Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos (e.g., Methylenedioxyphenyl Group, Etc.) Patents (Class 514/464)
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Publication number: 20090182040Abstract: The present invention relates to a method of preventing or reducing insecticidal resistance of adult insect pests of the family Nitidulidae, the family Curculionidae and Psylliodes spp. which method comprises contacting the plant or the soil or water in which the plant is growing, or the pest or its food supply, habitat, breeding grounds or locus, with pesticidally effective amounts of piperonyl butoxide and at least one pyrethroid, wherein piperonyl butoxide and the pyrethroid are applied in a weight ratio of from 0.0001 to 10000.Type: ApplicationFiled: May 11, 2007Publication date: July 16, 2009Applicant: BASF SEInventors: Martin Heger, Herve R. Vantieghem
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Patent number: 7553834Abstract: A method for determining the appropriate medication for a patient suffering from depression. A patient will take a questionnaire wherein the patient answers a number of questions with scaled responses concerning the degree to which the patient's mental state is affected by at least one or both of impaired modulation and impaired activation. Next, the patient's answers will be processed to arrive at scores for the at least one impaired modulation and impaired activation. Depending upon the patient's scores for demodulation and deactivation, at least one medication which affects the at least one impaired modulation and impaired activation is recommended.Type: GrantFiled: July 19, 2002Date of Patent: June 30, 2009Inventor: Richard J. Metzner
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Publication number: 20090163582Abstract: Pesticide concentrates are provided containing an emulsifier that is an EPA list 4 inert and is a polyglycerol fatty acid ester, a sorbitan fatty acid ester or a combination thereof, a pesticide and a solvent that is either a EPA list 3 inert of acetyl ester, EPA list 4 inert of a methyl fatty ester, an acetyltributyl citrate, white mineral oil or a combination thereof. The pesticide can be a water-insoluble synthetic pyrethroid, natural pyrethrum, channel blocking insecticide, acetylcholinesterase inhibitor, oxadiazine, organophosphate, neonicotinoid insecticide, thiamethoxam, imidacloprid, acetamiprid, thiacloprid, clothianidin, nitenpyran, insect growth regulator, juvenile hormone mimic, fermentation insecticide, plant oil insecticide acaracide, miticide, fungicide, herbicide and combinations thereof. The pesticide concentrate is diluted with a hydrocarbon solvent, a white mineral oil or a combination thereof and mixed with water.Type: ApplicationFiled: April 4, 2006Publication date: June 25, 2009Inventors: Yueh Wang, Ian R. Gecker, John Lucas, Ashish Shah
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Publication number: 20090137567Abstract: Methods of treating blood disorders are described.Type: ApplicationFiled: September 17, 2008Publication date: May 28, 2009Applicant: HEMAQUEST PHARMACEUTICALS, INC.Inventors: Susan P. Perrine, Regine Bojacek
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Publication number: 20090137393Abstract: The invention relates to novel 2,4,6-trialkylphenyl-substituted cyclopentane-1,3-diones of the formula (I) in which X, Y, A, B, Q1, Q2 and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the 2,4,6-trialkylphenyl-substituted cyclopentane-1,3-diones of the formula (I) and, secondly, at least one crop plant compatibility-improving compound.Type: ApplicationFiled: January 3, 2007Publication date: May 28, 2009Applicant: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Dieter Feucht, Ulrich Gorgens, Olga Malsam, Alfred Angermann, Guido Bojack, Alan Graff, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Hein Kehne, Christopher Hugh Rosinger, Jan Dittgen
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Publication number: 20090137664Abstract: Compounds and compositions that effectively block hypoxia-inducible factor-1 function, and methods of use thereof. The compounds and compositions of the present invention are useful in the prevention and treatment of cancer, stroke, heart disease, ocular neovascular diseases, and arthritis.Type: ApplicationFiled: October 20, 2008Publication date: May 28, 2009Inventors: Dale G. Nagle, Yu-Dong Zhou, Chowdhury Faiz Hossain, Tyler W. Hodges
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Publication number: 20090118363Abstract: Methods for treating coats and/or body odors of animals are provided. Foods and beverages for nonhuman animals that can be used in the methods are provided. Foods and beverages containing a sesamin-class compound(s) of 1 wt % or above and an additive acceptable as a food or beverage are provided. Methods for treating coats and/or body odors of nonhuman animals comprising administering to the nonhuman animals foods or beverages for nonhuman animals containing an effective amount of the sesamin-class compound(s) needed to treat the coats and/or the body odors of the nonhuman animals are provided. Preferably, the sesamin-class compound(s) are dissolved in fat or oil.Type: ApplicationFiled: April 3, 2007Publication date: May 7, 2009Applicant: SUNTORY LIMITEDInventors: Yukihiro Aoshima, Junko Tsuji
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Patent number: 7524884Abstract: The present invention provides an essentially pure compacted 2,2-Dibromo-3-nitrilopropionamide (DBNPA) in a granular and/or tablet and/or briquette and/or pellet form. The present invention further provides a process for preparing the same essentially pure compacted DBNPA.Type: GrantFiled: September 26, 2001Date of Patent: April 28, 2009Assignee: Bromine Compounds LimitedInventors: Ayala Lupin, legal representative, David Feldman, Michael Lupin
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Publication number: 20090105286Abstract: The invention relates to drugs and the use thereof, wherein said drugs contain compounds selected from a group comprising general formulas (1), (2), (3) and (4) and/or enantiomers, diastereomers or the pharmaceutically acceptable salts thereof. Said drugs are used for treating autoimmune and tumoral diseases and/or for immunosuppresion.Type: ApplicationFiled: November 18, 2005Publication date: April 23, 2009Applicant: Rheinische Friedrich-Wilhelms UniversitatInventors: Michael Famulok, Waldemar Kolanus, Markus Hafner, Imke Grune, Barbara Tappertzhofen, Mirko Theis
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Publication number: 20090054519Abstract: The present invention relates to the use of derivatives of monosaccharides as 5-lipoxygenase inhibitor.Type: ApplicationFiled: July 20, 2006Publication date: February 26, 2009Inventors: Abhijit Ray, Raj Kumar Shirumalla, Kasim Mookhtiar, Viswajanani J. Sattigeri, Venkata Palle, Mohammad Salman
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Patent number: 7491748Abstract: A carboxylic acid derivative of formula (I): wherein R1 is —COOH, —COOR6, etc.; A is a single bond, alkylene, etc.; R2 is alkyl, alkoxy, etc.; B is a carbocyclic ring or a heterocyclic ring; Q is alkylnene-Cyc2, etc.; D is a linking chain; and R3 is alkyl, a carbocyclic ring or a heterocyclic ring, or a non-toxic salt thereof. The compound of formula (I) binds to PGE2 receptor, especially subtypes EP3 and/or EP4 and show the antagonizing activity, are useful for the prevention and/or treatment of diseases induced pain, itch, urticaria, allergy, urinary frequency, urinary disturbance, Alzheimer's disease, cancer, dysmenorrhea, endometriosis, etc.Type: GrantFiled: August 8, 2002Date of Patent: February 17, 2009Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kousuke Tani, Masaki Asada, Kaoru Kobayashi, Masami Narita, Mikio Ogawa
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Publication number: 20090042976Abstract: The disclosure provides a molecular genetic approach of targeted mutagenesis and heterologous expression, coupled with in vitro and in vivo models of bacterial pathogenesis, to demonstrate that the S. aureus pigment is a virulence factor and potential novel target for antimicrobial therapy.Type: ApplicationFiled: April 17, 2006Publication date: February 12, 2009Applicant: The Regents of the University of CalifornisInventors: Victor Nizet, George Y. Liu
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Publication number: 20090035400Abstract: Described herein are compositions comprising a nematicide intermixed with lecithin and a co-surfactant that form stable dispersions in water. Also disclosed are methods of controlling nematodes in soil by application of such compositions.Type: ApplicationFiled: October 15, 2008Publication date: February 5, 2009Inventor: SHIREEN BASEETH
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Publication number: 20090012157Abstract: The invention relates to a novel class of inhibitor of arachidonic acid useful for treating inflammatory conditions. Specifically, the invention relates to hydrophobic and hydrophilic derivatives of sesamol that confer lower toxicity and increased circulatory lifetimes than pure sesamol.Type: ApplicationFiled: February 6, 2007Publication date: January 8, 2009Inventor: Barry D. Sears
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Publication number: 20090004236Abstract: Pesticidal compositions and articles providing topical application of a mixture of (1) a macrolide of the avermectin/milbemycin class, such as, but not limited to ivermectin, abamectin, or milbemectin, and (2) a synergist of the aryl aliphatic ether-class, such as, but not limited to piperonyl butoxide, present in (3) a weight ratio of synergist:macrolide that is great than 1:1. The compositions and articles demonstrate efficacy, even in point-of-contact applications, against various pests of domestic animals, such as, but not limited to arthropod ectoparasites including horn flies and buffalo flies. Methods are provided in which compositions can be employed as pour-ons, spot-ons, dusts, or sprays for direct topical application to the domestic animal; or in which articles comprising a polymer resin base, such as an ear tag, from which the active ingredients of the composition can be released, are affixed to the animal to provide long-term delivery.Type: ApplicationFiled: March 5, 2008Publication date: January 1, 2009Inventor: Joe D. Kellerby
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Patent number: 7470722Abstract: Disclosed herein are carbonyl compounds of Formula I as described herein. Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, central nervous system disorders, neurodegenerative disorders, fibrosis, bone disorders, polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, cardiovascular conditions, and disorders in which angiogenesis play a role in pathogenesis, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.Type: GrantFiled: June 9, 2005Date of Patent: December 30, 2008Assignee: Kalypsys, Inc.Inventors: James William Malecha, Stewart Alwyn Noble, Christian Andreus Hassig, Paul L. Wash, Brandon M. Wiley, Charles Maxwell Lawrence, Timothy Z. Hoffman
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Publication number: 20080319055Abstract: A method of providing a cooling sensation to the skin or the mucous membranes of the body by applying thereto a compound of Formula I in which X is H or (CH2)n—R, n is 0 or 1, Y and Z are selected independently from the group consisting of H, OH, phenyl, C1-C4 straight or branched alkyl, or, a C1-C4 straight or branched alkoxy, or X and Y form together a bivalent radical selected from the group consisting of —O—CH2—O—, —N?CH—O— and —N?CH—S— which forms together with the carbon atoms to which they are attached a 5-membered ring; and R is a group with non-bonding electrons, R1 is H or C1-C5 branched alkyl, R2 and R3 are C1-C4 branched alkyls, or R2 and R3 taken together form a monocyclic, bicyclic or tricyclic radical of up to 10 carbons provided that R1, R2 and R3 together comprise at least 6 carbons. The compounds may be incorporated into products such as dentifrices, foodstuffs, confectionery, beverages, and cosmetic and medicinal preparations.Type: ApplicationFiled: March 15, 2006Publication date: December 25, 2008Applicant: GIVAUDAN SAInventors: Lucienne Cole, Stefan Michael Furrer, Christophe C. Galopin, Pablo Victor Krawec, Jay Patrick Slack
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Patent number: 7453010Abstract: The invention relates to compounds of general formula (I): where R1 represents H or a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl optionally being substituted; R2 represents H, a halogen atom, an —S(O)z(C1-C4)alkyl group, where z is equal to 0, 1 or 2, an —NHSO2(C1-C4)alkyl group, an —NHSO2-phenyl group or an —NHSO2—(C1-C4)alkylphenyl group, said phenyl optionally being substituted; R3 represents an —X—R4 group—in which X represents a bond, an oxygen atom or a —CH2— group and R4 represents H or a —CR5R6—COOR7 group, where R5, R6 and R7 independently represent H or a (C1-C4)alkyl group—a phenyl group optionally substituted or fused with a dioxolane group, a —CO—NR8R9 group—where R8 represents H, a (C1-C4)alkyl group or a (C1-C4)alkyl(C1-C4)alkoxy group and R9 represents a (C1-C4)alkyl(C1-C4)alkoxy group, a —(CH2)n-A group, where n is equal to 0, 1, 2, 3 or 4 and where A represents an indolyl group, a fluorenyl group or a phenyl group which is substituted, an optionaType: GrantFiled: May 26, 2003Date of Patent: November 18, 2008Assignee: Sanofi AventisInventors: Philippe R. Bovy, Roberto Cecchi, Tiziano Croci, Olivier Venier
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Patent number: 7452556Abstract: The present invention relates to compositions for the treatment of pilosebaceous gland inflammations, especially of the hair follicle and its appendages, in particular of Acne Vulgaris and Folliculitis, comprising as active ingredient AIF or chemical compounds which finally release AIF, or combinations of aluminum and fluoride salts which finally release AIF. AIF in accordance with the present invention relates to Aluminum fluoride (Aluminum Trifluoride; Aluminum Fluoride), CAS No 7784-18-1, EINECS No. 232-051-1, having an empirical formula of AIF3. Said compositions have, inter alia, pharmaceutical, cosmetic or quasi-cosmetic properties. The present invention also relates to the use of said compositions in said treatment, and to methods for the treatment of pilosebaceous gland inflammations with said compositions.Type: GrantFiled: October 2, 2002Date of Patent: November 18, 2008Assignee: Medidermis Ltd.Inventor: Avi Dascalu
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Publication number: 20080275111Abstract: The present invention relates to the novel use of lignan compounds represented by Formula I. More particularly, the present invention relates to a pharmaceutical composition for treating or preventing a brain disease, comprising a lignan compound represented by Formula I or a Myristica fragrans extract as an active ingredient, as well as the method and use for treating or preventing a brain disease using the lignan compound. The lignan compound represented by Formula I has the effects of antioxidation, brain cell protection and antiinflammation. Accordingly, said lignan compound will be highly useful for treating or preventing a brain disease.Type: ApplicationFiled: March 31, 2006Publication date: November 6, 2008Inventors: Jae-Kwan Hwang, Jung-Soo Han, Chol-Seung Lim, Daqing Jin, Sun-Hee Lee, Kyu-Lee Han
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Publication number: 20080275110Abstract: Sesamin and episesamin are incorporated at specified weight ratios in oral compositions so that the oral absorption of episesamin and/or its transfer into blood circulation is increased. Sesamin and episesamin are also incorporated at specified weight ratios in oral compositions so that the physiological activities of sesamins are enhanced.Type: ApplicationFiled: December 28, 2005Publication date: November 6, 2008Inventors: Yoshiko Ono, Namino Tomimori, Saki Tokuda, Tomohiro Rogi
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Patent number: 7442718Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: July 2, 2003Date of Patent: October 28, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R Hale, Christopher T Baker, Timothy A Stammers, Ronald G Sherrill, Andrew Spaltenstein, Eric S Furfine, Francois Maltais, Clarence W Andrews, III, John F Miller, Vicente Samano
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Patent number: 7438923Abstract: Synergistic and residual pesticidal compositions containing synergistic and residual mixtures of plant essential oils in admixture with enzyme inhibitors, with or without other compounds not previously used as active ingredients in pesticidal formulations. In addition, the present invention is directed to a method for controlling pests by applying a pesticidally-effective amount of the above synergistic and residual pesticidal compositions to a locus where pest control is desired.Type: GrantFiled: October 31, 2005Date of Patent: October 21, 2008Assignee: Ecosmart Technologies, Inc.Inventor: Steven M. Bessette
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Publication number: 20080214661Abstract: A process to obtain dibenzylbutyrolactonic lignans from (-)-cubebin, isolated from a Piperaceae, especially Piper cubeba, and from (-)-methylpluviatolide, isolated from a Rutacea, especially Zanthoxylum naranjillo; their synthetic and semi-synthetic derivatives and tetrahydrofuranic lignans, such as galgravin and veragensin, isolated from Nectandra megapotamica, as well as the analgesic and anti-inflammatory activities of said lignans, and the topical and/or systemic formulations. Also presented is a therapeutic method using topic and/or systemic formulations based on said lignans for the treatment of inflammation and/or pain.Type: ApplicationFiled: April 28, 2006Publication date: September 4, 2008Applicant: FUNDACADO DE AMPARO A PESQUISA DO ESTADO DE SAO PAULOInventors: Marcio Luis Andrade e Silva, Jairo Kenupp Bastos, Paulo Marcos Donate, Sergio de Albuquerque, Rosangela da Silva
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Publication number: 20080194678Abstract: A process to obtain synthetic and semi-synthetic derivatives of lignans, especially dibenzylbutyrolactonic, tetrahydrofuranic, aryltetralynic, furofuranic and dibenzocyclooctanic lignans obtained by means of partial synthesis and/or full synthesis or also by isolation from plant extracts. It refers to a process to obtain synthetic and semi-synthetic derivatives of (?)-cubebin, such as: (?)-O-acetylcubebin; (?)-O-methylcubebin; (?)-O—N,N-(dimethylamino-ethyl)-cubebin; (?)-hinokinin; (?)-6,6?-dinitroinokinine; (?)-O-benzylcubebin; (?)-6,6?-diaminoinokinin, (?)-6,6?-dinitroinokinin, as well as to obtain dibenzocyclooctanic lignans from dibenzylbutyrolactoinic lignans by means of structural modifications in the positions 7, 7?, 8, 8?, 9? and in the aromatic rings (introduction and/or substitution of functional groups such as: —OH, —CO2H, —CO2CH3, —NO2, —NH2, —OCH3, —OAc, —SO2CH3, —SO2NH2, prenyl and halogens) is provided. A therapeutic method using the derivatives is also provided.Type: ApplicationFiled: July 14, 2006Publication date: August 14, 2008Applicant: Fundacao de Amparo a Pesquissa do Estado de Aao PaInventors: Marcio Luis Andrade e Silva, Rosangela da Silva, Vanderlei Rodrigues, Olavo dos Santos Pereira, Ademar Alves da Silva Filho, Paulo Marcos Donate, Sergio Albuquerque, Jairo Kenupp Bastos
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Publication number: 20080161387Abstract: The present invention provides new salts and/or addition compounds and/or complex compounds of guanidinoacetic acid with malic acid, aspartic acid, ascorbic acid, succinic acid, pyruvic acid, fumaric acid, gluconic acid, ?-ketoglutaric acid, oxalic acid, pyroglutamic acid, 3-nicotinic acid, lactic acid, citric acid, maleic acid, sulfuric acid, acetic acid, formic acid, 2-hydroxybenzoic acid, L-carnitine, acetyl-L-carnitine, taurine, betaine, choline, methionine and lipoic acid as well as in the form of sodium, potassium or calcium guanidinoacetate. These salts have improved physiological and therapeutic properties and are particularly suitable for use as dietary supplements, as animal feeds and in cosmetic or dermatological preparations in which especially the marked stability and good bioavailability of the salts come to the fore.Type: ApplicationFiled: March 2, 2006Publication date: July 3, 2008Inventors: Thomas Gastner, Hans-Peter Krimmer
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Publication number: 20080146445Abstract: The present invention concerns nematicidal compounds, their formulation as nematicidal composition and their use for controlling nematodes, preferably plant parasitic nematodes.Type: ApplicationFiled: December 16, 2005Publication date: June 19, 2008Applicant: Devgen NVInventors: Jan Octaaf De Kerpel, Dirk Leysen
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Publication number: 20080103195Abstract: The present invention relates a compound for inhibiting the growth of tumor cells. More specifically, the compound of the present invention is 4,7-dimethoxy-5-methy-1,3-benzodioxole. 4,7-dimethoxy-5-methy-1,3-benzodioxole of the present invention is used for inhibiting the growth of tumor cells of breast cancer, liver cancer, and prostate cancer, and the pharmaceutical composition comprises an effective dose of 4,7-dimethoxy-5-methy-1,3-benzodioxole.Type: ApplicationFiled: May 16, 2007Publication date: May 1, 2008Inventors: Sheng-Yun Liu, Wu-Che Wen, Wan-Ling Tsou, Mao-Tien Kuo
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Patent number: 7357939Abstract: Synergistic and residual pesticidal compositions containing synergistic and residual mixtures of plant essential oils in admixture with enzyme inhibitors, with or without other compounds not previously used as active ingredients in pesticidal formulations. In addition, the present invention is directed to a method for controlling pests by applying a pesticidally-effective amount of the above synergistic and residual pesticidal compositions to a locus where pest control is desired.Type: GrantFiled: October 31, 2005Date of Patent: April 15, 2008Assignee: Ecosmart Technologies, Inc.Inventor: Steven M. Bessette
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Patent number: 7345068Abstract: 1. An aromatic amino acid derivative represented by the formula (I) or its pharmacologically acceptable salt: wherein, R1 is a hydrogen atom or an amino-protecting group, R2 is a halogen atom or an alkyl, aralkyl or aryl group, R3 is {circle around (1)} a hydrogen atom, {circle around (2)} an aroylamino group, {circle around (3)} a phenyl group substituted with lower alkyl, phenyl, phenoxy, etc. {circle around (4)} a naphthyl or tetrahydronaphthyl group optionally substituted with hydroxy, lower alkoxy or di(lower)alkylamino, {circle around (5)} an unsaturated mono-cyclic heterocyclic group containing N, O and/or S substituted with lower alkyl, phenyl, naphthyl or tetrahydroquinolyl, {circle around (6)} an unsaturated or partially saturated condensed heterocyclic group containing N, O and/or S, optionally substituted with oxo, carboxy, amino, lower alkyl, etc.; X is a halogen atom, an alkyl group or an alkoxy group; Y is oxygen atom or nitrogen atom; l is 0 or 1; m is 0, 1 or 2; n is an integer of 0-5.Type: GrantFiled: February 3, 2003Date of Patent: March 18, 2008Inventors: Hitoshi Endou, Yoshikatsu Kanai, Kenji Tsujihara, Kunio Saito
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Patent number: 7339078Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, compositions, and methods for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: August 10, 2006Date of Patent: March 4, 2008Assignee: G.D. Searle LLCInventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 7323452Abstract: A method for accelerating the process of removing ethanol from the blood through the use of certain additives that accelerate the metabolic oxidation of ethanol, and others which in addition act as catalysts or “pseudo” enzymes for the oxidation. These additives include multivalent transition metal ions, as well as complexes thereof, and NAD+ which enhance the oxidation reaction. The method described can act as a sobriety inducer and/or as an effective palliative for the unpleasant effects of overuse of ethanol.Type: GrantFiled: December 20, 2004Date of Patent: January 29, 2008Assignee: Wardan, L.L.C.Inventors: Ward B. Bowen, Jr., Daniel S. Daniel
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Publication number: 20070231413Abstract: Containing the 1,3-benzodioxol compound represented by the formula (I): together with a pesticidal active ingredient in a pesticidal composition enhances a pest control effect of the pesticidal composition.Type: ApplicationFiled: March 15, 2007Publication date: October 4, 2007Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Noritada MATSUO, Hiroshi OKAMOTO
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Patent number: 7265130Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: December 30, 2003Date of Patent: September 4, 2007Assignee: Shionogi & Co., Ltd.Inventors: Yasuyuki Kawanishi, Hideyuki Takenaka, Kohji Hanasaki, Tetsuo Okada
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Patent number: 7256204Abstract: A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO2—, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc.Type: GrantFiled: August 21, 2003Date of Patent: August 14, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Kaneyoshi Kato, Jun Terauchi, Hiroaki Fukumoto, Mitsuru Kakihana
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Patent number: 7256218Abstract: Biguanide and dihydrotriazine derivatives, preferably substituted asymmetrical imidodicarbonimidic diamides derived from hydroxylamines, and compositions containing biguanide and dihydrotriazine derivatives are disclosed. In addition, methods of using the biguanide and dihydrotriazine derivatives, inter alia, as antimicrobial agents and methods of using the dihydrotriazine derivatives in biological assays are disclosed. Methods of making the biguanide and dihydrotriazine derivatives are also disclosed.Type: GrantFiled: November 18, 2003Date of Patent: August 14, 2007Assignee: Jacobus Pharmaceutical Company, Inc.Inventors: David P. Jacobus, Guy A. Schiehser, Hong-Ming Shieh, Norman P. Jensen, Jacek Terpinski
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Patent number: 7220752Abstract: This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in therapy and in the regulation of metabolism, especially lowering blood glucose levels. The compounds referred to are compounds according to the formula 1: wherein the variables are as defined herein.Type: GrantFiled: November 28, 2001Date of Patent: May 22, 2007Assignees: Karo Bio AB, Abbott LaboratoriesInventors: Benjamin Pelcman, Annika Gustafsson, Philip R. Kym
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Patent number: 7192965Abstract: Compounds of formula wherein A1, A2 and A3 are each independently of the others a bond or a C1–C6alkylene bridge; A4 is a C1–C6alkylene bridge; D is CH or N; W is, for example, O, NR7 or S; T is, for example, a bond, O, NH or NR7; Q is O, NR7, S, SO or SO2; Y is O, NR7, S, SO or SO2; X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, CN, nitro, C1–C6alkyl, C1–C6haloalkyl, C1–C6alkylcarbonyl or C2–C6alkenyl; R4 is, for example, H, halogen, CN, nitro or C1–C6alkyl; R5 and R6 are, for example, H, CN, OH, C1–C6alkyl, C3–C8cycloalkyl, C3–C8cycloalkyl-C1–C6alkyl, C1–C6haloalkyl, C1–C6alkoxy or C1–C6haloalkoxy; R7 is H, C1–C6alkyl, C1–C6alkoxyalkyl or C1–C6alkylcarbonyl; k, when D is nitrogen, is 1, 2 or 3; or, when D is CH, is 1, 2, 3 or 4; and m is 1 or 2; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtures and/or tautomers, in each case in free form or in salt form, a process for the preparation of those compounds andType: GrantFiled: June 27, 2003Date of Patent: March 20, 2007Assignee: Syngenta Crop Protection, Inc.Inventors: Werner Zambach, Peter Renold, Arthur Steiger, Stephan Trah, Roger Graham Hall
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Patent number: 7157495Abstract: Compositions comprising bis-tetrahydrofuran benzodioxyolyl sulfonamide compounds that are surprisingly effective protease inhibitors and a second antiretroviral compound are disclosed. Methods of inhibiting retrovirus proteases, in particular multi-drug resistant retrovirus proteases, methods of treating or preventing infection or disease associated with retrovirus infection in a mammal, and methods of inhibiting viral replication are also disclosed.Type: GrantFiled: June 25, 2003Date of Patent: January 2, 2007Assignees: Tibotec Pharmaceuticals, Ltd., The United States of America as represented by the Department of Health and Human ServicesInventors: Guangyang Wang, Michael Eissenstat, John W. Erickson, Piet T. B. P. Wigerinck
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Patent number: 7148242Abstract: N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl]-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes or imidazacyclo4-7alkanes have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by peptidyl deformylase inhibitors such as treatment of bacterial infections.Type: GrantFiled: June 14, 2002Date of Patent: December 12, 2006Assignee: Novartis AGInventors: Jeffrey Jacobs, Rakesh K. Jain, Dinesh V. Patel, Zhengyu Yuan
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Patent number: 7078431Abstract: It has been discovered certain 1,3-bis-(substituted-phenyl)-2-propen-1-ones, including compounds of formula (I) inhibit the expression of VCAM-1, and thus can be used to treat a patient with a disorder mediated by VCAM-1. Examples of inflammatory disorders that are mediated by VCAM-1 include, but are not limited to arthritis, asthma, dermatitis, cystic fibrosis, post transplantation late and chronic solid organ rejection, multiple sclerosis, systemic lupus erythematosis, inflammatory bowel diseases, autoimmune diabetes, diabetic retinopathy, rhinitis, ischemia-reperfusion injury, post-angioplasty restenosis, chronic obstructive pulmonary disease (COPD), glomerulonephritis, Graves disease, gastrointestinal allergies, conjunctivitis, atherosclerosis, coronary artery disease, angina and small artery disease.Type: GrantFiled: May 21, 2003Date of Patent: July 18, 2006Assignee: Atherogenics, Inc.Inventors: Charles Q. Meng, Liming Ni, James A. Sikorski, Lee K. Hoong
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Patent number: 7078057Abstract: Nanometer particles of poorly water-soluble or substantially water-insoluble compound are produced by finely-spraying a non-aqueous solution of said compound into a heated and fluidized bed of carrier excipient. The resulting product consists of a free flowing mixture of relatively large particles of carrier excipient and nanometer sized particles (less than 3 ?m)) of compound.Type: GrantFiled: December 19, 2000Date of Patent: July 18, 2006Inventor: Nicholas J. Kerkhof
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Patent number: 7045518Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: October 3, 2003Date of Patent: May 16, 2006Assignee: G.D. Searle & Co.Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, Joseph J. McDonald
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Patent number: 7037914Abstract: A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.Type: GrantFiled: September 23, 2002Date of Patent: May 2, 2006Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Tajima, Yoshisuke Nakayama, Daikichi Fukushima
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Patent number: 7019028Abstract: The invention relates to compounds of the formula (I) process for their preparation starting from the plant Beilschmiedia fulva, PLA 101037, and the use thereof for producing a medicament, in particular for the treatment of allergic disorders, of asthmatic disorders, of inflammatory concomitant symptoms of asthma and/or of diseases which can be treated by inhibiting c-maf and NFAT.Type: GrantFiled: July 25, 2003Date of Patent: March 28, 2006Assignees: Aventis Pharma Deutschland GmbH, Aventis Pharmaceuticals Inc.Inventors: Claudia Eder, Herbert Kogler, Sabine Haag-Richter
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Patent number: 6974832Abstract: The invention relates to compositions in the form of a powder or granules containing L-ascorbic acid and/or a pharmaceutically acceptable salt thereof, and pectin in a quantity within the range of about 0.1 to about 10% by weight.Type: GrantFiled: December 15, 2000Date of Patent: December 13, 2005Assignee: DSM Nutritional Products Inc.Inventors: Chyi-Cheng Chen, Bruno Leuenberger, Denise Voelki
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Patent number: 6964968Abstract: Viral infections selected from the group consisting of herpes simplex virus, varicella zoster virus, respiratory syncytial virus and cytomegalovirus can be treated by administering to the host a therapeutically effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof; wherein Y, Ra, and R1 are as defined herein. The compounds and salts can also be used to inhibit viral replication of these viruses in cells.Type: GrantFiled: March 31, 2003Date of Patent: November 15, 2005Assignee: Shire Biochem, Inc.Inventors: Francis J. Giles, Jean Bédard, Robert F. Rando
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Patent number: 6946462Abstract: New compounds represented by the formula or pharmaceutically acceptable salts or prodrugs thereof, wherein X1 and X2 are each independently selected from a CH group or a nitrogen atom; and R is an optionally substituted five or six membered nonaromatic carbocyclic ring or a nonaromatic or aromatic heterocyclic ring, whereby the ring is optionally condensed with a 6-membered, optionally substituted carbocyclic aromatic ring.Type: GrantFiled: April 13, 2004Date of Patent: September 20, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Rainer Haag, Ulrike Leser-Reiff, Anja Limberg, Michael Weidner, Gerd Zimmermann
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Patent number: 6943182Abstract: The invention relates to cyclopentabenzofuran derivatives, process for their preparation, the use of cyclopentabenzofuran derivatives for the production of a medicament for the therapy of NF-?B-dependent diseases and medicaments which contain the cyclopentabenzofuran derivatives.Type: GrantFiled: May 30, 2002Date of Patent: September 13, 2005Assignee: Bayer AktiengesellschaftInventors: Walter Guarnieri, Thomas Jaetsch, Andreas Schoop, Jörg Baumgarten, Axel Kretschmer, Horst-Peter Antonicek
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Patent number: 6894074Abstract: The invention relates to insecticidal mixtures comprising compounds of the formula (I) in which X?, Y?, Z?, n, G?, A? and B? are as defined above and agonists and/or antagonists of nicotinic acetylcholine receptors, for protecting plants against attack by pests.Type: GrantFiled: September 29, 2003Date of Patent: May 17, 2005Assignee: Bayer AktiengesellschaftInventors: Thomas Bretschneider, Reiner Fischer, Christoph Erdelen, Ernst Brück