Carbon To Carbon Unsaturation In R Patents (Class 514/627)
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Patent number: 5602164Abstract: Obesity is treated by the administration to a subject of a compound having the general formula (I): R.sub.4 --(CH.sub.2).sub.n --CO--N(R.sub.1)--CH(R.sub.2)--CO(--R.sub.3), wherein R.sub.1 represents H or CH.sub.3 ; R.sub.2 represents a side chain of a naturally occurring amino acid; R.sub.3 represents OH, OCH.sub.2 CH.sub.3 and NH.sub.2 ; n is 6-18; and R.sub.4 represents CH.sub.3 or a group having the general formula (II): R.sub.3 --CO--CH(R.sub.2)--N(R.sub.1)--CO--, wherein R.sub.1, R.sub.2 and R.sub.3 have the above meanings. The compounds of formula (I) wherein R.sub.4 is a group of formula (II), are novel compounds.Type: GrantFiled: March 18, 1996Date of Patent: February 11, 1997Assignee: Senyorina Ltd.Inventors: Meir Shinitzky, Avner Shenfeld
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Patent number: 5599803Abstract: Insecticidal compositions, comprising normally-employed insecticides but comprising also an effective activity-enhancing amount of capsaicin or other capsaicinoid, especially in the form of capsicum, exhibit synergistic effects against numerous insects, including especially bud worms, boll worms, cabbage loopers, army worms, beet army worms, and beetles, and are especially effective on cotton, soybeans, common garden vegetables, and flowers, when sprayed on the insect or its habitat, especially as an aqueous solution, suspension, or emulsion. Larger crop stands may be effectively treated by aerial spraying from the usual crop-dusting airplane.Type: GrantFiled: September 29, 1995Date of Patent: February 4, 1997Assignee: Kalamazoo Holdings, Inc.Inventors: Gary C. Hainrihar, James G. Dubberly, John T. Greenlee
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Patent number: 5596019Abstract: Certain N-acyl-cycloalkylamine derivatives are useful as melatonergic agents.Type: GrantFiled: June 7, 1995Date of Patent: January 21, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Ronald J. Mattson, Daniel J. Keavy, Michael F. Parker, Graham Johnson
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Patent number: 5589178Abstract: Cosmetic or dermatological compositions containing at least one anti-aging active agent having an irritant effect, a cosmetically or dermatologically acceptable medium, and in addition, as an agent mollifying the irritant effect, a ceramide of the following formula (I): ##STR1## R.sub.1 is a saturated or unsaturated, linear or branched C.sub.10 to C.sub.26 alkyl group;R.sub.2 is a saturated or unsaturated, linear or branched C.sub.12 to C.sub.32 alkyl group;R.sub.3 is H or --CO--CHOH--R.sub.2 ; andn is 0 or 1.Type: GrantFiled: December 30, 1994Date of Patent: December 31, 1996Assignee: L'OrealInventors: Lucien Aubert, Francoise Gagnebien-Cabanne
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Patent number: 5571794Abstract: A cosmetic treatment for inducing upper and lower lip augmentation in humans, wherein an active ingredient encouraging vasodilatation, preferably an ultra highly diluted homeopathic, ultra highly diluted element, local irritant or direct local vasodilator or a combination of two or more is administered by topical application or sublingually or gum by chewing. The vasodilators singly or in combinations of preferably ultra highly diluted elements, homeopathics, local irritant or vasodilators are diluted to preferably ten to fifteen percent for topical administration in a cosmetic cream or cosmetic gel or oral sublingual drops diluted in a 2% alcohol base or a five percent fructose-coated chewing gum. The treatment results in a significant non-invasive augmentation of both the upper and lower lip that onsets within a few moments and is effective for a duration on an average of four and one half hours.Type: GrantFiled: June 22, 1995Date of Patent: November 5, 1996Inventor: Bruce M. Frome
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Patent number: 5560910Abstract: The present invention comprises compositions and methods that are useful for topically treating inflammation caused by a wide variety of diseases. The compositions comprise an effective amount of a proteolytic enzyme, such as bromelain, in combination with capsaicin in a pharmaceutically acceptable carrier.Type: GrantFiled: August 26, 1994Date of Patent: October 1, 1996Inventor: Wilson T. Crandall
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Patent number: 5561162Abstract: Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops. Polar compounds, for example, 3,4,4-trifluoro-3-butene-1-amine or 3,4,4-trifluoro-3-butenoic acid, are particularly useful for systemic control of pests. Novel method and intermediates for the preparation of 3,4,4-trifluoro-3-butene-1-amine are also provided.Type: GrantFiled: March 8, 1995Date of Patent: October 1, 1996Assignee: Monsanto CompanyInventor: Peter G. Ruminski
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Patent number: 5547686Abstract: A fodder and a method are provided for increasing the amount of unsaturated fatty acids in the tissues and milk of ruminants. Specifically, the present invention includes feeding to a ruminant a composition containing the reaction product of an unsaturated fatty acid with a primary amine. The reaction product escapes hydrogenation in the stomachs of the ruminant allowing unsaturated fatty acids to be absorbed into the blood stream of the animal. In one embodiment, the unsaturated fatty acids used to react with the amine are derived from soybean oil. By increasing the amount of unsaturated fatty acids in the tissues and milk of ruminants, the food products obtained from those animals is healthier for human consumption.Type: GrantFiled: August 15, 1994Date of Patent: August 20, 1996Assignee: Clemson UniversityInventor: Thomas C. Jenkins
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Patent number: 5545630Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is C.sub.3 -C.sub.8 cycloalkyl, halo-C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, halo-C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, --Si(R.sub.3).sub.3, --S--R.sub.4, --SO.sub.2 --R.sub.6 or --CO--R.sub.9 ;R.sub.2 is halogen, C.sub.1 -C.sub.4 alkyl or CF.sub.3, the substituents R.sub.2 being identical or different when n is 2;R.sub.3 each independently of the others is C.sub.1 -C.sub.6 alkyl, halo-C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or phenyl;R.sub.4 is aryl or heteroaryl each of which is unsubstituted or substituted;R.sub.6 is unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.1 -C.sub.20 alkoxy, C.sub.2 -C.sub.6 alkenyloxy, C.sub.2 -C.sub.6 alkynyloxy, C.sub.1 -C.sub.4 alkylthio, aryl, aryloxy or arylthio, or is optionally substituted amino;R.sub.9 is hydroxy, unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.Type: GrantFiled: June 5, 1995Date of Patent: August 13, 1996Assignee: Ciba-Geigy CorporationInventors: Peter Maienfisch, Manfred B oger, Thomas Pitterna, Henry Szczepanski
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Patent number: 5543431Abstract: A compound having the formula ##STR1## which is an anti-fungal agent is described. The producing organism Colletotricum accutatum is also described, along with a method of production.Type: GrantFiled: May 24, 1995Date of Patent: August 6, 1996Assignee: Merck & Co., Inc.Inventors: Evon A. Bolessa, Robert E. Schwartz, Gerald F. Bills, Robert A. Giacobbe, Fernando Pelaez Perez, Angeles Cabello Arroyo, Teresa Diez Matas, Isabel Martin Fernandez, Francisca Vicente Perez, Suzanne M. Mandala, Deborah L. Zink, Rosemary Thornton, John R. Thompson, James E. Curotto
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Patent number: 5541228Abstract: New melatonergic agents are phenyl alkanyl or phenyl alkyl substituted carboxamides and ureas of Formula I: ##STR1## wherein: R.sub.1 =C.sub.1-3 alkyl, allyl, C.sub.3-6 cycloalkyl substituted C.sub.1-4 alkyl;R.sub.2 =hydrogen, halogen or C.sub.1-4 alkoxy;R.sub.3 =hydrogen or C.sub.1-4 alkyl;R.sub.4 =C.sub.1-4 alkyl, C.sub.1-4 alkyl substituted amino, carboxylic acid substitutedC.sub.1-4 alkyl or C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl, or straight or branched chain C.sub.2-4 alkenyl;A=a linear C.sub.2-4 alkanediyl or alkenediyl chain, provided that A not be --CH.sub.2 CH.sub.2 -- when X is a bond; andX=a covalent bond or oxygen.Type: GrantFiled: March 8, 1995Date of Patent: July 30, 1996Assignee: Bristol-Myers Squibb Co.Inventors: Katherine S, Takaki, George N. Karageorge, Daniel J. Keavy, Michael F. Parker, Brett T. Watson
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Patent number: 5538998Abstract: There are provided with a novel N-substituted-3-halopropiolamide compound, a method of producing the compound, and a composition for controlling noxious organisms containing the compound. The present compound exhibits superior antimicrobial and antifungal effects. Pest control agents containing the compound can advantageously be used for wide applications.Type: GrantFiled: October 21, 1994Date of Patent: July 23, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Yoshihiro Sugihara, Toshiro Yamashita, Sachio Shibata, Koichi Matsumura, Yosei Kuwazuru
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Patent number: 5525597Abstract: Insecticidal compositions, comprising normally-employed insecticides but comprising also an effective activity-enhancing amount of capsaicin or other capsaicinoid, especially in the form of capsicum, exhibit synergistic effects against numerous insects, including especially bud worms, boll worms, cabbage loopers, army worms, beet army worms, and beetles, and are especially effective on cotton, soybeans, common garden vegetables, and flowers, when sprayed on the insect or its habitat, especially as an aqueous solution, suspension, or emulsion. Larger crop stands may be effectively treated by aerial spraying from the usual crop-dusting airplane.Type: GrantFiled: December 14, 1993Date of Patent: June 11, 1996Assignee: Kalamazoo Holdings, Inc.Inventors: Gary C. Hainrihar, James G. Dubberly, John T. Greenlee
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Patent number: 5466712Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants ##STR1##Type: GrantFiled: November 4, 1994Date of Patent: November 14, 1995Assignee: American Home Products CorporationInventors: John A. Butera, Schuyler A. Antane, Bradford H. Hirth
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Patent number: 5464624Abstract: A method is provided for loading a delivery system for a chemical repellant composition. An aqueous mixture comprising one part water-soluble isothiuronium salt and two parts weak base is prepared. Capsaicin is added to the aqueous mixture before it is loaded into the delivery system. A fluorescent compound, such as dichlorofluorescine, may also be added to the aqueous mixture and capsaicin before loading the delivery system.Type: GrantFiled: December 18, 1992Date of Patent: November 7, 1995Inventor: Arthur F. Isbell
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Patent number: 5464867Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.Type: GrantFiled: November 16, 1994Date of Patent: November 7, 1995Assignee: American Home Products CorporationInventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
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Patent number: 5456916Abstract: The present invention provides a resin molding composition for preventing gnawing damage by the animal, a microcapsule filled with a capsaicine compound, and a process for producing the capsaicine compound and the microcapsule.Type: GrantFiled: February 22, 1994Date of Patent: October 10, 1995Assignee: Nippon Kayaku Kabushiki KaishaInventors: Mitsuo Kurata, Yasuhiro Ichikawa, Mika Toya, Iwao Takahashi, Yoshinobu Okui, Shoichi Kato, Takeshi Nishitani
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Patent number: 5455273Abstract: The invention relates to N,N-disubstituted arylcycloalkylamines of general formula ##STR1## wherein n, m, A, X and R.sup.1 to R.sup.7 are defined as in claim 1, the isomers, isomer mixtures and salts thereof, which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis.Type: GrantFiled: November 19, 1993Date of Patent: October 3, 1995Assignee: Karl Thomae GmbHInventors: Roland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
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Patent number: 5446027Abstract: Amino derivatives represented by the following general formula (1): ##STR1## and external skin care preparations containing such an amide derivative, are useful for preventing or curing skin roughness. Intermediates useful for the preparation of such amides are also disclosed.Type: GrantFiled: November 2, 1993Date of Patent: August 29, 1995Assignee: Kao CorporationInventors: Taketoshi Fujimori, Yukihiro Ohashi, Akira Kawamata
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Patent number: 5441980Abstract: The present invention relates to a dermatological and/or cosmetological composition which is useful in the treatment of pediculosis, characterized in that it contains a synergic combination of a pyrethroid and of crotamiton.The pyrethroids which are the subject of this composition are more particularly permethrin, bioallethrin, resmethrin, tetramethrin and deltamethrin.Type: GrantFiled: April 16, 1993Date of Patent: August 15, 1995Assignee: Pierre Fabre SanteInventors: Pierre Fabre, Gilbert Mouzin, Michel JeanJean, Nicole Monteny, Henri Cousse
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Patent number: 5434190Abstract: N-monosubstituted neoalkanamides of 11 to 14 carbon atoms wherein the substituent on the amide nitrogen is cyclic (aromatic or cycloaliphatic, such as aryl or cycloalkyl) and of at least five carbon atoms, have been discovered to be insect repellent, providing that any aromatic substituent is unsubstituted at the ortho position and that when the neoalkanoyl moiety is pivaloyl the total number of carbon atoms in the N-cyclic neoalkanamide is at least 12. Such neoalkanamides are useful as repellents against cockroaches, including American, German and Oriental cockroaches, and are also effective against mosquitoes (both Anopheles and Aedes), black flies and carpenter ants, and to some extent against deer ticks. They may be applied to areas, locations and items which are desirably to be kept free of such insects, with applications being direct or of solutions or emulsions thereof, preferably by spraying, or in detergent compositions or other products to be applied to such areas, etc.Type: GrantFiled: October 11, 1994Date of Patent: July 18, 1995Assignee: Colgate-Palmolive Co.Inventor: Robert J. Steltenkamp
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Patent number: 5434189Abstract: N-lower alkyl neoalkanamides of 1 to 2 carbon atoms in the lower alkyl thereof, and of 12 to 14 carbon atoms in the noalkanoyl 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 cockroaches. 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 amine or ethyl amine with neotridecanoyl chloride.Type: GrantFiled: January 25, 1994Date of Patent: July 18, 1995Assignee: Colgate-Palmolive Co.Inventor: Robert J. Steltenkamp
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Patent number: 5431914Abstract: A method of treating a pathological condition of an internal organ in a patient which comprises topically applying capsaicin to the skin of the patient containing nerves which lead to the spinal cord segments corresponding to the internal organ without the need of systemic absorption of the capsaicin.Type: GrantFiled: March 16, 1994Date of Patent: July 11, 1995Inventors: Michael Adekunle, James L. Flowers
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Patent number: 5416118Abstract: Novel bicyclic amides of the formula ##STR1## wherein Ar.sup.1 and Ar.sup.2 are phenyl, R.sup.2 -substituted phenyl, heteroaryl or R.sup.2 -substituted heteroaryl, wherein R.sup.2 is 1 to 3 substituents independently selected from the group consisting of halogeno, hydroxy, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino and lower dialkylamino;X, Y and Z are --CH.sub.2 --, --CH(alkyl)--, --C(alkyl).sub.2 --, --NH--, --N(alkyl)--, --O-- or --SO.sub.r, wherein r is 0, 1 or 2, and m, n and p are 0 or 1;R.sup.1 is an alkyl chain of 1 to 25 carbon atoms; an alkyl chain substituted by one or more optionally substituted phenyl or heteroaryl groups; an alkyl chain --O--, --SO.sub.r, phenylene, R.sup.2 -substituted phenylene, heteroarylene or R.sup.Type: GrantFiled: September 28, 1993Date of Patent: May 16, 1995Assignee: Schering CorporationInventors: John W. Clader, Thomas Fevig, Wayne Vaccaro, Joel G. Berger
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Patent number: 5414017Abstract: Compounds of the formula ##STR1## wherein m is zero or 1; n is zero, 1 or 2; p is zero or 1 to 6 provided that m and p are not both zero; R.sub.3 is hydrogen, acyl, or benzyl; and R.sub.1 is hydrogen, alkyl, phenyl, substituted phenyl, phenyl-alkylene, heterocyclic-alkylene, etc. These compounds are useful as cardiovascular agents.Type: GrantFiled: March 26, 1993Date of Patent: May 9, 1995Assignee: E. R. Squibb & Sons, Inc.Inventors: Norma G. Delaney, George C. Rovnyak, Melanie J. Loots
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Patent number: 5389680Abstract: Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops. Polar compounds, for example, 3,4,4-trifluoro-3-butene-1-amine or 3,4,4-trifluoro-3-butenoic acid, are particularly useful for systemic control of pests. Novel method and intermediates for the preparation of 3,4,4-trifluoro-3-butene-1-amine are also provided.Type: GrantFiled: October 18, 1993Date of Patent: February 14, 1995Assignee: Monsanto CompanyInventor: Peter G. Ruminski
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Patent number: 5368866Abstract: A deer repellent composition for the protection of vegetation includes an active ingredient comprising egg and a red hot sauce, composed of pepper, vinegar, garlic, salt and water; a carrier; and a diluent. The vegetation is protected by applying an effective amount of the composition thereto, preferably by spraying. The composition may include the aforementioned ingredients in the following percentages: about 3-7 percent eggs; about 6-19 percent red hot sauce; about 3-7 percent carrier; and about 68-91 percent diluent, the total composition equaling 100 percent by weight. A process for preparing the mixture is also enclosed.Type: GrantFiled: October 25, 1993Date of Patent: November 29, 1994Inventor: Athena P. Loucas
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Patent number: 5322862Abstract: The present invention provides a resin molding composition for preventing gnawing damage by the animal, a microcapsule filled with a capsaicine compound, and a process for producing the capsaicine compound and the microcapsule.Type: GrantFiled: August 17, 1992Date of Patent: June 21, 1994Assignee: Nippon Kayaku Kabushiki KaishaInventors: Mitsuo Kurata, Yasuhiro Ichikawa, Mika Toya, Iwao Takahashi, Yoshinobu Okui
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Patent number: 5321031Abstract: Amides of the formula ##STR1## wherein: R.sup.1 is A and R.sup.2 is B; R.sup.1 is B and R.sup.2 is A; or R.sup.1 and R.sup.2 are independently selected from the group B;A is phenyl, substituted phenyl, heteroaryl, or substituted heteroaryl;B is cycloalkyl, substituted cycloalkyl, heterocycloalkyl, or substituted heterocycloalkyl;R.sup.3 is an alkyl chain of 1 to 25 carbon atoms, branched or straight; an alkenyl chain of 2 to 25 carbon atoms, branched or straight; a substituted alkyl chain; a substituted alkenyl chain; an interrupted alkyl chain; an interrupted alkenyl chain; a substituted interrupted alkyl chain; or a substituted interrupted alkenyl chain;R.sup.4 is hydrogen, lower alkyl, phenyl, Q-substituted phenyl, heteroaryl or Q-substituted heteroaryl;R.sup.6 and R.sup.7 are both H, or R.sup.6 and R.sup.7 together represent =O;or a pharmaceutically acceptable salt thereof;useful as inhibitors of acyl-coenzyme A:cholesterol acyl transferase and therefore in the treatment of atherosclerosis are disclosed.Type: GrantFiled: September 23, 1992Date of Patent: June 14, 1994Assignee: Schering CorporationInventor: Sundeep Dugar
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Patent number: 5318960Abstract: Compositions for pain relieving non-steroidal anti-inflammatory drugs and/or medicaments such as ibuprofen, methotrexate, capsaicin, diphenhydramine, aspirin, methylnicotinate and other medicaments largely soluble in oil, alcohol, and/or water, are produced for transdermal delivery. The composition is manufactured by admixing an appropriate amount of oil surfactant with an appropriate amount of pharmaceutically approved co-solubilizer alcohol to establish a non aqueous phase. The oil surfactant may be a polyethoxylated oil such as castor oil. The co-solubilizer may be isopropyl alcohol or virtually any other alcohols except for methanol. Thereafter, an appropriate amount of distilled water is slowly added to the homogeneous or non-aqueous phase to further reduce viscosity. The final admixture is a clear, oil-continuous solution having a viscosity no greater than 850 centistokes as measured by the VST Hoppler method at 25 degrees Celsius.Type: GrantFiled: June 3, 1992Date of Patent: June 7, 1994Assignee: Frank ToppoInventor: Frank Toppo
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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: 5234946Abstract: The substituted alkylamine derivatives represented by formula (I) ##STR1## wherein R.sup.1 represents (a) substituted or unsubstituted C.sub.2-6 alkenyl group, (b) substituted or unsubstituted C.sub.3-6 cycloalkenyl group, (c) substituted or unsubstituted C.sub.2-6 alkynyl group, (d) substituted or unsubstituted aryl group, (e) substituted or unsubstituted heterocyclic group, (f) fused heterocyclic group which may be substituted, or (g) group represented by the formula Ru.sup.11 -Ar wherein R.sup.11 is a heterocyclic group and Ar is a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and which may be substituted; ##STR2## represents a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and may be substituted by R.sup.7,X and Y are linking groups,R.sup.2 is H or lower alkyl,R.sup.3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or lower cycloalkyl,R.sup.4 and R.sup.5 are independently hydrogen or halogen atoms,R.sup.Type: GrantFiled: August 30, 1991Date of Patent: August 10, 1993Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Hiroshi Takezawa, Masahiro Hayashi, Yoshikazu Iwasawa, Masaaki Hosoi, Yoshiaki Iida, Yoshimi Tsuchiya, Masahiro Horie, Toshio Kamei
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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: 5225447Abstract: The major component of the carbonate fraction of free acids extractable from alfalfa has shown excellent control of symptoms in patients with sickle cell disease. Its structure has been established by proton NMR spectrometry as being 16-hydroxy-9Z,12Z,14E-octadecatrienoic acid and closely related compounds, such as simple esters, amides, triglycerides, or other derivatives of the carboxylic acid function, and a method for its synthesis from linseed oil or methyl linolenate has been developed. The product from linseed oil, both in the form of the initially formed triglyceride and in the form of its free acid obtained by saponification, is useful for the treatment of sickle cell disease.Type: GrantFiled: February 14, 1992Date of Patent: July 6, 1993Assignee: Omex International, Inc.Inventor: Alfred J. Weinheimer
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Patent number: 5225429Abstract: Fluorinated arachidonic derivatives are 5-lipoxygenase inhibitors which have the useful pharmacologic activity as antiallergy and anti-inflammatory agents and are useful for treating, for example, asthma, anaphylaxis, allergy, rheumatoid arthritis, and psoriasis and cardiovascular diseases.Type: GrantFiled: June 24, 1991Date of Patent: July 6, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Jean-Bernard Ducep, Jean-Francois Nave, Detlef Jacobi
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Patent number: 5217708Abstract: The present invention provides a capsicum containing lachrymator. The lachrymator comprises a nonflammable carrier and capsicum. The nonflammable carrier comprises propylene glycol, ethyl alcohol and water. In one preferred embodiment the lachrymator comprises about 0.3 percent by weight capsicum, about 14.7 percent by weight propylene glycol, about 35 percent by weight ethyl alcohol and about 50 percent by weight water.Type: GrantFiled: February 5, 1992Date of Patent: June 8, 1993Assignee: Defense Technology Corporation of AmericaInventor: Barry D. Pinkney
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Patent number: 5178879Abstract: Clear, water-washable, non-greasy gels useful for topical pain relief contain capsaicin, water, alcohol and a carboxypoly-methylene emulsifier. A method of preparing the gels is disclosed.Type: GrantFiled: April 17, 1992Date of Patent: January 12, 1993Inventors: Michael Adekunle, James J. Flowers
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Patent number: 5151447Abstract: S-substituted beta-thioacrylamide compounds have been discovered to be useful as biocides and fungicides. Compositions comprising the compound and isothiazolin-3-ones and/or carriers, methods of preparation of the compounds and methods of using the compounds and compositions are also disclosed.Type: GrantFiled: June 5, 1990Date of Patent: September 29, 1992Assignee: Rohm and Haas CompanyInventor: David R. Amick
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Patent number: 5149709Abstract: Amides of the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently heteroaryl, X-substituted heteroaryl, X-substituted phenyl, N-substituted triazinyl or N-substituted imidazolyl;and in addition, one of R.sub.1 and R.sub.2 can be as defined above and the other can be phenyl;R.sub.3 is an alkyl chain of 2 to 25 carbon atoms, saturated or unsaturated; an alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl; an alkyl chain as defined interrupted by one or more groups independently selected from the group consisting of --O--, --S--, --SO--, --SO.sub.2 --, --NH--, --N(lower alkyl)--, --C(O)--, phenylene, X-substituted phenylene, heteroarylene and X-substituted heteroarylene; or an interrupted alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl;R.sub.Type: GrantFiled: July 3, 1990Date of Patent: September 22, 1992Assignee: Schering CorporationInventors: John Clader, Sundeep Dugar, Timothy Kogan, Bradley Tait, Wayne Vaccaro
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Patent number: 5145861Abstract: Fluorinated arachidonic derivatives are 5-lipoxygenase inhibitors which have the useful pharmacologic activity as antiallergy and anti-imflammatory agents and are useful for treating, for example, asthma, anaphylaxis, allergy, rheumatoid arthritis, and psoriasis.Type: GrantFiled: August 5, 1991Date of Patent: September 8, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Jean B. Ducep, Jean-Francois Nave
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Patent number: 5134166Abstract: Compositions and methods for treating the symptoms of certain allergy-related conditions using capsaicin in solution or suspension combined with a selected local anesthetic, topical steroid or antihistamine. The same methods and compositions may be used to treat headaches.Type: GrantFiled: October 9, 1990Date of Patent: July 28, 1992Assignee: GenDerm CorporationInventor: Joel E. Bernstein
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Patent number: 5118681Abstract: S-beta-dicarbonyl substituted beta-thioacrylamide compounds have been discovered to be useful as biocides and fungicides. Compositions comprising the compound and isothiazolin-3-ones and/or carries, methods of preparation of the compounds and methods of using the compounds and compositions are also disclosed.Type: GrantFiled: July 28, 1989Date of Patent: June 2, 1992Assignee: Rohm and Haas CompanyInventors: David R. Amick, Katherine E. Flynn, Cherylann Schieber
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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: 5063060Abstract: The invention relates to a method of treating painful, inflammatory or allergic disorders comprising treatment with an effective amount of a composition comprising cis-8-methyl-N-vanillyl-6-nonenamide. The invention also relates to compositions for use in the inventive method.Type: GrantFiled: December 19, 1989Date of Patent: November 5, 1991Assignee: Cisco Limited PartnershipInventor: Joel E. Bernstein
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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: 5023275Abstract: S-substituted beta-thioacrylamide compounds have been discovered to be useful as biocides and fungicides. Compositions comprising the compound and isothiazolin-3-ones and/or carriers, methods of preparation of the compounds and methods of using the compounds and compositions are also disclosed.Type: GrantFiled: June 5, 1990Date of Patent: June 11, 1991Assignee: Rohm and Haas CompanyInventor: David R. Amick
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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: 5008289Abstract: Compositions and methods for treating the symptoms of certain allergy-related conditions using capsaicin in solution or suspension combined with a selected local anesthetic, topical steroid or antihistamine. The same methods and compositions may be used to treat headaches.Type: GrantFiled: December 2, 1988Date of Patent: April 16, 1991Assignee: GalenPharma, Inc.Inventor: Joel E. Bernstein
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Patent number: 4997853Abstract: A method and composition for treating superficial pain syndromes incorporates capsaicin in a therapeutically effective amount into a pharmaceutically acceptable carrier and adding to this composition a local anesthetic such as lidocaine or benzocaine. The composition containing the anesthetic is then applied to the site of the pain. A variation on the treatment includes initial treatment with the composition containing the local anesthetic until the patient has become desenstitized to the presence of capsaicin and subsequent treatment with a composition ommitting the local anesthetic.Type: GrantFiled: March 28, 1990Date of Patent: March 5, 1991Assignee: Galenpharma, Inc.Inventor: Joel E. Bernstein