Abstract: Disclosed are imidazonaphthyridine derivatives represented by formula (I) ##STR1## wherein: R.sup.1 represents lower alkyl or substituted or unsubstituted aryl; andX-Y-Z represents ##STR2## wherein R.sup.2 represents hydrogen, lower alkyl, alkenyl, aralkenyl, or --C (R.sup.5) H--(CH.sub.2).sub.n --R.sup.4 (wherein R.sup.4 represents substituted or unsubstituted aryl, substituted or unsubstituted pyridyl, substituted or unsubstituted furyl, hydroxy-substituted lower alkyl, lower alkanoyloxy, morpholino, lower alkanoyl, carboxy, lower alkoxycarbonyl, cycloalkyl, hydroxy, lower alkoxy, halogen or NR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7 independently represents hydrogen or lower alkyl; R.sup.5 represents hydrogen, lower alkyl, or phenyl; and n represents an integer of 0 to 3); and R.sup.3 represents hydrogen, mercapto, hydroxy, lower alkyl, or aryl and pharmaceutically acceptable sails thereof.The compounds show a potent anti-inflammatory, anti-allergic and broncho-dilative activity.
Abstract: The present invention involves photoprotective compositions which are useful for topical application to prevent damage to skin caused by acute or chronic exposure to ultraviolet light comprising chelating agents having the formula ##STR1## wherein --R.sup.1 and --R.sup.2 are independently selected from the group consisting of alkyl, aryl, and heteroaryl, or R.sup.1 and R.sup.2 may be covalently bonded together to form a cyclic alkyl; --M is selected from the group consisting of =0, =S, --SR.sup.4 and --OR.sup.4 (when --M is --OR.sup.4 or --SR.sup.4, there is a hydrogen bonded to the carbon to which --M is bonded); --R.sup.4 is selected from the group consisting of hydrogen, alkyl, aryl and heteroaryl; --R.sup.3 is selected from the group consisting of hydrogen, alkyl, aryl and heteroaryl; --R.sup.6 is selected from the group consisting of hydrogen alkyl, aryl and heteroaryl; and i is selected from the group consisting of one and zero.
Type:
Grant
Filed:
November 9, 1992
Date of Patent:
November 15, 1994
Assignee:
The Procter & Gamble Company
Inventors:
Rodney D. Bush, Donald L. Bissett, Ranjit Chatterjee
Abstract: A compound of formula (I) ##STR1## wherein R' is hydrogen or methyl, m is zero or 1 and the symbol means that the azabicyclic rings may be in the .alpha. or the .beta. orientation, and the pharmaceutically acceptable salts thereof, are useful in treating CNS disorders, gut motility disorders, and/or emesis and/or pain in mammals, and/or migraine.
Type:
Grant
Filed:
November 30, 1992
Date of Patent:
November 8, 1994
Assignee:
Farmitalia Carlo Erba S.r.l.
Inventors:
Angelo Bedeschi, Walter Cabri, Ilaria Candiani, Silvia De Bernardinis, Marcello Marchi, Mario Varasi
Abstract: A process for the preparation of a compound of Formula (1): ##STR1## wherein: W.sup.1 is aryl;X.sup.1 and X.sup.2 are each independently selected from --H, --CN, halogen, alkyl, aryl and --COOH;Y is --H;Z is --OH; orY and Z together form a group of Formula (2): ##STR2## wherein: W.sup.2 is aryl;which comprises reacting a compound of Formula (3): ##STR3## wherein: X.sup.1, X.sup.2, Y and Z are as hereinbefore defined with a compound of Formula (4): ##STR4## wherein the substituents are as defined in the specification.
Abstract: 3- and 4-(1H-imidazol-1-yl)phenol compounds corresponding to the formula I ##STR1## in which R.sup.1 represents NH.sub.2 or CH.sub.3, R.sup.2 represents H or CH.sub.3, X represents O or S, Y represents H, OH or OCH.sub.3, and Z represents --CH.dbd.CH--, O or S, or their salts, which exhibit 5-lipoxygenase and thromboxane synthase inhibiting activities.
Type:
Grant
Filed:
February 17, 1993
Date of Patent:
October 18, 1994
Assignee:
Gruenenthal GmbH
Inventors:
Joachim Ammann, Michael Haurand, Cornelia Geist, Werner Englberger, Oswald Zimmer
Abstract: Method of stabilizing fabrics by impregnation with a water soluble stiffening agent so that the fabric will not readily stretch in any direction. The water soluble stiffening agent is prepared by producing a mixture of Poly Vinyl Alcohol and water and diluting such with Ethanol. The materials produced thereby is particularly suited for embroidery work, for accurate cutting of materials, and in the process of applique.
Abstract: A compound represented by the following general formula (II): ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, represent a hydrogen atom, an alkyl group having 1 to 20 carbon atoms, a phenyl group, a benzyl group, a phenethyl group, an alkylamine group having 1 to 4 carbon atoms, or a dialkylamino group having 2 to 8 carbon atoms, and ##STR2## represents a nobornylidene group or bicyclo [3,3,1]9-nonylidene group which may have a substituent, and ##STR3## represents a pyridine, quinoline, pyrrole or benzothiophene group which may have a substituent.
Abstract: Pharmaceutically useful nitrogen containing cyclic oxime and amine substituted compounds which are azabicyclo[2.2.1]oximes, azabicyclo[2.2.2]oximes, azabicyclo[2.2.1]amines, azabicyclo[2.2.2]amines, azabicyclo[3.2.1]oximes, and amine containing heterocyclic oximes wherein the heterocyclic ring contains from 3 to 7 carbon atoms are disclosed.
Type:
Grant
Filed:
August 24, 1993
Date of Patent:
September 13, 1994
Assignee:
Warner-Lambert Company
Inventors:
Corinne E. Augelli-Szafran, Stephen D. Barrett, Bradley W. Caprathe, Adam A. Galan, Juan C. Jaen, David J. Lauffer, Walter H. Moos, Michael R. Pavia, Kathryn B. Sanders, Haile Tecle, Anthony J. Thomas
Abstract: The invention relates to compounds of the formula (I): ##STR1## in which: Z represents an oxygen atom or a sulfur atom,R.sub.1 represents a hydrogen atom or an alkyl group,R.sub.2 represents a hydrogen atom or an alkyl group,n is one to six, inclusive,R.sub.3 represents an amino group, substituted with phenylsulfonyl, andmedicinal products containing the same.
Abstract: Certain N-acetonyl-substituted-amides of the formula: ##STR1## wherein A naphthyl; X, Y and Z are selected from the group consisting of hydrogen, halo, cyano, thiocyano, isothiocyano, thio(C.sub.1 -C.sub.2)alkyl, (C.sub.1 -C.sub.2)alkoxy, carbamoyl, dithiocarbomoyl, hydroxy, azide, thiophenyl, imidazolyl or triazolyl group as described herein; R.sup.1 and R.sup.2 are each independently a hydrogen atom or a (C.sub.1 -C.sub.6)alkyl group; and compositions containing these amides are fungicidally active, particularly against phytopathogenic fungi.
Abstract: The invention relates to hydrosoluble coumarin derivatives. These derivatives comply with the formula: ##STR1## in which R.sup.1 represents ##STR2## with m=1 to 30 and in which R.sup.7 can be a hydrogen atom or various groups, R.sup.2 to R.sup.6 can be different substituents, particularly substituents making it possible to introduce into the derivative an appropriate group as the enzyme substrate or for the synthesis of enzyme substrates.
Type:
Grant
Filed:
May 22, 1992
Date of Patent:
August 30, 1994
Assignee:
Laboratoires Eurobio
Inventors:
Joseph Chalom, Christine Griffoul, Michel Tod, Stephane Reveilleau
Abstract: Oxime ether derivatives of the formula I ##STR1## where R.sup.1 and R.sup.2 are each hydrogen or alkyl, Het is pyridyl, quinolyl, pyrimidinyl, pyrazinyl, pyridazinyl, thienyl, quinoxalinyl, isoxazolyl, benzoxazolyl or benzothiazolyl, the heterocyclic ring system being unsubstituted or substituted, and X is oxygen or sulfur, their plant-tolerated acid addition salts, metal complexes and N-oxides, and fungicides containing these compounds.
Type:
Grant
Filed:
December 4, 1990
Date of Patent:
August 2, 1994
Assignee:
BASF Aktiengesellschaft
Inventors:
Bernd Wenderoth, Siegbert Brand, Franz Schuetz, Thomas Kuekenhoehner, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
Abstract: A method of improving the strength, temper and water resistance of leather utilizing selected amphiphilic copolymers is provided. The amphiphilic copolymers are formed from a predominant amount of at least one hydrophobic monomer and a minor amount of at least one copolymerizable hydrophilic monomer. The method is particularly useful as a one step substitute for conventional retanning and fatliquoring treatment steps. In a preferred embodiment the amphiphilic copolymers also provide a significant degree of water resistance to the leather.
Type:
Grant
Filed:
December 7, 1992
Date of Patent:
July 19, 1994
Assignee:
Rohm and Haas Company
Inventors:
Thomas Stewart, Patricia M. Lekso, Anton G. El A'mma
Abstract: Novel all possible stereoisomers and mixtures thereof of vinylsulfone nor-pyrethric compounds of the formula ##STR1## wherein R.sub.a is selected from the group consisting of alkyl of 1 to 18 carbon atoms, alkenyl and alkynyl of 2 to 18 carbon atoms, cycloalkyl of 3 to 18 carbon atoms, cycloalkylalkyl of 4 to 18 carbon atoms and aryl of 6 to 14 carbon atoms unsubstituted or substituted with at least one functional group, n is 0, 1 or 2, R.sub.b is selected from the group consisting of alkyl of 1 to 18 carbon atoms, alkenyl and alkynyl of 2 to 18 carbon atoms, cycloalkyl of 3 to 18 carbon atoms, cycloalkylalkyl of 4 to 18 carbon atoms and aryl of 6 to 14 carbon atoms, all unsubstituted or unsubstituted with at least one functional group or R.sub.a and R.sub.
Type:
Grant
Filed:
April 22, 1993
Date of Patent:
July 12, 1994
Assignee:
Roussel-UCLAF
Inventors:
Didier Babin, Jean-Pierre Demoute, Jean Tessier
Abstract: The present invention concerns 3,4-annelated benzimidazol-2(1H)-one 1-carboxylic acid derivatives of the formula ##STR1## wherein R.sub.0, Z, A, B and C are as defined herein. Such derivatives are useful in the treatment of symptoms which are caused by over-excitation of 5-hydroxytryptamine receptors.
Type:
Grant
Filed:
September 28, 1992
Date of Patent:
July 5, 1994
Assignee:
Duphar International Research B.V.
Inventors:
Ineke Van Wijngaarden, Derk Hamminga, Wouter Wouters
Abstract: An antihypertensive, antianginal, antiarrhythmic and antiglaucomic pharamaceutical preparation consists of an active principle, namely 3-methyl-5-[2-(3-tert.butylamino-2-hydroxypropoxy-phenoxymethyl]-1,2,4-oxa diazole hydrochloride of the following formula: ##STR1## and a pharmaceutically acceptable diluent.
Type:
Grant
Filed:
August 11, 1992
Date of Patent:
July 5, 1994
Inventors:
Mikhail D. Mashovsky, Sergei D. Juzhakov, Leonid V. Rozenshtraukh, Oleg S. Medvedev, Evgeny P. Anjukhovsky, Elena V. Dorodnikova, Olga V. Dolgun, Aron Y. Bunin, Valentina N. Ermakova, Vladimir I. Metelitsa, Vladimir K. Piotrovsky
Abstract: The compound (S)-1-[(10-chloro-6,7-dihydro-4-oxo-3-phenyl-4H-benzo[a]quino-lizin-1-yl)c arbonyl]-3-ethoxypyrrolidine of the formula ##STR1## which has valuable pharmacological properties, is described. In particular, the compound of formula I has a non-sedating, hypnotic, that is, sleep-promoting, activity and can accordingly be used for the treatment of sleep disorders.
Type:
Grant
Filed:
March 24, 1993
Date of Patent:
July 5, 1994
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Richard R. Scherschlicht, Ulrich Widmer
Abstract: Enzymatically cleavable chemiluminescent 1,2-dioxetane compounds capable of producing light energy when decomposed, substantially stable at room temperature before a bond by which an enzymatically cleavable labile substituent thereof is intentionally cleaved, are disclosed. These compounds can be represented by the formula: ##STR1## The corresponding dioxetanes which, instead of being substituted at the 5' or 7', or at the 5' and 7' positions, instead contain a 4' methylene group, are also disclosed, as are intermediates for all these 3-substituted adamant-2'-ylidenedioxetanes, and their use as reporter molecules in assays.
Abstract: 1,3-Oxazole and 1,3-thiazole compounds of formula I, and their pharmaceutically acceptable salts and prodrugs: ##STR1## wherein X represents oxygen or sulphur;R.sup.1 represents a non-aromatic azacyclic or azabicyclic ring system.
Type:
Grant
Filed:
July 1, 1993
Date of Patent:
June 28, 1994
Assignee:
Merck Sharpe & Dohme Ltd.
Inventors:
Raymond Baker, John Saunders, Roger J. Snow, Graham A. Showell
Abstract: Amine derivatives having the general formula (I): ##STR1## wherein X is selected from the group consisting of ##STR2## Y is selected from the group consisting of ##STR3## R.sup.1 is hydrogen atom or an alkyl group; R.sup.2 is hydrogen atom or an alkyl group; R.sup.3 is hydrogen atom, a halogen atom or an alkyl group; R.sup.4 is hydrogen atom, an alkyl group, a cycloalkyl group, a halogenated alkyl group or a halogen atom; R.sup.5 is hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, nitro group or hydroxy group; R.sup.5 is attached to an arbitrary position of X, and R.sup.3 or R.sup.4 is attached to an arbitrary position of Y.The amine derivatives (I) are useful as fungicides.