Abstract: Amides of formula ##STR1## in which either R is 2-quinolyl, substituted phenyl (substituted by Br, 3-Cl, CF.sub.3, alkyloxycarbonyl, 4-dialkylamino), dichlorophenyl, trialkyloxyphenyl, benzyl, styryl, benzoyl or anilino and R' is halogen, phenyl or anilino or R' is phenoxy or 4-chlorophenoxy when R is 2-quinolyl, substituted phenyl, trialkyloxyphenyl, benzyl or styryl or R' is 4-fluoro(or alkyloxy)phenyl when R is 4-trifluoromethyl (or dialkylamino)phenyl, or R' is 3-bromophenyl when R is anilino, or R is phenyl or alkyloxyphenyl and R' is phenyl, 4-chlorophenoxy, anilino or 1-pyrrolidinyl or R' is 2-(or 4-)chlorophenyl, 3-(or 4-)bromophenyl, 4-alkyloxyphenyl or 3,4-dichloro(or dibromo)phenyl when R is phenyl or R is 3-halophenyl and R' is 3-(or 4-)fluorophenyl, 3-(or 4-)bromophenyl, 4-chlorophenyl, 2-(or 3-)-alkyloxyphenyl, 3-alkylphenyl or 3,4-difluoro(dichloro or dibromo)phenyl, the straight-chain or branched alkyl radical containing 1 to 4 carbon atoms each, are useful as immunostimulant agents.
Type:
Grant
Filed:
July 10, 1986
Date of Patent:
January 19, 1988
Assignee:
Rhone-Poulenc Sante
Inventors:
Claude Cotrel, Claude Guyon, Gerard Roussel, Gerard Taurand
Abstract: Hydrocarbons substituted with at least two anhydride moieties, are useful as dispersants in aqueous based hydraulic fluids and as curing agents in epoxy resins. These anhydrides are produced by reaction of a hydrocarbon derived from a soft wax or liquid hydrocarbon with a molar excess of an organic anhydride, preferably using a molar ratio excess of 3:1 to 8:1 of maleic anhydride, and under free radical conditions. The products are insoluble in the parent hydrocarbons.
Abstract: Imidazolyl-methane derivatives of the formula ##STR1## where Ar is an optionally substituted phenyl and R.sup.1 is alkyl or optionally substituted phenyl is prepared by reaction of a ketone of the formulaAr--CO--R.sup.1in which Ar and R.sup.1 have the abovementioned meanings is reacted with imidazole in the presence of formic acid.
Abstract: There are disclosed novel benzofurans having the following structural formula: ##STR1## wherein R is alkenyl of 1 to 6 carbon atoms or aryl of from 6 to 10 carbon atoms; R.sub.1 is H, alkali metal, or alkyl of 1 to 4 carbon atoms; and R.sub.2 is alkyl or alkoxy of from 1 to 5 carbon atoms, hydrogen, amino or dialkylamino, nitro, sulfonyl, alkyl or aryl thioether or halide. Also disclosed is a novel process of making the benzofurans, comprising the step of cyclizing an o-(2-carboxyvinyl)phenyl unsaturated alkyl ether in the presence of a base selected from the group consisting of KOH, NaOH, LiOH, dimsyl sodium, lithium diisopropylamide, potassium tert-butoxide, and mixtures thereof, at room temperature.
Abstract: A method for the preparation of substituted and unsubstituted 2-[(1-carbamoyl-1,2-dimethyl-propyl) carbamoyl]-3-quinolinecarboxylic, nicotinic and benzoic acids.
Type:
Grant
Filed:
November 21, 1983
Date of Patent:
January 12, 1988
Assignee:
American Cyanamid Company
Inventors:
William H. Gastrock, Timothy F. Mason, Gregory P. Withers
Abstract: There are disclosed compounds having the formula ##STR1## wherein R is hydrogen or lower alkyl;R.sup.1 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, phenyl or any of the foregoing substituted with halo;R.sup.2 is hydrogen, carboxy or lower alkoxy carbonyl; andR.sup.3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or any of the foregoing substituted with carboxy, methoxycarbonyl, hydroxy, amino, dilower alkyl amino, cyano, nitro or lower alkoxy;and their use as antifungal agents.
Type:
Grant
Filed:
March 13, 1987
Date of Patent:
January 12, 1988
Assignee:
American Home Products Corporation
Inventors:
Jerauld S. Skotnicki, Donald P. Strike, Bruce A. Steinbaugh
Abstract: New 3-[N-(mercaptoacyl)]amino-4-arylbutanoic acid derivatives are now provided, which exhibit analgesic activity and are effective to enhance the analgesia induced by a known analgesic compound, ]D-ala.sup.2,met.sup.5 ]-enkephalin (DAME).
Type:
Grant
Filed:
May 20, 1985
Date of Patent:
January 12, 1988
Assignee:
Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
Abstract: Compound of the formula ##STR1## wherein n is 1 or 2, Y is OH, R.sup.1 COO--, R.sup.2 R.sup.3 NCOO-- or R.sup.4 O whereby R.sup.1 is an alkyl group, or a possibly substituted phenyl group, R.sup.2 is an alkyl, phenethyl, or benzyl or phenyl group, R.sup.3 is H or an alkyl group and R.sup.4 is an allyl or benzyl group, and R is an alkyl, hydroxyalkyl, dimethylaminoalkyl or methylthioalkyl group or alkenyl group, processes for their preparations and methods of treatment employing such compounds. The compounds are useful for therapeutic purposes, especially for treatment of disorders in the central nervous system.
Type:
Grant
Filed:
October 1, 1984
Date of Patent:
January 12, 1988
Assignee:
Per A. E. Carlsson
Inventors:
Folke L. E. Arvidsson, Per A. E. Carlsson, Uli A. Hacksell, John S. M. Hjorth, Per L. Lindberg, John L. G. Nilsson, Domingo Sanchez, Nils U. E. Svensson, Hakan V. Wikstrom
Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is C.sub.1-6 alkyl;R.sub.2 is amino or C.sub.1-7 acylamino;R.sub.3 is halo or C.sub.1-6 alkythio;R.sub.4 and R.sub.5 are independently selected from hydrogen, C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-4 alkyl any of which phenyl moieties may be substituted by one or two of halo, CF.sub.3, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;R.sub.6 is C.sub.1-7 alkyl, --(CH.sub.2).sub.s R.sub.7, s being 0 to 2 andR.sub.7 being C.sub.3-8 cycloalky, --(CH.sub.2).sub.t R.sub.8, t being 1 or 2 andR.sub.8 being thienyl or phenyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy and C.sub.1-4 alkyl optionally substituted by hydroxy, C.sub.
Abstract: The invention relates to 5-oxo-1-imidazolidineacetamide derivatives which help restore learning and memory difficulties associated with ageing. A compound of the invention is 2,2-dimethyl-5-oxo-1-imidazolidineacetamide.
Type:
Grant
Filed:
June 20, 1986
Date of Patent:
January 12, 1988
Assignee:
Societe I.S.F. S.p.A.
Inventors:
Mario Pinza, Carlo Farina, Silvano Banfi, Ugo Pfeiffer
Abstract: A method of inhibiting the production of 5-lipoxygenase products in an animal in need thereof which comprises administering an effective, 5-lipoxygenase pathway inhibiting amount of a 2(3)-(pyridyl)-3-(2)-substituted phenyl)-6,7-dihydro-[5H]-pyrrolo-[1,2-a]imidazole, a 2(3)-(pyridyl)-3(2)-(substituted phenyl)-5,6,7,8-tetrahydro-imidazo[1,2,-a]pyridine, or a pharmaceutically acceptable salt thereof, to such animal.
Abstract: Novel compounds are disclosed, which are derivatives of 1,2,3,5,6,10b-hexahydropyrrolo[2,1-a]-isoquinolines, represented by general formula (I): ##STR1## as well as pharmaceutical compositions and methods for the treatment of depression in warm-blooded animals, e.g., man. Novel intermediates are also part of the invention.
Abstract: The present invention provides novel compounds of Formula I ##STR1## which are pharmacologically selectively useful as anti-thrombotic agents with minimal blood pressure lowering activity.
Abstract: Process for preparing pyrimidine by reacting in the gas phase 1,3-diaminopropane with a C.sub.1 reagent in the presence of an excess of methanol and/or carbon monoxide and of a metallic catalyst, wherein the reaction is carried out in the presence of a palladium catalyst promoted with an alkali metal and subsequently from the resulting reaction mixture pyrimidine is recovered.
Abstract: Imidazoles are prepared by subjecting an .alpha.,.beta.-dicarbonyl compound to a Radziszewski reaction with an aldehyde and ammonia and then catalytically hydrogenating the product.Imidazole and its derivatives are useful intermediates for drugs, crop protection agents and dyes.
Abstract: The invention relates to imidazopyrrolo-pyridine (or benzene) derivatives having herbicidal activity, herbicidal compositions thereof and the use thereof to control plant growth.
Abstract: The invention concerns thienoquinolizines of general formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts. In the formula R.sup.1 is hydrogen or lower alkyl and R.sup.2 is lower alkyl, halo(lower)alkyl, --A--NR.sup.3 R.sup.4 [where A represents a direct bond between the S and N atoms or a lower alkylene group having 1 to 3 carbon atoms in the chain between the S and N atoms and R.sup.3 and R.sup.4 each independently represent hydrogen, lower alkyl, aryl or aryl(lower)alkyl or together with the nitrogen atom to which they are attached represent a five or six membered heterocyclic ring], aryl or a heterocyclic radical or R.sup.1 is --A.sup.1 NR.sup.5.SO.sub.2 R.sup.6 [where A.sup.1 is a lower alkylene group having 1 to 3 carbon atoms in the chain between the two N atoms, R.sup.5 is hydrogen or lower alkyl and R.sup.6 is lower alkyl, halo(lower)alkyl or aryl] and R.sup.2 is lower alkyl, halo(lower)alkyl or aryl. The compounds possess .alpha..sub.
Type:
Grant
Filed:
October 23, 1986
Date of Patent:
January 5, 1988
Assignee:
John Wyeth & Brother Limited
Inventors:
Alan C. White, Robin G. Shepherd, Barry J. Langham
Abstract: Octahydroquinolizine and corresponding octahydroquinolizinium compounds of formulae (I) and (Va): ##STR1## where A is a 3 to 7 membered carbocyclic ring, R.sup.1 is a substituent, n is 0-2, x is 0-3, and Y is an anion. Also, pharmaceutical compositions for treating pain containing (I) and methods for synthesis and use as well as novel intermediates in the synthesis.
Abstract: 5-[1H-(5-membered-N-aromatic-heteryl)-1-yl]-7-R'-1,6-naphthyridin-2(1H)-one s (formula I) or salts thereof are useful as cardiotonic agents. Also shown as intermediates are 5-X-7-R'-1,6-naphthyridin-2(1H)-ones (formula II) or salts thereof, where X is bromo, chloro or hydrazino, 2-[2-(di-lower-alkylamino)ethenyl]-1,6-dihydro-6-oxo-3-pyridinecarbonitril e (formula III), and 2-[2-(di-lower-alkylamino)-2-propenyl]-6-methoxy-3-pyridinecarbonitrile (formula IIIa). Processes shown include the preparation of I from II, preparation of II from III or IIIa and the preparation of III from 1,6-dihydro-2-methyl-6-oxo-3-pyridinecarbonitrile, and the preparation of IIIa from 6-methoxy-2-methyl-3-pyridinecarbonitrile.