The Hetero Ring Contains Seven Members Including Nitrogen And Carbon Patents (Class 540/484)
Chalcogen double bonded directly to a ring carbon adjacent to the ring nitrogen (e.g., caprolactam, etc.) (Class 540/485)
Heavy metal or boron containing (Class 540/541)
Phosphorus attached directly or indirectly to the hetero ring by nonionic bonding (Class 540/542)
Spiro (Class 540/543)
The hetero ring contains chalcogen (Class 540/544)
The hetero ring contains plural nitrogens (e.g., 1,3-diazepines, etc.) (Class 540/553)
Polycyclo ring system which contains the hetero ring as one of the cyclos (Class 540/576)
Additional hetero ring attached directly or indirectly to the hetero ring by nonionic bonding (Class 540/596)
Chalcogen attached directly to the hetero ring by nonionic bonding (Class 540/604)
Nitrogen attached directly to the hetero ring by nonionic bonding (Class 540/605)
Having -c(=x)-, wherein x is chalcogen, bonded directly to nitrogen of the hetero ring (Class 540/607)
Chalcogen or nitrogen attached indirectly to the hetero ring by acyclic nonionic bonding (Class 540/609)
Benzene ring bonded directly to the hetero ring (Class 540/611)
The hetero ring is unsubstituted or alkyl substituted only (Class 540/612)
  • Fluorinated olefins as working fluids and methods of using same
    Patent number: 10557069
    Abstract: A working fluid that includes a fluorinated olefin compound represented by the following general formula (I):
    Type: Grant
    Filed: March 4, 2019
    Date of Patent: February 11, 2020
    Assignee: 3M Innovative Properties Company
    Inventors: Michael J. Bulinski, Michael G. Costello, John G. Owens, Michael J. Rice
  • Compound useful for altering the levels of bile acids for the treatment of diabetes and cardiometabolc disease
    Patent number: 10414774
    Abstract: Described herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as Cyp8b1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for diabetes and cardiovascular disease.
    Type: Grant
    Filed: August 10, 2017
    Date of Patent: September 17, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Kevin D. Dykstra, Alan Hruza, Derun Li, Hong Liu, Haiqun Tang, Brandon M. Taoka, Andreas Verras, Shawn P. Walsh, Wen-Lian Wu
  • Compounds useful for altering the levels of bile acids for the treatment of diabetes and cardiometabolic disease
    Patent number: 10414775
    Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as Cyp8b1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for diabetes and cardiovascular disease.
    Type: Grant
    Filed: August 10, 2017
    Date of Patent: September 17, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John P. Caldwell, Mary Ann Caplen, Jared N. Cumming, Kevin D. Dykstra, Alan Hruza, Claire Lankin, Derun Li, Hong Liu, Amy McCracken, Brian McKittrick, Ashwin Rao, Jayaram Tagat, Haiqun Tang, Brandon M. Taoka, Andreas Verras, Shawn P. Walsh, Wen-Lian Wu, Tianyuan Zhang
  • Method for producing epsilon-caprolactam
    Patent number: 10196352
    Abstract: A method for selective production of ?-caprolactam, wherein a substance inducible from a biomass resource is used as a material; the reaction process is short; ammonium sulfate is not produced as a by-product; and production of by-products is suppressed; is disclosed. The method for producing ?-caprolactam comprises the step of reacting a particular compound inducible from a biomass resource, such as ?-hydromuconic acid, 3-hydroxyadipic acid, or 3-hydroxyadipic acid-3,6-lactone, or a salt thereof with hydrogen or ammonia.
    Type: Grant
    Filed: October 27, 2015
    Date of Patent: February 5, 2019
    Assignee: TORAY INDUSTRIES, INC.
    Inventors: Masateru Ito, Daijiro Tsukamoto, Kenji Kawamura, Kohei Yamashita, Masato Akahira, Katsushige Yamada, Koji Yamauchi
  • Homopiperazine-based catalysts for neutralization of organophosphorus-based compounds
    Patent number: 10112912
    Abstract: Novel compositions of matter based on homopiperazine precursor materials and forming a homopiperazine-based ligand are disclosed, along with suitable techniques and materials for the synthesis and utilization thereof. In particular various synthetic schemes and techniques for applying the disclosed compositions of matter as a decontaminating agent. The decontaminating agents include homopiperazine-based ligand-metal complexes that are particularly effective at neutralizing toxicity of nerve agents, pesticides, and other toxic organophosphorus-based compounds. In preferred approaches, the homopiperazine-based ligand-metal complexes act as catalysts to facilitate substitution of a leaving group of the organophosphorus-based compound with a functional group that does not permit the organophosphorus-based compound to inactivate acetylcholinesterase upon introduction of the organophosphorus-based compound to a living organism such as insects and mammals.
    Type: Grant
    Filed: March 2, 2016
    Date of Patent: October 30, 2018
    Assignee: Lawrence Livermore National Security, LLC
    Inventors: Carlos Valdez, Edmond Y. Lau, Brian P. Mayer
  • Quinoline sulfonyl derivatives and uses thereof
    Patent number: 9975852
    Abstract: The present disclosure relates to quinoline sulfonyl compounds, compositions comprising these compounds and their use, in particular for the treatment of cancer.
    Type: Grant
    Filed: February 18, 2014
    Date of Patent: May 22, 2018
    Assignee: Health Sciences North Research Institute
    Inventors: Hoyun Lee, Viswas Raja Solomon, Sheetal Pundir
  • Hydrogenation reactor and process
    Patent number: 9902668
    Abstract: A reactor and process for removing unsaturated alkynes and diolefinic impurities from olefins and oxygenates.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: February 27, 2018
    Assignee: SAUDI BASIC INDUSTRIES CORPORATION
    Inventors: Zeeshan Nawaz, Faisal Baksh
  • Fused heterocyclic compounds as ion channel modulators
    Patent number: 9676760
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: May 11, 2016
    Date of Patent: June 13, 2017
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Michael Graupe, Juan Guerrero, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Chandrasekar Venkataramani, Jeff Zablocki
  • Mononuclear iron complex and organic synthesis reaction using same
    Patent number: 9421532
    Abstract: Provided is a mononuclear iron complex that comprises an iron-silicon bond that is represented by formula (1) and that exhibits excellent catalyst activity in each of a hydrosilylation reaction, a hydrogenation reaction, and reduction of a carbonyl compound. In formula (1), R1-R6 either independently represent an alkyl group, an aryl group, an aralkyl group or the like that may be substituted with a hydrogen atom or X, or represent a crosslinking substituent in which at least one pair comprising one of R1-R3 and one of R4-R6 is combined. X represents a halogen atom, an organoxy group, or the like. L represents a two-electron ligand other than CO. When a plurality of L are present, the plurality of L may be the same as or different from each other. When two L are present, the two L may be bonded to each other. n and m independently represent an integer of 1 to 3 with the stipulation that n+m equals 3 or 4.
    Type: Grant
    Filed: February 26, 2014
    Date of Patent: August 23, 2016
    Assignees: KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION, SHIN-ETSU CHEMICAL CO., LTD.
    Inventors: Hideo Nagashima, Yusuke Sunada, Hironori Tsutsumi, Toru Hashimoto, Koji Sakuta
  • Precursors for CVD Silicon Carbo-Nitride Films
    Publication number: 20150147893
    Abstract: Classes of liquid aminosilanes have been found which allow for the production of silicon carbo-nitride films of the general formula SixCyNz. These aminosilanes, in contrast, to some of the precursors employed heretofore, are liquid at room temperature and pressure allowing for convenient handling. In addition, the invention relates to a process for producing such films. The classes of compounds are generally represented by the formulas: and mixtures thereof, wherein R and R1 in the formulas represent aliphatic groups typically having from 2 to about 10 carbon atoms, e.g., alkyl, cycloalkyl with R and R1 in formula A also being combinable into a cyclic group, and R2 representing a single bond, (CH2)n, a ring, or SiH2.
    Type: Application
    Filed: December 16, 2014
    Publication date: May 28, 2015
    Applicant: AIR PRODUCTS AND CHEMICALS, INC.
    Inventors: Manchao Xiao, Arthur Kenneth Hochberg
  • Substituted pyridyl amide compounds as modulators of the histamine Hreceptor
    Patent number: 8940731
    Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: January 27, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: John M. Keith, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
  • Substituted bicyclic alkoxy pyrazole analogs as allosteric modulators of mGluR5 receptors
    Patent number: 8901125
    Abstract: In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: June 19, 2013
    Date of Patent: December 2, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Miguel Angel Pena-Piñón, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil
  • Highly selective sigma receptor ligands
    Patent number: 8809381
    Abstract: A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula I in which R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle such as, for example, radicals of optionally substituted piperidines, optionally substituted piperazines, optionally substituted tetrahydropyridines, optionally substituted azepanes, tertiary amines (cyclic or acyclic), isoindoline-1,3-dione, or optionally substituted tetrahydroisoquinolones (aromatically substituted): R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.
    Type: Grant
    Filed: August 18, 2008
    Date of Patent: August 19, 2014
    Assignees: The University of Mississippi, L'Universite Catholique de Louvain
    Inventors: Christopher R. McCurdy, Christophe Mesangeau, Sanju Narayanan, Rae Reiko Matsumoto, Jacques Henri Poupaert
  • Carboxylic acid amides, the preparation thereof and their use as medicaments
    Patent number: 8791103
    Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: July 29, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Kai Gerlach, Roland Pfau, Norbert Hauel, Iris Kauffmann-Hefner, Georg Dahmann, Herbert Nar, Sandra Handschuh, Wolfgang Wienen, Annette Schuler-Metz
  • Fused heterocyclic compounds as ion channel modulators
    Patent number: 8697863
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: April 15, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Elfatih Elzein, Dmitry Koltun, Xiaofen Li, Jeff Zablocki, Chandrasekar Venkataramani
  • Ionic liquids
    Patent number: 8686134
    Abstract: The invention relates to an ionic liquid composition and a method for preparing the ionic liquid. The ionic liquid comprises a cation containing the Formula I, as herein disclosed, and wherein: n is 2, R1 is selected from the group consisting of: H, C1-C12 alkyl, aryl or together with R2 may form a heterocyclic ring, and R2 is selected from the group consisting of: H, C1-C12 alkyl, aryl or together with R1 may form a heterocyclic ring, and R3 is selected from the group consisting of hydrogen and C1-C12 alkyl, and wherein R1 and R2 are not simultaneously selected from hydrogen.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: April 1, 2014
    Assignee: Invista North America S.A R.L.
    Inventors: Stewart Forsyth, Kenneth Richard Seddon, Keith Whiston
  • Bradykinin 1 receptor modulating compounds
    Patent number: 8680159
    Abstract: Substituted benzamide compounds corresponding to formula (I) in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions comprising such compounds, and a method of using such compounds to treat pain and other conditions mediated at least in part via the bradykinin 1 receptor.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: March 25, 2014
    Assignee: Gruenenthal GmbH
    Inventors: Melanie Reich, Stefan Schunk, Ruth Jostock, Jean De Vry, Christa Kneip, Tieno Germann, Michael Engels
  • PROCESS FOR PREPARING AMINES BY HOMOGENEOUSLY CATALYZED ALCOHOL AMINATION IN THE PRESENCE OF A COMPLEX CATALYST COMPRISING IRIDIUM AND AN AMINO ACID
    Publication number: 20140046054
    Abstract: The invention relates to a process for preparing amines (A) by alcohol amination of alcohols (Al) by means of an aminating agent (Am) with elimination of water, wherein the alcohol amination is carried out in the presence of a complex catalyst comprising iridium and an amino acid.
    Type: Application
    Filed: August 7, 2013
    Publication date: February 13, 2014
    Applicant: BASF SE
    Inventors: Alexander WETZEL, Michael Limbach, Marion Brinks, Mathias Schelwies
  • Compounds having a monogalactosyldiacylglycerol synthase inhibitory activity as herbicide or algaecide, herbicide and algaecide compositions
    Patent number: 8637496
    Abstract: The invention relates to the use of compounds having a monogalactosyldiacylglycerol (MGDG) synthase inhibitory activity as herbicide or algaecide, and to herbicide and algaecide compositions containing at least one of these compounds.
    Type: Grant
    Filed: June 2, 2008
    Date of Patent: January 28, 2014
    Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche Scientifique
    Inventors: Anne-Laure Bonneau, Cyrille Botte, Michael Deligny, Nadia Saidani, Hélène Hardre, Bernard Rousseau, Roman Lopez, Eric Marechal
  • (4-haloalkyl-3-thiobenzoyl)cyclohexanediones and use thereof as herbicides
    Patent number: 8603947
    Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: December 10, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
  • Fused heterocyclic compounds as ion channel modulators
    Patent number: 8586732
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: November 19, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • 3-aryl-substituted quinazolones, and uses thereof
    Patent number: 8575143
    Abstract: Compounds represented by Structural Formula (I): are useful, for example, in the effective killing or reducing the rate of proliferation of cancer cells, such as in patients suffering from cancer. In addition to the compounds themselves, the invention provides pharmaceutical compositions of the compounds and method of treatment using the compounds.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: November 5, 2013
    Assignee: Prolexys Pharmaceuticals, Inc.
    Inventors: Longwu Qi, Raj Gopal Venkat, Michael Pierce, Paul B. Robbins, Sudhir R. Sahasrabudhe, Robert Selliah
  • (4-trifluoromethyl-3-thiobenzoyl)cyclohexanediones and use thereof as herbicides
    Patent number: 8563779
    Abstract: A description is given of (4-trifluoromethyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 19, 2011
    Date of Patent: October 22, 2013
    Assignee: Bayer CropScience AG
    Inventors: Hartmut Ahrens, Andreas Van Almsick, Elmar Gatzweiler, Dieter Feucht, Isolde Haeuser-Hahn, Stefan Lehr, Christopher Hugh Rosinger
  • Method for separating amide from amino acid ionic liquid
    Patent number: 8552180
    Abstract: The present invention provides a method for separating an amide from an amino acid ionic liquid. The method includes the step of providing a polar solvent and an extracting agent to the amino acid ionic liquid, so as to separate the amide from the amino acid ionic liquid. In the method of the present invention, there is no need to add ammonium for neutralization, such that no byproduct, ammonium sulfate, is formed. In addition, after the amide is separated from the amino acid ionic liquid, the amino acid ionic liquid can be recycled.
    Type: Grant
    Filed: December 14, 2009
    Date of Patent: October 8, 2013
    Assignee: China Petrochemical Development Corporation
    Inventors: Cheng-Fa Hsieh, Chien-Chuan Shih, Chi-Yuan Chen
  • Precursors for CVD Silicon Carbo-Nitride Films
    Publication number: 20130244448
    Abstract: Classes of liquid aminosilanes have been found which allow for the production of silicon carbo-nitride films of the general formula SixCyNz. These aminosilanes, in contrast, to some of the precursors employed heretofore, are liquid at room temperature and pressure allowing for convenient handling. In addition, the invention relates to a process for producing such films. The classes of compounds are generally represented by the formulas: and mixtures thereof, wherein R and R1 in the formulas represent aliphatic groups typically having from 2 to about 10 carbon atoms, e.g., alkyl, cycloalkyl with R and R1 in formula A also being combinable into a cyclic group, and R2 representing a single bond, (CH2)n, a ring, or SiH2.
    Type: Application
    Filed: September 13, 2012
    Publication date: September 19, 2013
    Applicant: AIR PRODUCTS AND CHEMICALS, INC.
    Inventors: Manchao Xiao, Arthur Kenneth Hochberg
  • Method for preparing amide
    Patent number: 8524895
    Abstract: The present invention provides a method for preparing amides, in which an amino acid ionic liquid is used as both a reaction medium and a catalyst to catalyze Beckman rearrangement of a ketoxime, so as to produce an amide. In the method, the rearrangement is conducted by catalyzing a ketoxime with an amino acid ionic liquid having the asymmetric property at a moderate reaction temperature during a short reaction time, so as to produce an amide without adding other catalysts such as concentrate sulfuric acid. The method has advantages such as avoiding corrosion in equipments with pipelines, the high conversion rate of ketoximes and the high selectivity of amides.
    Type: Grant
    Filed: July 13, 2009
    Date of Patent: September 3, 2013
    Assignee: China Petrochemical Development Corporation
    Inventors: Tung-Han Tsai, Pin-To Yao, Cheng-Fa Hsieh
  • Extended release formulation of nevirapine
    Patent number: 8460704
    Abstract: The invention relates to an extended release pharmaceutical composition comprising nevirapine.
    Type: Grant
    Filed: June 4, 2008
    Date of Patent: June 11, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Michael L. Cappola, Svetlana Sienkiewicz, Glenn Charles Snow, Feng-Jing Chen
  • BIARYL AMIDE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
    Publication number: 20130116227
    Abstract: Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R1 is a substitutable aminosulfonyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; R4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R5a, R5b and R5c are each independently hydrogen atoms, etc.; R6 is a halogen atom, a cyano group, etc.; R7 and R8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.
    Type: Application
    Filed: July 12, 2011
    Publication date: May 9, 2013
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Seiji Katayama, Seiji Hori, Futoshi Hasegawa, Kuniko Suzuki
  • Chromen-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors
    Patent number: 8410271
    Abstract: This invention relates to chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: April 2, 2013
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Jorgen Scheel-Kruger, Elsebet Ostergaard Nielsen
  • Substituted aminothiazolone indazoles as estrogen related receptor-alpha modulators
    Patent number: 8399681
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: March 19, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
  • Modulators of aldehyde dehydrogenase and methods of use thereof
    Patent number: 8389522
    Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.
    Type: Grant
    Filed: October 19, 2009
    Date of Patent: March 5, 2013
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
  • Method and catalyst composition for preparing amide
    Patent number: 8367865
    Abstract: The present invention provides a catalyst composition for preparing an amide, including an amino acid ionic liquid having a cation of formula (I) and an anion selected from the group consisting of an inorganic acid group, an organic acid group and a combination thereof, wherein the numbers of the anion and the cation are such that the amino acid ionic liquid is electroneutral; and a Bronsted acid. The present invention also provides a method for preparing an amide in the presence of the catalyst composition, and the method has advantages such as decreasing viscosity of ionic liquid, and increasing conversion rate of ketoximes and selectivity of amides.
    Type: Grant
    Filed: November 30, 2009
    Date of Patent: February 5, 2013
    Assignee: China Petrichemical Development Corporation
    Inventors: Tung-Han Tsai, Cheng-Fa Hsieh, Chi-Yuan Chen
  • Tricyclic derivatives as inhibitors of poly(ADP-ribose) polymerase (PARP)
    Patent number: 8362030
    Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.
    Type: Grant
    Filed: March 13, 2009
    Date of Patent: January 29, 2013
    Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti S.R.L.
    Inventors: Raffaele Ingenito, Philip Jones, Laura Llauger Bufi, Jesus Maria Ontoria Ontoria, Rita Scarpelli
  • ORGANIC COMPOUNDS
    Publication number: 20130012485
    Abstract: Compounds of the formula (I) are provided: wherein V, W, X, Y, Z, R3, R4, R5, R6, R7 and m are as defined in the specification; and pharmaceutically acceptable salts and prodrugs thereof. The compounds may be useful in the treatment or prevention of various diseases and conditions in which dipeptidylpeptidase-IV (DPP-IV) is implicated.
    Type: Application
    Filed: December 20, 2007
    Publication date: January 10, 2013
    Inventors: Daniel Kaspar Bäschlin, Richard Sedrani, Stefanie Flohr, Kenji Namoto, Nils Ostermann, Finton Sirockin, François Gessier, Garry Fenton, Mandy Christine Beswick, David Edward Clark, Bohdan Waszkowycz
  • Substituted aminothiazolone indazoles as estrogen related receptor-alpha modulators
    Patent number: 8263781
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: September 11, 2012
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
  • Structural mimetics of proline-rich peptides and the pharmaceutical use thereof
    Patent number: 8242105
    Abstract: The invention relates to compounds of general formula (I), which can be used particularly as structural mimetics of proline-rich peptides and are therefore capable of binding PRM binding domains (proline-rich motif binding domains) of proteins. The invention also relates to the use of said compounds as pharmaceutical active agents and the use of these pharmaceutical active agents for treating bacterial diseases, neurodegenerative diseases and tumors.
    Type: Grant
    Filed: September 25, 2007
    Date of Patent: August 14, 2012
    Assignee: Forschungsverbund Berlin E.V.
    Inventors: Ronald Kuehne, Hartmut Oschkinat, Christoph Brockmann, Hans-Guenther Schmalz, Jan Zaminer
  • IONIC LIQUIDS
    Publication number: 20120190844
    Abstract: The invention relates to an ionic liquid composition and a method for preparing the ionic liquid. The ionic liquid comprises a cation containing the Formula I, as herein disclosed, and wherein: n is 2, R1 is selected from the group consisting of: H, C1-C12 alkyl, aryl or together with R2 may form a heterocyclic ring, and R2 is selected from the group consisting of: H, C1-C12 alkyl, aryl or together with R1 may form a heterocyclic ring, and R3 is selected from the group consisting of hydrogen and C1-C12 alkyl, and wherein R1 and R2 are not simultaneously selected from hydrogen.
    Type: Application
    Filed: July 20, 2011
    Publication date: July 26, 2012
    Applicant: INVISTA North America S.a r.l.
    Inventors: Stewart Forsyth, Kenneth Richard Seddon, Keith Whiston
  • GLYCINE COMPOUND
    Publication number: 20120184520
    Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that a compound of the present invention or a salt thereof exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. The present invention further relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound of the present invention or a salt thereof, and an excipient.
    Type: Application
    Filed: September 15, 2010
    Publication date: July 19, 2012
    Applicant: Astellas Pharma Inc.
    Inventors: Kousei Yoshihara, Daisuke Suzuki, Susumu Yamaki, Yuji Koga, Norio Seki, Jiro Fujiyasu, Masahiro Neya
  • Heat shock protein 90 inhibitors
    Patent number: 8188306
    Abstract: Novel compounds useful for inhibiting the 90kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.
    Type: Grant
    Filed: September 30, 2009
    Date of Patent: May 29, 2012
    Assignee: University of Kansas
    Inventors: Brian S. J. Blagg, Gang Shen
  • Chromen-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors
    Patent number: 8153797
    Abstract: This invention relates to novel chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: February 13, 2007
    Date of Patent: April 10, 2012
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, John Paul Redrobe, Elsebet Østergaard Nielsen
  • NOVEL SUBSTITUTED INDANES, METHOD FOR THE PRODUCTION THEREOF, AND USE THEREOF AS DRUGS
    Publication number: 20120022039
    Abstract: The invention relates to substituted indanes and derivatives thereof, to physiologically acceptable salts and physiologically functional derivatives thereof, to the production thereof, to drugs containing at least one substituted indane according to the invention or derivative thereof, and to the use of the substituted indanes according to the invention and to derivatives thereof as MCH antagonists.
    Type: Application
    Filed: February 12, 2010
    Publication date: January 26, 2012
    Applicant: SANOFI
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
  • Ionic liquids
    Patent number: 8088917
    Abstract: The invention relates to an ionic liquid composition and a method for preparing the ionic liquid. The ionic liquid comprises a cation containing the Formula I, as herein disclosed, and wherein: n is 2, R1 is selected from the group consisting of: H, C1-C12 alkyl, aryl or together with R2 may form a heterocyclic ring, and R2 is selected from the group consisting of: H, C1-C12 alkyl, aryl or together with R1 may form a heterocyclic ring, and R3 is selected from the group consisting of hydrogen and C1-C12 alkyl, and wherein R1 and R2 are not simultaneously selected from hydrogen.
    Type: Grant
    Filed: May 29, 2008
    Date of Patent: January 3, 2012
    Assignee: Invista North America S.A R.L.
    Inventors: Stewart Forsyth, Kenneth R. Seddon, Keith Whiston, Sudhir Aki
  • Imidazole compounds
    Patent number: 8017600
    Abstract: Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.
    Type: Grant
    Filed: June 9, 2010
    Date of Patent: September 13, 2011
    Assignee: Janssen Pharmaceutica NV
    Inventors: Daniel J. Buzard, James P. Edwards, David E. Kindrachuk, Jennifer D. Venable
  • N-substituted-heterocycloalkyloxybenzamide compounds and methods of use
    Patent number: 8012955
    Abstract: The present invention provides N-substituted-heterocycloalkyloxybenzamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment of the invention is a compound having the structure in which R1, R2, R3, R4, T, n, w and x are as described herein. In certain embodiments of the invention, a compound of the present invention activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: September 6, 2011
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Jiaxin Yu, Hui Hong, Sambaiah Thota, Xiang Xu, Ihab S. Darwish
  • Pyrimidin-2-one compounds and their use as dopamine Dreceptor ligands
    Patent number: 8008488
    Abstract: The invention relates to pyrimidin 2-one compounds of general formula (I), in addition to the derivatives and tautomers of (I) and the physiologically acceptable salts of said compounds. In said formula, A represents linear or branched C3-C6 alkene, which can have a double bond or triple bond and/or a group Z, which is not adjacent to the nitrogen atom of the pyrimidinone ring and is selected from O, S, C(O), NR3, C(O)NR3, NR3C(O), OC(O) and C(O)O; B represents a group of the formula (II), in which X stands for CH2 or N and Y stands for CH2 or CH2CH2, or X—Y can also jointly represent C?CH, C?CH—CH2 or CH—CH?CH; R1 and R2 are defined as cited in the description and the claims; and Ar represents an optionally substituted aromatic group. The invention also relates to a pharmaceutical agent, containing at least one compound (I) and the tautomers, derivatives and/or acid addition salts of said compound, optionally together with physiologically acceptable carriers and/or auxiliary agents.
    Type: Grant
    Filed: March 12, 2004
    Date of Patent: August 30, 2011
    Assignee: Abbott GmbH & Co. KG
    Inventors: Hervé Geneste, Andreas Kling, Wilfried Braje, Andreas Haupt, Liliane Unger
  • Bicyclic heterocycles, drugs containing said compounds, use thereof, and method for production thereof
    Patent number: 7998949
    Abstract: The present invention relates to bicyclic heterocycles of general formula wherein Ra, Rb and Rc are defined as in claim 1, their tautomers, their stereoisomers, their mixtures and their salts, in particular their physiologically acceptable salts with inorganic or organic acids and bases, which have valuable pharmacological properties, in particular an inhibitory action on the signal transduction mediated by tyrosine kinases, their use for the treatment of illnesses, in particular of tumoral diseases and of benign prostatic hyperplasia (BPH), of diseases of the lung and of the airways, and the preparation thereof.
    Type: Grant
    Filed: January 30, 2008
    Date of Patent: August 16, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Birgit Jung, Ralf Lotz, Markus Ostermeier
  • Precursors for CVD Silicon Carbo-Nitride Films
    Publication number: 20110165346
    Abstract: Classes of liquid aminosilanes have been found which allow for the production of silicon carbo-nitride films of the general formula SixCyNz. These aminosilanes, in contrast, to some of the precursors employed heretofore, are liquid at room temperature and pressure allowing for convenient handling. In addition, the invention relates to a process for producing such films. The classes of compounds are generally represented by the formulas: and mixtures thereof, wherein R and R1 in the formulas represent aliphatic groups typically having from 2 to about 10 carbon atoms, e.g., alkyl, cycloalkyl with R and R1 in formula A also being combinable into a cyclic group, and R2 representing a single bond, (CH2)n, a ring, or SiH2.
    Type: Application
    Filed: March 18, 2011
    Publication date: July 7, 2011
    Applicant: AIR PRODUCTS AND CHEMICALS, INC.
    Inventors: Manchao Xiao, Arthur Kenneth Hochberg
  • Trifluoromethylbenzamide derivatives and therapeutic uses thereof
    Patent number: 7947675
    Abstract: Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: February 16, 2006
    Date of Patent: May 24, 2011
    Assignee: Merck Patent GmbH
    Inventors: Bruno Roux, Isabelle Berard
  • Spiroindoline modulators of muscarinic receptors
    Patent number: 7879834
    Abstract: The present invention relates to spiroindoline modulators of muscarinic receptors. The present invention also provides compositions comprising such spiroindoline modulators, and methods therewith for treating muscarinic receptor mediated diseases.
    Type: Grant
    Filed: August 19, 2005
    Date of Patent: February 1, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Lewis R. Makings, Miguel Garcia-Guzman Blanco, Dennis R. Hurley, Ioana Drutu, Gabriel Raffai, Daniele J. Bergeron, Akiko Nakatani, Andreas P. Termin, Alina Silina
  • N-arylsulfonyl-3-substituted indoles having serotonin receptor affinity, process for their preparation and pharmaceutical composition containing them
    Patent number: 7875605
    Abstract: N-arylsulfonyl-3-substituted indole compounds, derivatives, analogs, tautomeric forms, stereoisomers, geometric forms, N-oxides, polymorphs and pharmaceutically acceptable salts.
    Type: Grant
    Filed: June 5, 2003
    Date of Patent: January 25, 2011
    Assignee: Suven Life Sciences Limited
    Inventors: Venkata Satya Nirogi Ramakrishna, Vikas Shreekrishna Shirsath, Rama Sastri Kambhampati, Venkata Satya Veerabhadra Vadlamudi Rao, Venkateswarlu Jasti