Abstract: The use of an olefinic compound of the formulaR.sup.1 R.sup.2 R.sup.3 C--CR.sup.4 =CR.sup.5 R.sup.6 (I),wherein R.sup.1 is a heterocyclyl radical selected from 1,2,4 -triazolyl, imidazolyl, 5-(1-6C alkyl)imidazol-1-yl, pyridyl and pyrimidinyl; R.sup.2 and R.sup.3, which may be the same or different, are each a hydrogen atom or a 1-6C alkyl radical; R.sup.4 is a phenyl or pyridyl radical, optionally bearing one or more substitutents selected from halogen atoms, amino, cyano, carbamoyl and nitro radicals, 1-6C alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylamino and alkylcarbamoyl radicals, di(1-6C alkyl)amino, di(1-6C alkyl)carbamoyl and 2-6C alkoxycarbonyl radicals; R.sup.5 is a hydrogen or halogen atom, a 1-6C alkyl radical or a phenyl radical optionally bearing one or more substituents as defined above for R.sup.4 ; and R.sup.6 is a phenyl or pyridyl radical optionally bearing one or more substitutents as defined above for R.sup.
Type:
Grant
Filed:
June 21, 1989
Date of Patent:
July 16, 1991
Assignee:
Imperial Chemical Industries PLC
Inventors:
Francis T. Boyle, Zbigniew S. Matusiak, James M. Wardleworth
Abstract: The invention relates to compounds of general formula (I) and physiologically acceptable salts and solvates thereof, methods for their preparation and pharmaceutical formulations thereof. ##STR1## wherein Ar represents a substituted phenyl or nitrogen-containing heterocyclic ring;X and Y represent alkylene, alkenylene or alkynylene chains;R.sup.1, R.sup.2 and R.sup.18 each represent hydrogen or alkyl groups; andQ represents an optionally substituted furan or thiophene ring.The compounds of the invention have a stimulant action at .beta..sub.2 -adrenoreceptors and are useful in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.
Type:
Grant
Filed:
December 16, 1988
Date of Patent:
July 16, 1991
Assignee:
Glaxo Group Limited
Inventors:
Ian F. Skidmore, Harry Finch, Alan Naylor, Lawrence H. C. Lunts, Charles Willbe, David Middlemiss
Abstract: The invention relates to tricyclic aromatase inhibitors, their preparation and their use in a pharmaceutical preparation.The compounds according to the invention possess the general formula I ##STR1## wherein R.sup.1 and R.sup.2 independently of one another denote H, halogen, alkyl, alkoxy, alkylthio, OH, CN, CF.sub.3, NO.sub.2, an amino group which is unsubstituted or substituted by alkyl, an NHacyl group, carbonamide or a free or esterified carboxylate group;R.sup.3 is H, alkyl, alkoxyalkyl or arylalkyl;R.sup.4 is H, OH, alkoxy or arylalkoxy;m is 1 or 2;n is 2, 3 or 4;the broken line represents an optional bond;Q denotes ##STR2## with the proviso that when R.sup.1 and R.sup.2 are H, halogen, alkyl, alkoxy or OH, m=1, n=3, the broken line does not represent a bond and Q is imidazolyl, R.sup.3 and R.sup.4 may not both be H;and also pharmaceutically acceptable salts.
Abstract: Disclosed are pyridine herbicides characterized by substitution with a fluorine-containing methyl group at the 2- or 6-position, a carboxylic acid-derived group at the 3-position, and a halogen or a substituted nitrogen-containing group at the 5-position.
Abstract: This invention provides a novel class of nicotine analogs which as therapeutic agents exhibit tranquilizing effects in mammals.Illustrative of invention nicotine analogs are 1-(3-dimethylaminopropyl)-2-(3-pyridyl)pyrrolidine: ##STR1## and (R,S)-6-(N,N-dimethyl-3-aminopropyl)nicotine: ##STR2## The nicotine analogs can exist in the form of acid addition salts.
Type:
Grant
Filed:
October 3, 1989
Date of Patent:
May 14, 1991
Assignee:
Philip Morris Incorporated
Inventors:
Thomas S. Osdene, Henry V. Secor, Jeffrey I. Seeman
Abstract: A water-in-oil type emulsified composition containing a water-swellable clay mineral, a nonionic surfactant, an oil component, and water as the essential constituents or containing a water-swellable clay mineral, a quaternary ammonium salt type cationic surfactant, one or two more kinds of polyoxyalkylene modified organopolysiloxane, an aqueous phase, and an oil phase containing one or two or more kinds of organic silicone resin comprising the units of the formula:RnSiO.sub.(4-n)/2wherein R is a hydrocarbon group having 1 to 6 carbon atoms or a phenyl group, and n represents a value of 1.0 to 1.8, and a water- and polyhydric alcohol-in-oil type emulsified composition containing an oil phase containing a polyoxyalkylene modified organopolysiloxane, a water-swellable clay mineral, a quaternary ammonium salt type cationic surfactant and a silicone oil, water, and a polyhydric alcohol.
Abstract: Compounds classified as 5,6-dihydro-4-alkylamino-4H-thieno (or furo) [2,3-b]thiopyran-2-sulfonamide-7,7-dioxide are carbonic anhydrase inhibitors useful in the treatment of ocular hypertension, and most of the carbonic anhydrase inhibitory activity resides in only one of the enantiomers. The undesired enantiomer is utilized by racemization by thermolysis of an N-acyl derivative in a basic environment followed by removal of the acyl group. The racemate may then be resolved into the enantiomers.
Type:
Grant
Filed:
February 5, 1990
Date of Patent:
April 30, 1991
Assignee:
Merck & Co., Inc.
Inventors:
Thomas J. Blacklock, Edward J. J. Grabowski, Paul Sohar
Abstract: Triarylsulfonium polyfluoro metal or metalloid salts are provided by effecting the oxidation of a diarylsulfide, while under dehydrating conditions, in the presence of a strong protonic acid. The resulting triarylsulfonium acid salt can thereafter be directly metathesized with an alkali metal or alkaline earth metal polyhalo salt.These compounds have the general formula ##STR1## where Q is selected from .dbd.S.fwdarw.O, --S-- and mixtures thereof, M is a transition metal or metalloid, "c" is an integer of 1 to 3, "d" is an integer of 0 to 3, R.sup.6 is phenyl or naphthyl, R.sup.7 is phenylene or naphthalene optionally substituted with one or more radicals selected from the class consisting of --CH.sub.3, --OCH.sub.3, --CO.sub.2 H, --Br, --Cl, and NO.sub.2.
Abstract: A compound of the formula: ##STR1## in which R.sup.1 is --OH or --NH.sub.2 ; R.sup.2 is a halogen or --CN; R.sup.3 is a halogen or --CN; and n is one of the integers 1, 2 or 3; or a pharmaceutically acceptable salt thereof, are useful as antithrombotic agents.
Type:
Grant
Filed:
May 1, 1990
Date of Patent:
March 26, 1991
Assignee:
American Home Products Corporation
Inventors:
Steven M. Peseckis, Jehan F. Bagli, Richard J. Heaslip, Thomas J. Colatsky
Abstract: Optically active oxiranes of the formula ##STR1## in which R represents substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or represents substituted or unsubstituted phenyl, andR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent hydrogen or alkyl, at least one of the radicals representing alkyl, orR.sup.4 and R.sup.5 together represent alkanediyl, which is unsubstituted or substituted by alkyl, or R.sup.4 and R.sup.5 together with the adjacent carbon atoms represent a fused bicyclic hydrocarbon radical, which is unsubstituted or substituted by alkylare produced by reacting an enantiomerically pure oxathiane ketone of the formula ##STR2## with a sulphonium or sulphoxonium salt.
Abstract: Radiation detecting solid elements consisting of conductive polymers and radiation sensitive materials which are capable of generating radiation induced substances composing the dopant of the conductive polymers. The elements are monolayer sheets obtained by impregnating or compounding the conductive polymers, such as, polythiophene and polyselenophene, with radiation sensitive materials, such as, diphenyliodonium chloride and triphenylsulfonium hexafluoroarsenate(V). The elements are also laminated sheets consisting of conductive polymer films and radiation sensitive material containing films. As radiation exposure causes variation in electrical conductivity and absorption spectrum of the elements, radiation can be detected by the variation of these properties.
Abstract: Novel light producing 1,2-dioxetanes are described of the formula ##STR1## wherein ArOX is an aryl ring substituted with an X oxy group and A are passive organic groups which allow the 1,2-dioxetane to produce light when triggered by removing X. X is a chemically labile group which is removed by an activating agent. The 1,2-dioxetane compounds can be triggered to produce light at room temperatures. The compounds are produced from novel alkenes.
Type:
Grant
Filed:
December 29, 1988
Date of Patent:
October 9, 1990
Assignee:
Board of Governors of Wayne State University
Abstract: An active agent delivery system for the controlled administration of macromolecular polypeptides which comprises a micro-suspension of water-soluble components in a polylactide matrix.
Abstract: The imidazolium compounds of the formula ##STR1## wherein Q is arylene or heteroarylene, the group --NR.sup.1 R.sup.2 is a basic amino group, R.sup.3 is lower alkylthio, lower alkoxy or the group --(A).sub.n --Ra, R.sup.4 is a saturated or partially unsaturated lower hydrocarbon group, a basic amino group, --N.dbd.CRc--Rb, --CHRcRd, --NH--CHRcRd, --NH--CO--Re or --CHRc--CO--Re, R.sup.5 is hydrogen, lower alkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower haloalkyl, aryl or a fused benzene ring, R.sup.6 is hydrogen or lower alkyl, Ra and Rb independently are aryl, heteroaryl or a basic amino group, Rc is hydrogen or lower alkyl, Rd is aryl or heteroaryl, Re is hydrogen, a saturated or partially unsaturated lower hydrocarbon group optionally attached via an oxygen atom, or an aryl, heteroaryl or basic amino group optionally attached via a lower alkyl group, A is vinylene or lower alkylene, n is the integer 0 or 1, the dotted line is an additional double bond and the symbol Y.sup.
Type:
Grant
Filed:
January 9, 1989
Date of Patent:
September 11, 1990
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Wilhelm Klotzer, Helmut Link, Renate Mussner, Werner Schiestl, Nicolas Singewald
Abstract: A novel compound having the formula (I): ##STR1## or a reactive derivative or functional equivalent thereof, wherein m is an integer from 1 to 4, and R.sub.1 and R.sub.2 are same or different and selected from hydrogen and 1-4C alkyl; a fluorescent conjugate having the formula (III): ##STR2## wherein m R.sub.1 and R.sub.2 have the meaning given in claim 1, and R.sub.4 is a substituent attached to the keto group of formula (III) by a covalen bond. The new compounds and conjugates are usefual as fluorescent labelling agents.
Abstract: An isoxazolidin-3,5-dione for the control of hyperlipidemia in mammals having the following structural formula: ##STR1## wherein R.sup.1 and R.sup.2 are each an alkyl of 1 to 4 carbons; R.sup.3 is an alkoxybenzoyl group containing from 1 to 3 alkoxy groups wherein the alkoxy groups have from 1 to 4 carbon atoms, an alkoxybenzoyl group wherein the alkyl group had from 1 to 4 carbons, a halobenzoyl group, or a group ##STR2## where together R.sup.10 and R.sup.11 form a C.sub.3 to C.sub.7 alkylene group, and R.sup.12 and R.sup.13 are each alkyl from 1 to 4 carbon atoms.
Type:
Grant
Filed:
October 31, 1988
Date of Patent:
August 7, 1990
Assignee:
The University of North Carolina at Chapel Hill
Abstract: Compounds of formula ##STR1## wherein the radicals R.sub.1 and R.sub.2 are the same or different and represent hydrogen, halogen atoms, a trifluoromethyl group, a cyano, a nitro group, an amino group, a mono-C.sub.1 -C.sub.6 -alkylamino group, a di-C.sub.1 -C.sub.6 -alkylamino group, an amino group that is substituted by a phenyl C.sub.1 -C.sub.4 -alkyl radical, a C.sub.2 -C.sub.6 -alkanoyl-amino group, a C.sub.1 -C.sub.6 -alkoxycarbonyl amino group, a C.sub.1 -C.sub.6 -alkyl group optionally substituted by a phenyl radical, a hydroxy group, a C.sub.1 -C.sub.6 -alkoxy group, a C.sub.2 -C.sub.6 -alkanoyloxy group, a phenoxy group or represent a carbamoyl group optionally substituted by one or two C.sub.1 -C.sub.6 -alkyl groups and the radical A is an acyl group which is derived from an amino acid as well as processes for their preparation.
Type:
Grant
Filed:
August 28, 1989
Date of Patent:
August 7, 1990
Assignee:
Asta Pharma AG
Inventors:
Jurgen Engel, Axel Kleemann, Bernd Nickel, Istvan Szelenyi
Abstract: This invention provides novel 5H-pyrazolo[4,3-a]-quinolizin-5-one compounds which exhibit a selective inhibitory activity against IgE-antibody formation, and have utility for treatment of allergic diseases associated with IgE formation in mammals, such as allergic bronchial asthma, allergic rhinitis, atopic dermaties, hypersensitiveness, and the like.