Benzene Ring Containing Patents (Class 514/520)
-
Patent number: 5672627Abstract: A class of substituted spirodienes is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein R.sup.3 is methylsulfonyl or sulfamyl; and wherein R.sup.8 is selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, n-propyl, isopropyl, butyl, tert-butyl, isobutyl, methoxy, ethoxy, propoxy, butoxy, hydroxyl, mercapto, methylthio, ethylthio, cyano, fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, difluoropropyl, dichloroethyl, dichloropropyl, trifluoromethoxy, hydroxymethyl, methoxymethyl and ethoxymethyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: July 9, 1996Date of Patent: September 30, 1997Assignee: G.D. Searle & Co.Inventors: Horng-Chih Huang, David R. Reitz
-
Patent number: 5637603Abstract: The present invention is directed to the use of disulfonyl methane compounds for the control of parasites in vertebrate animals.Type: GrantFiled: April 25, 1995Date of Patent: June 10, 1997Assignee: Eli Lilly and CompanyInventor: David I. Wickiser
-
Patent number: 5631286Abstract: Novel cyclohexanes of formulas (I) and (II) are described herein. They inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production: these compounds are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV.Type: GrantFiled: May 24, 1995Date of Patent: May 20, 1997Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Paul E. Bender, Cornelia J. Forster
-
Patent number: 5631247Abstract: The present invention provides compounds and pharmaceutical compositions, optionally containing estrogen or progestin, and the use of such compounds, alone, or in combination with estrogen or progestin, for inhibiting the symptoms of postmenopausal symptoms, particularly osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer.The present invention further provides the use of the compounds of the present invention for inhibiting uterine fibroid disease and endometriosis in women, and aortal smooth muscle cell proliferation, particularly restenosis, in humans.Type: GrantFiled: July 15, 1996Date of Patent: May 20, 1997Assignee: Eli Lilly and CompanyInventor: Jeffrey A. Dodge
-
Patent number: 5627207Abstract: The present invention provides compounds of the formula ##STR1## wherein Y is a naphthyl, tetrahydronaphthyl, pyridyl, quinolyl, isoquinolyl or indolyl ring system, R is a moiety which is an acrylic acid, a CN-substituted acrylic acid, acrylamide, acrylonitrile or thioacrylamide, or a group of formulae (e) to (j): ##STR2## wherein R.sub.3 is OH or NH.sub.2, R.sub.1 is H, alkyl or alkanoyl, R.sub.2 is H, halogen, CN or alkyl; and n is 0, 1, 2 or 3; and the pharmaceutically acceptable salts thereof are useful as tyrosine kinase inhibitors.Type: GrantFiled: May 31, 1995Date of Patent: May 6, 1997Assignee: Farmitalia Carlo Erba S r lInventors: Franco Buzzetti, Antonio Longo, Maristella Colombo
-
Patent number: 5605923Abstract: Novel cyclohexene-ylidene derivatives of formula (I) are described herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production; they are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.Type: GrantFiled: September 29, 1994Date of Patent: February 25, 1997Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Cornelia J. Forster
-
Patent number: 5602173Abstract: Novel cyclohexane-ylidene derivatives of formula (I) are described. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production. These compounds are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.Type: GrantFiled: September 29, 1994Date of Patent: February 11, 1997Assignee: SmithKline Beecham CorporationInventor: Siegfried B. Christensen, IV
-
Patent number: 5591727Abstract: The invention relates to an insecticidal composition which comprises at least one pyrethroid, at least one UV absorbing agent and at least one antioxidant from the group consisting of tocopherol derivatives and citric acid esters. This insecticidal composition can in particular be used as an emulsion or on a powdery carrier for the control of flying and crawling insects such as flies and cockroaches.Type: GrantFiled: February 7, 1995Date of Patent: January 7, 1997Assignees: Perycut-Chemie AG, Franz BencsitsInventor: Franz Bencsits
-
Patent number: 5589506Abstract: The present invention relates to a novel compound having a 12-lipoxygenase inhibitory effect, of the general formula (I), a precursor thereof, and a medicine containing the same, ##STR1## wherein R.sup.1 represents a hydrogen atom or a hydroxy group; one of R.sup.2 and R.sup.3 represents a hydrogen atom, while the other cyano group ; and Ar is a group represented by the following general formula (a), (b) or (c), ##STR2## wherein R.sup.4 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom, a thrifluoromethyl group or a cyano group.Type: GrantFiled: December 30, 1994Date of Patent: December 31, 1996Assignee: Morinaga Milk Industry Co., Ltd.Inventors: Koichi Hashimoto, Akio Yamada, Hirokazu Hamano, Shigehiro Mori, Hisako Moriuchi
-
Patent number: 5571842Abstract: Perfluoroalkyl-substituted benzoylguanidines, a process for their preparation, their use as a medicament or diagnostic agent, and a medicament containing themA description is given of perfluoroalkyl-substituted benzoylguanidines of the formula I ##STR1## where R(1) is (C.sub.1 -C.sub.6)-perfluoroalkyl-SO.sub.m ; R(2) and R(3) are H, halogen, alk(yl)(oxy), phenoxy; R(4) and R(5) are H, alkyl, Hal, CN, OR(7), NR(8)R(9), --(CH.sub.2).sub.n --(CF.sub.2).sub.o --CF.sub.3 and of the pharmacologically acceptable salts thereof; the compounds I are obtained by reacting a compound II ##STR2## with guanidine, L being a leaving group which is able readily to undergo nucleophilic substitution.Type: GrantFiled: May 11, 1995Date of Patent: November 5, 1996Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
-
Patent number: 5565191Abstract: Stilbene derivatives of formula (I) ##STR1## wherein A, R.sub.1 and R.sub.2 are as defined in the following, are useful for the protection against UV radiation.Type: GrantFiled: December 13, 1994Date of Patent: October 15, 1996Assignee: 3V Inc.Inventor: Giuseppe Raspanti
-
Patent number: 5563161Abstract: Compounds of formula (I), and salt and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; R.sup.1 is H; optionally substituted C.sub.1-6 alkyl; optionally substituted phenyl(C.sub.1-4 alkyl); C.sub.2-6 alkenyl; C.sub.2-6 alkynyl; COR.sup.a ; COOR.sup.a ; COHet; COC.sub.1-6 alkylhalo; COC.sub.1-6 alkylNR.sup.a R.sup.b ; CONR.sup.12 C.sub.1-6 alkylCONR.sup.a R.sup.b ; CONR.sup.a R.sup.b ; or SO.sub.2 R.sup.a ; R.sup.2 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.q optionally substituted by oxo where q is 4 or 5 and where one methylene group may optionally be replaced by an oxygen atom or a group NR.sup.x, where R.sup.x is H or C.sub.1-6 alkyl; R.sup.3 is C.sub.1-3 alkyl substituted by optionally substituted phenyl; R.sup.4 and R.sup.5 are each H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; and Z represents O or S; are tachykinin receptor antagonists useful in therapy.Type: GrantFiled: March 10, 1995Date of Patent: October 8, 1996Assignee: Merck Sharp & Dohme Ltd.Inventors: Ian T. Huscroft, Graeme I. Stevenson, Brain J. Williams
-
Patent number: 5552438Abstract: Novel compounds of Formula (I) ##STR1## where X.sub.4 is a substituted cyclohexane or cyclohexane group and the other radicals are defined herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production. The compounds of the present invention are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.Type: GrantFiled: September 29, 1994Date of Patent: September 3, 1996Assignee: SmithKline Beecham CorporationInventor: Siegfried B. Christensen, IV
-
Patent number: 5494932Abstract: Sulfonic acid stilbenes block the infection of cells by HSV, and CMV and these compounds can be used to treat viral infection.Type: GrantFiled: May 25, 1994Date of Patent: February 27, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Alan D. Cardin, A. Stanley Tyms
-
Patent number: 5492687Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising iodophenoxy alkylene ethers and pharmaceutically acceptable clays in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.Type: GrantFiled: May 3, 1994Date of Patent: February 20, 1996Assignee: Sterling Winthrop Inc.Inventors: Stephen B. Ruddy, Gregory L. McIntire, Mary E. Roberts, Edward R. Bacon
-
Patent number: 5478862Abstract: The invention is drawn to 17-oxo-15,16-seco-19-nor steroids which are useful as intermediates in the production of various 15,16-seco-19-nor progestins. These progestins display elevated progestational activity with a minimum of ancillary hormonal activity and are thus useful in the suppression of ovulation in the human female.Type: GrantFiled: May 13, 1994Date of Patent: December 26, 1995Assignee: SRI InternationalInventors: Richard H. Peters, Masato Tanabe
-
Patent number: 5466435Abstract: Disclosed are contrast agents of the formula ##STR1## wherein Z is H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, alkoxycarbonyl, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R is C.sub.1 -C.sub.25 alkyl, cycloalkyl, ##STR2## or halo-lower-alkyl; each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy;(CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H or lower-alkyl, optionally substituted with halo;x is 1-4;n is 1-4;m is 1-15;p is 1-20; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl;in an aqueous, pharmaceutically acceptable carrier comprising a cellulose derivative.Type: GrantFiled: April 4, 1994Date of Patent: November 14, 1995Assignee: Sterling Winthrop Inc.Inventors: Edward J. Baker, Edward R Bacon, Carl R. Illig, Thomas J. Caulfield, Brent D. Douty, Kurt A. Josef, John L. Toner, Robert W. Lee
-
Patent number: 5462954Abstract: Antagonists having a substituted phenyl phenol or a substituted phenolic biphenyl structure, and various derivatives thereof, are specific leukotriene antagonists. Their structures, use and synthesis are disclosed. Also, pharmaceutical formulations are disclosed for use in applications treating diseases or conditions characterized by excessive release of leukotriene B.sub.4, one of the metabolites of arachidonic acid.The primary LTB.sub.Type: GrantFiled: November 1, 1994Date of Patent: October 31, 1995Assignee: Eli Lilly and CompanyInventors: S. Richard Baker, Robert D. Dillard, Paul E. Floreancig, J. Scott Sawyer, Michael J. Sofia
-
Patent number: 5449687Abstract: Novel compounds of Formulas (I) and (II) ##STR1## are described herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production; these compounds are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV.Type: GrantFiled: September 29, 1994Date of Patent: September 12, 1995Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Paul E. Bender, Cornelia J. Forster, John G. Gleason
-
Patent number: 5449681Abstract: The present invention is directed to the use of disulfonyl methane compounds for the control of parasites in vertebrate animals.Type: GrantFiled: November 22, 1993Date of Patent: September 12, 1995Assignee: Eli Lilly and CompanyInventor: David I. Wickiser
-
Patent number: 5446067Abstract: Oxime ethers of the formula ##STR1## wherein m, G, R, R.sup.1, X, Y, and Z are as defined herein and fungicides containing these compounds.Type: GrantFiled: July 12, 1994Date of Patent: August 29, 1995Assignee: BASF AktiengesellschaftInventors: Remy Benoit, Hubert Sauter, Reinhard Kirstgen, Gisela Lorenz, Eberhard Ammermann
-
Patent number: 5436267Abstract: A novel N-phenylcarbamate compound or its salt where possible, which is useful as the active ingredient of a biocidal composition for control of harmful organisms, is represented by the following general formula (I): ##STR1## wherein R.sup.1 is unsubstituted or substituted alkyl; R.sup.2 is H, unsubstituted or substituted alkyl, alkenyl, alkynyl or cycloalkyl, or --COX.sup.1 wherein X.sup.1 is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl or alkoxy; Z is --CH.sub.2 S--, --SCH.sub.2 --, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 SO--, --CH.sub.2 SO.sub.2 --, --CH.sub.2 SCH.sub.2 --, or --CH.sub.2 O--N.dbd.C(R.sup.4)--; R.sup.Type: GrantFiled: July 11, 1994Date of Patent: July 25, 1995Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Terumasa Komyoji, Itaru Shigehara, Norifusa Matsuo, Hiroshi Shimoharada, Takeshi Ohshima, Toshio Akagi, Shigeru Mitani
-
Patent number: 5430060Abstract: The invention concerns novel N-phenylacetyl and related acyl derivatives of (4-amino-2,6-dimethylphenylsulphonyl)nitromethane and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.Type: GrantFiled: September 15, 1993Date of Patent: July 4, 1995Assignee: Zeneca LimitedInventors: David R. Brittain, Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston, Linda Slater
-
Patent number: 5430030Abstract: A prophylactic pretreatment for nerve gas and pesticide poisons which can be administered orally and which comprises the following agents, in combination: a. Pyridostigmine (pyridostigmine bromide) b. Diazepam c. N-methyl-4-pipyridinyl phenylcyclopentanecarboxylateThese agents may be administered in the form of a capsule which contains, for example, tablets, one a normal release dosage form and one or two in a slow release dosage form.Type: GrantFiled: December 15, 1993Date of Patent: July 4, 1995Assignee: Arzneimittelwerk Dresden GmbHInventors: Armin Sommer, Bleyer Holm
-
Patent number: 5430062Abstract: The present invention relates to stilbene derivatives which possess utility as anti-cancer agents. The compounds can be used to treat cancers which are susceptible to treatment therewith, and can be utilized in a method of treating such cancers. Pharmaceutical compositions containing the compounds are disclosed. Three preferred compounds among those disclosed are (Z)-1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene, (Z)-1-(4-methylphenyl)-2-(3,4,5-trimethoxyphenyl)ethene, and 4-methyl-3',4',5'-trimethoxybenzylaniline hydrochloride.Type: GrantFiled: June 23, 1993Date of Patent: July 4, 1995Assignee: Research Corporation Technologies, Inc.Inventors: Mark S. Cushman, Ernest Hamel
-
Patent number: 5424327Abstract: The invention relates to novel combined compositions for combatting plant, animal and sanitarian as well as forestry, horticultural and warehouse pests. These compositions contain a pyrethroid-type insecticide as an insecticidally active ingredient and at least one fungicide inhibiting the ergosterol biosynthesis as activity-strengthening agent as well as optionally piperonylbutoxide and other additives.The advantages of the compositions according to the invention consist therein that the activity-strengthening substances used are fungicidal agents widely used and have an advantageous toxicology. The activity-strengthening agent exerts a synergistic effect together with the pyrethroid-type insecticide.The combinations according to the invention bear an outstanding importance in the protection of stored crops.Type: GrantFiled: September 9, 1994Date of Patent: June 13, 1995Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara RTInventors: Laszlo Pap, Istvan Szekely, Lajos Nagy, Andras Szego, Andrea Toth, Eva Somfai, Csaba Szantay, Lajos Novak, Laszlo Poppe
-
Patent number: 5411733Abstract: Antiviral agent containing a crude drug effective on a broad range of viruses.Type: GrantFiled: April 26, 1993Date of Patent: May 2, 1995Inventors: Toyoharu Hozumi, Takao Matsumoto, Haruo Ooyama, Tsuneo Namba, Kimiyasu Shiraki, Masao Hattori, Masahiko Kurokawa, Shigetoshi Kadota
-
Patent number: 5393790Abstract: A class of substituted spiro compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein n is a number selected from 0, 1 and 2; wherein R.sup.3 is methylsulfonyl or sulfamyl; and wherein R.sup.8 is selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, n-propyl, isopropyl, butyl, tert-butyl, isobutyl, methoxy, ethoxy, propoxy, butoxy, hydroxyl, mercapto, methylthio, ethylthio, cyano, fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, difluoropropyl, dichloroethyl, dichloropropyl, trifluoromethoxy, hydroxymethyl, methoxymethyl and ethoxymethyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: February 10, 1994Date of Patent: February 28, 1995Assignee: G.D. Searle & Co.Inventors: David B. Reitz, Robert E. Manning, Horng-Chi Huang, Jinglin Li
-
Patent number: 5389619Abstract: Compounds of the formula I ##STR1## where n, W, X, Y, Z, R.sup.1, R.sup.2, and R.sup.3 are as defined herein exhibit fungicidal, insecticidal, and acaracidal activity.Type: GrantFiled: March 29, 1993Date of Patent: February 14, 1995Assignee: BASF AktiengesellschaftInventors: Reinhard Doetzer, Hubert Sauter, Horst Wingert, Reinhard Kirstgen, Albrecht Harreus, Gisela Lorenz, Eberhard Ammermann
-
Patent number: 5362747Abstract: 2-Nitroaryl or 2-cyanoaryl compounds of the formula ##STR1## pharmaceutical compositions thereof, intermediates useful in the preparation of these compounds, and methods for treating disorders of vascular smooth muscles or diseases of the cartilage, macrophages, neurons, platelets, bronchial smooth muscles, optic muscles and gastrointestinal smooth muscles, in addition to sickle cell anemia, diabetes, synovitis, chondroarthritis and osteoarthritis by employing these compounds.Type: GrantFiled: November 3, 1993Date of Patent: November 8, 1994Assignee: Abbott LaboratoriesInventors: Marlon Cowart, James F. Kerwin
-
Patent number: 5356931Abstract: Alpha-Arylacrylic acid derivatives of the general formula I ##STR1## where X is ethylene or ethenylene; n is 0 or 1;m is 0, 1, 2, 3 or 4;R.sup.1 is cyano, cyanato, thiocyanato, nitro, hydroxyl, carboxyl, haloalkyl, haloalkoxy, unsubstituted or substituted cycloalkyl, cycloalkenyl, cycloalkadienyl, alkenyl, alkynyl or amino, alkylcarbonyl, alkoxycarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, unsubstituted or substituted benzyloxycarbonyl, benzoyl, phenylalkyl, phenylalkoxy or phenoxyalkyl,or R.sup.1 together with one of the radicals R.sup.2 forms an unsubstituted or substituted 1,3-butadiene-1,4-diyl group or an unsubstituted or substituted chain consisting of carbon members and an oxygen member, andR.sup.2 is halogen, unsubstituted or substituted alkyl, alkoxy, alkenyloxy, alkynyloxy, alkadienyloxy, benzyloxy or benzylthio, are used for controlling pests.Type: GrantFiled: January 4, 1993Date of Patent: October 18, 1994Assignee: BASF AktiengesellschaftInventors: Reinhard Kirstgen, Rainer Otter, Christoph Kuenast, Uwe Kardorff, Wolfgang Steglich, Gunda Bertram
-
Patent number: 5348727Abstract: A compound of the formula: ##STR1## wherein Z.dbd.H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, alkoxycarbonyl, cyano, wherein thealkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R.dbd.C.sub.1 -C.sub.25 alkyl, cycloalkyl, ##STR2## or halo-lower-alkyl; each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CR.sub.1 R.sub.2).sub.p -(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C-Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H, or lower-alkyl, optionally substituted with halo;x is 1-4;n is [1-5]1-4;m is 1-15;p is 1-20; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, these compounds are useful as X-ray contrast agents or aryl-lower alkyl.Type: GrantFiled: March 11, 1993Date of Patent: September 20, 1994Assignee: Sterling Winthrop Inc.Inventors: Edward R. Bacon, Carl R. Illig, Thomas J. Caulfield, Brent D. Douty, Kurt A. Josef
-
Patent number: 5314914Abstract: A group of known naphthoquinone derivatives have been found to be useful for preventing or relieving herpes viral infections.Type: GrantFiled: February 19, 1992Date of Patent: May 24, 1994Assignee: BioMega/Boehringer Ingelheim Research Inc.Inventor: Yvan Guindon
-
Patent number: 5310538Abstract: R=C.sub.1 -C.sub.25 alkyl, cycloalkyl, ##STR2## or halo-lower-alkyl, each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CR.sub.1 R.sub.2).sub.p --(CR.sub.3 =CR.sub.4).sub.m Q ,or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2 and R.sub.3 and R.sub.4 are independently H, or lower-alkyl, optionally substituted with halo;x is 1-4;n is 1-4;m is 1-15;p is 1-20; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkylThese compounds are combined in a polymer for use as an X-ray contrast agent.Type: GrantFiled: March 11, 1993Date of Patent: May 10, 1994Assignee: Sterling Winthrop Inc.Inventors: Edward R. Bacon, Carl R. Illig, Thomas J. Caulfield, Brent D. Douty, Kurt A. Josef
-
Patent number: 5302615Abstract: A bactericidal composition and method for inhibiting and controlling the growth of the capsulated, facultative bacterium, Klebisella pneumoniae, are disclosed. The compositions comprise 2-(2-bromo-2-nitroethenyl) furan and phenyl-(2-cyano-2-chlorovinyl) sulfone. The method comprises adding from 1 part to about 200 parts composition to the aqueous system for which treatment is desired.Type: GrantFiled: May 19, 1993Date of Patent: April 12, 1994Assignee: Betz Laboratories, Inc.Inventors: Deborah K. Donofrio, Wilson K. Whitekettle
-
Patent number: 5302592Abstract: Use as microbicides of thioacryloyl compounds of the formula ##STR1## Compounds and compositions are also disclosed.Type: GrantFiled: August 16, 1993Date of Patent: April 12, 1994Assignee: Rohm and Haas CompanyInventors: Peter Osei-Gyimah, Samuel E. Sherba, Raj J. Mehta, Barry C. Lange, Rhoda W. Joseph
-
Patent number: 5294613Abstract: This invention provides benzene derivatives, pharmaceutical formulations of those derivatives, and a method of using the derivatives for the treatment of inflammation in mammals.Type: GrantFiled: February 7, 1992Date of Patent: March 15, 1994Assignee: Eli Lilly and CompanyInventors: Nancy G. Bollinger, Theodore Goodson, Jr., David K. Herron
-
Patent number: 5292771Abstract: Compound of formula ##STR1## wherein n is 0 or 1, R.sub.1 and R.sub.2 are independently methyl, ethyl or cyclopropyl and R is an optionally substituted phenyl or heteroaryl group or salt or ester thereof are useful in the treatment of inflammatory bowel disease.Type: GrantFiled: October 8, 1992Date of Patent: March 8, 1994Assignee: Orion-yhtyma OyInventors: Reijo J. Backstrom, Erkki J. Honkanen, Jarmo J. Pystynen, Anne M. Luiro, Paivi A. Aho, Inge-Britt Y. Linden, Erkki A. O. Nissinen, Pentti Pohto
-
Patent number: 5288742Abstract: The invention concerns .alpha.,.alpha.-dialkylbenzyl derivatives of the formula I ##STR1## wherein Ar.sup.1 is phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;the phenylene group may optionally bear one or two substituents R.sup.3 ;each of R.sup.1 and R.sup.2, which may be the same or different, is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, fluoro-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl, provided that both of R.sup.1 and R.sup.2 are not methyl or fluoromethyl; andQ is cyano, amino, nitro, formyl, (1-4C)alkoxy, thiazolyl or (2-4C)alkanoyl;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.Type: GrantFiled: March 18, 1992Date of Patent: February 22, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Philip N. Edwards, David Waterson
-
Patent number: 5288750Type: GrantFiled: January 31, 1991Date of Patent: February 22, 1994Assignee: Orion-yhtyma OyInventors: Pentti Pohto, Paivi A. Aho, Reijo J. Backstrom, Erkki J. Honkanen, Inge-Britt Y. Linden, Erkki A. O. Nissinen
-
Patent number: 5270342Abstract: The invention concerns novel N-phenylacetyl and related acyl derivatives of (4-amino-2,6-dimethylphenylsulphonyl)nitromethane and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.Type: GrantFiled: July 31, 1991Date of Patent: December 14, 1993Assignee: Imperial Chemical Industries PLCInventors: David R. Brittain, Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston, Linda Salter
-
Patent number: 5268385Abstract: This invention provides a method for treating the symptoms of schizophrenia by interacting selectively with presynaptic dopaminergic D.sub.2 receptors without appreciably activating postsynaptic dopamine receptors which comprises administering to a schizophrenic an effective amount of a compound selected from the group consisting essentially of the stereoisomers of mixtures thereof of compounds represented by the general formula: ##STR1## wherein R.sub.1 is selected from the group consisting of pyridyl and ##STR2## X is oxygen or sulfur, Y, if present, is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, and a is an integer between zero and 3, R.sub.2 is H, R.sub.Type: GrantFiled: November 18, 1991Date of Patent: December 7, 1993Assignee: Whitby Research, Inc.Inventor: Alan S. Horn
-
Patent number: 5256538Abstract: The present invention relates to a highly sensitive diagnostic/prediagnostic test to identify persons at risk of a thrombotic event. Thrombotic events include myocardial infarction, deep venous thrombosis, pulmonary embolism, thromboembolic stroke pulmonary embolism deep venous and cardiovascular disease. The test is based on the early detection of elevated levels of resting platelet surface thrombospondin. The present invention also includes methods of determining the presence of thrombospondin on the surface TSP receptors of resting platelets in a biological sample. An anti-thrombospondin monoclonal antibody which is specific for thrombospondin on resting platelets is also disclosed. A diagnostic test in the form of a test kit for the determination of thrombospondin levels in a patient sample, and also for the prediagnosis of persons at risk for thrombotic events, is also described.Type: GrantFiled: March 8, 1991Date of Patent: October 26, 1993Assignee: Board of Regents, The University of Texas SystemInventors: Martha L. Aiken, Richard G. Painter
-
Patent number: 5254589Abstract: A pharmaceutically useful compound which lowers blood cholesterol levels having the formula ##STR1## wherein X is oxygen or --NH--; Ar is phenyl, substituted phenyl, naphthyl or substituted naphthyl; R.sub.1 is hydrogen, lower alkyl or benzyl; and R.sub.2 is a straight or branched alkyl group having from 5 to 17 carbon atoms which may be substituted on the 1-carbon position with methyl, ethyl, phenyl, or substituted phenyl, or a cycloalkyl group having from 3 to 8 carbon atoms.Type: GrantFiled: October 15, 1991Date of Patent: October 19, 1993Assignee: Warner-Lambert CompanyInventors: Joseph A. Picard, William H. Roark, Bruce D. Roth
-
Patent number: 5236952Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adensoylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuornal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.Type: GrantFiled: April 16, 1991Date of Patent: August 17, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose DaPrada, Gerhard Zurcher
-
Patent number: 5223536Abstract: The 1,4-diaryl-1-cyclopropyl-4-substituted butane pesticides of the following formula are effective as insecticides and acaricides: ##STR1## in which X and Y are independently hydrogen, halogen, alkyl, alkoxy, cycloalkylalkoxy, alkylcarbonyl, alkoxycarbonyl, haloalkyl, haloalkoxy, alkylthio, haloalkylthio, alkylsulfinyl, alkylsulfonyl, trialkylamino, nitro, or cyano; or X and Y together are --OCH.sub.2 O-- or --OCF.sub.2 O-- bridging the 2-3 or 3-4 positions of the phenyl ring; Ar is 3-phenoxyphenyl, 4-fluoro-3-phenoxyphenyl, 6-phenoxypyridin-2-yl, or 2-methyl(1,1'-biphenyl)-3-yl;R is cyano, methyl, trifluoromethyl, alkenyl, alkynyl, or halogen.Type: GrantFiled: July 23, 1991Date of Patent: June 29, 1993Assignee: FMC CorporationInventors: Thomas G. Cullen, Scott McN. Sieburth, Gary A. Meier, John F. Engel
-
Patent number: 5198445Abstract: Substituted 3-thio-2-propynenitriles are prepared which correspond to the formula:R--S--C.tbd.C--C.tbd.Nwherein R is an alkyl, cyclic alkyl, aryl, or heterocyclo group.These compounds have been found to exhibit a high degree of antimicrobial activity in industrial and commercial applications and compositions containing these compounds are so employed.Type: GrantFiled: April 20, 1992Date of Patent: March 30, 1993Assignee: The Dow Chemical CompanyInventors: Connie L. Deford, Charles D. Gartner, Kalakota S. Reddy, John K. Swayze, David E. Wallick, Warren L. Treptow, George A. Paul, Billy R. Hardas
-
Patent number: 5185370Abstract: Compound of formula ##STR1## wherein n is 0 or 1, R.sub.1 and R.sub.2 are independently methyl, ethyl or cyclopropyl and R is an optionally substituted phenyl or heteroaryl group or salt or ester thereof are useful in the treatment of inflammatory bowel disease.Type: GrantFiled: January 31, 1991Date of Patent: February 9, 1993Assignee: Orion-yhtyma OyInventors: Reijo J. Backstrom, Erkki J. Honkanen, Jarmo J. Pystynen, Anne M. Luiro, Paivi A. Aho, Inge-Britt Y. Linden, Erkki A. O. Nissinen, Pentti Pohto
-
Patent number: 5147891Abstract: A bactericidal composition and method for inhibiting and controlling the growth of the capsulated, facultative bacterium, Klebsiella pneumoniae, are disclosed. The composition comprises an amount, effective for the intended purpose of 3-iodo-2-propynylbutyl carbamate and phenyl-(2-cyano-2-chlorovinyl) sulfone. The method comprises administering between about 0.1 to about 200 parts of this combined treatment (based on one million parts of the desired aqueous system) to the particular water containing system for which treatment is desired.Type: GrantFiled: December 16, 1991Date of Patent: September 15, 1992Assignee: Betz Laboratories, Inc.Inventors: Deborah K. Donofrio, Wilson K. Whitekettle
-
Patent number: H1595Abstract: The invention relates to diketontrile derivatives which have been discovered useful against arthropods, plant nematodes, helminth protozoan pests or as intermediates for such useful compounds which have a general formula: ##STR1##Type: GrantFiled: June 13, 1994Date of Patent: September 3, 1996Assignee: Rhone-Poulene Inc.Inventors: Paul A. Cain, David T.-W. Chou, Themistocles D. J. D'Silva, Daniel B. Grant, Nancy D. Herman