: Novel aryl aliphatic acids or derivatives thereof of the general formulaR--(C.sub.x --C.sub.y)--(C.sub.m H.sub.2m)--G--C(R.sup.1).sub.2 --Ar--(C.sub.n H.sub.2n)--COOR.sup.2are described which exhibit inhibiting activity against 12-lipoxygenase. The compounds are characterized by having a low level of toxicity. Also included are salts and esters of the aliphatic acids.Type: GrantFiled: June 8, 1992Date of Patent: August 24, 1993Assignees: Board of Governors of Wayne State University, Vanderbilt UniversityInventors: Carl R. Johnson, Gilles Gorins, Kenneth V. Honn, Lawrence J. Marnett
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Patent number: 5232945Abstract: A method of using certain 3-aryl-2-hydroxypropionic acid derivatives and analogs in the treatment of hypertension.Type: GrantFiled: July 20, 1992Date of Patent: August 3, 1993Assignee: Pfizer Inc.Inventor: Bernard Hulin
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Patent number: 5179097Abstract: Novel choline salts of non-steroidal anti-inflammatory carboxylic acids and anti-lipidemic carboxylic acids are described. Additionally, blends of choline salts with the above carboxylic acids are also described. The new salts and compositions offer new therapeutic advantages.Type: GrantFiled: June 10, 1991Date of Patent: January 12, 1993Inventor: Isaac A. Angres
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Patent number: 5153222Abstract: The present invention is concerned with methods for the prophylaxis, treatment and diagnosis of pulmonary hypertension which comprise the administrative of an effective amount of a compound of formula (I) ##STR1## wherein a is an integer of from 1 to 3; X and Y, which may be the same or different, are selected from --O-- and --CH.sub.2 --;R is --(CH.sub.2).sub.5 R.sup.1 wherein R.sup.1 is hydrogen or methyl, or R is cyclohexyl, orR is --CH(CH.sub.3)CH.sub.2 C.tbd.CCH.sub.3 ; andthe dotted line represents an optional double bond;or of a physiologically acceptable salt or acid derivative thereof.Medicaments and diagnostic aids for use in the methods of the invention are also within the scope of the invention.Type: GrantFiled: June 14, 1991Date of Patent: October 6, 1992Assignee: Burroughs Wellcome Co.Inventors: Anjaneyulu S. Tadepalli, Walker A. Long, James W. Crow, Kenneth B. Klein
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Patent number: 5135940Abstract: Compounds of the Formulae: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.Type: GrantFiled: March 20, 1991Date of Patent: August 4, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Patrice C. Belanger, Joshua Rokach, Rejean Fortin, Christiane Yoakim, Yvan Guindon
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Patent number: 5106871Abstract: The present invention relates to an anti-ulcer agent comprising a compound represented by the following general formula I as the effective ingredient, and a novel chalcone derivative included in the compound represented by this general formula I: ##STR1## wherein X and Y independently stand for a hydrogen atom or together form a single bond, R.sub.1 stands for a hydroxyl group, an acetoxy group, a carboxymethoxy group or a methoxycarbonylmethoxy group, R.sub.2 stands for a hydrogen atom, an isoprenyl group, isopentyl group or a propyl group, R.sub.3 stands for hydroxyl group or a methoxy group, R.sub.4 stands for a hydrogen atom, a hydroxyl group or a methoxy group, R.sub.5 stands for a hydrogen atom, a hydroxyl group, a methoxy group or an isopentyl group, R.sub.6 stands for a hydroxyl group, a methoxy group or a carboxymethoxy group, and R.sub.7 stands for a hydrogen atom or a methoxy group.Type: GrantFiled: July 19, 1991Date of Patent: April 21, 1992Assignee: Tsumura & Co.Inventors: Yukio Komazawa, Shigefumi Takeda, Kunio Hosaka, Hiroshi Mitsuhashi, Toshihiko Watanabe
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Patent number: 5073375Abstract: A pharmaceutical preparation for the percutaneous administration comprises eperisone or tolperisone, including salts thereof, and a monoglyceride of an aliphatic acid having 8 to 12 carbon atoms or/and an ester of lactic acid with an aliphatic alcohol having 12 to 18 carbon atoms. It is improved in the percutaneous absorption.Type: GrantFiled: August 2, 1990Date of Patent: December 17, 1991Assignees: Sansho Co., Ltd., Eisai Co., Ltd.Inventors: Mitsuhiro Yoshida, Yutaka Morita, Yoshio Ishino, Shigemitsu Ohsawa
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Patent number: 5070099Abstract: Arylthioalkylphenylcarboxylic acids are provided which have the structure ##STR1## wherein Ar represents an aryl group including phenyl or naphthyl which may or may not include one or more substituents, X is COOR where R is hydrogen, alkali metal, or lower alkyl, or X is 5-tetrazolyl or ##STR2## wherein R.sup.1 is lower alkyl or aryl, p is 1 to 5, and m is 1 to 4. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic and vasospastic diseases.Type: GrantFiled: February 4, 1991Date of Patent: December 3, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Steven E. Hall, Philip D. Stein
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Patent number: 5047420Abstract: Novel 1,3-diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediate by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.Type: GrantFiled: August 21, 1989Date of Patent: September 10, 1991Assignee: Merck & Co., Inc.Inventors: Donald W. Graham, Tesfaye Biftu, John C. Chabala, Michael N. Chang, Yuan-Ching P. Chiang, Kathryn L. Thompson, Shu S. Yang
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Patent number: 5023364Abstract: Phenoxyalkylcarboxylic acid derivatives of the following formula, ##STR1## wherein R.sup.1 indicates a hydrogen atom, a methyl group or an ethyl group, m is equal to 2, 3 or 4, and n is equal to 3 or 4, their alkali salts and hydrates thereof are useful as antiallergic agents.Type: GrantFiled: March 17, 1989Date of Patent: June 11, 1991Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Mitsuo Ohashi, Katsuya Awano, Toshio Tanaka, Tetsuya Kimura
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Patent number: 5006542Abstract: Arylthioalkylphenylcarboxylic acids are provided which have the structure ##STR1## wherein Ar represents an aryl group including phenyl or naphthyl which may or may not include one or more substituents, X is COOR where R is hydrogen, alkali metal, or lower alkyl, or X is 5-tetrazolyl or ##STR2## where R.sup.1 is lower alkyl or aryl, p is 1 to 5, and m is 1 to 4. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic and vasopastic diseases.Type: GrantFiled: October 31, 1988Date of Patent: April 9, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Steven E. Hall, Philip D. Stein
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Patent number: 4939171Abstract: Alkyl and alkenyl aryl ether derivatives corresponding to the formula: ##STR1## in which R.sup.1 is a saturated cycloaliphatic C.sub.6 -C.sub.20 alkyl group or a mono- or polyunsaturated, linear, branched or cycloaliphatic C.sub.6 -C.sub.20 alkyl group and R.sup.2 is a C.sub.1 -C.sub.4 hydroxyalkyl group, a C.sub.3 or C.sub.4 hydroxyalkenyl group, a group --COOR.sup.3, --CH.sub.2 --COOR.sup.3, --CH.sub.2 --CH.sub.2 --COOR.sup.3 or --CH.dbd.CH--COOR.sup.3, are suitable as sebosuppressive agents in cosmetic or pharmaceutical preparations for topical application to the hair and to the skin.Type: GrantFiled: November 10, 1988Date of Patent: July 3, 1990Assignee: Henkel Kommanditgesellschaft auf AktienInventors: Hinrich Moeller, Norbert Banduhn
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Patent number: 4925873Abstract: A method for treating skin injuries is provided by administering a thromboxane A.sub.2 receptor antagonist systemically or topically to the skin area to be treated.Type: GrantFiled: September 1, 1988Date of Patent: May 15, 1990Assignee: E. R. Squibb & Sons, Inc.Inventors: Lawrence T. Friedhoff, Laura L. Bolton
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Patent number: 4891220Abstract: Serum levels of cholesterol are improved by administration of yeast cell wall extract LCP-100 Series.TM. product LR323.TM. in combination with a cholesterol regulating agent, preferably niacin or gemfibrozil.Type: GrantFiled: July 14, 1988Date of Patent: January 2, 1990Assignee: ImmuDyne, Inc.Inventor: Byron A. Donzis
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Patent number: 4883818Abstract: Onset-hastened and enhanced analgesic response is elicited in a mammalian organism in need of such treatment, i.e., a mammal suffering pain, by administering thereto a unit dosage onset-hastening/enhancing analgesically effective amount of the S(+) fenoprofen enantiomer, said enantiomer being substantially free of its R(-) fenoprofen antipode.Type: GrantFiled: November 17, 1987Date of Patent: November 28, 1989Assignee: Analgesic AssociatesInventors: Abraham Sunshine, Eugene M. Laska
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Patent number: 4871756Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4, E.sub.4 and the slow reacting substance of anaphylaxis.As such, these compounds will be useful as anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: GrantFiled: February 17, 1987Date of Patent: October 3, 1989Assignee: Merck Frosst Canada, Inc.Inventors: John Gillard, Joshua Rokach, Patrice C. Belanger
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Patent number: 4859703Abstract: Single dose formulations containing a combination of a lipid regulating agent selected from gemfibrozil, clofibrate, bezafibrate, or fenofibrate and an ACAT inhibiting agent are effective pharmacological formulations for regulating blood serum lipid and cholesterol levels.Type: GrantFiled: June 15, 1987Date of Patent: August 22, 1989Assignee: Warner-Lambert CompanyInventor: Brian R. Krause
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Patent number: 4855324Abstract: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, or --CH.dbd.CH--;wherein Z is OR.sup.1 or --NR.sup.4 R.sup.5 ;wherein R.sup.1 is hydrogen, lower alkyl, or a pharmaceutically acceptable cation;wherein R.sup.2 is H, --CH.sub.3 or --C.sub.2 H.sub.5 ;wherein R.sup.3 is OH, H or .dbd.O;wherein R.sup.4 and R.sup.5 may independently be hydrogen, or lower alkyl having 1-6 carbon atoms, or R.sup.4 and R.sup.5 may act together with N to form a cyclic amide of the formula: ##STR2## wherein n is an integer from 4-5; and m is an integer from 0-4. More particularly, this invention relates to compounds of the above formula which have utility as LTB.sub.4 antagonists.Type: GrantFiled: February 18, 1988Date of Patent: August 8, 1989Assignee: G. D. Searle & Co.Inventors: Stevan W. Djuric, Richard A. Haack, Stella S. Yu
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Patent number: 4855323Abstract: Leukotriene antagonists, a process for the preparation thereof, and the use thereof for the treatment of diseases ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and X have the indicated meanings, a process for the preparation of these compounds, the use thereof as pharmaceuticals, and pharmaceutical products based on these compounds, are described.Type: GrantFiled: July 22, 1988Date of Patent: August 8, 1989Assignee: Hoechst AktiengesellschaftInventors: Gunther Wess, Wilhelm Bartmann, Gerhard Beck, Hiristo Anagnostopulos
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Patent number: 4855289Abstract: The invention concerns the use of a compound with diuretic properties and of a magnesium supplementation in the form of magnesium monoaspartate hydrochloride, magnesium oxide, magnesium hydroxide or magnesium carbonate, and optionally of a potassium supplementation, and pharmaceutical preparations comprising a compound with diuretic properties and a magnesium supplementation in the form of magnesium monoasparate hydrochloride, magnesium oxide, magnesium hydroxide, or magnesium carbonate and optionally a potassium supplementation.Type: GrantFiled: July 30, 1987Date of Patent: August 8, 1989Inventors: Per O. Wester, Thomas R. Dyckner
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Patent number: 4853398Abstract: This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.Type: GrantFiled: April 13, 1987Date of Patent: August 1, 1989Assignee: Eli Lilly and CompanyInventors: F. P. Carr, Robert D. Dillard, Doris E. McCullough
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Patent number: 4851440Abstract: Leukotriene antagonists, processes for the preparation thereof, the use thereof for the treatment of diseases, and precursors.Compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and X have the indicated meanings, processes for the preparation of these compounds, the use thereof as pharmaceuticals, and pharmaceutical products based on these compounds are described. In addition, precursors for the preparation of compounds of the formula I are described.Type: GrantFiled: July 22, 1988Date of Patent: July 25, 1989Assignee: Hoechst AktiengesellschaftInventors: Gerhard Beck, Peter Below, Andreas Bergmann
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Patent number: 4837363Abstract: Compounds are described of formula (1) ##STR1## in which n is 1 or 2;m is 2-5 and X is --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --, or m is 1-4 and X is --CH.dbd.C.dbd.CH--;R.sup.1 is --H, C.sub.1-6 alkyl or C.sub.7-10 phenalkyl,Y substituted or unsubstituted 3-phenoxy-2-hydroxypropyl,and their salts.These compounds inhibit gastric acid secretion and provide gastrointestinal cytoprotection, and may be formulated for use in the treatment of ulcers.Type: GrantFiled: April 23, 1985Date of Patent: June 6, 1989Assignee: Glaxo Group LimitedInventor: Eric W. Collington
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Patent number: 4826876Abstract: This invention relates to chemical compounds which have selective thyromimetic activity. A compound of this invention is 3,5-dibromo-3'-[6-oxo-3(1H)-pyridazinyl-methyl]-thyronine.Type: GrantFiled: December 21, 1987Date of Patent: May 2, 1989Assignee: Smith Kline & French Laboratories LimitedInventors: David Ellis, John C. Emmett, Anthony H. Underwood, Paul D. Leeson
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Patent number: 4808572Abstract: Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: a is an integer of from 1 to 7,R.sup.o represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted at the terminal carbon atom by a free or acylated hydroxy group, by a halogen atom having an atomic number of at most 17, or by methoxy, or represents C.sub.1-3 -perfluoroalkyl,R.sup.2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene or alternatively, if R.sup.1 represents a halogenated radical and/or B represents phenylene or ethylene, a single bond or vinylene,B represents a single bond, ethynylene or phenylene,R.sup.3 represents hydroxy, C.sub.Type: GrantFiled: December 1, 1986Date of Patent: February 28, 1989Assignee: Ciba-Geigy CorporationInventors: Andreas Beck, Werner Breitenstein, Andreas von Sprecher, Robert W. Lang, Konrad Oertle
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Patent number: 4801616Abstract: This invention provides certain diphenylmethane derivatives, their pharmaceutical formulations, and their use in treating inflammation and arthritis in mammals.Type: GrantFiled: March 25, 1986Date of Patent: January 31, 1989Assignee: Eli Lilly and CompanyInventor: D. Mark Gapinski
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Patent number: 4791133Abstract: This invention relates to leukotriene B.sub.4 antagonists having the structure ##STR1## and the pharmaceutically acceptable addition salts thereof; wherein R.sup.1 is lower alkyl having 1-10 carbon atoms; or lower alkenyl or alkynyl having 2-10 carbon atoms; or lower alkadienyl having 3-10 carbon atoms; or lower alkadiynyl or alkenynyl having 4-10 carbon atoms;wherein R.sup.2 and R.sup.3 are the same or different and represent hydrogen or lower alkyl having 1-6 carbon atoms;wherein X is CH.dbd.CH, S, or O;wherein Y is CH.dbd.CH or C.tbd.C;wherein Z is OR.sup.4 or NR.sup.5 R.sup.6, and wherein R.sup.4 represent H, lower alkyl having 1-6 carbon atoms, or a pharmaceutically acceptable cation, and wherein R.sup.5 and R.sup.6 act independently and represent H or lower alkyl having 1-6 carbon atoms, or R.sup.5 and R.sup.Type: GrantFiled: June 26, 1987Date of Patent: December 13, 1988Assignee: G. D. Searle & Co.Inventors: Stevan W. Djuric, Richard A. Haack, Julie M. Miyashiro
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Patent number: 4785004Abstract: Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: R.sup.0 represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted by one or more halogen atoms having an atomic number of at most 17,R.sup.2 represents an aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene, a single bond or vinylene,B.sup.1 represents C.sub.1-7 -alkylene or phenylene,B.sup.2 represents a single bond, ethylene or phenylene, andM represents an aromatic radical of the partial formula ##STR2## in which the symbols have the following meanings: R.sup.3 represents hydrogen or C.sub.1-4 -alkyl,X represents NH, O, S or if R.sup.4 represents hydrogen, a single bond,one of the symbols R.sup.4 and R.sup.5 represents hydrogen and the other represents the group --CO--R.sup.6, orR.sup.4 and R.sup.5 together represent the radical --CO--C(R.sup.6).dbd.C(R.sup.7)--or--CO--C(R.sup.7).dbd.C(R.sup.6)--orR.sup.4 R.sup.Type: GrantFiled: December 15, 1986Date of Patent: November 15, 1988Assignee: Ciba-Geigy CorporationInventors: Andreas Von Sprecher, Werner Breitenstein, Andreas Beck, Robert W. Lang, Konrad Oertle
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Patent number: 4783480Abstract: A 6-keto-prostaglandin E.sub.1 derivative of the formula: ##STR1## (wherein R.sup.1 represents an amino acid or amino alcohol residue, R.sup.2 represents a single bond or an alkylene group of from 1 to 4 carbon atoms, R.sup.3 represents (i) an alkyl group of from 1 to 8 carbon atoms, (ii) a cycloalkyl group of from 4 to 7 carbon atoms, which may be unsubstituted or substituted by at least one alkyl group of from 1 to 8 carbon atoms or (iii) a phenyl or phenoxy group, which may be unsubstituted or substituted by chlorine, trifluoromethyl or alkyl of from 1 to 3 carbon atoms, provided that when R.sup.2 represents a single bond R.sup.3 does not represent phenoxy)cyclodextrin clathrates thereof and non-toxic salts thereof possess selective cytoprotective activity.Type: GrantFiled: January 28, 1987Date of Patent: November 8, 1988Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hirohisa Wakatsuka, Tadao Okegawa, Yoshinobu Arai
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Patent number: 4782176Abstract: Phenoxycarboxylic acids of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 R.sub.5, Z and n are as hereinafter set forth, are as described. The compounds of formula I are antagonists of slow reacting substance of anaphylaxis (SRS-A), which renders them useful as agents for the treatment of allergic conditions.Type: GrantFiled: May 23, 1983Date of Patent: November 1, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Matthew Carson, Ronald A. LeMahieu, William C. Nason
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Patent number: 4764521Abstract: This invention provides novel compounds which are leukotriene antagonists, certain novel intermediates to the compounds, formulations of the compounds, and a method of using the compounds for the treatment of conditions characterized by an excessive release of leukotrienes.Type: GrantFiled: May 7, 1986Date of Patent: August 16, 1988Assignee: Eli Lilly and CompanyInventor: David K. Herron
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Patent number: 4757089Abstract: A method of increasing aqueous humor outflow in the eye of a human patient including topically administering to the eye an outflow increasing amount of a compound characterized in that it contains one or more groups capable of reacting with sulfhydryl groups in the trabecular meshwork of the eye, and it has a margin of safety of at least 2.0.Type: GrantFiled: December 30, 1986Date of Patent: July 12, 1988Assignee: Massachusetts Eye and Ear InfirmaryInventor: David L. Epstein
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Patent number: 4755524Abstract: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different and independently represent tert-alkyl or phenyl; A represents methylene or methylene substituted by alkyl, dialkyl or hydroxy, provided that when A includes hydroxymethylene, the hydroxymethylene group is not adjacent to a heteroatom; B represents sulfur, sulfoxide, sulfone, oxygen, --NH-- or nitrogen substituted by alkyl, phenyl, benzyl, substituted phenyl or substituted benzyl; C represents methylene or methylene substituted by alkyl; R.sub.3 represents CO.sub.2 H, CO.sub.2 -alkyl or a tetrazole group; m is 0 or 1, n is 2, 3 or 4 and p is 1, 2 or 3; and the pharmaceutically acceptable salts thereof.Type: GrantFiled: January 15, 1987Date of Patent: July 5, 1988Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
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Patent number: 4752612Abstract: A method of percutaneously administering a physiologically active agent which comprises applying to the skin of a mammal a physiologically active agent in a carrier system which comprises at least one adjuvant and at least one solvent. The adjuvant can be selected from higher monoalcohols or mixtures thereof. The solvent can be selected from thioglycerols, lactic acid and esters thereof, cyclic ureas, compounds represented by the general formula R.sub.1 R.sub.2 NCONR.sub.3 R.sub.4, pyrrolidone-type compounds, amides, lactones or mixtures thereof.Type: GrantFiled: January 23, 1986Date of Patent: June 21, 1988Assignee: Nitto Electrical Industrial Co., Ltd.Inventors: Kenichiro Saito, Jorge Heller, Wilfred Skinner
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Patent number: 4751244Abstract: The present invention is directed to compounds of the general formula I and pharmaceutically acceptable salts thereof: ##STR1## wherein: R.sup.1 =HO or HOOC(CH.sub.2).sub.x CHR.sup.2 NH--;R.sup.2 =H, lower alkyl, benzyl or --CH.sub.2 OH;x=0 or 1;A=--(CH.sub.2).sub.n -- or ##STR2## n=1 to 5; and Y=H, Cl or OCH.sub.3Z=H or Clm=0 or 1R=lower alkyl;with the proviso that where R.sup.1 =OH, Y is H or Cl and m is 1, n is 4 or 5.The present invention is also directed to an antisickling pharmaceutical carrier and an antisickling agent of the general formula (I) (without the proviso) and pharmaceutically acceptable salts thereof.Type: GrantFiled: April 30, 1987Date of Patent: June 14, 1988Assignees: Merck & Co., Inc., The University of PittsburghInventors: Donald J. Abraham, Otto W. Woltersdorf, Jr., Edward J. Cragoe, Jr.