Halogen Bonded Directly To Carbon In R Patents (Class 514/628)
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Publication number: 20100292079Abstract: The invention provides aqueous pesticidal concentrates comprising at least one colloidal solid and a dispersed emulsion phase comprising at least one substantially water-insoluble pesticidally active ingredient, which is either itself an oily liquid comprising the oil phase, is a solid but is dissolved in an oily liquid present in the oil phase, is a solid and is dispersed within the oil phase or is present as a colloidal solid adsorbed to the liquid-liquid interface between the continuous aqueous phase and the dispersed oil phase.Type: ApplicationFiled: August 30, 2007Publication date: November 18, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventor: Jeffrey Fowler
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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: 20100260813Abstract: A rodenticidal mixture comprising a) 0.0015 to 99.89% by weight of at least one rodenticide, b) 10?8 to 95% by weight of at least one painkiller and c) 0.01 to 99.9984% by weight of at least one biocide, where the percentages by weight are based on the total of components (a), (b) and (c), is suitable for the preparation of rodenticidal bait formulations which are employed for controlling rodent pests.Type: ApplicationFiled: September 30, 2008Publication date: October 14, 2010Applicant: BASF SEInventors: Gerhard Schnabel, Michael Ishaque, Dieter Zeller, Lars Weichel, Andrej Brejc
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Patent number: 7799334Abstract: The present invention relates to pyrazolecarboxamides of the formula I in which the variables are as defined below: X is trifluoromethyl; R1 is F, Cl, Br, C1-C4-alkyl or C1-C4-haloalkyl; R2 is hydrogen, halogen or C1-C4-alkyl; R3 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C2-C4-alkynyl or C3-C6-cycloalkyl; W is O or S; with the proviso that, if R3 is hydrogen and W is oxygen, a) R1 and R2 are not simultaneously methyl and F, respectively; b) R1 and R2 are not simultaneously trifluoromethyl and hydrogen or fluorine, respectively. to processes for preparing these compounds, to seeds and compositions comprising them and to methods for controlling harmful fungi.Type: GrantFiled: May 10, 2006Date of Patent: September 21, 2010Assignee: BASF AktiengesellschaftInventors: Markus Gewehr, Jochen Dietz, Thomas Grote, Wassilios Grammenos, Udo Hünger, Bernd Müller, Frank Schieweck, Anja Schwögler, Jan Klaas Lohmann, Joachim Rheinheimer, Jens Renner, Peter Schäfer
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Publication number: 20100190705Abstract: Provided herein are methods of decreasing glial fibrillary acidic protein (GFAP) levels in a cell. Such methods include administering an effective amount of a GFAP lowering compound to the cell. Also provided are compounds useful for the treatment of Alexander disease in subjects at risk of or diagnosed with Alexander disease and methods for the identification of such compounds.Type: ApplicationFiled: October 26, 2009Publication date: July 29, 2010Inventors: Albee Messing, Woosung Cho, Jon Scott Thorson, Randal D. Goff
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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: 20100160444Abstract: Methods of treating or inhibiting ischemia and reperfusion injury are provided.Type: ApplicationFiled: November 4, 2009Publication date: June 24, 2010Applicant: RADICAL THERAPEUTIXInventors: Roberta Gottlieb, Paul Wentworth, Eric F. Johnson, Mark J. Yeager, David Granville
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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: 20100137198Abstract: A pharmaceutical or cosmetic carrier or composition for topical application characterized by rheological properties which render the carrier or composition semi-solid at rest and a liquid upon application of shear forces thereto. The composition or carrier are prepared by mixing 1-25 percent of a solidifying agent and 75-99 percent of a hydrophobic solvent, by weight, wherein at least one of them has therapeutic or cosmetic benefits, in the presence or absence of a biologically active substance.Type: ApplicationFiled: February 12, 2010Publication date: June 3, 2010Applicant: FOAMIX LTD.Inventors: Meir EINI, Dov TAMARKIN
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Publication number: 20100105559Abstract: An agrochemical composition includes a homogeneous single-phase liquid crystal in thermodynamic equilibrium. The agrochemical composition can be a surfactant composition or a pesticide composition. The surfactant composition is a blend of surfactants, whereas a pesticide composition has an active ingredient and one or more surfactant adjuvants. A pesticide composition, or a surfactant composition in combination with an active ingredient, may be used to control pests.Type: ApplicationFiled: October 9, 2007Publication date: April 29, 2010Applicant: Huntsman Petrochemical CorporationInventors: Curtis M. Elsik, Joe C. Arzola, Howard M. Stridde, Alan Stern
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Publication number: 20100041717Abstract: Compounds of formula (Ia) and (Ib), wherein A, B, C, R1and R14 are described herein.Type: ApplicationFiled: November 28, 2007Publication date: February 18, 2010Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Mark E. Salvati, James A. Johnson, Ningning Xu
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Publication number: 20100009937Abstract: A pesticide composition exhibiting streaming birefringence and methods for making the pesticide composition are disclosed. In one embodiment, the pesticide composition comprises an active ingredient and a surfactant adjuvant.Type: ApplicationFiled: September 20, 2007Publication date: January 14, 2010Applicant: Huntsman Petrochemical CorporationInventors: Curtis M. Elsik, Joe C. Arzola, Howard M. Stridde, Alan J. Stern
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Publication number: 20090312432Abstract: The present invention relates to fatty acid alkanolamides or polyolamides containing at least one group Y, where Y stands for CF3—(CH2)a—O—, SF5—, CF3—(CH2)a—S—, CF3CF2S—, [CF3—(CH2)a]2N— or [CF3—(CH2)a]NH—, where a stands for an integer selected from the range from 0 to 5, or formula (I), where Rf stands for CF3—(CH2)r—, CF3—(CH2)r—O—, CF3—(CH2)r—S—, CF3CF2—S—, SF5—(CH2)r— or (CH2)r]2N—, [CF3—(CH2)r]NH— or (CF3)2N—(CH2)r—, B stands for a single bond, O, NH, NR, CH2, C(O)—O, C(O), S, CH2—O, O—C(O), N—C(O), C(O)—N, O—C(O)—N, N—C(O)—N, O—SO2 or SO2—O, R stands for alkyl having 1 to 4 C atoms, b stands for 0 or 1 and c stands for 0 or 1, q stands for 0 or 1, where at least one radical from b and q stands for 1, and r stands for 0, 1, 2, 3, 4 or 5, to processes for the preparation of these compounds, and to uses of these surface-active compounds.Type: ApplicationFiled: July 2, 2007Publication date: December 17, 2009Inventors: Wolfgang Hierse, Nikolai (Mykola) Ignatyev, Martin Seidel, Elvira Montenegro, Peer Kirsch, Andreas Bathe
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Publication number: 20090298898Abstract: Compounds of formula wherein A0, A1 and A2 are each independently of the others a bond or a C1-C6alkylene bridge; A3 is a C1-C6alkylene bridge which is unsubstituted or substituted by from one to six identical or different substituents selected from halogen and C3-C8cycloalkyl; Y is, for example, O, S, SO or SO2; M is O or NOR6, X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylcarbonyl, C2-C6alkenyl, C2-C6haloalkenyl or C2-C6alkynyl; Q is, for example, O, S, SO or SO2; W is, for example, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; T is, for example, a bond, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; D is CH or N; R4 is, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl or C1-C6haloalkyl; R5 is, for example, C1-C12alkyl, C3-C8cycloalkyl or —N(R7)2; R7 is H, C1-C6alkyl, C1-C3haloalkyl, C1-C6alkylcarbonyl, C1-C3haloalkylcarbonyl, C1-C6alkoxycarbonyl, C3-C8cycloalkyl, C3-C8 cycloalkylType: ApplicationFiled: July 31, 2009Publication date: December 3, 2009Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Werner Zambach, Roger Graham Hall, Peter Renold, Stephan Trah
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Publication number: 20090275662Abstract: Injectable veterinary composition comprising a fluorinated chloramphenicol or thiamphenicol derivative and a solvent system comprising an ether of 1,2-ethanediol oligo- or polymers, and a pyrrolidone solvent.Type: ApplicationFiled: December 20, 2005Publication date: November 5, 2009Applicant: Intervet International B.V.Inventor: Carole Barbot
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Patent number: 7569727Abstract: Compounds of formula wherein A0, A1 and A2 are each independently of the others a bond or a C1-C6alkylene bridge; A3 is a C1-C6alkylene bridge which is unsubstituted or substituted by from one to six identical or different substituents selected from halogen and C3-C8cycloalkyl; Y is, for example, O, S, SO or SO2; M is O or NOR6, X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylcarbonyl, C2-C6alkenyl, C2-C6haloalkenyl or C2-C6alkynyl; Q is, for example, O, S, SO or SO2; W is, for example, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; T is, for example, a bond, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; D is CH or N; R4 is, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl or C1-C6haloalkyl; R5 is, for example, C1-C12alkyl, C3-C8cycloalkyl or —N(R7)2; R7 is H, C1-C6alkyl, C1-C3haloalkyl, C1-C6alkylcarbonyl, C1-C3haloalkylcarbonyl, C1-C6alkoxycarbonyl, C3-C8cycloalkyl, C3-C8 cycloalkylType: GrantFiled: April 7, 2008Date of Patent: August 4, 2009Assignee: Syngenta Crop Protection, Inc.Inventors: Werner Zambach, Roger Graham Hall, Peter Renold, Stephan Trah
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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: 20090170954Abstract: This invention is generally directed to a method for recovering florfenicol and florfenicol analogs from pharmaceutical compositions. The recovered florfenicol and analogs can be, for example, reused to make new pharmaceutical compositions and thereby reduce the need and expense of manufacturing new florfenicol and florfenicol analogs.Type: ApplicationFiled: December 12, 2008Publication date: July 2, 2009Applicant: Schering-Plough Ltd.Inventors: James C. Towson, Donal Coveney
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Patent number: 7550151Abstract: There is provided a cosmetic composition, preferably a cream, which continually provides a self-renewable textured surface appearance while in a container. The cosmetic composition has at least one volatile compound, preferably a fluorocarbon, such that the volatile compound expands resulting in expansion of the composition. The cosmetic composition has a viscosity from about 5,000 cps to about 2,500,000 cps.Type: GrantFiled: December 22, 2003Date of Patent: June 23, 2009Assignee: Avon Products, Inc.Inventor: Mark S. Garrison
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Publication number: 20090148512Abstract: A method for reducing the resistance of an MRSA bacterium to an antibiotic selected from the group consisting of vancomycin and methicillin comprising administering to a patient in need thereof an effective amount of chloramphenicol or analogues thereof. The invention is also directed to chloramphenicol containing pharmaceutical compositions.Type: ApplicationFiled: April 17, 2008Publication date: June 11, 2009Applicant: LANNETT CO INCInventor: Arthur P. Bedrosian
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Patent number: 7518017Abstract: Methods of preparing compounds of formula (I): wherein Y, Y1, and R2 are defined herein; methods of making D-(threo)-1-aryl-2-acylamido-1-propanol compounds, D-(threo)-1-aryl-2-acylamido-3-fluoro-1-propanol compounds, and D-(threo)-1-aryl-2-acylamido-3-hydroxy-1-propanol compounds (collectively, “fenicol compounds”) from the compound of formula (I); and new fenicol compounds, which can be made using the method.Type: GrantFiled: January 31, 2007Date of Patent: April 14, 2009Assignee: Idexx LaboratoriesInventors: Yerramilli V. S. N. Murthy, Felix Vattakunnel
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Publication number: 20090062397Abstract: The relatively low solubility of florfenicol (FEC) in water (1.3 mg/mL) limits its use in medicated drinking water systems for treatment of pulmonary disease of swine and poultry. Current formulations use a high volume organic solvent to reach the required FFC concentration of 13.5 mg/mL in an automated proportioner mixing tank system, with practical disadvantages for the users in the field. This invention relates to the effects of complex formation with natural and modified cyclodextrins on the aqueous solubility of FFC and antibiotics of related structure. Furthermore, this invention relates to the effects of polyethylene glycol (PEG-300) as a co-solvent in an FFC-cyclodextrin system to achieve the required FFC dose in the mixing tank system and to avoid high volumes of the organic solvent.Type: ApplicationFiled: April 23, 2008Publication date: March 5, 2009Inventors: Serena Tongiani, Keith Alan Freehauf
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Publication number: 20090062244Abstract: Topical composition for enhanced local and systemic delivery of poorly soluble biologically active compounds, comprises of non-volatile solvent or mixture of solvents to dissolve active component, and moisture absorbent or mixture of sorbents to prevent precipitation or crystallization of insoluble material after applicationType: ApplicationFiled: September 4, 2007Publication date: March 5, 2009Inventors: Joseph Schwarz, Michael Weisspapir
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Publication number: 20090012100Abstract: The present invention relates to the use of selective insecticidal compositions, characterized in that they comprise an effective amount of an active compound combination comprising (a) at least one compound of the formula (I) in which CKE, W, X, Y and Z are as defined in the description, and (b) at least one crop plant compatibility-improving compound, from the group of compounds mentioned in the description, for controlling insects and/or arachnids, and to a method for controlling insects and/or arachnids using the compositions.Type: ApplicationFiled: July 18, 2005Publication date: January 8, 2009Inventors: Reiner Fischer, Udo Reckmann, Christopher Hugh Rosinger, Erich Sanwald, Christian Arnold
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Publication number: 20080274184Abstract: This invention is directed to graft materials comprising an extracellular matrix (ECM) and therapeutic agents. This invention is also directed to methods of using the graft materials for healing of damaged or diseased tissues on a patient's body.Type: ApplicationFiled: March 31, 2005Publication date: November 6, 2008Inventor: James B. Hunt
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Patent number: 7402697Abstract: D-(threo)-1-aryl-2-disubstitutedacylamido-3-fluoro-1-propanol compounds compounds and analogues thereof (“Fenicol Compounds”), compositions comprising an effective amount of a Fenicol Compound, and methods for treating or preventing a bacterial infection in an animal comprising administering to an animal in need thereof an effective amount of a Fenicol Compound are disclosed.Type: GrantFiled: August 23, 2005Date of Patent: July 22, 2008Assignee: Idexx Laboratories Inc.Inventor: Yerramilli V. S. N. Murthy
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Publication number: 20080146527Abstract: Novel florfenicol compounds having the chemical structure: or a pharmaceutically-acceptable salt thereof or a solvate thereof, or prodrug thereof, wherein R1 is CHCl2, CHClF, CHF2, CHBrCl, CH3, CH2N3, CH2CN, CH(R2)NH2 or CH X1X2; where R2 is H, CH3 or CH2OH, and X1 and X2 are independently selected halogens; and R3 is CH2Cl, CH2F, CHF2, CHCl2 or CH2OH are disclosed. The compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals.Type: ApplicationFiled: February 27, 2008Publication date: June 19, 2008Inventors: Dale E. Shuster, Scott Hecker, Tomasz W. Glinka, Rajeshwar Singh, Zhuoyi Su
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Publication number: 20080132456Abstract: A pharmaceutical composition comprises a pharmaceutically effective amount of an active ingredient and low crystallinity cellulose having a crystallinity index of less than about 75% as measured by X-ray diffraction. The compositions advantageously may be provided in tablet form or granulate form and provide good stability against moisture degradation.Type: ApplicationFiled: December 9, 2005Publication date: June 5, 2008Inventors: Ragnar Ek, Maria Stromme, Albert Mihranyan
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Patent number: 7361689Abstract: Novel florfenicol compounds having the chemical structure: or a pharmaceutically-acceptable salt thereof or a solvate thereof, or prodrug thereof, wherein R1 is CHCl2, CHClF, CHF2, CHBrCl, CH3, CH2N3, CH2CN, CH(R2)NH2 or CH X1X2; where R2 is H, CH3 or CH2OH, and X1 and X2 are independently selected halogens; and R3 is CH2Cl, CH2F, CHF2, CHCl2 or CH2OH are disclosed. The compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals.Type: GrantFiled: December 21, 2004Date of Patent: April 22, 2008Assignee: Schering-Plough Animal Health CorporationInventors: Dale E. Shuster, Scott Hecker, Tomasz W. Glinka, Rajeshwar Singh, Zhuoyi Su
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Patent number: 7119229Abstract: Colchicine derivatives represented by the formula (I) with a halogen or nitric ester group, or pharmaceutically acceptable salts thereof, are described. Pharmaceutical compositions containing the same as effective components are also described. The colchicine derivatives were found to have anticancer, anti-proliferous and immunosuppressive function. Methods for preparing the colchicines derivatives are also provided.Type: GrantFiled: May 27, 2002Date of Patent: October 10, 2006Assignees: Chemtech Research Incorporation, KT & G CorporationInventors: Wan Joo Kim, Kyoung Soo Kim, Myung Hwa Kim, Jong Yek Park, Jung Min Jang, Jae Won Choi, Dong Hoo Kim
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Patent number: 7094431Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.Type: GrantFiled: September 30, 2003Date of Patent: August 22, 2006Inventor: Mickey L. Peshoff
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Patent number: 7026358Abstract: The present invention is directed to novel themisone derivative compounds that have been modified to prevent the formation of the toxic metabolite, 2-phenyl-acrylamide. Compositions comprising such derivative compounds have activity as anesthetics and as neuroprotective agents.Type: GrantFiled: April 15, 2002Date of Patent: April 11, 2006Assignee: University of Virginia Patent FoundationInventor: Milton L. Brown
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Patent number: 6964963Abstract: The present invention describes a process for preparing 4-amino-1-naphthol ethers which is characterized in that naphthol ethers are first prepared from 1-naphthols, the former are then converted to the corresponding 4-acetamino-1-naphthol ethers and then the acyl group is cleaved off, and further describes 4-acetamino-1-naphthol ethers obtained thereby.Type: GrantFiled: August 27, 2002Date of Patent: November 15, 2005Assignee: Bayer AktiengesellschaftInventors: Joachim Komoschinski, Herbert Diehl
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Patent number: 6960688Abstract: The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (I), Ring C is phenyl or a carbon linked heteroaryl ring substituted as defined within; R1 is an ortho substituent as defined within; n is 1 or 2; A-B is a linking group as defined within; R2 and R3 are as defined within; R4 is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described.Type: GrantFiled: October 23, 2002Date of Patent: November 1, 2005Assignee: AstraZeneca ABInventors: Roger J Butlin, Thorsten Nowak, Jeremy N Burrows, Michael H Block
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Patent number: 6870069Abstract: A phenyloxyaniline derivative useful as a ligand for peripheral benzodiazepine receptor having a strong affinity and a high selectivity, which is represented by formula (1): wherein X1 and X2 are same or different and each is hydrogen atom or halogen atom; R1 and R2 are same or different and each is hydrogen atom, an alkyl group having 1 to 10 carbon(s) or a halogen-substituted alkyl group having 1 to 10 carbon(s); and R3 is a halogen-substituted alkyl group having 1 to 5 carbon(s), or a radioisotope thereof.Type: GrantFiled: November 4, 2003Date of Patent: March 22, 2005Assignees: National Institute of Radiological Sciences, Taisho Pharmaceutical Co., Ltd., Nihon Nohyaku Co., Ltd.Inventors: Kazutoshi Suzuki, Ming-Rong Zhang, Tetsuya Suhara, Atsuro Nakazato, Makoto Goto
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Patent number: 6852888Abstract: There are described compounds of formula in free form or in salt form, a process for the preparation of such compounds and the use of such compounds, pesticidal compositions in which the active ingredient is selected from those compounds, in free form or in an agrochemically suitable salt form, a method of preparing such compositions and the use of such compositions, plant propagation material treated with such compositions, and a method of controlling pests.Type: GrantFiled: December 2, 2000Date of Patent: February 8, 2005Assignee: Syngenta Crop Protection, Inc.Inventors: Franziska Boeger, Peter Maienfisch, Thomas Pitterna, Christian Martin Boeger, Oliver Wolfang Boeger, Manfred Boeger
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Patent number: 6833389Abstract: Use of thiamphenicol and derivatives thereof for the preparation of pharmaceutical compositions useful for the treatment Chlamydia pneumoniae infections is described.Type: GrantFiled: December 11, 2001Date of Patent: December 21, 2004Assignee: Zambon Group S.p.A.Inventors: Giovanni Battista Colombo, Domenico Ungheri, Luciano Licciardello, Maria Rita Gismondo, Lorenzo Drago
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Patent number: 6790867Abstract: Novel formulations combining a non-steroidal anti-inflammatory drug (NSAID) such as flunixin, with a fluorinated chloramphenicol or thiamphenicol derivative antibiotic such as florfenicol are disclosed. Methods for using such formulations in the treatment and prevention of infectious diseases of bovines and swine, including bovine respiratory disease and swine respiratory disease, are also disclosed.Type: GrantFiled: January 24, 2003Date of Patent: September 14, 2004Assignee: Schering-Plough Animal Health CorporationInventors: Raul E. Kohan, Kanwal J. Varma, Robert D. Simmons, Abu Huq, Keith A. Freehauf
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Patent number: 6689909Abstract: A compound of formula (I) wherein: n is 1 or 2; R1 is chloro, fluoro, bromo, methyl or methoxy; R2 is as defined within; R3 is as defined within; and R4 is hydrogen or fluoro; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.Type: GrantFiled: June 17, 2002Date of Patent: February 10, 2004Assignee: AstraZeneca ABInventors: Roger John Butlin, Janet Elizabeth Pease, Michael Howard Block, Thorsten Nowak, Jeremy Nicholas Burrows
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Patent number: 6660773Abstract: A process for preparing 6-hydroxy-3,4-dihydroquinolinone by intramolecular Friedel-Crafts alkylation of N-(4-methoxyphenyl)-3-chloropropionamide in which an equivalent of N-(4-methoxyphenyl)-3-chloropropionamide is contacted with a Lewis acid in DMSO or a high boiling amide or amine at an elevated temperature of from about 150° C. to about 220° C. is provided. The process produces 6-HQ in high yield and a high state of purity such that it may be used in subsequent reactions toward the preparation of cilostazol without intermediate purification. A process for preparing cilostazol from 6-hydroxy-3,4-dihydroquinolinone prepared by the process and improved processes for preparing N-(4-methoxyphenyl)-3-chloropropionamide are also provided.Type: GrantFiled: March 8, 2002Date of Patent: December 9, 2003Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Marioara Mendelovici, Gideon Pilarsky, Tamar Nidam, Ben-Zion Dolitzky
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Publication number: 20030220302Abstract: Novel formulations combining a non-steroidal anti-inflammatory drug (NSAID) such as flunixin, with a fluorinated chloramphenicol or thiamphenicol derivative antibiotic such as florfenicol are disclosed. Methods for using such formulations in the treatment and prevention of infectious diseases of bovines and swine, including bovine respiratory disease and swine respiratory disease, are also disclosed.Type: ApplicationFiled: January 24, 2003Publication date: November 27, 2003Applicant: Schering-Plough Animal Health CorporationInventors: Raul E. Kohan, Kanwal J. Varma, Robert D. Simmons, Abu Huq, Keith A. Freehauf
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Patent number: 6589993Abstract: The present invention relates to methods of treating vancomycin-intermediates and multiresistant staphylococci infection using thiamphenicol or a salt thereof.Type: GrantFiled: October 16, 2001Date of Patent: July 8, 2003Assignee: Zambon Group S.p.A.Inventors: Domenico Ungheri, Luciano Licciardello
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Patent number: 6566554Abstract: The present invention relates to a compound of general formula (I) wherein R1, R2, and R3 represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)akylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl, or nitro; further R2 can be hydrogen, and R3 can be carboxy and carbamoyl; R4 represents hydrogen, (C1-C3)alkyl, or allyl; X represents oxygen or sulphur; Q represents —(CO)—, —(CS)—, or a bond; Y represents (C5-C15)alkyl; (C2-C15)olefinic group; (C3-C10)monocyclic hydrocarbon group; or phenyl; any of which may be optionally substituted by one or more, same or different substituents selected from the group consisting of the formula R5 defined below; (C1-C4)alkyl substituted by one or more substituents selected for the group R5; or a group of the formula —(Z—O)n—Z, wherein Z is a (C1-C3)alkyl, n is anType: GrantFiled: February 22, 2002Date of Patent: May 20, 2003Assignee: Leo Pharmaceutical Products Ltd. a/s (Lovens Kemiske Fabrik Produktionsaktieselskab)Inventor: Erik Rytter Ottosen
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Patent number: 6555710Abstract: The present invention relates to compounds of formula (I) wherein R1 and R2 independently represent one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl, or nitro; R2 further being represented by hydrogen; R3 represents hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, phenyl, cyano, carboxy or carbomoyl; R4 represents hydrogen, (C1-C3)alkyl, or allyl; X represents oxygen or sulpher; with the proviso that formula (I) does not comprise the compound 2,2,2-trifluoro-N-[2-[3-chloro-4-(2-methylbenzoyl)-phenylamino]-phenyl]acetamide wherein R1 is a 2-methyl, R2 is 2-chloro, R3 and R4 is hydrogen, and X is oxygen; and a salt thereof with a pharmaceutically accepType: GrantFiled: March 15, 2002Date of Patent: April 29, 2003Assignee: Leo Pharmaceutical Products Ltd a/s Lovens Kemiske Fabrik ProduktionsaktieselskabInventor: Erik Rytter Ottosen
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Publication number: 20030068339Abstract: An antibiotic formulation for animals is provided. This formulation includes florfenicol, a preservative and N-methyl-2-pyrrolidone. The florfenicol and preservative are dissolved in the N-methyl-2-pyrrolidone solvent. The formulation is suitable for veterinary applications in colder temperatures. More specifically, it is usable during winter months because it has a lower cold temperature viscosity than previous formulations resulting in it having superior syringeability.Type: ApplicationFiled: October 2, 2001Publication date: April 10, 2003Applicant: Phoenix Scientific, Inc.Inventors: John R. Carpenter, Richard Mihalik
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Publication number: 20030036564Abstract: A method is described for controlling the spread of Lyme disease spirochete from rodents which have been infected. The method involves orally administering to the rodents a composition which includes an antibiotic, e.g. chloramphenicol, thiamphenicol, florfenicol, or a salt or derivative thereof, or mixtures of antibiotics, capable of killing the spirochete. Bait compositions are described which include an antibiotic. The bait compositions may be solid or liquid.Type: ApplicationFiled: August 8, 2002Publication date: February 20, 2003Inventors: Jeff N. Borchert, Richard M. Poche
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Patent number: 6518310Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: March 16, 2001Date of Patent: February 11, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L Fedde, Carl R Illig, Thomas P. Markotan, Thomas P Stagnaro
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Patent number: 6498275Abstract: The use of compounds of the formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs: wherein: Ring C is phenyl or a carbon linked heteroaryl ring substituted as defmed within; R1 is an ortho substituent as defined within; n is 1 or 2; A—B is a linking group as defined within; R2 and R3 are as defined within; R4 is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are also described.Type: GrantFiled: November 15, 2000Date of Patent: December 24, 2002Assignee: AstraZeneca ABInventors: Roger J Butlin, Thorsten Nowak, Jeremy N Burrows, Michael H Block
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Publication number: 20020160978Abstract: This invention provides a method for the treatment of a subject in need of treatment for osteoarthritis comprising administering to said subject an amount of an inhibitor of spermidine biosynthesis sufficient to effect a substantial inhibition of spermidine biosynthesis. This invention also provides the use of an inhibitor of spermidine biosynthesis in the treatment of a subject in need of treatment of osteoarthritis in an amount sufficient to effect a substantial inhibition of spermidine biosynthesis. This invention further provides a method of preparing a therapeutic composition for the treatment of a subject in need of a treatment for osteoarthritis and the invention further provides a method of identifying an inhibitor of spermidine biosynthesis, whereby the inhibitor is a spermidine synthase inhibitor.Type: ApplicationFiled: December 12, 2001Publication date: October 31, 2002Inventors: Dganit Bar, Elena Feinstein, Orit Segev
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Patent number: 6472393Abstract: Compounds having the structure shown below wherein A, B, N1, N2, X, Y, Q, R2, R5 and R6 are as defined herein are useful to inhibit serine protease enzymes, such as TF/factor VIIa factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.Type: GrantFiled: March 21, 2000Date of Patent: October 29, 2002Assignee: Genentech, Inc.Inventors: Ignacio Aliagas-Martin, Dean R. Artis, Michael S. Dina, John A. Flygare, Richard A. Goldsmith, Regina A. Munroe, Alan G. Olivero, Richard Pastor, Thomas E. Rawson, Kirk D. Robarge, Daniel P. Sutherlin, Kenneth J. Weese, Aihe Zhou, Yan Zhu