Carboxyl, Or Salt Thereof, Bonded Directly To A Ring Patents (Class 562/458)
  • Publication number: 20150105559
    Abstract: Disclosed is a method for producing a compound having an amino group and/or a hydroxyl group from a substrate compound having an atomic group containing CO or CS by eliminating such atomic group. The substrate compound, having an atomic group containing CO or CS (for example, an amide, a carbamate, or the like), is allowed to react with a compound expressed by formula (I) below, at a temperature of 120° C. or lower, preferably in the presence of an ammonium salt, to eliminate such atomic group containing CO or CS. In formula (I) A may not be present, and in a case where A is present, A represents an alkyl group having 1 to 6 carbon atoms. H2N-A—NH2 (I) - - -.
    Type: Application
    Filed: March 4, 2013
    Publication date: April 16, 2015
    Applicant: Kyushu University, National University Corporation
    Inventors: Takashi Ohshima, Hiroyuki Morimoto, Yuhei Shimizu
  • Patent number: 8907127
    Abstract: The present invention relates to a preparation method of 4-aminomethylbenzoic acid comprising the following steps: preparing 4-carboxylbenzaldehyde or an alkyl ester thereof (methyl 4-formyl benzoate); reacting the 4-carboxylbenzaldehyde or an alkyl ester thereof (methyl 4-formyl benzoate) with hydroxyamine to oximate the same; and contact reducing 4-carboxylbenzaldehyde oxime or an alkyl ester oxime thereof obtained by the oximation, through hydrogen in a sodium hydroxide aqueous solution. Since methyl 4-hydroxyiminomethylbenzoate is reacted as a raw material in the presence of an alkali, hydrogen of a relatively low pressure can be used and a purification process is also simple, thereby enabling preparation of 4-aminomethylbenzoic acid with a low cost and high yield.
    Type: Grant
    Filed: December 9, 2010
    Date of Patent: December 9, 2014
    Assignees: NAF Co Ltd, SK Petrochemical Co Ltd
    Inventor: Woo Sun Kim
  • Patent number: 8846946
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also provides selective herbicidal compositions comprising, firstly, geminally alkoxy/alkylspirocyclically substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.
    Type: Grant
    Filed: January 31, 2013
    Date of Patent: September 30, 2014
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Stefan Lehr, Jan Dittgen, Dieter Feucht, Ulrich Görgens, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Arnd Voerste, Eva-Maria Franken, Olga Malsam
  • Publication number: 20140162064
    Abstract: Disclosed herein are high structured carbon blacks, methods of synthesis and treatment, and dispersions and inkjet ink formulations prepared therefrom. The carbon black can have the following properties: OAN?170 mL/100 g; and STSA ranging from 160 to 220 m2/g. The carbon black can also have the following properties: OAN?170 mL/100 g; and a ratio of STSA/BET surface area ranging from 0.7 to 1.
    Type: Application
    Filed: July 12, 2013
    Publication date: June 12, 2014
    Inventors: Andrew P. Dikan, Stephane F. Rouanet, Heather E. Clarke, Bruce E. MacKay, Danny Pierre
  • Patent number: 8703988
    Abstract: Nanostructures are formed from alkylated derivatives of aromatic acids of the formula: wherein at least one of R1 to R6 represents a carboxylic acid group, a primary amide group, an ester group, an amidine group, or a salt thereof, at least one other of R1 to R6 is X—Rc, and the remaining of R1 to R6 independently represent H or substituted or unsubstituted organic groups; X represents a linking group; and Rc represents a substituted or unsubstituted alkyl group.
    Type: Grant
    Filed: June 22, 2010
    Date of Patent: April 22, 2014
    Assignees: Xerox Corporation, National Research Council of Canada
    Inventors: Darren Andrew Makeiff, Rina Carlini
  • Patent number: 8686185
    Abstract: The present invention provides an efficient method for mass-producing 2-hydroxy-5-(substituted)phenylalkylamino benzoic acid derivatives represented by specific Chemical formulas or their salts, particularly 2-hydroxy-5-[2-(4-trifluoromethylphenyl)ethylamino]benzoic acid or its salt.
    Type: Grant
    Filed: October 30, 2008
    Date of Patent: April 1, 2014
    Assignee: Neurotech Pharmaceuticals Co., Ltd.
    Inventors: Byoung Joo Gwag, Jae Young Cho, Young Ae Lee, Cheng Qiling, Yulian Wu, Li Xing
  • Patent number: 8669209
    Abstract: Soluble granule formulations of amine salts of pyridine containing carboxylic acids with improved handling properties are provided by an improved process in which the pyridine containing carboxylic acid is partially neutralized with an amine.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: March 11, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Franklin N. Keeney, Neil A. Foster, Martin C. Logan, Maria G. Perry
  • Publication number: 20130288268
    Abstract: The present invention provides compounds of Formula I: wherein: R1 is a label (e.g., a detectable groups; an anti-tumor agent)s; L is present or absent and when present is a linking group; and x represents an integer from 1 to 10; or a pharmaceutically acceptable salt thereof. the compounds are useful for, among other things, identifying cysteine sulfenic acids in proteins and monitoring oxidative damage in proteins and cells.
    Type: Application
    Filed: June 18, 2013
    Publication date: October 31, 2013
    Inventors: Leslie B. Poole, S. Bruce King, Jacquelyn S. Fetrow
  • Publication number: 20130131006
    Abstract: The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death.
    Type: Application
    Filed: April 28, 2011
    Publication date: May 23, 2013
    Applicant: Gachon University of Industry-Academic Cooperation Foundation
    Inventors: Bong Hee Lee, Kyung Hee Byun
  • Publication number: 20120330056
    Abstract: A method for preparing aromatic carboxylic acid derivatives by nucleophilic aromatic substitution, involves reacting an aromatic carboxylic acid derivative supporting only one carboxyl function, or one of the salts thereof, the carboxylic acid derivative supporting, orthogonally to the carboxyl function, a leaving group which is a fluorine or chlorine atom or an alkoxy group, chiral or otherwise and, in the latter case, preferably a methoxy group; the carboxylic acid derivative being substituted by at least one electro-attractive group other than the leaving group, preferably by a fluorine atom, with a MNu reagent, wherein M is a metal and Nu an optionally chiral nucleophile, the nucleophilic aromatic substitution reaction being carried out without a catalyst and without a step of protecting/unprotecting the acid function of the initial compound, the method being selective in that the reaction leads to the formation of ketone derivatives in a very minority fashion during the reaction.
    Type: Application
    Filed: February 18, 2011
    Publication date: December 27, 2012
    Applicants: UNIVERSITE DU MAINE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Jacques Mortier, Anne-Sophie Castanet, Arnaud Nourry, Mickael Belaud-Rotureau
  • Publication number: 20120316337
    Abstract: Method for preparing carboxylic acid derivatives by aromatic nucleophilic substitution, in which a carboxylic acid derivative having a single carboxyl functional group, or one of the salts thereof, the carboxylic acid derivative having, in the ortho position of the carboxyl functional group, a leaving group, which is preferably an atom of fluorine or of chlorine or an alkoxy group, chiral or not, preferably a methoxy group, the carboxylic acid derivative not being substituted by an electro attractive group other than the leaving group if any; is reacted with a reactant MNu, where M is a metal and Nu is a nucleophile, chiral or not, the aromatic nucleophilic substitution reaction being carried out without a catalyst and without a step of protecting/deprotecting the acid functional group of the starting compound.
    Type: Application
    Filed: February 17, 2011
    Publication date: December 13, 2012
    Applicants: UNIVERSITE DU MAINE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Jacques Mortier, Anne-Sophie Castanet, Mickael Belaud-Rotureau
  • Patent number: 8327467
    Abstract: The anthranilic acid derivative or the salt thereof represented by the general formula wherein R1 and R2 are hydrogen atom, or the like; R3 is a phenyl, cycloalkyl or bicyclic heterocyclic group which may be substituted, or the like; R4 is a phenyl, cycloalkyl or pyridyl group which may be substituted, or the like; X1 is an alkylene or alkenylene group which may be substituted or a bond; X2 is the general formula —X3—X4— or —X4—X3—, wherein X3 is a sulfur atom, an imino group or a bond, or the like; X4 means an alkylene or alkenylene group which may be substituted or a bond; is useful for a remedy such as rheumatoid arthritis, osteoarthritis and carcinoma, because it shows MMP—13 production inhibitory effect.
    Type: Grant
    Filed: March 14, 2006
    Date of Patent: December 11, 2012
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Junichi Yokotani, Yoichi Taniguchi, Eiji Hara, Hitoshi Akitsu, Hidehiko Tanaka, Shuzo Anzai
  • Publication number: 20120294866
    Abstract: The present invention provides a liquid pharmaceutical formulation comprising a therapeutic protein, a surfactant and at least an antioxidant selected from the group of radical scavengers, chelating agents or chain terminators.
    Type: Application
    Filed: January 14, 2010
    Publication date: November 22, 2012
    Applicant: F. HOFFMANN-LA ROCHE AG
    Inventors: Hanns-Christian Mahler, Satya Krishna Kishore Ravuri
  • Publication number: 20120296114
    Abstract: The present invention relates to a preparation method of 4-aminomethylbenzoic acid comprising the following steps: preparing 4-carboxylbenzaldehyde or an alkyl ester thereof (methyl 4-formyl benzoate); reacting the 4-carboxylbenzaldehyde or an alkyl ester thereof (methyl 4-formyl benzoate) with hydroxyamine to oximate the same; and contact reducing 4-carboxylbenzaldehyde oxime or an alkyl ester oxime thereof obtained by the oximation, through hydrogen in a sodium hydroxide aqueous solution. Since methyl 4-hydroxyiminomethylbenzoate is reacted as a raw material in the presence of an alkali, hydrogen of a relatively low pressure can be used and a purification process is also simple, thereby enabling preparation of 4-aminomethylbenzoic acid with a low cost and high yield.
    Type: Application
    Filed: December 9, 2010
    Publication date: November 22, 2012
    Applicants: SK PETROCHEMICAL CO., LTD., NAF CO., LTD.
    Inventor: Woo Sun Kim
  • Patent number: 8283453
    Abstract: The present invention provides a method for selectively placing carbon nanotubes on a substrate surface by using functionalized carbon nanotubes having an organic compound that is covalently bonded to such carbon nanotubes. The organic compound comprises at least two functional groups, the first of which is capable of forming covalent bonds with carbon nanotubes, and the second of which is capable of selectively bonding metal oxides. Such functionalized carbon nanotubes are contacted with a substrate surface that has at least one portion containing a metal oxide. The second functional group of the organic compound selectively bonds to the metal oxide, so as to selectively place the functionalized carbon nanotubes on the at least one portion of the substrate surface that comprises the metal oxide.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: October 9, 2012
    Assignee: International Business Machines Corporation
    Inventors: Ali Afzali-Ardakani, Phaedon Avouris, James B. Hannon, Christian Klinke
  • Patent number: 8263658
    Abstract: Compounds of formula (I) are provided, wherein X is CH?CH, CH2O wherein the oxygen atom is bound to ring B, or OCH2 wherein the oxygen atom is bound to ring A; Y is hydrogen, straight or branched C1-C6 alkyl or a pharmaceutically acceptable inorganic cation; R1 is ethyl or cyclopropyl; and R2 and R3 are the same or different and are selected from F, Cl, Br, CF3 and OCF3. The compounds are useful for the treatment of autoimmune diseases, inflammatory diseases, organ transplant rejection, and malignant neoplasia. Pharmaceutical compositions comprising the compounds, methods of using the compounds, and methods for preparing the compounds are also provided.
    Type: Grant
    Filed: August 4, 2009
    Date of Patent: September 11, 2012
    Assignee: Chelsea Therapeutics, Inc.
    Inventors: Helén Tuvesson Andersson, Ulf Vellmar, Ingrid Hallin, Leif Svenson, Ingela Fritzson
  • Publication number: 20120214742
    Abstract: A GABA (gamma-aminobutyric acid) release-inhibiting agent in the cerebellum and a composition for treating pathological symptoms caused by over-release of GABA in the cerebellum, each comprising a Bestrophin 1(Best1) channel inhibitor as an active ingredient; a GABA release-promoting agent in the cerebellum and a composition for treating pathological symptoms caused by the deficit of GABA in the cerebellum, each comprising a Best1 channel activator as an active ingredient; and a method for screening a GABA release-regulating agent in the cerebellum, which uses Best1 channel as target, are provided.
    Type: Application
    Filed: August 24, 2010
    Publication date: August 23, 2012
    Inventors: Changjoon Justin Lee, Soo-Jung Lee, Bo-Eun Yoon
  • Publication number: 20120203031
    Abstract: The process of the present invention creates a sustainable and closed water loop allowing inherent recycles of all liquid streams generated in the process. The liquid streams generated during the process of the invention are inherently recycled completely, making the process of the present invention a zero liquid discharge process which is environmentally friendly and sustainable. This invention further relates to a sustainable chemical process of reduction of R—NO2 or R—NO into corresponding R—NH2 that produces environmentally friendly R—NH2 in good yields and selectivity with large of mother liquor recycle. The process has a wide scope in that it can be applied to a number of molecules.
    Type: Application
    Filed: October 18, 2010
    Publication date: August 9, 2012
    Applicant: NEWREKA CHEMICALS PRIVATE LIMITED
    Inventors: Bhadresh K. Padia, Nitesh H. Mehta
  • Patent number: 8211878
    Abstract: The present invention provides methods for prevention and prophylaxis of neurological diseases accompanied by neuronal death in a patient. The invention includes use of 5-benzylamino salicylic acid (BAS) and its derivatives. Thus, the present invention provides methods for reducing neuronal death in nervous system injuries resulting from amyotrophic lateral sclerosis.
    Type: Grant
    Filed: May 24, 2010
    Date of Patent: July 3, 2012
    Assignee: Neurotech Pharmaceuticals Co., Ltd.
    Inventors: Byoung Joo Gwag, Young Ae Lee, Bo Rum Ryu, Sung Hwa Yoon, Ho Sang Moon
  • Patent number: 8178516
    Abstract: This invention defines novel compositions that can be used for clinical treatment of a class of chronic inflammatory diseases. Increased generation of carbonyl substances, namely aldehydes and ketones, occurs at sites of chronic inflammation and is common to the etiologies of all of the clinical disorders addressed herein. Such carbonyl substances are cytotoxic and additionally serve to perpetuate and disseminate the inflammatory process. This invention defines use of compositions, the orally administered required primary agents of which are primary amine derivatives of benzoic acid capable of covalently reacting with the carbonyl substances. p-Aminobenzoic acid (or PABA) is an example of the required primary agent of the present invention. PABA has a small molecular weight, is water-soluble, has a primary amine group which reacts with carbonyl-containing substances and is tolerated by the body in relatively high dosages for extended periods.
    Type: Grant
    Filed: February 20, 2008
    Date of Patent: May 15, 2012
    Assignee: Sylvan Labs, LLC
    Inventor: Howard K. Shapiro
  • Publication number: 20120101164
    Abstract: A composition comprising a compound selected from an auxin, an auxin precursor, an auxin metabolite or a derivative of said auxin, auxin precursor or auxin metabolite or a mixture thereof and optionally acetaminophen or a derivative thereof for improving post-harvest storability of crops.
    Type: Application
    Filed: April 7, 2010
    Publication date: April 26, 2012
    Applicant: TAMINCO, NAAMLOZE VENNOOTSCHAP
    Inventors: Richard Henry Williams, Peter Roose, Johan Josef De Saegher
  • Publication number: 20120088668
    Abstract: A composition comprising a compound selected from an auxin, an auxin precursor, an auxin metabolite or a derivative of said auxin, auxin precursor or auxin metabolite or a mixture thereof and acetaminophen or a derivative thereof for use as a chemical thinning agent.
    Type: Application
    Filed: April 7, 2010
    Publication date: April 12, 2012
    Applicant: TAMINCO, NAAMLOZE VENNOOTSCHAP
    Inventors: Richard Williams, Tom Deckers, Peter Roose, Johan Josef De Saegher
  • Publication number: 20120052757
    Abstract: The present invention provides methods of designing molecularly imprinted polymers (MIPs) which have applications in extracting bioactive compounds from a range of bioprocessing feedstocks and wastes. The present invention is further directed to MIPs designed by the methods of the present invention.
    Type: Application
    Filed: January 29, 2010
    Publication date: March 1, 2012
    Applicant: MONASH UNIVERSITY
    Inventors: Milton T. W. Hearn, Steven Langford, Kellie Louise Tuck, Simon Harris, Reinhard Ingemar Boysen, Victoria Tamara Perchyonok, Basil Danylec, Lachlan Schwarz, Jamil Chowdhury
  • Publication number: 20120041224
    Abstract: The present invention relates to a process for the preparation of iodinated anilines; in particular, it relates to a process including the direct iodination, with suitably activated iodine, of 3,5-disubstituted anilines to the corresponding 3,5-disubstituted-2,4,6-triiodoanilines, which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves.
    Type: Application
    Filed: April 8, 2010
    Publication date: February 16, 2012
    Applicant: BRACCO IMAGING S.P.A.
    Inventors: Attilio Citterio, Luciano Lattuada, Gabriella Leonardi, Fulvio Uggeri, Evelin Vignale, Massimo Visigalli, Aurelia Ferrigato, Gabriele Meli, Roberta Fretta, Roberta Mazzon
  • Publication number: 20120010233
    Abstract: Small molecules and their derivatives are described for the treatment and/or prevention of intestinal fluid loss. Also disclosed are methods of using said molecules and their derivatives to treat and/or prevent conditions associated with increased levels of 3?,5?-adenosine monophosphate. Specific compositions of the invention are also novel.
    Type: Application
    Filed: June 7, 2011
    Publication date: January 12, 2012
    Applicants: Board of Regents, The University of Texas, Mission Pharmacal Co.
    Inventors: Catherine H. Schein, Scott R. Gilbertson, Johnny W. Peterson, Deliang Chen, Maria Esterlla-Jimenez, Mary A. Walter, Jian Gao
  • Patent number: 8084634
    Abstract: The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein R1 is defined as in claim 1.
    Type: Grant
    Filed: February 23, 2010
    Date of Patent: December 27, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Guenther Huchler, Werner Rall, Uwe Reis
  • Publication number: 20110313154
    Abstract: A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c): (a) reacting an acyl phenylalanine derivative represented by the following formula (2): with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative; (b) converting the carboxy-asymmetric urea derivative into the corresponding quinazoline-dione derivative in the presence of a carboxyl group-activating agent: (c) if desired, substituting an N-alkyl group for the hydrogen atom bonded to the nitrogen atom present in the quinazoline-dione ring of the quinazoline-dione derivative using an N-alkylation agent and then deprotecting the resulting product, when the substituent R3? which is a group corresponding to R3 is protected.
    Type: Application
    Filed: August 26, 2011
    Publication date: December 22, 2011
    Applicant: AJINOMOTO CO., INC.
    Inventors: Noriyasu KATAOKA, Kotaro OKADO, Tatsuhiro YAMADA, Koichi FUJITA, Tamotsu SUZUKI, Tatsuya OKUZUMI, Masayuki SUGIKI, Akinori TATARA
  • Publication number: 20110311813
    Abstract: Nanostructures are formed from alkylated derivatives of aromatic acids of the formula: wherein at least one of R1 to R6 represents a carboxylic acid group, a primary amide group, an ester group, an amidine group, or a salt thereof, at least one other of R1 to R6 is X—Rc, and the remaining of R1 to R6 independently represent H or substituted or unsubstituted organic groups; X represents a linking group; and Rc represents a substituted or unsubstituted alkyl group.
    Type: Application
    Filed: June 22, 2010
    Publication date: December 22, 2011
    Applicants: NATIONAL RESEARCH COUNCIL OF CANADA, XEROX CORPORATION
    Inventors: Darren Andrew MAKEIFF, Rina Carlini
  • Patent number: 8003704
    Abstract: Use is disclosed of (a) an AlDH-inhibitory amount of a Trp metabolite, or an analogue or derivative thereof or (b) a bioprecursor thereof, or (c) a potentiator of (a) and/or (b), in the preparation of a medicament for treating alcoholism and/or alcohol dependence.
    Type: Grant
    Filed: July 2, 2001
    Date of Patent: August 23, 2011
    Inventor: Abdulla Abu-Bakr Badawy
  • Patent number: 7947851
    Abstract: The present invention is related to carboxylic acids of Formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of carboxylic acids of Formula (I) to modulate, notably to inhibit the activity of PTPs.
    Type: Grant
    Filed: March 29, 2005
    Date of Patent: May 24, 2011
    Assignee: Merck Serono SA
    Inventors: Dominique Swinnen, Catherine Jorand-Lebrun, Patrick Gerber, Jerome Gonzalez, Agnes Bombrun
  • Publication number: 20110112187
    Abstract: The present invention relates to the use of tranilast and derivatives thereof for the preparation of a pharmaceutical composition for treating and/or preventing a neuronal condition where there is a need of neuroprotection and neuroregeneration. The invention furthermore relates to the use of tranilast and derivatives thereof for the in vitro differentiation of neuronal stem cells and the use of such pre-treated cells for stem cell therapy von neurological conditions.
    Type: Application
    Filed: August 15, 2008
    Publication date: May 12, 2011
    Inventors: Armin Schneider, Anja Moraru, Carola Krüger, Rice Laage, Claudia Pitzer
  • Publication number: 20110009626
    Abstract: The present invention relates to an adenosine A3 receptor ligand of the general formula (VI?), (VII?) and (VIII?) and their preparation.
    Type: Application
    Filed: August 11, 2010
    Publication date: January 13, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Peter ARANYI, Sandor BATORI, Geza TIMARI, Kinga BOER, Zoltan KAPUI, Endre MIKUS, Katalin URBAN-SZABO, Katalin GERBER, Judit VARGANE SZEREDI, Michel FINET
  • Publication number: 20100041748
    Abstract: The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative.
    Type: Application
    Filed: July 8, 2009
    Publication date: February 18, 2010
    Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Jesse J. Smith
  • Publication number: 20090318688
    Abstract: A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c): (a) reacting an acyl phenylalanine derivative represented by the following formula (2): with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative; (b) converting the carboxy-asymmetric urea derivative into the corresponding quinazoline-dione derivative in the presence of a carboxyl group-activating agent: (c) if desired, substituting an N-alkyl group for the hydrogen atom bonded to the nitrogen atom present in the quinazoline-dione ring of the quinazoline-dione derivative using an N-alkylation agent and then deprotecting the resulting product, when the substituent R3? which is a group corresponding to R3 is protected.
    Type: Application
    Filed: May 22, 2009
    Publication date: December 24, 2009
    Applicant: AJINOMOTO CO., INC.
    Inventors: Noriyasu KATAOKA, Kotaro OKADO, Tatsuhiro YAMADA, Koichi FUJITA, Tamotsu SUZUKI, Tatsuya OKUZUMI, Masayuki SUGIKI, Akinori TATARA
  • Publication number: 20090197957
    Abstract: The present invention relates generally to the area of pain management and more particularly, to a method of analgesia and agents useful for same. More particularly, the present invention relates to a method of analgesia utilising a compound of formula (I). The method of the present invention is useful, inter alia, in the therapeutic or prophylactic treatment of pain, including acute pain, chronic non-malignant pain and chronic malignant pain. Also provided are compounds for use in the method of the invention.
    Type: Application
    Filed: May 16, 2006
    Publication date: August 6, 2009
    Inventors: Michael Lionel Selley, Richard Owen Williams, Julia Jane Inglis
  • Publication number: 20090188869
    Abstract: Multi-layered macromolecules wherein the layers are covalently bonded together and wherein the macromolecules are covalently bonded to solid particulate substrates, methods for the preparation of such compositions, and methods for their uses in a multitude of end use applications ranging from the purification of waste chemical and metal process streams to the separation and identification of proteins, peptides, and oligionucleotides.
    Type: Application
    Filed: May 2, 2008
    Publication date: July 30, 2009
    Inventors: Charles E. Skinner, William Henry Campbell, Yung K. Kim
  • Publication number: 20090171116
    Abstract: A continuous process for forming an anthranilic acid which includes treating in a first step a mixture comprising a carbonate salt and an anthranilic acid salt of the formula (I) where R is selected from hydrogen and one or more substituted or unsubstituted hydrocarbon groups, and M is a univalent cation, with an inorganic acid in an aqueous medium to form an aqueous slurry comprising anthranilic acid and inorganic salts. The slurry is filtered to provide a residue comprising part of said anthranilic acid and a filtrate comprising the remainder of said anthranilic acid and said inorganic salts. Further anthranilic acid is extracted from said filtrate with a water-immiscible organic solvent, whereby the further anthranilic acid is separated into an organic phase while the inorganic salts remain in an aqueous phase. The organic phase is contacted with an aqueous alkali to thereby transfer said further anthranilic acid from said organic phase to an aqueous phase as an anthranilic acid salt.
    Type: Application
    Filed: January 30, 2007
    Publication date: July 2, 2009
    Inventor: Carsten Berg
  • Patent number: 7528260
    Abstract: A method is disclosed for preparing compounds of Formula 1 by combining compounds of Formulae 2 and 3 and a sulfonyl chloride. Also disclosed are compounds of Formula 3, which are useful as starting materials for this method.
    Type: Grant
    Filed: December 6, 2005
    Date of Patent: May 5, 2009
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Rafael Shapiro, Eric de Guyon Taylor, William T. Zimmerman
  • Publication number: 20090105474
    Abstract: The anthranilic acid derivative or the salt thereof represented by the general formula wherein R1 and R2 are hydrogen atom, or the like; R3 is a phenyl, cycloalkyl or bicyclic heterocyclic group which may be substituted, or the like; R4 is a phenyl, cycloalkyl or pyridyl group which may be substituted, or the like; X1 is an alkylene or alkenylene group which may be substituted or a bond; X2 is the general formula -X3-X4- or -X4-X3-, wherein X3 is a sulfur atom, an imino group or a bond, or the like; X4 means an alkylene or alkenylene group which may be substituted or a bond; is useful for a remedy such as rheumatoid arthritis, osteoarthritis and carcinoma, because it shows MMP-13 production inhibitory effect.
    Type: Application
    Filed: March 14, 2006
    Publication date: April 23, 2009
    Applicant: Toyama Chemical Co., Ltd.
    Inventors: Junichi Yokotani, Yoichi Taniguchi, Eiji Hara, Hitoshi Akitsu, Hidehiko Tanaka, Shuzo Anzai
  • Publication number: 20090076150
    Abstract: The present application describes deuterium-enriched bromfenac, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: August 22, 2008
    Publication date: March 19, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Publication number: 20090023734
    Abstract: The invention provides compounds and methods for treating cell proliferative diseases. The invention provides new inhibitors of histone deacetylase enzymatic activity, compositions of the compounds comprising the inhibitors and a pharmaceutically acceptable carrier, excipient, or diluent, and methods of using the compounds to inhibit cellular proliferation in vitro and therapeutically.
    Type: Application
    Filed: January 8, 2007
    Publication date: January 22, 2009
    Applicant: METHYLGENE INC.
    Inventors: Stephane Raeppel, Frederic Gaudette, Isabelle Paquin, Arkadii Vaisburg, Daniel Delorme
  • Patent number: 7408076
    Abstract: Disclosed are 2-bromoaniline or 2-chloroaniline compounds of formula (I): wherein R, R1 and X are as defined. The compounds are useful as intermediates for preparing indole compounds.
    Type: Grant
    Filed: August 29, 2006
    Date of Patent: August 5, 2008
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Guisheng Li, Jianxiu Liu, Zhi-Hui Lu, Frank Roschangar, Chris Hugh Senanayake, Ming Shen
  • Patent number: 7408078
    Abstract: The present invention provides pharmaceutical compositions useful in treating hepatitis C infection. The present invention also provides methods of treating hepatitis C infection by administering to a mammal the pharmaceutical compositions of the present invention.
    Type: Grant
    Filed: October 8, 2003
    Date of Patent: August 5, 2008
    Assignees: Wyeth, ViroPharma Incorporated
    Inventors: Jonathan D. Bloom, Thomas R. Bailey
  • Patent number: 7371896
    Abstract: The present invention relates to a tetrafluorobenzyl derivative and a pharmaceutical composition for prevention and treatment of acute and chronic neurodegenerative disease in central nervous system and ophthalmic diseases containing the same. The tetrafluorobenzyl derivative of the present invention can effectively be used to prevent and treat chronic neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease and Huntington's disease, degenerative brain disease such as epilepsy and ischemic brain disease such as stroke.
    Type: Grant
    Filed: June 8, 2006
    Date of Patent: May 13, 2008
    Assignee: AmKor Pharma, Inc.
    Inventors: Byoung-Joo Gwag, Sung-Hwa Yoon, Ho-Sang Moon, Eun-Chan Park, Seok-Joon Won, Young-Ae Lee, Hae-Un Lee
  • Patent number: 7279597
    Abstract: Phenyl amine carboxylic acid compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.
    Type: Grant
    Filed: November 6, 2000
    Date of Patent: October 9, 2007
    Assignee: Emisphere Technologies, Inc.
    Inventors: Andrea Leone-Bay, Kelly Kraft, Maria A. P. Boyd
  • Patent number: 7268248
    Abstract: The present invention relates to 3-cyano-2,4,5-trifluorobenzoyl fluoride and to intermediates for its preparation and to the process for the preparation of 3-cyano-2,4,5-trifluoro-benzoyl fluoride, which starts from 5-fluoro-1,3-xylene (VIII); which is bichlorinated in the ring in the presence of a catalyst under ionic conditions to give 2,4-dichloro-5-fluoro-1,3-dimethylbenzene (VII). The latter is chlorinated in the side chains under free-radical conditions to give 2,4-dichloro-5-fluoro-3-dichloromethyl-1-trichloromethylbenzene (VI).
    Type: Grant
    Filed: December 31, 2003
    Date of Patent: September 11, 2007
    Assignee: Bayer Aktiengesellschaft
    Inventors: Albrecht Marhold, Peter Wolfrum
  • Patent number: 6936597
    Abstract: Polymeric prodrugs of the formula: wherein B is selected from the group consisting of OH, leaving groups, residues of amine-containing moieties and a residues of hydroxyl-containing moieties; Y1 is selected from the group consisting of O, S, and NR5; M is NR3, O or S; Ar is a moiety which when included in Formula I forms a multi-substituted aromatic or heteroaromatic hydrocarbon or a multi-substituted heterocyclic group; (m) is zero or a positive integer; R1-3 and R5 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; and R4 is a polymeric residue; as well as methods of making and using the same are disclosed.
    Type: Grant
    Filed: March 21, 2002
    Date of Patent: August 30, 2005
    Assignee: Enzon, Inc.
    Inventors: Richard B. Greenwald, Yun H. Choe
  • Patent number: 6747170
    Abstract: A thermosensitive recording material has a support and a thermosensitive coloring layer formed thereon containing a leuco dye and a color developer capable of inducing color formation in the leuco dye upon application of heat thereto, with the color developer including at least one compound (A) having in a molecule thereof at least two aromatic ring moieties with specific structures, selected from the group consisting of an aromatic ring moiety having at least one carboxyl group and electron-attracting functional group, an aromatic ring moiety having at least one carboxyl group and electron-donating functional group, and an aromatic ring moiety having at least one carboxyl group, free of the electron-attracting and electron-donating functional groups. An aromatic carboxylic acid compound serving as the above-mentioned compound (A) and the producing method thereof are also disclosed.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: June 8, 2004
    Assignee: Ricoh Company, Ltd.
    Inventors: Kunio Hayakawa, Mitsunobu Morita
  • Patent number: 6727098
    Abstract: A novel achiral biaryl-type compound and a circular dichroism (CD) color fixing agent are provided. Furthermore, a method for determining an absolute configuration of a chiral compound is carried out by introducing the above achiral biaryl-type compound into the chiral compound.
    Type: Grant
    Filed: February 26, 2002
    Date of Patent: April 27, 2004
    Assignee: Kanazawa University
    Inventors: Tomihisa Ohta, Shinzo Hosoi
  • Patent number: RE39682
    Abstract: Novel farnesyl derivatives which are inhibitors of the prenylated protein methyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: wherein R1represents farnesyl, geranyl or geranyl-geranyl; Z represents C—R6 or N; R2 represents H, CN, the groups COOR7, SO3R7, CONR7R8 and SO2NR7R7, wherein R7 and R8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO3M, wherein M is a cation; R3, R4, R5 and R6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato; X represents O, S, SO, SO2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.
    Type: Grant
    Filed: March 30, 2005
    Date of Patent: June 5, 2007
    Assignee: Ramot at Tel Aviv University Ltd.
    Inventor: Yoel Kloog