The Benzene Ring Is Part Of A Substituent Which Contains Nitrogen Patents (Class 564/50)
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Patent number: 5142095Abstract: The present invention is novel diarylalkanoids having activity as lipoxygenase inhibitors, novel pharmaceutical compositions therefor, and novel methods of use in treating asthma, allergies, cardiovascular diseases, migraines, psoriasis and immunoinflammatory diseases for diarylalkanoids. The compounds of this invention are also useful as cytoprotective agents.Type: GrantFiled: August 17, 1989Date of Patent: August 25, 1992Assignee: Warner-Lambert CompanyInventors: David T. Connor, Daniel L. Flynn
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Patent number: 5130430Abstract: The invention encompasses compounds of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 represent organic or inorganic substituents; X represents hydrogen, halogen, hydroxy or amino and W represents phenyl, thienyl or pyridyl, each of which may be unsubstituted or mono or disubstituted with organic or inorganic substituents.These compounds are highly selective agonists, antagonists or inverse agonists for GABA a brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.Type: GrantFiled: October 31, 1990Date of Patent: July 14, 1992Assignee: Neurogen CorporationInventor: Kenneth Shaw
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Patent number: 5106873Abstract: This invention relates to novel compounds which are ACAT inhibitors rendering them useful in lowering blood cholesterol levels. The compounds contain two urea or thiourea, amide, or amine moieties or combinations of said moieties and have the following general formula: ##STR1## wherein m and n are zero or one, W and YNH and ##STR2## form the urea, thiourea, amide or amine moieties; and R.sub.1 and R .sub.2 are hydrogen or a hydrocarbon radical.Type: GrantFiled: June 26, 1990Date of Patent: April 21, 1992Assignee: Warner-Lambert CompanyInventors: Patrick M. O'Brien, Drago R. Sliskovic, Michael W. Wilson
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Patent number: 5091419Abstract: Diurea derivatives are provided which are represented by the following general formula and salts thereof: ##STR1## The above compounds inhibit acyl-coenzyme A cholesterol acyl-transferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester on the smooth muscle of arterial wall in the blood vessels.Type: GrantFiled: October 2, 1990Date of Patent: February 25, 1992Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
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Patent number: 5090914Abstract: Macromolecular species such as enzymes, proteins, drugs, and solid supports which contain reactive carbonyl groups or groups which are readily converted to reactive carbonyl groups are modified by reaction with a compound of the formula ##STR1## in which R.sup.1 is H, C.sub.1 -C.sub.20 alkyl, phenyl, (C.sub.1 -C.sub.10 alkyl)-substituted phenyl, or phenyl-substituted C.sub.1 -C.sub.10 alkyl; R.sup.2 is C.sub.2 -C.sub.5 alkylene or (C.sub.1 -C.sub.4 alkoxy)-substituted C.sub.2 -C.sub.5 alkylene; R.sup.3 is ##STR2## R.sup.4 is H or C.sub.1 -C.sub.4 alkyl; n is at least 5; and m is zero or 1.Type: GrantFiled: August 24, 1990Date of Patent: February 25, 1992Assignee: Xoma CorporationInventors: Dayton T. Reardan, Dane A. Goff
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Patent number: 5068306Abstract: Disclosed herein is a process for the preparation of an o-aminophenyl derivative of a polyalkyleneoxy polyamine which comprises adding a polyalkyleneoxy polyamine to a dispersion or solution of an isatoic anhydride under reaction conditions sufficient to form the corresponding o-aminophenyl derivative. Also disclosed is an o-aminophenyl derivative of a modified polyamine comprising a backbone portion containing at least one polyalkyleneoxy moiety and one or more internal urea, biuret, amide, thiourea, dithiobiuret, or thioamide moieties, and a plurality of o-aminophenyl end groups wherein each o-aminophenyl group is separated from each urea, biuret, amide, thiourea, dithiobiuret, or thioamide moiety by at least one alkylene, cycloalkylene, aralkylene, arylene, or alkyleneoxy moiety with 4-20 carbon atoms, or at least one polyalkyleneoxy moiety containing from 2-50 alkyleneoxy units; as well as prepolymers and polymers prepared therefrom.Type: GrantFiled: October 30, 1990Date of Patent: November 26, 1991Assignee: The Dow Chemical CompanyInventors: Robert F. Harris, Michael D. Joseph
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Patent number: 5055582Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.Type: GrantFiled: December 13, 1988Date of Patent: October 8, 1991Assignee: National Research Development CorporationInventors: Robert B. Garland, Masateru Miyano
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Patent number: 5053430Abstract: Novel compounds having the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds are useful in the treatment of schizophrenia.Type: GrantFiled: September 22, 1989Date of Patent: October 1, 1991Assignee: Boehringer Ingelheim KGInventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
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Patent number: 5030754Abstract: Hydroxy-terminated substituted diurea derivatives of hydroxy-terminated polyurea derivatives of secondary monoalkylamines and organic diisocyanates and hydroxy-terminated polyurea derivatives of secondary monalkylamines and prepolymers of organic diisocyanates with polyoxyalkylene polyols, such as hydroxy-terminated polyurea derivatives of secondary monoalkylamines and organic diisocyanates having the formula: ##STR1## wherein: R represents an aliphatic or an aromatic group containing from 6 to about 20 carbon atoms,R' represents H or an alkyl group containing 1 to 6 carbon atoms, andn is a positive integer having a value of 1 to 4.Type: GrantFiled: November 19, 1990Date of Patent: July 9, 1991Assignee: Texaco Chemical CompanyInventors: George P. Speranza, Jiang-Jen Lin
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Patent number: 5015644Abstract: Certain substituted urea, thiourea, carbamate, and thiocarbamate compounds are potent inhibitors of the enzyme acyl-CoA: cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol, and for lowering blood plasma cholesterol.Type: GrantFiled: June 1, 1989Date of Patent: May 14, 1991Assignee: Warner-Lambert CompanyInventors: Bruce D. Roth, Bharat K. Trivedi
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Patent number: 5006660Abstract: The present invention relates to a process for producing an alkoxybenzene compound or an aryloxybenzene compound by reacting a halogenobenzene compound with an alcohol or a phenol compound in the presence of copper or a copper compound, an amine, and a base. According to the disclosure, an alkoxybenzene compound and an aryloxybenzene compound can be produced under moderate conditions in good yield with high selectivity.Type: GrantFiled: June 28, 1989Date of Patent: April 9, 1991Assignee: Fuji Photo Film Co., Ltd.Inventor: Katsuyoshi Yamakawa
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Patent number: 5006523Abstract: Novel compounds of the formula ##STR1## and tautomers thereof are disclosed. These compounds possess potassium channel blocking activity and, as such, are useful as antiarrhythmic agents.Type: GrantFiled: October 26, 1989Date of Patent: April 9, 1991Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 4997980Abstract: Disclosed are novel compounds of the formula: ##STR1## wherein: X=--NR.sub.5 R.sub.6, or --OR.sub.7 ;R.sub.1 and R.sub.2 are independently hydrogen, substituted or unsubstituted alkyl, haloalkyl, hydroxyalkyl alkoxyalkyl, alkylaminoalkyl or arylalkyl having up to 18 carbons, cycloalkyl; phenyl or naphthyl; alkylphenyl, cyanophenyl, halophenyl or alkoxyphenyl substituents;R.sub.3 is hydrogen, benzyl, alkoxybenzyl, halobenzyl or alkylbenzyl, provided that if neither R.sub.1 nor R.sub.2 is hydrogen, then R.sub.3 is hydrogen;R.sub.4 is a divalent aromatic group which is substituted or unsubstituted;R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen, alkyl, hydroxyalkyl, haloalkyl, alkoxyalkyl, alkylaminoalkyl, acylaminoalkyl, aminoalkyl or phenylalkyl having up to 12 carbons; a cycloalkyl substitutent; phenyl or naphthyl; an alkylphenyl, cyanophenyl, halophenyl or alkoxyphenyl substituent;Furthermore, either R.sub.1 and R.sub.3 or R.sub.1 and R.sub.Type: GrantFiled: April 17, 1989Date of Patent: March 5, 1991Assignee: Anitec Image CorporationInventors: Bruce M. Resnick, Allan J. Wexler
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Patent number: 4996359Abstract: Aromatic bis (dialkyl) ureas such as the bis (dimethyl) urea of 2,4-toluenediamine are prepared by reacting an aromatic diamine with isocyanic acid (HNCO) to convert the amino groups of the diamine to urea groups (--NHCONH.sub.2) to give an aromatic bis urea which is then reacted with a dialkyl amine having from 1 to 8 carbon atoms to produce the desired aromatic bis (dialkyl) urea.Type: GrantFiled: March 14, 1988Date of Patent: February 26, 1991Assignee: Arco Chemical Technology, Inc.Inventors: Haven S. Kesling, Jr., Edward T. Shawl, John G. Zajacek
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Patent number: 4994611Abstract: The present invention is directed to a process for the preparation of N,N'-bis-(3-aminophenyl)-ureas corresponding to formula (I) ##STR1## wherein R represents a linear or branched C.sub.1 -C.sub.6 alkyl group which is in the 2-, 4- and/or 6-position,characterized in that the corresponding phenylene diamines are reacted with urea in a molar ratio of greater than 2:1 in chlorobenzene as solvent.Type: GrantFiled: November 14, 1989Date of Patent: February 19, 1991Assignee: Bayer AktiengesellschaftInventors: Andreas Ruckes, Gerhard Grogler, Richard Kopp
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Patent number: 4983630Abstract: There are provided new 2,2-difluorocyclopropylethane derivatives of general formula I ##STR1## in which A, B and R.sup.1-5 have the meanings given in the description and processes for their preparation. The compounds of the invention can be used as pesticides, especially against insects and mites.Type: GrantFiled: November 28, 1988Date of Patent: January 8, 1991Assignee: Schering AktiengesellschaftInventors: Peter Wegner, Hartmut Joppien, Gunter Homberger, Arnim Kohn
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Patent number: 4943591Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein X represents a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain andY represents a bond, or a C.sub.1-4 alkylene, C.sub.2-4 alkenylene or C.sub.2-4 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is not more than 8;Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms or the groups C.sub.1-3 alkyl, nitro, --(CH.sub.2).sub.q R [where R is hydroxy, C.sub.1-3 alkoxy, --NR.sup.3 R.sup.4 (where R.sup.3 and R.sup.4 each represent a hydrogen atom, or a C.sub.1-4 alkyl group, or --NR.sup.3 R.sup.4 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from --O-- or --S-- or a group --NH-- or --N(CH.sub.3)--), --NR.sup.5 COR.sup.6 (where R.sup.5 represents a hydrogen atom or a C.sub.1-4 alkyl group, and R.sup.6 represents a hydrogen atom or a C.sub.Type: GrantFiled: October 14, 1986Date of Patent: July 24, 1990Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, Ian B. Campbell
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Patent number: 4908386Abstract: The present invention provides compounds of general formula (I) ##STR1## wherein Ar represents an unsubstituted or substituted phenyl gorup;R.sup.1 and R.sup.2 each represents a hydrogen atom or a C.sub.1-3 alkyl group;X represents a bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene chain;Y represents a bond or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain;Q represents a substituted phenyl or pyridyl ring;and physiologically acceptable salts and solvates thereof useful as stimulants of .sub.2 -adrenoreceptors and particularly in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: December 20, 1988Date of Patent: March 13, 1990Assignee: Glaxo Group LimitedInventors: Harry Finch, Lawrence H. C. Lunts, Alan Naylor, Ian F. Skidmore, Ian B. Campbell, David Middlemiss, Charles Willbe
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Patent number: 4906767Abstract: There is disclosed a family of new vinyl monomers capable of forming polymers by free radical polymerization. The vinyl monomer is of the formula ##STR1## wherein R.sub.1 and R.sub.2 are substituted or unsubstituted hydrocarbons, X is O, NH or NR.sub.3, and R.sub.3 is substituted or unsubstituted hydrocarbon.The intermediates in the synthesis of these monomers are new beta-chloroalanine ureas. The polymers are useful in film and fiber formation and display good toughness. These new vinyl monomers also form a cyclic monomer.Type: GrantFiled: June 30, 1987Date of Patent: March 6, 1990Assignee: The University of Southern MississippiInventors: Lon J. Mathias, David W. Kurz
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Patent number: 4888043Abstract: The invention concerns compounds of the formula I ##STR1## wherein: Z is selected from hydrogen, alkyl, alkanoyl, sulfamoyl, carboxy and trifluoroacetamido;Y is selected from various carboxy or thiocarboxy groups, haloalkanoyl, alkylsulfonyl and haloalkylsulfonyl;R.sup.1 is selected from hydrogen, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl and alkynyl;R.sup.3 is selected from alkyl; andR.sup.4 is selected from hydrogen, alkyl, and alkoxycarbonyl.The compounds of the invention show herbicidal properties and plant growth regulating properties and in further embodiments and the invention provides processes for the preparation of compounds of formula I, intermediates useful in the preparation of the compounds of formula I, compositions containing as active ingredient a compound of formula I, and herbicidal and plant growth regulating processes utilizing compounds of formula I.Type: GrantFiled: June 20, 1986Date of Patent: December 19, 1989Assignee: ICI Australia LimitedInventors: Keith G. Watson, Craig G. Lovel
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Patent number: 4886909Abstract: A novel aromatic amine terminated trifunctional polyoxyalkylene urea which is useful as an epoxy curing agent is disclosed and is prepared in a two step process comprising reacting a triamine or a triol with a diisocyanate to form an intermediate product and subsequently reacting the intermediate with a diprimary amine in the presence of an alcohol solvent.Type: GrantFiled: July 22, 1988Date of Patent: December 12, 1989Assignee: Texaco Chemical CompanyInventors: Jiang-Jen Lin, George P. Speranza
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Patent number: 4872902Abstract: The invention relates to the novel cyclohexanediones of formula I ##STR1## in which R is hydrogen or C.sub.1 -C.sub.6 -alkyl,A is R.sub.2, OR.sub.3 or NR.sub.3 R.sub.4,R.sub.2 is C.sub.1 -C.sub.6 -alkyl that is unsubstituted or is mono-substituted by C.sub.1 -C.sub.4 -alkoxy or mono- or poly-substituted by halogen, or is C.sub.3 -C.sub.6 -cycloalkyl,R.sub.3 is C.sub.1 -C.sub.6 -alkyl or C.sub.3 -C.sub.6 -cycloalkyl, or is phenyl or benzyl each of which is unsubstituted or is mono-, di- or tri-substituted by R.sub.5,R.sub.4 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.3 -C.sub.6 -cycloalkyl,R.sub.3 and R.sub.4 are, in addition, together with the nitrogen atom to which they are bonded, a pyrrolidine, morpholine or piperidine radical,B is one of the radicals ##STR2## m is 0, 1, 2 or 3, R.sub.5 is halogen, nitro, cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkylsulphinyl or C.sub.1 -C.sub.Type: GrantFiled: February 8, 1988Date of Patent: October 10, 1989Assignee: Ciba-Geigy CorporationInventor: Hans-Georg Brunner
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Patent number: 4873338Abstract: Compounds corresponding to Formula I ##STR1## wherein R.sup.1 denotes an acyl group andX denotes hydrogen, halogen, alkoxy, aroxy, SO.sub.3 H or a heterocyclic group attached through --O-- or --N<are prepared form a compound corresponding to Formula II ##STR2## wherein X has the meaning already indicated and Q denotes the group required for completing a dicarbonimide ringby reduction of the said compound to the amino compound and acylation into a compound corresponding to Formula III ##STR3## wherein X, Q and R.sup.1 have the meanings indicatedfollowed by conversion of the compound corresponding to Formula III into a compound corresponding to Formula I by hydrazinolytic or hydrolytic decomposition of the dicarbonimide ring.Type: GrantFiled: November 23, 1987Date of Patent: October 10, 1989Assignee: Agfa-Gevaert AktiengesellschaftInventors: Heinz Wiesen, Erich Wolff
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Patent number: 4868210Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.Type: GrantFiled: March 30, 1988Date of Patent: September 19, 1989Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 4820871Abstract: N,N-Diaryl-ureas of the formulaR.sup.1 --NR.sup.2 --CO--NH--R.sup.3whereinR.sup.1 and R.sup.2 denote aryl andR.sup.3 denotes alkyl, aralkyl or aryl, can be prepared by a process in which a diarylamine of the formulaR.sup.1 --NH--R.sup.2is reacted with an isocyanate of the formulaR.sup.3 --NCOwherein R.sup.1, R.sup.2 and R.sup.34 have the above meaning, in the presence of acid compounds and in the presence or absence of an inert solvent and/or diluent at elevated temperature.Type: GrantFiled: October 7, 1987Date of Patent: April 11, 1989Assignee: Bayer AktiengesellschaftInventors: Wolfram Kissener, Joachim Franke, Helmut Fiege, Karlfried Wedemeyer
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Patent number: 4816600Abstract: Modified organic isocyanate composition containing urea and/or biuret groups and/or salts of these groups, obtained from the reaction of a blocked polyamine composition and an unblocked isocyanate composition.Type: GrantFiled: September 14, 1987Date of Patent: March 28, 1989Assignee: ICI Americas Inc.Inventor: Herbert R. Gillis, Jr.
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Patent number: 4803223Abstract: A substituted aminophenylurea derivative represented by the general formula ##STR1## wherein X.sup.1 and X.sup.2 are identical or different and each represents a halogen atom, andR represents a substituted or unsubstituted saturated or unsaturated aliphatic hydrocarbon group,and an acid addition salt thereof, and a process for preparation thereof, the compound of formula (I) being useful as antitumor agent.Type: GrantFiled: February 20, 1986Date of Patent: February 7, 1989Assignee: Tokuyama Soda Kabushiki KaishaInventor: Shozo Kato
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Patent number: 4788287Abstract: A high performance water and oil repellant composed of a compound comprising at least two terminal segments and an intermediate segment connecting the terminal segments and having a molecular weight of from 800 to 20,000, each terminal segment containing at least one polyfluoroalkyl group connected by a --CONH-- linking group, said intermediate segment being a urethane oligomer containing at least two --CONH-- linking groups in one molecule, and said terminal segments and intermediate segment being connected by a --CONH-- linking group.Type: GrantFiled: September 3, 1986Date of Patent: November 29, 1988Assignee: Asahi Glass Company Ltd.Inventors: Masashi Matsuo, Masayuki Tamura, Katsuji Ito
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Patent number: 4752615Abstract: A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, particularly their strains resistant to benzimidazole, thiophanate and/or cyclic imide fungicides.Type: GrantFiled: November 13, 1986Date of Patent: June 21, 1988Assignee: Sumitomo Chemical Company, LimitedInventors: Junya Takahashi, Toshiro Kato, Hiroshi Noguchi, Yukio Oguri, Shigeo Yamamoto, Katsuzo Kamoshita
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Patent number: 4730008Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein Ar, R.sup.1, R.sup.2, X, Y and Q are defined in the specification and physiologically acceptable salts and solvates thereof.The compounds have a selective stimulant action at .beta..sub.2 -adrenoreceptors and may be used, inter alia, in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: January 10, 1986Date of Patent: March 8, 1988Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Harry Finch, Alan Naylor, Lawrence H. C. Lunts, Ian B. Campbell
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Patent number: 4704401Abstract: This invention relates to a method of lowering blood pressure in humans and mammals using 2,6-disubstituted phenyl amidinoureas in which the phenyl ring is additionally substituted by a hydroxy, alkoxy, aralkoxy, alkenyloxy, alkynyloxy, haloacyloxy, or acyloxy group and to novel 2,6-disubstituted phenyl amidinoureas which possess pharmaceutical properties, including blood pressure lowering activity.Type: GrantFiled: December 6, 1984Date of Patent: November 3, 1987Assignee: Rorer Pharmaceutical CorporationInventors: William L. Studt, Richard L. Riley, George H. Douglas
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Patent number: 4692553Abstract: Cyclohexenone derivatives of the formula ##STR1## where R.sup.1 is hydrogen, methoxycarbonyl, ethoxycarbonyl, methyl or cyano, R.sup.2 is alkyl, R.sup.3 is alkyl, alkenyl, haloalkenyl, or propargyl, R.sup.4 is hydrogen or alkyl, R.sup.5 is hydrogen, alkyl, acyl, formyl, cycloalkylcarbonyl, methoxyalkylcarbonyl, unsubstituted or substituted benzoyl, alkoxycarbonyl, benzyloxycarbonyl, phenoxycarbonyl, alkylthiocarbonyl, N,N-dialkylcarbamyl, N-alkylcarbamyl, N-cycloalkylcarbamyl, N-alkoxy-N-alkylcarbamyl, unsubstituted or substituted N-phenylcarbamyl, alkylsulfonyl, alkenylsulfonyl, haloalkylsulfonyl, N-alkylsulfamyl, N,N-dialkylsulfamyl, N-acyl-N-alkylsulfamyl, N-alkyl-N-methoxycarbonylsulfamyl, dialkoxyphosphoryl, dialkoxythiophosphoryl, 2-haloalkanoyl, acyloxyacetyl or alkoxyoxalyl, and R.sup.6 is alkyl, halogen, hydroxyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkylsulfinyl, alkylsulfonyl, nitro or amino, and salts of these compounds, and the use of these compounds for controlling unwanted plant growth.Type: GrantFiled: July 26, 1985Date of Patent: September 8, 1987Assignee: BASF AktiengesellschaftInventors: Michael Keil, Ulrich Schirmer, Dieter Jahn, Rainer Becker, Bruno Wuerzer, Norbert Meyer
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Patent number: 4665235Abstract: The invention relates to new benzoylurea compounds of the general formula ##STR1## wherein R.sub.1 is a halogen atom,R.sub.2 is a hydrogen atom or a halogen atom,R.sub.3 is a hydrogen atom or represents 1 or 2 substituents which are selected from the group consisting of chlorine, methyl and trifluormethyl,R.sub.4 is a hydrogen atom or represents 1-3 substituents which are selected from the group consisting of halogen, and alkyl, alkoxy, haloalkyl and haloalkoxy, having 1-4 carbon atoms,X is N or CH,n is 0 or 1, andR.sub.5 is a hydrogen atom, an alkyl group having 1-6 carbon atoms, an alkenyl group having 2-6 carbon atoms, or a cycloalkyl group having 3-6 carbon atoms, with the proviso, that, if n is 0 and R.sub.5 is a hydrogen atom, R.sub.3 is a hydrogen atom.The compounds have an insecticidal and acaricidal activity. After having been processed to compositions, the compounds may be used for the control of insects and/or mites in a dosage of 1 to 5000 grams of active substance per hectare.Type: GrantFiled: January 19, 1984Date of Patent: May 12, 1987Assignee: Duphar International Research B.V.Inventors: Marius S. Brouwer, Arnoldus C. Grosscurt
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Patent number: 4661515Abstract: Novel compounds possessing both angiotensin enzyme inhibitory activity and diuretic activity are disclosed. The compounds are represented by the general formula ##STR1## in which X is ##STR2## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, and cycloalkyl, and may be the same or different; n is an integer from 0 to 4 inclusive; M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cyloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl, or M and R.sub.6 taken together with the nitrogen to which M is bonded and the carbon to which R.sub.Type: GrantFiled: January 17, 1986Date of Patent: April 28, 1987Assignee: USV Pharmaceutical CorporationInventors: Edward S. Neiss, John T. Suh, John J. Piwinski
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Patent number: 4603125Abstract: Compounds represented by the general formula (I): ##STR1## in which R.sub.1 represents ##STR2## A and B each represent H or a lower alkane optionally substituted with amino and/or hydroxyl functions, except that A and B are not both H; R.sub.3 represents H, OCH.sub.3, CH.sub.3, halogen, NH.sub.2, NO.sub.2, NHCH.sub.3, N.sub.3 (CH.sub.3).sub.2, N.sub.3, NHCOCH.sub.3, NHCOOCH.sub.3, N(CH.sub.3)COOCH.sub.3, CONH.sub.2 or CONHCH.sub.3 ; R.sub.4 represents H, alkyl, O-alkyl, CONH.sub.2, CONHCH.sub.3 or CONHCH.sub.2 CONHCH.sub.3, except that R.sub.3 and R.sub.4 taken together can represent --C.dbd.CH--CH.dbd.N--; R.sub.5 represents H, alkyl, O-alkyl, CONH.sub.2, CONHCH.sub.3 or CONH.sub.2 CH.sub.2 CONHCH.sub.3 ; R.sub.6 represents lower alkyl; R.sub.7 represents CH.sub.3 or C.sub.6 H.sub.5 (phenyl); R.sub.8 represents lower alkyl or C.sub.6 H.sub.5 (phenyl); R.sub.9 represents H, NHCOCH.sub.3, NH.sub.2 or N.dbd.CHN(CH.sub.3).sub.2 ; and R.sub.10 represents H or NH.sub.Type: GrantFiled: November 14, 1983Date of Patent: July 29, 1986Assignee: Development Finance Corporation of New ZealandInventors: Graham J. Atwell, Bruce C. Baguley, William A. Denny, Gordon W. Rewcastle
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Patent number: 4564640Abstract: A method of inducing blood pressure reduction in humans and mammals by administering 2,6-disubstituted phenyl N-alkyl amidinoureas in which the phenyl ring is additionally substituted by a hydroxy, alkoxy, aralkoxy, alkenyloxy, alkynyloxy, acyloxy or halo acyloxy group and a novel class of amidinourea compounds having pharmaceutical uses, including blood pressure lowering activity.Type: GrantFiled: February 2, 1984Date of Patent: January 14, 1986Assignee: William H. Rorer, Inc.Inventors: William L. Studt, Richard L. Riley, George H. Douglas
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Patent number: 4557756Abstract: A compound having the structural formula ##STR1## wherein R is hydrogen or C.sub.1 -C.sub.3 alkyl, preferably methyl;R.sup.1 is C.sub.1 -C.sub.3 alkyl, preferably ethyl; andR.sup.2 is C.sub.1 -C.sub.3 alkyl, preferably ethyl; C.sub.1 -C.sub.2 alkylamino, preferably methylamino; C.sub.2 -C.sub.4 dialkylamino, preferably dimethylamino; or C.sub.2 -C.sub.4 alkylalkoxyamino, preferably methylmethoxyamino; and its use as a post-emergent herbicide.Type: GrantFiled: December 30, 1983Date of Patent: December 10, 1985Assignee: Stauffer Chemical CompanyInventors: Eugene G. Teach, Jeffery T. Springer
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Patent number: 4552970Abstract: Compounds of the formula I ##STR1## in which X denotes hydrogen, fluorine, chlorine or bromine, Y and Z denote hydrogen, lower alkyl or lower alkoxy, M denotes sodium, potassium or one equivalent of calcium and L denotes a dipolar aprotic solvent, are obtained from compounds of the formula II ##STR2## in which X, Y and Z have the abovementioned meanings, and a metal cyanamide of the formula IIIM.sub.2 N--CNin which M has the abovementioned meaning, in a dipolar aprotic solvent, which after the reaction is substantially removed, whereupon a lower molecular weight aliphatic alcohol is added to the residue and the product precipitated is isolated. Nitrophenylureas of the formula IV ##STR3## in which X, Y and Z have the abovementioned meanings, are obtained from the compounds of the formula I by acid hydrolysis.Type: GrantFiled: February 1, 1984Date of Patent: November 12, 1985Assignee: Hoechst AktiengesellschaftInventors: Otto Arndt, Theodor Papenfuhs, Wolfgang Tronich
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Patent number: 4536598Abstract: A new color-forming 4-(4'-secondary or tertiary-amino)anilino-1-carboxamidonaphthalene dye precursor in a photographic material and process enables formation of a dye image by means of cross-oxidation without the need for a coupling reaction. The color-forming 4-(4'-secondary or tertiary-amino)anilino-1-carboxamidonaphthalene dye precursor is useful in a photographic silver halide material for producing (i) a dye image, or (ii) a dye image and silver image. The exposed photographic material is processed to produce (a) a positive dye image, (b) a negative dye and negative silver image, (c) a negative dye image or (d) a positive dye image and a positive silver image. New naphthoquinoneimide dyes are also described.Type: GrantFiled: March 10, 1983Date of Patent: August 20, 1985Assignee: Eastman Kodak CompanyInventors: James E. Klijanowicz, Csaba A. Kovacs
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Patent number: 4529820Abstract: This invention relates to novel cyanourea compounds of the formula: ##STR1## wherein R is the organic moiety of a polyisocyanate remaining after reaction of the isocyanate groups to form cyanourea groups and n is at least 2. The compound can be polymerized at room temperature to form a polymer having the recurring structural formula: ##STR2## i.e., N,N'-biscarbamyl-N-cyanoguanidine units connected together through the R group of the carbamyl moiety and m is greater than 2, or can be cured to a thermoset material on heating above 90.degree. C.Type: GrantFiled: July 9, 1984Date of Patent: July 16, 1985Assignee: W. R. Grace & Co.Inventor: Shiow-Ching Lin
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Patent number: 4526997Abstract: The present invention is directed to novel anticoccidial compositions and methods of employing the same to control coccidiosis in poultry. These compositions comprise a polyether antibiotic and a second component which is a selected carbanilide.Type: GrantFiled: May 18, 1984Date of Patent: July 2, 1985Inventors: George O. P. O'Doherty, Albert J. Clinton
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Patent number: 4519834Abstract: The ethynyl-phenylureas of the formula I ##STR1## wherein X is hydrogen, halogen, lower alkyl, lower alkoxy, haloalkyl or nitro, Y is oxygen or sulfur, R.sub.1 is hydrogen, alkyl, alkoxy, alkenyl, phenyl or benzyl, R.sub.2 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl or benzyl, R.sub.1 and R.sub.2 together with the nitrogen atom to which they are bound are also a pyrrolidine, piperidine, morpholino or piperazine ring, R.sub.3 is hydrogen or lower alkyl, and R.sub.4 is hydrogen, alkyl, phenyl, pyridyl, alkenyl, cycloalkyl or cycloalkenyl, are novel substances. They are characterized by strong herbicidal activity.Type: GrantFiled: July 11, 1983Date of Patent: May 28, 1985Assignee: Ciba-Geigy CorporationInventor: Henry Szczepanski
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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: 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: 4488993Abstract: Novel phenylamidinourea compounds and processes for their preparation are described. These compounds have an effective degree of anti-hypertensive properties and exert activities on the cardiovascular system. A method for the treatment of hypertensive disorders is also described.Type: GrantFiled: October 25, 1982Date of Patent: December 18, 1984Assignee: William H. Rorer, Inc.Inventors: George H. Douglas, Julius Diamond
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Patent number: 4487779Abstract: This invention relates to a method of lowering blood pressure in humans and mammals using 2,6-disubstituted phenyl amidinoureas in which the phenyl ring is additionally substituted by a hydroxy, alkoxy, aralkoxy, alkenyloxy, alkynyloxy, haloacyloxy, or acyloxy group and to novel 2,6-disubstituted phenyl amidinoureas which possess pharmaceutical properties, including blood pressure lowering activity.Type: GrantFiled: July 6, 1981Date of Patent: December 11, 1984Assignee: William H. Rorer, Inc.Inventors: William L. Studt, Richard L. Riley, George H. Douglas
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Patent number: 4478849Abstract: The compounds of the formula (II): ##STR1## and their pharmaceutically acceptable salts wherein R.sub.1 is a hydrogen, fluorine or chlorine atom or a hydroxyl, hydroxymethyl, methyl, methoxyl, amino, formamido, acetamido, methylsulphonylamido, nitro, benzyloxy, methylsulphonylmethyl, ureido, trifluoromethyl or p-methoxybenzylamino group; R.sub.2 is a hydrogen, fluorine or chlorine atom or a hydroxyl group; R.sub.3 is a hydrogen or chlorine atom or a hydroxyl group; R.sub.4 is a carboxylic acid group or a salt, ester or amide thereof; R.sub.5 is a hydrogen, chlorine or fluorine atom or a methyl, methoxyl or hydroxyl group or a carboxylic acid group or a salt, ester or amide thereof; R.sub.6 is a hydrogen atom or a methyl, or propyl group; X is an oxygen atom or a bond; and Y is an alkylene group of up to 6 carbon atoms or a bond have been found to possess anti-obesity and/or antihyperglycaemic activity.Type: GrantFiled: March 10, 1983Date of Patent: October 23, 1984Assignee: Beecham Group LimitedInventors: Anthony T. Ainsworth, David G. Smith
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Patent number: 4478852Abstract: The present invention relates to new urea derivatives having pesticidal activity, particularly fungicidal activity. The urea derivatives, according to the invention, have the general formula ##STR1## wherein X, Y and Z represent hydrogen or halogen atoms and at least one of the substituents X, Y or Z is a halogen atom.Type: GrantFiled: May 12, 1982Date of Patent: October 23, 1984Assignee: Celamerck GmbH & Co. KG.Inventors: Heinz-Manfred Becher, Christo A. Drandarevski, Sigmund Lust
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Patent number: 4474806Abstract: Sulfonyl or carbonyl derivatives of inositols are found to be effective phospholipase C inhibitors and thereby potent anti-inflammatory and analgesic agents. These inositol derivatives are prepared by condensation of a protected inositol with a substituted sulfonic or carboxylic acid derivative followed by removal of protecting groups.Type: GrantFiled: May 10, 1982Date of Patent: October 2, 1984Assignee: Merck & Co., Inc.Inventors: Thomas R. Beattie, Shu S. Yang
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Patent number: RE31731Abstract: Compounds of the formula ##STR1## wherein X is a hydrogen atom, a halogen atom, a trihalomethyl group, an alkyl group, or a cyano group,Y is a hydrogen atom, or a trihalomethyl group, andZ is an alkoxy group, an alkoxyalkoxy group, a hydroxyalkoxy group, an alkyl group, a halogen atom, an alkylamino group, a dialkylamino group, an alkylthio group, a carboxy group, a carbalkoxy group, a carboxyalkoxy group, a carbalkoxyalkoxy group, a carboxyalkyl group, a carbalkoxyalkyl group, a dialkylureido group, an alkanoylamino group, or carbalkoxyamino group,and compositions containing these compounds exhibit herbicidal activity.Type: GrantFiled: September 1, 1978Date of Patent: November 13, 1984Inventors: Horst O. Bayer, Colin Swithenbank, Roy Y. Yih