R Is Acyclic Patents (Class 514/625)
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Patent number: 5254590Abstract: The invention relates to the compounds of formula (I): ##STR1## in which R represents higher alkyl, 1-(higher alkyl)lower cycloalkyl-1-yl or higher alkenyl comprising one or more double bonds, and eitherR.sub.3 represents hydroxyl,R.sub.1 and R.sub.2, which are different, represent hydrogen or lower alkyl,R.sub.4 and R.sub.5, which are identical or different, represent lower alkyl or alkoxy, orR.sub.1 and R.sub.4 represent hydroxyl andR.sub.2, R.sub.3 and R.sub.5, which are identical or different, represent lower alkyl or alkoxy,their isomers as well as their salts, and a method for treating an animal or human living body afflicted with dylipidemias or atherosclerosis.Type: GrantFiled: March 5, 1992Date of Patent: October 19, 1993Assignee: Adir et CompagnieInventors: Charles Malen, Jean-Michel Lacoste, Jean-Paul Vilaine, Albert Lenaers
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Patent number: 5231087Abstract: Noninfectious inflammatory and hyperpigmentation skin diseases, thermal injuries and premalignant skin tumors induced by radiation or virus, in both humans and animals, are treated with topical formulations of an ester or amide of a monocarboxylic acid, the acid moiety of which is 9 to 18 carbon atoms.Type: GrantFiled: January 22, 1992Date of Patent: July 27, 1993Assignee: Cellegy Pharmaceuticals, Inc.Inventor: Carl R. Thornfeldt
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Patent number: 5221692Abstract: The present invention provides a series of ether linked analogues of N-nonanoyl vanillylamide. They are found pharmaceutically effective in antinociceptive treatment and relatively nonpungent.Type: GrantFiled: August 22, 1991Date of Patent: June 22, 1993Assignee: National Science CouncilInventor: Ing-Jun Chen
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Patent number: 5208034Abstract: Disclosed are novel tetraamide compounds and intermediates therefor which are useful in methods for improving feed conversion and/or weight gain in animals such as chickens.Type: GrantFiled: August 25, 1992Date of Patent: May 4, 1993Assignee: Eastman Kodak CompanyInventors: David C. Herting, Alan W. White
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Patent number: 5206225Abstract: Crystallization of active material in spraying an aqueous solution of one of ##STR1## and is prevented by incorporation therein of an alkylcarboxylic acid dimethylamide of the formula ##STR2## in which R represents alkyl having 5 to 19 carbon atoms.Type: GrantFiled: April 19, 1991Date of Patent: April 27, 1993Assignee: Bayer AktiengesellschaftInventors: Heinz-Otto Horstmann, Uwe Priesnitz, Ulrich Engelhardt, Karl Reizlein, Klaus Wangermann
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Patent number: 5182304Abstract: N-lower alkyl neoalkanamides (N-lower alkyl trialkylacetamides of certain types) of 1 to 4 carbon atoms in the lower alkyl thereof and of 5 to 14 carbon atoms in the neoalkanoyl (or trialkylacetyl) group, e.g., N-methyl- and N-ethyl neodecanamides and N-methyl and N-ethyl neotridecanamides, are new compounds, secondary amides which have insect repellent properties, being especially effective against cockroaches, e.g., the German cockroach. However, they are also useful as repellents for other insects, including American cockroaches, mosquitoes, flies, fleas, ants, and lice. Additionally, they may repel arachnids, such as spiders, ticks and mites. The new neoalkanamides may be synthesized easily, as by reacting a primary lower alkyl amine with a neoalkanoyl halide, e.g. by reacting methyl amine or ethyl amine with neodecanoyl chloride.The most effective of the described amides for insect repellency are normally liquid and are sufficiently volatile to be detectable in air by insects.Type: GrantFiled: November 13, 1990Date of Patent: January 26, 1993Assignee: Colgate-Palmolive Co.Inventor: Robert J. Steltenkamp
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Patent number: 5151446Abstract: The present invention relates generally to compounds having melatonin receptor activities and in particular to substituted 2-amidotetralin derivatives; to pharmaceutical preparations comprising such compounds; and to methods for using these compounds as therapeutic and diagnostic reagents.Type: GrantFiled: March 28, 1991Date of Patent: September 29, 1992Assignee: Northwestern UniversityInventors: Alan S. Horn, deceased, Margarita L. Dubocovich
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Patent number: 5139784Abstract: Comsetic compositions containing alkyl diamides for use in providing moisturizing and/or softening properties to treat dry human skin and for use in other cosmetic applications and including also various novel alkyl diamides.Type: GrantFiled: March 13, 1990Date of Patent: August 18, 1992Assignee: Revlon, Inc.Inventor: Joseph P. Ciaudelli
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Patent number: 5114978Abstract: A composition, or an aqueous mixture containing a composition of a substantially anhydrous blends of parachlorometaxylenol, fatty acid diethanolamides, and anionic surfactants of the class diethanolammonium alkylpolyoxyethyl sulfate and method for making such compositions. The compositions and solutions containing the composition have antimicrobial and cleansing properties.Type: GrantFiled: October 15, 1990Date of Patent: May 19, 1992Assignee: Rhone-Poulenc Surfactants and Specialties, L.P.Inventors: Mike E. Corti, Richard R. Tenore
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Patent number: 5098934Abstract: Novel .omega.-mercaptopropanamides and their homologs of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and ##STR2## R.sub.1 ' is selected from the group consisting of alkyl of 1 to 5 carbon atoms and aryl optionally substituted with at least one member of the group consisting of --OH, alkyl and alkoxy of 1 to 5 carbon atoms, --NO.sub.2 and halogen, n is an integer from 1 to 5, R.sub.2 is selected from the group consisting of hydrogen alkyl of 1 to 5 carbon atoms and aryl and aralkyl of 6 to 15 carbon atoms optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, --OH, halogen and --CF.sub.3, R.sub.3 is selected from the group consisting of a) hydrogen, b) phenyl optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, --OH, --NO.sub.2, halogen, --CF.sub.Type: GrantFiled: June 22, 1990Date of Patent: March 24, 1992Assignee: Roussel UclafInventors: Jean-Paul Vevert, Francoise Delevallee, Rogert Deraedt
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Patent number: 5084270Abstract: Cosmetic compositions containing N-alkoxyalkylamides for use in providing moisturizing and/or softening properties to treat dry human skin and for use in other cosmetic applications and including also various novel N-alkoxyalkylamides.Type: GrantFiled: December 15, 1989Date of Patent: January 28, 1992Assignee: Revlon, Inc.Inventor: Joseph P. Ciaudelli
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Patent number: 5079245Abstract: The compounds 2-trifluoromethyl-7-substituted-6,7,8,9-tetrahydro-[5H]-benzocycloheptenes are disclosed and disclosed to be useful in the treatment of metabolic illnesses such as diabetes, obesity, and their complications. A perferred compound is 2-trifluoromethyl-7-amino-6,7,8,9-tetrahydro-[5H-benzocycloheptane.Type: GrantFiled: July 5, 1989Date of Patent: January 7, 1992Assignee: Adir et CompagnieInventors: Michel Wierzbicki, Pierre Hugon, Jacques Duhault, Francoise Lacour
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Patent number: 5071875Abstract: The present invention relates generally to compounds having melatonin receptor activities and in particular to substituted 2-amidotetralin derivatives; to pharmaceutical preparations comprising such compounds; and to methods for using these compounds as therapeutic and diagnostic reagents.Type: GrantFiled: September 25, 1989Date of Patent: December 10, 1991Assignee: Northwestern UniversityInventors: Alan S. Horn, Margarita L. Dubocovich
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Patent number: 5068064Abstract: The invention relates to N-substituted lauramides.These compounds have the formula ##STR1## in which R.sub.1 is a benzyl group and R.sub.2 is an alkyl having from 1 to 4 carbon atoms, or R.sub.1 and R.sub.2 form a 4-benzylpiperidino group with the nitrogen atom to which they are bonded, and n=2 to 6, or one of its salts with organic or mineral acids. Application: Preparation of compositions for antiseptic or antimicrobial use, or disinfectants and preservatives, especially in the sectors of pharmacy, cosmetology or agri-foodstuffs.Type: GrantFiled: June 7, 1990Date of Patent: November 26, 1991Assignee: SanofiInventors: Vincenzo Proietto, Ali Salhi
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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: 5059620Abstract: The present invention relates to new compounds of the formula ##STR1## wherein X is ##STR2## wherein R.sub.1 is hydrogen, lower alkyl, phenyl, benzyl, cinnamoyl, thiophene, furan, pyrrole, imidazole, pyrazole oxazole or thiazole; W is hydrogen or hydroxy; (Y).sub.A is positioned ortho to W and is an aminoloweralkyl having the formula --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 are the same or different and may be lower alkyl or R.sub.2 and R.sub.3 may together with N form a pyrrolidine, piperidine or azepine ring, and A is 2; n and m are independently from 0 to 5; and R is straight or branched C.sub.1 -C.sub.10 alkyl, straight or branched C.sub.3 -C.sub.10 cycloalkyl, straight or branched C.sub.2 -C.sub.4 alkenyl or straight or branched C.sub.2 -C.sub.4 alkynyl, or a pharmaceutically acceptable salt thereof.These compounds are useful in the treatment of various cardiac arrhythmias.Type: GrantFiled: April 7, 1988Date of Patent: October 22, 1991Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: David M. Stout, William L. Matier, Lawrence A. Black
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Patent number: 5057500Abstract: This invention relates to a new topical pharmaceutical composition for the treatment of pruritis, especially psychogenic and senile types, that contains esters and amides of 5 to 19 carbon atom length monocarboxylic acids. These esters and amides are formulated alone or with other known topical antipruritic agents, such as amine and "Caine" anesthetics, alcohols, ketones, antihistamines, corticosteroids, counterirritants, and any combination of these.Type: GrantFiled: February 12, 1990Date of Patent: October 15, 1991Assignee: Dermatologic Research CorporationInventor: Carl R. Thornfeldt
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Patent number: 5037848Abstract: A compound and method are disclosed for reducing the effects of epilepsy, especially temporal lobe epilepsy. The treatment disclosed by the subject invention is provided by administering an aryl-cycloalkyl-alkanolamine substance having the general formula: ##STR1## The compounds procyclidine, biperiden, and trihexyphenidyl fall within this class of compounds. Although not previously recognized to be effective against epilepsy, all three representative compounds were tested against soman and pilocarpine, two cholinergic neurotoxins used in animal research on epilepsy. All three of those compounds were shown to be highly effective in providing protection against the seizures and neurological damage caused by cholinergic neurotoxins, even when administered only after the onset of convulsions.Type: GrantFiled: August 25, 1989Date of Patent: August 6, 1991Assignee: Washington UniversityInventor: John W. Olney
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Patent number: 5036051Abstract: A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: ##STR1## where A is a substituent; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 wherein R.sub.2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is Ch.sub.2 ; R.sub.1 is loweralkyl, cycloalkyl methyl, benzyl, (alpha, alpha)-dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, 1-bezyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R.sub.3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)loweralkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R.sub.4 is substituted hydroxyalkyamino.Type: GrantFiled: March 2, 1990Date of Patent: July 30, 1991Assignee: Abbott LaboratoriesInventors: Herman H. Stein, Jacob J. Plattner
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Patent number: 5021414Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus;wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages,wherein R.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --,wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene;wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro;or a salt thereof when appropriate.Type: GrantFiled: December 18, 1989Date of Patent: June 4, 1991Assignee: Imperial Chemical Industries PLCInventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
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Patent number: 5017618Abstract: Compounds having the formula ##STR1## and their pharmaceutically acceptable acid addition salts, wherein --X-- is --O--, --CH.sub.2 -- or --; .dbd.Y is .dbd.O or a derivatized keto group which is hydrolyzable or enzymatically convertible to a keto group; R is alkyl having from 1 to 12 carbon atoms or aralkyl having from 7 to 20 carbon atoms; and Ar is the 3-aromatic or heterocyclic residue of a 1-alkylamino-2-propanol having an aromatic or heterocyclic substituent at the 3-position and having .beta.-adrenergic blocking properties; are useful as .beta.-adrenergic blocking agents and are of particular interest in the treatment of glaucoma or for lowering intraocular pressure.Type: GrantFiled: September 18, 1989Date of Patent: May 21, 1991Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 5015665Abstract: N-lower alkyl neoalkanamides of 1 to 4 carbon atoms in the lower alkyl thereof, and of 12 to 14 carbon atoms in the neoalkanoyl group, e.g., N-methyl- and N-ethyl neotridecanamides, are new compounds which have insect repellent properties, being especially effective against cockroaches, e.g., the German and American cocoroaches. However, they are also useful as repellents for other insects, including mosquitoes, moths, flies, fleas, ants, and lice. Additionally, they may repel arachnids, such as spiders, ticks and mites. The new neoalkanamides may be synthesized easily, as by reacting a primary lower alkyl amine with a neoalkanoyl halide, e.g., by reacting methyl amino or ethyl amine with neotridecanoyl chloride. The most effective of the described amides for insect repellency, N-methyl neotridecanamide, is normally liquid and is sufficiently volatile to be detectable in air by insects.Type: GrantFiled: October 31, 1988Date of Patent: May 14, 1991Assignee: Colgate-Palmolive Co.Inventor: Robert J. Steltenkamp
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Patent number: 5006562Abstract: N-lower alkyl neoalkanamides (N-lower alkyl trialkylacetamides of certain types) of 1 to 4 carbon atoms in the lower alkyl thereof and of 5 to 14 carbon atoms in the neoalkanoyl (or trialkylacetyl) group, e.g., N-methyl- and N-ethyl neodecanamides and N-methyl and N-ethyl neotridecanamides, are new componds, secondary amides which have insect repellent properties, being especially effective against cockroaches, e.g., the German cockroach. However, they are also useful as repellents for other insects, including American cockroaches, mosquitoes, flies, fleas, ants, and lice. Additionally, they may repel arachnids, such as spiders, ticks and mites. The new neoalkanamides may be synthesized easily, as by reacting a primary lower alkyl amine with a neoalkanoyl halide, e.g. by reacting methyl amine or ethyl amine with neodecanoyl chloride.The most effective of the described amides for insect repellency are normally liquid and are sufficiently volatile to be detectable in air by insects.Type: GrantFiled: November 4, 1988Date of Patent: April 9, 1991Assignee: Colgate-Palmolive Co.Inventor: Robert J. Steltenkamp
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Patent number: 4980462Abstract: A second-step virus binding receptor is found in nature on the surface of animal and plant cells. This receptor is thought to be needed for virus penetration into target cells. The second-step receptor has been found to bind a wide variety of viruses belonging to a number of different families. The second-step receptor and natural or synthetic substances which correspond to or are analogous to the binding epitope of the second-step receptor in that they are able to bind to a site on the virus which recognizes the binding epitope of the natural second-step receptor, are therefore indicated for the diagnosis, prophylaxis or treatment of viral infections.Type: GrantFiled: June 19, 1989Date of Patent: December 25, 1990Assignee: Symbicom AktiebolagInventors: Karl-Anders Karlsson, Erling Norrby, Goran Wadell
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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: 4962129Abstract: A method for treating the symptoms of a neoplastic disease without treating the disease itself which includes administering by injection an effective amount of a composition which includes the combination of two or more ketones, aldehydes, alcohols or amines having certain twin formation in a vegetable oil solution to a patient who is suffering from the symptoms of a neoplastic disease to alleviate at least some of such symptoms.Type: GrantFiled: February 28, 1986Date of Patent: October 9, 1990Assignee: Elena AvramInventor: Emanuel Revici
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Patent number: 4960798Abstract: Acetylene compounds of the formula (I): ##STR1## wherein Y, R.sub.1, R.sub.2 R.sub.3, and R.sub.4 are as described herein, m is 0-3, n is 0-2 and Ar is phenyl or an aromatic heterocycle are disclosed. The compounds possess anti-hypertensive and anti-anginal properties and may be used in the treatment of humans. Methods for the preparation and use of such acetylene compounds are also disclosed.Type: GrantFiled: January 26, 1990Date of Patent: October 2, 1990Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4943307Abstract: The invention relates to a plant-protective solution containing 2.5 to 40 % by weight of one or more water-insoluble plant-protective ingredient(s) 20 to 71.5 % by weight of dimethylformamide and/or dimethylsulfoxide and/or acetone as water-miscible solvent, 10 to 71.5 % by weight of furfurol and/or furfuryl alcohol as partially water-miscible solvent, 1 to 15 % by weight of commonly used additives such as anionic and/or nonionic surface active agents and macromolecules.The invention also relates to the ready-for-use plant-protective suspension containing 0.2 to 10 % by weight of one or more water-insoluble plant-protective ingredient(s) with a particle size of 0.1 to 50 .mu.m, 0 to 60 % by weight of a fertilizer, 0.2 to 10 % by weight of dimethylformamide and/or dimethylsulfoxide and/or acetone as water-miscible solvent, 0.2 to 10 % by weight of furfurol and/or furfuryl alcohol as partially water-miscible solvent, 0.05 to 2.Type: GrantFiled: July 15, 1988Date of Patent: July 24, 1990Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.Inventors: Tamas Detre, Sandor ngyan, Laszlo Pap, Andras Szego, Zoltan Karadi, Klara Bertus nee Bende, Katalin Marmarosi nee Kellner
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Patent number: 4940730Abstract: The present invention relates to a composition with enhanced angiogenic activity which contains a compound of the formula:R--Awherein R stands for a higher aliphatic hydrocarbon residue, and A stands for hydrogen atom, carboxyl group, hydroxyl group, carbamoyl group which may be substituted or amino group which may be substituted or quaternized.The composition of the present invention has been found to enhance blood vessel formation, which is useful for the treatment of various ischemic diseases, trauma, thermal burns, alopecia, etc.Type: GrantFiled: October 3, 1988Date of Patent: July 10, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaori Wakamatsu, Koichi Kondo, Katsuichi Sudo
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Patent number: 4938797Abstract: The invention relates to a process for the preparation of microcapsules having a capsule wall of polyurea and encapsulating a water-immiscible pesticide. The process comprises first dispersing a solution of a polyisocyanate in the sparingly water-soluble pesticide, in the presence of an anionic dispersant and at least one nonionic protective colloid and/or a nonionic surfactant, and subsequently reacting the dispersion with a polyamine, to give a stable aqueous suspension of microcapsules which can be used either direct or after dilution with water as pesticidal composition.Type: GrantFiled: June 7, 1988Date of Patent: July 3, 1990Assignee: Ciba-Geigy CorporationInventors: Hans W. Hasslin, Michael J. Hopkinson
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Patent number: 4927807Abstract: A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 wherein R.sub.2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkyl, benzyl, (alpha, alpha)-dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, 1-benzyloxyethyl, phenoxy, thiophenoxy or anilino; R.sub.3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)alkyl, carboxyalkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R.sub.4 is a substituted amino group; or pharmaceutically acceptable salts or esters thereof.Type: GrantFiled: September 8, 1988Date of Patent: May 22, 1990Assignee: Abbott LaboratoriesInventors: Herman H. Stein, Jacob J. Pattner, Steven R. Crowley
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Patent number: 4902676Abstract: This invention provides compositions comprising a physiologically-active agent and a compound represented by the general formula ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of alkyl radicals and cycloalkyl radicals comprising from 1 to 10 carbon atoms and R is selected from the group consisting of alkyl radicals and cycloalkyl radicals comprising from 1 to 30 carbon atoms; provided, however, that the total number of carbon atoms in said compound is 15 or more and the total number of carbon atoms in R.sup.1 and R.sup.2 is 5 or more.Type: GrantFiled: September 29, 1986Date of Patent: February 20, 1990Assignee: Nelson Research & Development Co.Inventors: James V. Peck, Gevork Minaskanian
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Patent number: 4898889Abstract: Acetylene compounds of the formula (I): ##STR1## wherein Y, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as described herein, m is 0-3, n is 0-2 and Ar is phenyl or an aromatic heterocycle are disclosed. The compounds possess antihypertensive and anti-anginal properties and may be used in the treatment of humans. Methods for the preparation and use of such acetylene compounds are also disclosed.Type: GrantFiled: March 27, 1989Date of Patent: February 6, 1990Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4897382Abstract: Organic amide compounds of the formula ##STR1## wherein R.sub.1 --CO is a residue of a carboxylic acid with the proviso that the carboxylic acid is not a natural fatty acid normally bound to nitrogen of nitrogenous lipids, R.sub.2 is a hydrogen atom, a C.sub.1-7 alkyl group, or a C.sub.4-7 cycloalkyl group, and R.sub.3-N is a residue of a nitrogenous lipid. The compounds are useful in increasing or stimulating the in vivo biological activity of in vitro biologically active carboxylic acids.Type: GrantFiled: June 21, 1988Date of Patent: January 30, 1990Assignee: Fidia S.p.A.Inventors: Francesco della Valle, Aurelio Romeo
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Patent number: 4859769Abstract: A second-step virus binding receptor is found in nature on the surface of animal and plant cells. This receptor is thought to be needed for virus penetration into target cells. The second-step receptor has been found to bind a wide variety of viruses belonging to a number of different families. The second-step receptor and natural or synthetic substances which correspond to or are analogous to the binding epitope of the second-step receptor in that they are able to bind to a site on the virus which recognizes the binding epitope of the natural second-step receptor, are therefore indicated for the diagnosis, prophylaxis or treatment of viral infections.Type: GrantFiled: November 5, 1986Date of Patent: August 22, 1989Assignee: Symbicom ABInventors: Karl-Anders Karlsson, Erling Norrby, Goran Wadell
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Patent number: 4859706Abstract: Carboxamides of the general formula I ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.3 -C.sub.10 -cycloalkyl, C.sub.3 -C.sub.10 -cycloalkyenyl or C.sub.4 -C.sub.10 -cycloalkenylalkyl, and R.sup.2 and R.sup.3 are each hydrogen, halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.3 -haloalkyl. C.sub.1 -C.sub.3 -haloalkoxy or methylthio, and their use for combating pests.Type: GrantFiled: August 6, 1987Date of Patent: August 22, 1989Assignee: BASF AktiengesellschaftInventors: Rainer Buerstinghaus, Peter Hofmeister, Christoph Kuenast
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Patent number: 4859707Abstract: This invention relates to sulfur-substituted phenylacetamides of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different and are H or CH.sub.3 ; R.sub.4 is SR.sub.5, ##STR2## R.sub.5 and R.sub.6 may be the same or different and are lower alkyl containing 1-4 carbon atoms and R.sub.5 and R.sub.6 may be taken together with S to form a 5-7 member ring; and X.sup.- is a pharmaceutically acceptable anion, which exhibit arrhythmia activity.Type: GrantFiled: August 23, 1983Date of Patent: August 22, 1989Assignee: Key Pharmaceuticals, Inc.Inventors: Thorsteinn Loftsson, Nicholas Bodor
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Patent number: 4851434Abstract: A non-greasy skin moisturizing composition is provided which includes as the major component a compound which has the formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each may be H or lower alkyl, X is ##STR2## and n is 2 to 20, one or more preservatives and water, and optionally one or more thickeners, one or more skin soothing agents, such as allantoin and/or dl-panthenol, one or more astringents, and/or one or more colorants.Type: GrantFiled: May 27, 1983Date of Patent: July 25, 1989Inventor: George E. Deckner
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Patent number: 4808572Abstract: Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: a is an integer of from 1 to 7,R.sup.o represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted at the terminal carbon atom by a free or acylated hydroxy group, by a halogen atom having an atomic number of at most 17, or by methoxy, or represents C.sub.1-3 -perfluoroalkyl,R.sup.2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene or alternatively, if R.sup.1 represents a halogenated radical and/or B represents phenylene or ethylene, a single bond or vinylene,B represents a single bond, ethynylene or phenylene,R.sup.3 represents hydroxy, C.sub.Type: GrantFiled: December 1, 1986Date of Patent: February 28, 1989Assignee: Ciba-Geigy CorporationInventors: Andreas Beck, Werner Breitenstein, Andreas von Sprecher, Robert W. Lang, Konrad Oertle
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Patent number: 4789687Abstract: A food product comprising a food substance in combination with vanillylamine or a vanillylamide.Type: GrantFiled: January 13, 1987Date of Patent: December 6, 1988Assignee: Ajinomoto Co., Inc.Inventor: Kazuo Iwai
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Patent number: 4778823Abstract: An external medicament comprises a novel amide derivative represented by the following formula (I). ##STR1## The external medicament is applicable to both a pharmaceutical external medicament and a cosmetic composition, and it provides excellent improving and preventing effects for chapping of the skin.Type: GrantFiled: December 8, 1986Date of Patent: October 18, 1988Assignee: Kao CorporationInventors: Akira Kawamata, Shinji Yano, Michihiro Hattori, Shuichi Akazaki, Genji Imokawa, Naotake Takaishi
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Patent number: 4762829Abstract: A novel polyprenyl compound such as a polyprenyl carboxylic acid amide is disclosed. It has antithrombic and antiplatelet aggregation activity.Type: GrantFiled: October 23, 1986Date of Patent: August 9, 1988Assignee: Eisai Co., Ltd.Inventors: Isao Yamatsu, Takeshi Suzuki, Shinya Abe, Kouji Nakamoto, Akiharu Kajiwara, Tohru Fujimori, Koukichi Harada, Shinichi Kitamura
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Patent number: 4743588Abstract: Compositions and methods useful for enhancing the transdermal and transmembrane drug delivery of topical and systemic agents. The compositions and methods comprise the active agent together with an effective amount of certain amides of heterocyclic amines as defined herein as penetration enhancers and topically administering to human or animal skin or other membranes the resulting compositions.Type: GrantFiled: June 13, 1984Date of Patent: May 10, 1988Assignee: Allergan Pharmaceuticals, Inc.Inventors: Dorla Mirejovsky, Harun Takruri
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Patent number: 4689344Abstract: A novel class of compounds has been found to be effective in blocking cholesterol and neutral lipid synthesis in-vivo without adversely affecting energy metabolism, useful for the treatment of obesity, hyperlipidemia and maturity-onset diabetes. The active compounds have the general formula ##STR1## or in-vivo hydrolyzable functional derivatives of the carboxylic groups thereof,whereinR.sub.1 and R.sub.2 each independently represents an unsubstituted or substituted hydrocarbyl or hetercyclyl radical;X and Y each independently represents hydrogen, optionally substituted lower alkyl, halogen, cyano, carboxy, lower alkoxycarbonyl or carbamoyl; andQ represents a diradical consisting of a linear chain of 8 to 14 carbon atoms, one or more of which may be replaced by heteroatoms, said chain being optionally substituted by inert substituents and one or more of said carbon or heteratom chain members optionally forming part of a ring structure.Type: GrantFiled: June 22, 1984Date of Patent: August 25, 1987Assignee: Epis S.A.Inventor: Jacob Bar-Tana
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Patent number: 4680313Abstract: A food product comprising a food substance in combination with vanillylamine or a vanillylamide.Type: GrantFiled: February 24, 1986Date of Patent: July 14, 1987Assignee: Ajinomoto Co., Inc.Inventor: Kazuo Iwai
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Patent number: 4666943Abstract: Use of an anilide of the formula: ##STR1## as a fungicidal agent against phytophatogenic fungi, particularly their strains resistant to benzimidazole thiophanate fungicides and/or cyclic imide fungicides.Type: GrantFiled: July 19, 1983Date of Patent: May 19, 1987Assignee: Sumitomo Chemical Company, LimitedInventors: Hiroshi Noguchi, Toshiro Kato, Junya Takahashi, Yukio Ishiguri, Shigeo Yamamoto, Naonori Hirata
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Patent number: 4647589Abstract: Aqueous substrates are treated to inhibit microbiological growth by addition of dimethylaminopropylmethacrylamide or dimethylaminopropylacrylamide.In the presence of corrosion inhibitors, it is found that the instant biocides will permit attainment of 100% biocidal kill when present in lesser amounts than are required when no corrosion inhibitor is present. Presence of the instant biocides causes no deletrious impact upon the corrosion inhibitors; and in fact an improvement in corrosion inhibition is observed in the presence of the biocide.Type: GrantFiled: May 25, 1984Date of Patent: March 3, 1987Assignee: Texaco Inc.Inventor: Frederick W. Valone
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Patent number: 4636505Abstract: Acylanilides of the formula ##STR1## wherein R.sup.1 and R.sup.2, the same or different, each is cyano, carbamoyl, nitro, halogeno, perfluoroalkyl or other defined substituents;R.sup.3 is hydrogen or halogen;R.sup.4 is hydrogen or alkyl, or is joined to R.sup.5 ;R.sup.5 is hydrogen, hydroxy, alkoxy or acyloxy or is joined to R.sup.4 ;R.sup.6 is alkyl or halogenoalkyl, or has the formula --A.sup.3 --R.sup.8 or --A.sup.4 --X.sup.2 --A.sup.5 --R.sup.9 ;A.sup.1 and A.sup.4, the same or different, each is alkylene;A.sup.2, A.sup.3 and A.sup.5, the same or different, each is a direct link or alkylene;X.sup.1 and X.sup.2, the same or different, each is oxygen, sulphur, sulphinyl, sulphonyl, imino or alkylimino;R.sup.7 and R.sup.9, the same or different, each is alkyl, alkenyl, hydroxyalkyl, cycloalkyl, phenyl optionally substituted, naphthyl or heterocyclic optionally substituted;and R.sup.8 is phenyl, naphthyl or heterocyclic as defined above for R.sup.7 or R.sup.Type: GrantFiled: July 15, 1983Date of Patent: January 13, 1987Assignee: Imperial Chemical Industries PLCInventor: Howard Tucker
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Patent number: 4619944Abstract: Provided are antihypertensive compounds of the formula ##STR1## wherein 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, or cycloalkyl, and may be the same or different,m is an integer from 0 to 2 inclusive,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-cycloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl.Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl-alkyl, heterocyclic, --CO--SR, --CS--SR, ##STR2## CH.sub.2 CO.sub.2 R, --CHM--CO.sub.2 R, --CH.sub.2 --CO--SR, --CN, ##STR3## --CO--NH--CH.sub.2 CO.sub.2 R, ##STR4## or --CO--CO.sub.Type: GrantFiled: February 19, 1985Date of Patent: October 28, 1986Assignee: USV Pharmaceutical CorporationInventors: Raymond D. Youssefyeh, Howard Jones
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Patent number: 4567198Abstract: Novel analgesic and enkephalinase inhibiting compositions comprising an analgesically and enkephalinase inhibitory effective amount of at least one compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and acetyl, n is 1 or 2 and when n is 1, R.sub.2 is selected from the group consisting of phenyl, p-chlorophenyl, m-trifluoromethylphenyl and thiazolyl and when n is 2, R.sub.2 is selected from the group consisting of phenyl and p-chlorophenyl and their salts with non-toxic, pharmaceutically acceptable acids and bases and an inert pharmaceutical carrier and novel method of relieving pain and inhibiting enkephalinase activity in warm-blooded animals and novel amides.Type: GrantFiled: February 6, 1984Date of Patent: January 28, 1986Assignee: Roussel UclafInventors: Francoise Delevallee, Roger Deraedt, Odile Le Martret