Nitrogen In Substituent Q Patents (Class 564/163)
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Patent number: 4870096Abstract: Indoles are disclosed of formula (I): ##STR1## wherein R.sub.1 represents R.sub.5 R.sub.6 NCOCH.sub.2 --, R.sub.5 CONH(CH.sub.2).sub.p --,R.sub.5 R.sub.6 NSO.sub.2 (CH.sub.2).sub.p -- or R.sub.7 SO.sub.2 NH(CH.sub.2).sub.p --, (where R.sub.5 and R.sub.6 each represents a hydrogen atom or a C.sub.1-3 alkyl group, R.sub.7 represents C.sub.1-3 alkyl and p is zero or one),R.sub.2 is hydrogen or C.sub.1-3 alkyl;R.sub.3 and R.sub.4 each represents hydrogen atom, C.sub.1-3 alkyl, or 2-propenyl;m is zero or an integer from 1 to 4; andn is an integer from 2 to 5; and physiologically acceptable salts and solvates (e.g. hydrates) thereof.The compounds have potent and selective vasoconstrictor activity and are indicated as useful for the treatment of migraine. They may be formulated as pharmaceutical compositions with pharmaceutically acceptable carriers of excipients for administration by any convenient route.Various methods for the preparation of the compounds (I) are disclosed.Type: GrantFiled: December 11, 1986Date of Patent: September 26, 1989Assignee: Glaxo Group LimitedInventors: Alexander W. Oxford, Ian H. Coates, David E. Bays, Colin F. Webb
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Patent number: 4845110Abstract: There are provided anti-allergic pharmaceutical compounds of formula: ##STR1## in which n is 0, 1 or 2; R.sup.1 is a hydrocarbyl group containing 6 to 30 carbon atoms and optionally substituted with an optionally substituted phenyl group; R.sup.2 is (i) optionally optionally protected tetrazolyl, --COR.sup.6 where R.sup.6 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, an optionally protected amino acid residue or --NR.sub.2.sup.7 where each R.sup.7 is hydrogen or C.sub.1-4 alkyl, and --NHR.sup.8 where R.sup.8 is hydrogen, a protecting group, an optionally protected amino acid residue, C.sub.1-4 alkyl or --COR.sup.9 where R.sup.9 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy, or (iii) C.sub.1-10 alkyl substituted with a group selected from ##STR2## where each R.sup.10 is hydrogen or C.sub.1-4 alkyl; and R.sup.3, R.sup.4 and R.sup.5 are each selected from hydrogen, carboxyl, C.sub.2-5 alkoxycarbonyl, C.sub.1-4 alkyl, hydroxyl, optionally protected tetrazolyl, halo, trifluoromethyl, nitrile, nitro and --CONR.sub.2.sup.Type: GrantFiled: December 4, 1986Date of Patent: July 4, 1989Assignee: Lilly Industries LimitedInventors: Stephen R. Baker, Alec Todd
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Patent number: 4827016Abstract: Dermal inflammations which are induced and propagated by leukotrienes are treated by topically applying to the inflamed dermis the following compound: ##STR1## wherein R.sup.3 is H or a thiol; n is 1 to 12; p is 0 to 12; X is a substituted carbonyl, such as an ester or a carboxylic acid; and Y is an aliphatic or branched hydrocarbon, aromatic ring, carbonyl or substituted amide.Type: GrantFiled: July 20, 1987Date of Patent: May 2, 1989Inventor: Lee R. Morgan
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Patent number: 4816066Abstract: Compounds of the formula ##STR1## wherein R is halogen, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkyl, cyano, nitro, S(O).sub.n R wherein R is C.sub.1 -C.sub.4 alkyl and n is the integer 0, 1 or 2; and R.sup.2 through R.sup.8 are hydrogen or certain substituents, their salts, herbicidal compositions containing the compound or salts and the herbicidal use thereof.Type: GrantFiled: December 4, 1987Date of Patent: March 28, 1989Assignee: Stauffer Chemical CompanyInventors: William J. Michaely, Gary W. Kraatz
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Patent number: 4808732Abstract: Amino-tetraalkylbenzoylphthalic acids are intermediates for preparing homopolyimides and copolyimides which contain structural elements of the formula I ##STR1## in which R.sup.1 and R.sup.2 are halogen, nitro, aryl, aryloxy, alkyl or alkoxy, m is 0 or a number from 1 to 4, n is 0 or a number from 1 to 3 and p is 0, 1 or 2, the free carbonyl groups are bonded in the ortho-position relative to one another and R is a divalent aromatic radical which is substituted by at least one alkyl group or aralkyl group, are autophotocrosslinkable. They are suitable for the production of protective films and photographic relief images.Type: GrantFiled: October 28, 1987Date of Patent: February 28, 1989Assignee: Ciba-Geigy CorporationInventor: Josef Pfeifer
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Patent number: 4797152Abstract: Novel cyclohexenonecarboxylic acid derivatives exhibit herbicidal and plant growth regulating activity.The cyclohexanedionecarboxylic derivatives are of the formula I ##STR1## wherein A is an aliphatic or aromatic alcohol, or is an amino group which may be substituted by halogen, lower alkoxy, lower alkylthio, nitro or cyano, or is a heterocyclic amino group which is unsubstituted or substituted,R is C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl, each unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio,R.sub.1 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 haloalkenyl or C.sub.3 -C.sub.6 alkylnyl,B is an aliphatic or aromatic radical or is an aliphatic or aromatic carbonyl or sulfonyl group which may be substitued by halogen, lower alkoxy, lower alkylthio, nitro or cyano.The compounds are suitable for selectively controlling grasses in crops of useful plants.Type: GrantFiled: November 14, 1986Date of Patent: January 10, 1989Assignee: Ciba-Geigy CorporationInventor: Hans-Georg Brunner
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Patent number: 4760161Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit lipoxygenase, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.Type: GrantFiled: April 25, 1983Date of Patent: July 26, 1988Assignee: Merck & Co., Inc.Inventors: Philippe L. Durette, Timothy F. Gallagher
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Patent number: 4755511Abstract: This invention relates to tricyclic pyridazinone compounds, pharmaceutical compositions containing the compounds, and a method of stimulating cardiac activity in a mammal by administering an effective amount of the compound. A compound of the invention is 7-carboxamido-4,4a-dihydro-4a-methyl-[5H]-indeno[1,2-c]-pyridazin-3[2H]-on e.Type: GrantFiled: September 22, 1987Date of Patent: July 5, 1988Assignee: Smith Kline & French Laboratories LimitedInventor: Brian H. Warrington
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Patent number: 4753934Abstract: Compounds of the formula ##STR1## wherein A, B, R.sub.1, X and Q are substituents of various types, and acid addition salts thereof. The compounds are useful as fungicides.Type: GrantFiled: September 29, 1986Date of Patent: June 28, 1988Assignee: Celamerck GmbH & Co. KGInventors: Josef Nickl, Helmut Pieper, Jurgen Curtze, Christo Drandarevski, Sigmund Lust
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Patent number: 4739059Abstract: A novel amine amide of the formula: ##STR1## wherein the various substituents are defined hereinbelow. The compounds are useful as thickening agents, disoxidation catalysts and monomers.Type: GrantFiled: March 27, 1987Date of Patent: April 19, 1988Assignee: Daikin Industries Ltd.Inventors: Yohnosuke Ohsaka, Yoshio Amimoto, Yoshio Negishi
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Patent number: 4736056Abstract: This invention relates to a process for preparing a malonic acid derivative compound of formula (i) depicted herein in high yield and high purity by reacting a malonic acid derivative compound of formula (ii) depicted herein with an alkylating agent of formula (iii) depicted herein in the presence of a solvent and a base.Type: GrantFiled: December 15, 1986Date of Patent: April 5, 1988Inventors: Oliver W. Smith, Russell J. Outcalt
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Patent number: 4727188Abstract: o,o'-Dithiodibenzamides of the formula ##STR1## where R.sup.1 and R.sup.2 are each hydrogen, alkyl or phenyl, R.sup.3 is hydrogen, halogen, nitro, methyl or methoxy, and R.sup.4 has the same meanings as R.sup.3, are prepared by nitrosating an anthranilamide of the formula ##STR2## and reacting the product with sulfur dioxide in the presence of copper or a copper salt.Type: GrantFiled: March 28, 1985Date of Patent: February 23, 1988Assignee: BASF AktiengesellschaftInventor: Hagen Jaedicke
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Patent number: 4699992Abstract: Novel 3-amino-2-benzoyl-acrylic acid derivatives of the formula ##STR1## in which R.sup.1 represents the nitrile group, an ester group --COOR.sup.4 or carboxamide group ##STR2## R.sup.4 denoting C.sub.1 -C.sub.6 -alkyl, and R.sup.5 and R.sup.6 representing hydrogen or C.sub.1 -C.sub.3 -alkyl or phenyl,R.sup.2 and R.sup.3, which can be identical or different, represent a C.sub.1 -C.sub.6 -alkyl radical and, furthermore, can form, together with the nitrogen atom to which they are bonded, a 5- or 6-membered heterocyclic ring which can additionally contain as ring member the atoms or groups --O--, --S--, --SO-- or --SO.sub.2 --,X represents halogen,X.sup.1 denotes hydrogen, methyl, nitro or halogen,X.sup.2 denotes halogen or methyl, andX.sup.3 denotes hydrogen or halogen,are prepared by reacting ##STR3## The products can be converted into known antibacterials.Type: GrantFiled: September 12, 1985Date of Patent: October 13, 1987Assignee: Bayer AktiengesellschaftInventor: Klaus Grohe
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Patent number: 4681898Abstract: Compounds of the formula ##STR1## where n is 0 or 1,R is alkyl, phenyl or R.sub.4 -substituted phenyl,R.sub.2 and R.sub.3 are, independently, alkyl orR.sub.2 and R.sub.3 together with N is ##STR2## m is 1, 2 or 3, R.sub.1 and R.sub.4 are, independently hydrogen, halo, alkyl or alkoxy, andR.sub.5 is hydrogen or alkyl of 1 to 6 carbon atomsor their pharmaceutically acceptable salts are useful as anti-diabetic agents, in particular, as hypoglycemic agents or inhibitors of post-prandial hypoglycemia.Type: GrantFiled: May 8, 1984Date of Patent: July 21, 1987Assignee: Sandoz Pharmaceuticals Corp.Inventor: Jeffrey Nadelson
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Patent number: 4673763Abstract: Procainamide and N-acetylprocainamide (NAPA) immunogens, antibodies prepared therefrom, labeled conjugates, synthetic intermediates, and the use of such antibodies and labeled conjugates in immunoassays for determining the respective drugs. The immunogens comprise the drugs coupled at the .alpha.-position of the amide side chain to an immunogenic carrier material. The labeled conjugates and synthetic intermediates similarly are .alpha.-position derivatives of the drugs or precursors thereof. The antibodies and labeled conjugates are particularly useful in homogeneous nonradioisotopic immunoassays for measuring the respective drugs in biological fluids such as serum.Type: GrantFiled: March 18, 1985Date of Patent: June 16, 1987Assignee: Miles Laboratories, Inc.Inventors: Robert T. Buckler, Frederick E. Ward
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Patent number: 4670592Abstract: A bisbiguanide compound of the formula:R.sup.1 R.sup.2 N.C(:NR.sup.6)NH.C(:NH)NH.CH.sub.2 X-- --(CH.sub.2).sub.3 NH.C(:NH)NH.C(:NR.sup.7)NR.sup.3 R.sup.4 Vor a tautomer thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 which may be the same or different, are each hydrogen, a 1-16C alkyl radical, a 2-16C alkoxyalkyl radical, a 3-12C cycloalkyl radical, a (3-12C cycloalkyl)-(1-4C alkyl) radical, or an optionally substituted phenyl or phenyl(1-4C alkyl) radical, or R.sup.1 and R.sup.2 and the nitrogen atom to which they are attached, or R.sup.3 and R.sup.4 and the nitrogen atom to which they are attached, which may be the same or different, are each a 1-azetidinyl, 1-pyrrolidinyl, piperidino, hexamethyleneimino, heptamethyleneimino, morpholino or 4-(1-8C alkanoyl)-1-piperazinyl radical each of which may bear 1-3C alkyl substituents; each of R.sup.6 and R.sup.7, which may be the same or different, is hydrogen or a 1-8C alkyl radical; and X is a substituted ethylene or ethylidene radical of the formula:--CH.Type: GrantFiled: May 7, 1984Date of Patent: June 2, 1987Assignee: Imperial Chemical Industries PLCInventors: Murdoch A. Eakin, Philip N. Edwards, Michael S. Large
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Patent number: 4656182Abstract: Substituted trans-1,2-diaminocyclohexyl amide compounds demonstrating selective opioid receptor binding possess utility as analgesic, diuretic, and psychotherapeutic agents. A method of preparing the compounds, pharmaceutical compositions employing the compounds, and a method of alleviating pain employing the compounds are also disclosed.Type: GrantFiled: November 13, 1984Date of Patent: April 7, 1987Assignee: Warner-Lambert CompanyInventor: David Horwell
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Patent number: 4610819Abstract: A process for the preparation of 1,4-oxazepinones and thiones having the formula: ##STR1## wherein A is an aromatic ring selected from benzene, naphthalene, quinoline or pyridine; n is 1 to 3; Z is an amino radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; and R.sup.4 and R.sup.5 are hydrogen and loweralkyl starting from chloroaromatic carboxylates and alkanolamines is disclosed.Type: GrantFiled: September 19, 1984Date of Patent: September 9, 1986Assignee: A. H. Robins Company, Inc.Inventors: Young S. Lo, Albert D. Cale, Jr.
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Patent number: 4609753Abstract: The invention relates to new diphenyl ethers of the general formula ##STR1## wherein X is a trifluoromethyl group or an alkylsulphonyl group having 1-4 carbon atoms;R is an alkylene or alkylidene group having 1-12 carbon atoms; andA is a bis(alkoxyethoxy)phosphinyl group having 6-12 carbon atoms, a bis(alkoxyethoxyethoxy)phosphinyl group having 10-16 carbon atoms, a carboxy group, an alkenyloxycarbonyl group having 3-6 carbon atoms, an unsubstituted aminocarbonyl group, an N-alkylaminocarbonyl group having 2-5 carbon atoms, the alkyl group of which is substituted with a dialkylamino group having 2-4 carbon atoms, a cyano group, or an alkyloxycarbonyl group having 2-5 carbon atoms, the alkyl group of which may be substituted with an alkoxy, alkylthio or alkylsulphonyl group having 1-4 carbon atoms, with an alkoxyethoxy group having 3-6 carbon atoms, with a dialkylamino group having 2-4 carbon atoms, or with a hydroxyalkyldithio group having 2-4 carbon atoms;with the provisos, that(a) when X is a trifluoromethyType: GrantFiled: May 2, 1984Date of Patent: September 2, 1986Assignee: Duphar International Research B.V.Inventors: Gerard B. Paerels, Cornelis W. Raven
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Patent number: 4602041Abstract: Compounds of formula (I): ##STR1## or a salt or acyl derivative thereof; whereinY is either --CH.dbd.N or ##STR2## R.sup.1 is hydroxy, halogen, (C.sub.1-4) alkyl, or (C.sub.1-4)alkoxy, R.sup.2 is a nitrogen-containing, basic substituent,R.sup.3 is hydrogen, hydroxy, halogen, (C.sub.1-4) alkyl, (C.sub.1-4) alkoxy or a nitrogen-containing, basic substituent, andR.sup.4 is hydrogen or hydroxy,are useful in treating diarrhoea and scours.Type: GrantFiled: February 8, 1983Date of Patent: July 22, 1986Assignee: Beecham Group P.L.C.Inventors: Peter M. Newsome, Lee J. Beeley, Stephen F. Moss
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Patent number: 4602097Abstract: Photoinitiators of the formulaG--O--(CH.sub.2 CH.sub.2 O).sub.n --CH.sub.2 --CH.sub.2 --O--Qwherein G is a photoinitiator moiety, R is hydrogen or lower alkyl, n has a value of at least 10, and Q is G or a lower alkyl are soluble in water and common organic solvents and are useful in polymerization systems employed in coatings used in screen printing.Type: GrantFiled: June 11, 1984Date of Patent: July 22, 1986Assignee: Ulano CorporationInventor: John R. Curtis
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Patent number: 4598093Abstract: 4-Amino-1,2,3,4-tetrahydro-2-naphthoic acid derivative of the formula: ##STR1## wherein X is halogen atom, n is 1 or 2, R.sup.1 is hydroxy group, lower alkoxy group or amino group, and R.sup.2 is hydrogen atom, lower alkanoyl group or carbamoyl group, or their salts, which are useful as hypotensive diuretic.Type: GrantFiled: May 7, 1984Date of Patent: July 1, 1986Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Tetsuya Tahara, Masafumi Arita, Tsuyoshi Kuroda
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Patent number: 4596885Abstract: A process for the preparation of a phenylglyocylic acid ester of the formula ##STR1## wherein R.sup.1 represents alkyl,X represents halogen, alkyl, halogenoalkyl, alkoxy or nitro, andn represents 0, 1, 2, or 3by contacting a benzoyl cyanide of the formula ##STR2## wherein X and n have the meanings stated above, in a sulphuric acid/water system in the presence of chloride ions at a temperature between 0.degree. and 70.degree. C. to form phenylglyoxylic acid amide and reacting the phenylglyoxylic acid amide without isolation with an alcohol of the formula R.sup.1 -OH, wherein R.sup.1 has the meaning stated above, optionally in the presence of a diluent, at a temperature between 40.degree. and 100.degree. C.Type: GrantFiled: February 6, 1978Date of Patent: June 24, 1986Assignee: Bayer AktiengesellschaftInventors: Winfried Lunkenheimer, Andreas Wittig, Wilfried Draber, Helmut Timmler
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Patent number: 4549016Abstract: Novel 2-(hydroxyphenylamino)benzamides and oxidation products thereof, useful as inhibitors of lipoxygenase, are of the formulas ##STR1## wherein R is hydrogen, lower-alkyl, halo or lower-alkoxy; R' is hydrogen or lower-alkyl; R" is hydrogen, lower-alkyl or halo; and N.dbd.Z is amino or substituted amino. The compounds of Formula I are prepared by de-etherification of the corresponding alkyl or benzyl ethers; and the compounds of Formula II are prepared by oxidation of the compounds of Formula I where R' is hydrogen and OH is in the 4-position.Type: GrantFiled: January 9, 1985Date of Patent: October 22, 1985Assignee: Sterling Drug Inc.Inventor: Denis M. Bailey
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Patent number: 4548744Abstract: Water-soluble ethoxylated amine oxides having clay soil removal/anti-redeposition properties are disclosed herein. These amine oxides are selected from ethoxylated monoamine oxides, ethoxylated diamine oxides, ethoxylated polyamine oxides, ethoxylated amine oxide polymers, and mixtures thereof. These amine oxides are useful at from about 0.05 to about 95% by weight in detergent compositions which further comprise from about 1 to about 75% by weight of a nonionic, anionic, ampholytic, zwitterionic, or cationic detergent surfactant or mixture thereof. In addition to these detergent surfactants, the detergent composition can optionally comprise from 0 to about 80% by weight of a detergent builder.Type: GrantFiled: July 22, 1983Date of Patent: October 22, 1985Inventor: Daniel S. Connor
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Patent number: 4536346Abstract: This disclosure describes novel substituted aralkanamidobenzoic acids and analogs thereof. These compounds are useful pharmaceutical agents for ameliorating atherosclerosis by inhibiting the formation and development of atherosclerotic lesions in the arterial wall of mammals.Type: GrantFiled: May 6, 1983Date of Patent: August 20, 1985Assignee: American Cyanamid CompanyInventors: Robert G. Shepherd, Janis Upeslacis
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Patent number: 4528392Abstract: There are disclosed compounds of the formula ##STR1## wherein X is OR.sup.2, SR.sup.2, N(R.sup.2).sub.2 or halo;W is --CH.sub.2 --, ##STR2## Y is --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, --SCH.sub.2 --, ##STR3## m is 0-6; n is 0-6;p is 1-3;A is O or S;B is OR.sup.2, SR.sup.2 or N(R.sup.2).sub.2 ;R.sup.1 is hydrogen, loweralkyl, loweralkoxy or halo;R.sup.2 is hydrogen or loweralkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like.Type: GrantFiled: April 18, 1984Date of Patent: July 9, 1985Assignee: American Home Products CorporationInventors: John H. Musser, Kenneth L. Kees
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Patent number: 4526999Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit lipoxygenase, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.Type: GrantFiled: April 25, 1983Date of Patent: July 2, 1985Assignee: Merck & Co., Inc.Inventors: Philippe L. Durette, Timothy F. Gallagher
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Patent number: 4510139Abstract: Novel 2-(hydroxyphenylamino)benzamides and oxidation products thereof, useful as inhibitors of lipoxygenase, are of the formulas ##STR1## wherein R is hydrogen, lower-alkyl, halo or lower-alkoxy; R' is hydrogen or lower-alkyl; R" is hydrogen, lower-alkyl or halo; and N.dbd.Z is amino or substituted amino. The compounds of Formula I are prepared by de-etherification of the corresponding alkyl or benzyl ethers; and the compounds of Formula II are prepared by oxidation of the compounds of Formula I where R' is hydrogen and OH is in the 4-position.Type: GrantFiled: January 6, 1984Date of Patent: April 9, 1985Assignee: Sterling Drug Inc.Inventor: Denis M. Bailey
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Patent number: 4504278Abstract: A novel fuel composition contains ethanol or methanol plus, as a corrosion inhibitor, a reaction product of a secondary amine, an isatoic anhydride and a (C.sub.10 -C.sub.14 alkoxy)-n-alkyl primary amine.Type: GrantFiled: June 27, 1984Date of Patent: March 12, 1985Assignee: Texaco Inc.Inventor: Rodney L. Sung
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Patent number: 4504305Abstract: A compound having the general formula ##STR1## wherein R.sub.1 is alkyl having 1-3 carbon atoms;R.sub.2 is alkyl having 1-3 carbon atoms, allyl, propargyl or haloalkenyl; andA is selected from the group consisting of ##STR2## wherein R.sub.3 is --SO.sub.2 R.sub.6 group, ##STR3## R.sub.4 is hydrogen, alkyl having 1-6 carbon atoms; phenyl or halophenyl; R.sub.5 is alkyl having 1-3 carbon atoms; X is oxygen or sulfur; and n is 0 or 1; wherein R.sub.6 is alkyl having 1-6 carbon atoms, haloalkyl having 1-6 carbon atoms or propenyl; R.sub.7 is hydrogen or alkyl having 1-4 carbon atoms; R.sub.8 is hydrogen, alkyl having 1-6 carbon atoms; propenyl or methoxy; R.sub.9 is hydrogen, alkyl having 1-8 carbon atoms, haloalkyl having 1-3 carbon atoms, alkoxy having 1-6 carbon atoms, propenyl or phenyl substituted with methyl; and Y and Z are oxygen or sulfur; and a metal salt or a quaternary ammonium salt of a compound defined herein above.The compound is useful as a herbicide.Type: GrantFiled: December 27, 1982Date of Patent: March 12, 1985Assignee: Nippon Soda Co., Ltd.Inventors: Isao Iwataki, Akira Nakayama, Minoru Kaeriyama, Hisao Ishikawa, Hideo Hosaka, Kenichi Kohara
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Patent number: 4486592Abstract: 9-Carbamoylfluorene derivatives are useful intermediates in a synthesis of 9-carbamoyl-9-(3-aminopropyl)fluorene antiarrhythmic agents.Type: GrantFiled: October 19, 1983Date of Patent: December 4, 1984Assignee: Eli Lilly and CompanyInventors: William B. Lacefield, Terry D. Lindstrom
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Patent number: 4478836Abstract: The present invention concerns new derivatives of 1-aryl 2-aminomethyl cyclopropane carboxamides (Z) of general formula I: ##STR1## in which: R represents a hydrogen or halogen atom, a lower alkyl group, a lower alkoxy group, or a hydroxy. nitro or amino group;n represents the value 1 or 2;R.sub.1 and R.sub.2 represent a hydrogen atom, a lower alkyl group, an aryl or lower alkaryl group, possibly substituted, preferably in para position, by a halogen atom, preferably a chlorine atom;R.sub.1 and R.sub.2 may also form a heterocycle having 5 or 6 members with the adjacent nitrogen atom;R.sub.3 and R.sub.4 represent a hydrogen atom or a lower alkyl group;R.sub.3 and R.sub.Type: GrantFiled: June 22, 1982Date of Patent: October 23, 1984Assignee: Pierre Fabre S.A.Inventors: Gilbert Mouzin, Henri Cousse, Bernard Bonnaud, Michel Morre, Antoine Stenger
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Patent number: 4473694Abstract: Process for the synthesis of hindered polysubstituted .alpha.-amino acetamides which comprises first reacting an .alpha.-haloacetamide with a base to form an intermediate .alpha.-lactam which in turn is reacted with a primary or secondary amine. The product thus obtained can comprise a multifunctional compound having one or more hindered amino moieties. These compounds are highly effective as UV stabilizers in a variety of plastics, especially the alpha monoolefins.Type: GrantFiled: September 29, 1982Date of Patent: September 25, 1984Assignee: The B. F. Goodrich CompanyInventor: John T. Lai
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Patent number: 4466977Abstract: Cis- and trans-N-[2-amino(oxy- or thia group-substituted-cycloaliphatic)]benzeneacetamide and -benzamide compounds, e.g., 3,4-dichloro-N-[4,4-dimethoxy-2-(1-pyrrolidinyl)cyclohexyl]-N-methylbenzen eacetamide, and salts thereof, are provided. These compounds have analgesic properties. Processes for their preparation are disclosed. Pharmaceutical compositions and methods of use are also provided.Type: GrantFiled: November 4, 1982Date of Patent: August 21, 1984Assignee: The Upjohn CompanyInventors: Moses W. McMillan, Jacob Szmuszkovicz
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Patent number: 4460600Abstract: Cis- and trans-N-[2-amino(adjacenty substituted bis(alkyloxy), bis(alkylthio), alkylthio or mercapto group substituted)-cycloaliphatic]benzeneacetamide and -benzamide compounds, e.g., (.+-.)-(1.alpha.,2.beta.)-4-bromo-N-[3,3-dimethoxy-2-(1-pyrrolidinyl)cyclo hexyl]-N-methylbenzamide, and salts thereof, are provided. These compounds have analgesic properties. Processes for their preparation are disclosed. Pharmaceutical compositions and methods of use are also provided.Type: GrantFiled: November 4, 1982Date of Patent: July 17, 1984Assignee: The Upjohn CompanyInventors: Lester J. Kaplan, Moses W. McMillan, Jacob Szmuszkovicz
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Patent number: 4440940Abstract: This disclosure describes 2- or 3-[(unsaturated or cyclopropylated alkyl)amino]phenyl compounds and derivatives useful as hypolipidemic and antiatherosclerotic agents.Type: GrantFiled: November 19, 1981Date of Patent: April 3, 1984Assignee: American Cyanamid CompanyInventor: Robert G. Shepherd
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Patent number: 4431834Abstract: This invention relates to certain bicyclic derivatives which are indane and tetralin compounds and which have herbicidal properties, to processes for their preparation, to herbicidal compositions containing them and to a method of using them as herbicides.Type: GrantFiled: March 29, 1982Date of Patent: February 14, 1984Assignee: Imperial Chemical Industries PLCInventor: David Cartwright
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Patent number: 4421931Abstract: Anthranilic acid amides are prepared by mixing phthalamic acid with a caustic alkali solution, a catalyst and a hypohalite, allowing the mixture to stand for from 1 to 1,000 seconds, then introducing the amine and thereafter addig acid until the pH of the mixture is from 6 to 8.The anthranilic acid amides obtainable by the process of the invention are valuable starting materials for the preparation of dyes, scents and pesticides.Type: GrantFiled: January 11, 1982Date of Patent: December 20, 1983Assignee: BASF AktiengesellschaftInventors: Peter Tonne, Winfried Ludwig, Gerhard Kilpper, Johannes Grimmer
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Patent number: 4387247Abstract: In the reduction of di- or polynitro aromatic compounds by gaseous H.sub.2 S over a solid catalyst, addition of CO gas promotes formation of amino groups from all nitro groups in the molecule. A preferred embodiment is reduction of 2,4- and/or 2,6-dinitrotoluene in vapor phase at 325.degree. C. over a supported iron or supported cobalt catalyst on a support comprising alumina. The amino products are useful for production of polyurethane resins.Type: GrantFiled: June 11, 1980Date of Patent: June 7, 1983Assignee: Allied CorporationInventors: Charles T. Ratcliffe, Geza Pap
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Patent number: 4379165Abstract: New amino-benzamides and their use for the treatment of epilepsy.Type: GrantFiled: May 18, 1981Date of Patent: April 5, 1983Assignee: Research CorporationInventor: Charles R. Clark
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Patent number: 4370497Abstract: The present invention relates to the use of telluroxides as mild and selective oxidizing agents serving to oxidize certain functions, notably >C.dbd.S groups, in the presence of other relatively easily oxidized functions which remain unaffected; telluroxides of interest as oxidizing agents include, for example, compounds of the formula: ##STR1## wherein R and R.sup.1, which may be the same or different, each represent an optionally substituted aryl or heterocyclic group; or R and R.sup.1 together with the tellurium atom therebetween represent a heterocyclic ring, which may contain one or more further heteroatoms, and which may carry substituents and/or fused aromatic rings.Type: GrantFiled: August 7, 1980Date of Patent: January 25, 1983Inventors: Derek H. R. Barton, Steven V. Ley, Clive A. Meerholz
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Patent number: 4360531Abstract: [2-Amino(substituted cycloaliphatic)]benzeneacetamide and benzamide compounds, e.g., trans-3,4-dichloro-N-methyl-N-[7-(1-pyrrolidinyl)-1,4-dioxaspiro[4.5]dec-8 -yl]benzeneacetamide, have useful analgesic activity and low abuse or physical dependence liability, or are useful as chemical intermediates for producing such analgesic compounds. Processes for their preparation are disclosed. Pharmaceutical compositions and methods of use are also disclosed.Type: GrantFiled: April 9, 1981Date of Patent: November 23, 1982Assignee: The Upjohn CompanyInventors: Moses W. McMillan, Jacob Szmuszkovicz
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Patent number: 4359476Abstract: N-[2-Amino(oxy or thio group) substituted-cycloaliphatic]phenylacetamide and -benzamide compounds, having the oxy- or thio group substituents on a cycloaliphatic ring carbon adjacent to either of the nitrogen bearing carbons of the cycloaliphatic ring, e.g., cis- and trans-4-bromo-N-[3-methoxy-2-(1-pyrrolidinyl)cyclohexyl]-N-methylbenzamide , and trans-3,4-dichloro-N-methyl-N-[7-(1-pyrridolinyl)-1,4-dioxaspiro[4.5]dec-6 -yl]benzeneacetamide, and salts thereof, have useful analgesic activity and low abuse liability in humans and valuable warm blooded animals. Processes for their production and pharmaceutical compositions and method of use are also disclosed.Type: GrantFiled: April 9, 1981Date of Patent: November 16, 1982Assignee: The Upjohn CompanyInventors: Lester J. Kaplan, Moses W. McMillan, Jacob Szmuszkovicz
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Patent number: 4348399Abstract: This disclosure describes novel 4-(monoalkylamino)phenyl alkane, alkene and alkyne carbinols, aldehydes, carboxylic acids and derivatives useful as hypolipidemic and antiatherosclerotic agents.Type: GrantFiled: February 2, 1978Date of Patent: September 7, 1982Assignee: American Cyanamid CompanyInventor: Robert G. Shepherd
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Patent number: 4343939Abstract: Glyolic acid esters and amides of bis(p-disubstitutedaminophenyl)carbinols are disclosed as color formers for use in transfer sets.Type: GrantFiled: April 22, 1981Date of Patent: August 10, 1982Assignee: American Cyanamid CompanyInventors: Frank F. Cesark, Robert J. Manfre, Daniel W. Thomas
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Patent number: 4340765Abstract: 4-Phenoxy-2-butene derivatives are disclosed as inhibitors of cytokinin plant growth regulatory activity and as possessing seed germination regulatory properties and senescence delaying activity when applied to plants. 4-Phenoxy-2-butene derivatives can also be useful as plant dwarfing agents, agents to retard seedling development or as herbicides.Type: GrantFiled: August 14, 1980Date of Patent: July 20, 1982Inventors: Gary M. Gray, George Schwartzkopf, Jr., J. T. Baker Chemical Co.
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Patent number: 4335054Abstract: Compounds of the formula I ##STR1## in which p, m, Z, R, R' and Y are as defined in claim 1, can be obtained in a simple and economical manner by a novel process which comprises reacting a halide of the formula ##STR2## with the corresponding acrylic acid derivative, in the presence of a base and of certain palladium catalysts, such as palladium acetate. The compounds (I), and functional derivatives prepared therefrom, are useful for the preparation of photocrosslinkable polymers, which can in particular be employed as (so-called) photoresists.Type: GrantFiled: May 8, 1981Date of Patent: June 15, 1982Assignee: Ciba-Geigy CorporationInventors: Hans-Ulrich Blaser, Dieter Reinehr, Alwyn Spencer
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Patent number: 4329344Abstract: This invention provides compounds, having major tranquilizing activity, of the formula (II): ##STR1## wherein R.sub.1 is a phenyl group optionally substituted by a fluorine, chlorine or bromine atom or an alkyl or alkoxyl group of up to 3 carbon atoms; R.sub.2 is a hydrogen atom or an alkyl group of up to 4 carbon atoms; R.sub.3 is a hydrogen atom or an amino group, a nitro group or a group of the formula NHCOR.sub.4 or NHCO.sub.2 R.sub.4 where R.sub.4 is an alkyl group of up to 4 carbon atoms optionally substituted by one, two or three chlorine atoms or by three fluorine atoms attached to the same carbon atom; n is 0, 1 or 2; and X is a group of the sub-formula (a), (b), (c) or (d): ##STR2## wherein R.sub.5 is an alkyl group of up to 4 carbon atoms; or a N-oxide thereof of the nitrogen atom to which the CHR.sub.2 --(CH.sub.2).sub.n --R.sub.1 moiety is attached; and salts thereof; pharmaceutical compositions containing them; processes for their preparation; and intermediates useful in said process.Type: GrantFiled: May 12, 1980Date of Patent: May 11, 1982Assignee: Beecham Group LimitedInventor: Michael S. Hadley
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Patent number: 4311846Abstract: This disclosure describes novel 4-[(monosubstituted-alkyl)amino]benzoic acids and analogs which are useful as hypolipidemic and antiatherosclerotic agents.Type: GrantFiled: August 11, 1980Date of Patent: January 19, 1982Assignee: American Cyanamid CompanyInventor: Robert G. Shepherd