Naphthyl Ring System Patents (Class 514/682)
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Publication number: 20020177585Abstract: The use of a pharmaceutical formulation in treating coronary arteriosclerosis and a two-component pharmaceutical formulation. The pharmaceutical formulation contains peroxidic species or reaction products resulting from oxidation of an alkene, such as geraniol, by an oxygen-containing oxidizing agent, such as ozone; a penetrating solvent, such as dimithyl sulfoxide; a dye containing a chelated metal, such as hematoporphyrin; and an aromatic redox compound, such as benzoquinone.Type: ApplicationFiled: March 30, 2001Publication date: November 28, 2002Inventors: Robert F. Hofmann, Robert H. Carpenter
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Publication number: 20020169135Abstract: Multiple myeloma and other hematologic tumors and/or malignancies can be treated by administration of a G1 and/or S phase drug, which is preferably &bgr;-lapachone, or a derivative or analog thereof, combined with a G2/M phase drug such as a taxane derivative, which is advantageously paclitaxel. This combination of the G1 and/or S phase drug with the G2/M phase drug results in an unexpectedly greater than additive (i.e., synergistic) apoptosis in multiple myeloma cells. The invention includes methods of treating multiple myeloma by administering the combination of the G1 and/or S phase drug and the G2/M phase drug, pharmaceutical compositions comprising the combination of drugs used in these methods, as well as pharmaceutical kits.Type: ApplicationFiled: November 7, 2001Publication date: November 14, 2002Inventors: Arthur B. Pardee, Kenneth Anderson, Deepak Gupta, Chiang Li, Youzhi Li
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Publication number: 20020146463Abstract: The present invention discloses compositions useful as food additives or in medicaments to improve health by treating, preventing, or curing diseases and medical disorders. In particular, the compositions are formulated to provide the nutrients necessary for maintaining optimal free radical defenses in the body.Type: ApplicationFiled: December 14, 2001Publication date: October 10, 2002Inventor: Paul Clayton
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Publication number: 20020143028Abstract: Disclosed is a pharmaceutical composition, comprising a combination of a dose of nabumetone or a pharmaceutically acceptable salt thereof and a dose of oxycodone or a pharmaceutically acceptable salt thereof, said combination in an amount sufficient to provide an analgesic effect in a human patient. Also disclosed is a method of effectively treating pain in humans or other mammals, comprising administering to the patient a combination of a dose of nabumetone or a pharmaceutically acceptable salt thereof and a dose of oxycodone or a pharmaceutically acceptable salt thereof such that the dosing interval of the nabumetone overlaps with the dosing interval of the oxycodone, said combination in an amount sufficient to provide an analgesic effect in a human patient.Type: ApplicationFiled: January 25, 2002Publication date: October 3, 2002Inventors: Ronald M. Burch, Richard S. Sackler, Paul D. Goldenheim
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Publication number: 20020127536Abstract: The disclosed invention provides a method and system of assaying chemical compounds to determine their effect on mitochondrial cellular respiration. Many neuroleptics have been implicated as interfering with mitochondrial function, and these effects may lead to long term side effects such as extrapyramidal side effects and tardive dyskinesia. In order to develop better pharmaceutical agents with fewer side effects, the mitochondrial assay as disclosed herein allows one to screen many drug candidates quickly for their effect on mitochondrial function and predict long term side effects.Type: ApplicationFiled: January 11, 2001Publication date: September 12, 2002Inventor: June R. Aprille
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Patent number: 6436423Abstract: A product and method for reducing and preventing the ingestion of substrates by avians wherein the substrates are disposed within an avian house. The product is a bird repellent in combination with a substrate disposed within an avian house. As a result of the reduced ingestion of substrates such as litter, healthier avians are achieved.Type: GrantFiled: June 15, 1999Date of Patent: August 20, 2002Assignee: Arkion Life SciencesInventors: Kenneth E. Ballinger, Jr., Craig W. Henry
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Patent number: 6436446Abstract: A method including administering a beverage composition suitable for human consumption including effective amounts of the following solubilized components, a calcium compound, an organic acid in an amount up to the equivalent amount of a calcium of the calcium compound, an isoflavone, and inulin wherein the effective amounts are sufficient to reduce the risk of bone density loss and are solubilized by a stabilizing agent including one or more of maltol, carrageenan and maltodextrin, and xanthan gum.Type: GrantFiled: July 30, 1999Date of Patent: August 20, 2002Assignee: Pharmavite LLCInventors: Samuel L. Forusz, Hanlan Liu, Rose M. Muatine
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Patent number: 6433022Abstract: There is provided a method of contraception, comprising exposing a spermicidally sufficient quantity of an agent to spermatozoa. The agent is a quinone represented by the following formula: Each group A is H or an electron releasing moiety. The agent is capable of generating reactive oxygen species including free radicals, superoxide and hydrogen peroxide in the presence of spermatozoa.Type: GrantFiled: September 13, 1999Date of Patent: August 13, 2002Assignee: Medical Research CouncilInventor: Robert John Aitken
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Publication number: 20020099086Abstract: This invention relates to the use of extracts and compounds derived from the plant Aristolochia taliscana and their analogues in the treatment of AIDS.Type: ApplicationFiled: January 31, 2001Publication date: July 25, 2002Applicant: PROTEOME SCIENCES PLCInventors: Hans Achenbach, Carlos Navarro, Alejandro Navarro
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Patent number: 6413993Abstract: Methods of treatment and prevention of malarial infection caused by Plasmodium vivax, in which combinations of atovaquone, proguanil and primaquine are administered to a patient.Type: GrantFiled: October 9, 2001Date of Patent: July 2, 2002Assignee: SmithKline Beecham CorporationInventor: Jeffrey David Chulay
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Publication number: 20020081326Abstract: A product and method for reducing and preventing the ingestion of substrates by avians wherein the substrates are disposed within an avian house. The product is a bird repellent in combination with a substrate disposed within an avian house. As a result of the reduced ingestion of substrates such as litter, healthier avians are achieved.Type: ApplicationFiled: June 15, 1999Publication date: June 27, 2002Inventors: KENNETH E. BALLLINGER, CRAIG W. HENRY
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Patent number: 6410601Abstract: A pharmaceutical composition is provided, which comprises an aqeous solution containing a mixture of di- and tri-sodium salts of echinochrome in an amount of 0.90 to 1.10 g/ml (Histochrome). It meets the requirements that apply to injectable formulations. Administration of Histochrome reduces by 57% the necrosis zone in patients with acute myocardial infarction, restores the contractility of the left ventricle, reduces the incidence of reperfusion-induced ventricular arrhythmias and exerts an antiarrhythmogenic effect. Histochrome suppresses the aggregation of erythrocytes and thrombocytes, produces a beneficial effect on the clinical course of the disease, reduces the incidence of complications and lethal outcomes in cases of acute myocardial infarction. It is well tolerated by patients.Type: GrantFiled: April 12, 2001Date of Patent: June 25, 2002Assignee: Tikhookeansky Institut Bioorganicheskoi Khimii Dalnevostochnogo Otdeleniya Rossiiskoi Akademii NaukInventors: Georgy Borisovich Elyakov, Oleg Borisovich Maximov, Natalya Petrovna Mischenko, Evgenia Alexandrovna Koltsova, Sergei Alexandrovich Fedoreev, Ljutsia Ignatievna Glebko, Natalya Petrovna Krasovskaya, Alexandr Alexeevich Artjukov
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Publication number: 20020040011Abstract: A method of treatment of a host with a cellular proliferative disease, comprising contacting the host with a naphthoquinone and an antiproliferative agent, each in an amount sufficient to modulate said cellular proliferative disease, is described. In some embodiments, the naphthoquinone comprises menadione (Kativ-G; 2-Methyl-1,4-Naphthoquinone; Menaphthone; Vitamin K3; Panosine; 2-Methyl-1,4-naphthalenedione; Vitamin K2(0); Methyl-1,4-naphthalenedione; Methyl-1,4-naphthoquinone). Antiproliferative agents of the invention comprise alkylating agents, intercalating agents, metal coordination complexes, pyrimidine nucleosides, purine nucleosides, inhibitors of nucleic acid associated enzymes and proteins, and agents affecting structural proteins and cytoplasmic enzymes. The invention comprises the described methods as well as compositions comprising a naphthoquinine and an antiproliferative agent.Type: ApplicationFiled: May 31, 2001Publication date: April 4, 2002Inventor: Dennis M. Brown
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Publication number: 20020025983Abstract: Nutritional and pharmaceutical formulations comprising in combination vitamin K and a source of at least one essential fatty acid (EFA) as the essential ingredients, and foodstuff containing EFA(s) and an artificially elevated quantity of vitamin K are provided for the treatment or prevention of a variety of diseases or conditions.Type: ApplicationFiled: July 5, 2001Publication date: February 28, 2002Inventor: David Frederick Horrobin
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Publication number: 20020016372Abstract: A method for preventing and treating AD is supplementation with vitamin K so that the concentration of the vitamin in the circulation is sufficient for its functions outside the liver. Vitamin K supplementation will also be useful to reduce brain damage associated with cardiovascular disease and injury. Vitamin K can be administered orally, subcutaneously, intramuscularly or intravenously. The vitamin K can be phylloquinone, menaquinones of varying chain lengths, or menadione. Preferred forms of the vitamin are all-trans menadione and menaquinone-4. These are formulated so as to ensure efficient absorption from the gastrointestinal tract and rapid bioavailability in the brain following administration.Type: ApplicationFiled: June 11, 2001Publication date: February 7, 2002Inventor: Anthony Clifford Allison
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Patent number: 6342499Abstract: The present invention provides a method to control parasitic and saprophagous mites on beneficial insects such as honeybees via the application of a parasiticidally or saprophagouscidally effective amount of a mitochondrial electron transport inhibitor or a pyrimidine compound of formula I.Type: GrantFiled: July 12, 1999Date of Patent: January 29, 2002Assignee: BASF AktiengesellschaftInventors: Bruce Christian Black, William R. Baumbach, Michael P. Beluch
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Patent number: 6340468Abstract: A method of controlling or inhibiting the growth of aquatic plants and animals applies an effective amount of an active compound. The active compounds are selected from the group consisting of quinones, anthraquinones, naphthalenediones, quinine, warfarin, coumarins, amphotalide, cyclohexadiene-1,4-dione, phenidione, pirdone, sodium rhodizonate, apirulosin and thymoquinone. The compounds are particularly effective for treating ballast water of ships to control the relocation of plants and animals contained in the ballast water.Type: GrantFiled: February 17, 2000Date of Patent: January 22, 2002Assignee: Garnett, Inc.Inventors: Horace G. Cutler, Stephen J. Cutler, David Wright, Rodger Dawson
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Patent number: 6313163Abstract: Compounds of formula 1 wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, Y is cyclopropyl optionally substituted with one or two R4 groups, the divalent Y radical being substituted by the Z and —CR1═CR1—CR1═CR1 groups on adjacent carbons; X is S, O, or NR5; n is 1 or 2; R1 and R2 independently are H, lower alkyl or fluoroalkyl; R3 is hydrogen, lower alkyl, Cl or Br; R4 is lower alkyl, fluoroalkyl or halogen; R5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR8, CONR9R10, —CH2OH, CH2OR11, CH2OCOR11, CHO, CH(OR12)2, CHOR13O, 13 COR7, CR7(OR12)2, CR7OR13O, or tri-lower alkylsilyl, where R7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R8 is an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or R8 is phenyl or lower alkylphenyl, R9 and R10 indepType: GrantFiled: August 17, 2000Date of Patent: November 6, 2001Assignee: Allergen Sales, Inc.Inventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Publication number: 20010029270Abstract: A pharmaceutical composition is provided, which comprises an aqeous solution containing a mixture of di- and tri-sodium salts of echinochrome in an amount of 0.90 to 1.10 g/ml (Histochrome). It meets the requirements that apply to injectable formulations. Administration of Histochrome reduces by 57% the necrosis zone in patients with acute myocardial infarction, restores the contractility of the left ventricle, reduces the incidence of reperfusion-induced ventricular arrhythmias and exerts an antiarrhythmogenic effect. Histochrome suppresses the aggregation of erythrocytes and thrombocytes, produces a beneficial effect on the clinical course of the disease, reduces the incidence of complications and lethal outcomes in cases of acute myocardial infarction. It is well tolerated by patients.Type: ApplicationFiled: April 12, 2001Publication date: October 11, 2001Inventors: Georgy Borisovich Elyakov, Oleg Borisovich Maximov, Natalya Petrovna Mischenko, Evgenia Alexandrovna Koltsova, Sergei Alexandrovich Fedoreev, Ljutsia Ignatievna Glebko, Natalya Petrovna Krasovskaya, Alexandr Alexeevich Artjukov
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Patent number: 6291488Abstract: The invention relates to combinations of atovaquone and proguanil, their use in the treatment and prophylaxis of parasitic infections such as protozoal parasitic infections, e.g., malaria and toxoplasmosis, and infections caused by P. carinii and their use in the manufacture of medicaments for the treatment and/or prophylaxis of such infections. The combinations can conveniently be administered in a single pharmaceutical formulation. Preferably, atovaquone and proguanil are administered in a potentiating ratio so that they act in synergy.Type: GrantFiled: October 4, 2000Date of Patent: September 18, 2001Assignee: Glaxo Wellcome Inc.Inventors: Winston Edward Gutteridge, David Brian Ashton Hutchinson, Victoria Susan Latter, Mary Pudney
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Patent number: 6291533Abstract: Dietary supplement compositions designed to be responsive to specific blood types, and thus most beneficial for people with specific antigenic blood types.Type: GrantFiled: December 22, 1999Date of Patent: September 18, 2001Assignee: Vitamerica, Inc.Inventor: Albert M. Fleischner
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Publication number: 20010021723Abstract: A pharmaceutical composition is provided which comprises an isotonic solution of an 0.02% mixture of di- and trisodim salts of echinochrome (Histochrome). It meets the requirements that apply to injectable formulations. Histochrome administration to human patients normalizes metabolic processes and eliminates inflammation in the retina, vascular membrane and cornea of the eye, improves trophic functions, reduces edema and accelerates epithelization.Type: ApplicationFiled: April 12, 2001Publication date: September 13, 2001Inventors: Georgy Borisovich Elyakov, Oleg Borisovich Maximov, Natalya Petrovna Mischenko, Evgenia Alexandrovna Koltsova, Sergei Alexandrovich Fedoreev, Ljutsia Ignatievna Glebko, Natalya Petrovna Krasovskaya, Alexander Alexeevich Artjukov
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Patent number: 6248751Abstract: Mammalian hair growth is reduced by applying to the skin a composition including an inhibitor of cyclooxygenase.Type: GrantFiled: May 28, 1993Date of Patent: June 19, 2001Inventors: Gurpreet S. Ahluwalia, Douglas Shander
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Patent number: 6197763Abstract: Novel dietary complexes for gastrointestinal symptoms and gastrointestinal microbes are provided. They comprise a dietary metal and a dietary ligand wherein the dietary metal is selected from zinc, copper, cobalt, manganese and iron and the dietary ligand is lawsone or tropolone.Type: GrantFiled: August 30, 1999Date of Patent: March 6, 2001Assignee: Pflori LimitedInventors: Richard Paul Hepworth Thompson, Jonathan Joseph Powell, Rosemary Helen Phillips, Sylvaine Francoise Aline Chevalier
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Patent number: 6169111Abstract: Conformationally rigid aryl prostaglandins are useful in the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic pharmaceutical compositions comprising said prostaglandins.Type: GrantFiled: May 12, 1999Date of Patent: January 2, 2001Assignee: Alcon Laboratories, Inc.Inventors: Paul W. Zinke, John E. Bishop, Thomas R. Dean, Mark R. Hellberg
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Patent number: 6166046Abstract: The invention relates to combinations of atovaquone and proguanil, their use in the treatment and prophylaxis of parasitic infections such as protozoal parasitic infections, e.g., malaria and toxoplasmosis, and infections caused by P. carinii and their use in the manufacture of medicaments for the treatment and/or prophylaxis of such infections. The combinations can conveniently be administered in a single pharmaceutical formulation. Preferably, atovaquone and proguanil are administered in a potentiating ratio so that they act in synergy.Type: GrantFiled: October 1, 1999Date of Patent: December 26, 2000Assignee: Glaxo Wellcome Inc.Inventors: Winston Edward Gutteridge, David Brian Ashton Hutchinson, Victoria Susan Latter, Mary Pudney
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Patent number: 6114397Abstract: A method for treating cancer in a human, which comprises administering to the human subject an anti-cancer effective amount of a compound selected from gossypol, gossypol acetic acid, gossypolone, metabolites thereof, or physiologically acceptable salts thereof. Also included is a method for treating cancer in a human which comprises administering to the human subject an anti-cancer effective amount of any of the compounds listed above in combination with an anti-cancer effective amount of other conventional chemotherapeutic agents. Finally, the invention also encompasses a pharmaceutical composition comprising an anti-cancer effective amount of gossypol, gossypol acetic acid, or gossypolone, and an anti-cancer effective amount of a conventional chemotherapeutic agent, or combinations of the latter.Type: GrantFiled: January 27, 1995Date of Patent: September 5, 2000Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Mary R. Flack, Richard Knazek, Marcus Reidenberg
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Patent number: 6103768Abstract: The invention described here concerns the unique utility of fatty acids and their derivatives to eradicate existing fungal and bacterial infections in plants. Also, described herein are combination treatments whereby fatty acids are used to enhance or augment the activity of fungicides, bactericides, and biological control agents.Type: GrantFiled: September 8, 1997Date of Patent: August 15, 2000Assignee: Mycogen CorporationInventors: Steven D. Savage, Steven L. Evans, Robert A. Haygood, Paul S. Zorner, Keith Jones
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Patent number: 6100267Abstract: Pharmaceutical compositions and methods of inhibiting calpain using novel quinoline- or naphthatenecarboxamides are disclosed.Type: GrantFiled: August 30, 1999Date of Patent: August 8, 2000Assignees: SmithKline Beecham Corporation, Cephalon, Inc.Inventors: Robert A Daines, William D Kingsbury, Israil Pendrak, John P Mallamo
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Patent number: 6080791Abstract: A method of preventing and treating a viral condition caused by an enveloped virus is described, comprising using a therapeutically effective amount of a compound selected from the group consisting of a substituted hydroquinone and the corresponding benzoquinone, wherein said hydroquinone comprises a 2-R.sup.1, 3-R.sup.2 -1,4-hydroquinone where at least one of R.sup.1 and R.sup.2 include a carbon linkage to the benzene ring of the hydroquinone. Particularly useful compounds include 5,8-dihydro-5,8-methano-1,4-naphthalenediol, 1,4-naphthoquinone, 3', 6'-dihydroxybenzo-norbornane, tert-butylhydroquinone, other diols, e.g. 1,5-naphthalenediol, and alkylated diols, e.g. 4-methoxy-1-naphthol.Type: GrantFiled: July 24, 1992Date of Patent: June 27, 2000Assignees: Seres Laboratories, Inc., University of CaliforniaInventors: Dale L. Bodian, Judith M. White, Irwin D. Kuntz, Jay F. Stearns, R. Bryan Yamasaki
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Patent number: 6074634Abstract: The present invention provides an composition for attracting noctuid and/or other lepidopteran species. Liquid and solid formulations are provided, along with methods for their use, for controlling or eliminating noctuid and/or other lepidopteran species, and/or protecting plants susceptible to noctuid and/or other lepidopteran species damage.Type: GrantFiled: October 5, 1998Date of Patent: June 13, 2000Assignee: The United States of America as represented by the Secretary of AgricultureInventors: Juan D. Lopez, Jr., Ted N. Shaver, Kenneth R. Beerwinkle, Peter D. Lingren
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Patent number: 6075057Abstract: Optically pure enantiomers of avarol are obtained. The enantiomers of avarol are demonstrated to be highly effective inhibitors of .alpha.-glucosidase and .alpha.-mannosidase. Other enzymes assayed were not inhibited by these optically pure compounds. Inhibition of these two enzymes is useful for a variety of assays and probes, and offers particular utility in the treatment of retroviral infection-associated syndromes, such as AIDS.Type: GrantFiled: April 1, 1997Date of Patent: June 13, 2000Assignee: The University of Virginia Patent FoundationInventors: Sidney M. Hecht, Edward Locke
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Patent number: 6051588Abstract: A compound comprising a non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO group, a pharmaceutical composition including the compounds and methods of treatment of pain and/or inflammation using the compounds and compositions are disclosed. Also disclosed is a composition comprising a non-steroidal antiinflammatory agent and a compound that donates, transfers or releases nitric oxide.Type: GrantFiled: April 19, 1995Date of Patent: April 18, 2000Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6048877Abstract: Tetralone derivatives of the formula ##STR1## where R.sup.1 is halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, (aryl)alkenyl, (aryl)alkynyl, alkoxy, O-alkenyl, O-aryl, O-alkyl(heterocyclo), COO-alkyl,alkanoyl, CO-amino, CO-substituted amino, alkyl-CO-amino, alkyl-CO-substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-alkyl(heterocyclo), N(alkyl)CO-alkyl, N(alkyl)CO-aryl, N(alkyl)CO-heterocyclo, N(alkyl)CO-alkyl(heterocyclo);R.sup.2 is hydrogen, alkyl, halo, aryl, alkoxy, amino, substituted amino;R.sup.3 is oxo, hydroxy, alkoxy, O--COalkyl, --O--COaryl, --O--COheterocyclo, NOH, NO-alkyl, N-amino, N-substituted amino, N-NHCONHalkyl, N-NHSO.sub.2 alkyl, N-NHSO.sub.2 aryl, amino, substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-heterocyclo, spiroheterocyclo;R.sup.4 is hydrogen, alkyl, alkyl(COalkyl), alkyl(COOalkyl); orR.sup.3 and R.sup.4 taken together with the atoms to which they are attached form a five- to seven-membered ring which can contain up to three heteroatoms selected from oxygen, nitrogen and sulfur;R.sup.Type: GrantFiled: January 20, 1998Date of Patent: April 11, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Saleem Ahmad, Philip D. Stein, Francis N. Ferrara, Karnail S. Atwal
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Patent number: 6043286Abstract: Pesticidal as a pesticide against whitefly, Lepidoptera and certain fungi is provided of compound of general formula (I) ##STR1## or a salt thereof is provided, in which n represents an integer from 0 to 4; m represents an integer 0 or 1;each R independently represents a halogen atom or a nitro, cyano, hydroxyl, alkyl, alkenyl, haloalkyl, haloalkenyl, alkoxy, haloalkoxy, haloalkenoxy, amino, alkylamino, dialkylamino, alkoxycarbonyl, carboxyl, alkanoyl, alkylthio, alkylsulphinyl, alkylsulphonyl, carbamoyl, alkylamido, cycloalkyl, aryl or aralkyl group;R.sup.1 and R.sup.2 each independently represent an optionally substituted alkoxy group or together represent a group .dbd.O, .dbd.S or .dbd.N--OR.sup.9, where R.sup.9 represents a hydrogen atom or an optionally substituted alkyl group;R.sup.3 represents a hydroxyl group, or a group --OL where L is a leaving group, or a group which in vivo is transformed into a group --OL.sup.1 where L.sup.1 is a leaving group;R.sup.7 and R.sup.Type: GrantFiled: July 10, 1997Date of Patent: March 28, 2000Assignee: BTG International LimitedInventors: Bhupinder Pall Singh Khambay, Duncan Batty
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Patent number: 6025400Abstract: Compositions for treatment of antibiotic-resistant gram-positive bacterial infections, as well as methods for using and preparing the same, are disclosed.Type: GrantFiled: August 24, 1998Date of Patent: February 15, 2000Assignee: Marco Polo TechnologiesInventor: Yuan Lin
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Patent number: 6017932Abstract: A novel composition for increasing the bioavailability of Non-steroidal Anti-inflammatory Drugs (NSAIDs), particularly those belonging to the category which exhibits its activity by selectively inhibiting cyclooxygenases-II (COX-II) and/or lipooxygenases, is disclosed. The composition is characterized in having clinically significant increased bioavailability when compared to the known compositions of the drugs. The pharmaceutical compositions comprise NSAIDs and Piperine, as herein disclosed. Enhanced bioavailability of NSAIDs results in the reduction of both dosages and dose-related side effects.Type: GrantFiled: December 10, 1997Date of Patent: January 25, 2000Assignee: Panacea Biotec LimitedInventors: Amarjit Singh, Rajesh Jain
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Patent number: 6008204Abstract: Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.Type: GrantFiled: December 30, 1998Date of Patent: December 28, 1999Assignee: Allergan Sales, Inc.Inventors: Elliott S. Klein, Alan T. Johnson, Andrew M. Standeven, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Sunil Nagpal, Vidyasagar Vuligonda, Min Teng, Roshantha A. Chandraratna
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Patent number: 6001883Abstract: Substituted benzophenone compounds are disclosed, having the formula: ##STR1## The compounds are useful as fungicides having high systemicities.Type: GrantFiled: June 24, 1998Date of Patent: December 14, 1999Assignee: American Cyanamid CompanyInventors: Juergen Curtze, Gerd Morschhaeuser, Henry Van Tuyl Cotter
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Patent number: 5998449Abstract: The invention relates to combinations of atovaquone and proguanil, their use in the treatment and propinylaxis of parasitic infections, such as protozoal parasitic infections, e.g. malaria and toxoplasmosis, and infections caused by P.carinii and their use in the manunfacture of medicaments for the treatment and/or prophylaxis of such infections. The combinations can conveniently be administered in a single pharmaceutical formulation. Preferably, atovaquone and proguanil are administered in a potentiating ratio so that they act in synergy.Type: GrantFiled: October 31, 1997Date of Patent: December 7, 1999Assignee: Glaxo Wellcome Inc.Inventors: Winston Edward Gutteridge, David Brian Ashton Hutchinson, Victoria Susan Latter, Mary Pudney
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Patent number: 5929109Abstract: The present invention relates to an agent for enhancing and stabilizing the activity of Bifidus factor, containing at least one member selected from the group consisting of ascorbic acid, hyposulfurous acid and acetic anhydride as the effective ingredient, and by preparing the agent singly or in combination with Bifidus factor as a food and drink type or as a composition of pharmaceutical type, intestinal microflora can be ameliorated. The agent can be used as a selective medium for assaying the number of bifidobacteria.Type: GrantFiled: October 3, 1997Date of Patent: July 27, 1999Assignee: Meiji Milk Products Company LimitedInventors: Hiroharu Mori, Kakuhei Isawa, Tsutomu Kaneko
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Patent number: 5922774Abstract: Method for repelling insect herbivores from plant surfaces and deterring them from feeding on plant surfaces by applying an aqueous dispersion of polycyclic quinone or precursor thereof to the foliage of the plant and/or to the surrounding soil in which the plant is rooted.Type: GrantFiled: October 22, 1996Date of Patent: July 13, 1999Assignee: DCV, Inc.Inventor: Anna Louise Winslow
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Patent number: 5919829Abstract: Compounds of formula (Ia), (Ib), or (Ic), wherein A represents a group having two fused rings, or a group of formula (Id), R.sup.1.sub.(m) represents up to 6 substituents, K represents --O--, --S--, --CH.sub.2 --, --N(R.sup.2)-- or --N(COR.sup.2)--, in which R.sup.2 is H or C.sub.1 to C.sub.3 alkyl, W is a carbonyl, sulfonyl or sulfinyl group, provided that at least one of W and X contains carbonyl, Y and Z are as given in the description, and their pharmaceutically acceptable salts are ligands at CCK and/or gastrin receptors.Type: GrantFiled: April 23, 1998Date of Patent: July 6, 1999Assignee: James Black Foundation LimitedInventors: Sarkis Barret Kalindjian, Katherine Isobel Mary Steel, Michael John Pether, Jonathan Michael Richard Davies, Caroline Minli Rachel Low, Martin Lyn Hudson, Ildiko Maria Buck, Iain Mair McDonald, David John Dunstone, Matthew John Tozer
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Patent number: 5861385Abstract: Substituted triols are prepared by reducing appropriately substituted carboxylic esters. The substituted triols can be used as active substances in medicaments.Type: GrantFiled: August 8, 1995Date of Patent: January 19, 1999Assignee: Bayer AktiengesellschaftInventors: Rolf Angerbauer, Peter Fey, Walter Hubsch, Thomas Philipps, deceased, Hilmar Bischoff, Hans-Peter Krause, Jorg Petersen von Gehr, Delf Schmidt
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Patent number: 5859066Abstract: A method useful for the treatment of itching is disclosed. The method comprises applying an effective amount a 1,4-naphthoquinone to the affected area of the skin. The 1,4-naphthoquinone is hydroxy or keto at the 2 position or the 3 position, or a juglone. A composition comprising an effective amount of the 1,4-naphthoquinone, and a kit for conducting the method are also provided.Type: GrantFiled: April 8, 1997Date of Patent: January 12, 1999Assignee: Rutgers, The State University of New JerseyInventor: Robert T. Rosen
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Patent number: 5856362Abstract: The present invention relates to the use of 2-?4-(4-chlorophenyl)cyclohexyl!-3-hydroxy-1,4-naphthoquinone or a physiologically acceptable salt or other physiologically funtional derivative thereof for the manufacture of a medicament for the treatment and/or prophylaxis of toxoplasmosis in animals, to pharmaceutical compositions for the treatment and/or prophylaxis of toxoplasmosis, comprising said compound as active ingredient and to a method of treating or preventing toxoplasmosis in an animal which comprises administering to said animal an effective amount of said compound.Type: GrantFiled: June 6, 1995Date of Patent: January 5, 1999Assignee: Glaxo Wellcome Inc.Inventor: Alan Thomas Hudson
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Patent number: 5834515Abstract: The invention relates to certain naphthoquinone derivatives, some of which are novel, of the general formula I ##STR1## in which R represents a hydrogen atom or a hydroxyl or an ethanoyloxy group; methods for their preparation; compositions containing such compounds and their use as pesticides, such as fungicides and, especially, insecticides and acaricides. Compounds of formula I may be derived from plants of the genus Calceolaria and the invention therefore also relates to extracts of a Calceolaria species and their use as pesticides.Type: GrantFiled: August 9, 1996Date of Patent: November 10, 1998Assignee: British Technology Group LimitedInventors: Bhupinder Pall Singh Khambay, Duncan Batty, August Hermann Niemeyer Marich, Matthew Robert Cahill
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Patent number: 5780514Abstract: The present invention relates to pharmaceutical compositions for the treatment and/or prophylaxis of protozoal infections caused by Kinetoplastida, Apicomplexa, Anaerobic protozoa and Microsporidia comprising 2-?4-(4-chlorophenyl)cyclohexyl!-3-hydroxy-1,4-naphthoquinone or a physiologically acceptable salt or other functional derivative thereof as active ingredient and to a method of treating or preventing said protozoal infections in an animal which comprises administering to said animal an effective amount of said compound.Type: GrantFiled: July 16, 1996Date of Patent: July 14, 1998Assignee: Glaxo Welcome Inc.Inventors: Winston Edward Gutteridge, Alan Thomas Hudson, Victoria Susan Latter, Mary Pudney
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Patent number: 5763479Abstract: A redox, hydrogen-acceptor compound, having utility in treating inflammation, is a 1,4-dioxonaphthalene or 1,4-dilminon aphthalene having either a 2,3-double bond, in which cast there are 2 and 3-substituents, or a 2,3-single bond. Examples of such compounds are menadione epoxide and water-soluble derivatives or menadione such as menadione bisulphite.Type: GrantFiled: July 12, 1993Date of Patent: June 9, 1998Assignee: KS Biomedix Ltd.Inventors: Joseph Chayen, Lucille Bitensky, George T. B. Frost
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Patent number: RE37087Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.Type: GrantFiled: June 20, 1991Date of Patent: March 6, 2001Assignee: Schering AktiengesellschaftInventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles