The Nitrogen Is Bonded Directly To -c(=x)-, Wherein X Is Chalcogen Patents (Class 562/15)
  • Patent number: 8993544
    Abstract: The present invention relates to novel metalloproteinase inhibitors having an aryloxybenzenesulfonamide moiety and a carbamoylphosphonic acid moiety, to pharmaceutical compositions comprising them, and to their uses in the prevention and/or treatment of disease or disorder associated with MMP.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: March 31, 2015
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem, Ltd.
    Inventors: Eli Breuer, Reuven Reich, Julia Frant, Amnon Hoffman, Veerendhar Ainelly
  • Patent number: 8940927
    Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinase activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: May 25, 2011
    Date of Patent: January 27, 2015
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
  • Publication number: 20140378529
    Abstract: Methods for treating a subject determined to have a cancer comprising a heterozygous inactivation of a housekeeping gene (or a homozygous deletion of a functionally redundant housekeeping gene) by treating the subject with an inhibitor of the gene. For example, a subject having a cancer with an ENO gene deletion can be treated with a glycolysis inhibitor, such as an enolase inhibitor. In some aspects, a subject having a cancer with an ARS gene deletion can be treated with an ARS inhibitor.
    Type: Application
    Filed: December 14, 2012
    Publication date: December 25, 2014
    Applicants: DANA-FARBER CANCER INSTITUTE, INC., BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Florian L. Muller, Eliot Fletcher-Sananikone, Simona Colla, Elisa Aquilanti, Ronald DePinho
  • Publication number: 20140303122
    Abstract: By searching various kinds of compounds having CaSR agonistic activity, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise the compound. More specifically, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise a glutamic acid derivative having CaSR agonistic activity or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: March 28, 2014
    Publication date: October 9, 2014
    Applicant: AJINOMOTO CO., INC.
    Inventors: Masayuki SUGIKI, Toru Okamatsu, Sayaka Asari, Yayoi Kawato, Toshihiro Hatanaka, Tetsuo Yano, Yukie Seki, Naohiro Miyamura, Hiroaki Nagasaki, Yuzuru Eto, Reiko Yasuda
  • Publication number: 20140256945
    Abstract: The present invention relates to novel derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: March 4, 2014
    Publication date: September 11, 2014
    Applicant: Allergan, Inc.
    Inventors: Phong X. Nguyen, Todd M. Heidelbaugh
  • Patent number: 8828974
    Abstract: The present invention relates to a series of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R1, P1, P2 and P3 are as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.
    Type: Grant
    Filed: April 24, 2012
    Date of Patent: September 9, 2014
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Yong Mi Choi-Sledeski, Julian Levell, Gregory Bernard Poli, Mark Czekaj, Alan John Collis, Roy Vaz
  • Patent number: 8829233
    Abstract: The present invention describes tripodal bisphosphonate derivatives with a flexible basic framework for the functionalization of surfaces, and methods for their production and use. The central atom of the flexible framework is hereby a tertiary aliphatic carbon atom. A fourth remaining position of the flexible framework is suitable to be optionally functionalized by so-called click reactions, for example with biomolecules, polyethylene glycol or active agents.
    Type: Grant
    Filed: September 7, 2011
    Date of Patent: September 9, 2014
    Assignee: Justus-Liebig-Universitaet Giessen
    Inventors: Wolfgang Maison, Elisa Franzmann, Faiza Khalil
  • Publication number: 20140228323
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 14, 2014
    Applicant: NOVARTIS AG
    Inventors: David Weninger BARNES, Scott Louis COHEN, Dean Franklin Rigel
  • Patent number: 8796485
    Abstract: By searching various kinds of compounds having CaSR agonistic activity, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise the compound. More specifically, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise a glutamic acid derivative having CaSR agonistic activity or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 4, 2011
    Date of Patent: August 5, 2014
    Assignee: Ajinomoto Co., Inc.
    Inventors: Masayuki Sugiki, Toru Okamatsu, Sayaka Asari, Yayoi Kawato, Toshihiro Hatanaka, Tetsuo Yano, Yukie Seki, Naohiro Miyamura, Hiroaki Nagasaki, Yuzuru Eto, Reiko Yasuda
  • Publication number: 20140073789
    Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.
    Type: Application
    Filed: November 13, 2013
    Publication date: March 13, 2014
    Inventor: Thomas Daly
  • Publication number: 20130281387
    Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.
    Type: Application
    Filed: October 18, 2011
    Publication date: October 24, 2013
    Applicant: ELCELYX THERAPEUTICS, INC.
    Inventors: Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley
  • Publication number: 20130102570
    Abstract: A medicament having an excellent CaSR agonist action which enables the prevention or treatment of diabetes or obesity is provided by a composition comprising the compound represented by general formula (I) as defined, or a salt thereof.
    Type: Application
    Filed: September 28, 2012
    Publication date: April 25, 2013
    Applicant: AJINOMOTO CO., INC.
    Inventor: AJINOMOTO CO., INC
  • Publication number: 20120316358
    Abstract: Provided is a method for producing a compound expressed by the following formula (3): [where R1 represents a hydrogen atom or C1-4 alkyl group, and R2 represents C1-4 alkyl group, C1-4 alkoxy group, aryl group, aryloxy group or benzyloxy group], the method comprising a reaction of dehydro-condensing a compound expressed by the following formula (1) and a compound expressed by the following formula (2): while being converted to a desired geometric isomer in the presence or absence of an acid catalyst, under a condition that an organic solvent to be used for the reaction is a mixed solvent of acetic acid and a solvent selected from the group consisting of toluene, xylene and chlorobenzene.
    Type: Application
    Filed: June 14, 2011
    Publication date: December 13, 2012
    Applicant: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Takashi Ando, Nobuto Minowa, Masaaki Mitomi
  • Publication number: 20120208784
    Abstract: The present invention relates to a series of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R1, P1, P2 and P3 are as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.
    Type: Application
    Filed: April 24, 2012
    Publication date: August 16, 2012
    Applicant: AVENTIS PHARMACEUTICALS INC.
    Inventors: Yong Mi CHOI-SLEDESKI, Julian LEVELL, Gregory Bernard POLI, Mark CZEKAJ, Alan John COLLIS, Roy VAZ
  • Publication number: 20120202958
    Abstract: This invention relates to new monomers prepared from phosphorus-containing diene monomers and (meth)acrylonitrile via Ritter reactions, and the preparation method thereof. The polymer of these monomers can be utilized in various applications such as water treatment, rheology modifier, surface modification, etc. The monomers have the following structure (II), Wherein R1, R2, R3, R4, R5, R6and R7 represent, independently, hydrogen, alkyl, aryl, alkaryl, aralkyl, cycloalkyl, heterocycloalkyl, or alkenyl groups; R6 and R7 represents R9O, and R10 respectively wherein R9 and R10 represents hydrogen, alkyl, aryl, alkaryl, aralkyl, cycloalkyl, alkenyl groups, or metals selected from the group consisting of Na, Li, Ca; Rs represents H, or CH3.
    Type: Application
    Filed: October 30, 2009
    Publication date: August 9, 2012
    Inventors: Zhaoqing Liu, Floryan De Campo
  • Patent number: 8227450
    Abstract: The present invention provides processes for synthesizing lysine based compounds of the formula; wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, wherein X may be, for example, NH2, Y may be H, F, Cl, or Br, and wherein n, X?, Y?, R2, R3, R4, R5 and R6 are as defined herein.
    Type: Grant
    Filed: November 30, 2006
    Date of Patent: July 24, 2012
    Assignee: Ambrilia Biopharma Inc.
    Inventors: Guy Milot, Stephane Branchaud, Brent R. Stranix
  • Publication number: 20120177681
    Abstract: Immunopotentiators can be adsorbed to insoluble metal salts, such as aluminium salts, to modify their pharmacokinetics, pharmacodynamics, intramuscular retention time, and/or immunostimulatory effect. Immunopotentiators are modified to introduce a moiety, such as a phosphonate group, which can mediate adsorption. These modified compounds can retain or improve their in vivo immunological activity even when delivered in an adsorbed form.
    Type: Application
    Filed: September 1, 2011
    Publication date: July 12, 2012
    Inventors: Manmohan Singh, David A.G. Skibinski, Tom Yao-Hsiang Wu, Yongkai Li, Alex Cortez, Xiaoyue Zhang, Yefen Zou, Timothy Z. Hoffman, Jianfeng Pan, Kathy Yue
  • Patent number: 8183231
    Abstract: The present invention relates to a series of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R1, P1, P2 and P3 are as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.
    Type: Grant
    Filed: October 24, 2006
    Date of Patent: May 22, 2012
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Yong Mi Choi-Sledeski, Julian Levell, Gregory Bernard Poli, Mark Czekaj, Alan John Collis, Roy Vaz
  • Publication number: 20120108551
    Abstract: The present invention relates to compositions that may alleviate symptoms of ocular stress, as well as methods of their production, use, and storage compositions. The compositions comprise at least one ocular epithelial cell associating group and at least one hydrophilic group. In one embodiment the at least one ocular epithelial cell associating group and at least one hydrophilic group are substituents on a conjugated polyaromatic core. The compositions may be used in ophthalmic compositions and ophthalmic devices.
    Type: Application
    Filed: October 29, 2010
    Publication date: May 3, 2012
    Inventors: Frank F. Molock, JR., John C. Heaton
  • Publication number: 20120088720
    Abstract: Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.
    Type: Application
    Filed: April 8, 2010
    Publication date: April 12, 2012
    Applicant: Indiana University Research & Technology Corporati
    Inventors: Zhong-Yin Zhang, Sheng Zhang
  • Patent number: 8129087
    Abstract: A block copolymer that can form selectively a microphase-separated structure under exposure with an ultraviolet exposure device, and a substrate processing method by which a micropattern can be formed at a low cost on the substrate by using the block copolymer. The block copolymer has as a basic skeleton a hydrophobic block that has a repeating structure of a hydrophobic monomer and a hydrophilic block that has a repeating structure of a hydrophilic monomer having a hydrophilic functional group. At least some of the hydrophilic functional groups are covered with a hydrophobic protective group and the hydrophobic protective group, which covers the hydrophilic functional group, is dissociated from the hydrophilic functional group by light irradiation. The substrate processing method uses the block copolymer to form a micropattern on the substrate.
    Type: Grant
    Filed: June 10, 2009
    Date of Patent: March 6, 2012
    Assignee: Canon Kabushiki Kaisha
    Inventor: Toshiki Ito
  • Publication number: 20120035140
    Abstract: The present invention relates to novel metalloproteinase inhibitors having an aryloxybenzenesulfonamide moiety and a carbamoylphosphonic acid moiety, to pharmaceutical compositions comprising them, and to their uses in the prevention and/or treatment of disease or disorder associated with MMP.
    Type: Application
    Filed: February 9, 2010
    Publication date: February 9, 2012
    Applicant: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM, LTD.
    Inventors: Eli Breuer, Reuven Reich, Julia Frant, Amnon Hoffman, Veerendhar Ainelly
  • Publication number: 20120022024
    Abstract: This disclosure relates to compositions and methods including for the inhibition, prevention, and/or treatment of microbial infections, including infections from such pathogens as Staphylococcus aureus.
    Type: Application
    Filed: July 21, 2011
    Publication date: January 26, 2012
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Eric Oldfield, Yongcheng Song
  • Publication number: 20110319366
    Abstract: Compounds of the following formula (I), for example: wherein R1, R2, R3, and R4 are described herein, are useful as inhibitors of plasma carboxypeptidase B. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.
    Type: Application
    Filed: August 29, 2011
    Publication date: December 29, 2011
    Inventors: Brad Buckman, Kumar Emayan, Imadul Islam, Karen May, Judi Bryant, Raju Mohan, Christopher West, Shendong Yuan
  • Publication number: 20110318290
    Abstract: Enzymes mediating in the release of compounds characteristic of human malodour and in particular axillary malodour, and compounds that inhibit said enzymes having the general formula (I)
    Type: Application
    Filed: June 27, 2011
    Publication date: December 29, 2011
    Applicant: GIVAUDAN SA
    Inventors: Andreas Natsch, Gonzalo Acuna, Marie Claude Fournie-Zaluski, Hans Gfeller
  • Patent number: 8076503
    Abstract: The present invention is a process for producing optically active aminophosphinylbutanoic acids represented by the formula (2), comprising asymmetrically hydrogenating a compound represented by the formula (1) in the presence of a ruthenium-optically active phosphine complex, a process for the production thereof, and a compound useful in a herbicide such as L-AHPB that can be produced with good efficiency and high asymmetric yield.
    Type: Grant
    Filed: September 3, 2007
    Date of Patent: December 13, 2011
    Assignees: Meiji Seika Pharma Co., Ltd., Takasago International Corporation
    Inventors: Nobuto Minowa, Nozomu Nakanishi, Masaaki Mitomi, Hideki Nara, Tohru Yokozawa
  • Publication number: 20110251418
    Abstract: By searching various kinds of compounds having CaSR agonistic activity, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise the compound. More specifically, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise a glutamic acid derivative having CaSR agonistic activity or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 4, 2011
    Publication date: October 13, 2011
    Applicant: AJINOMOTO CO., INC.
    Inventors: Masayuki Sugiki, Toru Okamatsu, Sayaka Asari, Yayoi Kawato, Toshihiro Hatanaka, Tetsuo Yano, Yukie Seki, Naohiro Miyamura, Hiroaki Nagasaki, Yuzuru Eto, Reiko Yasuda
  • Publication number: 20110104072
    Abstract: The present application discloses treating water insoluble nanoparticles, particularly nanoparticles of metals and metal compounds which find utility in diagnostic imaging such as MR and X-ray imaging, with an alpha-hydroxyphosphonic acid conjugate with a hydrophilic moiety to render the nanoparticles sufficiently hydrophilic to find utility in diagnostic imaging. Among the modified hydrophilic nanoparticles disclosed are those in which the hydrophilic moieties of the modifying conjugate are ethylene oxide based polymers and copolymers and zwitterions and the nanoparticles are composed of transition metal oxides such as superparamagnetic iron oxide and tantalum oxide. Disclosed are nanoparticles which are sufficiently hydrophilic to form stable aqueous colloidal suspensions. Also disclosed is diagnostic imaging such as MR and X-ray using the modified hydrophilic nanoparticles as contrast agents.
    Type: Application
    Filed: October 30, 2009
    Publication date: May 5, 2011
    Applicant: GENERAL ELECTRIC COMPANY
    Inventors: Brian Christopher Bales, Bruce Allan Hay, Binil Itty Ipe Kandapallil
  • Publication number: 20110092457
    Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
    Type: Application
    Filed: December 20, 2010
    Publication date: April 21, 2011
    Inventors: Michael N. Greco, Harold R. Almond, JR., Michael J. Hawkins, Eugene Powell
  • Publication number: 20110092715
    Abstract: A process for reacting, in the presence of a particular calcium containing catalyst, an amine having an active hydrogen and one or more of a fatty acid ester or a fatty acid.
    Type: Application
    Filed: October 16, 2009
    Publication date: April 21, 2011
    Inventors: Upali Weerasooriya, John Boorem, Brian Hodle, Aaron Boorem, Peter Radford, Howard Stevenson, G. Gerald Barr
  • Patent number: 7888528
    Abstract: A photosensitive monolayer is self-assembled on an oxide surface. The chemical compound of the photosensitive monolayer has three components. A first end group provides covalent bonds with the oxide surface for self assembly on the oxide surface. A photosensitive group that dissociates upon exposure to ultraviolet radiation is linked to the first end group. A second end group linked to the photosensitive group provides hydrophobicity. Upon exposure to the ultraviolet radiation, the dissociated photosensitive group is cleaved and forms a hydrophilic derivative in the exposed region, rendering the exposed region hydrophilic. Carbon nanotubes or nanocrystals applied in an aqueous dispersion are selectively attracted to the hydrophilic exposed region to from electrostatic bonding with the hydrophilic surface of the cleaved photosensitive group.
    Type: Grant
    Filed: August 8, 2009
    Date of Patent: February 15, 2011
    Assignee: International Business Machines Corporation
    Inventors: Ali Afzali-Ardakani, Teresita O. Graham, James B. Hannon, George S. Tulevski
  • Patent number: 7888527
    Abstract: The present invention provides compounds that have antagonist activity at the S1P1 and/or S1P3 receptors. These compounds have enhanced selectivity and potency at the S1P1 and/or S1P3 receptors.
    Type: Grant
    Filed: December 6, 2005
    Date of Patent: February 15, 2011
    Assignee: University of Virginia Patent Foundation
    Inventors: Kevin R. Lynch, Timothy L. Macdonald, Jeremy J. Clemens, Michael D. Davis
  • Publication number: 20100173166
    Abstract: A composition represented by formula: (I) Rf is a monovalent or divalent perfluoropolyether group. Each R is independently selected from the group consisting of hydrogen and alkyl having from 1 to 4 carbon atoms. Each X is independently a divalent or trivalent group selected from the group consisting of alkylene, arylalkylene, and alkylarylene, wherein alkylene, arylalkylene, and alkylarylene are each optionally interrupted by at least one ether linkage. Each V is independently alkylene that is optionally interrupted by at least one ether linkage or amine linkage. Each Y is independently selected from the group consisting of hydrogen, alkyl, and a counter cation; y is 1 or 2; and z is 1 or 2. Methods of treating a surface using these compositions, formulations including these compositions, and articles with a surface in contact with these compositions are provided. Rf—{C(O)—N(R)—X—[OC(O)—V—P(O)—(OY)2]y}z.
    Type: Application
    Filed: June 5, 2008
    Publication date: July 8, 2010
    Inventors: Rudolf J. Dams, Steven J. Martin
  • Patent number: 7745489
    Abstract: Specific, highly potent 2-oxo-amide based inhibitors of phospholipase A2 (PLA2) activity are provided. A role for PLA2 activity in spinally mediated inflammatory processes is established, and a method for treating hyperalgesia and other inflammatory conditions associated with PLA2 activity is provided.
    Type: Grant
    Filed: March 7, 2003
    Date of Patent: June 29, 2010
    Assignee: The Regents of the University of California
    Inventors: Edward Dennis, Tony Yaksh, Karin Killermann Lucas, Camilla Svensson, David A. Six, George Kokotos, Violetta Constantinou-Kokotou
  • Publication number: 20100130773
    Abstract: The present invention relates to a new process for the synthesis of alkyl phosphinic acids, and more particularly to a coupling reaction between an alkylhalide and a hypophosphorous acid derivative in the presence of an amine and an amineoxide.
    Type: Application
    Filed: April 30, 2008
    Publication date: May 27, 2010
    Applicant: ASTRAZENECA AB
    Inventors: Daniel Finnhult, Roger Sohlberg, Fredrik Stalfors, Carina Svensson, Johanna Wachtmeister, Thomas Wannman
  • Patent number: 7678426
    Abstract: Perfluoropolyether amide-linked phosphonates and derivatives thereof are provided. Compositions containing perfluoropolyether amide-linked phosphonates or derivatives thereof, perfluoropolyether amide-linked phosphates or derivatives thereof, or combinations thereof are also provided. Additionally, articles, methods of making articles, and methods of reducing contaminant adhesion to a substrate are described.
    Type: Grant
    Filed: July 7, 2004
    Date of Patent: March 16, 2010
    Assignee: 3M Innovative Properties Company
    Inventors: Richard M. Flynn, Mark J. Pellerite
  • Publication number: 20090186855
    Abstract: The present invention relates to compounds and methods useful in the prevention or treatment of diseases or conditions associated with Toll-like receptor 2 activation.
    Type: Application
    Filed: April 1, 2009
    Publication date: July 23, 2009
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Jesse Chow, Fabian Gusovksy, Lynn Hawkins, Mark Spyvee
  • Publication number: 20090137531
    Abstract: The present invention provides compounds that have antagonist activity at the S1P1 and/or S1P3 receptors. These compounds have enhanced selectivity and potency at the S1P1 and/or S1P3 receptors.
    Type: Application
    Filed: December 6, 2005
    Publication date: May 28, 2009
    Inventors: Kevin R. Lynch, Timothy L. MacDonald, Jeremy J. Clemens, Michael D. Davis
  • Publication number: 20090118235
    Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
    Type: Application
    Filed: October 24, 2008
    Publication date: May 7, 2009
    Inventors: Michael N. Greco, Harold R. Almond, JR., Lawrence de Garavilla, Michael J. Hawkins, Michael J. Humora, Yun Qian, Donald Gilmore Walker, Sergio Cesco-Cancian, Christopher Norman Nilsen, Mitul N. Patel, Kirk Leonard Sorgi, Eugene Powell
  • Publication number: 20090048426
    Abstract: The present invention provides an adhesive composition comprising a polymerizable phosphonic acid derivative which is a composition having intramolecularly a polymerizable group and a phosphonic acid group, represented by the general formula [1]: wherein R represents a polymerizable group; A represents an oxygen atom or a sulfur atom; Xqs represent independently an oxygen atom or a sulfur atom; Yqs represent independently the same or different organic group; Zqs may be independently the same or different from each other and, a part of the Zqs optionally selected or all of the Zqs represent organic groups having a substituent which is an organic group other than a polymerizable group and a phosphonic acid group; p is an integer from 1 to 10; q is an integer from 1 to p; when p is 1, q is 1; X1 represents an oxygen atom or a sulfur atom; Y1 represents an organic group; Z1 represents an organic group having one or more of substituents which are organic groups other than an acidic group and a polymerizab
    Type: Application
    Filed: December 4, 2007
    Publication date: February 19, 2009
    Applicant: KABUSHIKI KAISHA SHOFU
    Inventors: Kunio IKEMURA, Yoshiyuki Jogetsu, So Ito
  • Publication number: 20080317700
    Abstract: The present invention holds forth improvements in the field of herbicide synthesis, their application, and methods of plant and weed control and antifouling. The present invention includes the synthesis of new acrylate and methacrylate derivatives of a glyphosate. Two isomers resulting from a hindered rotation around the amide CN bond are observed for both acrylic and methacrylic analogs and barriers for internal rotation are obtained. Biological activity tests indicate that functionalized glyphosates possess herbicidal activity similar to the parent compound.
    Type: Application
    Filed: December 21, 2007
    Publication date: December 25, 2008
    Applicant: Bowling Green State University
    Inventors: Douglas C. Neckers, Aneta Bogdanova, Andrei V. Fedorov
  • Patent number: 7452487
    Abstract: A phosphorus-acid-group-containing (meth)acrylamide polymer having high electrolytic group density and excellent conductivity is obtained by introducing a phosphorus acid group into a (meth)acrylamide monomer which may be N-substituted, and polymerizing the resultant monomer. This polymer is usable for conductive resins, proton-conductive polymer electrolyte membranes and coating agents.
    Type: Grant
    Filed: February 23, 2005
    Date of Patent: November 18, 2008
    Assignee: Uni-Chemical Co., Ltd.
    Inventor: Yoshio Kanzaki
  • Publication number: 20080161592
    Abstract: The present invention provides compounds of Formula (I) and Formula (II) that are useful for modulating the biological activity of the protein tyrosine phosphatase-1b (PTP1B) enzyme. Compounds of this invention can be used to treat diseases and/or conditions in which the PTP1B enzyme is a factor. Such diseases and/or conditions include, but are not limited to, Type 1 diabetes, Type 2 diabetes, inadequate glucose tolerance, insulin resistance, obesity, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, low HDL levels, atherosclerosis, vascular restenosis, inflammatory bowel disease, pancreatitis, adipose cell tumors, adipose cell carcinoma, liposarcoma, dyslipidemia, cancer, and neurodegenerative diseases.
    Type: Application
    Filed: March 6, 2008
    Publication date: July 3, 2008
    Applicant: CEPTYR, INC.
    Inventors: Mark Arnold Thomas Blaskovich, Ted Baughman, Thomas Little, William Patt, Maher Qabar, Lauri Marie Schultz, Feng Hong, Gangadhar Nagula, Jennifer Lynn Gage, James Jeffrey Howbert
  • Patent number: 7345033
    Abstract: The present invention provides a compound of the following formula I: R3—NH—C(?X)—P(?O)OR1OR2 including pharmaceutically acceptable salts, solvates, hydrates and polymorphs of the compounds of formula I, as well as geometrical isomers and optically active forms of the compounds of formula I and pharmaceutically acceptable salts, solvates, hydrates and polymorphs of said isomers and forms, wherein R1 and R2 may be the same or different and are each selected from hydrogen, acyloxyalkyl and aryl or R1 and R2 may form together with the oxygen and phosphorus atoms a dioxaphosphacycloalkane ring; X is O or S; and R3 is selected, when X is O, from bicycloalkyl, cycloalkylalkyl and substituted cycloalkyl by at least one of alkyl, amino, amidino and guanidino; and R3 is selected, when X is S, from bicycloalkyl, cycloalkylalkyl and cycloalkyl optionally substituted by at least one of alkyl, amino, amidino and guanidino; with the proviso that: when X is O, R3 is not cyclohexylmethyl, and when X is S, R3 is not cycl
    Type: Grant
    Filed: October 6, 2005
    Date of Patent: March 18, 2008
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventors: Eli Breuer, Reuven Reich, Gershon Golomb, Yiffat Katz
  • Patent number: 7157092
    Abstract: Compounds of the formula wherein the substitutents are defined as in the specification useful for modulating immune responses in warm-blooded animals.
    Type: Grant
    Filed: June 23, 1999
    Date of Patent: January 2, 2007
    Assignee: Om Pharma
    Inventors: Jacques Bauer, Olivier Richard Martin
  • Patent number: 6919322
    Abstract: Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.
    Type: Grant
    Filed: March 7, 2001
    Date of Patent: July 19, 2005
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Brett C. Bookser, Qun Dang, K. Raja Reddy
  • Publication number: 20040229848
    Abstract: The present invention relates dipeptidyl peptidase IV inhibition and, more particularly, relates to glutaminyl derivatives, wherein the glutamin residue is bound in a peptide manner to a moiety which imitates the amino acid residue prolin, especially to a nitrogen containing moiety, pharmaceutical compositions containing said compounds, and the use of said compounds in inhibiting dipeptidyl peptidase IV and dipeptidyl peptidase IV-like enzyme activity.
    Type: Application
    Filed: May 5, 2004
    Publication date: November 18, 2004
    Inventors: Hans-Ulrich Demuth, Matthias Hoffmann, Torsten Hoffmann, Andre J. Niestroj, Stephan Schilling, Ulrich Heiser
  • Patent number: 6737416
    Abstract: A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: wherein R1 represents hydrogen atom, an alkyl group, a substituted alkyl group and the like; R2 and R3 represent hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group and the like; X represents —CH2—, —O—, or —NH—; A represents the following group (II): [in which R7 and R8 represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group and the like; R9 and R10 represents hydrogen atom, a halogen atom, hydroxyl group, phenyl group, an alkyl group and the like] and the like; and E represents hydrogen atom and the like, which has inhibitory activity against carboxypeptidase B and is useful for therapeutic and/or preventive treatment of a thrombotic disease.
    Type: Grant
    Filed: October 7, 2002
    Date of Patent: May 18, 2004
    Assignee: Meiji Seika Kaisha Ltd.
    Inventors: Kenichi Fushihara, Chika Kikuchi, Tetsuya Matsushima, Kenichi Kanemoto, Eriko Satoh, Takehiro Yamamoto, Kokichi Suzuki
  • Patent number: 6576627
    Abstract: A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: wherein R1 represents hydrogen atom, an alkyl group, a substituted alkyl group and the like; R2 and R3 represent hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group and the like; X represents —CH2—, —O—, or —NH—; A represents the following group (II): [in which R7 and R8 represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group and the like; R9 and R10 represents hydrogen atom, a halogen atom, hydroxyl group, phenyl group, an alkyl group and the like] and the like; and E represents hydrogen atom and the like, which has inhibitory activity against carboxypeptidase B and is useful for therapeutic and/or preventive treatment of a thrombotic disease.
    Type: Grant
    Filed: November 13, 2001
    Date of Patent: June 10, 2003
    Assignee: Meiji Seika Kaisha Ltd.
    Inventors: Kenichi Fushihara, Chika Kikuchi, Tetsuya Matsushima, Kenichi Kanemoto, Eriko Satoh, Takehiro Yamamoto, Kokichi Suzuki
  • Patent number: 6576766
    Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediate by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutic compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of formula (1) as defined herein.
    Type: Grant
    Filed: August 17, 2000
    Date of Patent: June 10, 2003
    Assignee: Ariad Pharmaceuticals, Inc.
    Inventors: Manfred Weigele, Regine Bohacek, Virginia A. Jacobsen, Karina Macek, Michael G. Yang, Noriyuki H. Kawahata, Rajeswari Sundaramoorthi, Yihan Wang, Craig S. Takeuchi, George P. Luke, Chester A. Metcalf, III, William C. Shakespeare, Tomi K. Sawyer