Z Radical Contains Sulfur Or Halogen Patents (Class 514/550)
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Publication number: 20100323990Abstract: The present invention provides the use of prodrugs of pelorol and homopelorol, related compounds and pharmaceutical compositions thereof as modulators of SHIP1 activity. A compound or a pharmaceutical composition of the present invention may be used for the treatment or prophylaxis of an inflammatory, neoplastic, hematopoetic or immune disorder or condition in addition to other disorders and conditions.Type: ApplicationFiled: June 21, 2007Publication date: December 23, 2010Applicant: THE UNIVERSITY OF BRITISH COLUMBIAInventors: Raymond Andersen, Matthew Nodwell, Alice Mui
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Publication number: 20100311791Abstract: The present invention relates to active bactericidal, antibacterial, anti-infective, antimicrobial, sporicidal, disinfectant, antifungal and antiviral compounds and compositions and to new uses of these compositions in therapy. This specification also describes methods of use for the new compounds and compositions. The specification further describes methods for preparing these compounds.Type: ApplicationFiled: December 28, 2007Publication date: December 9, 2010Inventors: Ramin Najafi, Rakesh K. Jain, Timothy P. Shiau, Eddy Low, Satheesh K. Nair
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Publication number: 20100280113Abstract: The invention is directed to novel pharmaceutical compositions comprising chemicals agents that are useful in the treatment and prevention of cystic fibrosis and the prevention of signs and symptoms of this disease. These pharmaceutical compositions are surprisingly successful in the treatment disorders related to cystic fibrosis including disorders of blood production. Many of these compositions of the invention are even more effective when administered to a patient in pulses. Pulse therapy is not a form of discontinuous administration of the same amount of a composition over time, but comprises administration of the same dose of the composition at a reduced frequency or administration of reduced doses.Type: ApplicationFiled: July 14, 2010Publication date: November 4, 2010Applicant: TRUSTEES OF BOSTON UNIVERSITYInventors: Douglas V. Faller, Susan P. Perrine, George Stamatoyannopoulos
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Publication number: 20100247462Abstract: Processes for synthesizing resveratrol-based oligomers are provided. In addition, resveratrol-based oligomer compounds free of plant extract are provided.Type: ApplicationFiled: September 17, 2008Publication date: September 30, 2010Inventors: Scott Alan Snyder, Steven P. Breazzano, Audrey G. Ross, Yunqing Lin, Alexandros L. Zografos
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Patent number: 7795308Abstract: By using a composition for preventing onset and/or recurrence of stroke which contains ethyl icosapentate as its effective component, onset and/or recurrence of stroke is prevented, or in particular, the onset and/or recurrence of stroke in a hyperlipidemia patient who has been treated with HMG-CoA RI, or in particular the recurrence of stroke in a patient who is beyond six months after the onset of stroke, is prevented.Type: GrantFiled: December 24, 2008Date of Patent: September 14, 2010Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Mitsuhiro Yokoyama, Hideki Origasa, Masunori Matsuzaki, Yuji Matsuzawa, Yasushi Saito
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Publication number: 20100221220Abstract: The present invention relates to methods of treating a cancerous tumor using selective inhibitors of ATP production. The present invention also relates to pharmaceutical preparations comprising such inhibitors and methods for administering them intraarterially directly to a tumor, as well as methods for identifying compositions that selectively inhibitor ATP production for use in the invention.Type: ApplicationFiled: June 15, 2009Publication date: September 2, 2010Inventor: Young Hee Ko
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Patent number: 7776913Abstract: L-carnitine, propionyl L-carnitine and/or acetyl L-carnitine are used to prevent or treat disorders of male andropause caused by ageing or by chemical or surgical castration.Type: GrantFiled: March 14, 2008Date of Patent: August 17, 2010Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Aleardo Koverech, Giulio Biagiotti, Giorgio Cavallini
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Publication number: 20100190753Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-+related disease.Type: ApplicationFiled: August 27, 2009Publication date: July 29, 2010Applicant: BELLUS Health (International) LimitedInventors: Xianqi KONG, Walter A. Szarek, Francine Gervais
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Patent number: 7754679Abstract: Pharmaceutical compositions comprising an aptamer and an amino acid ester or amide or an aptamer; a divalent metal cation; and a carboxylic acid, a phospholipid, a phosphatidyl choline, or a sphingomyelin. Methods of treating or preventing a condition in an animal comprising administering to the animal the pharmaceutical compositions.Type: GrantFiled: April 10, 2006Date of Patent: July 13, 2010Assignee: IDEXX Laboratories, Inc.Inventor: Yerramilli V. S. N. Murthy
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Publication number: 20100173781Abstract: A method for modulating the release rate of microencapsulated active ingredients comprising the following steps: I) preparation of an aqueous suspension A) comprising microcapsules of at least one active ingredient, II) preparation of a liquid emulsifiable in water, component B), comprising a solvent of the active ingredient and at least a surfactant, III) water, component C), for diluting to the application dose the active ingredient, and mixing A), B) and C).Type: ApplicationFiled: June 27, 2008Publication date: July 8, 2010Applicant: ENDURA S.p.A.Inventors: Carlotta Gobbi, Lucio Bassetti, Valerio Borzatta, Marco Bernardini, Francesca Borgo, Luigi Capuzzi
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Publication number: 20100160430Abstract: There is provided an organic sulfur compound having an excellent controlling effect on harmful arthropods represented by the formula (I): wherein, R1 represents a C1-C5 haloalkyl group having at least one fluorine atom, R2 represents a C1-C4 alkyl group optionally substituted with at least one halogen atom or the like, R3 represents a hydrogen atom or the like, R4 represents a cyano group or the like, R5 represents a hydrogen atom or the like, m represents an integer of 1 to 4, and n represents 0, 1 or 2.Type: ApplicationFiled: May 16, 2008Publication date: June 24, 2010Inventor: Hiroyuki Miyazaki
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Publication number: 20100160434Abstract: There is provided an organic sulfur compound having an excellent controlling effect on harmful arthropods represented by the formula (I): wherein, R1 represents a C3-C10 alkenyl group optionally substituted with at least one halogen atom, a C3-C10 alkynyl group optionally substituted with at least one halogen atom, or the like, R2 represents a cyano group or the like, R3 represents a hydrogen atom, a halogen atom or a C1-C4 alkyl group, R4 represents a C1-C5 fluoroalkyl group, and n represents 0, 1 or 2.Type: ApplicationFiled: May 16, 2008Publication date: June 24, 2010Inventor: Hiroyuki Miyazaki
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Publication number: 20100152289Abstract: There is provided an organic sulfur compound having an excellent controlling effect on harmful arthropods which is represented by formula (I): wherein R1 represents a C3-C6 haloalkyl group having at least one fluorine atom and at least one atom selected from group consisting of a chlorine atom, a bromine atom and an iodine atom, R2 represents a cyano group and the like, R3 represents a hydrogen atom, a halogen atom or a C1-C4 alkyl group, R4 represents a C1-C5 fluoroalkyl group, and n represents 0, 1 or 2.Type: ApplicationFiled: May 18, 2008Publication date: June 17, 2010Inventor: Hiroyuki Miyazaki
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Publication number: 20100144671Abstract: Bromoacetoxycalcidiol (B3CD), which is structurally related to calcidiol, exhibits cytotoxic and apoptotic activity toward cancer cells, including highly aggressive neuroblastoma cells. A series of small molecules designed around the structure of B3CD is expected to have growth inhibitory and apoptogenic activities toward a wide range of malignancies. B3CD shows no apparent toxicity in vivo, indicating potential value as a chemotherapeutic agent which will be particularly useful in treating highly aggressive tumors.Type: ApplicationFiled: March 3, 2006Publication date: June 10, 2010Applicant: Women and Infants Hospital of RI, Inc.Inventors: Narasimha Swamy, Hema Malini K. Sundaresha
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Publication number: 20100093671Abstract: The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.Type: ApplicationFiled: December 11, 2009Publication date: April 15, 2010Inventors: Richard A. EARL, Maiko EZAWA, Xinqin FANG, David S. GARVEY, Ricky D. GASTON, Subhash P. KHANAPURE, L. Gordon LETTS, Chia-En LIN, Ramani R. RANATUNGE, Stewart K. RICHARDSON, Joseph D. SCHROEDER, Cheri A. STEVENSON, Shiow-Jyi WEY
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Publication number: 20090281109Abstract: The present invention provides cysteine and cystine prodrugs for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing prodrugs and methods of using the prodrugs and compositions for treatment of schizophrenia and drug addiction.Type: ApplicationFiled: February 9, 2009Publication date: November 12, 2009Inventors: James M. Cook, David A. Baker, Wenyuan Yin, Edward Merle Johnson, II
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Publication number: 20090215708Abstract: Methods of treating a subject for sexual dysfunction are provided. Aspects of the methods include administering to the subject an effective amount of a proton pump agonist. Aspects of the invention further include proton pump agonist compositions employed in methods of the invention.Type: ApplicationFiled: February 18, 2009Publication date: August 27, 2009Inventor: Bradley Stuart Galer
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Publication number: 20090186941Abstract: A compound given by the formula (I): has an excellent controlling activity against noxious arthropods.Type: ApplicationFiled: November 1, 2006Publication date: July 23, 2009Inventor: Hiroyuki Miyazaki
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Publication number: 20090156674Abstract: The invention relates to the production of a new salt form of valnemulin, a compound of formula I, which is notable for its good crystallinity in higher purity, its simpler technical usability and improved storage stability.Type: ApplicationFiled: January 26, 2006Publication date: June 18, 2009Inventors: Ingolf Macher, Annett Geissler, Susanne Christine Wieland-Berghausen, Uwe Thomas Schote, Ferenc Jozsef Rakoczi
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Publication number: 20090155240Abstract: The present invention provides compositions and methods for using cardioprotective or hemodynamic drugs in combination with dichloroacetate enabling usage of cardioprotective or hemodynamic drugs at concentrations higher than used in normal clinical practice without increasing deleterious side effects normally associated with the cardioprotective or hemodynamic drug, thereby conferring added clinical benefit. The present invention teaches administration of DCA with cardioprotective or hemodynamic drugs as an adjunct therapy thereby conferring added clinical benefit to clinically recommended protocols.Type: ApplicationFiled: February 20, 2009Publication date: June 18, 2009Applicant: THE GOVERNORS OF THE UNIVERSITY OF ALBERTA TEC EdmontonInventors: GARY D. LOPASCHUK, Ruth L. Collins-Nakai
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Publication number: 20090143467Abstract: Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.Type: ApplicationFiled: September 4, 2008Publication date: June 4, 2009Inventors: Seth D. Rose, Scott R. Lefler, Steven R. Ottersberg, Ann Y. Kim, Karl J. Okolotowicz, Rosemarie F. Hartman
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Publication number: 20090028791Abstract: A compound having structure I: wherein xC is selected from the group consisting of 11C, 12C, and 13C; R is selected from the group consisting of —OH, —O?R4+ wherein R4 is selected from the group consisting of Na and K, —OR3 wherein R3 is selected from the group consisting of C1-8 alkyl and C1-8 alkenyl, —NH2, and NHR3; R? is selected from the group consisting of —H, —Cl, —F, —Br, and —I; R? is selected from the group consisting of —H, —Cl, —F, —Br, and —I; and R?? is selected from the group consisting of —H, —Cl, —F, —Br, —I, 18F, 19F, 75Br, 76Br, 77Br, 123I, 124I, and 131I; provided, when xC is 12C, R?? is selected from the group consisting of 18F, 19F, 75Br, 76Br, 77Br, 123I, 124I, and 131I.Type: ApplicationFiled: July 24, 2008Publication date: January 29, 2009Inventors: Julius A. Balatoni, Louis R. DePalatis, William Tong, Juri Gelovani
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Publication number: 20080269172Abstract: The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.Type: ApplicationFiled: April 4, 2008Publication date: October 30, 2008Inventors: Brent Richard Stranix, Valerie Perron
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Publication number: 20080153906Abstract: The present invention discloses pharmaceutical compositions containing a suspension of a therapeutically effective amount of a water-soluble prodrug of a phenicol in a lipophilic vehicle system.Type: ApplicationFiled: December 11, 2007Publication date: June 26, 2008Inventors: Chander S. Celly, Keith A. Freehauf
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Patent number: 7385086Abstract: This invention provides compounds and methods for treating, with said compound, a mycobacterial infection by administering to an animal a pharmaceutical composition containing a compound having the formula R—SOn-Z-CO—Y, where R is an alkyl groups having 6-20 carbon atoms, unsaturated hydrocarbon groups having 6-20 carbon atoms, or alkyl groups having 6-20 carbon atoms interrupted by at least one aromatic ring; Z is —CH2—, —CH2CH2—, —NH—NH—, —O—, ——NH—, —O—NH—, —CH2—NH—, —CH2—O—, —NH—O—, —NH—CH2—, —O—CH2—, and —CH?CH—; Y is —NH2, —O—CH2—C6H5, —CO—CO—O—CH3, and —O—CH3; and n is 1 or 2. It has been discovered that these compounds treat microbially-based infections caused by corynebacteria, nocardiae, rhodococcus, and mycobacteria. These compounds may be used to treat mycobacterial cells, such as Mycobacteria tuberculosis, drug resistant M. tuberculosis, M. avium intracellulare, M. leprae, M. paratuberculosis, and pathogenic Mycobacteria sp.Type: GrantFiled: January 27, 2004Date of Patent: June 10, 2008Assignee: The Johns Hopkins University School of MedicineInventors: Craig A. Townsend, James D. Dick, Gary R. Pasternack, Francis P. Kuhajda, Nicole M. Parrish
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Patent number: 7378443Abstract: A fatty acid analogue of the general formula: R1-[xi-CH2]n—COOR2, wherein R1 is: a C2-C24 alkene with one or more double bonds and/or with one or more triple bonds, and/or a C2-C24 alkyne, and/or a C1-C24 alkyl, or a C1-C24 alkyl substituted in one or several positions with one or more compounds selected from the group comprising fluoride, chloride, hydroxy, C1-C4 alkoxy, C1-C4 alkylthio, C2-C5 acyloxy or C1-C4 alkyl, and wherein R2 represents hydrogen or C1-C4 alkyl, and wherein n is an integer from 1 to 12, and wherein i is an odd number and indicates the position relative to COOR2, and wherein Xi independent of each other are selected from the group comprising O, S, SO, SO2, Se and CH2, and with the proviso that at least one of the Xi is not CH2, and or a salt, prodrug or complex thereof is used in the treatment and/or prevention of primary and secondary metastatic neoplasms.Type: GrantFiled: July 13, 2001Date of Patent: May 27, 2008Assignee: Thia Medica, ASInventor: Rolf Berge
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Patent number: 7294651Abstract: Methods and compositions for inhibiting the production of exotoxins are disclosed. The compositions include an effective amount of an isoprenoid inhibitory compound to substantially inhibit the production of exotoxins by Gram positive bacteria.Type: GrantFiled: July 27, 2004Date of Patent: November 13, 2007Assignee: Kimberly-Clark Worldwide, Inc.Inventors: Rae Ellen Syverson, Richard A. Proctor
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Patent number: 7230029Abstract: The present invention relates to fatty acid analogues of the general formula (I): R1-[xi-CH2]n—COOR2 wherein R1 is; a C1–C24 alkene with one or more double bonds and/or with one or more triple bonds, and/or a C1–C24 alkyne, and/or a C1–C24 alkyl, or a C1–C24 alkyl substituted in one or several positions with one or more compounds selected from the group comprising fluoride, chloride, hydroxy, C1–C4 alkoxy, C2–C4 alkylthio, C1–C5 acyloxy or C1–C4 alkyl, and wherein R2 represents hydrogen or C1–C4 alkyl, and wherein n is an integer from 1 to 12, and wherein i is an odd number and indicates the position relative to COOR2, and wherein Xi independent of each other are selected from the group comprising O, S, SO, SO2, Se and CH2, and with the proviso that at least one of the Xi is not CH2, and with the proviso that if R1 is an alkyne or alkene, then the carbon-carbon triple bond or double bond is positioned between the (?-1) carbon and the (?-2) carbon, or between the (?-2) carbon and the (?-3) carbon, or between tType: GrantFiled: September 27, 2001Date of Patent: June 12, 2007Assignee: Thia Medica ASInventors: Rolf Berge, Karsten Kristiansen
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Patent number: 7199156Abstract: A method to treat an animal, including a human, having a solid tumor. The method provides a lipophilic lathyrogen. The method administers a therapeutically effective amount of the lipophilic lathyrogen within the solid tumor.Type: GrantFiled: October 10, 2003Date of Patent: April 3, 2007Inventor: Milos Chvapil
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Patent number: 7105570Abstract: Objects of the present invention are to provide an oxidative stress inhibitor which is capable of suppressing the expression of a cytotoxic protein and the activation of a gene transcriptional regulatory factor taking part such expression of a cytotoxic protein and exhibits good feeling upon use and safety; to provide a method for preventing, retarding, alleviating or treating a skin change due to aging or an undesirable aesthetic skin change, both caused or promoted by an oxidative stress; and to provide a cosmetic composition or dermatologic preparation for external use comprising the oxidative stress inhibitor as an effective ingredient, and for those purposes are employed an oxidative stress inhibiting agent which comprises, as an effective ingredient, at least one selected from cysteine or cystine derivatives and the salts thereof.Type: GrantFiled: December 20, 2002Date of Patent: September 12, 2006Assignee: Ajinomoto Co., Inc.Inventors: Keiji Iwasaki, Manabu Kitazawa, Eiji Shiojiri, Kazutami Sakamoto
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Patent number: 7030158Abstract: A group of new compounds, N-(all-trans-Retinoyl)-L-cysteic acid, N-(13-cis-Retinoyl)-L-cysteic acid, N-(all-trans-Retinoyl)-L-cysteinesulfinic acid, N-(13-cis-Retinoyl)-L-cysteinesulfinic acid, N-(all-trans-Retinoyl)-L-homocysteic acid, N-(13-cis-Retinoyl)-L-homocysteic acid, and sodium salts of these compounds, including sodium salts of their esters and amides, is shown to exhibit therapeutic effects per se, and which compounds in combination with cytotoxic compounds, such as docetaxel, paclitaxel, doxorubicin and mitoxantrone, exhibit a synergistic effect. These compounds make it possible to manufacture new formulations of poorly soluble pharmaceutical compounds, and the present invention discloses a process of manufacturing water-soluble formulations of such compounds, exemplified by docetaxel, and paclitaxel, exhibiting enhanced pharmacological activity, and formulations of water-soluble pharmaceuticals exemplified by doxorubicin and mitoxantrone, exhibiting improved therapeutic efficacy.Type: GrantFiled: November 15, 2002Date of Patent: April 18, 2006Assignee: Ardenia Investments Ltd.Inventors: Oleg Strelchenok, Julian Aleksov
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Patent number: 7026356Abstract: The present invention relates to novel fatty acid analogues of the general formula (I): CH3—[CH2]m—[xi—CH2]n—COOR, wherein n is an integer from 1 to 12, and wherein m is an integer from 0 to 23, and wherein i is an odd number which indicates the position relative to COOR, and wherein Xi independent of each other are selected from the group comprising O, S, SO, SO2, Se and CH2, and wherein R represents hydrogen or C1–C4 alkyl, with the proviso that at least one of the Xi is not CH2, or a salt, prodrug or complex thereof, for the preparation of a pharmaceutical composition for the treatment and/or prevention of primary and/or secondary stenosis. Further the present invention relates to the use of said compounds for the prevention and/or treatment of a disease caused by procedural vascular trauma and/or pathological proliferation of smooth muscle cells, and/or an increased level of plasma homocysteine.Type: GrantFiled: May 17, 2002Date of Patent: April 11, 2006Inventor: Rolf Berge
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Patent number: 6946474Abstract: The present invention provides trichloroethyl-sulfonylurea-containing compounds that inhibit glycing transporters, pharmaceutical compositions comprising such compounds, methods for using such compounds for inhibiting glycine transporters and methods for using such compounds for the treatment of disease states in which glycine is involved.Type: GrantFiled: September 13, 2001Date of Patent: September 20, 2005Assignee: Merck & Co., Inc.Inventors: Syed M. Ali, Kurt R. Brunden, Jack B. Jiang
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Patent number: 6916850Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.Type: GrantFiled: May 3, 2002Date of Patent: July 12, 2005Assignee: Galileo Pharmaceuticals, Inc.Inventors: Bing Wang, Guy Miller, Wei Zhang
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Patent number: 6903052Abstract: The invention concerns the use of certain compounds related to fatty acids to control nematodes that infest plants or the situs of plants. Nematodes that parasitize animals can also be controlled using the methods and composition of this invention. Certain of the useful compounds are fatty acid esters that are predicted inhibitors of nematode delta-12 fatty acid desaturases and can be, for example, from C16 to C20 in length.Type: GrantFiled: July 1, 2002Date of Patent: June 7, 2005Assignee: Divergence, Inc.Inventors: Deryck J. Williams, Andrew P. Kloek, Michelle Coutu Hresko
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Patent number: 6872749Abstract: The present invention relates to a method for supplying bioavailable methionine to a cow which comprises supplying to the cow an ester of methionine or methionine amide and/or an ester of the hydroxy analogue of methionine or a salt thereof.Type: GrantFiled: January 6, 2003Date of Patent: March 29, 2005Assignee: Adisseo Ireland LimitedInventors: Jean-Claude Robert, Robert Bennett, Georges Gros
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Patent number: 6852756Abstract: Described is a method for transdermally controlling a bacterial infection in a non-human animal which comprises the step of topically applying to the non-human animal a medicament comprising valnemulin in free base or a pharmaceutically acceptable salt form.Type: GrantFiled: November 20, 2000Date of Patent: February 8, 2005Assignee: Novartis Animal Health US Inc.Inventors: Paul Howard Ripley, Erich Zeisl, Stefan Horkovics-Kovats
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Publication number: 20040254225Abstract: Novel compounds and compositions including those compounds, as well as methods of using and making the compounds are herein described. The compounds are useful in therapeutic applications, including modulation of disease or disease symptoms in a subject (e.g., mammal, human, dog, cat, horse). The compounds are useful as modulators of the mu opioid receptor (MOR) through their binding affinity with that receptor.Type: ApplicationFiled: October 10, 2003Publication date: December 16, 2004Inventors: Bryce A. Harrison, Tiffany M. Gierasch, Gregory L. Verdine, Zhangjie Shi
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Publication number: 20040242663Abstract: The present invention ralates to compounds of formula (I): wherein R is hydrogen (H) or C1-6 alkyl; and X is defined such that —NH—(X)—COOH is the residue of an amino acid, which amino acid may itself optionally be substituted at any pendant amino group thereof by a residue of a carboxylic acid or a derivative thereof; or a salt thereof. The use of these compounds, in particular as potential anti-inflammatory and immunomodulatory drugs, and their preparation are described.Type: ApplicationFiled: June 28, 2004Publication date: December 2, 2004Inventor: Keith Coupland
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Publication number: 20040235910Abstract: A compound of formula 1Type: ApplicationFiled: June 14, 2004Publication date: November 25, 2004Inventors: Gerd Ascher, Heinz Berner, Johannes Hildebrandt
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Patent number: 6814988Abstract: A method of supplying a ruminant with its nutritional requirements for methionine is provided wherein a hydroxy analogue of methionine that is available for absorption by a ruminant is administered to the ruminant. Preferably, the, ruminant is administered an isopropyl ester of a hydroxy analogue of methionine, wherein at least 40% of the isopropyl ester of the hydroxy analogue of methionine is available for absorption by the cow.Type: GrantFiled: November 16, 2001Date of Patent: November 9, 2004Assignee: Novus International, Inc.Inventors: Christopher D. Knight, Karen M. Koenig, Lyle M. Rode, Michael J. Vandenberg, Mercedes Vazquez-Anon
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Patent number: 6806261Abstract: The present invention relates to methods for regulating the release of TGF-&bgr; from living cells in vitro or in vivo, comprising bringing the cells into contact with an effective amount of a NAALADase inhibitor. Such methods are believed to be useful for affecting neuroregeneration, cell proliferation, cell differentiation, extracellular matrix formation, myelination, inflammation, immune function, liver function, pancreatic function, angiogenesis, or wound healing; and/or for preventing or treating diabetes.Type: GrantFiled: August 1, 2002Date of Patent: October 19, 2004Assignee: Guilford Pharmaceuticals Inc.Inventors: Barbara S. Slusher, Xi-Chun May Lu, Krystyna Wozniak
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Patent number: 6803057Abstract: An acidic aqueous hydrogen peroxide solution is provided with improved disinfectant activity. Concentrated solutions preferably contain up to about 8 wt./wt. % H2O2 and as-used concentrations contain about 0.5% wt./wt. % H2O2. The solution also contains from 0.05 to 8.0 wt./wt. % of at least one phosphorous-based acid, e.g. phosphoric acid and/or a phosphonic acid with from 1 to 5 phosphonic acid groups, and from 0.02 to 5 wt./wt. % of at least one anionic surfactant. The surfactant is selected from C8 to C16 alkyl aryl sulfonic acids, sulfonated C12 to C22 carboxylic acids, C8 to C22 alkyl diphenyl oxide sulfonic acids, naphthalene sulfonic acids, C8 to C22 alkyl sulfonic acids, and alkali metal and ammonium salts thereof, and alkali metal C8 to C18 alkyl sulfates, and mixtures thereof. Most preferably the solution has an emulsifier and/or hydrotrope, e.g. an alkylated sulfonated diphenyl oxide salt, an alkyl aryl polyoxyethylene surfactant, and/or a polyoxyethylene surfactant.Type: GrantFiled: December 28, 2001Date of Patent: October 12, 2004Assignee: Virox Technologies Inc.Inventors: Jose A. Ramirez, Michael J. Rochon
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Publication number: 20040186176Abstract: This invention provides methods for treating a mycobacterial infection by administering to an animal a pharmaceutical composition containing a compound having the formula R—SOn-Z-CO—Y, where R is an alkyl group having 6-20 carbons; Z is a radical selected from —CH2—, —O—, and —NH—, two of these radicals coupled together, or —CH2═CH2—; Y is —NH2, O—CH2—C6H5, —CO—CO—O—CH3, or O—CH3; and n is 1 or 2. It has been discovered that these compounds inhibit growth of microbial cells which synthesize &agr;-substitued. &bgr;-hydroxy fatty acids, particularly corynemycolic acid, nocardic acid, and mycolic acid. These compounds may be used to inhibit growth of mycobacterial cells, such as Mycobacterium tuberculosis, drug-resistant M. tuberculosis, M. avium intracellulare, and M. leprae.Type: ApplicationFiled: January 27, 2004Publication date: September 23, 2004Applicant: The Johns Hopkins University of MedicineInventors: Craig A. Townsend, James D. Dick, Gary R. Pasternack, Francis P. Kuhajda, Nicole M. Parrish
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Publication number: 20040180954Abstract: A fluorine-containing cyclic ester is represented by the formula 1: 1Type: ApplicationFiled: February 27, 2004Publication date: September 16, 2004Applicant: Central Glass Company, LimitedInventors: Satoru Kobayashi, Katsunori Kawamura, Haruhiko Komoriya, Kazuhiko Maeda
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Publication number: 20040162329Abstract: A method for inhibiting and/or ameliorating the occurrence of diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals in a subject whereby a subject is administered a carotenoid structural analog, either alone or in combination with another carotenoid analog, or co-antioxidant formulation. The analog or analog combination is administered such that the subject's risk of experiencing diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals may be thereby reduced. The analog or analog combination may be administered to a subject for the inhibition and/or amelioration of ischemia-reperfusion injury. The analog or analog combination may be administered to a subject for the inhibition and/or amelioration of liver disease. The analog or analog combination may be administered to a subject for the inhibition and/or amelioration of cancer.Type: ApplicationFiled: July 29, 2003Publication date: August 19, 2004Inventors: Samuel Fournier Lockwood, Sean O'Malley, David G. Watumull, Laura M. Hix, Henry Jackson, Geoff Nadolski
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Patent number: 6777443Abstract: Compounds of the formula wherein R, R1, COOR2, R3-R7, alk, and X have meaning as defined, such being useful as dual inhibitors of angiotensin converting enzyme and neutral endopeptidase, as well as inhibitors of endothelin converting enzyme.Type: GrantFiled: May 9, 2002Date of Patent: August 17, 2004Assignee: Novartis AGInventor: Cynthia Anne Fink
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Publication number: 20040138302Abstract: This disclosure describes antifungal antibiotics designated Hygroscopene A, Hygroscopene B and Hygroscopene C to their production by fermentation, to methods for recovery and concentration from the crude solutions, to a process for purification and to new analogs of Hygroscopene A, Hygroscopene B and Hygroscopene C prepared by synthetic procedures.Type: ApplicationFiled: December 18, 2003Publication date: July 15, 2004Applicant: Wyeth Holdings CorporationInventors: Ping Cai, Fangming Kong, Pamela Fink Charbonneau, Mark Edward Ruppen
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Patent number: RE39403Abstract: The present invention relates to a method for supplying bioavailable methionine to a cow which comprises supplying to the cow an ester of methionine or methionine amide and/or an ester of the hydroxy analogue of methionine or a salt thereof.Type: GrantFiled: May 20, 2003Date of Patent: November 14, 2006Assignee: Adisseo Ireland LimitedInventors: Jean-Claude Robert, Robert Bennett, Georges Gros
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Patent number: RE39576Abstract: A compound of formula (I) wherein R1 is a C1-6 straight or branched chain alkyl group, a C2-6alkenyl group, a C2-6 alkynyl group, a C3-6cycloalkyl group or a C3-6cycloalkylC1-6alkyl group, each optionally substituted by one to three groups independently selected from: —CN; —NO2; a group —COR2 wherein R2 is hydrogen, C1-6 alkyl, —OR3 wherein R3 is hydrogen or C1-6alkyl or NR4R5 wherein R4 and R5 are independently selected from hydrogen or C1-6 alkyl; a group —S(O)mR6 wherein m is 0, 1 or 2, R6 is hydrogen, C1-6 alkyl, hydroxy or NR7R8 wherein R7 and R8 are independently hydrogen or C1-6 alkyl; a group PO(OR9)2 wherein R9 is hydrogen or C1-6 alkyl; a group NR10R11 wherein R10 and R11 are independently selected from hydrogen, C1-6 alkyl, —COR12 wherein R12 is hydrogen or C1-6 alkyl, or —S(O)m?R13 wherein m? is 0, 1 or 2 and R13 is hydrogen or C1-6 alkyl; halo; or a group —OR14 wherein R14 is hydrogen, C1-6 alkyl optionally substituted by one to three halo atoms, C6-10 aryl or —COR15 wherein R15 is hydrogeType: GrantFiled: June 14, 1995Date of Patent: April 17, 2007Assignee: Smithkline Beecham CorporationInventors: Harold Francis Hodson, Richard Michael John Palmer, David Alan Sawyer, Richard Graham Knowles, Karl Witold Franzmann, Martin James Drysdale, Patricia Ifeyinwa Davies, Helen Alice Rebecca Clark, Barry George Shearer, Steven Smith