Carbon To Carbon Unsaturation In R Patents (Class 514/627)
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Patent number: 6028112Abstract: There is provided novel spirocyclopropyl fluorene derivatives having the general Formula I ##STR1## wherein R, R.sup.1 and X are as defined herein which are useful as melatonergic agents.Type: GrantFiled: July 31, 1998Date of Patent: February 22, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Karen L. Leboulluec, Katherine S. Takaki
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Patent number: 6011067Abstract: The present invention deals with the combination of several synergistic antioxidants including enzymatic co-factors as adjuncts to therapy of desquamating inflammatory disorders, such as psoriasis. These topical compositions are aimed to neutralize free radical species generated by such inflammatory conditions which are responsible for certain clinical signs and symptoms. As such, damage to skin causing destruction of elastin and collagen tissues is reduced. The present synergistic antioxidants may be combined with anti-inflammatories, including corticosteroids, anti-microbials, including zinc pyrithione, and other preparations useful in the therapy of desquamating disorders as psoriasis, seborrhoeic dermatitis and related skin and scalp conditions.Type: GrantFiled: June 11, 1999Date of Patent: January 4, 2000Assignee: Thione International, Inc.Inventor: Theodore Hersh
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Patent number: 6001375Abstract: The present invention discloses the topical application of ceramides. The present invention provides specific cosmetic compositions comprising a ceramide and an agent to target said ceramide to the proper site of the skin. Specifically it is shown that the ceramide-containing compositions have a high capacity for recovering diminished water-retaining properties of preheated or damaged skin. Furthermore, the ceramide-containing compositions are shown to protect the skin again irritation.Type: GrantFiled: October 16, 1996Date of Patent: December 14, 1999Assignee: Gist-brocades, B.V.Inventors: Johannes Wilhelmus Jacobus Lambers, Ernst-Ludwig Roehl
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Patent number: 5994407Abstract: The present invention refers to a procedure to prepare a Capsaicin solution in various steps, preferentially three; the first steps consists in the preparation of the solution "A" by mixing 80 milliliters of saline solution, 10 milliliters of polyoxyenthylenesorbitan monooleate and 10 milliliters of paraffin oil. Later on, the second stage is the preparation of solution "B" by mixing 3 milligrams of 8-Methyl-N-Vanillyl-6-Nonenamide in 100 milliliters of the solution "A". Finally the third stage includes the preparation of solution "C" mixing 10 milliliters of solution "B" in 90 milliliters of solution "A" in order to obtain a 10-micromolar concentration of 8-Methyl-N-Vanillyl-6-Nonenamide.Type: GrantFiled: June 16, 1999Date of Patent: November 30, 1999Inventor: Carlos Cuilty-Siller
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Patent number: 5985860Abstract: Compositions for pain relieving non-steroidal anti-inflammatory drugs and/or medicaments such as ibuprofen, methotrexate, capsaicin, diphenhydramine, aspirin, methyl-nicotinate 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 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 7, 1994Date of Patent: November 16, 1999Inventor: Frank Toppo
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Patent number: 5977180Abstract: Anandamide analogues useful for the treatment of intraocular hypertension, as well as ophthalmic compositions comprising the same and a cyclodextrin, and methods of use of these compounds to treat intraocular hypertension.Type: GrantFiled: January 10, 1997Date of Patent: November 2, 1999Inventors: David W. Pate, Tomi Jarvinen, Kristina Jarvinen, Arto Urtti
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Patent number: 5972928Abstract: The present invention includes methods for treatment and prophylaxis of diseases, post-surgical disorders and bacterial infections associated with lactosylceramide. The methods generally provide for administration for a mammal, particularly a human, of a therapeutically effective amount of a compound that inhibits UDPGal:GlcCer.beta.1->4 galactosylceramide (GalT-2). In vitro and in vivo assays for detecting compounds with therapeutic capacity to modulate GalT-2 are also provided.Type: GrantFiled: December 24, 1997Date of Patent: October 26, 1999Assignee: Johns Hopkins UniversityInventor: Subroto Chatterjee
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Patent number: 5968916Abstract: Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops. Polar compounds are particularly useful for systemic control of pests.Type: GrantFiled: January 12, 1998Date of Patent: October 19, 1999Assignee: Monsanto CompanyInventors: Dennis Paul Phillion, Peter Gerrard Ruminski, Gopichand Yalamanchili
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Patent number: 5962532Abstract: Methods and compositions for treating pain at a specific site with an effective concentration of capsaicin or analogues thereof are described. The methods involve providing anesthesia to the site where the capsaicin or analogues thereof is to be administered, and then administering an effective concentration of capsaicin to the joint. The anesthesia can be provided directly to the site, or at remote site that causes anesthesia at the site where the capsaicin is to be administered. For example, epidural regional anesthesia can be provided to patients to which the capsaicin is to be administered at a site located from the waist down. By pretreating the site with the anesthetic, a significantly higher concentration of capsaicin can be used. Effective concentrations of capsaicin or analogues thereof range from between 0.01 and 10% by weight, preferably between 1 and 7.5% by weight, and more preferably, about 5% by weight.Type: GrantFiled: March 12, 1998Date of Patent: October 5, 1999Inventors: James N. Campbell, Marco Pappagallo, Richard A. Meyer
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Patent number: 5958439Abstract: A composition containing, as active ingredient, one or more water soluble plant protection active materials and further containing an effective amount of one or more polyalkoxylated amidoamines of average formula (1) or (2), wherein all R.sup.1, which are the same or different, are a straight or branched C.sub.2 -C.sub.22 alkyl or alkenyl hydrocarbon group, cycloalkyl or alkylaryl, all R.sup.2, which are the same or different, are hydrogen or a C.sub.1 -C.sub.4 alkyl radical, and p, q, r, s and t, which are the same or different, are integers that can be zero, such that p+q is 1-20 and r+s+t is 1-20. Applications of said composition as a herbicide, a fungicide or a fertilizer are also described.Type: GrantFiled: January 30, 1998Date of Patent: September 28, 1999Assignee: Rhodia ChimieInventor: Isabelle Gubelmann
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Patent number: 5955092Abstract: N-substituted fatty acid amides which sufficiently inhibit LRAT or ARAT catalyzed esterification of retinol into inactive retinyl esters, have the same effect on keratinocytes as retinoic acid. Thus, effects of the retinol or retinyl esters in combination with N-substituted fatty acid amides are analogous to treatment with retinoic acid.Type: GrantFiled: September 27, 1996Date of Patent: September 21, 1999Assignee: Elizabeth Arden Co., Division of Conopco, Inc.Inventors: Stewart Paton Granger, Anthony Vincent Rawlings, Ian Richard Scott
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Patent number: 5948418Abstract: Novel sulfhydryl group-containing amides and disulfide group-containing bis-amides useful for treating or preventing an abnormal biological condition or a disease, and/or improving the texture or appearance of the skin, as well as compositions containing amides and bis-amides and methods for their use are described. Such types of abnormal biological conditions or diseases include skin atrophy, i.e., the thinning and/or general degradation of the dermis often characterized by a decrease in collagen and/or elastin as well as decreased number, size and doubling potential of fibroblast cells, and other maladies including, but are not limited to dry skin, severe dry skin, dandruff, acne, keratoses, psoriasis, eczema, skin flakiness, pruritus, age spots, lentigines, melasmas, wrinkles, warts, blemished skin, hyperpigmented skin, hyperkeratotic skin, inflammatory dermatoses, age-related skin changes and skin in need of cleansers.Type: GrantFiled: July 30, 1997Date of Patent: September 7, 1999Assignee: Estee Lauder, Inc.Inventors: Daniel H. Maes, Jules Zecchino, Althea Knight
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Patent number: 5945091Abstract: A method of using compounds of formula I ##STR1## in which the C.dbd.C double bond is present in E and/or Z configuration and the variables have the following meanings:R.sup.1 denotes COOR.sup.5, COR.sup.5, CONR.sup.5 R.sup.6, CN, O.dbd.S(--R.sup.5).dbd.O, O.dbd.S(--OR.sup.5).dbd.O, R.sup.7 O--P(--OR.sup.8).dbd.O;R.sup.2 denotes COOR.sup.6, COR.sup.6, CONR.sup.5 R.sup.6, CN, O.dbd.S(--R.sup.6).dbd.O, O.dbd.S(--OR.sup.6).dbd.O, R.sup.7 O--P(--OR.sup.8).dbd.O;R.sup.3 denotes hydrogen, an optionally substituted aliphatic, cycloaliphatic, araliphatic or aromatic radical having in each case up to 18 carbon atoms;R.sup.4 denotes an optionally substituted aromatic or heteroaromatic radical containing from 5 to 12 ring atoms;R.sup.5 toR.sup.8 independently denote hydrogen, an open-chain or branched-chain aliphatic, araliphatic, cycloaliphatic or optionally substituted aromatic radical containing in each case up to 18 carbon atoms,where the variables R.sup.3 to R.sup.Type: GrantFiled: November 18, 1997Date of Patent: August 31, 1999Assignee: BASF AktiengesellschaftInventors: Thorsten Habeck, Alexander Aumuller, Volker Schehlmann, Horst Westenfelder, Thomas Wunsch
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Patent number: 5932233Abstract: Described is a cosmetic composition comprising (A) an amide compound having a melting point of 0 to 50.degree. C. and (B) a hydrophilic surfactant. The cosmetic composition according to the present invention can enhance the water-retaining ability of the stratum corneum and is excellent in skin-roughness lessening effects.Type: GrantFiled: October 14, 1997Date of Patent: August 3, 1999Assignee: Kao CorporationInventors: Tomoyuki Yamamoto, Yumiko Sato, Seiji Yamasaki, Atsushi Nakajima, Masataka Fukuda
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Patent number: 5925365Abstract: Described is a water-in-oil type cosmetic emulsion comprising (A) an amide compound having a melting point of 0 to 50.degree. C. and (B) a nonionic surfactant having an HLB smaller than 8. The cosmetic composition according to the present invention has excellent stability, can enhance the water-retaining ability of the stratum corneum and has excellent skin-roughness lessening effects.Type: GrantFiled: October 14, 1997Date of Patent: July 20, 1999Assignee: Kao CorporationInventor: Tomoyuki Yamamoto
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Patent number: 5925681Abstract: Concentrated aqueous liquid disinfectant compositions which exhibit a blooming effect when diluted in a larger volume of water are provided. The concentrate compositions include non-phenolic constituents to provide a disinfecting effect, and are non pine-oil containing. Working strength dilutions of the concentrated aqueous liquid disinfectant compositions are effective against gram positive type pathogenic bacteria such as Staphylococcus aureus, as well as gram negative type pathogenic bacteria such as Salmonella choleraesuis.Type: GrantFiled: October 7, 1997Date of Patent: July 20, 1999Assignee: Reckitt & Colman Inc.Inventors: Michael George Crisanti, Dennis Thomas Smialowicz
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Patent number: 5922771Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.Type: GrantFiled: August 19, 1996Date of Patent: July 13, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Osamu Uchikawa, Kohji Fukatsu, Masaomi Miyamoto
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Patent number: 5891846Abstract: A stable emulsion composition containing cyclosporin, a polyalkyl ester of polycarboxylic acid in the form of liquid at ordinary temperature, an oil component having an I.O.B. of 0 to 0.25 in the form of a liquid at ordinary temperature, and a surfactant.Type: GrantFiled: February 19, 1998Date of Patent: April 6, 1999Assignee: Shiseido Company, Ltd.Inventors: Masami Ishida, Takashi Suzuki
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Patent number: 5869533Abstract: A delivery system for applying a formula containing capsaicin together with another ingredient to neutralize the discomfort resulting from the application of capsaicin to the skin which involves the topical application of capsaicin by use of patches, use of second skin, use of sprays and includes a unique method for applying the formulation using laser on the epidermis.Type: GrantFiled: June 30, 1998Date of Patent: February 9, 1999Inventor: Stephen D. Holt
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Patent number: 5869532Abstract: Taurine derivatives represented by the following formula (1) and cleanser compositions containing the same: ##STR1## wherein R is a linear or branched alkyl or alkenyl group having 5 to 21 carbon atoms, and M.sub.1 and M.sub.2 are the same or different from each other and each independently is a hydrogen atom, an alkali metal atom, 1/2 (an alkaline earth metal atom), an ammonium group, etc.,are excellent in foaming, detergency, comfort in use, rinsability, safety and biodegradability and are employed as a cleanser for the hair and body or tableware.Type: GrantFiled: August 19, 1996Date of Patent: February 9, 1999Assignee: Kao CorporationInventors: Hiromoto Mizushima, Masakatsu Takahashi, Hiroe Tanahashi, Takashi Matsuo
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Patent number: 5859017Abstract: In a method for treating or preventing allergy or allergic disorders an effective amount of a compound that inhibits intracellular generation of phosphatidic acid and diacylglycerol is administered. The intracellular generation of phosphatidic acid and diacylglycerol results from allergen presentation or mast cell/basophil activation.Type: GrantFiled: April 1, 1994Date of Patent: January 12, 1999Assignee: Cell Therapeutics, Inc.Inventors: Elisa Eiseman, Emer Clarke, Jack W. Singer, Stuart L. Bursten
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Patent number: 5856537Abstract: Inhibitors of oleamide hydrolase, responsible for the hydrolysis of an endogenous sleep-inducing lipid (1, cis-9-octadecenamide) were designed and synthesized. The most potent inhibitors possess an electrophilic carbonyl group capable of reversibly forming a (thio) hemiacetal or (thio) hemiketal to mimic the transition state of a serine or cysteine protease catalyzed reaction. In particular, the tight binding .alpha.-keto ethyl ester 8 (1.4 nM) and the trifluoromethyl ketone inhibitor 12 (1.2 nM) were found to have exceptional inhibitory activity. In addition to the inhibitory activity, some of the inhibitors displayed agonist activity which resulted in the induction of sleep in laboratory animals.Type: GrantFiled: June 26, 1996Date of Patent: January 5, 1999Assignee: The Scripps Research InstituteInventors: Richard A. Lerner, Chi-Huey Wong, Dale L. Boger, Steven J. Henriksen
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Patent number: 5856361Abstract: A composition containing capsaicin together with another ingredient to neutralize the discomfort resulting from the application of capsaicin to the skin can be used to treat many types of discomforts, including musculo-skeletal pain, neuralgia and neurpathies, without the discomfort normally associated with the topical application of capsaicin.Type: GrantFiled: June 6, 1997Date of Patent: January 5, 1999Assignee: Medical Merchandising, Inc.Inventors: Stephen D. Holt, Timothy R. Laughlin
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Patent number: 5840755Abstract: A composition for topical therapy of headaches, which contains a topical carrier system for intact mammalian skin of forehead or temples or both, which contains a therapeutically effective dose of a local anesthetic for delivery to a skin surface underneath the topical carrier system.Type: GrantFiled: July 17, 1996Date of Patent: November 24, 1998Assignee: American Pharmed Labs, Inc.Inventor: Rainer K. Liedtke
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Patent number: 5840762Abstract: The invention relates to the use of zucapsaicin (cis-8-methly-N-vanillly-6-nonenamide), the cis-isomer of capsaicin, to treat myocardial disorders, including the prevention, suppression or reversal of an abnormal cardiac rhythm, such as ventricular tachycardia. In vitro, zucapsaicin exhibits electrophysiologic properties distinct from capsaicin. In contrast to capsaicin, zucapsaicin significantly shortens the action potential duration at a dose of 10.sup.-5 M and has no effect on the amplitude of Phase 1 of the action potential in normal Purkinje cells. Zucapsaicin also prevents the induction of ventricular tachycardia of focal Purkinje origin when given intravenously after coronary occlusion in a dog model of acute myocardial infarction.Type: GrantFiled: January 12, 1996Date of Patent: November 24, 1998Assignee: GenDerm CorporationInventors: Joel E. Bernstein, Kenneth M. Verburg
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Patent number: 5834517Abstract: The present invention deals with a process for cleaning and conditioning hair and skin which comprises the contacting of hair or skin woth an effective concentration of certain novel meadowfoam derived sulfosuccinates. These materials are useful as cosmetic ingredients as additives to shampoo systems where outstanding liquidity, resistance to oxidation, and minimal odor variation are required.Type: GrantFiled: May 1, 1997Date of Patent: November 10, 1998Assignee: Fan Tech Ltd.Inventor: Anthony J. O'Lenick, Jr.
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Patent number: 5827886Abstract: A composition and method of using it for ameliorating inflammatory reactions and painful and other symptoms of the diseases of arthritis, lumbago, low back pain, myalgias and neuralgias. The composition includes reduced glutathione, a selenoamino acid and an anesthetic, such as capsaicin, in a suitable carrier for topical application.Type: GrantFiled: May 7, 1997Date of Patent: October 27, 1998Assignee: Thione International, Inc.Inventor: Theodore Hersh
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Patent number: 5821269Abstract: The present invention is directed to preparations of birdseed treated with capsaicin or capsaicin derivatives or analogs thereof in an amount sufficient to be unpalatable to animals having capsaicin sensitive receptors, and more specifically to mammals such as rodents. These "hot" compounds, extracts or whole plant material containing these compounds may be coated on, impregnated in or combined (e.g., mixed) with birdseed to repel troublesome mammals which recognize these compounds as "hot". These "hot" compounds, in contrast, will not repel birds because birds do not recognize these compounds as "hot" since they do not have capsaicin sensitive receptors. The invention is further directed to a method of selectively repelling animals having capsaicin sensitive receptors, which comprises feeding the treated birdseed of the invention to birds, in an amount effective for repelling animals having capsaicin sensitive receptors, thereby discouraging said animals from eating the treated birdseed.Type: GrantFiled: June 3, 1992Date of Patent: October 13, 1998Assignee: The United States of America as represented by the Department of Health and Human ServicesInventor: Peter M. Blumberg
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Patent number: 5814649Abstract: A pharmaceutical composition for prophylaxis or treatment of Type I allergic diseases which comprises as an active ingredient an anilide compound represented by the general formula (I) ##STR1## ?wherein R.sub.1 is a trifluoromethyl group, a halogen atom or a cyano group, R.sub.2 is a hydrogen atom or a straight or branched C.sub.1 -C.sub.4 alkyl group and R.sub.3 is a group of the formula (II) or (III) ##STR2## (wherein R.sub.4 is a straight or branched C.sub.1 -C.sub.4 alkyl group, a straight or branched C.sub.2 -C.sub.6 alkenyl group, a straight or branched C.sub.2 -C.sub.6 alkynyl group or a C.sub.2 -C.sub.6 cycloalkyl group) or a stereoisomer thereof or a physiologically acceptable salt thereof.The present composition remarkably inhibits the production of IgE, which is the direct cause of Type I allergic diseases, and it can radically prevent or cure Type I allergic diseases.Type: GrantFiled: June 6, 1997Date of Patent: September 29, 1998Assignee: Hoechst Pharmaceuticals & Chemicals K.K.Inventors: Yukio Amano, Yuko Mizushima, Kenji Ogata
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Patent number: 5801178Abstract: An aniline derivative of the formula (1) ##STR1## wherein R.sup.1 is an eicosapentaenoyl or docosahexaenoyl; R.sup.2 and R.sup.3 are each independently an alkyl or alkoxy having 1 to 6 carbon atoms, or a halogen atom; R.sup.4 is a hydrogen atom, an alkyl or alkoxy having 1 to 6 carbon atoms, or a halogen atom; and A is a single bond, --C(.dbd.O)NH--(CH.sub.2).sub.n --NH-- wherein n is 2 or 3, or a bivalent group of the following formula ##STR2## wherein m and p are each independently 0 or 1. The aniline derivative of the present invention has high inhibitory activity against and high selectivity for ACAT derived from macrophage and is useful as an agent for the prophylaxis and treatment of arteriosclerosis.Type: GrantFiled: February 7, 1996Date of Patent: September 1, 1998Assignees: Nippon Shoji Kaish Ltd., Sagami Chemical ResearchInventors: Kazunaga Yazawa, Kazuo Watanabe, Yasuharu Ijuin, Mayumi Shikano, Yasuji Soda, Tetsuya Kosaka, Naoto Matsuyama, Koji Mizuno
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Patent number: 5783604Abstract: Germicidal compositions containing iodine compounds with formulae I and II, where n is a whole number between 8 and 18. These compositions may include other chemical compounds which have a sterilizing and disinfecting function and which synergize and improve the activity of said compounds I and II. These germicidal compositions can be used, for example, for preventing infections in hospitals as well as in the food canning, pharmaceutical and other related industries.Type: GrantFiled: December 10, 1996Date of Patent: July 21, 1998Inventor: Maria Rosalia Garcia Nunez
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Patent number: 5780512Abstract: The invention relates to a compounds selected from these of formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and A are as defined in the description, and a medicinal product containing the same useful for treating a melatoninergic disorder.Type: GrantFiled: March 26, 1997Date of Patent: July 14, 1998Assignee: Adir et CompagnieInventors: Daniel Lesieur, Eric Fourmaintraux, Patrick Depreux, Philippe Delagrange, Pierre Renard, Beatrice Guardiola-Lemaitre
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Patent number: 5780505Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.7 and R.sub.8 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a phenyl group with either two or three substituents of the following formula: ##STR2## wherein the positions of substitution are R.sub.2,R.sub.3 -, R.sub.2,R.sub.4 -, R.sub.2,R.sub.5 -, R.sub.2,R.sub.6 -, R.sub.3,R.sub.4 -, R.sub.3,R.sub.5 -, and R.sub.2,R.sub.4,R.sub.6 - and R.sub.2 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.3 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.4 is methyl, fluoro, bromo, methoxy or cyano; R.sub.5 is methyl, fluoro, chloro, methoxy, cyano or trifluoromethyl; R.sub.Type: GrantFiled: July 7, 1997Date of Patent: July 14, 1998Assignee: American Home Products CorporationInventors: Madelene M. Antane, David R. Herbst, Geraldine R. McFarlane, Eric G. Gundersen, Bradford H. Hirth, Dominick A. Quagliato, Russell F. Graceffa, John A. Butera
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Patent number: 5762963Abstract: Methods and compositions are provided for the oral delivery of temporally increasing concentrations of capsaicin, its derivatives, and analogs (collectively, "capsaicinoids"), to provide oral or pharyngeal analgesia while minimizing sensations of nausea and burning associated with the oral administration of capsaicinoids. The methods and compositions described herein soothe and relieve oral or pharynx pain. In one embodiment, one or more capsaicinoids are dispersed within a lollipop, with successively decreasing concentrations of capsaicin from the center out to the periphery, and administered to a patient in need of amelioration of oral pain. Alternatively, the capsaicinoid can be dispersed, with decreasing concentrations from the center to the periphery, in a tablet, caplet, lozenge, troche, pill, candy, or similar formulation.Type: GrantFiled: June 7, 1995Date of Patent: June 9, 1998Assignee: Emory UniversityInventor: Michael G. Byas-Smith
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Patent number: 5763481Abstract: 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: July 10, 1996Date of Patent: June 9, 1998Assignee: Novartis CorproationInventors: Peter Maienfisch, Manfred Boger, Thomas Pitterna, Henry Szczepanski
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Patent number: 5753709Abstract: Certain N-acyl 2-aryl cyclopropylmethylamine derivatives are useful as melatonergic agents.Type: GrantFiled: May 9, 1996Date of Patent: May 19, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Daniel J. Keavy, Michael F. Parker, Ronald J. Mattson, Graham Johnson
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Patent number: 5736578Abstract: Novel substituted fluorene compunds of Formula I are active as melatonergic agents: ##STR1## wherein: X=H, halogen, OH or OZ;Z=C.sub.1-6 alkyl; --(CH.sub.2).sub.m --CF.sub.3 (m=0-2); CD.sub.3 ; or ##STR2## n=1 or 2; and R=C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, halogen substituted C.sub.1-6 alkyl, or C.sub.1-6 alkoxy substituted C.sub.1-6 alkyl.Type: GrantFiled: May 10, 1996Date of Patent: April 7, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Brett T. Watson, Katherine S. Takaki, Joseph P. Yevich, James R. Epperson, George N. Karageorge, Karen L. Leboulluec
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Patent number: 5733935Abstract: A hydroxylamine derivatives of formula (I): ##STR1## wherein R represents ##STR2## in which R.sup.1 and R.sup.2 represents alkyl group, alkenyl group, alkynyl group, cycloalkyl group, haloalkyl group, haloalkynyl group, alkoxy - alkyl group, phenoxy - alkyl group, alkylthio - alkyl group, alkylsulfonyl - alkyl group, alkylamino - alkyl group, phenyl group, benzyl group, phenethyl group, cinnamyl group, pyridyl group, furyl group, thienyl group, X represents CO.sub.2, CO or SO.sub.2, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent a hydrogen atom or a lower alkyl group, and n represents 0 or 1, and fungicides contain said compound as an active ingredient.The compounds of the present invention have excellent effects for controlling wood-rot fungi, plant diseases and fungi of humans and animals, and are useful as industrial, agricultural and medical fungicides.Type: GrantFiled: June 17, 1996Date of Patent: March 31, 1998Assignee: Nihon Nohyaku Co., Ltd.Inventors: Nobuharu Andoh, Tsutomu Nishiguchi, Katsutoshi Endo
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Patent number: 5731352Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which A, R.sub.1, R'.sub.1, R.sub.2, R.sub.3 and n are as defined in the description, and medicinal product containing the same useful for treating a mammal afflicted with a disorder of the melatoninergic system.Type: GrantFiled: May 30, 1996Date of Patent: March 24, 1998Assignee: Adir Et CompagnieInventors: Daniel Lesieur, Veronique Leclerc, Patrick Depreux, Philippe Delagrange, Pierre Renard
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Patent number: 5728392Abstract: 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## wherein A is ##STR2## 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,are effective for combating the aging of skin and at the same time exhibit a reduced tendency to cause smarting, itching, or a sensation of tightness when applied to the skin.Type: GrantFiled: June 5, 1996Date of Patent: March 17, 1998Assignee: L'OrealInventors: Lucien Aubert, Francoise Gagnebien-Cabanne
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Patent number: 5712312Abstract: The invention relates to a compound selected from these of formula (I): ##STR1## in which R.sub.7, R.sub.8, Y, n and A are as defined in the description, and medicinal product containing the same useful for treating a disorder of the melatoninergic system.Type: GrantFiled: April 12, 1996Date of Patent: January 27, 1998Assignee: Adir et CompagnieInventors: Michel Langlois, Monique Mathe-Allainmat, Philippe Delagrange, Pierre Renard, Beatrice Guardiola
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Patent number: 5681859Abstract: A non-toxic, environmentally safe and easily employable insecticide and insect repellant is achieved by providing an aqueous composition incorporating ethanolamine based compounds, either independently or in combination with the ethanolamine based compounds being selected from both simple compounds and conjugated compounds. In one preferred embodiment, a highly effective composition is attained for safe, effective, direct topical application to humans and animals by employing between about 10% and 70% by volume of the entire composition of the ethanolamine-based compound. In alternate preferred embodiments, the insecticide is formulated for application to plants, trees, crops, and other vegetation to provide a composition which effectively controls bothersome insects, while being completely safe and non-injurious to the plant, tree, or crop, as well as to the flowers or fruit thereof.Type: GrantFiled: September 6, 1995Date of Patent: October 28, 1997Assignee: Lynn Sue JamesInventors: Lynn Sue James, Michael A. Siedman
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Patent number: 5679709Abstract: A pharmaceutical composition for use in the treatment of chronic Graft-versus-host diseases as well as autoimmune diseases, in particular for the treatment of systemic lupus erythematosus containing as an active ingredient at least one compound of the formula 1 or 2 ##STR1## the latter being present per se or in the form of a physiologically tolerable salt.The invention also relates to a dosage unit form of said pharmaceutical composition and a method of treating chronic Graft-versus host diseases as well as autoimmune diseases, in particular systemic lupus erythematosus.Type: GrantFiled: June 7, 1995Date of Patent: October 21, 1997Assignee: Hoechst AktiengesellschaftInventors: Robert R. Bartlett, Rudolf Schleyerbach, Friedrich-Johannes Kammerer
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Patent number: 5660830Abstract: Counter-irritants produce a slight irritation, as on an area of the skin, in order to relieve more serious inflammation elsewhere. Peppers, members of the Capsicum species, are a source of counter-irritants. The Scoville rating for a pepper provides a measure of the counter-irritant content of a given pepper. This invention provides for the solubilizing and recovery of the counter-irritants contained within peppers, having Scoville ratings of from 30,000 to 250,000, in the common capsaicin containing ethyl alcohol extract from the same specific peppers. The synergisitic pain relieving benefits of the counter-irritants in combination with the capsaicin provides superior pain relief for many hours after an application.Type: GrantFiled: September 14, 1994Date of Patent: August 26, 1997Inventor: Cleve Richard Anderson
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Patent number: 5631297Abstract: Anandamides useful for the treatment of intraocular hypertension, as well as ophthalmic compositions comprising the same and a cyclodextrin, and methods of use of these compounds to treat intraocular hypertension.Type: GrantFiled: July 11, 1994Date of Patent: May 20, 1997Inventors: David W. Pate, Tomi Jarvinen, Kristiina Jarvinen, Arto Urtti
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Patent number: 5621008Abstract: Disclosed is the novel use of N-acyl-N,N',N'-ethylenediaminetriacetic acids and N-acyl-N,N',N'-(ethylenedioxy) diethylenedinitrilotriacetic acids as active ingredients in preventative as well as therapeutic topical compositions to promote exfoliation and alleviate symptoms of skin conditions caused by abnormal keratinization.Type: GrantFiled: October 27, 1995Date of Patent: April 15, 1997Assignee: Avon Products, Inc.Inventor: Dmitri Ptchelintsev
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Patent number: 5614558Abstract: A non-toxic, environmentally safe and easily employable insecticide and insect repellant is achieved by providing an aqueous composition incorporating ethanolamine based compounds, either independently or in combination with the ethanolamine based compounds being selected from both simple compounds and conjugated compounds. In one preferred embodiment, a highly effective composition is attained for safe, effective, direct topical application to humans and animals by employing between about 10% and 70% by volume of the entire composition of the ethanolamine-based compound. In alternate preferred embodiments, the insecticide is formulated for application to plants, trees, crops, and other vegetation to provide a composition which effectively controls bothersome insects, while being completely safe and non-injurious to the plant, tree, or crop, as well as to the flowers or fruit thereof.Type: GrantFiled: June 2, 1995Date of Patent: March 25, 1997Assignee: Lynn Sue JamesInventors: Lynn S. James, Michael A. Siedman
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Patent number: 5612380Abstract: Sleep may be induced by administration of fatty acid primary amides, including cis-9,10-octadecenoamide. Furthermore, sleep deprivation may be assayed by analyzing cerebrospinal fluid with respect to the presence of fatty acid primary amides, including cis-9,10-octadecenoamide. The presence of cis-9,10-octadecenoamide in cerebrospinal fluid is correlated with comparative sleep deprivation.Type: GrantFiled: January 5, 1995Date of Patent: March 18, 1997Assignee: The Scripps Research InstituteInventors: Richard A. Lerner, Dale Boger, Ben Cravatt, Gary E. Siuzdak, Steven J. Henriksen
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Patent number: 5610194Abstract: Insect repellent compositions are provided comprising mixtures of:(a) from about 5 to about 95%, by weight, of an N-alkyl neoalkanamide having the formula: ##STR1## wherein R.sub.1 R.sub.2, and R.sub.3 are alkyl groups and the sum of the carbon atoms therein is from 6 to 12, and wherein R.sub.4 is either a hydrogen atom or an alkyl group having one to two carbon atoms, and wherein R.sub.5 is methyl, ethyl, or propyl; and(b) from about 5 to about 95%, by weight, of N,N-diethyl-meta-toluamide (DEET).Preferred repellent composition comprise mixtures of N-methyl neodecanamide (MNDA) and DEET which provide synergistic repellency effects against a variety of insects including cockroaches, silverfish, mosquitoes, flies and ants. The repellent compositions may be applied directly to surfaces to be treated or they may be incorporated in detergent compositions such as laundry detergents, floor and wall cleaners, rug cleaners and shampoos, hair shampoos and liquid and bar soaps.Type: GrantFiled: June 10, 1996Date of Patent: March 11, 1997Assignee: Colgate-Palmolive CompanyInventors: Thomas G. Polefka, Pallassana Ramachandran, Robert J. Steltenkamp, Thomas F. Connors, Kevin M. Kinscherf
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Patent number: 5607931Abstract: 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 .dbd.Type: GrantFiled: March 20, 1995Date of Patent: March 4, 1997Assignee: Schering CorporationInventor: Sundeep Dugar