Polycyclo Ring System Patents (Class 514/765)
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Patent number: 5591715Abstract: The present invention comprises methods and compositions for reducing or eliminating multidrug resistance in cancers or certain infections by drug resistant microorganisms in patients. According to the method and composition of the present invention, a non-ionic amphipathic diester of fatty acids or a reverse poloxmer is administered to a patient in which a cancer or microorganism exhibits multidrug resistance to the chemotherapeutic agent. The method and composition of the present invention may be employed with particular efficacy where multidrug resistance to any chemotherapeutic agent has been conferred upon a cancer.Type: GrantFiled: June 7, 1995Date of Patent: January 7, 1997Assignee: Rush Presbyterian-St. Luke's Medical CenterInventors: John S. Coon, Mannarsamy Balasubramanian, R. Martin Emanuele, Himanshu Shah
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Patent number: 5576330Abstract: The new use of a compound of formula (I) ##STR1## wherein Y is a bicyclic ring selected from naphthalene, tetralin, quinoline, isoquinoline and indole;n is zero or an integer of 1 to 3;R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl;R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, cyano, carboxy, nitro, or NHR, wherein R is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkanoyloxy, carboxy, nitro or NHR, wherein R is as defined above;R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or halogen; or a pharmaceutically acceptable salt thereof;and wherein when Y is naphthalene then n is zero or an integer of 1 to 3, whereas when Y is tetralin, quinoline, isoquinoline or indole then n is zero, 1 or 2; and wherein when the bicyclic ring Y is naphthalene, quinoline, isoquinoline or indole, then each of the substituents OR.sub.1, R.sub.Type: GrantFiled: December 12, 1994Date of Patent: November 19, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Antonio Longo, Maria G. Brasca, Fabrizio Orzi, Angelo Crugnola, Dario Ballinari, Mariangela Mariani
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Patent number: 5574026Abstract: The invention relates to a method for inhibiting angiogenesis and proliferation of endothelial cells by administering an inhibitory amount of a 7-halogen-9-[hydrogen or [(substituted glycyl)amido]]-6-demethyl-6-deoxytetracycline of Formula I: ##STR1## wherein X and W are as defined in the specification. The invention also relates to a method for inhibiting proliferation of tumor cells and tumor growth by administering an inhibitory amount of a compound of Formula I in combination with a chemotherapeutic agent or radiation therapy. The invention also relates to compositions containing an effective inhibitory amount of a compound of Formula I in a pharmaceutically acceptable carrier.Type: GrantFiled: December 13, 1994Date of Patent: November 12, 1996Assignee: American Cyanamid CompanyInventors: Joseph M. Backer, Peter Bohlen, Phaik-Eng Sum
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Patent number: 5550145Abstract: An antimicrobial composition comprising an antimicrobially effective amount of a combination of: A) a monoglyceride of lauric acid, a monoglyceride of monomyristic acid or a mixture of these monoglycerides, and B) at least one chemical substance selected from the following groups: i) local anesthetics of the amide type; ii) carbamide, iii) antibacterial substances in the form of steroid antibiotics, imidazole derivatives or nitroimidazole derivatives, and iv) diols with 3-6 carbon atoms, and C) optionally, a conventional physiologically acceptable carrier and/or physiologically acceptable additives. A process for the preparation of this composition by heating (A) to the transition temperature of the lipid, adding (B), and optionally (C), and cooling the mixture to form a solid lipid crystal composition. Use of the composition for the preparation of a dermatological preparation for combatting bacteria and fungi or as a preservative additive in a cosmetic product, a food product, or a medical product.Type: GrantFiled: September 27, 1994Date of Patent: August 27, 1996Assignee: Bioglan ABInventors: Karin Olund, Lena-Karin L utz, Rickard Bryland, .ANG.ke Lindahl
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Patent number: 5455265Abstract: Process of treatment of mammals, including humans to treat diseases or conditions of the type which are normally treated with retinoid-like compounds is disclosed, with pharmaceutical compositions containing an active compound which is a selective agonist of the RXR retinoid receptor sites in preference to the RAR retinoid receptor sites. A compound is defined to be a selective agonist of the RXR receptor site if the compound is at least approximately ten times more effective as an agonist in the RXR receptor sites than in the RAR receptor sites.Type: GrantFiled: February 11, 1993Date of Patent: October 3, 1995Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
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Patent number: 5290546Abstract: The present invention provides a cordless thermal vaporizer of the liquid type wherein the body of the vaporizer has a heater for heating a wick for drawing up a chemical solution from a bottle, and a socket disposed under the heater and removably fittable in the form of a cap to the bottle for attachment thereto. The body is reduced in weight and thereby made attachable to an electric outlet with stability. The solution bottle can be attached directly to the socket of the body and is therefore easy to replace.Type: GrantFiled: September 9, 1992Date of Patent: March 1, 1994Assignee: Earth Chemical Co., Ltd.Inventors: Takahiro Hasegawa, Takanobu Kashihara, Junichiro Mesaki, Akira Nishimura
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Patent number: 5118676Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals and into the blood stream in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer being a carboxylic acid derivative or a salt thereof represented in one embodiment by the general formula ##STR1## wherein W represents oxygen, sulfur, or two hydrogen radicals; wherein Z represents oxygen, sulfur, or --CH.sub.2 --;wherein R represents alkyl optionally substituted with one to three double or triple bonds, --SR'", --OR'", --NHR'", --CH.sub.3, or COOR.sub.1, and wherein R.sub.1 represents hydrogen or lower alkyl;wherein R'" represents alkyl, alkylthioalkyl, alkoxyalkyl, substituted aminoalkyl, optionally substituted with a phenyl, benzoyl or heterocyclic group;wherein R' represents hydrogen, alkyl, alkoxy, acyloxy, alkylthio, hydroxy, --(CH.sub.2).sub.Type: GrantFiled: November 13, 1990Date of Patent: June 2, 1992Assignee: Whitby Research, Inc.Inventors: Gevork Minaskanian, James V. Peck
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Patent number: 5104900Abstract: A new use for naphthalene comprising a snake repellant in the form of granules comprising 8% naphthalene, 32% sulfur and 60% montmorillonite. The compound is spread in a strip across an area where snakes are to be repelled and is effective against venomous and non-venomous varieties.Type: GrantFiled: February 28, 1990Date of Patent: April 14, 1992Inventor: James B. Tennyson
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Patent number: 5063059Abstract: Microencapsulated pyrethroidal cockroach-controlling composition is provided, which has an excellent residual effect. The composition comprises phenylxylylethane and a pyrethroidal compound and is encapsulated in microcapsules formed of a polyurethane wall which have an average particle diameter of not more than 80 .mu.m, a wall thickness of not more than 0.3 .mu.m, and a value of the average particle diameter/wall thickness of 100-400.Type: GrantFiled: November 15, 1990Date of Patent: November 5, 1991Assignee: Sumitomo Chemical Co., Ltd.Inventors: Toshiro Ohtsubo, Shigenori Tsuda, Hitoshi Kawada, Goro Shinjo, Kozo Tsuji
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Patent number: 5053547Abstract: A compound of formula (I) ##STR1## its isomers and its salts in which --R.sub.1, R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, halogen, C.sub.1 -C.sub.8 -acyloxy or hydroxyl;--R' is hydrogen or C.sub.1 -C.sub.6 -alkyl;--R" is either a polyene chain or a benzene ring are useful in cosmetics and in the treatment of various dermatological and other complaints.Type: GrantFiled: November 14, 1989Date of Patent: October 1, 1991Assignee: L'OrealInventors: Gerard Lang, Jean Maignan, Serge Restle, Braham Shroot
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Patent number: 4986988Abstract: The Indian Ocean sea hare Dolabella auricularia has been found to contain a new cell growth inhibitory and antineoplastic (P388 leukemia) cyclodepsipeptide designated dolastatin 13.sup.(1) and a companion substance dehydrodolastatin 13.sup.(2). A series of high field (400 MHz) 2D-NMR experiments including sequential analyses by HMBC and NOE techniques and tandem mass spectrometry provided structural determinations. Dolastatin 13 and dehydrodolastatin 13 represent a new class of cyclodepsipeptides. Pharmaceutical preparations and therapeutic regimens employing these new cytostatic depsipeptides are disclosed.Type: GrantFiled: May 18, 1989Date of Patent: January 22, 1991Assignee: Arizona Board of RegentsInventors: George R. Pettit, Yoshiaki Kamano
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Patent number: 4892889Abstract: A process for making a directly-compressible vitamin powder utilizes a conventional spray-dryer. The resulting powder is comprised of a fat-soluble vitamin, a water-soluble carbohydrate, and a gelatin having a bloom number between 30 and 300.Type: GrantFiled: October 2, 1987Date of Patent: January 9, 1990Assignee: BASF CorporationInventors: Paula S. Kirk, Dale R. Olson
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Patent number: 4863969Abstract: 1,2,3,4-Tetrahydro-1,1,4,4-tetramethyl-6-(.alpha.-methylstyryl)naphthalene possesses antihyperplastic, antimetaplastic, antineoplastic tumor-preventative and tumor-therapeutic properties and can accordingly be used in the treatment of precancerous or premalignant lesions as well as in the treatment of malignant tumors of epithelial and mesenchymal nature.Type: GrantFiled: March 4, 1988Date of Patent: September 5, 1989Assignee: Hoffmann-La Roche Inc.Inventor: Werner Bollag
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Patent number: 4719238Abstract: 1,2,3,4-Tetrahydro-1,1,4,4-tetramethyl-6-(alpha-methylstyryl)naphthalene possesses antikeratinizing, antiinflammatory and immunomodulatory properties and can be used in the treatment or prevention of dermatoses which are accompanied by a pathological cornification as well as inflammatory, autoimmune, rheumatic and allergic illnesses.Type: GrantFiled: June 1, 1987Date of Patent: January 12, 1988Assignee: Hoffmann-La Roche Inc.Inventor: Werner Bollag
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Patent number: 4689350Abstract: 1,2,3,4-Tetrahydro-1,1,4,4-tetramethyl-6-(alpha-methylstyryl)naphthalene possesses antikeratinizing, antiinflammatory and immunomodulatory properties and can be used in the treatment or prevention of dermatoses which are accompanied by a pathological cornification as well as inflammatory, autoimmune, rheumatic and allergic illnesses.Type: GrantFiled: June 16, 1986Date of Patent: August 25, 1987Assignee: Hoffman-La Roche Inc.Inventor: Werner Bollag
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Patent number: 4668667Abstract: The present invention involves compounds of the class of acylphosphorotriamides and methods for altering the blood plasma lipid content of mammals which comprises systemically administering to mammals an effective but nontoxic amount of a composition comprising such compounds.Type: GrantFiled: August 1, 1985Date of Patent: May 26, 1987Assignee: Norwich Eaton Pharmaceuticals, Inc.Inventors: Thomas J. Moorehead, Allan V. Bayless
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Patent number: 4609677Abstract: A non-steroidal anti-inflammatory composition comprising a therapeutically effective amount of active anti-inflammatory agent selected from the group consisting of 1-phenyl-1 cyclohexene, 4-phenylcyclohexanone, and mixtures thereof. The active agent may be formulated in a pharmaceutically acceptable carrier. These compositions are useful in the treatment in mammals of inflammation and other related symptoms, including pain.Type: GrantFiled: November 7, 1985Date of Patent: September 2, 1986Assignee: Warner-Lambert CompanyInventor: Martin M. Rieger
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Patent number: 4588750Abstract: This invention is directed to methods for and compositions useful in reducing sebum secretion utilizing 1,2,3,4-tetrahydro-1,1,4,4-tetramethyl-6-[.alpha.-methylstyryl]naphthalene as an active ingredient.Type: GrantFiled: April 25, 1983Date of Patent: May 13, 1986Assignee: Hoffmann-La Roche Inc.Inventor: Alfred Boris
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Patent number: 4581380Abstract: New 2,6-disubstituted derivatives of naphthalene have the formula ##STR1## wherein n is 1 or 2,R.sub.1 to R.sub.4 are hydrogen or CH.sub.3,R.sub.5 is ##STR2## (iv) 2-oxazolinyl, wherein m is 0 or 1, R.sub.6 is hydrogen, alkyl, OR.sub.9 wherein R.sub.9 is H, alkyl or ##STR3## wherein R.sub.10 is alkyl or aryl, or R.sub.6 is ##STR4## when m=1, r' and r" representing H, alkyl, mono- or poly-hydroxyalkyl, aryl or a heterocycle when taken together, R.sub.7 is H or alkyl, R.sub.8 is H, alkyl and the acetal of said compounds, and the salts of the compounds of formula I. These compounds are usefully employed in the pharmaceutical and cosmetic fields.Type: GrantFiled: November 28, 1984Date of Patent: April 8, 1986Assignee: Groupement Economique dite: Centre National de Recherches Dermatologiques C.I.R.D.Inventors: Braham Shroot, Jacques Eustache, Martine Bouclier
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Patent number: 4559328Abstract: A non-steroidal anti-inflammatory composition comprising an active anti-inflammatory agent having the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 is hydrogen, hydroxy, phenyl, methoxy, carboxylic acid, sulfhydryl or hydroxamic acid.The active agent is formulated with a pharmaceutically acceptable carrier for use in the treatment of pain, inflammation and other related symptoms on mammals. p-Hydroxydiphenyl, p-methoxyphenol, thiosalicylic acid, benzyl alcohol and salicylhydroxamic acid are preferred.Type: GrantFiled: June 21, 1984Date of Patent: December 17, 1985Assignee: Warner-Lambert CompanyInventors: Richard V. Smerbeck, Eugene P. Pittz