Esters Having The Thiocarboxylate Group, -c(=x)x-, Wherein The X's Are The Same Or Diverse Chalcogens, With At Least One X Being Sulfur, And Wherein The Single Bonded X Is Bonded Directly To An Additional Carbon, Which Carbon May Be Single Bonded To Any Atom, But May Be Multiple Bonded Only To Carbon Patents (Class 558/230)
  • Patent number: 8853393
    Abstract: The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: October 7, 2014
    Assignee: Anhui New Star Pharmaceutical Development Co., Ltd.
    Inventors: Ziao Xu, Yuanhai Zhao, Degang Li, Xiaoxiang Li
  • Patent number: 8536363
    Abstract: This invention pertains generally to prostacyclin analogs and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis. Generally, the compounds and methods of the present invention increase the oral bioavailability and circulating concentrations of treprostinil when administered orally.
    Type: Grant
    Filed: July 26, 2012
    Date of Patent: September 17, 2013
    Assignee: United Therapeutics Corporation
    Inventors: Ken Phares, David Mottola
  • Publication number: 20130231478
    Abstract: The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.
    Type: Application
    Filed: July 29, 2011
    Publication date: September 5, 2013
    Inventors: Ziao Xu, Yuanhai Zhao, Degang Li, Xiaoxiang Li
  • Publication number: 20120309900
    Abstract: To provide a novel compound having both a surface-activating ability and a polymerization controlling ability. A compound represented by the following general formula (1) or (2): wherein, R1 and R3 are an organic group having the hydrophile-lipophile balance (HLB) determined by Griffin's method of 3 or more. The definitions of R1, R2, R3, R4, Z, p and q are described in the Description.
    Type: Application
    Filed: January 27, 2011
    Publication date: December 6, 2012
    Applicant: Mitsubishi Rayon Co., Ltd.
    Inventors: Tetsuya Noda, Fuminori Nakaya, Keiichi Sakashita, Yousuke Matsunaga, Taeko Oonuma, Yoshiko Irie
  • Publication number: 20120234721
    Abstract: The present invention provides compounds that are effective in treating central nervous system disorders and maintaining normal brain function. Methods of making and using the compounds are also provided.
    Type: Application
    Filed: September 9, 2011
    Publication date: September 20, 2012
    Applicant: Neurotherapeutics Pharma, Inc.
    Inventors: Daryl W. HOCHMAN, John J. Partridge
  • Publication number: 20120108757
    Abstract: A thiocarbonyl compound represented by the following formula (a) is useful as a RAFT agent. By using this, a process for producing a polymer having a excellent reactivity or monomer conversion rate and its polymer are provided.
    Type: Application
    Filed: April 13, 2010
    Publication date: May 3, 2012
    Applicant: Nippon Carbide Industries Co., Inc.
    Inventors: Naoki Musashi, Atsushi Shibata, Noboru Yamagata
  • Patent number: 7968743
    Abstract: A thiocarbonylthio compound and free radical polymerization employing the same. The thiocarbonylthio compound is represented by formula (I) or (II): wherein Z can be independently perfluoroalkyl, alkyl, haloalkyl, aryl, alkylaryl, haloalkylaryl, arylalkyl, aminoalkyl, alkylamino, alkoxy, alkoxyaryl, alkylsulfonyl, alkylsulfonylaryl, dialkylphosphinyl, or dialkylphosphinothioyl; R1 and R2 can be each independently hydrogen, alkyl, aryl, alkylaryl, arylalkyl, aminoalkyl, alkylamino, alkoxy or alkoxyaryl; R3 is alkyl, aryl, aminoalkyl, alkylamino, alkoxy or alkoxyaryl. Furthermore, R3 can also be alkyl, aryl, alkylaryl, arylalkyl, aminoalkyl, alkylamino, alkoxy, haloalkylaryl, alkylsilyl, alkylthio, alkylthioaryl, or substituent containing CN, CO, COOH, COOCH3 or heterocyclic moieties; and R4 is perfluoroalkyl. The thiocarbonylthio compound can be used as a reversible chain transfer agent in a free radical polymerization to obtain a polymer with a controlled molecular weight and narrow polydispersity.
    Type: Grant
    Filed: November 4, 2009
    Date of Patent: June 28, 2011
    Assignee: Industrial Technology Research Institute
    Inventors: Kuo Chen Shih, Po Wen Chung, Mei Hua Wang
  • Patent number: 7863474
    Abstract: The present invention relates to a process for the preparation of 1-(2-ethyl-butyl)-cyclohexanecarboxylic acid which is useful as an intermediate in the preparation of pharmaceutical active compounds.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: January 4, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ursula Hoffmann, Bruno Lohri
  • Publication number: 20100227975
    Abstract: The invention provides a method for preparing an aqueous dispersion of polymer particles comprising the following steps: (i) preparing a dispersion having a continuous aqueous phase, a dispersed organic phase comprising one or more ethylenically unsaturated monomers, and an amphiphilic RAFT agent as a stabiliser for said organic phase, and (ii) polymerising said one or more ethylenically unsaturated monomers under the control of said amphiphilic RAFT agent to form said aqueous dispersion of polymer particles, novel amphiphilic RAFT agents for use in this method, novel RAFT agents useful in making these amphiphilic RAFT agents and methods for their manufacture.
    Type: Application
    Filed: May 14, 2010
    Publication date: September 9, 2010
    Applicant: UNIVERSITY OF SYDNEY
    Inventors: Christopher Henry SUCH, Ezio RIZZARDO, Algirdas Kazimieras SERELIS, Brian Stanley HAWKETT, Robert Goulston GILBERT, Christopher James FERGUSON, Robert John HUGHES, Edna Olejnik
  • Publication number: 20100152289
    Abstract: 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: Application
    Filed: May 18, 2008
    Publication date: June 17, 2010
    Inventor: Hiroyuki Miyazaki
  • Patent number: 7662986
    Abstract: This invention concerns a free radical polymerization process, selected chain transfer agents employed in the process and polymers made thereby, in which the process comprises preparing polymer of general Formula (A) and Formula (B) comprising contacting: (i) a monomer selected from the group consisting of vinyl monomers (of structure CH2?CUV), maleic anhydride, N-alkylmaleimide, N-arylmaleimide, dialkyl fumarate and cyclopolymerizable monomers; (ii) a thiocarbonylthio compound selected from Formula (C) and Formula (D) having a chain transfer constant greater than about 0.1; and (iii) free radicals produced from a free radical source; the polymer of Formula (A) being made by contacting (i), (ii) C and (iii) and that of Formula (B) by contacting (i), (ii) D, and (iii); and (iv) controlling the polydispersity of the polymer being formed by varying the ratio of the number of molecules of (ii) to the number of molecules of (iii); wherein Q, R, U, V, Z, Z?, m, p and q are as defined in the text.
    Type: Grant
    Filed: May 25, 2007
    Date of Patent: February 16, 2010
    Assignee: Commonwealth Scientific and Industrial Research Organisation
    Inventors: Tam Phuong Le, Graeme Moad, Ezio Rizzardo, San Hoa Thang
  • Patent number: 7632959
    Abstract: A thiocarbonylthio compound and free radical polymerization employing the same. The thiocarbonylthio compound is represented by formula (I) or (II): wherein Z can be independently perfluoroalkyl, alkyl, haloalkyl, aryl, alkylaryl, haloalkylaryl, arylalkyl, aminoalkyl, alkylamino, alkoxy, alkoxyaryl, alkylsulfonyl, alkylsulfonylaryl, dialkylphosphinyl, or dialkylphosphinothioyl; R1 and R2 can be each independently hydrogen, alkyl, aryl, alkylaryl, arylalkyl, aminoalkyl, alkylamino, alkoxy or alkoxyaryl; R3 is alkyl, aryl, aminoalkyl, alkylamino, alkoxy or alkoxyaryl. Furthermore, R can also be alkyl, aryl, alkylaryl, arylalkyl, aminoalkyl, alkylamino, alkoxy, haloalkylaryl, alkylsilyl, alkylthio, alkylthioaryl, or substituent contaning CN, CO, COOH, COOCH3 or heterocyclic moieties; and R4 is perfluoroalkyl. The thiocarbonylthio compound can be used as a reversible chain transfer agent in a free radical polymerization to obtain a polymer with a controlled molecular weight and narrow polydispersity.
    Type: Grant
    Filed: May 24, 2005
    Date of Patent: December 15, 2009
    Assignee: Industrial Technology Research Institute
    Inventors: Kuo Chen Shih, Po Wen Chung, Mei Hua Wang
  • Publication number: 20090215965
    Abstract: The invention provides a process for synthesising functionalised chain transfer polymers of Formula (1) or Formula (2) using thiocarbonyl thio compounds as chain transfer agents. Why R1 is a moiety comprising a functional group; Q is obtained from an olefinically unsaturated monomer; R? is selected from the group consisting of alkyl, substituted alkyl, alkoxy, substituted alkoxy, an aromatic saturated or unsaturated carbocyclic or heterocyclic ring, optionally substituted with one or more substituents, amino alkyl, cyanoalkyl, hydroxylalkyl, saturated and unsaturated amido; an organometallic species, a polymer chain and any of the foregoing substituted with one or more CN or OH groups; q=an integer of at least 2; p=an integer of at least 1. Chain transfer agents and polymers produced by the method are also provided.
    Type: Application
    Filed: April 8, 2009
    Publication date: August 27, 2009
    Applicant: The University of Leeds
    Inventor: Sebastian Perrier
  • Patent number: 7511168
    Abstract: The present invention provides novel processes for the preparation of a cyclopentanone of Formula II and a lactone of Formula I, which are useful in the production of prostaglandins: wherein Z, R2, R3, X1, X2, and are as defined in the specification. The invention also provides novel enantiomerically enriched compounds.
    Type: Grant
    Filed: January 18, 2006
    Date of Patent: March 31, 2009
    Inventors: Shih-Yi Wei, Yu-Chih Yeh
  • Patent number: 7439266
    Abstract: The present invention relates to a novel malononitrile compound represented by the formula (A): wherein, R1 represents C1 to C6 alkyl that may be substituted with halogen, C2 to C6 alkenyl that may be substituted with halogen, etc; R2 represents hydrogen atom or C1 to C6 alkyl that may be substituted with halogen; R3 represents hydrogen atom or C1 to C6 alkyl; R4 represents hydrogen atom or C1 to C6 alkyl; R5 represents C1 to C6 alkyl that may be substituted with halogen, C3 to C6 alkenyl that may be substituted with halogen, etc, or R4 and R5 may be combined at their terminal and represent ethylene that may be substituted with C1 to C3 alkyl or trimethylene that may be substituted with C1 to C3 alkyl; and Z1 and Z2, which are the same or different, represent oxygen atom or sulfur atom. The malononitrile compound has an efficient pesticidal activity and can control effectively pests such as insect pests, acarine pests, nematode pests and the like.
    Type: Grant
    Filed: August 26, 2003
    Date of Patent: October 21, 2008
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Satoshi Okada, Daisuke Oohira, Ken Otaka
  • Publication number: 20080139836
    Abstract: This invention concerns a free radical polymerization process, selected chain transfer agents employed in the process and polymers made thereby, in which the process comprises preparing polymer of general Formula (A) and Formula (B) comprising contacting: (i) a monomer selected from the group consisting of vinyl monomers (of structure CH2?CUV), maleic anhydride, N-alkylmaleimide, N-arylmaleimide, dialkyl fumarate and cyclopolymerizable monomers; (ii) a thiocarbonylthio compound selected from Formula (C) and Formula (D) having a chain transfer constant greater than about 0.1; and (iii) free radicals produced from a free radical source; the polymer of Formula (A) being made by contacting (i), (ii) C and (iii) and that of Formula (B) by contacting (i), (ii) D, and (iii); and (iv) controlling the polydispersity of the polymer being formed by varying the ratio of the number of molecules of (ii) to the number of molecules of (iii); wherein Q, R, U, V, Z, Z?, m, p and q are as defined in the text.
    Type: Application
    Filed: May 25, 2007
    Publication date: June 12, 2008
    Inventors: Tam Phuong Le, Graeme Moad, Ezio Rizzardo, San Hoa Thang
  • Patent number: 7332552
    Abstract: The present invention relates to low odor ?-cyano-dithiocarboxylic ester compounds of formula I for use as chain transfer agents in free radical polymerizations, and polymerization processes employing them: wherein R1 is selected from alkyl, substituted alkyl, heteroaryl, substituted heteroaryl, alkylaryl, substituted alkylaryl, aryl, substituted aryl, alkoxy, aryloxy, thioalkyl, thioaryl, substituted thioalkyl, substituted thioaryl, secondary amino and tertiary amino; R2 is selected from alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, and COOR3; and R3 is alkyl.
    Type: Grant
    Filed: May 27, 2004
    Date of Patent: February 19, 2008
    Assignee: Rensselaer Polytechnic Institute
    Inventors: Brian Benicewicz, Chunzhao Li
  • Patent number: 6855840
    Abstract: Polymers and copolymers synthesized by means that yield a narrow range of molecular weights can have different properties than polymers synthesized by conventional means. In order to obtain such polymers, however, polymerization must be controlled. One type of controlled polymerization is the reversible addition-fragmentation chain transfer (RAFT) process, which has characteristics of a living polymerization. The present invention discloses a group of dithioesters and trithioesters suitable as chain transfer agents for RAFT polymerization. The present invention also discloses RAFT polymerizations conducted in aqueous media.
    Type: Grant
    Filed: January 6, 2003
    Date of Patent: February 15, 2005
    Assignee: University of Southern Mississippi
    Inventors: Charles L. McCormick, Michael S. Donovan, Andrew B. Lowe, Brent S. Sumerlin, David B. Thomas
  • Patent number: 6841695
    Abstract: The present invention relates to a process for preparing dithioesters in which a dithiocarboxylic acid and/or a dithiocarboxylic salt is reacted with a vinyl compound and/or an alkyl compound which includes a leaving group, the reaction being carried out in a biphasic system in which one of the phases comprises water and the weight ratio of the aqueous phase to the organic phase lies in the range from 95:5 to 5:95.
    Type: Grant
    Filed: March 18, 2003
    Date of Patent: January 11, 2005
    Assignee: Rohmax Additives GmbH
    Inventors: Joseph Martin Bollinger, Jen-Lung Wang
  • Publication number: 20030069307
    Abstract: The invention relates to the use of 2-(3,4-dihydroxyphenyl)ethyl-substituted carbonic acid derivatives as antioxidants or free-radical scavengers, in particular to the use for protecting human cells and tissues from the harmful, aging-accelerating effects of free-radicals and reactive oxygen compounds.
    Type: Application
    Filed: August 15, 2002
    Publication date: April 10, 2003
    Inventor: Jakob Peter Ley
  • Publication number: 20030013903
    Abstract: The present invention provides an industrial method for recovering and purifying 2-acetylthio-3-phenylpropionic acid, particularly an optically active
    Type: Application
    Filed: March 13, 2002
    Publication date: January 16, 2003
    Inventors: Koichi Kinoshita, Koki Yamashita, Yasuyoshi Ueda
  • Patent number: 6420423
    Abstract: Compounds of the formula: in which n, q, A, X, G, Y, Z, R, R2, R3, R4, R5, R7 and R9 are as defined in claim 1, and, where appropriate, E/Z isomers, E/Z isomer mixtures and/or tautomers thereof, in each case in the free form or in an agrochemically suitable salt form, can be used as agrochemical active compounds and can be prepared in a manner known per se.
    Type: Grant
    Filed: June 29, 1999
    Date of Patent: July 16, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Saleem Farooq, Stephan Trah, Hugo Ziegler, René Zurflüh, Alfons Pascual, Henry Szczepanski, Roger Graham Hall
  • Publication number: 20020040157
    Abstract: Compounds of the formula I 1
    Type: Application
    Filed: September 25, 2001
    Publication date: April 4, 2002
    Inventors: Walter Kunz, Beat Jau
  • Publication number: 20020038048
    Abstract: The present invention relates to methods for the synthesis of chiral non-racemic products, e.g., enantiomerically-enriched hemiesters, from prochiral starting materials, e.g., meso anhydrides. The present invention also relates to catalysts for the aforementioned methods, and methods for synthesizing these catalysts.
    Type: Application
    Filed: April 3, 2001
    Publication date: March 28, 2002
    Inventors: Li Deng, Yonggang Chen, Shikai Tian
  • Publication number: 20010020079
    Abstract: Method of separating molecules by providing a cross-linked polymer gel having a cross-linking moiety of the formula 1
    Type: Application
    Filed: December 21, 2000
    Publication date: September 6, 2001
    Applicant: The University of Melbourne
    Inventors: David Henry Solomon, Grace Chan, Peter Agapitos Kambouris, Mark Graham Looney
  • Publication number: 20010016664
    Abstract: New phenolic compounds of formula (I) 1
    Type: Application
    Filed: February 7, 2001
    Publication date: August 23, 2001
    Applicant: Clariant (France) S.A.
    Inventors: Didier Wilhelm, Florence Esmard
  • Patent number: 6037455
    Abstract: The present invention is directed to novel propoxyphene derivatives which are synthesized for the covalent attachment to antigens (proteins or polypeptides) for the preparation of antibodies or receptors to propoxyphene and propoxyphene metabolites. The resulting novel antigens may be used for the production of antibodies or receptors using standard methods. Once generated, the antibodies or receptors and the novel derivatives which are covalently attached to proteins, polypeptides or labels may be used in the immunoassay process.
    Type: Grant
    Filed: November 9, 1992
    Date of Patent: March 14, 2000
    Assignee: Biosite Diagnostics Incorporated
    Inventor: Kenneth F. Buechler
  • Patent number: 5985921
    Abstract: Compounds of the formula ##STR1## in which n, q, A, X, G, Y, Z, R, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.7 and R.sub.9 are as defined in claim 1, and, where appropriate, E/Z isomers, E/Z isomer mixtures and/or tautomers thereof, in each case in the free form or in an agrochemically suitable salt form, can be used as agrochemical active compounds and can be prepared in a manner known per se.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: November 16, 1999
    Assignee: Novartis Corporation
    Inventors: Saleem Farooq, Stephen Trah, Hugo Ziegler, Rene Zurfluh, Alfons Pascual, Henry Szczepanski, Roger Graham Hall
  • Patent number: 5965119
    Abstract: The present invention is directed to double prodrugs containing polymeric-based transport forms. These polymeric prodrugs are preferably of the formula: ##STR1## wherein: B is a leaving group or a residue of an amine-containing target moiety;G is ##STR2## or CH.sub.2 ; Y.sub.1-2 are independently O or S;M is X or Q; where X is an electron withdrawing group and Q is a moiety containing a free electron pair positioned three to six atoms from C(.dbd.Y.sub.2);R.sub.1, R.sub.4, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.13 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyls, C.sub.3-12 branched alkyls, C.sub.3-8 cycloalkyls, C.sub.1-6 substituted alkyls, C.sub.3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C.sub.1-6 heteroalkyls, substituted C.sub.1-6 heteroalkyls;R.sub.2, R.sub.3, R.sub.5 and R.sub.6 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyls, C.sub.1-6 alkoxy, phenoxy, C.sub.1-8 heteroalkyls, C.sub.
    Type: Grant
    Filed: December 30, 1997
    Date of Patent: October 12, 1999
    Assignee: Enzon, Inc.
    Inventors: Richard B. Greenwald, Yun H. Choe
  • Patent number: 5821260
    Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 13, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, Margaret K. Offermann, R. Wayne Alexander, Sampath Parthasarathy
  • Patent number: 5811449
    Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 22, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
  • Patent number: 5792787
    Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 11, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Margaret K. Offermann
  • Patent number: 5783596
    Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 21, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, Margaret K. Offermann, R. Wayne Alexander, Sampath Parthasarathy
  • Patent number: 5773209
    Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 30, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
  • Patent number: 5773231
    Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 30, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
  • Patent number: 5770758
    Abstract: Compounds of the formula I ##STR1## and disulfides thereof and salts thereof are important intermediate products for the preparation of compounds having a microbicidal and plant-immunizing action, of the formula III ##STR2## In the compounds of the formulae I and III: X is halogen,n is 0,1,2 or 3;Z is CN, CO-A or CS-A,A is hydrogen, halogen, OR.sub.1, SR.sub.2 and N(R.sub.3)R.sub.4 ;R.sub.1 to R .sub.4 are hydrogen, a substituted or unsubstituted, open-chain, saturated or unsaturated hydrocarbon radical containing not more than 8 carbon atoms, a substituted or unsubstituted cyclic, saturated or unsaturated hydrocarbon radical containing not more than 10 carbon atoms, substituted or unsubstituted benzyl or phenethyl, a substituted or unsubstituted alkanoyl group containing not more than 8 carbon atoms, a substituted or unsubstituted benzoyl group or a substituted or unsubstituted heterocyclyl radical; or R.sub.3 and R.sub.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: June 23, 1998
    Assignee: Novartis Corporation
    Inventors: Walter Kunz, Beat Jau
  • Patent number: 5750351
    Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 12, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
  • Patent number: 5736747
    Abstract: Organic compounds having at least one ethylenically-unsaturated group are described, the organic compounds being suitable for use in coatable compositions as reactive diluents; compounds of the invention preferably have a divalent organic linking moiety devoid of reactive groups other than optional ethylenically-unsaturated groups, and a polar organic moiety and are particularly adept in solubilizing aminoplast resins having radiation-curable pendant groups.
    Type: Grant
    Filed: February 23, 1996
    Date of Patent: April 7, 1998
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
  • Patent number: 5708032
    Abstract: Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops, these compounds having the structure: ##STR1## where Q is --(C.dbd.S)--R.sub.1 and R.sub.1 is --OR.sub.5, --SR.sub.5, halogen, --NHOH or --NR.sub.5 R.sub.6. Each of R.sub.5 and R.sub.6 is independently hydrogen; an aliphatic or an aromatic group; a C.sub.1 -C.sub.12 aliphatic amine group; a C.sub.2 -C.sub.12 aliphatic carboxylic acid group; or R.sub.5 and R.sub.6 when taken together with the N of R.sub.1 are a protein amino acid or a cyclic group. Polar compounds are particularly useful for systemic control of pests.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: January 13, 1998
    Assignee: Monsanto Company
    Inventors: Dennis Paul Phillion, Peter Gerrard Ruminski, Gopichand Yalamanchili
  • Patent number: 5637616
    Abstract: A method for the topical or systemic treatment of disorders mediated by proteases which result in skin or mucosal lesions, and in particular, pemphigus, cicatricial pemphigoid, bullous pemphigoid, lichen planus, and canker sores, is disclosed wherein the host is treated with an effective amount of N-acetyl ysteine or a derivative thereof, or its pharmaceutically acceptable salt, optionally in a pharmaceutically acceptable diluent or carrier for systemic or topical delivery.
    Type: Grant
    Filed: October 5, 1993
    Date of Patent: June 10, 1997
    Assignee: Arcturus Pharmaceutical Corporation
    Inventors: Richard J. Sharpe, Maureen H. McAloon, Stephen J. Galli, Kenneth A. Arndt
  • Patent number: 5597839
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: January 28, 1997
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William R. Pilgrim
  • Patent number: 5523152
    Abstract: Organic compounds having at least one ethylenically-unsaturated group are described, the organic compounds being suitable for use in coatable compositions as reactive diluents; compounds of the invention preferably have a divalent organic linking moiety devoid of reactive groups other than optional ethylenically-unsaturated groups, and a polar organic moiety and are particularly adept in solubilizing aminoplast resins having radiation-curable pendant groups.
    Type: Grant
    Filed: November 4, 1994
    Date of Patent: June 4, 1996
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
  • Patent number: 5468870
    Abstract: Dye-donor element for use according to thermal dye sublimation transfer comprising a support having thereon a dye layer containing a dye corresponding to the following formula ##STR1## wherein Z represents CN, COOR.sup.1 or CONR.sup.2 R.sup.3 ;R.sup.1, R.sup.2 and R.sup.3 each independently represent hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, or R.sup.2 and R.sup.3 together represent the necessary atoms to close a heterocyclic nucleus or substituted heterocyclic nucleus;Y represents OR.sup.4 or NR.sup.5 R.sup.6 or CN;R.sup.4 represents hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, SO.sub.2 R.sup.7, COR.sup.7, CSR.sup.7, POR.sup.7 R.sup.8 ;R.sup.5 and R.sup.6 each independently has one of the significances given to R.sup.4 or represent substituted or unsubstituted amino, or R.sup.5 and R.sup.
    Type: Grant
    Filed: October 20, 1994
    Date of Patent: November 21, 1995
    Assignee: AGFA-GAVAERT, N.V.
    Inventor: Luc J. Vanmaele
  • Patent number: 5449812
    Abstract: The compounds of the formula (I) ##STR1## in which R.sup.1 -R.sup.4, W, X, Y and Z are as defined in claim 1 are suitable for controlling harmful plants in crops.
    Type: Grant
    Filed: October 28, 1993
    Date of Patent: September 12, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
  • Patent number: 5439925
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function. Use is in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: August 8, 1995
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, Willliam R. Pilgrim
  • Patent number: 5420349
    Abstract: A group of 2-amino-3-aroyl-benzo[.beta.]thiophenes are prepared by preparing an .alpha.-hydroxy thioacetamide by silyl mediated condensation of an aldehyde with an anion of dialkylamino thioformamide, cyclizing the .alpha.-hydroxy thioamide, and subsequently acylating the benzo[.beta.]thiophene to yield the 2-amino-3-aryl derivative. These compounds may be treated with suitable phenyl Grignard reagents, and after deprotection, yield 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[.beta .]thiophene.
    Type: Grant
    Filed: June 10, 1994
    Date of Patent: May 30, 1995
    Assignee: Eli Lilly and Company
    Inventor: Alexander G. Godfrey
  • Patent number: 5389619
    Abstract: Compounds of the formula I ##STR1## where n, W, X, Y, Z, R.sup.1, R.sup.2, and R.sup.3 are as defined herein exhibit fungicidal, insecticidal, and acaracidal activity.
    Type: Grant
    Filed: March 29, 1993
    Date of Patent: February 14, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Doetzer, Hubert Sauter, Horst Wingert, Reinhard Kirstgen, Albrecht Harreus, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5359003
    Abstract: Polysulfide derivatives, having the general formula (A--S--S--).sub.2 X--S--S--A processes for their production and their use for crosslinking of reversion-stable rubber vulcanizates are provided. Crosslinking with reduced reversion and loss of elastomeric properties with age is achieved by the crosslinking system provided by the invention.
    Type: Grant
    Filed: August 11, 1993
    Date of Patent: October 25, 1994
    Assignee: Huls Aktiengesellschaft
    Inventors: Gerhard Horpel, Karl-Heinz Nordsiek
  • Patent number: 5344939
    Abstract: The preparation of magnesium benzyl fluoromalonate and other equivalent materials, the synthetic equivalents of the --CH.sub.2 F moiety, is described. Reaction between these reagents and the in situ-formed imidazolides of various carboxylic acids gives beta-keto-alpha-fluoroesters, which upon hydrogenation and spontaneous decarboxylation yields fluoromethyl ketones in excellent yields. The overall transformation from RCOOH to RCOCH.sub.2 F is thus illustrated.
    Type: Grant
    Filed: March 11, 1993
    Date of Patent: September 6, 1994
    Assignee: Prototek, Inc.
    Inventor: James T. Palmer
  • Patent number: 5310763
    Abstract: Compounds of general formula I: ##STR1## wherein: R.sup.1 represents a C.sub.1 -C.sub.6 alkyl, phenyl, thiophenyl, substituted phenyl, phenyl(C.sub.1 -C.sub.6)alkyl, heterocyclyl, (C.sub.1 -C.sub.6)alkylcarbonyl phenacyl or substituted phenacyl group; or, when n=O, R.sup.1 represents SR.sup.x, wherein R.sup.x represents a group: ##STR2## R.sup.2 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, phenyl(C.sub.1 -C.sub.6)alkyl, cycloalkyl(C.sub.1 -C.sub.6)alkyl or cycloalkenyl(C.sub.1 -C.sub.6)alkyl group;R.sup.3 represents an amino acid residue with R or S stereochemistry or a C.sub.1 -C.sub.6 alkyl, benzyl, (C.sub.1 -C.sub.6 alkoxy)benzyl or benzyloxy(C.sub.1 -C.sub.6 alkyl) group;R.sup.4 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group;R.sup.5 represents a hydrogen atom or a methyl group;n is an integer having the value 0, 1 or 2; andA represents a C.sub.1 -C.sub.6 hydrocarbon chain, optionaly substituted with one or more C.sub.1 -C.sub.
    Type: Grant
    Filed: April 14, 1993
    Date of Patent: May 10, 1994
    Assignee: British Bio-technology Limited
    Inventors: Colin Campion, Alan H. Davidson, Jonathan P. Dickens, Michael J. Crimmin