The Ring Nitrogen Of The Six-membered Hetero Ring Is Pentavalent (e.g., Quaternary Pyridinium Salt, Etc.) Patents (Class 514/358)
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Publication number: 20100158818Abstract: The present application relates to N-chlorinated cationic compounds of Formula I or a salt thereof, and associated compositions and methods of use as antimicrobial agents.Type: ApplicationFiled: November 6, 2009Publication date: June 24, 2010Inventors: Rakesh K. Jain, Eddy Low, Charles Francavilla, Timothy P. Shiau, Satheesh K. Nair
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Publication number: 20100137379Abstract: Antimicrobial lubricant compositions are disclosed. The antimicrobial lubricant compositions are particularly useful in providing antimicrobial capability to a wide-range of medical devices. The compositions include an oil lubricant. Representative lubricants may include polydimethyl siloxane, trifluoropropyl copolymer polysiloxane, and a copolymer of dimethylsiloxane and trifluoropropylmethylsiloxane. The compositions include rheology modifiers as necessary. The compositions also include antimicrobial agents, which may be selected from a wide array of agents. Representative antimicrobial agents include of aldehydes, anilides, biguanides, bis-phenols, quaternary ammonium compounds, cetyl pyridium chloride, cetrimide, alexidine, chlorhexidine diacetate, benzalkonium chloride, and o-phthalaldehyde.Type: ApplicationFiled: May 6, 2009Publication date: June 3, 2010Applicant: BECTON, DICKINSON AND COMPANYInventor: David Tien-Tung Ou-Yang
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Mono Quaternary Ammonium Salts and Methods for Modulating Neuronal Nicotinic Acetylcholine Receptors
Publication number: 20100113511Abstract: Provided are monoquaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.Type: ApplicationFiled: June 15, 2007Publication date: May 6, 2010Applicant: University of Kentucky Research FoundationInventors: Peter Crooks, Linda P. Dwoskin, Guangrong Zheng, Sangeetha Sumithran, Zhenfa Zheng -
Publication number: 20100113537Abstract: An antimicrobial fiber bearing an anionic functional group, and a method of producing it wherein at least a part of the anionic functional group forms a quaternary ammonium salt and at least another part thereof forms an antimicrobial metal salt. The quaternary ammonium salt is preferably a cetylpyridinium salt, and the antimicrobial metal salt is preferably a zinc salt. The fiber is preferably a carboxyalkylated cellulose fiber. An antimicrobial fiber product comprising the antimicrobial fiber.Type: ApplicationFiled: September 20, 2007Publication date: May 6, 2010Applicant: ALCARE CO., LTD.Inventor: Eiji Nonaka
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Publication number: 20100003330Abstract: The present invention relates to compositions and methods for decreasing the infectivity, morbidity, and rate of mortality associated with a variety of pathogenic organisms and viruses. The present invention also relates to methods and compositions for decontaminating areas colonized or otherwise infected by pathogenic organisms and viruses. Moreover, the present invention relates to methods and compositions for decreasing the infectivity of pathogenic organisms in foodstuffs.Type: ApplicationFiled: June 25, 2002Publication date: January 7, 2010Applicant: The Regents of the University of MichiganInventors: James R. Baker, JR., Tarek Hamouda, Amy Shih, Andrzej Myc
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Publication number: 20090318512Abstract: A multi-purpose contact lens care solution having high antimicrobial activity comprising, in an aqueous liquid medium, cetylpyridinium chloride and a non-ionic surfactant. In one embodiment of the invention, the non-ionic surfactant is a poly(oxypropylene)-poly(oxyethylene) block copolymer. The solution may optionally also include additional antimicrobial components, a buffer component, a viscosity inducing component, a surfactant, taurine, propylene glycol and/or a tonicity component. This solution additionally prevents losses in ocular tissue membrane integrity during contact lens wear.Type: ApplicationFiled: May 21, 2009Publication date: December 24, 2009Applicant: Advanced Medical Optics, Inc.Inventors: Zhi-Jian Yu, Stanley W. Huth
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Publication number: 20090318503Abstract: Provided are bis-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.Type: ApplicationFiled: January 16, 2007Publication date: December 24, 2009Inventors: Peter Crooks, Linda P. Dwoskin, Guangrong Zheng, Sangeetha Sumithran
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Publication number: 20090298893Abstract: Addition salts of 2,4?-dimethyl-3-piperidinopropiophenone (tolperisone) are described, wherein the salt is formed with an acid R—COOH and wherein R is the organic group of a physiologically compatible organic acid. Described also are processes for the preparation of these addition salts, the use thereof for pharmaceutical preparations and pharmaceuticals containing these addition salts.Type: ApplicationFiled: March 21, 2006Publication date: December 3, 2009Inventors: Rudolf-Giesbert Alken, Frank Schneider
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Publication number: 20090239912Abstract: A concentrated quaternary ammonium compound (QAC) solution comprising a QAC with a concentration from greater than about 10% by weight and at least one solubility enhancing agent, such as an alcohol, is disclosed. A diluted QAC solution is used to contact food products to prevent microbial growth on the food products from a broad spectrum of foodborne microbial contamination. A method of contacting the food products with the dilute QAC for an application time of at least 0.1 second is disclosed. The foods that can be treated by this method are meat and meat products, seafood, vegetables, fruit, dairy products, pet foods and snacks, and any other food that can be treated and still retain its appearance and texture. One of the treatment methods is spraying and misting the QAC solutions on the food products for an application time of at least 0.1 second to prevent broad spectrum foodborne microbial contamination.Type: ApplicationFiled: June 1, 2009Publication date: September 24, 2009Inventors: CESAR COMPADRE, Philip Breen, Hamid Salari, E. Kim Fifer, Danny L. Lattin, Michael Slavik, Yanbin Li, Timothy O'Brien, Amy L. Waldroup, Thomas F. Berg
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Publication number: 20090232748Abstract: This disclosure relates to inventive methods for inactivating viral pathogens comprising providing a virucidal composition comprising a liquid media containing less than 1% weight per volume of a quaternary ammonium compound, such as cetylpyridinium chloride and between 0% and 0.5% weight per volume of citric acid, and contacting a surface targeted for disinfection with the virucidal composition. This disclosure further relates to inventive virucidal compositions comprising a liquid media, a quaternary ammonium compound, such as cetylpyridinium chloride, at a concentration of less than 1% weight per volume, citric acid at a concentration of between 0.0% and 0.5% weight per volume, an extender, and an enhancer.Type: ApplicationFiled: March 18, 2009Publication date: September 17, 2009Applicant: ViraTox, L.L.C.Inventor: Charles L. Capps
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Patent number: 7550491Abstract: The present invention relates to salts comprising bis(trifluoromethyl)imide anions and saturated, partially or fully unsaturated, heterocyclic cations, to a process for the preparation thereof, and to the use thereof as ionic liquids.Type: GrantFiled: November 17, 2003Date of Patent: June 23, 2009Assignee: Merck Patent GmbHInventors: Nikolai Ignatyev, Urs Welz-Biermann, Michale Schmidt, Helge Willner, Andriy Kucheryna
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Patent number: 7547444Abstract: The present invention includes compounds of pyridinium salts and methods of their use for agricultural purposes. The present invention also relates to methods of controlling fungi and/or bacteria.Type: GrantFiled: March 3, 2004Date of Patent: June 16, 2009Assignee: Mycosol, Inc.Inventors: Richard B. Klein, Jeffrey L. Selph, John J. Partridge, John Reinhard
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Patent number: 7541045Abstract: A concentrated quaternary ammonium compound (QAC) solution comprising a QAC with a concentration from greater than about 10% by weight and at least one solubility enhancing agent, such as an alcohol, is disclosed. A diluted QAC solution is used to contact food products to prevent microbial growth on the food products from a broad spectrum of foodborne microbial contamination. A method of contacting the food products with the dilute QAC for an application time of at least 0.1 second is disclosed. The foods that can be treated by this method are meat and meat products, seafood, vegetables, fruit, dairy products, pet foods and snacks, and any other food that can be treated and still retain its appearance and texture. One of the treatment methods is spraying and misting the QAC solutions on the food products for an application time of at least 0.1 second to prevent broad spectrum foodborne microbial contamination.Type: GrantFiled: September 17, 2004Date of Patent: June 2, 2009Assignee: University of ArkansasInventors: Cesar Compadre, Philip Breen, Hamid Salari, E. Kim Fifer, Danny L. Lattin, Michael Slavik, Yanbin Li, Timothy O'Brien, Amy L. Waldroup, Thomas F. Berg
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Publication number: 20090118340Abstract: The invention relates to a method for inhibiting and/or preventing formation of cancer metastases and secondary malignant cancers by administration to a subject of an effective amount of a quaternary pyridinium salt of formula I wherein R? is selected from the group consisting of H, OH, CONH2, COCH3, R? is selected from the group consisting of H, CH3, R?? represents H or CH3, and X? is a pharmaceutically acceptable counterion.Type: ApplicationFiled: October 9, 2008Publication date: May 7, 2009Inventors: Jerzy Gebicki, Andrzej Marcinek, Stefan Chlopicki
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Publication number: 20090036387Abstract: Disclosed are neuroblastoma tumor-initiating cell inhibiting compositions comprising chemical entities capable of affecting neuroblastoma tumor-initiating cells. Pharmaceutical preparations that include these chemical entities are also provided for the treatment of neuroblastoma. These pharmaceutical preparations are suitable for the treatment of humans, and are particularly suited for the treatment of children of 12 years of age or younger having neuroblastoma. The compositions and pharmaceutical preparations posses reduced normal cell cytotoxicity. The compositions and pharmaceutical preparations may be used alone or together with other conventional neuroblastoma preparations as part of a clinical regimen in the treatment and management of neuroblastoma.Type: ApplicationFiled: September 9, 2008Publication date: February 5, 2009Applicant: The Hospital for Sick ChildrenInventors: DAVID R. KAPLAN, Kristen M. Smith, Alessandro Datti
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Patent number: 7456197Abstract: Pyridinium cationic lipids useful as non-viral gene delivery agents are disclosed. The agents are prepared by reaction of pyrylium salts with primary amines. Also disclosed are methods of trasfectind cells using the pyridinium cationic lipids as gene transfer agents.Type: GrantFiled: July 1, 2004Date of Patent: November 25, 2008Assignee: The Texas A&M University SystemInventors: Alexandru T. Balaban, William A. Seitz, Marc A. C. Ilies, Edward Bradbridge Thompson, Robert E. Garfield, Betty H. Johnson, Aaron L. Miller, Melissa J. Wentz
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Publication number: 20080102094Abstract: Microbicidal compositions including (a) cyanodithiocarbimate and (b) an N-alkyl heterocyclic compound; a triazole compound or salt thereof or metal complex thereof; a microbicide with an activated halogen atom or a formaldehyde releasing compound; 1,4-bis(bromoacetoxy)-2-butene; 2-(thiocyanomethylthio)benzothiazole; a methylene-bis(thiocyanate); a halogenated acetophenone; a halopropynl compound; an iodosulfone; a phenol; a halocyanoacetamide compound and/or a quaternary ammonium compound are described. Components (a) and (b) can be present in a synergistically effective amount to control the growth of at least one microorganism. Methods for controlling the growth of microorganisms with the compositions are also disclosed.Type: ApplicationFiled: November 1, 2006Publication date: May 1, 2008Inventor: Stephen D. Bryant
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Publication number: 20080033021Abstract: A method for minimizing microbial contamination of contact lenses during the handling of the lenses. The method comprises instructing a person that wears contact lenses to wash their hands prior to the handling of the contact lenses with a wash composition. The wash composition includes one or more surfactants selected from the group consisting of non-ionic, cationic, amphoteric or zwitterionic surfactants, and optionally, an anionic surfactant. The wash composition also includes an antimicrobial agent that is compatible with ocular tissue. The invention is also directed to a kit for to assist contact lens wearers with the care maintenance of their lenses. The kit includes the wash composition and a multipurpose contact lens solution. The wash composition is suitable for use with the multipurpose contact lens solution.Type: ApplicationFiled: June 26, 2007Publication date: February 7, 2008Inventor: Susan Burke
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Patent number: 7300948Abstract: Inhibitors of HIV reverse transcriptase which are useful for the treatment of HIV infection. Exemplars of the invention are compounds of the formula wherein the substituents are as defined in the following table R1 R2 R4 R5 R8a F CF3 Me H —OH F CF3 Cl H —OH F CF3 Me H —O—CH2CO2H Cl CN Cl H —OH.Type: GrantFiled: September 29, 2005Date of Patent: November 27, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Pierre Bonneau, Patrick Deroy, Alexandre Gagnon, Jeffrey O′Meara, Bruno Simoneau, Christiane Yoakim
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Patent number: 7250428Abstract: Cetylpyridinium salt of diclofenac.Type: GrantFiled: February 12, 2004Date of Patent: July 31, 2007Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventor: Giorgio Pifferi
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Patent number: 7235576Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.Type: GrantFiled: January 11, 2002Date of Patent: June 26, 2007Assignee: Bayer Pharmaceuticals CorporationInventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
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Patent number: 7189383Abstract: The present invention relates to Halogenated amino acid analogues for use in diagnosis, which compounds have the general formula (I) wherein: R is (C1–C6) alkyl optionally substituted with thioether or ether oxygen atom when n=0, or a substituted aromatic or heteraromatic ring when n=1–6; and m=0 or 1; and X is a halogen atom.Type: GrantFiled: August 1, 2003Date of Patent: March 13, 2007Assignee: Mallinckrodt Inc.Inventor: John J. R. Mertens
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Patent number: 7141590Abstract: Disclosed are nicotinanilide-N-oxide compounds, methods for their production, pharmaceutical compositions which include these compounds, and methods for their use in various therapies.Type: GrantFiled: December 12, 2001Date of Patent: November 28, 2006Assignee: UCB SAInventors: Neil S Cutshall, Kraig M Yager
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Patent number: 7064139Abstract: Compositions and methods of treating a retroviral infection in an afflicted host and/or inhibiting replication of a retrovirus involve administering a therapeutically effective amount of the following compound of formula I: A-L-B??(I) wherein A is a substituted or unsubstituted aryl compound, substituted or unsubstituted piperidyl, or substituted or unsubstituted thiopheneyl; L is sulfonyl, sulfinyl or thio; and B is a substituted or unsubstituted aromatic nitrogen containing heteroaryl compound; or pharmacologically acceptable acid-addition and base-addition salts thereof.Type: GrantFiled: October 29, 2001Date of Patent: June 20, 2006Assignee: Uniroyal Chemical Company, Inc.Inventors: John A. Lacadie, James B. Pierce
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Patent number: 7015239Abstract: A fungicidal composition and method of treating plant diseases using a compound of formulaType: GrantFiled: September 2, 2004Date of Patent: March 21, 2006Assignee: Valent BioSciences, Inc.Inventors: Daniel F. Heiman, Peter D. Petracek, Judith A. Fugiel, Prem Warrior
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Patent number: 6984645Abstract: Compounds that are dual aP2/k-FABP inhibitors are provided having the formula wherein A, B, X, Y, R1, R2 and R3 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing dual aP2/k-FABP inhibitors alone or in combination with at least one other antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.Type: GrantFiled: November 15, 2002Date of Patent: January 10, 2006Assignee: Bristol-Myers Squibb CompanyInventors: David R. Magnin, Richard B. Sulsky, Jeffrey A. Robl, Thomas J. Caulfield, Rex A. Parker
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Patent number: 6953811Abstract: A description is given of compounds of the formula in which R1 and R2 independently of one another are halogen, C1-C6alkyl, halo-C1-C6alkyl, C1-C6alkoxy, halo-C1-C6alkoxy, or SF5, R3 is hydrogen, OH, halogen, C1-C6alkoxy or —O—C(?O)—C1-C6alkyl, R4 is for example hydrogen, halogen, C1-C6alkyl, halo-C1-C6alkyl, C1-C6alkoxy, halo-C1-C6alkoxy or SCN; R5 and R6 independently of one another are for example hydrogen, C1-C12alkyl, halo-C1-C12alkyl, C2-C12alkenyl, halo-C2-C12alkenyl or C2-C12alkynyl; and q is 0 or 1; and, where appropriate, E/Z isomers, E/Z isomer mixtures and/or tautomers, each in free form or in salt form; a process for the preparation of these compounds and their use, pesticide compositions whose active ingredient is selected from these compounds, or an agrochemically useable salt thereof, a process for preparing these compositions, and their use, plant propagation material treated with these compositions, and a method of combating pests.Type: GrantFiled: February 4, 2002Date of Patent: October 11, 2005Assignee: Syngenta Crop Protection, Inc.Inventors: Stephan Trah, Josef Ehrenfreund, Peter Maienfisch, André Jeanguenat, Saleem Farooq
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Patent number: 6939885Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: GrantFiled: November 17, 2003Date of Patent: September 6, 2005Assignee: ChemocentryxInventors: Solomon Ungashe, Zheng Wei, John Jessen Wright, Andrew Pennell
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Patent number: 6903118Abstract: The invention relates to new piperazinyl-substituted pyridylalkane, alkene, and alkine acid amides substituted with saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group according to the general formula (I) as well as methods for the production of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.Type: GrantFiled: June 16, 2000Date of Patent: June 7, 2005Assignee: Klinge Pharma GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt, Katja Wosikowski, Isabel Schemainda
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Patent number: 6878730Abstract: The invention features quaternary ammonium compounds of formula I, described herein, and their use in treating asthma, chronic obstructive pulmonary disorder, allergic rhinitis, and infectious rhinitis.Type: GrantFiled: October 17, 2003Date of Patent: April 12, 2005Assignee: Pharmacia & UpJohnInventor: Timothy Gordon Heath
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Patent number: 6864276Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: May 7, 2001Date of Patent: March 8, 2005Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 6864269Abstract: A concentrated quaternary ammonium compound (QAC) solution comprising a QAC with a concentration from greater than about 10% by weight and at least one solubility enhancing agent, such as an alcohol, is disclosed. A diluted QAC solution is used to contact food products to prevent microbial growth on the food products from a broad spectrum of foodborne microbial contamination. A method of contacting the food products with the dilute QAC for an application time of at least 0.1 second is disclosed. The foods that can be treated by this method are meat and meat products, seafood, vegetables, fruit, dairy products, pet foods and snacks, and any other food that can be treated and still retain its appearance and texture. One of the treatment methods is spraying and misting the QAC solutions on the food products for an application time of at least 0.1 second to prevent broad spectrum foodborne microbial contamination.Type: GrantFiled: January 31, 2000Date of Patent: March 8, 2005Assignee: University of ArkansasInventors: Cesar Compadre, Philip Breen, Hamid Salari, E. Kim Fifer, Danny L. Lattin, Michael Slavik, Yanbin Li, Timothy O'Brien, Amy L. Waldroup, Thomas F. Berg
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Patent number: 6858623Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.Type: GrantFiled: May 29, 2003Date of Patent: February 22, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Eugene R. Hickey, Weimin Liu, Usha R. Patel, Denice M. Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R. R. Young
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Publication number: 20040259823Abstract: The invention relates to novel cationic amphiphiles having an aromatic ring comprising at least one nitrogen atom. The cationic amphiphiles are particularly useful for the introduction of biologically compounds such as DNA, RNA, proteins and the like into eukaryotic cells. The cationic amphiphiles are represented by the following basic formula:(I). Characteristic is that R1 and R2 ?are single C6-C24 carbon chains. For the mode of action it is assumed that R1 folds back over the aromatic ring towards R2.Type: ApplicationFiled: June 17, 2004Publication date: December 23, 2004Inventors: Anthony Jacques Ronald Lambert Hulst, Jarmila Smisterova, Jan Bernard Frederik Nicolaas Engberts, Dirk Hoekstra
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Publication number: 20040254147Abstract: The present invention discloses an organic ionic compound having anti-viral activity and the method for antagonizing virus in vitro by putting the compounds in contact with the virus.Type: ApplicationFiled: October 3, 2003Publication date: December 16, 2004Applicant: Industrial Technology Research InstituteInventors: Li-Ching Lo, Wen-Yueh Ho, Lien-Tai Chen
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Publication number: 20040223913Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.Type: ApplicationFiled: December 23, 2003Publication date: November 11, 2004Applicant: Mallinckrodt, Inc.Inventors: Samuel Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj, Muthunadar P. Periasamy
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Patent number: 6815458Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is adminstered to a patient in need of such treatment.Type: GrantFiled: March 6, 2001Date of Patent: November 9, 2004Assignee: Acadia Pharmaceuticals, IncInventors: Carl-Magnus A. Andersson, Glenn Croston, Eva Louise Hansen, Allan Kjaersgaard Uldam
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Patent number: 6784194Abstract: A method of inhibiting effects of exogenous neurotoxic or neurotoxinic products in warm-blooded animals comprising administering to warm-blooded animals before exposure to said products an inhibitorily effective amount of reversible cholinesterase inhibitor selected from the group consisting of pyridostigmine and physostigmine followed by administration of an inhibitorily effective amount of 2-methyl-1-(1-piperidinyl)-1-(2-thienyl)-cyclohexane in substantially pure racemic, diastereoisomeric or enantiomeric form.Type: GrantFiled: April 13, 2001Date of Patent: August 31, 2004Assignee: Societe de Conseils de Recherches et D'Applications Scientifiques (S.C.R.A.S.)Inventors: Guy Lallement, Pierre D'Arbigny, Jean-Marc Kamenka
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Patent number: 6756393Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is adminstered to a patient in need of such treatment.Type: GrantFiled: April 7, 2003Date of Patent: June 29, 2004Assignee: Acadia Pharmaceuticals, Inc.Inventors: Carl-Magnus A. Andersson, Glenn Croston, Eva L. Hansen, Allan Kjaersgaard Uldam
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Patent number: 6726894Abstract: The invention relates to new compounds with the general formula I for use as a tool to introduce macromolecules into cells. The invention further relates to compositions for introducing macromolecules into cells, comprising vesicles formed by at least one compound in a solvent. The macromolecule can be incorporated in the vesicles and/or bound to the vesicles or another aggregate of the new compounds.Type: GrantFiled: December 28, 1998Date of Patent: April 27, 2004Assignee: Synvolux IP B.V.Inventors: Jan Bernard Frederik Nicolaas Engberts, Anno Wagenaar, Dirk Hoekstra, Irene Van Der Woude, Marcel Herman Jozef Ruiters
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Patent number: 6727237Abstract: The present invention provides methods of synthesizing and screening inhibitors of bacterial NAD synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections with inhibitors of bacterial NAD synthetase enzyme.Type: GrantFiled: October 25, 2002Date of Patent: April 27, 2004Inventors: Wayne J. Brouillette, Donald Muccio, Mark J. Jedrzejas, Christie G. Brouillette, Yancho Devedjiev, Walter Cristofoli, Lawrence J. DeLucas, Jose Gabriel Garcia, Laurent Schmitt, Sadanadan E. Velu
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Patent number: 6706741Abstract: The present invention provides an excellent acetylcholinesterase inhibitor. That is, it provides an acetylcholinesterase inhibitor comprising a 1-benzylpyridinium salt represented by the following formula: wherein R1, R2, R3 and R4 are the same as or different from each other and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a nitrile group, a C1-6 alkyl group, a C1-6 alkoxy group etc.; R5 represents a hydrogen atom, a halogen atom etc.; the partial structure: is a group represented by the formula >C(R6)—CH2— (wherein R6 is a hydrogen atom or a halogen atom) or >C═CH—; X− represents a halide ion or organic sulfonic acid ion; and m is 0 or an integer from 1 to 5.Type: GrantFiled: September 18, 2002Date of Patent: March 16, 2004Assignee: Eisai Co., Ltd.Inventors: Yoichi Iimura, Takashi Kosasa
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Patent number: 6686358Abstract: A compound of formula (I): wherein: R1 represents hydrogen, or linear or branched (C1-C6)alkyl optionally substituted by one or more identical or different groups selected from aryl, heteroaryl, cycloalkyl and heterocycloalkyl, represents a saturated ring having from 4 to 7 ring members that may contain, in addition to nitrogen, one or two hetero atoms selected from O, S and —NR3 groups, wherein R3 represents hydrogen or linear or branched (C1-C6)alkyl, n represents an integer such that 1≦n≦6, R2 represents any one of the groups described in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as inhibitor of trypsin-related serine proteases and thrombin.Type: GrantFiled: December 14, 2001Date of Patent: February 3, 2004Assignee: Les Laboratoires ServierInventors: Guillaume De Nanteuil, Philippe Gloanec, Tony Verbeuren, Alain Rupin, Marie-Odile Vallez
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Publication number: 20040019012Abstract: There is provided a pharmaceutical composition suitable for topical administration to an eye, the composition comprising (a) an antibiotic antibiotic drug, for example linezolid, in a therapeutically or prophylactically effective drug concentration, (b) as a solubilizing agent, a pharmaceutically acceptable cyclodextrin compound in a concentration sufficient to maintain the drug in solution at such a drug concentration, and (c) as a preservative, cetyl pyridinium chloride. The composition is particularly useful for the treatment and/or prevention of eye infections due to gram positive bacteria.Type: ApplicationFiled: February 20, 2003Publication date: January 29, 2004Inventors: Satish K. Singh, Paramita Bandyopadhyay, Syed Hasan
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Publication number: 20040019043Abstract: The current invention provides novel thiomolybdate derivatives, methods of making novel thiomolybdate derivatives, pharmaceutical compositions of novel thiomolybdate derivatives, methods of using novel thiomolybdate derivatives to treat diseases associated with aberrant vascularization and methods of using pharmaceutical compositions of thiomolybdate derivatives to treat diseases associated with aberrant vascularization.Type: ApplicationFiled: July 23, 2002Publication date: January 29, 2004Inventors: Dimitri Coucouvanis, Robert J. Ternansky, Patricia L. Gladstone, Amy L. Allan, Melissa L.P. Price, Sean M. O'Hare
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Patent number: 6677361Abstract: Niacin and niacin prodrugs are topically administered as suitable formulations to device for impoving the lipid profiles of subjects, preferably humans.Type: GrantFiled: April 16, 2001Date of Patent: January 13, 2004Assignee: University of Kentucky Research FoundationInventors: Elaine L. Jacobson, Myron K. Jacobson, Hyuntae Kim, Moonsun Kim, Jaber G. Qasem
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Patent number: 6664280Abstract: As disclosed herein, the present invention provides a compound having the structural formula wherein R1, R2, R3, and R4 are each independently H, or a methyl, halo, trifluoromethyl, nitro, alkyloxy, or acyloxy group, or a pharmaceutically acceptable salt or prodrug thereof. Also disclosed are compounds, compositions, methods and kits for treating, preventing, or inhibiting injuries induced by a vesicant agent, such as bis-2-chloroethylsulfide (HD). Additionally, protectants and decontaminants are disclosed.Type: GrantFiled: June 17, 2002Date of Patent: December 16, 2003Assignee: The United States of America as represented by the Secretary of the ArmyInventors: Ai J. Lin, Michael C. Babin
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Patent number: 6649633Abstract: This application is directed to compounds useful as inhibitors at PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis and chronic obstructuive pulmonary disease, of the formula: where j is 0 or 1 provided that when j is 0, n must be 2; k is 0 or 1; m is 0, 1, or 2; n is 1 or 2; W1 is —O—; or —S(═O)t—, where t is 0, 1, or 2; Y is —C(R1a); Q1 is phenyl or substituted phenyl; Q2 is biphenyl or substituted biphenyl; and the remaining variables are defined as set forth in the specification. This application is also directed to pharmaceutical compositions comprising those compounds and to methods of treating diseases regulated by the activation and degranulation of eosinophils, in particular asthma, chronic bronchitis and chronic obstructive pulmonary disease.Type: GrantFiled: January 31, 2002Date of Patent: November 18, 2003Assignee: Pfizer IncInventors: Robert J. Chambers, Anthony Marfat, Thomas V. Magee
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Publication number: 20030211136Abstract: A consumable film adapted to adhere to and dissolve in the oral cavity of a warm-blooded animal including humans, comprising at least one water soluble polymer, a taste masking effective amount of a sweetener, and a pharmaceutically active agent having a sufficiently unpleasant taste that it is desirably masked by the sweetener.Type: ApplicationFiled: April 25, 2003Publication date: November 13, 2003Inventors: Neema Kulkarni, Lori D. Kumar, Albert Sorg
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Patent number: 6638946Abstract: The invention relates to a compound of formula (I): wherein: A represents pyridine, pyridinium or piperidine R1, R2, R3 and R4 are as defined in the description R5 represents hydrogen, a nitrogen-containing heterocycle or a group of formula (II): R6 represents hydrogen or linear or branched (C1-C6)alkyl. and medicinal products containing the same which are useful in treating pain or deficiencies in memory.Type: GrantFiled: September 25, 2001Date of Patent: October 28, 2003Assignee: Les Laboratoires ServierInventors: Otto Meth-Cohn, Chu-Yi Yu, Pierre Lestage, Marie-Cécile Lebrun, Daniel-Henri Caignard, Pierre Renard