Plural Rings In Acid Moiety With Nitrogen Bonded Directly To At Least One Of The Rings Patents (Class 560/48)
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Patent number: 4504491Abstract: New pesticidal e.g. insecticidal, compounds are of formula ##STR1## wherein X represents hydrogen, halogeno or an alkyl group, Z represents hydrogen, an alkyl group or a cyano or ethynyl group and R represents the residue of a carboxylic acid RCOOH which is an acid forming a pesticidal compound when esterified with .alpha.-cyano-3-phenoxybenzyl alcohol.The compounds can be prepared by conventional methods e.g. esterification.Type: GrantFiled: July 6, 1982Date of Patent: March 12, 1985Assignee: National Research Development CorporationInventors: Michael Elliott, Norman F. Janes, Bhypinder P. S. Khambay
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Patent number: 4495174Abstract: A long-acting, local anesthetic, comprising a polymeric phosphazene backbone, and 2-amino-4-picoline radical having local anesthetic activity and an amino functional group on the ring of said radical through which said radical is covalently attached to the phosphazene backbone by a phosphorous-nitrogen single bond is disclosed along with medicaments containing such anesthetics.Type: GrantFiled: June 21, 1982Date of Patent: January 22, 1985Assignee: Research CorporationInventors: Harry R. Allcock, Paul E. Austin, Thomas X. Neenan
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Patent number: 4489090Abstract: This disclosure describes novel dibenzocycloalkanamido-benzoic acids and esters. Also described are dibenzothioxanthenyl-benzoic acids and esters. These compounds are useful pharmaceutical agents for ameliorating atherosclerosis by inhibiting the formation and development of atherosclerotic lesions in the arterial walls of mammals.Type: GrantFiled: May 6, 1983Date of Patent: December 18, 1984Assignee: American Cyanamid CompanyInventors: Vern G. DeVries, Robert G. Shepherd
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Patent number: 4472466Abstract: Fluorinated esters based on multi-ring anhydride systems are disclosed which have excellent anti-soiling properties, durability and resistance to laundering. The compounds are represented by the formula ##STR1## wherein n is 2 or 3, Q is a linking group such as --CO--, --O--, or (C.sub.a H.sub.2a+2-n --(O.sub.2 C).sub.n, R.sub.f is a fluorinated radical, and R is derived from an epoxide such as ethylene oxide or epichlorohydrin. Also disclosed are polyester and nylon fibers having these compounds incorporated therein, and a process for producing such soil-repellent fibers.Type: GrantFiled: March 8, 1982Date of Patent: September 18, 1984Assignee: American Hoechst CorporationInventors: Michael G. Kelly, Willi R. Steckelberg
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Patent number: 4464358Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 stands for hydrogen or a defined hydrocarbyl or halogenoalkenyl radical, R.sup.2 stands for a defined hydrocarbyl, halogenoalkenyl or furylmethyl radical, R.sup.3 is a substituent at position (a) or (b) and stands for a hydroxy or defined alkoxy or alkanoyloxy radical, R.sup.4 stands for a defined alkoxy, cyanoalkoxy or alkenyloxy radical or a defined amino acid residue or peptide residue, and n stands for 1, 2 or 3, and pharmaceutically-acceptable salts thereof. Processes for the manufacture of the compounds. Pharmaceutical compositions comprising one of the compounds and a pharmaceutical diluent or carrier. The compounds are antagonists at the opiate receptors, and most of them are selective .delta.-receptor antagonists.Type: GrantFiled: August 30, 1982Date of Patent: August 7, 1984Assignee: Imperial Chemical Industries PLCInventor: Michael T. Cox
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Patent number: 4451664Abstract: An improved process for preparing diaryl esters of a monohydroxy aromatic compound with dicarboxylic acids is disclosed, in which the esterification reaction is optimized by continuously removing water and/or other by-products of the reaction from the reactor, while supplying to the reactor a make-up amount of the monohydroxy aromatic compound containing no more than about 100 ppm of water. The make-up stream may be obtained by stripping the by-product stream of water and other by-products of the reaction.Type: GrantFiled: September 24, 1982Date of Patent: May 29, 1984Assignee: Occidental Chemical CorporationInventor: Gautam R. Ranade
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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: 4435589Abstract: Process for the preparation of dimethyl succinylosuccinate, or the disodium salt thereof, by condensation of dimethyl succinate in a 35-45 percent by weight solution of sodium methylate in methanol, and a process for the preparation of dianilinodihydroterephthalic acids, the dimethyl esters and salts thereof, and of dianilinoterephthalic acids, and the dimethyl esters and salts thereof, starting from the disodium salt of dimethyl succinylosuccinate prepared according to the new process, without intermediate isolation.Type: GrantFiled: January 21, 1982Date of Patent: March 6, 1984Assignee: Bayer AktiengesellschaftInventors: Meinhard Rolf, Detlef-Ingo Schutze, Rutger Neeff, Hans-Volker Runzheimer
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Patent number: 4423051Abstract: This disclosure describes novel 4-[(cycloalkyl or cycloalkenyl substituted)amino, alkylamino or alkenylamino]-benzoic acids, salts and derviatives of these such as cycloalkylamino, cycloalkenylamino, cycloalkyl-alkylamino, cycloalkyl-alkenylamino, cycloalkenyl-alkylamino, and cycloalkyl-cycloalkylamino benzoic acids and derivatives and suitable salts of these; these compounds are useful as hypolipidemic and antiatherosclerotic agents.Type: GrantFiled: July 20, 1981Date of Patent: December 27, 1983Assignee: American Cyanamid CompanyInventor: Robert G. Shepherd
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Patent number: 4407823Abstract: Phenylacetic acid derivatives of the formula ##STR1## wherein n is an integer of 2 to 5; ##STR2## R.sub.1 is hydrogen, halogen, trifluoromethyl, nitro or amino; R.sub.2 and R.sub.3 each independently is hydrogen or lower alkyl; or together form an ethylene group;X.sub.1 represents two hydrogen atoms or an oxo group; andY.sub.1 is cyano, hydroxyamidocarbonyl, carbamoyl, 5-tetrazolyl or carboxyl;and for derivatives wherein Y is carboxyl, salts thereof with physiologically compatible bases, esters thereof from physiologically acceptable alcohols and amides thereof from physiologically acceptable amines have valuable pharmacological activity, e.g., as antiinflammatory agents.Type: GrantFiled: November 5, 1979Date of Patent: October 4, 1983Assignee: Schering AktiengesellschaftInventors: Gerald Kirsch, Joachim-Friedrich Kapp, Clemens Rufer
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Patent number: 4390714Abstract: Tertiary aromatic amines derived from aminoglutethimide or para-aminophenylacetic acid act as accelerators for the peroxide catalyzed polymerization of acrylic resins, especially methacrylates, acrylates and unsaturated polyesters. The amines are characterized by good hardening, strength, color and toxicity characteristics, and are thereby particularly suited for use in the filling and restoration of human teeth and the cementing of bone.Type: GrantFiled: July 7, 1980Date of Patent: June 28, 1983Assignee: American Dental Association Health FoundationInventor: Harold Argentar
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Patent number: 4389413Abstract: The 9,11-methano-13-aza-11a-carbathrombanoic acid analogues of the general formula: ##STR1## [wherein A represents ##STR2## (in which m is an integer of 1 to 6, the double bond between the carbon atoms in positions 5 and 6 in (iv) is in cis or trans-configuration or a mixture thereof and the phenylene group in (iv) represents o-, m- or p-phenylene), R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group of 1 to 12 carbon atoms, two R.sup.2 both represent hydrogen atoms or methyl groups, R.sup.3 represents a hydrogen atom or a hydroxy group, R.sup.4 represents a single bond or a straight- or branched-chain alkylene group of 1 to 5 carbon atoms, R.sup.Type: GrantFiled: July 22, 1981Date of Patent: June 21, 1983Inventors: Nobuyuki Hamanaka, Shinsuke Hashimoto, Masaki Hayashi
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Patent number: 4388459Abstract: This disclosure describes novel 4-[(cycloalkyl or cycloalkenyl substituted)amino, alkylamino or alkenylamino]phenyl compounds, salts and derivatives of these such as cycloalkylamino, cycloalkenylamino, cycloalkyl-alkylamino, cycloalkyl-alkenylamino, cycloalkenyl-alkylamino, and cycloalkyl-cycloalkylamino phenyl compounds and derivatives and suitable salts of these; these compounds are useful as hypolipidemic and antiatherosclerotic agents.Type: GrantFiled: November 28, 1980Date of Patent: June 14, 1983Assignee: American Cyanamid CompanyInventor: Robert G. Shepherd
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Patent number: 4387241Abstract: This disclosure describes novel 16-aryloxy-17,18,19,20-tetranorprostanoic acids and derivatives thereof useful as bronchodilators and as hypotensive and contraceptive agents.Type: GrantFiled: November 1, 1974Date of Patent: June 7, 1983Assignee: American Cyanamid CompanyInventors: Charles V. Grudzinskas, Martin J. Weiss
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Patent number: 4382954Abstract: Compounds represented by the formula ##STR1## wherein R and R.sup.1 are independently hydrogen or lower alkyl; R.sup.2 is lower alkenyl, lower alkynyl or --CH.sub.2 X wherein X is halogen, hydroxyl, lower alkoxy, lower alkylthio or a furanyl ring; and Z is hydroxyl, lower alkoxy or --NR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are independently hydrogen or lower alkyl possess fungicidal activity. Moreover, some of the compounds of this invention also possess herbicidal activity.Type: GrantFiled: January 27, 1982Date of Patent: May 10, 1983Assignee: Chevron Research CompanyInventor: David C. K. Chan
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Patent number: 4372776Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.3 each is hydrogen or R.sup.1 and R.sup.3 together form a second carbon-to-nitrogen bond, R.sup.2 is hydrogen or cyano, R.sup.4 is alkyl and Ar is one of certain aromatic moieties.The compounds can be used as abscission agents for the loosening of fruit and/or leaves on plants.Type: GrantFiled: October 16, 1981Date of Patent: February 8, 1983Assignee: Shell Oil CompanyInventors: Janet A. Day, Robert J. G. Searle
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Patent number: 4371547Abstract: 2-Benzylideneglutaraldehydes of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen or a substituent selected from the group consisting of halo, lower-alkyl, phenyl, carboxy, lower-alkoxycarbonyl, phenoxycarbonyl, aminocarbonyl, hydroxysulfonyl, nitro, cyano, hydroxy, lower-alkoxy and phenoxy, a method of use thereof as disinfectants, disinfectant compositions comprising them, and 2,6-dialkoxy-3-(.alpha.-alkoxybenzyl)tetrahydropyrans of the formula ##STR2## where R.sup.1, R.sup.2 and R.sup.3 are as defined above and R.sup.4 and R.sup.5 independently are alkyl of one to four carbon atoms, which are intermediates for their preparation are disclosed.Type: GrantFiled: August 21, 1981Date of Patent: February 1, 1983Assignee: Sterling Drug Inc.Inventors: Wolfgang Munzenmaier, Heinz Eggensperger, Helmut H. Ehlers, Wolfgang Beilfuss, Lothar Bucklers, Hans-Peter Harke
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Patent number: 4367344Abstract: A process for the preparation of 1-amino-cyclopropane-carboxylic acid or a derivative thereof of the general formula ##STR1## in which R.sup.1 represents hydrogen or alkyl andR.sup.2 represents hydrogen or a radical --CO--R.sup.3, whereinR.sup.3 represents hydrogen, alkyl, aryl or alkoxy, in which a 2-cycloamino-4-methylthio-butanoic acid ester ("acyl-methionine ester") of the general formula ##STR2## in which R.sup.3 has the meaning indicated above andR.sup.4 represents alkyl,is reacted successively with dimethyl sulphate and an alkali metal alcoholate, if appropriate in the presence of a diluent, at a temperature between 80.degree. C. and 150.degree. C., the product is then optionally saponified with aqueous alkali metal hydroxide or alkaline-earth metal hydroxide at a temperature between 70.degree. C. and 150.degree. C., the reaction mixture thereby obtained is acidified with concentrated hydrochloric acid at a temperature between 0.degree. C. and 30.degree. C.Type: GrantFiled: August 22, 1980Date of Patent: January 4, 1983Assignee: Bayer AktiengesellschaftInventor: Bernd Gallenkamp
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Patent number: 4360690Abstract: 1-Aryl-cyclopropane-1-carboxylic acid esters of the formula ##STR1## in which R.sup.1 represents a hydrogen atom, a cyano radical or an alkyl, alkenyl or alkinyl radical within each case up to 7 carbon atoms, andR.sup.2 represents a phenyl radical which is substituted by halogen and/or optionally halogen-substituted phenoxy, with the proviso that the radical R.sup.2 in total contains at least one fluorine substituent,R.sup.3 and R.sup.4, which can be identical or different, represents a fluorine, chlorine or bromine atom or a methyl radical,R.sup.5 represents a hydrogen or halogen atom or a methyl or methoxy radical, andR.sup.6 represents a hydrogen or halogen atom, a cyano nitro or amino radical or an optionally halogen-substituted radical selected from C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy and C.sub.1 to C.sub.4 alkylthio,or whereinthe two radicals R.sup.5 and R.sup.6 together represent an optionally halogen-substituted C.sub.1 or C.sub.Type: GrantFiled: June 12, 1981Date of Patent: November 23, 1982Assignee: Bayer AktiengesellschaftInventors: Rainer Fuchs, Klaus Naumann, Ingeborg Hammann, Bernhard Homeyer, Wolfgang Behrenz, Wilhelm Stendel
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Patent number: 4354033Abstract: Anthranilic acid esters having the generic formula: ##STR1## have been discovered. In the above formula (I) R.sub.1, R.sub.2 and R.sub.3 represent any of hydrogen, chlorine, methoxy and methyl groups and X represents a straight or branched alkyl chain comprising 1 to 4 carbon atoms. These esters are anti-inflaments, blood platelet aggregation inhibitors and prostaglandin synthetase inhibitors.The compounds of the above formula (I) may be prepared by reacting alkali metal salt of a compound of the formula (II): ##STR2## in which R.sub.1, R.sub.2, R.sub.3 and X are the same as before with the compound of formula (III): ##STR3## in which R.sub.3 has the same meaning as before and z represents a chlorine or a bromine radical.Type: GrantFiled: August 31, 1981Date of Patent: October 12, 1982Assignee: Council of Scientific & Industrial ResearchInventors: Nanduri Bhanumati, Pralhad B. Sattur
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Patent number: 4350822Abstract: Novel para-[aryl(alkyl or alkenyl)amino]benzoic acids, esters, pharmaceutically acceptable salts and pharmaceutical compositions thereof and a method of lowering serum lipid levels in mammals therewith.Type: GrantFiled: March 15, 1979Date of Patent: September 21, 1982Assignee: American Cyanamid CompanyInventors: Jay D. Albright, Thomas G. Miner, Robert G. Shepherd
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Patent number: 4333951Abstract: Novel 2-amino-6-biphenylacetic acids, esters, and metal salts are provided of the formula: ##STR1## wherein R represents hydrogen or lower alkyl, R.sup.1 represents fluoro, chloro, bromo, lower-alkyl or amino; R.sup.2 represents lower-alkyl, lower-alkoxy, fluoro, chloro, bromo, amino or trifluoromethyl; n is 0-3 and m is 0-2, and the pharmaceutically acceptable salts thereof. The compounds exhibit muscle relaxant activity, and are also useful as anti-inflammatory agents.Type: GrantFiled: July 2, 1980Date of Patent: June 8, 1982Assignee: A. H. Robins Company, Inc.Inventor: David A. Walsh
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Patent number: 4308394Abstract: Compounds added to initiate photopolymerization of monomers to produce polymeric coatings include compounds of the formula ##STR1## wherein Ar is phenyl or naphthyl,R is hydrogen, alkyl with 1-4 carbon atoms, alkoxy with 1-4 carbon atoms, halogen, dialkylamino with 1-4 carbon atoms in each alkyl group, carboxyl, or alkoxycarbonyl with 1-4 carbon atoms in the alkoxy group,X is alkyl having 3 to 6 carbon atoms or alkyl having 6 to 72 carbon atoms interrupted by at least one member selected from the group consisting of ##STR2## and the precursor of X being a polyol having 3 to 6 hydroxyls and having a hydroxyl number of from 100 to 1850,R.sub.1 is hydrogen or methyl,n is a number with a value from about 2 to about 5, andn+m is a number with a value from about 3 to about 6.Type: GrantFiled: June 8, 1979Date of Patent: December 29, 1981Assignee: Bayer AktiengesellschaftInventors: Karl-Ernst Shuster, Hans Rudolph, Wolfram Mayer, Hans J. Rosenkranz
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Patent number: 4307112Abstract: 9-deoxy-9A-methylene-isosteres of PGI.sub.2, including processes for their preparation and pharmaceutical and veterinary compositions containing same, are disclosed. The compounds are useful as therapeutic agents, for example as anti-aggregating agents, disaggregating agents, and as vasodilators.Type: GrantFiled: February 26, 1980Date of Patent: December 22, 1981Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Carmelo Gandolfi, Carlo Passarotti, William Fava, Angelo Fumagalli, Franco Faustini, Roberto Ceserani
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Patent number: 4272546Abstract: This disclosure describes esters of 4-(monoalkylamino)benzoic acids with hydroxyalkanoic acids and derivatives, phenols, or 3-pyridinols useful as hypolipidemic and antiatherosclerotic agents.Type: GrantFiled: October 22, 1979Date of Patent: June 9, 1981Assignee: American Cyanamid CompanyInventor: Robert G. Shepherd
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Patent number: 4271188Abstract: Compounds having hypolipidaemic activity which are substituted aralkylanilines, their preparation and pharmaceutical compositions containing them.Type: GrantFiled: December 17, 1979Date of Patent: June 2, 1981Assignee: Beecham Group LimitedInventor: Richard M. Hindley
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Patent number: 4268685Abstract: Esters of salicylamide with anti-inflammatory and analgesic action are disclosed.These esters have the following general formula: ##STR1## wherein R is a radical of an acid selected among d-2-(6'-methoxy-2'-naphtyl)-propionic acid, 2[[3-(trifluoromethyl)phenyl]-amino]-3-pyridine carboxylic acid, 2- {[3-(trifluoromethyl)-phenyl]-amino}-3-pyridincarboxylic acid, 2-(4-isobutyl-phenyl)-propionic acid, 4-allyloxy-3-chloro-phenylacetic acid, 2-(3-benzoylphenyl)-propionic acid, 2-[(2,3-dimethylphenyl)amino]-benzoic acid and 2[[3-trifluoromethyl)phenyl]-amino]benzoic acid.The process for preparing the subject esters comprises reacting a halide, preferably a chloride of the desired acid, with a solution of salicylamide.Type: GrantFiled: March 12, 1980Date of Patent: May 19, 1981Assignee: Neopharmed S.p.A.Inventor: Alberto Reiner
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Patent number: 4266069Abstract: The invention concerns the novel compounds dialkyl 2-(3-fluoro-4-nitrophenyl)-2-methylmalonate IIIa and dialkyl 2-(3-fluoro-4-aminophenyl)-2-methylmalonate IVa useful as intermediates in an improved process for making 2-(2-fluoro-4-biphenylyl)propionic acid, known as flurbiprofen, having the formula ##STR1## and ester thereof. It has anti-inflammatory activity which is about 240 times that of aspirin and analgesic activity which is about 180 times that of aspirin in standard laboratory tests. However, despite this high activity, the toxicity (LD.sub.50) is only 1.2 to 2.4 times greater than that of aspirin in standard laboratory tests.Also within the invention is a novel method of making the above intermediates and analogs thereof useful to prepare corresponding biaryl compounds which have pharmaceutical uses.Type: GrantFiled: December 19, 1979Date of Patent: May 5, 1981Assignee: The Upjohn CompanyInventor: Jerry A. Walker
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Patent number: 4261898Abstract: The invention relates to Si-modified phthalic acid derivatives (acids, esters and anhydrides) of the formula I ##STR1## in which R.sub.1 and R.sub.2 independently of one another are --OH, alkoxy with 1-12 C atoms or phenoxy or R.sub.1 and R.sub.2 together are the --O--group, X is a ##STR2## R.sub.3 is alkyl with 2-7 C atoms, cycloalkyl with 5-7 C atoms, benzyl or ##STR3## Q is methyl, phenyl or --OQ.sub.3 and Q.sub.1, Q.sub.2 and Q.sub.3 independently of one another are alkyl with 1-6 C atoms or phenyl.The products of the invention are prepared by reacting the corresponding allylamino-phthalic anhydrides or allylamino-phthalic acid esters with compounds of the formula III ##STR4## They are used as adhesion promoters, for example between inorganic solids and organic resins. They may also be used for the preparation of other Si-modified adhesion promoters, and as curing agents for epoxide resins.Type: GrantFiled: June 18, 1979Date of Patent: April 14, 1981Assignee: Ciba-Geigy CorporationInventors: Roland Darms, Siegfried Wyler, Gerd Greber
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Patent number: 4255313Abstract: The products of the invention are end-capped polyimide oligomers prepared from a dianhydride of an aromatic tetracarboxylic acid such as 3,3'4',4'-benzophenonetetracarboxylic acid, an aromatic diamine, and a 1-(aminoaryl)-3-hydroxy-3-methyl-1-butyne. The structure of the polyimide oligomers is shown in FIG. 3.Type: GrantFiled: April 20, 1979Date of Patent: March 10, 1981Assignee: Gulf Oil CorporationInventors: Patricia A. Antonoplos, William J. Heilman
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Patent number: 4252981Abstract: Covers a process for the production of methylene bis(methylanthranilate) which comprises the steps of condensing methylanthranilate with formaldehyde in the presence of a siliceous catalyst.Type: GrantFiled: December 3, 1979Date of Patent: February 24, 1981Assignee: Texaco Development Corp.Inventors: Edward T. Marquis, Ernest L. Yeakey
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Patent number: 4251417Abstract: The products of the invention are acetylene end-capped polyimide oligomers prepared from a dianhydride of an aromatic tetracarboxylic acid such as 3,3',4,4' benzophenonetetracarboxylic acid, an aromatic triamine, and an acetylene-substituted aromatic monoamine. The structure of the polyimide oligomers is shown in FIG. 3.Type: GrantFiled: April 25, 1979Date of Patent: February 17, 1981Assignee: Gulf Oil CorporationInventors: Wai Y. Chow, William J. Heilman
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Patent number: 4251418Abstract: The products of the invention are acetylene end-capped polyimide oligomers prepared from a dianhydride of an aromatic tetracarboxylic such as 3,3', 4,4'-benzophenonetetracarboxylic acid, an aromatic diamine, and a propargyl ester of an amino-substituted aromatic acid such as aminobenzoic acid. The structure of the polyimide oligomers is shown in FIG. 3.Type: GrantFiled: April 27, 1979Date of Patent: February 17, 1981Assignee: Gulf Oil CorporationInventors: Wai Y. Chow, S. Paul Thackaberry
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Patent number: 4251419Abstract: The products of the invention are vinyl end-capped oligomers which have the structure as shown in FIG. 3. The products are prepared from either of two (2) precursors. The first precursor is a compound which has the structure as shown in FIG. 2. The second precursor is a complex amine salt which has the structure shown in FIG. 5.Type: GrantFiled: April 5, 1979Date of Patent: February 17, 1981Assignee: Gulf Oil CorporationInventors: William J. Heilman, Daniel J. Hurley
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Patent number: 4251420Abstract: The products of the invention are end-capped polyimide oligomers prepared from a dianhydride of an aromatic tetracarboxylic acid such as 3,3'4,4'-benzophenonetetracarboxylic acid, an aromatic triamine, and a 1-(aminoaryl)-3-hydroxy-3-methyl-1-butyne. The structure of the polyimide oligomers is shown in FIG. 3.Type: GrantFiled: April 23, 1979Date of Patent: February 17, 1981Assignee: Gulf Oil CorporationInventors: Patricia A. Antonoplos, William J. Heilman
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Patent number: 4249021Abstract: Substituted 1-oxo-2,2-disubstituted-5-indanacetic acids and their salts, esters and amides are disclosed. The products display a dual pharmaceutical utility in that they exhibit diuretic, saluretic and uricosuric activity.Type: GrantFiled: February 26, 1979Date of Patent: February 3, 1981Assignee: Merck & Co., Inc.Inventors: Edward J. Cragoe, Jr., Haydn W. R. Williams, Otto W. Woltersdorf, Jr.
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Patent number: 4242523Abstract: An improved process for the preparation of para-nitroso-diphenyl-hydroxylamines is discussed. In the improved process the dimerizing rearrangement of a nitroso benzene is performed in the presence of at least 0.5 mole of a Lewis acid per mole of nitroso compound.Type: GrantFiled: August 20, 1979Date of Patent: December 30, 1980Assignee: Akzona IncorporatedInventors: Paul K. Battey, Manfred Bergfeld, Peter Hope
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Patent number: 4238351Abstract: Polymers comprising terephthalyl-or oxal arylamide groups represent excellent light stabilizers for synthetic, semi-synthetic and/or naturally occurring organic materials.Type: GrantFiled: April 12, 1976Date of Patent: December 9, 1980Assignee: Bayer AktiengesellschaftInventors: Franz Alfes, Wolfgang Jacob, Karl-Heinrich Meyer, Ludwig Bottenbruch
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Patent number: 4230878Abstract: This disclosure describes 4-[(unsaturated or cyclopropylated alkyl)amino]benzoic acids and derivatives useful as hypolipidemic and antiatherosclerotic agents.Type: GrantFiled: March 8, 1978Date of Patent: October 28, 1980Assignee: American Cyanamid CompanyInventor: Robert G. Shepherd
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Patent number: 4227015Abstract: Aryl substituted diketones and keto-esters, useful as antiviral agents and insecticides, are prepared by reacting an arylalkyl or arylalkenyl iodide with a metal salt of the appropriate diketone or keto-ester. The intermediate iodides are prepared by condensing a methyl cyclopropyl ketone with an aromatic aldehyde to give an arylvinyl cyclopropyl ketone, reducing the latter to an arylethyl cyclopropyl carbinol or arylvinyl cyclopropyl carbinol, treating the carbinol with phosphorus tribromide and then with zinc bromide to give an arylalkyl or arylalkenyl bromide, and then replacing the bromine atom by iodine.Type: GrantFiled: February 14, 1979Date of Patent: October 7, 1980Assignee: Sterling Drug Inc.Inventor: Joseph C. Collins
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Patent number: 4227014Abstract: This disclosure describes novel 4-[(cycloalkyl or cycloalkenyl substituted)amino, alkylamino or alkenylamino]-benzoic acids, salts and derivatives of these such as cycloalkylamino, cycloalkenylamino, cycloalkyl-alkylamino, cycloalkylalkenylamino, cycloalkenyl-alkylamino, and cycloalkyl-cycloalkylamino benzoic acids and derivatives and suitable salts of these; these compounds are useful as hypolipidemic and antiatherosclerotic agents.Type: GrantFiled: February 27, 1978Date of Patent: October 7, 1980Assignee: American Cyanamid CompanyInventor: Robert G. Shepherd
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Patent number: 4221815Abstract: Acyl-aminoalkyl-benzoic acid and derivates thereof show a blood sugar lowering effect upon oral administration and can be used as orally applicable hypoglycemiants.Type: GrantFiled: January 2, 1976Date of Patent: September 9, 1980Assignee: Hoechst AktiengesellschaftInventors: Rudi Weyer, Volker Hitzel, Karl Geisen, Werner Pfaff
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Patent number: 4221814Abstract: A terephthalic acid monoamide derivative of the formula: ##STR1## (wherein R is a straight- or branched-chain lower alkyl group; R' and R" may be the same or different, and represent a hydrogen atom, or a straight- or branched-chain lower alkyl group) or pharmaceutically acceptable salts thereof are disclosed. A process for preparing such terephthalic acid monoamide derivative or its salts, as well as an anti-allergic agent containing such derivative or its salts as an effective ingredient are also disclosed.Type: GrantFiled: June 1, 1979Date of Patent: September 9, 1980Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Sakae Takaku, Takashi Mori, Yasushi Murakami, Yoshiyuki Ohsugi, Shigeyuki Kataoka, Yasuhisa Takeda, Takashi Matsuno, Yoshimitsu Iida, Akiko Ariga, Akira Okazaki, Kazuo Igusa, Toshichika Ogasawara, Minoru Shindo
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Patent number: 4218475Abstract: Substituted or unsubstituted benzylaminobenzene alkanoic or alkenoic acids are disclosed as hypolipidemic agents and especially as hypocholesterolemic agents; along with a method of use and pharmaceutical compositions thereof.Type: GrantFiled: October 26, 1978Date of Patent: August 19, 1980Assignee: The Dow Chemical CompanyInventors: Eugene R. Wagner, Donald P. Matthews, Alfred A. Renzi
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Patent number: 4216172Abstract: A process for the preparation of a cyclobutanone of the formula ##STR1## in which R.sup.1 to R.sup.6 each independently is a hydrogen, halogen, cyano, alkoxy, alkoxycarbonyl, carboxamido, dialkylphosphono, alkyl, cycloalkyl, aryl, aralkyl or alkenyl radical, or two of them together with the carbon atom to which each is linked form a ring,comprising reacting an N,N-disubstituted carboxylic acid amide of the formula ##STR2## in which R.sup.7 and R.sup.8 each independently is an alkyl, cycloalkyl, alkenyl, aryl or aralkyl radical or together form a ring, with an inorganic acid halide, and then reacting the product with a tertiary amine, an olefin of the formula ##STR3## and a Lewis acid, and subsequently hydrolyzing the mass. Preferably isobutyric acid dimethylamide is employed as the carboxylic acid amide, phosgene is employed as the inorganic acid halide, triethylamine is employed as the tertiary amine and zinc chloride or titanium tetrachloride is employed as the Lewis acid.Type: GrantFiled: March 13, 1978Date of Patent: August 5, 1980Assignee: Bayer AktiengesellschaftInventors: Hans-Georg Heine, Willy Hartmann
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Patent number: 4214093Abstract: Amino- or guanidino-1,2,3,4-tetrahydro-1-naphthoic esters represented by the formula, ##STR1## wherein R.sub.1 is --NH.sub.2 or ##STR2## R.sub.3 is --H, --R.sub.4, --O--R.sub.4, --NHCOCH.sub.3, a halogen, --CN, ##STR3## --COOH, --COOR.sub.4, ##STR4## or --(CH.sub.2).sub.n --COOCH.sub.2 --CO--R.sub.5 ; R.sub.5 is --O--R.sub.4, --NH.sub.2 or ##STR5## n is 0, 1 or 2, and R.sub.4 is a lower alkyl, or pharmaceutically acceptable acid addition salts thereof. Owing to their inhibitory activity on proteolytic enzymes the said esters and acid addition salts thereof are useful in the therapy of diseases caused by such enzymes.Type: GrantFiled: April 16, 1979Date of Patent: July 22, 1980Assignee: Torii & Co., Ltd.Inventors: Setsuro Fujii, Yojiro Sakurai, Toyoo Nakayama, Ryoji Matsui
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Patent number: 4209633Abstract: The maleic acid adduct of anthracene is used as a starting material for 11-amino-12-carboalkoxy-9,10-dihydro-9,10-ethanoanthracene, which through reaction with nitrous acid in a protic solvent provides an 11-substituted-12-carboalkoxy-10,11-dihydro-5,10-methano-5H-dibenzo[a,d]cy cloheptene which is then converted into the useful intermediate 12-carboxy-10,11-dihydro-5,10-methano-5H-dibenzo[a,d]cycloheptene.Type: GrantFiled: April 17, 1978Date of Patent: June 24, 1980Assignee: Riker Laboratories, Inc.Inventor: Walton J. Hammar
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Patent number: 4207341Abstract: Phenylacetic acid derivatives of the formula ##STR1## wherein A is an aryl radical optionally substituted by halogen, trifluoromethyl, alkyl, alkoxy, alkenyloxy, alkoxyalkoxy, alkyl-substituted amino or aryloxy, or a heterocyclic ring system optionally substituted by halogen, alkyl or alkoxy,Y is a valency bond or an optionally branched alkylene radical containing up to 3 carbon atoms, andR.sub.1 and R.sub.2 each independently is hydrogen or a lower alkyl radical,or a physiologically compatible salt or ester thereof, exhibit marked hypoglycaemic and hypolipidaemic activity.Type: GrantFiled: July 1, 1976Date of Patent: June 10, 1980Assignee: Boehringer-Mannheim GmbHInventors: Manfred Hubner, Hans Kuhnle, Ernst-Christian Witte, Ruth Heerdt, Rudi Weyer, Volker Hitzel
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Patent number: 4187316Abstract: Compounds of the following general formula and salts thereof are irreversible inhibitors of .gamma.-aminobutyric acid transaminase: ##STR1## wherein R.sub.1 is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, the radical ##STR2## wherein R.sub.4 is hydrogen, a straight or branched alkyl group having from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.2 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, the group-NR.sub.5 R.sub.6wherein each of R.sub.5 and R.sub.6 is hydrogen or a straight or branched alkyl group having from 1 to 4 carbon atoms, or ##STR3## wherein R.sub.7 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; and R.sub.3 is hydrogen or bromine.Type: GrantFiled: January 12, 1978Date of Patent: February 5, 1980Assignee: Merrell Toraude et CompagnieInventors: Brian W. Metcalf, Michel Jung
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Patent number: 4185115Abstract: Novel para-[aryl(alkyl or alkenyl)amino]benzoic acids, esters, pharmaceutically acceptable salts and pharmaceutical compositions thereof and a method of lowering serum lipid levels in mammals therewith.Type: GrantFiled: March 12, 1975Date of Patent: January 22, 1980Assignee: American Cyanamid CompanyInventors: Jay D. Albright, Thomas G. Miner, Robert G. Shepherd