Sulfur In Acid Moiety Patents (Class 560/9)
  • Patent number: 10442761
    Abstract: This invention relates to novel deuterated forms of GFT-505, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are characterized by reduced PPAR-alpha and/or PPAR-delta activity.
    Type: Grant
    Filed: February 16, 2017
    Date of Patent: October 15, 2019
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Roger D. Tung
  • Publication number: 20150119458
    Abstract: The present invention discloses a 4-((substituted phenyl)difluoromethyl)phenoxycarboxylic acid derivative and preparation process and use thereof. More specifically, the present invention relates to a compound of the following formula I, which is defined in the specification. The compounds according to the present invention can be used as PPAR agonists, and demonstrates a strong effect on reducing the levels of total cholesterol (TC), triglyceride (TG), and low density lipoprotein cholesterol (LDL-C) in blood plasma, and thus the compound according to the present invention can be used in the preparation of a medicament for treating or preventing hyperlipoidemia or cardio-cerebrovascular diseases caused by hyperlipoidemia, such as diabetes, atherosclerosis, stroke, coronary heart disease, etc. The present invention also relates to a novel intermediate compound for the preparation of the compound of formula I and preparation method thereof.
    Type: Application
    Filed: April 25, 2013
    Publication date: April 30, 2015
    Applicant: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Hua Bai, Jian Hong, Lifeng Cai, Hegeng Wei, Xiaoyu Liu, Xiaohe Zheng
  • Patent number: 8987498
    Abstract: A compound of formula wherein PROT is an amine protecting group and PROT? is hydrogen; or PROT and PROT? together with the nitrogen atom to which they are attached form a heterocyclic ring as an amine protecting group, and PROT? is a thiol protecting group, processes for its production, intermediates in their production and production of intermediates in stereoisomerically pure form, and their use for the production of pharmaceutically active compounds.
    Type: Grant
    Filed: May 23, 2011
    Date of Patent: March 24, 2015
    Assignee: Nabriva Therapeutics AG
    Inventors: Rosemarie Riedl, Werner Heilmayer, Lee Spence, Atchyuta Rama Chandra Murty Bulusu
  • Publication number: 20150056305
    Abstract: Provided are dithiol mucolytic agents. These agents increase the liquefaction of mucus in a patient with excessive mucus or mucus with increased viscoelastic, cohesive, or adhesive properties. Also provided are a variety of methods of treatment using these inventive mucolytic agents.
    Type: Application
    Filed: August 13, 2014
    Publication date: February 26, 2015
    Applicant: PARION SCIENCES, INC.
    Inventors: Michael R. Johnson, William R. Thelin, Ronald A. Aungst, JR.
  • Patent number: 8841476
    Abstract: Provided herein are processes of preparing ezatiostat hydrochloride, and crystalline ezatiostat hydrochloride ansolvate form D.
    Type: Grant
    Filed: April 26, 2011
    Date of Patent: September 23, 2014
    Assignee: Telik, Inc.
    Inventors: Guyselaine Leclerc, Hervé Lhermitte, Christian Picherit
  • Patent number: 8765992
    Abstract: The invention relates to methods for producing chalcone (1,3-diphenylprop-2-en-1-one) derivatives that have multiple substitutions on a phenyl ring. Intermediate chalcone derivatives are modified by Phase Transfer Catalysis (PTC) for introducing a substituted alkyl group that is provided by a sulfonic acid derivative on a phenyl ring already containing substituent groups on one or two carbon atoms adjacent to the carbon atom where a substituent group is being introduced. The methods of the invention allow producing efficiently, by either S-alkylation or O-alkylation, chalcones derivatives that are characterized for their biological activities that are intermediate compounds for producing molecules having such activities, or that can be used for generating libraries of compounds to be screened by means of in vitro and/or in vivo assays and establishing structure-activity relationships.
    Type: Grant
    Filed: May 16, 2011
    Date of Patent: July 1, 2014
    Assignee: Genfit
    Inventors: Karine Bertrand, Alice Roudot, Patrice Rool
  • Patent number: 8722745
    Abstract: The invention relates to a sulfur-containing compound and the preparation thereof. The invention also relates to the uses of the sulfur-containing compound in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2. This invention also describes a series of chemical analogues of the said sulfur-containing compound and the preparation of these compounds.
    Type: Grant
    Filed: February 6, 2013
    Date of Patent: May 13, 2014
    Assignee: National Sun Yat-Sen University
    Inventors: Jyh-Horng Sheu, Chih-Hua Chao, Zhi-Hong Wen
  • Publication number: 20140120471
    Abstract: A compound having the formula (I): wherein a is an integer of from 1 to 10, and x is an integer of from 1 to 3, X1 comprises a fluoroalcohol, fluorinated ester, or fluorinated anhydride, Y is a single bond, C1-20 alkylene group, O, S, NR, ester, carbonate, sulfonate, sulfone, or sulfonamide, wherein R is H or C1-20 alkyl, and wherein the C1-20 alkylene group is structurally only carbon, or one or more structural carbon atoms in the C1-20 alkylene group is replaced by oxygen, carbonyl, ester, or a combination comprising at least one of the foregoing, Ar is a substituted or unsubstituted, C5 or greater monocyclic, polycyclic, or fused polycyclic cycloalkyl; or a substituted or unsubstituted, C5 or greater monocyclic, polycyclic, or fused polycyclic aryl group, wherein the cycloalkyl or aryl is a carbocycle or comprises a heteroatom comprising O, S, N, F, or a combination comprising at least one of the foregoing, each R1 is independently a substituted C5-40 aryl, substituted C5-40 heteroaryl, C1-40 alkyl, a
    Type: Application
    Filed: October 26, 2012
    Publication date: May 1, 2014
    Inventors: Emad Aqad, Cheng-Bai Xu, Cong Liu, Mingqi Li, Shintaro Yamada
  • Patent number: 8658803
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Grant
    Filed: October 23, 2012
    Date of Patent: February 25, 2014
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20140039215
    Abstract: The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) in which A, D, G, W, X, Y and Z are as defined above, to a plurality of processes for the preparation and to their use as pesticides and/or herbicides and/or microbicides. Moreover, the invention relates to selective herbicidal compositions comprising both the 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) and a crop plant compatibility-improving compound.
    Type: Application
    Filed: July 29, 2013
    Publication date: February 6, 2014
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Reiner FISCHER, Thomas BRETSCHNEIDER, Ernst Rudolf F. GESING, Dieter FEUCHT, Karl-Heinz KUCK, Peter LÖSEL, Olga MALSAM, Christian ARNOLD, Thomas AULER, Martin Jeffrey HILLS, Heinz KEHNE
  • Patent number: 8637496
    Abstract: The invention relates to the use of compounds having a monogalactosyldiacylglycerol (MGDG) synthase inhibitory activity as herbicide or algaecide, and to herbicide and algaecide compositions containing at least one of these compounds.
    Type: Grant
    Filed: June 2, 2008
    Date of Patent: January 28, 2014
    Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche Scientifique
    Inventors: Anne-Laure Bonneau, Cyrille Botte, Michael Deligny, Nadia Saidani, Hélène Hardre, Bernard Rousseau, Roman Lopez, Eric Marechal
  • Publication number: 20130323645
    Abstract: A resist composition including a base component (A) which exhibits changed solubility in a developing solution under action of acid and an acid generator component (B) which generates acid upon exposure, the acid generator component (B) including a sulfonium compound (B1) having a sulfonio group and an anion group represented by general formula (b1-r-1) shown below in one molecule thereof (wherein Y1 represents a divalent linking group or a single bond; L1 represents an ester bond or a single bond; V1 represents a divalent hydrocarbon group having a fluorine atom; and n represents 0 or 1, provided that, when L1 represents a single bond, n=1).
    Type: Application
    Filed: May 29, 2013
    Publication date: December 5, 2013
    Inventors: Yoshitaka Komuro, Shinji Kumada
  • Publication number: 20130324521
    Abstract: A medical product (1) introducible into a blood vessel (2) comprising a drug (3) for the treatment of an aneurysm and of arteriosclerotic diseases. The drug (3) is a farnesyltransferase inhibitor.
    Type: Application
    Filed: November 24, 2011
    Publication date: December 5, 2013
    Inventor: Reza Ghotbi
  • Patent number: 8574607
    Abstract: Compounds of the formula (I) useful as pesticides are disclosed, wherein the substituents are as defined in claim 1.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: November 5, 2013
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Jürgen Harry Schaetzer, Thomas Pitterna, Long Lu, Yaming Wu, Peter Renold, Francesca Perruccio, Jérome Yves Cassayre, Michel Mueglebach
  • Patent number: 8541157
    Abstract: A resist composition including a base component (A) which exhibits changed solubility in an alkali developing solution under the action of acid and an acid-generator component (B) which generates acid upon exposure, wherein the acid-generator component (B) includes an acid generator (B1) composed of a compound having a base dissociable group within a cation moiety.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: September 24, 2013
    Assignee: Tokyo Ohka Kogyo Co., Ltd.
    Inventors: Akiya Kawaue, Yoshiyuki Utsumi, Sho Abe
  • Publication number: 20130131372
    Abstract: The invention relates to methods for producing chalcone (1,3-diphenylprop-2-en-1-one) derivatives that have multiple substitutions on a phenyl ring. Intermediate chalcone derivatives are modified by Phase Transfer Catalysis (PTC) for introducing a substituted alkyl group that is provided by a sulfonic acid derivative on a phenyl ring already containing substituent groups on one or two carbon atoms adjacent to the carbon atom where a substituent group is being introduced. The methods of the invention allow producing efficiently, by either S-alkylation or O-alkylation, chalcones derivatives that are characterized for their biological activities that are intermediate compounds for producing molecules having such activities, or that can be used for generating libraries of compounds to be screened by means of in vitro and/or in vivo assays and establishing structure-activity relationships.
    Type: Application
    Filed: May 16, 2011
    Publication date: May 23, 2013
    Applicant: GENFIT
    Inventors: Karine Bertrand, Alice Roudot, Patrice Rool
  • Patent number: 8445610
    Abstract: A transition metal mediated chain transfer agent controlled polymerization process is described. The process combines the advantages of atom transfer radical polymerization (ATRP) and reversible addition fragmentation transfer (RAFT) polymerization. Synthesis of chain transfer agents useful in the disclosed processes is also disclosed. Other improvements on ATRP RAFT processes are also described.
    Type: Grant
    Filed: March 6, 2009
    Date of Patent: May 21, 2013
    Assignee: Carnegie Mellon University
    Inventors: Yungwan Kwak, Renaud Nicolay, Krzysztof Matyjaszewski
  • Publication number: 20130109866
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: October 23, 2012
    Publication date: May 2, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Patent number: 8399661
    Abstract: The invention relates to a sulfur-containing compound and the preparation thereof. The invention also relates to the uses of the sulfur-containing compound in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2. This invention also describes a series of chemical analogues of the said sulfur-containing compound and the preparation of these compounds.
    Type: Grant
    Filed: July 14, 2008
    Date of Patent: March 19, 2013
    Assignee: National Sun Yat-Sen University
    Inventors: Jyh-Horng Sheu, Chih-Hua Chao, Zhi-Hong Wen
  • Publication number: 20130060050
    Abstract: Provided are ?-ketosulfide compounds represented by the formula (5): where the structural variables R1, R2, R3 and R4 are as defined herein.
    Type: Application
    Filed: October 16, 2012
    Publication date: March 7, 2013
    Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Kazufumi YANAGIHARA, Shingo UMEZAWA, Katsuaki MIYAJI
  • Publication number: 20130018202
    Abstract: The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) in which A, D, G, W, X, Y and Z are as defined above, to a plurality of processes for the preparation and to their use as pesticides and/or herbicides and/or microbicides. Moreover, the invention relates to selective herbicidal compositions comprising both the 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) and a crop plant compatibility-improving compound.
    Type: Application
    Filed: January 11, 2012
    Publication date: January 17, 2013
    Applicant: Bayer CropScience AG
    Inventors: Reiner Fischer, Thomas Bretschneider, Ernst Rudolf F. Gesing, Dieter Feucht, Karl-Heinz Kuck, Peter Lösel, Olga Malsam, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne
  • Publication number: 20120302780
    Abstract: Compounds useful as nutritional supplements, antioxidants, heavy metal chelators and/or as intermediates for producing other related compounds with like uses have a formula: where R1 is an aromatic backbone and R2 is a psulfur containing ligand.
    Type: Application
    Filed: August 2, 2012
    Publication date: November 29, 2012
    Applicant: THE UNIVERSITY OF KENTUCKY RESEARCH FOUNDATION
    Inventors: Boyd E. Haley, Niladri Narayan Gupta
  • Publication number: 20120271055
    Abstract: The present invention relates to a compound as a peroxisome proliferator activated receptor (PPAR) activator and a hydrate, a solvate, a stereoisomer and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition, a cosmetic composition, a muscle strengthening agent, a memory improving agent, a therapeutic agent for dementia and Parkinson's disease, a functional food and a feed composition containing the same.
    Type: Application
    Filed: December 1, 2007
    Publication date: October 25, 2012
    Applicant: SEOUL NATIONAL UNIVERSITY INDUSTRY FOUNDATION
    Inventors: Heonjoong Kang, Jungwook Chin, Jaehwan Lee
  • Patent number: 8222314
    Abstract: Urethane acrylates of the general Formula (I), corresponding salts, solvates or solvates of a salt thereof: wherein R1, R2, R3, R4 and R5 each independently represent a substituent selected from the group consisting of hydrogen, halogens, C1-6-alkyls, trifluoromethyl, C1-6-alkylthios, C1-6-alkylselenos, C1-6-alkyltelluros, and nitro groups, with the proviso that at least one of R1, R2, R3, R4 and R5 is not hydrogen; R6 and R7 each independently represent a substituent selected from the group consisting of hydrogen and C1-6-alkyls; and A represents a saturated or unsaturated or linear or branched C1-6-alkyl radical or a polyalkylene oxide radical having 2-6 ethylene oxide or propylene oxide units; processes for producing and methods of using the same.
    Type: Grant
    Filed: August 7, 2009
    Date of Patent: July 17, 2012
    Assignee: Bayer MaterialScience AG
    Inventors: Thomas Roelle, Friedrich-Karl Bruder, Thomas Fäcke, Marc-Stephan Weiser, Dennis Hönel
  • Patent number: 8188306
    Abstract: Novel compounds useful for inhibiting the 90kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.
    Type: Grant
    Filed: September 30, 2009
    Date of Patent: May 29, 2012
    Assignee: University of Kansas
    Inventors: Brian S. J. Blagg, Gang Shen
  • Publication number: 20110301376
    Abstract: Provided herein are processes of preparing ezatiostat hydrochloride, and crystalline ezatiostat hydrochloride ansolvate form D.
    Type: Application
    Filed: April 26, 2011
    Publication date: December 8, 2011
    Inventors: Guyselaine LECLERC, Hervé LHERMITTE, Christian PICHERIT
  • Publication number: 20110212994
    Abstract: Small molecule choline kinase inhibitors, pharmaceutical compositions thereof, and screening methods for identifying and evaluating choline kinase inhibitors are provided. Safe and effective methods for treating subjects suffering from a disorder or disease characterized by neoplastic cell proliferation employing the choline kinase inhibitors are also provided.
    Type: Application
    Filed: June 28, 2010
    Publication date: September 1, 2011
    Inventors: BRIAN CLEM, SUCHETA TELANG, JOHN TRENT, JASON CHESNEY, POORAN CHAND, GILLES TAPOLSKY
  • Publication number: 20110046324
    Abstract: A transition metal mediated chain transfer agent controlled polymerization process is described. The process combines the advantages of atom transfer radical polymerization (ATRP) and reversible addition fragmentation transfer (RAFT) polymerization. Synthesis of chain transfer agents useful in the disclosed processes is also disclosed. Other improvements on ATRP RAFT processes are also described.
    Type: Application
    Filed: March 6, 2009
    Publication date: February 24, 2011
    Inventors: Krzysztof Matyjaszewski, Yungwan Kwak, Renaud Nicolay
  • Publication number: 20110039874
    Abstract: Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.
    Type: Application
    Filed: April 16, 2010
    Publication date: February 17, 2011
    Applicant: Northeastern University
    Inventors: Alexandros Makriyannis, Spyridon P. Nikas, Shakiru O. Alapafuja, Vidyanand G. Shukla
  • Publication number: 20110021534
    Abstract: The present invention relates to 2-(substituted sulphur, sulphone or sulphoxide)-3-(substituted phenyl) propionic acid derivatives, 2-(substituted oxygen)-3-(substituted phenyl) propionic acid derivatives, benzoic acid derivatives, and derivatives of 2-methyl-2-(phenoxy or phenylthio)propanoic acid and 2-(methylor ethyl)-2-(phenoxy or phenylthio)butanoic acid, to processes for preparing such compounds, to their use in the treatment of inflammatory conditions, and to pharmaceutical compositions containing them.
    Type: Application
    Filed: March 7, 2008
    Publication date: January 27, 2011
    Applicant: ALBIREO AB
    Inventors: Anders Broo, Johan Gottfries, Michael Kossenjans, Li Lanna, Eva-Lotte Lindstedt-Alstermark, Kristina A. Nilsson, Bengt Ohlsson, Maria Thorstensson, Maria Boije, Olof Sjogren
  • Patent number: 7863332
    Abstract: Novel biaromatic compounds having the general formula (I): and cosmetic/pharmaceutical compositions comprised thereof are useful in human or veterinary medicine (in dermatology and also in the fields of cardiovascular diseases, of immune diseases and/or of diseases related to the metabolism of lipids) or, alternatively, in cosmetic compositions.
    Type: Grant
    Filed: February 16, 2007
    Date of Patent: January 4, 2011
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Jean-Guy Boiteau, Corinne Millois Barbuis
  • Publication number: 20100286266
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl sulfonamides and related compounds (collectively referred to herein as ‘BPSAAA compounds’), as described herein, and including, for example, biphenyl-4-sulfonic acid (hydroxyalkyl-phenyl)-amides and related compounds.
    Type: Application
    Filed: March 20, 2008
    Publication date: November 11, 2010
    Applicant: THE UNIVERSITY COURT OF THE UNIVERSITY OF ABERDEEN
    Inventors: Iain Robert Greig, Robert Jurgen Van't Hof, Stuart Hamilton Ralston
  • Patent number: 7816385
    Abstract: A novel class of dicarboxylic acid derivatives, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator -Activated Receptors (PPAR).
    Type: Grant
    Filed: December 12, 2003
    Date of Patent: October 19, 2010
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Per Sauerberg, Lone Jeppesen, Zdenek Polivka, Karel Sindelar
  • Publication number: 20100261788
    Abstract: Various phenylamine derivatives are described as well as the use of compounds to inhibit BID protein for controlling apoptotic cascade.
    Type: Application
    Filed: June 22, 2010
    Publication date: October 14, 2010
    Inventors: John C. Reed, Maurizio Pellecchia
  • Patent number: 7786057
    Abstract: Linked aromatic compounds found to act as potent soot dispersants in lubricating oil compositions; lubricating, oil compositions containing such soot dispersants and precursor compounds from which the soot dispersants are derived.
    Type: Grant
    Filed: February 8, 2007
    Date of Patent: August 31, 2010
    Assignee: Infineum International Limited
    Inventors: Tushar K. Bera, Jacob Emert, Jun Hua
  • Publication number: 20100173332
    Abstract: A method utilising one or more fluorogenic probes, for the detection of nitroreductase activity. The non-fluorescent probes are reduced in the presence of nitroreductase to form fluorescent derivatives that may be detected using fluorescence spectroscopy.
    Type: Application
    Filed: September 7, 2007
    Publication date: July 8, 2010
    Inventors: Jeffrey B. Smaill, Adam V. Patterson, Dean C. Singleton
  • Patent number: 7662993
    Abstract: The present invention is directed to labeled compounds of the formulae wherein Q is selected from the group consisting of —S(?O)—, and —S(?O)2—, Z is selected from the group consisting of 1-naphthyl, substituted 1-naphthyl, 2-naphthyl, substituted 2-naphthyl, and phenyl groups with the structure wherein R1, R2, R3, R4 and R5 are each independently selected from the group consisting of hydrogen, a C1-C4 lower alkyl, a halogen, and an amino group selected from the group consisting of NH2, NHR and NRR? where R and R? are each independently selected from the group consisting of a C1-C4 lower alkyl, an aryl, and an alkoxy group, and X is selected from the group consisting of hydrogen, a C1-C4 lower alkyl group, and a fully-deuterated C1-C4 lower alkyl group.
    Type: Grant
    Filed: November 2, 2006
    Date of Patent: February 16, 2010
    Assignee: Los Alamos National Security, LLC
    Inventors: Marc A. Alvarez, Rodolfo A. Martinez, Clifford J. Unkefer
  • Publication number: 20090275539
    Abstract: The present invention relates to novel compounds that are nuclear transcription factors (NTF) regulators. The present invention also provides methods for treating, preventing and/or reducing inflammation associated diseases by regulating NTF in the cardiovascular, connective tissue, pulmonary, gastrointestinal, respiratory, urogenital, nervous, or cutaneous systems as well as tumoral and infective diseases employing said compounds.
    Type: Application
    Filed: October 5, 2005
    Publication date: November 5, 2009
    Applicant: CTG PHARMA S.R.L.
    Inventor: Anna Sparatore
  • Patent number: 7605288
    Abstract: Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.
    Type: Grant
    Filed: March 26, 2007
    Date of Patent: October 20, 2009
    Assignee: University of Kansas
    Inventors: Brian Blagg, Gang Shen, Randell C. Clevenger
  • Patent number: 7576234
    Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.
    Type: Grant
    Filed: December 16, 2005
    Date of Patent: August 18, 2009
    Assignee: Genzyme Corporation
    Inventors: Mukund S. Chorghade, Mukund K. Gurjar, Debendra K. Mohapatra
  • Publication number: 20090156653
    Abstract: An amino alcohol derivative represented by the following general formula (1) (for example, (±)-2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentane-1-ol) exhibits strong immunosuppressive effect while causing less side effects:
    Type: Application
    Filed: November 21, 2008
    Publication date: June 18, 2009
    Inventors: Yasushi Kohno, Kiyoaki Tanaka, Kazuhiko Kuriyama
  • Patent number: 7495029
    Abstract: Disclosed are prodrugs of (2R)-2-propyloctanoic acid, and pharmaceutical compositions comprising them, which may be effective in modulating multiple events in the biochemical cascade of stroke. Also disclosed are methods of treating patients who have had a stroke, or are at risk of stroke, by administering the compounds or compositions of the invention.
    Type: Grant
    Filed: November 10, 2005
    Date of Patent: February 24, 2009
    Assignee: Merck & Co., Inc
    Inventors: Benito Munoz, Joseph E. Payne, Petpiboon Prasit, Thomas S. Reger, Nicholas D. Smith
  • Patent number: 7491747
    Abstract: The present invention relates to a compound of the formula I: (Formula I) in which: A, B, R1, Z, n and R2 are as defined in claim 1. These compounds are useful in the treatment of dyslipidaemia, atherosclerosis and diabetes.
    Type: Grant
    Filed: July 3, 2002
    Date of Patent: February 17, 2009
    Assignee: Merck Patent GmbH
    Inventors: Roche Didier, Jean-Jacques Zeiller, Francis Contard, Valérie Guyard-Dangremont, Daniel Guerrier, Hervé Dupont, Jean-Jacques Berthelon
  • Patent number: 7482484
    Abstract: Disclosed are Compounds of formula I And methods of use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes.
    Type: Grant
    Filed: December 16, 2003
    Date of Patent: January 27, 2009
    Assignee: Merck Patent GmbH
    Inventors: Nathalie Adje, Michel Brunet, Didier Roche, Jean-Jacques Zeiller, Stéphane Yvon, Valérie Guyard-Dangremont, Francis Contard, Daniel Guerrier, Gérard Ferrand, Yves Bonhomme
  • Publication number: 20090023085
    Abstract: A photosensitive composition includes a compound represented by Formula (I) and a curable composition contains the compound of Formula (I) and a polymerizable compound. A compound is represented by a Formula (1) and a photocurable composition contains the compound of Formula (1) and a polymerizable compound. In Formula (I), R, R1 and R2 each independently represent a hydrogen atom or a monovalent substituent. In Formula (1), R and B each independently represent a monovalent substituent, A represents a divalent organic group, and Ar represents an aryl group.
    Type: Application
    Filed: July 17, 2008
    Publication date: January 22, 2009
    Applicant: FUJIFILM CORPORATION
    Inventor: Tomotaka Tsuchimura
  • Publication number: 20090023730
    Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.
    Type: Application
    Filed: February 25, 2008
    Publication date: January 22, 2009
    Applicant: ACHILLION PHARMACEUTICALS
    Inventors: Avinash Phadke, Dawei Chen, Milind Deshpande, Andrew Thurkauf, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
  • Publication number: 20080305530
    Abstract: A method for preparing optically active methyl 4-(1-ammoniumethyl)benzoate sulfate by reacting racemic methyl 4-(1-aminoethyl)benzoate with an acylating agent in the presence of a lipase to give methyl 4-(1-aminoethyl)benzoate and subsequently precipitating methyl 4-(1-ammoniumethyl)benzoate sulfate by adding sulfuric acid.
    Type: Application
    Filed: December 19, 2006
    Publication date: December 11, 2008
    Inventors: Klaus Ditrich, Harald Winsel, Dominique Moulin
  • Publication number: 20080221289
    Abstract: The present invention relates to compounds of the general formula I in which the variables are each defined as follows: Z1, Z2 are each independently hydrogen, optionally substituted C1-C20-alkyl in which the carbon chain may be interrupted by oxygen atoms in ether function, sulfur atoms in thioether function or by nonadjacent imino or C1-C4-alkylimino groups, or reactive radicals by means of which polymerization can be brought about, A1, A2 are each independently spacers having from 1 to 30 carbon atoms, in which the carbon chain may be interrupted by oxygen atoms in ether function, sulfur atoms in thioether function or by nonadjacent imino or C1-C4-alkylimino groups, Y1, Y2 are each independently a chemical single bond, oxygen, sulfur, —CO—, —O—CO—, —CO—O—, —S—CO—, —CO—S—, —NR—CO— or —CO—NR—, Y3, Y4 are each independently a chemical single bond, oxygen, sulfur, —CR?CR—, —C?C—, —CR?CR—CO—O—, —O—CO—CR?CR—, —C?C—O—, —O—C?C—, —CH2—CH2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, —CO—, —O—CO—, —CO—O—, —S—CO—, —C
    Type: Application
    Filed: May 10, 2006
    Publication date: September 11, 2008
    Applicant: BASF AKTIENGESELLSCHAFT
    Inventors: Olivier Enger, Rudiger Sens, Christian Lennartz, Robert Parker
  • Publication number: 20080214660
    Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.
    Type: Application
    Filed: May 15, 2008
    Publication date: September 4, 2008
    Inventors: Russell M. Medford, Patricia K. Somers, Lee K. Hoong, Charles O. Meng
  • Patent number: 7417059
    Abstract: The present invention is directed to a class of cyclohexene derivatives bearing sulfamoyl and ester groups which have an inhibitory activity on nitric oxide (NO) production and cytokine production, and are useful as an agent for the prophylaxis and/or treatment of diseases such as, cardiac disease, autoimmune disease, inflammatory disease, central nervous system disease, infectious disease, sepsis, and septic shock.
    Type: Grant
    Filed: March 31, 2005
    Date of Patent: August 26, 2008
    Assignee: Takeda Pharmacetical Company Limited
    Inventors: Norikazu Tamura, Takashi Ichikawa, Masayuki Ii