Two Of The Cyclos Share At Least Three Ring Members (i.e., Bridged) Patents (Class 514/511)
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Patent number: 6458373Abstract: An emulsion of &agr;-tocopherol, stabilized by biocompatible surfactants, as a vehicle or carrier for therapeutic drugs, which is substantially ethanol free and which can be administered to animals or humans various routes is disclosed. Also included in the emulsion is PEGylated vitamin E. PEGylated &agr;-tocopherol includes polyethylene glycol subunits attached by a succinic acid diester at the ring hydroxyl of vitamin E and serves as a primary surfactant, stabilizer and a secondary solvent in emulsions of &agr;-tocopherol.Type: GrantFiled: January 5, 1998Date of Patent: October 1, 2002Assignee: Sonus Pharmaceuticals, Inc.Inventors: Karel J. Lambert, Panayiotis P. Constantinides, Steven C. Quay
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Patent number: 6444702Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.Type: GrantFiled: February 22, 2000Date of Patent: September 3, 2002Assignee: NeuroMolecular, Inc.Inventors: Yuqiang Wang, Wenqing Ye, James W. Larrick, Jonathan S. Stemler, Stuart A. Lipton
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Patent number: 6403571Abstract: The instant invention involves a combination therapy and pharmaceutical compositions comprised of a therapeutically effective amount of a cholesterol reducing agent such as an HMG-CoA reductase inhibitor in combination with a platelet aggregation inhibitor which is useful for inhibiting platelet aggregation, for inhibiting the formation of thrombotic occlusions, and for treating, preventing and reducing the risk of occurrence of cardiovascular and cerebrovascular events and related vaso-occlusive disorders.Type: GrantFiled: January 18, 2001Date of Patent: June 11, 2002Assignee: Merck & Co., Inc.Inventors: Robert J. Gould, Steven A. Nichtberger, Patricia A. Rhymer, Lars Olofsson
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Publication number: 20020019343Abstract: Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at least one HS—, HO— or H2N group and cytostatic compounds derived through maleinimide or N-hydroxysuccinimide ester compounds, such as doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxandrone, chloroambucil, melphalan, 5-fluorouracyl, 5′-desoxy-5-fluorouridine, thioguanine, methotrexate, paclitaxel, docetaxel, topotecan, 9-aminocamptothecin, etoposide, teniposide, mitopodoside, vinblastine, vincristine, vindesine, vinorelbine or a compound of general formula A, B, C or D, where n=0-6, X=—NH2, —OH, —COOH, —O—CO—R—COR*, —NH—CO—R—COR*, where R is an aliphatic carbon chain with 1-6 carbon atoms or a substituted or unsubstituted phenylene group and R* H, phenyl, alkyl with 1-6 carbon atoms.Type: ApplicationFiled: August 20, 2001Publication date: February 14, 2002Inventor: Felix Kratz
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Patent number: 6235706Abstract: The present invention involves a combination therapy of administering a cholesterol reducing agent, such as a 3-hydroxy-3-methylglutaryl coenzyme a (HMG-CoA) reductase inhibitor and a platelet aggregation inhibitor for treating, preventing or reducing the risk of developing cardiovascular and cerebrovascular events and disorders in a mammal.Type: GrantFiled: May 27, 1999Date of Patent: May 22, 2001Assignee: Merck & Co., Inc.Inventors: Robert J. Gould, Steven A. Nichtberger, Patricia A. Rhymer, Lars Olofsson
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Patent number: 6063797Abstract: The use of a combination of an alpha RAR receptor-specific agonist ligand and a gamma RAR receptor-specific antagonist ligand to reduce the rate of apoptosis is disclosed.Type: GrantFiled: July 15, 1998Date of Patent: May 16, 2000Assignee: C.I.R.D. GaldermaInventors: Laszlo Fesus, Zsuzsa Szondy, Uwe Reichert
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Patent number: 6057364Abstract: The invention relates to fluoro-substituted adamantane derivatives of the formula ##STR1## and to pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined herein. The invention also relates to methods of treating neurological disorders, such as memory loss and Parkinson's disease, and bacterial and viral infections, through administration of a therapeutically effective amount of a compound of formula I.Type: GrantFiled: April 9, 1998Date of Patent: May 2, 2000Assignee: Pfizer IncInventors: Vytautas John Jasys, Robert A. Volkmann
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Patent number: 6020370Abstract: Bridged cyclic amino acids of formula ##STR1## are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain and neuropathological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.Type: GrantFiled: May 19, 1998Date of Patent: February 1, 2000Assignee: Warner-Lambert CompanyInventors: David Christopher Horwell, Justin S. Bryans, Clare O. Kneen, Andrew I. Morrell, Giles S. Ratcliffe
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Patent number: 5935943Abstract: The presence of isobornyl thiocyanoethyl ether exerts a synergistic effect on the insecticidal activity against harmful wood eating insects of certain known insecticides selected from the group consisting of imidacloprid, phenyl pyrazole insecticides, pyrethroid insecticides and non-ester pyrethroid insecticides.Type: GrantFiled: September 9, 1997Date of Patent: August 10, 1999Assignee: Sankyo Company, LimitedInventors: Takehito Asai, Kenya Okumura, Toshiyasu Shizawa
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Patent number: 5854284Abstract: An insect repellent candle including a liquid containing DEET and a fragrance oil which acts as a carrier for dispersing DEET vapor into the atmosphere upon evaporation of the fragrance oil. The liquid system is contained within the wax of a candle which can be burned to emit DEET vapor into the atmosphere.Type: GrantFiled: December 4, 1997Date of Patent: December 29, 1998Inventor: Carl J. Abraham
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Patent number: 5738862Abstract: An insect repellent including a liquid system containing DEET and a fragrance oil which acts as a carrier for dispersing DEET vapor into the atmosphere upon evaporation of the fragrance oil. In one embodiment of the invention, the liquid system is contained within a solid thermoplastic system which can be formed as pellets for fabricating utilitarian products, e.g., wristbands and tablecloths. In another embodiment of the invention, the liquid system is contained within the wax of a candle which can be burned to emit DEET vapor into the atmosphere. In a third embodiment, the liquid system can be mixed with alcohol, with or without water, and dispersed by an air-wick to repel insects. In a fourth embodiment, towelettes can be soaked in the liquid system for later use as applicators of the liquid system to areas of the skin from which Deet vapor can be released into the atmosphere for effectively repelling insects from around the entire body.Type: GrantFiled: February 24, 1997Date of Patent: April 14, 1998Inventor: Carl J. Abraham
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Patent number: 5681846Abstract: The present invention is directed to improved pharmaceutical compositions employing paclitaxel that are formulated to increase stability and solubility. These improved formulations are useful in long-term, multi-day continuous infusion protocols, and have the advantage of reducing the number of infusion system breaks during the entire period of drug administration. Also disclosed are kits for use in preparing paclitaxel for long-term infusion and enhanced solubility.Type: GrantFiled: March 17, 1995Date of Patent: October 28, 1997Assignee: Board of Regents, The University of Texas SystemInventor: Lawrence A. Trissel
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Patent number: 5674893Abstract: A method is provided for preventing or reducing the risk of onset of a cardiovascular event by administering an HMG CoA reductase inhibitor such as pravastatin, to a patient which has one or more risk factors for a coronary and/or cerebrovascular event such as hypercholesterolemia.Type: GrantFiled: June 26, 1996Date of Patent: October 7, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Bruce D. Behounek, Mark E. McGovern, Adeoye Y. Olukotun
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Patent number: 5629045Abstract: Fouling of marine structures such as boats by shell bearing sea animals which attach themselves to such structures, such as barnacles, is inhibited by coatings containing lipid soluble, non-toxic, biodegradable substances which prevent the animals from sitting down on the structures. These substances attack the nervous system of the barnacle, neutralize the glue extruded by the barnacle, and otherwise prevent the barnacles from attaching themselves to surfaces immersed in the aqueous marine environment while being benign to the environment. A preferred inhibitor is pepper containing capsaicin. The inhibitor is incorporated into standard marine paints, impregnants, varnishes and the like.Type: GrantFiled: October 7, 1993Date of Patent: May 13, 1997Assignee: Richard L. VeechInventor: Richard L. Veech
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Patent number: 5616330Abstract: This invention is directed to a composition of a taxine in a stable oil-in-water emulsion for intravenous administration. The invention also relates to a method for incorporating a taxine into an oil and making a stable oil-in-water emulsion.The composition includes a taxine, an oil, water and a surfactant. In a preferred embodiment, the taxine is taxol, the oil is safflower oil and the surfactant is lecithin, The taxine is incorporated into the oil by dissolving the taxine in a solution of an oil and a taxine co-solvent, such as isopropanol, for example. The co-solvent then is removed to form a solution of the taxine in oil. This solution may be dispersed in water with a surfactant to form a stable oil-in-water emulsion for intravenous administration.Type: GrantFiled: July 19, 1994Date of Patent: April 1, 1997Assignee: HemaGen/PFCInventors: Robert J. Kaufman, Thomas J. Richard, Ralph W. Fuhrhop
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Patent number: 5616615Abstract: The present invention concerns enaminones having the formula: ##STR1## wherein R is COOCH.sub.3 ; R.sup.1 is CH.sub.3 ; R.sup.2 is H; and R.sup.3 is selected from the group consisting of C.sub.6 H.sub.4 (p-Cl) and CH.sub.2 C.sub.6 H.sub.5.Type: GrantFiled: June 7, 1995Date of Patent: April 1, 1997Assignee: Howard UniversityInventors: Kenneth R. Scott, Jesse M. Nicholson, Ivan O. Edafiogho
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Patent number: 5369109Abstract: The present invention provides optically active esters of 7-substituted 3,5-difunctionalized 6-heptenoic acids represented by the following formula: ##STR1## wherein R is a substituted or unsubstituted aromatic group, a substituted or unsubstituted heteroaromatic group or a substituted vinyl group;Ar is a condensed aromatic group;X.sup.1 and Y.sup.1 are not the same and each is a hydrogen atom or a hydroxyl group; andX.sup.2 and Y.sup.2 are not the same and each is a hydrogen atom or a hydroxyl group or enantiomers thereof.Type: GrantFiled: June 17, 1993Date of Patent: November 29, 1994Assignee: Sagami Chemical Research CenterInventors: Tamejiro Hiyama, Tatsuya Minami, Takeshi Hanamoto, Guntoori B. Reddy
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Patent number: 5356931Abstract: Alpha-Arylacrylic acid derivatives of the general formula I ##STR1## where X is ethylene or ethenylene; n is 0 or 1;m is 0, 1, 2, 3 or 4;R.sup.1 is cyano, cyanato, thiocyanato, nitro, hydroxyl, carboxyl, haloalkyl, haloalkoxy, unsubstituted or substituted cycloalkyl, cycloalkenyl, cycloalkadienyl, alkenyl, alkynyl or amino, alkylcarbonyl, alkoxycarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, unsubstituted or substituted benzyloxycarbonyl, benzoyl, phenylalkyl, phenylalkoxy or phenoxyalkyl,or R.sup.1 together with one of the radicals R.sup.2 forms an unsubstituted or substituted 1,3-butadiene-1,4-diyl group or an unsubstituted or substituted chain consisting of carbon members and an oxygen member, andR.sup.2 is halogen, unsubstituted or substituted alkyl, alkoxy, alkenyloxy, alkynyloxy, alkadienyloxy, benzyloxy or benzylthio, are used for controlling pests.Type: GrantFiled: January 4, 1993Date of Patent: October 18, 1994Assignee: BASF AktiengesellschaftInventors: Reinhard Kirstgen, Rainer Otter, Christoph Kuenast, Uwe Kardorff, Wolfgang Steglich, Gunda Bertram
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Patent number: 5318989Abstract: The present invention relates to a novel and efficient process for the preparation of 8-hydroxybicyclo[7.3.1]tridec-4-ene-2,6-diyne ring system which is part of the aglycone of esperemicin and to novel cytotoxic antitumor agents having said bicyclic ring system. The present invention also provides a method for treating mammalian malignant tumors by administering to an animal in need of such treatment an antitumor effective amount of a compound of the present invention.Type: GrantFiled: December 18, 1992Date of Patent: June 7, 1994Assignee: Bristol-Myers Squibb CompanyInventors: John F. Kadow, Mark D. Wittman
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Patent number: 5166212Abstract: Disclosed are compound of the formula ##STR1## wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, or each said grouping substituted by lower alkyl; R and R.sub.o independently represent lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl; A represents methylene; or A represents methylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by aryl-lower alkylthio-lower alkyl, by arylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by alkyloxy-lower alkyl, by aryloxy-lower alkyl, by amino-lower alkyl by acylamino-lower alkyl, by guanidino-lower amino-lower alkyl, by (C.sub.3 -C.sub.7)-cycloalkyl, by (C.sub.3 -C.sub.Type: GrantFiled: April 25, 1991Date of Patent: November 24, 1992Assignee: Ciba-Geigy CorporationInventor: Gary M. Ksander
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Patent number: 5141937Abstract: Pharmaceutical products containing a 7-diphenylmethylenebicycloheptane or 7-diphenylmethylenebicycloheptene derivative of the formula I ##STR1## in which A, B, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the stated meanings, or a physiologically tolerated acid addition salt of these compounds, and the use thereof as hypolipidemics are described. In addition, new 7-diphenylmethylenebicycloheptane and -heptene derivatives of the formula Ia ##STR2## in which A, B, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the stated meanings, and the physiologically tolerated acid addition salts thereof, as well as processes for the preparation thereof, are described.Type: GrantFiled: September 21, 1988Date of Patent: August 25, 1992Assignee: Hoechst AktiengesellschaftInventors: Herbert Siegel, Ernold Granzer
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Patent number: 5039710Abstract: Aphidicolane derivatives of the formula: ##STR1## wherein R.sup.1 stands for hydrogen or a hydroxy radical, R.sup.2 stands for a hydroxy or methyl radical, or the group CR.sup.1 R.sup.2 stands for a keto group; R.sup.3 stands for a formyl or hydroxymethyl radical, or for the group --CH.sub.2 O.CO.OR.sup.6, wherein R.sup.6 stands for a defined radical or R.sup.2 and R.sup.3 are joined together to form the group --O.CO.OCH.sub.2 --; R.sup.4 stands for a hydroxy radical; R.sup.5 stands for a formyl radical, a hydroxyalkyl radical --(CH.sub.2).sub.1-3 OH, a radical --CHR.sup.7 OH, wherein R.sup.7 stands for a defined radical, or R.sup.5 stands for an azidomethyl or pyrrolidinylcarbonyloxymethyl radical, or for the group --CH.sub.2 O.CO.OR.sup.8, wherein R.sup.8 stands for a defined radical, or R.sup.5 stands for the group --CH.sub.2 O.CO.(CH.sub.2).sub.m.CR.sup.11 R.sup.12.(CH.sub.2).sub.n.NR.sup.9 R.sup.10, wherein m, n, R.sup.9, R.sup.10, R.sup.11 and R.sup.12 have defined values, or R.sup.Type: GrantFiled: September 17, 1990Date of Patent: August 13, 1991Assignee: Imperial Chemical Industries PLCInventor: Arnold H. Ratcliffe
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Patent number: 5021430Abstract: Disclosed are compound of the formula ##STR1## wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, or each said grouping substituted by lower alkyl; R and R.sub.o independently represent lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl; A represents methylene; or A represents methylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by aryl-lower alkylthio-lower alkyl, by arylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by aryl-lower alkyloxy-lower alkyl, by aryloxy-lower alkyl, by amino-lower alkyl, by acylamino-lower alkyl, by guanidino-lower alkyl, by (C.sub.3 -C.sub.7)-cycloalkyl, by (C.sub.3 -C.sub.Type: GrantFiled: June 29, 1987Date of Patent: June 4, 1991Assignee: Ciba-Geigy CorporationInventor: Gary M. Ksander
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Patent number: 4957940Abstract: Certain bicyclo [2.2.1] heptane and bicyclo [2.2.2] octane substituted tetrahydro-2H-pyran-2-ones and the corresponding ring-opened acids derived therefrom are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) and are useful as hypocholesterolemic and hypolipidemic agents.Type: GrantFiled: November 21, 1989Date of Patent: September 18, 1990Assignee: Warner-Lambert CompanyInventor: Bruce D. Roth
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Patent number: 4931475Abstract: A cholagogic and/or gallstone solubilizer comprising a borneol compound as its active component.Type: GrantFiled: December 10, 1985Date of Patent: June 5, 1990Assignee: Hiya Pharmaceutical Co., Ltd.Inventor: Akira Uji
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Patent number: 4767625Abstract: A lamella type, single phase liquid crystal composition is prepared from a hydrophilic nonionic surfactant, a water-soluble substance having a hydroxyl group in a molecule thereof, an oil substance, and water.Oil-base cosmetic compositions including cleansing compositions, massage creams or drugs for external application are incorporated with the liquid crystal.The compositions are readily washed off simply by water, and exhibit good properties of non-stickiness and long storage stability.Type: GrantFiled: August 14, 1986Date of Patent: August 30, 1988Assignee: Kao CorporationInventors: Yuichiro Mitsuno, Keiko Nomaguchi, Toshiyuki Suzuki
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Patent number: 4678805Abstract: Compounds useful in treating cardiovascular disorders such as thrombosis, hypertension, and atherosclerosis are compounds depicted in formulas (1), (2), and (3): ##STR1## wherein: Y is exo-(lower alkyl) or endo-(lower alkyl);n is 2 or 3;R.sub.1 is CH.sub.2 OH, CHO, CO.sub.2 R or CO.sub.2 H;R.sub.2 is hydrogen or methyl; andR.sub.3 is linear or branched alkyl having 5-10 carbon atoms, ##STR2## or --(CH.sub.2).sub.m -phenyl optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen,in whicha is 0, 1 or 2;b is 3-7;m is 1 or 2; andR is ##STR3## wherein X is ##STR4## in which each R.sub.4 is independently hydrogen or lower alkyl having 1-6 carbon atoms, and the pharmaceutically acceptable, non-toxic salts and esters thereof.Type: GrantFiled: July 28, 1986Date of Patent: July 7, 1987Assignee: Syntex (U.S.A.) Inc.Inventors: Arthur F. Kluge, Helen Y. Wu
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Patent number: 4622339Abstract: Norbornane- and norbornene-carboxylic acid amides of the formula ##STR1## in which ##STR2## represents the part structure ##STR3## A represents a ##STR4## or --CH.sub.2 --CH.sub.2 -- group, R.sup.1 and R.sup.2 each independently is hydrogen or an alkyl radical with 1-6 carbon atoms,R.sup.3 is alkyl or alkenyl which has 1-8 carbon atoms and is optionally substituted by halogen or alkyl with 1 or 2 carbon atoms, cycloalkyl or cycloalkeny wtih 3 to 7 carbon atoms, an aromatic radical which has 6 or 10 carbon atoms and and is optionally substituted by halogen, by alkyl with 1 or 2 carbon atoms or by halogenoalkyl with 1 or 2 carbon atoms, or is a five-membered or six-membered heteroaromatic radical,R.sup.4 is hydrogen or a hydroxyl group,R.sup.5 and R.sup.6 each independently is hydrogen or alkyl with 1 to 4 carbon atoms, andn is a number from 2 to 6,and, if R.sup.1 is hydrogen, also physiologically acceptable salts thereof, perform as thromboxan antagonists.Type: GrantFiled: January 11, 1985Date of Patent: November 11, 1986Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Hermann Oediger, Hans-Joachim Kabbe, Ulrich Niewohner, Elisabeth Perzborn, Friedel Seuter
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Patent number: 4608388Abstract: Compounds useful in treating cardiovascular disorders such as thrombosis, hypertension, and atherosclerosis are compounds depicted in formulas (1), (2), and (3): ##STR1## wherein: n is 2 or 3;R.sub.1 is CH.sub.2 OH, CHO, CO.sub.2 R or CO.sub.2 H;R.sub.2 is hydrogen or methyl; andR.sub.3 is linear or branched alkyl having 5-10 carbon atoms, ##STR2## optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen,in whicha is 0, 1 or 2;b is 3-7;m is 1 or 2; andR is ##STR3## in which each R.sub.4 is independently hydrogen or lower alkyl having 1-6 carbon atoms,and the pharmaceutically acceptable, non-toxic salts and esters thereof.Type: GrantFiled: March 27, 1985Date of Patent: August 26, 1986Assignee: Syntex (U.S.A.) Inc.Inventors: Arthur F. Kluge, Anthony L. Willis, Counde O'Yang
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Patent number: 4529599Abstract: Carboxylate esters of the formula (I):R.sub.1 --COOR.sub.2wherein R.sub.1 is a tricyclodecyl or tricycloundecyl group, and R.sub.2 is a group of the formula ##STR1## wherein R.sub.3 is hydrogen or a cyano group; ##STR2## wherein R.sub.3 is a hydrogen or a cyano group; ##STR3## which are useful as insecticides.Type: GrantFiled: December 9, 1983Date of Patent: July 16, 1985Assignee: Kao CorporationInventor: Shoji Nakagawa
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Patent number: H303Abstract: This invention describes a composition of matter and a method of treating agricultural substrates in which an active ingredient selected from the group consisting of fungicides, bactericides, insecticides, insect repellents, herbicides and plant growth regulators and mixtures thereof is utilized in conjunction with an amount of a glycoside dispersing agent selected from the group consisting of fructoside, glucoside, mannoside, galactoside, taloside, guloside, alloside, altroside, idoside, arabinsode, xyloside, lyxoside and riboside and mixtures thereof which is sufficient to form an emulsion or dispersion of the active ingredient.Type: GrantFiled: October 22, 1986Date of Patent: July 7, 1987Assignee: A. E. Staley Manufacturing CompanyInventors: Arshad H. Malik, Arno Cahn