Aralkyl Bonded Directly To Urea Nitrogen Patents (Class 564/56)
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Patent number: 5482947Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: November 15, 1993Date of Patent: January 9, 1996Inventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Ko-Chung Lin, Michael L. Vazquez, Richard A. Mueller, Kathryn L. Reed, Robert M. Heintz, Michael Clare, John N. Freskos, Eric T. Sun
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Patent number: 5475013Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 20, 1992Date of Patent: December 12, 1995Assignee: Monsanto CompanyInventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
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Patent number: 5449690Abstract: A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are as defined in the specification, and medicinal products containing the same which are useful in treating or in preventing a disorder of the melatoninergic system.Type: GrantFiled: December 20, 1994Date of Patent: September 12, 1995Assignee: Adir et CompagnieInventors: Daniel Lesieur, Said Yous, Patrick DePreux, Gerard Adam, Pierre Renard, Bruno Pfeiffer, Beatrice Guardiola-Lemaitre
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Patent number: 5449689Abstract: A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are as defined in the specification, andmedicinal products containing the same which are useful in treating or in preventing a disorder of the melatoninergic system.Type: GrantFiled: December 20, 1994Date of Patent: September 12, 1995Assignee: Adir et CompagnieInventors: Daniel Lesieur, Said Yous, Patrick Depreux, Gerard Adam, Pierre Renard, Bruno Pfeiffer, Beatrice Guardiola-Lemaitre
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Patent number: 5441984Abstract: The present invention provides novel urea, thiourea and guanidine derivatives, pharmaceutical formulations thereof and a method of using same to prevent diabetic complications.Type: GrantFiled: November 14, 1994Date of Patent: August 15, 1995Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., Jill A. Panetta, John K. Shadle
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Patent number: 5434265Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating HIV infection.Type: GrantFiled: December 22, 1992Date of Patent: July 18, 1995Assignee: Eli Lilly and CompanyInventors: James E. Fritz, Marlys Hammond, Stephen W. Kaldor
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Patent number: 5401426Abstract: Lactobionic acid amide compositions synthesized from lactobionic acid and a mixture of primary fatty amines, which contains at least 30 percent by weight of fatty amines having a chain length of 14 to 18 carbon atoms, and their use as softening, detergent, emulsifying, foam stabilizing and/or thickening components of detergents, rinsing or cleaning agents, softeners or cosmetic formulations.Type: GrantFiled: October 15, 1993Date of Patent: March 28, 1995Assignee: Solvay Deutschland GmbHInventors: Klaus-Guenter Gerling, Sabine Joisten, Kornelia Wendler, Claudia Schreer
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Patent number: 5389683Abstract: A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are as defined in the specification, andmedicinal products containing the same which are in treating or in preventing a disorder of the melatoninergic system.Type: GrantFiled: August 14, 1992Date of Patent: February 14, 1995Assignee: Adir et CompagnieInventors: Daniel Lesieur, Said Yous, Patrick Depreux, Gerard Adam, Pierre Renard, Bruno Pfeiffer, Beatrice Guardiola-Lemaitre
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Patent number: 5389682Abstract: The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.Type: GrantFiled: September 13, 1993Date of Patent: February 14, 1995Assignee: Warner-Lambert CompanyInventors: Bradley D. Tait, Michael W. Wilson
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Patent number: 5385944Abstract: A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are defined in the specification, andmedicinal products containing the same which are useful in treating or in preventing a disorder of the melatoninergic system.Type: GrantFiled: April 27, 1993Date of Patent: January 31, 1995Assignee: Adir et CompagnieInventors: Daniel Lesieur, Said Yous, Patrick Depreux, Gerard Adam, Pierre Renard, Bruno Pfeiffer, Beatrice Guardiola-Lemaitre
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Patent number: 5384425Abstract: Diurea derivatives are provided which can be represented by the following general formula and salts thereof: ##STR1## wherein, R.sup.1 and R.sup.2 are the same or different, and each represents C.sup.1 -10 alkyl group, a C.sup.3 -18 cycloalkyl group, or a lower alkyl group substituted by cycloalkyl radical(s);R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different, and each represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, hydrocarbyl aralkyl group, a pyridyl group, or an unsubstituted or substituted phenyl group, the substituents of the phenyl group being selected from a group consisting of lower alkyl radical, halogen atom-substituted lower alkyl radical, halogen atom, nitro radical, amino radical, mono- or di-lower alkylamino radical, lower acylamino radical, hydroxyl radical, lower alkoxy radical and lower acyloxy radical;X represents an oxygen atom or a sulfur atom, and n.sup.1 and n.sup.2 represent an integer of 1 to 6; and wherein at least one of R.sup.3 -R.sup.Type: GrantFiled: October 7, 1993Date of Patent: January 24, 1995Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
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Patent number: 5364850Abstract: The present invention provides substituted tyrosyl diamide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable salts thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: September 24, 1993Date of Patent: November 15, 1994Assignee: G. D. Searle & Co.Inventors: Donald W. Hansen, Jr., Nizal S. Chandrakumar, Karen B. Peterson, Sofya Tsymbalov, Robert K. Husa
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Patent number: 5294582Abstract: As a curing catalyst of epoxy resins, superacid salts of an N,N'-di- or N,N',N'-trisubstitued urea, the urea component of which is produced by reacting an organic isocyanate and a primary or secondary amine, at least one of which is monofunctional, are soluble in conventional organic solvents compatible with epoxy resins and catalyze the cationic polymerization reaction of epoxy resins at room temperature.Type: GrantFiled: June 14, 1993Date of Patent: March 15, 1994Assignee: Nippon Paint Co., Ltd.Inventors: Tadafumi Miyazono, Koji Tabuchi
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Patent number: 5288758Abstract: New urea derivatives corresponding to the general formula 1 ##STR1## in which: R.sup.1 represents a C.sub.1 -C.sub.4 alkyl group;R.sup.2 represents:a C.sub.5 -C.sub.7 cycloalkyl groupa cycloalkylmethyl group in which the cycloalkyl radical contains from 5 to 7 carbon atomsa benzyl groupa benzyl group in which the aromatic ring bears a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a halogen atom or a nitro group;A represents an oxygen atom or a methylene radical;n represents 1 or 2;X represents an oxygen or sulfur atom;B represents a direct bond, a methylene radical or a carbonyl radical;as well as the therapeutically acceptable salts of these molecules.The invention also relates to the application of the compounds of general formula 1 in therapy, and to the preparation processes.Type: GrantFiled: July 22, 1992Date of Patent: February 22, 1994Assignee: Pierre Fabre MedicamentInventors: Jean-Louis Vidaluc, Dennis Bigg
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Patent number: 5283361Abstract: This invention relates to N-hydroxy-N-[3-[2-(4'-halophenylthio)phenyl]prop-2-enyl]ureas, formulations containing those compounds and methods of using such compounds as 5-lipoxygenase inhibiting agents.Type: GrantFiled: April 8, 1992Date of Patent: February 1, 1994Assignee: Eli Lilly and CompanyInventors: Gary A. Hite, Edward D. Mihelich, David W. Snyder, Tulio Suarez
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Patent number: 5276139Abstract: N-substituted azetidinones are a class of inhibitors of human leukocytes elastase which are known to be useful in the treatment of a wide variety of antiinflammatory and antidegenerative diseases. In inhibiting elastase, the therapeutic agents are shown to form a characteristic stable complex with the enzyme. In the radioimmune assay disclosed herein, the inhibitor-enzyme complex is advantageously hydrolyzed and specific product(s) of the hydrolysis are measured. The assays are useful in a clinical setting, for determining appropriate dosage and assessing the effectiveness of treatment.Type: GrantFiled: August 26, 1991Date of Patent: January 4, 1994Assignee: Merck & Co., Inc.Inventors: Paul E. Finke, William K. Hagmann, Richard A. Mumford, Shrenik K. Shah
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Patent number: 5274080Abstract: Inhibitors of human leukocytes elastase are known to be useful in the treatment of a wide variety of antiinflammatory and antidegenerative diseases. In inhibiting elastase, the therapeutic agents are shown to form a characteristic stable complex with the enzyme. In the radioimmunoassay disclosed herein, the inhibitor-enzyme complex is advantageously hydrolyzed and specific product(s) of the hydrolysis are measured utilizing polyclonal antibodies capable of binding to one or more haptens of formula II ##STR1## wherein M is allyl or n-propyl,Z.sub.1 is(a) 5-benzofuranyl or(b) substituted phenyl wherein the substituent is methyl or ethyloxy.The assays utilizing these antibodies are useful in a clinical setting, for determining appropriate dosage and assessing the effectiveness of treatment.Type: GrantFiled: August 26, 1991Date of Patent: December 28, 1993Assignee: Merck & Co., Inc.Inventors: Malcolm MacCoss, Richard A. Mumford
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Patent number: 5272175Abstract: The present invention provides substituted tyrosyl diamide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable salts thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: May 20, 1992Date of Patent: December 21, 1993Assignee: G. D. Searle & Co.Inventors: Donald W. Hansen, Jr., Nizal S. Chandrakumar, Karen B. Peterson, Sofya Tsymbalov, Robert K. Husa
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Patent number: 5248821Abstract: High molecular weight active polyoxyalkylene reaction product formed in two steps and containing urea or urethane and urea linkages are disclosed which contain as the principle reaction component, a diamine having the formula: ##STR1## or a diol having the formula: ##STR2## wherein R' independently represents hydrogen or methyl and x is a number having an average value of at least 1 to about 70 and a diisocyanate of the formula: ##STR3## an active amine selected from the group consisting of amine terminated triethylene glycol, amine terminated tetraethylene glycol, isophorone diamine, dipropylene triamine, or diethylene triamine.Type: GrantFiled: March 9, 1992Date of Patent: September 28, 1993Assignee: Texaco Inc.Inventors: Jiang-Jen Lin, George P. Speranza
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Patent number: 5246965Abstract: The invention relates to the compounds of the formula ##STR1## wherein the C(.dbd.NH)--NHR group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which:R is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid;R.sub.1 is a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical and a cycloaliphatic hydrocarbon radical;X.sub.1 and X.sub.3, independently of one another, are oxygen (--O--) or sulphur (--S--); andX.sub.Type: GrantFiled: September 17, 1992Date of Patent: September 21, 1993Assignee: Ciba-GeigyInventor: Alan J. Main
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Patent number: 5227492Abstract: Diurea derivatives are provided which can be represented by the following general formula and salts thereof: ##STR1## Illustrative derivatives include 1,3-bis[[1-cycloheptyl-3-(3-pyridyl)ureido]-methyl]benzene, 1,3-bis[[1-cycloheptyl-3-(2-pyridyl)ureido]-methyl]benzene, and 1,3-bis[[1-cycloheptyl-3-(4-pyridyl)ureido]-methyl]benzene.The above compounds inhibit acyl-coenzyme A cholesterol acyltransferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester to the smooth muscle of arterial wall in the blood vessel.Type: GrantFiled: June 30, 1992Date of Patent: July 13, 1993Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
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Patent number: 5220059Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is selected from (1) hydrogen; (2) --NR.sub.2 R.sub.3, --OR.sub.2 or --SR.sub.2 where R.sub.2 and R.sub.3 are independently selected from hydrogen, alkyl, aryl and alkylaryl; and (3) optionally substituted C1-C8 alkyl, C2-C8 alkenyl, arylalkyl or cycloalkyl;Y is selected from sulfur and oxygen;n is an integer selected from 0 and 1;M is hydrogen, a pharmaceutically acceptable cation, or a metabolically cleavable group; andZ is a residue of a non-steroidal antiinflammatory drug of general form Z--COOH;or a pharmaceutically acceptable salt, ester or prodrug thereof,as well as pharmaceutical compositions containing the above compounds and a method for their use as lipoxygenase inhibitors.Type: GrantFiled: April 19, 1990Date of Patent: June 15, 1993Assignee: Abbott LaboratoriesInventors: Dee W. Brooks, Joseph F. Dellaria, Jr., James B. Summers, Jr.
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Patent number: 5190974Abstract: Novel .alpha.-mercapto-alkylamines in all possible racemic, enantiomeric and diastereoisomeric forms of the formula ##STR1## wherein n, R.sub.1, R.sub.2, X, A, R.sub.3A and R.sub.4A are set forth in the claims and their non-toxic, pharmaceutically acceptable acid addition salts having excellent analgesic, psychotropic and enkephalinase inhibiting properties.Type: GrantFiled: July 5, 1991Date of Patent: March 2, 1993Assignee: Roussel UclafInventors: Francoise Clemence, Odile Le Martret, Francis Petit
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Patent number: 5179231Abstract: Hexene-1,6-dioic acids, e.g., hex-3-ene-1,6-dioic acid, are prepared by reacting carbon monoxide with at least one butenediol, in a polar, aprotic, basic solvent, in the presence of a catalytically effective amount of palladium values and at least one inorganic halide, the cation of which halide being an alkali or alkaline earth metal and the anion thereof being a chloride or bromide.Type: GrantFiled: December 13, 1990Date of Patent: January 12, 1993Assignee: Rhone-Poulenc ChimieInventor: Philippe Denis
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Patent number: 5169954Abstract: Process for the N-alkylation of ureas by reacting a urea with an alkylating agent in the presence of a solid base and a phase transfer catalyst in a diluent.Type: GrantFiled: December 16, 1991Date of Patent: December 8, 1992Assignee: Chemie Linz Gesellschaft m.b.H.Inventors: Kurt A. Hackl, Heinz Falk
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Patent number: 5166429Abstract: Diurea Derivatives represented by the following general formula and salts thereof: ##STR1## The above compounds inhibit acyl-coenzyme A chloresterol acyl-transferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester to the smooth muscle of arterial wall in the blood vessel.Type: GrantFiled: September 24, 1991Date of Patent: November 24, 1992Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
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Patent number: 5155267Abstract: A selective process for the production of unsymmetric carbamates and ureas is disclosed. In the process, a primary formamide is reacted with a dialkyl amine or an alcohol in the presence of a Group VIII transition metal catalyst. The unsymmetric carbamates and ureas are useful precursors to isocyanates.Type: GrantFiled: October 24, 1991Date of Patent: October 13, 1992Assignee: Arco Chemical Technology, L.P.Inventor: Mahmoud K. Faraj
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Patent number: 5126483Abstract: Novel 1-phenylakyl-3-phenylurea derivatives represented by the following formula (I): ##STR1## wherein R.sup.1 is an alkyl group of 1 to 8 carbon atoms, an alkoxy group of 1 to 5 carbon atoms or a halogen atom, R.sup.2 is an alkyl group of 1 to 15 carbon atoms, each of R.sup.3 and R.sup.4 is independently an alkyl group of 1 to 5 carbon atoms, m is an integer of 1 to 3, and n is 0 or 1, are provided.The compounds are potent in reducing the cholesterol level in serum, and useful for treating hyperlipemia and atherosclerosis.Type: GrantFiled: August 3, 1990Date of Patent: June 30, 1992Assignee: Mitsubishi Kasei CorporationInventors: Tetsuo Sekiya, Shinya Inoue, Chiaki Hyodo, Hiromi Okushima, Kohei Umezu, Kazuo Suzuki
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Patent number: 5124451Abstract: Process for the N-alkylation of ureas by reacting a urea with an alkylating agent in the presence of a solid base and a phase transfer catalyst in a diluent.Type: GrantFiled: July 10, 1991Date of Patent: June 23, 1992Assignee: Chemie Linz Gesellschaft m.b.H.Inventors: Kurt A. Hackl, Heinz Falk
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Patent number: 5099030Abstract: The present invention relates to beta-aminoethyl-substituted phenyl compounds, especially beta-aminoethoxy-substituted phenyl compounds. The present invention also relates to pharmaceutical compositions comprising a safe and effective amount of a compound of the present invention and a pharmaceutically-acceptable carrier. The present invention further relates to methods for producing analgesia and reducing inflammation, in humans and lower animals, by administering the compounds or compositions of the present invention. In addition, the present invention relates to methods for making compounds of the present invention and intermediates useful in these synthesis methods.Type: GrantFiled: June 27, 1991Date of Patent: March 24, 1992Assignee: The Procter & Gamble CompanyInventors: Joseph H. Gardner, Gerald B. Kasting, Thomas L. Cupps, Richard S. Echler, Thomas W. Gibson, Joel I. Shulman
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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: 5081294Abstract: There are disclosed quaternary ammonium salts which are obtainable by reacting basic carbamides containing a quaternisable nitrogen atom with epihalohydrins.These quaternary ammonium salts are particularly suitable for enhancing the color yield and the wet fastness properties of dyeings or printings produced on cellulosic fibre materials with anionic dye, e.g. reactive or direct dyes.Type: GrantFiled: March 21, 1989Date of Patent: January 14, 1992Assignee: Ciba-Geigy CorporationInventors: Rosemarie Topfl, Jorg Binz
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Patent number: 5066678Abstract: The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof; wherein;R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a C.sub.1-3 -alkyl group with the proviso that the sum total of carbon atom in R.sup.1 and R.sup.2 is not more than 4;X represents a direct bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene group and Y represents a direct bond or a C.sub.1-6 alkylene C.sub.2-6 alkenylene or C.sub.2-6 alknylene group with the proviso that the sum total of carbon atoms in X and Y is not more than 10;W represents a group ##STR2## wherein Z represents a group R.sup.3 (CH.sub.2).sub.q where q is 0, 1 or 2 and R.sup.3 is a group R.sup.4 CONH--, R.sup.4 NHCONH--, R.sup.4 R.sup.5 NSO.sub.2 NH--, R.sup.6 SO.sub.2 NH-- or --OH;R.sup.4 and R.sup.5 each represent a hydrogen atom or a C.sub.1-3 alkyl group;R.sup.6 represents a C.sub.1-3 alkyl group;R.sup.7 represents a chlorine atom or the group --CF.sub.Type: GrantFiled: April 23, 1990Date of Patent: November 19, 1991Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, Ian B. Campbell, Charles Willbe, William L. Mitchell, Stephen Swanson, Brian D. Judkins
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Patent number: 5064827Abstract: Compounds of the present invention, are represented by the general formula ##STR1## wherein R.sub.1 group which may be alkyl of from 1 to about 6 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 10 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, nitro, alkylamino of from 1 to about 6 carbon atoms, hydroxy, hydroxyalkyl of from 1 to about 6 carbon atoms, cyano or arylalkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms R.sub.2, R.sub.3 and R.sub.4 are hydrogen or hydroxyl groups or the combination of either hydrogen or hydroxyl groups; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NHCOR.sub.5, --NHCONR.sub.5 R.sub.6, or --NHCOOR.sub.5 wherein R.sub.5 and R.sub.Type: GrantFiled: August 23, 1990Date of Patent: November 12, 1991Assignee: Du Pont Merck Pharmaceutical CompanyInventors: Ghanshyam Patil, William L. Matier, Khuong H. X. Mai
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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: 5045565Abstract: The present invention relates to beta-aminoethyl-substituted phenyl compounds, especially beta-aminoethoxy-substituted phenyl compounds. The present invention also relates to pharmaceutical compositions comprising a safe and effective amount of a compound of the present invention and a pharmaceutically-acceptable carrier. The present invention further relates to methods for producing analgesia and reducing inflammation, in humans and lower animals, by administering the compounds or compositions of the present invention. In addition, the present invention relates to methods for making compounds of the present invention and intermediates useful in these synthesis methods.Type: GrantFiled: September 8, 1989Date of Patent: September 3, 1991Assignee: The Procter & Gamble CompanyInventors: Joseph H. Gardner, Gerald B. Kasting, Thomas L. Cupps, Richard S. Echler, Thomas W. Gibson, Joel I. Shulman
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Patent number: 5043444Abstract: Process for the preparation of asymmetrically substituted ureas by reaction of a gaseous mixture of isocyanic acid and ammonia having a temperature of 260.degree. to 600.degree. C. with a primary or secondary amine.Type: GrantFiled: July 12, 1990Date of Patent: August 27, 1991Assignee: Chemie Linz Gesellschaft m.b.H.Inventors: Martin Mullner, Gerhard Stern, Markus Rossler
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Patent number: 5039801Abstract: The invention provides an improved method for obtaining optically active amines, carbamates, and isocyanates by thermal fragmentation of optically active ureas through refluxing the ureas in C.sub.3 -C.sub.7 alcohol solution with or without catalytic amounts of alkali metal.Type: GrantFiled: August 28, 1987Date of Patent: August 13, 1991Assignee: The United States of America as represented by the Department of Health & Human ServicesInventors: Arnold Brossi, Bernhard Schonenberger
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Patent number: 5011978Abstract: A thickened aqueous copolymer solution useful for thickening and improving the properties of latex systems comprising a copolymer having as monomeric units: about 79-99 percent of a (meth)acrylic acid salt of sodium, potassium, or ammonium; about 0-20 percent of (meth)acrylic acid; about 0-20 percent of a lower alkyl ester of (meth)acrylic acid; about 1-21 percent of surfactant units selected from the urea reaction product of a monoethylenically unsaturated monoisocyanate with a nonionic surfactant having amine functionality; and about 0-1 percent of a copolymerizable polyethylenically unsatured monomer, said percentages being by weight based on the total weight of monomeric units in said copolymer.Type: GrantFiled: December 29, 1989Date of Patent: April 30, 1991Assignee: National Starch and Chemical Investment Holding CorporationInventors: Milagros C. Barron, Ronald L. Swope, John M. Wilkerson, III, Charles G. Ruffner
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Patent number: 4990575Abstract: Disclosed are novel compositions derived from polyoxyalkylene amines comprising olefin-terminated polyoxyalkylene ureas prepared by reacting polyoxyalkylene amines of the formula: ##STR1## with isopropenyl dimethylbenzyl isocyanate represented by the formula: ##STR2## said composition being represented by the formulas: ##STR3## where R'=H or methyl or ethyl and R" is the nucleus of a trifunctional polyol such as glycerine, trimethylolpropane, etc. and x has a value of 2 to 70.Type: GrantFiled: September 20, 1989Date of Patent: February 5, 1991Assignee: Texaco Chemical Co.Inventors: Jiang-Jen Lin, George P. Speranza
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Patent number: 4980366Abstract: Novel 4'-hydroxybenzylamine derivatives of the formula ##STR1## pharmaceutical compositions and methods of use thereof are the present invention. Utility is for the treatment of arthritis, asthma, Raynaud's disease, inflammatory bowel disorders, trigeminal or herpetic neuralgia, inflammatory eye disorders, psoriasis, dental pain, and headaches, particularly vascular headache, succh as migraine, cluster, mixed vascular syndromes, as well as nonvascular, tension headaches.Type: GrantFiled: March 16, 1989Date of Patent: December 25, 1990Assignee: Warner-Lambert Co.Inventors: Graham Johnson, Michael F. Rafferty
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Patent number: 4977153Abstract: Compounds of formula (I), ##STR1## characterized in that R signifies optionally substituted heteroaryl-, heteroarylakyl or heteroarylalkenyl, R.sub.1 signifies hydrogen or a substituent, R.sub.2 is hydroxy or a group --z--(CH.sub.2).sub.n --Y--R.sub.3 wherein R.sub.3 is hydrogen, alkyl, hydroxyalkyl, alkenyl, cycloalkyl, cycloalkylalkylene, hydroxy substituted cycloalkyl or cycloalkylalkylene, or optionally substituted aryl or aralkyl or aralkenyl moiety, and Y signifies oxygen or sulfur, and either Z is an oxygen atom and n is 2 or 3, or Z is a bond and n is 1, 2 or 3, A signifies alkylene or branched alkylene of 2 to 5 carbon atoms, W signifies a bond or imino, and X signifies a bond or imino, and their physiologically hydrolyzable derivatives, in which at least one hydroxy group is in esterified form. The compounds exhibit beta adrenoceptor blocking activity. Processes for the preparation of the compounds are also disclosed.Type: GrantFiled: January 14, 1987Date of Patent: December 11, 1990Assignee: William J. LouisInventors: William J. Louis, Richard Berthold, Max-Peter Seiler, Andre Stoll
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Patent number: 4968679Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: May 22, 1989Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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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: 4906774Abstract: Polyoxyalkylene diamine reaction products which contain as the principle reaction component, a diamine having the formula: ##STR1## wherein R' independently represents hydrogen or methyl and x is a number having an average value of at least 1 to about 60 and a diisocyanate of the formula: ##STR2## The products of the invention are obtained by reacting an excess of polyoxyalkylene diamine with a diisocyanate in the presence of a polar solvent and have the following general structures: ##STR3## where B is alkyl group from diisocyanates, and R' has the same meaning as above.These products are further used to prepare coatings with improved properties by reacting said amine products with isocyanates prepolymers and epoxy material.Type: GrantFiled: July 27, 1987Date of Patent: March 6, 1990Assignee: Texaco Inc.Inventors: George P. Speranza, Jiang-Jen Lin, Michael Cuscurida
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Patent number: 4883815Abstract: Hydrocinnamic acid derivatives of the formula ##STR1## wherein one or two of the symbols R.sup.1 to R.sup.4 are halogen or methoxy and the others are hydrogen;R.sup.5 is hydrogen or phenyl;R.sup.6 is a residue of the formula ##STR2## R.sup.7 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.2 -C.sub.5)-alkanoylamino-(C.sub.2 -C.sub.5)-alkyl, amino or (C.sub.1 -C.sub.4)-alkoxyphenyl;R.sup.8 and R.sup.9 each, independently, are hydrogen or (C.sub.1 -C.sub.4)-alkyl;R.sup.10 is hydrogen and R.sup.11 is hydroxy or R.sup.10 and R.sup.11 taken together are oxo;R.sup.12 is hydrogen, (C.sub.1 -C.sub.10)-alkyl, pyridylmethyl or carbamoylmethyl;R.sup.13 is hydrogen, (C.sub.1 -C.sub.4)-alkyl and R.sup.14 is hydrogen, (C.sub.1 -C.sub.4)-alkyl, pyridyl, phenyl-(C.sub.1 -C.sub.4)-alkyl, carboxy-(C.sub.1 -C.sub.4)-alkyl, carbamoyl-(C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy carbonyl-(C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkoxy carbonyl-C.sub.2 -C.sub.5)-alky, piperidino-C.sub.2 -C.sub.Type: GrantFiled: July 5, 1988Date of Patent: November 28, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwenden, Rene Imhof, Roland Jakob-Roetne, Emilio Kyburz
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Patent number: 4879410Abstract: A process is disclosed for the preparation of aralkyl mono- and diurethanes or ureas by carbamylmethylation, or acid-catalyzed addition at a temperature of 40.degree. C. to about 100.degree. C. of formaldehyde and esters of carbamic acid to aromatic hydrocarbons. Aralkyl carbamates and ureas formed by this process can be cracked directly to produce aralkyl diisocyanates, or hydrogenated and then cracked to produce aliphatic diisocyanates, or reacted directly with polyols to produce polyurethanes by functioning as blocked isocyanates.Type: GrantFiled: November 3, 1986Date of Patent: November 7, 1989Assignee: American Cyanamid CompanyInventors: Balwant Singh, Laurence W. Chang, William A. Henderson, Jr.
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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