Acyclic -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/473)
  • Patent number: 10874103
    Abstract: A bactericidal or bacteriostatic composition comprising an acetal or a hexitan ether preferentially of a long-chain alkyl sorbitan, arlitan or mannitan, its use in the treatment or prevention of Gram-positive bacterial infections, its use as a hygiene or dermatological product for external use and a method for disinfecting surfaces.
    Type: Grant
    Filed: December 17, 2015
    Date of Patent: December 29, 2020
    Assignee: TEREOS STARCH & SWEETENERS BELGIUM
    Inventors: Charlotte Gozlan, Dorine Belmessieri, Marie-Christine Duclos, Nicolas Duguet, Marc Lemaire, Gérard Lina, Oana Dumitrescu, Andreas Redl
  • Patent number: 10059700
    Abstract: A supported catalyst for aldehyde coupling reaction, comprising a carrier having supported thereon a catalyst comprising at least one azolium compound selected from the group consisting of a thiazolium salt, an imidazolium salt, a benzimidazolium salt and a triazolium salt, the azolium compound having, at a nitrogen atom thereof, a substituent selected from the group consisting of an aliphatic group having 6 or more carbon atoms and an aromatic group having 6 or more carbon atoms.
    Type: Grant
    Filed: May 31, 2016
    Date of Patent: August 28, 2018
    Assignees: SEKISUI CHEMICAL CO., LTD., COLORADO STATE UNIVERSITY RESEARCH CORPORATION
    Inventors: Eugene Y. X. Chen, Lu Wang, Yuji Eguchi
  • Patent number: 9416068
    Abstract: The invention relates to a method for producing liquid fuel having a high alkane content and a low oxygenized compound content, said method comprising at least: a first step of treating 2-methylfuran with a catalyst and water in reaction conditions in order to form a mixture of products with at least ten carbon atoms; and a second step of catalytic hydrogenation and dehydration of the product or the mixture obtained in step 1, using suitable hydrogenation and dehydration catalysts.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: August 16, 2016
    Assignees: CONSEJO SUPERIOR DE INVESTIGACIONES CIENTIFICAS (CSIC), UNIVERSIDAD POLITECNICA DE VALENCIA
    Inventors: Avelino Corma Canos, Michael Renz, Olalla De La Torre Alfaro
  • Publication number: 20150141417
    Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.
    Type: Application
    Filed: May 14, 2012
    Publication date: May 21, 2015
    Inventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
  • Patent number: 9012490
    Abstract: Compounds having formulas (I) to (VIII), salts thereof, or combinations thereof and pharmaceutical compositions comprising one or more these compounds are described herein for the treatment of HIV and neurodegenerative effects caused by HIV. Also provided herein are methods and a kit for inhibiting HIV-1, treating latent HIV in the brain, and preventing HIV-mediated cognitive decline and HIV dementia comprising administering the compounds having the formulas (I) to (VIII) and pharmaceutical compositions comprising the compounds having these formulas. The compounds having formulas I through VIII are curcumin analogs which are advantageously characterized as having anti-retroviral, neuroprotective, anti-glucosidase, and anti-HIV integrase properties. In one aspect, the pharmaceutical composition is delivered intranasally.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: April 21, 2015
    Assignee: Howard University
    Inventors: Evaristus A. Nwulia, Amol Kulkarni
  • Publication number: 20150072969
    Abstract: The present invention relates to phenyl alkanoic acid derivatives (the compounds of Formula (I)); and their isotopic forms, stereoisomeric and tautomeric forms and mixtures thereof in all ratios, or pharmaceutically acceptable salts, pharmaceutically acceptable solvates, prodrugs, polymorphs, N-oxides, S-oxides or carboxylic acid isosteres thereof. The invention also relates to processes for the preparation of compounds of Formula (I) and pharmaceutical compositions comprising one or more of the compounds of Formula (I). The said compounds and the pharmaceutical composition function as GPR (G-protein coupled receptor) agonists, particularly as GPR40 agonists, and are useful in the treatment of diseases or conditions mediated by GPR40. The present invention further relates to a method of treatment of diseases or conditions mediated by GPR40 comprising administering to a subject in need thereof a therapeutically effective amount of the compounds of Formula (I).
    Type: Application
    Filed: February 27, 2013
    Publication date: March 12, 2015
    Applicant: PIRAMAL ENTERPRISES LIMITED
    Inventors: Sanjay Kumar, Rajiv Sharma, Vishal Ashok Mahajan, Sangameshwar Prabhakar Sawargave
  • Patent number: 8956799
    Abstract: A photoacid generator includes those of formula (I): wherein each Ra in formula 1 is independently H, F, a C1-10 nonfluorinated organic group, C1-10 fluorinated organic group, or a combination comprising at least one of the foregoing, provided at least one Ra is F or a C1-10 fluorinated organic group, the C1-10 fluorinated and nonfluorinated organic groups each optionally comprising O, S, N, or a combination comprising at least one of the foregoing heteroatoms; L1 is a linking group comprising a heteroatom comprising O, S, N, F, or a combination comprising at least one of the foregoing; G+ is an onium salt of the formula (II): wherein in formula (II), X is S or I, each R0 is independently C1-30 alkyl group; a polycyclic or monocyclic C3-30 cycloalkyl group; a polycyclic or monocyclic C4-30 aryl group; or a combination comprising at least one of the foregoing, provided at least one R0 is substituted where each R0 is a C6 monocyclic aryl group, and wherein when X is I, a is 2, and where X is S, a is 3,
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: February 17, 2015
    Assignee: Rohm and Haas Electronic Materials LLC
    Inventors: Emad Aqad, Cheng-Bai Xu, Mingqi Li, William Williams, III
  • Patent number: 8940914
    Abstract: Disclosed are compositions and methods for the production of mono-esters and di-esters from the reaction of HMF and a reactant selected from a diacid or a diacid derivative; typical reactants are PAN, phthaloyl dichloride, dimethyl phthalate, maleic acid, and maleic anhydride or mono-esters that can be prepared from HMF and MAN.
    Type: Grant
    Filed: July 20, 2012
    Date of Patent: January 27, 2015
    Assignee: Battelle Memorial Institute
    Inventors: Herman P. Benecke, Jerry L. King, II, Alex Walter Kawczak, Donald W. Zehnder, II, Erica E. Hirschl
  • Patent number: 8906351
    Abstract: The invention relates to the use of compounds of the formula (I), in which R1, R2, m and n have the meanings indicated in the Claims, and/or physiologically acceptable salts, tautomers, stereoisomers and/or solvates thereof, including mixtures thereof in all ratios, for the inhibition of tyrosinase and for lightening the skin. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of pigment disorders of the skin. The invention furthermore relates to preparations comprising the compounds of the formula (I) in combination with at least one further active compound and to a process for the preparation of the preparations by mixing the compounds of the formula (I) with a vehicle which is physiologically acceptable for topical applications.
    Type: Grant
    Filed: August 18, 2011
    Date of Patent: December 9, 2014
    Assignee: Merck Patent GmbH
    Inventor: Rene Peter Scheurich
  • Patent number: 8895587
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, G1, n, A1, A2, A3, A4, Y1, Y2, and Y3 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: May 15, 2012
    Date of Patent: November 25, 2014
    Assignee: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
  • Patent number: 8883824
    Abstract: Disclosed is a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is 1: a C3-8 cycloalkyl C1-4 alkyl group, 2: a C7-14 aralkyl group, in which the aryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, (b) C1-4 alkyl, which is optionally substituted with 1 to 3 fluorine atoms, (c) C1-4 alkoxy, which is optionally substituted with 1 to 3 fluorine atoms, and (d) C1-4 alkylcarbonyl, which is optionally substituted with C1-4 alkoxy, 3: a five-to ten-membered heteroaryl-C1-4 alkyl group, in which the heteroaryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, and (b) C1-4 alkyl, or 4: a C6-10 aryl C2-6 alkenyl group; and R2 is a cyano group or a nitro group.
    Type: Grant
    Filed: May 12, 2010
    Date of Patent: November 11, 2014
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Akihito Fujii, Kazumi Niidome, Chiaki Migihashi, Toshiyuki Kamei, Takafumi Matsumoto, Tomoyuki Hirata
  • Publication number: 20140316148
    Abstract: Polyol ether compounds and processes for their preparation. A representative process comprises melting a polyol, and reacting the molten polyol, a carbonyl compound, and hydrogen in the presence of a hydrogenation catalyst to provide the poly of ether. The polyol ether has surfactant properties.
    Type: Application
    Filed: February 22, 2012
    Publication date: October 23, 2014
    Applicant: DOW GLOBAL TECHNOLOGIES LLC
    Inventors: Michael L. Tulchinsky, Sze-Sze Ng, Cynthia L. Rand
  • Publication number: 20140309208
    Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are disclosed that are represented by general formula (I). Also disclosed, are pharmaceutical compositions including these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated pathologies.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Inventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
  • Publication number: 20140296254
    Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are described that correspond to general formula (I). Also described, are pharmaceutical compositions that include these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated diseases.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 2, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
  • Publication number: 20140256963
    Abstract: The present invention provides a novel process and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren, or a salt thereof, preferably Aliskiren hemifumarate.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 11, 2014
    Inventors: Sujay Biswas, Sankareswaran Srimurugan, Anjul Kumar, Atulya Kumar Panda, Danish Jamshad, Mukesh Masand, Bidyut Biswas, Vikas Bansal, Ashish Kumar Gupta, Dharam Vir
  • Publication number: 20140107161
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R2, R3, R4, G1, n, A1, A2, A3, A4, Y1, Y2, and Y3 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: May 12, 2012
    Publication date: April 17, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
  • Publication number: 20140094455
    Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.
    Type: Application
    Filed: August 19, 2013
    Publication date: April 3, 2014
    Applicant: ARIZONA BOARD OF REAGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
    Inventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
  • Patent number: 8685975
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: April 1, 2014
    Assignee: Omeros Corporation
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
  • Publication number: 20140051742
    Abstract: Compounds having formulas (I) to (VIII), salts thereof, or combinations thereof and pharmaceutical compositions comprising one or more these compounds are described herein for the treatment of HIV and neurodegenerative effects caused by HIV. Also provided herein are methods and a kit for inhibiting HIV-1, treating latent HIV in the brain, and preventing HIV-mediated cognitive decline and HIV dementia comprising administering the compounds having the formulas (I) to (VIII) and pharmaceutical compositions comprising the compounds having these formulas. The compounds having formulas I through VIII are curcumin analogs which are advantageously characterized as having anti-retroviral, neuroprotective, anti-glucosidase, and anti-HIV integrase properties. In one aspect, the pharmaceutical composition is delivered intranasally.
    Type: Application
    Filed: March 11, 2013
    Publication date: February 20, 2014
    Inventors: Evaristus A. Nwulia, Amol Kulkarni
  • Publication number: 20140007497
    Abstract: The invention provides new methods for the direct umpolung self-condensation of 5-hydroxymethylfurfural (HMF) by organocatalysis, thereby upgrading the readily available substrate into 5,5?-di(hydroxymethyl)furoin (DHMF). While many efficient catalyst systems have been developed for conversion of plant biomass resources into HMF, the invention now provides methods to convert such nonfood biomass directly into DHMF by a simple process as described herein. The invention also provides highly effective new methods for upgrading other biomass furaldehydes and related compound to liquid fuels. The methods include the organocatalytic self-condensation (umpolung) of biomass furaldehydes into (C8-C12)furoin intermediates, followed by hydrogenation, etherification or esterification into oxygenated biodiesel, or hydrodeoxygenation by metal-acid tandem catalysis into premium hydrocarbon fuels.
    Type: Application
    Filed: July 2, 2013
    Publication date: January 9, 2014
    Inventors: Eugene Y. CHEN, Dajiang LIU
  • Patent number: 8623859
    Abstract: The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
    Type: Grant
    Filed: August 10, 2009
    Date of Patent: January 7, 2014
    Assignee: Evotec AG
    Inventors: James Madden, David James Hallett, Alastair Parkes, Ali Raoof, Xiaolu Wang
  • Publication number: 20130338313
    Abstract: The invention is based on the discovery that a remarkable improvement in the performance of maleimide thermosets can be achieved by incorporating amide-extended maleimides into an adhesive formulation. Amide-extended maleimides described herein can be used to toughen bismaleimide thermosetting materials without sacrificing any thermal stability. Amide-extended maleimides are readily prepared by reacting a bismaleimide with an appropriate amine via the well-known Michael addition reaction. Acylation of the resulting secondary amines provides the amide-extended maleimide. The acylating agent can also be used to introduce polymerizable functional groups into the backbones of these thermoset monomers. Amide-extended acrylate and methacrylate monomers can also be prepared.
    Type: Application
    Filed: August 19, 2013
    Publication date: December 19, 2013
    Applicant: Designer Molecules, Inc.
    Inventors: Stephen M. Dershem, Farhad G. Mizori
  • Publication number: 20130303466
    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: November 14, 2013
    Applicant: ELCELYX THERAPEUTICS, INC.
    Inventors: Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley, Alain D. Baron
  • Publication number: 20130303531
    Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.
    Type: Application
    Filed: May 14, 2012
    Publication date: November 14, 2013
    Inventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
  • Publication number: 20130274283
    Abstract: Premature termination codons readthrough compounds, composition thereof, and methods of making and using the same are provided.
    Type: Application
    Filed: February 11, 2013
    Publication date: October 17, 2013
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Richard A. GATTI, Liutao DU, Robert DAMOISEAUX, Chih-Hung LAI, Michael JUNG, Jin-Mo KU, Carmen BERTONI
  • Publication number: 20130239852
    Abstract: A biobased plasticizer and a surface covering are disclosed. The biobased plasticizer includes an ester formed as a reaction product of a furan derivative selected from the group consisting of furoic acid, furfural and furfuryl alcohol reacted with a carboxylic acid or an alcohol, or includes an ester formed as a reaction product of a biobased aromatic compound and a biobased aliphatic compound. The surface covering is plasticized with a composition comprising an ester formed as a reaction product of a functionalized aromatic heterocyclic compound reacted with a carboxylic acid or an alcohol.
    Type: Application
    Filed: March 19, 2012
    Publication date: September 19, 2013
    Applicant: ARMSTRONG WORLD INDUSTRIES
    Inventors: Mary Kate DAVIES, Dong TIAN
  • Patent number: 8507700
    Abstract: Method of producing C8-C15 hydrocarbons comprising providing a ketone starting material; providing an aldol starting material comprising hydroxymethylfurfural; mixing the ketone starting material and the aldol starting material in a reaction in the presence of a proline-containing catalyst selected from the group consisting of Zn(Pro)2, Yb(Pro)2, and combinations thereof, or a catalyst having one of the structures (I), (II) or (III), and in the presence of a solvent, wherein the solvent comprises water and is substantially free of organic solvents, where (I), (II) and (III) respectively are: where R1 is a C1-C6 alkyl moiety, X=(OH) and n=2. In (III), X may be CH2, sulfur or selenium, M may be Zn, Mg, or a lanthanide, and R1 and R2 each independently may be a methyl, ethyl, phenyl moiety.
    Type: Grant
    Filed: July 24, 2012
    Date of Patent: August 13, 2013
    Assignee: Los Alamos National Security, LLC
    Inventors: Louis A. Silks, John C. Gordon, Ruilan Wu, Susan Kloek Hanson
  • Patent number: 8497386
    Abstract: Method of producing C8-C15 hydrocarbons. comprising providing a ketone starting material; providing an aldol starting material comprising chloromethylfurfural; mixing the ketone starting material and the aldol starting material in a reaction in the presence of a proline-containing catalyst selected from the group consisting of Zn(Pro)2, Yb(Pro)3, and combinations thereof, or a catalyst having one of the structures (I), (II) or (III), and in the presence of a solvent, wherein the solvent comprises water and is substantially free of organic solvents, where (I), (II) and (III) respectively are: where R1 is a C1-C6 alkyl moiety, X=(OH) and n=2. In (III), X may be CH2, sulfur or selenium, M may be Zn, Mg, or a lanthanide, and R1 and R2 each independently may be a methyl, ethyl, phenyl moiety.
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: July 30, 2013
    Assignee: Los Alamos National Security, LLC
    Inventors: Louis A. Silks, John C. Gordon, Ruilan Wu, Susan Kloek Hanson
  • Publication number: 20130190516
    Abstract: Disclosed are compositions and methods for the production of mono-esters and di-esters from the reaction of HMF and a reactant selected from a diacid or a diacid derivative; typical reactants are PAN, phthaloyl dichloride, dimethyl phthalate, maleic acid, and maleic anhydride or mono-esters that can be prepared from HMF and MAN.
    Type: Application
    Filed: July 20, 2012
    Publication date: July 25, 2013
    Applicant: Battelle Memorial Institute
    Inventors: Herman Paul Benecke, Jerry L. King, II, Alex Walter Kawczak, Donald W. Zehnder, II, Erica E. Hirschl
  • Publication number: 20130164230
    Abstract: The invention relates to the use of compounds of the formula (I), in which R1, R2, m and n have the meanings indicated in the Claims, and/or physiologically acceptable salts, tautomers, stereoisomers and/or solvates thereof, including mixtures thereof in all ratios, for the inhibition of tyrosinase and for lightening the skin. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of pigment disorders of the skin. The invention furthermore relates to preparations comprising the compounds of the formula (I) in combination with at least one further active compound and to a process for the preparation of the preparations by mixing the compounds of the formula (I) with a vehicle which is physiologically acceptable for topical applications.
    Type: Application
    Filed: August 18, 2011
    Publication date: June 27, 2013
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventor: Rene Peter Scheurich
  • Publication number: 20130053417
    Abstract: The invention provides a compound that is a CETP activity inhibitor. The compound can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity, the invention also provides for the use of the compound to prevent or treat atherosclerosis or hyperlipidemia.
    Type: Application
    Filed: March 21, 2012
    Publication date: February 28, 2013
    Applicant: JAPAN TOBACCO INC.
    Inventors: Hisashi Shinkai, Kimiya Maeda, Hiroshi Okamoto
  • Patent number: 8350067
    Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: January 8, 2013
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Atsushi Endo, Charles E. Chase, Francis G. Fang
  • Patent number: 8343970
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: January 1, 2013
    Assignee: Omeros Corporation
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
  • Patent number: 8334393
    Abstract: The invention relates to compounds of formula (I): wherein R1 and R2 are each independently selected from the group: H, F, Cl and CH3; n1 and n2 are each independently integers 3 to 20; q and r are each independently integers 0, 1 or 2, with the proviso that q+r is ?1; D is a divalent chiral radical selected from the group: wherein R3 is a C1 to C6 straight or branched chain alkyl group; and each B1 and B2 is a divalent radical independently selected from the group: R4-substituted-1,4-phenyl, wherein R4 is H, —CH3 or —OCH3; 2,6-naphthyl; and 4,4?-biphenyl; with the provisos that when q+r=3, at least one of B1 and B2 is R4-substituted-1,4-phenyl; and when q+r=4, at least two of B1 and B2 are R4-substituted-1,4-phenyl. The invention further relates to liquid crystal compositions comprising compounds of formula (I) and polymer networks derived from the polymerization of the liquid crystal compositions.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: December 18, 2012
    Assignee: E I du Pont de Nemours and Company
    Inventors: Marc B. Goldfinger, Jose Manuel Rodriguez-Parada, Lee A. Silverman, Kai Qi
  • Patent number: 8324268
    Abstract: The present invention relates to novel substituted furancarboxamides, methods for their production, their use for the treatment and/or prevention of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially retroviral diseases, in humans and/or animals.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: December 4, 2012
    Assignee: AiCuris GmbH & Co. KG
    Inventors: Kai Thede, Susanne Greschat, Steffen Wildum, Daniela Paulsen
  • Publication number: 20120302752
    Abstract: Methods are described for efficient and regioselective reactions that are Ru-catalyzed and either (i) amide-directed C—H, C—N, C—O activation/C—C bond forming reactions, (ii) ester-directed C—O and C—N activation/C—C bond forming reactions, or (iii) amide-directed C—O activation/hydrodemethoxylation reactions. All of these reactions of directed C—H, C—N, C—O activation/coupling reactions establish a catalytic base-free DoM-cross coupling process at non-cryogenic temperature. High regioselectivity, yields, operational simplicity, low cost, and convenient scale-up make these reactions suitable for industrial applications. Many previously unknown amide-substituted or ester-substituted aryl and heteroaryl compounds are presented with synthetic details also provided.
    Type: Application
    Filed: May 24, 2012
    Publication date: November 29, 2012
    Inventors: Yigang Zhao, Victor A. Snieckus
  • Publication number: 20120289719
    Abstract: Method of producing C8-C15 hydrocarbons comprising providing a ketone starting material; providing an aldol starting material comprising hydroxymethylfurfural; mixing the ketone starting material and the aldol starting material in a reaction in the presence of a proline-containing catalyst selected from the group consisting of Zn(Pro)2, Yb(Pro)2, and combinations thereof, or a catalyst having one of the structures (I), (II) or (III), and in the presence of a solvent, wherein the solvent comprises water and is substantially free of organic solvents, where (I), (II) and (III) respectively are: where R1 is a C1-C6 alkyl moiety, X=(OH) and n=2. In (III), X may be CH2, sulfur or selenium, M may be Zn, Mg, or a lanthanide, and R1 and R2 each independently may be a methyl, ethyl, phenyl moiety.
    Type: Application
    Filed: July 24, 2012
    Publication date: November 15, 2012
    Inventors: Louis A. Silks, John C. Gordon, Ruilan Wu, Susan Kloek Hanson
  • Publication number: 20120289720
    Abstract: Method of producing C8-C15 hydrocarbons. comprising providing a ketone starting material; providing an aldol starting material comprising chloromethylfurfural; mixing the ketone starting material and the aldol starting material in a reaction in the presence of a proline-containing catalyst selected from the group consisting of Zn(Pro)2, Yb(Pro)3, and combinations thereof, or a catalyst having one of the structures (I), (II) or (III), and in the presence of a solvent, wherein the solvent comprises water and is substantially free of organic solvents, where (I), (II) and (III) respectively are: where R1 is a C1-C6 alkyl moiety, X?(OH) and n=2. In (III), X may be CH2, sulfur or selenium, M may be Zn, Mg, or a lanthanide, and R1 and R2 each independently may be a methyl, ethyl, phenyl moiety.
    Type: Application
    Filed: July 25, 2012
    Publication date: November 15, 2012
    Inventors: Louis A. Silks, John C. Gordon, Ruilan Wu, Susan Kloek Hanson
  • Publication number: 20120289718
    Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate.
    Type: Application
    Filed: May 22, 2012
    Publication date: November 15, 2012
    Inventors: Atsushi ENDO, Charles E. CHASE, Francis G. FANG
  • Patent number: 8247582
    Abstract: Disclosed are compositions and methods for the production of mono-esters and di-esters from the reaction of HMF and a reactant selected from a diacid or a diacid derivative; typical reactants are PAN, phthaloyl dichloride, dimethyl phthalate, maleic acid, and maleic anhydride or mono-esters that can be prepared from HMF and MAN.
    Type: Grant
    Filed: February 7, 2007
    Date of Patent: August 21, 2012
    Assignee: Battelle Memorial Institute
    Inventors: Herman P. Benecke, Jerry L. King, II, Alex Walter Kawczak, Donald W. Zehnder, II, Erica E. Hirschl
  • Patent number: 8173700
    Abstract: The present invention relates to salts of substituted allophanates, methods for their production, medicaments containing said compounds and the use of said compound for the production of medicaments.
    Type: Grant
    Filed: May 17, 2006
    Date of Patent: May 8, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Ruth Jostock, Hans Schick, Fritz Theil, Olga Groeger, Rene Kudick, Helmut Sonnenschein, Birgitta Henkel
  • Publication number: 20110294848
    Abstract: The invention provides potent quinolinol-based BoNT/A small-molecule inhibitors of botulinum neurotoxins, in particular of Clostridium botulinum serotype A neurotoxins. The invention also provides methods of using these small-molecule inhibitors to inhibit infections by Clostridium botulinum, as well as, methods of preventing infections by Clostridium botulinum through materials that may be ingested.
    Type: Application
    Filed: May 28, 2009
    Publication date: December 1, 2011
    Inventors: Virginia I. Roxas-Duncan, Leonard A. Smith, Nizamettin Gul, John H. Cardellina, II, Rebecca C. Vieira, Susan M. Ensel, David C.H. Yang, Istvan J. Enyedy, Sivanesan Darkshanamurthy, Salimuddin Shah
  • Publication number: 20110275625
    Abstract: Disclosed are compounds and compositions of the formula (I) as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula (I).
    Type: Application
    Filed: November 5, 2009
    Publication date: November 10, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Shuang Liang, Sabine Schlyer, Lana Louise Smith Keenan, Steven John Taylor, Bernd Wellenzohn, Dieter Wiedenmayer, Zhaoming Xiong, Qiang Zhang
  • Publication number: 20110245262
    Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: August 20, 2007
    Publication date: October 6, 2011
    Inventors: Lijun Sun, Keizo Koya, Shoujun Chen, Zachary Demko, Zhi-Qiang Xia
  • Publication number: 20110213156
    Abstract: A compound represented by the following general formula (I): [wherein R1 and R2 represent an alkyl group, X represents —S—, —O— or —NH—, Y represents C or N, R3 represents hydrogen atom or a C1-10 alkyl group, Z represents —CO—N(R5)— (R5 represents hydrogen atom or a C1-6 alkyl group) or —C(R6)?C(R7)—CO—NH— (R6 and R7 represent hydrogen atom or a C1-6 alkyl group), Ar represents an aryldiyl group or a heteroaryldiyl group, and R4 represents —COOH, —OCH2—COOH, —CH2—COOH, or —CH2—CH2—COOH], which has a retinoid action and is useful as an active ingredient of a medicament.
    Type: Application
    Filed: August 14, 2008
    Publication date: September 1, 2011
    Applicant: RESEARCH FOUNDATION ITSUU LABORATORY
    Inventors: Hideaki Muratake, Masayuki Noguchi, Koichi Shudo
  • Publication number: 20110184190
    Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate.
    Type: Application
    Filed: January 26, 2011
    Publication date: July 28, 2011
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Atsushi Endo, Charles E. Chase, Francis G. Fang
  • Publication number: 20110172195
    Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.
    Type: Application
    Filed: March 15, 2011
    Publication date: July 14, 2011
    Applicant: ARIZONA BOARD OF REG. ON BEHALF OF THE UNIV. OF AZ
    Inventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
  • Publication number: 20110160192
    Abstract: Compounds of formula (I): Z?-CO-A-B—NH-Z (I) wherein: Z is H or an amino protecting group; Z? is OH, a protected or activated hydroxyl group or Cl; A is an optionally substituted C5-6 arylene group; and B is an optionally substituted C5-6 arylene group.
    Type: Application
    Filed: March 7, 2011
    Publication date: June 30, 2011
    Applicant: SPIROGEN LIMITED
    Inventors: Philip Wilson Howard, Geoffrey Wells
  • Publication number: 20110152466
    Abstract: The invention is based on the discovery that a remarkable improvement in the performance of maleimide thermosets can be achieved by incorporating amide-extended maleimides into an adhesive formulation. Amide-extended maleimides described herein can be used to toughen bismaleimide thermosetting materials without sacrificing any thermal stability. Amide-extended maleimides are readily prepared by reacting a bismaleimide with an appropriate amine via the well-known Michael addition reaction. Acylation of the resulting secondary amines provides the amide-extended maleimide. The acylating agent can also be used to introduce polymerizable functional groups into the backbones of these thermoset monomers. Amide-extended acrylate and methacrylate monomers can also be prepared.
    Type: Application
    Filed: August 13, 2009
    Publication date: June 23, 2011
    Applicant: DESIGNER MOLECULES, INC.
    Inventor: Stephen M. Dershem
  • Patent number: 7927780
    Abstract: A compound represented by formula (I); and a compound represented by formula (b1-1): wherein X represents —O—, —S—, —O—R3— or —S—R4—, wherein each of R3 and R4 independently represents an alkylene group of 1 to 5 carbon atoms; R2 represents an alkyl group of 1 to 6 carbon atoms, an alkoxy group of 1 to 6 carbon atoms, a halogenated alkyl group of 1 to 6 carbon atoms, a halogen atom, a hydroxyalkyl group of 1 to 6 carbon atoms, a hydroxyl group or a cyano group; a represents an integer of 0 to 2; Q1 represents an alkylene group of 1 to 12 carbon atoms or a single bond; Y1 represents an alkylene group of 1 to 4 carbon atoms or a fluorinated alkylene group; M+ represents an alkali metal ion; and A+ represents an organic cation.
    Type: Grant
    Filed: September 10, 2008
    Date of Patent: April 19, 2011
    Assignee: Tokyo Ohka Kogyo Co., Ltd.
    Inventors: Akiya Kawaue, Takeshi Iwai, Hideo Hada, Shinichi Hidesaka, Tsuyoshi Kurosawa, Natsuko Maruyama, Kensuke Matsuzawa, Takehiro Seshimo, Hiroaki Shimizu, Tsuyoshi Nakamura