Piperazines (i.e., Fully Hydrogenated 1,4-diazines) Patents (Class 544/358)
  • Publication number: 20130310560
    Abstract: Processes for preparing an amine are described which comprise reacting a primary or secondary alcohol, aldehyde and/or ketone with hydrogen and a nitrogen compound selected from the group of ammonia, primary and secondary amines, in the presence of a zirconium dioxide-, copper- and nickel-containing catalyst. The catalytically active composition of the catalyst, before its reduction with hydrogen, comprises oxygen compounds of zirconium, of copper, of nickel, in the range from 1.0 to 5.0% by weight of oxygen compounds of cobalt, calculated as CoO, and in the range from 0.2 to 5.0% by weight of oxygen compounds of sulfur, of phosphorus, of gallium, of lead and/or of antimony, calculated in each case as H2SO4, H3PO4, Ga203, PbO and Sb203 respectively.
    Type: Application
    Filed: November 8, 2012
    Publication date: November 21, 2013
    Applicant: BASF SE
    Inventors: PETR KUBANEK, WOLFGANG MÄRGELEIN, EKKEHARD SCHWAB, JOHANN-PETER MELDER, MANFRED JULIUS
  • Patent number: 8569071
    Abstract: The present teachings provide methods for analyzing one or more amine-containing compounds in one or more samples using isobaric labels and parent-daughter ion transition monitoring (PDITM). In various embodiments, the methods comprise the steps of: (a) labeling one or more amine-containing compounds with different isobaric tags from a set of isobaric tags, each isobaric tag comprising a reporter ion portion; (b) combining at least a portion of each of the isobarically labeled amine-containing compounds to produce a combined sample; (c) subjecting at least a portion of the combined sample to PDITM; (d) measuring the ion signal of one or more of the transmitted reporter ions; and (e) determining the concentration of one or more of the isobarically labeled amine-containing compounds based at least on a comparison of the measured ion signal of the corresponding reporter ion to one or more measured ion signals of a standard compound.
    Type: Grant
    Filed: September 8, 2009
    Date of Patent: October 29, 2013
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Subodh B. Nimkar, Subhasish Purkayastha, Darryl Pappin, Scott Daniels
  • Patent number: 8569304
    Abstract: In some embodiments, this invention pertains to active esters of N-substituted piperazine acetic acid, including isotopically enriched versions thereof. In some embodiments, this invention pertains to methods for the preparation of active esters of N-substituted piperazine acetic acid, including isotopically enriched versions thereof.
    Type: Grant
    Filed: March 5, 2009
    Date of Patent: October 29, 2013
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Subhakar Dey, Darryl J. C. Pappin, Subhasish Purkayastha, Sasi Pillai, James M. Coull
  • Patent number: 8563582
    Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.
    Type: Grant
    Filed: April 29, 2009
    Date of Patent: October 22, 2013
    Assignee: Incyte Corporation
    Inventors: Chu-Biao Xue, Changsheng Zheng, Hao Feng, Michael Xia, Joseph Glenn, Ganfeng Cao, Brian W. Metcalf
  • Patent number: 8536178
    Abstract: Disclosed herein is a method for treating diseases associated with beta amyloid accumulation, including administering to a patient a therapeutically effective amount of morpholine or piperazine based compounds including a sulfuric or carboxylic acid structure represented by the following chemical formula 1 or a pharmaceutically acceptable salt thereof: (wherein Z, R1 and R2 are as defined in the specification).
    Type: Grant
    Filed: December 6, 2010
    Date of Patent: September 17, 2013
    Assignee: Korea Institute of Science and Technology
    Inventors: Dong Jin Kim, YoungSoo Kim, Hye Yun Kim
  • Patent number: 8530475
    Abstract: The present invention is directed to bridged aryl piperazine derivatives, pharmaceutical compositions containing them and their use in the treatment of depression and related disorders. The compounds of the present invention are serotonin transport inhibitors and/or modulators of 5HT1A.
    Type: Grant
    Filed: May 18, 2007
    Date of Patent: September 10, 2013
    Inventors: Christopher J. Creighton, Tina Morgan Ross, Allen B. Reitz, Cheryl P. Kordik, Steven Paget, Gregor J. MacDonald
  • Publication number: 20130231476
    Abstract: A transamination process is described to prepare polyamine product mixtures from reactants comprising mixed nitrogen-containing compounds with binary carbon spacing between nitrogen-containing groups (a binary component). A second nitrogen-containing component with a second carbon atom spacing between nitrogen-containing groups may also be employed. The molar ratio between the binary and second components can be adjusted to customize the product composition for desired end uses.
    Type: Application
    Filed: October 20, 2011
    Publication date: September 5, 2013
    Applicant: Dow Global Technologies LLC
    Inventor: Stephen W. King
  • Patent number: 8524716
    Abstract: The present invention relates to inhibitors of HCV replication of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein R1; R3; and R4 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.
    Type: Grant
    Filed: December 23, 2008
    Date of Patent: September 3, 2013
    Assignee: Janssen R&D Ireland
    Inventors: Pierre Jean-Marie Bernard Raboisson, Lili Hu, Sandrine Marie Helene Vendeville, Origène Nyanguile, Abdellah Tahri
  • Patent number: 8497369
    Abstract: The present invention relates to spirocyclic heterocycles of general formula (I) the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways, and the preparation thereof.
    Type: Grant
    Filed: February 5, 2009
    Date of Patent: July 30, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Birgit Jung, Ralf Lotz
  • Patent number: 8492163
    Abstract: This invention pertains to methods, mixtures, kits and compositions pertaining to analyte determination by mass spectrometry using labeling reagents that comprise a nucleophilic reactive group that reacts with a functional group of an analyte to produce a labeled analyte. The labeling reagents can be used as isobaric sets, mass differential labeling sets or in a combination of isobaric and mass differential labeling sets.
    Type: Grant
    Filed: January 31, 2011
    Date of Patent: July 23, 2013
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Subhasish Purkayastha, Subhakar Dey, Scott B. Daniels
  • Patent number: 8487135
    Abstract: A process for preparing an amine by reacting a primary or secondary alcohol, aldehyde and/or ketone with hydrogen and a nitrogen compound selected from the group of ammonia and primary and secondary amines, in the presence of a supported copper-, nickel- and cobalt-containing catalyst, wherein the catalytically active material of the catalyst, before the reduction thereof with hydrogen, comprises oxygen compounds of aluminum, of copper, of nickel and of cobalt, and in the range from 0.2 to 5.0% by weight of oxygen compounds of tin, calculated as SnO, and catalysts as defined above.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: July 16, 2013
    Assignee: BASF SE
    Inventors: Petr Kubanek, Wolfgang Mägerlein, Johann-Peter Melder, Thomas Heidemann
  • Patent number: 8476475
    Abstract: A premix is described for producing an absorption medium for removing acid gases from fluid streams. The premix comprises at least one alkanolamine, piperazine and water, the premix having a total amine content of more than 65% by weight, the molar ratio of water to piperazine in the premix being 1.6 to 4.8. The premix is characterized by a low solidification point. It is diluted with water and/or alkanolamine to give the ready-to-use absorption medium.
    Type: Grant
    Filed: May 18, 2007
    Date of Patent: July 2, 2013
    Assignee: BASF SE
    Inventor: Norbert Asprion
  • Patent number: 8470827
    Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.
    Type: Grant
    Filed: September 25, 2008
    Date of Patent: June 25, 2013
    Assignee: Incyte Corporation
    Inventors: Chu-Biao Xue, Changsheng Zheng, Hao Feng, Michael Xia, Joseph Glenn, Ganfeng Cao, Brian W. Metcalf
  • Patent number: 8461335
    Abstract: This invention provides novel compositions comprising substituted polyamines as acid gas scrubbing solutions and methods of using the compositions in an industrial system. The invention relates to the use of such polyamine compounds in industrial processes to remove acidic contaminants from natural and industrial fluid streams, such as natural gas, combustion gas, natural gas, synthesis gas, biogas, and other industrial fluid streams. The compositions and methods of the invention are useful for removal, absorption, or sequestration of acidic contaminants and sulfide contaminants including CO2, H2S, RSH, CS2, COS, and SO2.
    Type: Grant
    Filed: June 30, 2009
    Date of Patent: June 11, 2013
    Assignee: Nalco Company
    Inventors: Alan M. Blair, Keith N. Garside, William J. Andrews, Kailas B. Sawant
  • Patent number: 8436169
    Abstract: Process for preparing 1,4-bishydroxyethylpiperazine (BHEPIP) of the formula I wherein diethanolamine (DEOA) of the formula II is reacted in the liquid phase in a reactor at a temperature in the range from 130 to 300° C. in the presence of a copper-comprising, chromium-free heterogeneous catalyst.
    Type: Grant
    Filed: October 28, 2011
    Date of Patent: May 7, 2013
    Assignee: BASF SE
    Inventors: Christof Wilhelm Wigbers, Nina Challand, Johann-Peter Melder, Udo Rheude, Roman Dostalek
  • Patent number: 8420680
    Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein: each (L)k-Ar1 is a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NR1 or O and each R1 and R2 is independently H, alkyl, alkenyl or aralkyl or R1 and R2 taken together form a 5-8 membered ring; R3?R6 are selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO2, CH2, NH, N(alkyl), or NHC(?O); and Z is OH, NR6R7, NR8SO2(alkyl), NR8C(O)NR6R7, NR8C(O)O(alkyl), NR8-dihydrothiazole, or NR8-dihydroimidazole or wherein Z can fuse with Ar2 to form selected heterocycles.
    Type: Grant
    Filed: June 30, 2008
    Date of Patent: April 16, 2013
    Assignees: Emory University, NeurOp, Inc.
    Inventors: Dennis C. Liotta, James P. Snyder, Stephen F. Traynelis, Lawrence Wilson, Cara Mosley, Raymond J. Dingledine, Yesim Altas Tahirovic, Scott J. Myers
  • Patent number: 8410108
    Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Grant
    Filed: May 3, 2010
    Date of Patent: April 2, 2013
    Assignee: Cytokinetics, Inc.
    Inventors: Bradley P. Morgan, Erica A. Kraynack, Pu-Ping Lu, Alex Muci, David J. Morgans, Jr.
  • Patent number: 8404689
    Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.
    Type: Grant
    Filed: March 2, 2011
    Date of Patent: March 26, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Stephen T. Wrobleski, Jagabandhu Das, T. G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
  • Patent number: 8404900
    Abstract: An absorbent for separating acidic gases is disclosed. The absorbent or an absorbent composition for separating acidic gases has more than 3 kinds of compounds along with Chemical Formula 1 and 2, and has ability of rapid carbon dioxide elimination, excellent absorption ability, and less energy consumption for regenerating an absorbent due to easy desorption of carbon dioxide.
    Type: Grant
    Filed: October 27, 2009
    Date of Patent: March 26, 2013
    Assignee: Korea Electric Power Corporation
    Inventors: Jun-Han Kim, Jae-Goo Shim, Kyung-Ryong Jang, Ji-Hyun Lee
  • Patent number: 8383860
    Abstract: The present invention reacts ethylenediamine with one or more additional ethyleneamines in the presence of a transamination catalyst to provide a different, preferably more desirable product mix of one or more ethyleneamines.
    Type: Grant
    Filed: October 6, 2009
    Date of Patent: February 26, 2013
    Assignee: Union Carbide Chemicals & Plastics Technology LLC
    Inventors: Ronald G. Cook, Stephen W. King, David M. Petraitis, Thomas Z. Smak
  • Patent number: 8377869
    Abstract: A method for preventing or reducing adverse effects such as profuse sweating, nausea and vomiting, which normally are associated with subcutaneous and intravenous administration of glucagon-like peptide 1 (GLP-1) therapy is provided. In particular, the method comprises the rapid administration of a GLP-1 formulation into the pulmonary circulation such as by inhalation, directly into pulmonary alveolar capillaries using a dry powder drug delivery system.
    Type: Grant
    Filed: October 24, 2008
    Date of Patent: February 19, 2013
    Assignee: MannKind Corporation
    Inventors: Peter Richardson, Robert A. Baughman, Donald Costello
  • Patent number: 8367844
    Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or X—N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.
    Type: Grant
    Filed: August 6, 2010
    Date of Patent: February 5, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Laura Quaranta, Mathias Stephan Respondek
  • Patent number: 8361426
    Abstract: Absorption medium for acid gases comprising an oligoamine (A) of the general formula (I) and a piperazine derivative (B) of the general formula (II) in which the weight ratio of oligoamine (A) to the piperazine derivative (B) is 0.2 to 25, and also process for removing acid gases from a gas stream by contacting the gas stream at a pressure of 0.05 to 10 MPa abs with an aqueous solution of said absorption medium which is brought to and maintained at a temperature of 20 to 80° C.
    Type: Grant
    Filed: June 9, 2009
    Date of Patent: January 29, 2013
    Assignee: BASF SE
    Inventors: Ute Lichtfers, Robin Thiele, Susanna Voges, Georg Sieder, Oliver Spuhl, Hugo Rafael Garcia Andarcia
  • Publication number: 20130018101
    Abstract: In one aspect, the present invention relates to a formulation in the form of molecular dispersion comprising i) fenofibric acid, a physiologically acceptable salt or derivative thereof and optionally other active substances, ii) a binder component comprising at least one enteric binder, and optionally iii) other physiologically acceptable excipients. In a second aspect, the present invention relates to novel salts of fenofibric acid that are photostable when compared to other salts of fenofibric acid.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 17, 2013
    Inventors: Russell Drew Cink, Joseph B. Paterson, JR., Yi Gao, Geoff G. Z. Zhang, Michelle A. Long, John B. Morris, Joerg Rosenberg
  • Patent number: 8338414
    Abstract: A novel method for immunosuppressive in a mammal suffering from an immune disease, including administering to the mammal a therapeutically effective amount of a heterocyclic compound represented by the general formula (I) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is disclosed. A novel heterocyclic compound represented by the general formula (II) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is also disclosed.
    Type: Grant
    Filed: May 24, 2010
    Date of Patent: December 25, 2012
    Assignee: Zenyaku Kogyo KabushikiKaisha
    Inventors: Kazuhiko Haruta, Shinichi Yaguchi, Toshiyuki Matsuno, Yoshio Tsuchida, Tetsuo Watanabe, Kimitomo Yoshioka, Ryogo Yui
  • Patent number: 8329700
    Abstract: Pyrazine compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein m, n, p, R1, R2, R3, R4, X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, Y and Z are defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: March 7, 2011
    Date of Patent: December 11, 2012
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Matthew Paul Bourbeau, Ning Chen, Essa Hu, Roxanne Kunz, Shannon Rumfelt
  • Patent number: 8324430
    Abstract: Processes for preparing an amine, the processes comprising: reacting a reactant selected from the group consisting of primary alcohols, secondary alcohols, aldehydes, ketones, and mixtures thereof, with hydrogen and a nitrogen compound selected from the group consisting of ammonia, primary amines, secondary amines and mixtures thereof, in the presence of a zirconium dioxide-, copper- and nickel-containing catalyst; wherein the catalyst comprises a catalytically active composition which comprises, before reduction with hydrogen, oxygen compounds of zirconium, copper, and nickel, 1.5 to 4.5% by weight of an oxygen compound of cobalt, calculated as CoO, and 0.2 to 5.0% by weight of at least one oxygen compound of niobium, sulfur, phosphorus, gallium, boron, lead or antimony, calculated in each case as Nb2O5, H2SO4, H3PO4, Ga2O3, B2O3, PbO and Sb2O3 respectively, and wherein the catalytically active composition does not comprise any molybdenum.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: December 4, 2012
    Assignee: BASF SE
    Inventors: Petr Kubanek, Wolfgang Mägerlein, Ekkehard Schwab, Johann-Peter Melder, Manfred Julius
  • Patent number: 8318982
    Abstract: A process for preparing an amine by reacting a primary or secondary alcohol, aldehyde and/or ketone with hydrogen and a nitrogen compound selected from the group of ammonia and primary and secondary amines, in the presence of a supported copper-, nickel- and cobalt-containing catalyst, wherein the catalytically active material of the catalyst, before the reduction thereof with hydrogen, comprises oxygen compounds of aluminum, of copper, of nickel, of cobalt and of tin, and in the range from 0.2 to 5.0% by weight of oxygen compounds of yttrium, of lanthanum, of cerium and/or of hafnium, each calculated as Y2O3, La2O3, Ce2O3 and Hf2O3 respectively, and catalysts as defined above.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: November 27, 2012
    Assignee: BASF SE
    Inventors: Petr Kubanek, Wolfgang Mägerlein, Johann-Peter Melder, Thomas Heidemann
  • Patent number: 8309740
    Abstract: The present invention relates to a method for one-pot synthesis of ionic liquid with fluoroalkyl group, more particularly to a method for one-pot synthesis of ionic liquid with fluoroalkyl group represented by the following Chemical Formula 1 by adding and reacting a nitrogen-containing compound, a Brønsted acid of the formula YH and a fluoroolefin compound of the formula CFR1?CR2R3 in a single reactor: wherein represents a nitrogen-containing compound; Y? represents an anion of the Brønsted acid; and R1, R2 and R3, which may be same or different, represent hydrogen, fluorine, C1-C10 alkyl or C1-C10 fluoroalkyl having from 1 to 23 fluorine atoms.
    Type: Grant
    Filed: August 15, 2008
    Date of Patent: November 13, 2012
    Assignee: Korea Institute of Science and Technology
    Inventors: Hyun Joo Lee, Dong Jin Suh, Byoung Sung Ahn, Hong Gon Kim, Chang Soo Kim, Hoon Sik Kim
  • Patent number: 8304430
    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: Grant
    Filed: December 20, 2010
    Date of Patent: November 6, 2012
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Michael N. Greco, Harold R. Almond, Jr., Michael J. Hawkins, Eugene Powell
  • Patent number: 8299065
    Abstract: Compound of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, or —C(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; Z1 is —N? or —CH?Z2 is —N? or —C(R1)?; R1 is hydrogen, methyl, ethyl, ethenyl, ethynyl, methoxy, mercapto, mercaptomethyl, halo, fully or partially fluorinated (C1-C2)alkyl, (C1-C2JaIkoxy or (C1-C2)alkylthio, nitro, or nitrile (—CN); R2 is a group Q1-[Alk1]q-Q2-, wherein q is 0 or 1; AIk1 is an optionally substituted, divalent, straight chain or branched C1-C6 alkylene, or C2-C6 alkenylene or C2-C6 alkynylene radical which may contain or terminate in an ether (—O—), thioether (—S—) or amino (—NR)— link; Q2 is an optionally substituted divalent monocyclic carbocyclic or heterocyclic ra
    Type: Grant
    Filed: December 12, 2008
    Date of Patent: October 30, 2012
    Assignee: Biota Europe Ltd.
    Inventors: David John Haydon, Lloyd George Czaplewski
  • Patent number: 8293945
    Abstract: Processes for preparing an amine, which processes comprise: reacting a reactant selected from the group consisting of primary alcohols, secondary alcohols, aldehydes, ketones, and mixtures thereof, with hydrogen and a nitrogen compound selected from the group consisting of ammonia, primary amines, secondary amines and mixtures thereof, in the presence of a zirconium dioxide-and nickel-containing catalyst; wherein the catalyst comprises a catalytically active composition which comprises, before reduction with hydrogen, oxygen compounds of zirconium, nickel, and iron, and 0.2 to 5.5% by weight of at least one oxygen compound of tin, lead, bismuth, molybdenum, antimony or phosphorus, calculated as SnO, PbO, Bi2O3, MoO3, Sb2O3 and H3PO4 respectively; and wherein the catalytically active composition of the catalyst does not comprise any copper.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: October 23, 2012
    Assignee: BASF SE
    Inventors: Petr Kubanek, Wolfgang Mägerlein, Ekkehard Schwab, Johann-Peter Melder, Manfred Julius
  • Patent number: 8287969
    Abstract: An isosorbide derivative of Formula (I) is provided. In Formula (I), Z is —CH2—CH2—, —CH?CH—, —C?C—, —CH2—O—, —CH2—S—, —CH?N—O—, —CO—O—, —CO—S—, single bond, -ph-, —CO—O-ph- or —CO—O-ph-CO—O—, and ph represents benzene, R1 and R2 are, independently, C1-25 alkyl, —CN, —NCS, —CX3 or —OCX3, and X represents halogen, and m and n are, independently, 0, 1 or 2. The invention also provides a liquid crystal display including the isosorbide derivative.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: October 16, 2012
    Assignee: Industrial Technology Research Institute
    Inventors: Chun-Ming Wu, Kevin Lin, Shih-Hsien Liu, Chih-Lung Chin, An-Cheng Chen, Kung-Lung Cheng, Chien-Hsien Cheng
  • Publication number: 20120255898
    Abstract: A polyamide membrane comprising reaction product of an anhydrous solution comprising an anhydrous solvent, at least one polyfunctional secondary amine and a pre-polymer deposition catalyst; and an anhydrous, organic solvent solution comprising a polyfunctional aromatic amine-reactive reactant comprising one ring. A composite semipermeable membrane comprising the polyamide membrane on a porous support. A method of making a composite semipermeable membrane by coating a porous support with an anhydrous solution comprising an anhydrous solvent, a polyfunctional secondary amine and a pre-polymer deposition catalyst, to form an activated pre-polymer layer on the porous support and contacting the activated pre-polymer layer with an anhydrous, organic solvent solution comprising a polyfunctional amine-reactive reactant to interfacially condense the amine-reactive reactant with the polyfunctional secondary amine, thereby forming a cross-linked, interfacial polyamide layer on the porous support.
    Type: Application
    Filed: March 5, 2012
    Publication date: October 11, 2012
    Applicant: Eltron Research & Development, Inc.
    Inventor: Wayne E. Buschmann
  • Patent number: 8278489
    Abstract: Processes for preparing an amine, which processes comprise: reacting a reactant selected from the group consisting of primary alcohols, secondary alcohols, aldehydes, ketones, and mixtures thereof, with hydrogen and a nitrogen compound selected from the group consisting of ammonia, primary amines, secondary amines and mixtures thereof, in the presence of a zirconium dioxide-, copper- and nickel-containing catalyst; wherein the catalyst comprises a catalytically active composition which comprises, before reduction with hydrogen, oxygen compounds of zirconium, copper, nickel and tin, and 0.5 to 8.0% by weight of an oxygen compound of cobalt, calculated as CoO, and wherein the catalytically active composition does not comprise any ruthenium.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: October 2, 2012
    Assignee: BASF SE
    Inventors: Petr Kubanek, Wolfgang Mägerlein, Ekkehard Schwab, Johann-Peter Melder, Manfred Julius
  • Patent number: 8258139
    Abstract: The invention relates to a medicament or a method for treating mental disorders, in detail, ADHD comprising lurasidone, or a combination of lurasidone and a D4 receptor agonist.
    Type: Grant
    Filed: May 23, 2011
    Date of Patent: September 4, 2012
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Kazuhito Ikeda, Takeo Ishiyama
  • Patent number: 8252785
    Abstract: The present invention relates to compounds of general formula I wherein A, B, D, Y, R1, R2, R3, R4 and R5 are defined as in the specification, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.
    Type: Grant
    Filed: October 5, 2010
    Date of Patent: August 28, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Iris Kauffmann-Hefner, Norbert Hauel, Rainer Walter, Heiner Ebel, Henri Doods, Angelo Ceci, Annette Schuler-Metz, Ingo Konetzki
  • Patent number: 8252798
    Abstract: A compound of the formula: and pharmaceutical compositions for the treatment of pain.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: August 28, 2012
    Assignee: Eli Lilly and Company
    Inventors: Peter Charles Astles, Rossella Guidetti, Sean Patrick Hollinshead, Michael Wade Tidwell
  • Patent number: 8247401
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Grant
    Filed: October 29, 2008
    Date of Patent: August 21, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Diem Nguyen, Zhengwu Deng, Daniel V. Paone, Craig M. Potteiger, Joseph P. Vacca
  • Patent number: 8114999
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: January 27, 2009
    Date of Patent: February 14, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Kristof Van Emelen, Hans Louis Jos De Winter, Alexy Borisovich Dyatkin, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Jimmy Arnold Viviane Van heusden
  • Publication number: 20120035176
    Abstract: Analogs of 3-O-acetyl-11-keto-beta-boswellic acid and their method of preparation are presented. The analogs may be used as anti-inflammatory and anti-cancer agents. The compounds inhibit 5-lipoxygenase enzyme and various cell lines related to inflammation as well as to cancer showing a significantly better efficacy when compared to the normal boswellic acids. The analogs are capable of controlling and treating various inflammatory diseases and cancers.
    Type: Application
    Filed: September 30, 2011
    Publication date: February 9, 2012
    Inventors: Ganga Raju Gokaraju, Rama Raju Gokaraju, Venkata Subbaraju Gottumukkala, Trimurtulu Golakoti, Krishanu Sengupta
  • Publication number: 20120022004
    Abstract: The invention provides a method of treating T-cell mediated diseases and a method of inhibiting the activation of T-cells using certain diketopiperazines. The invention also provides methods of synthesizing diketopiperazines and pharmaceutical compositions comprising certain diketopiperazines. The invention further provides methods of making improved pharmaceutical compositions of proteins and peptides by either increasing or decreasing the content of diketopiperazines in the compositions and the resultant improved pharmaceutical compositions.
    Type: Application
    Filed: September 28, 2011
    Publication date: January 26, 2012
    Inventors: David Bar-Or, Raphael Bar-Or, Richard Shimonkevitz
  • Patent number: 8058299
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
    Type: Grant
    Filed: May 1, 2008
    Date of Patent: November 15, 2011
    Assignee: VIA Pharmaceuticals, Inc.
    Inventors: David Robert Bolin, Adrian Wai-Hing Cheung, Fariborz Firooznia, Matthew Michael Hamilton, Lee Apostle McDermott, Yimin Qian, Jenny Tan, Weiya Yun
  • Patent number: 8022111
    Abstract: Compounds of formula (I) [in which: A and B are terminal groups; R1 represents a group of formula (II) or (III); R2 is alkyl or aryl; Z is a group —(CHR3)n, where R3 is hydrogen, hydroxy or alkyl, and n is a number from 0 to 6; Y is carbonyl or a group —CH2—; Q represents a residue of a dihydroxy compound; and x is a number from 1 to 100] are useful sensitisers for use with Type II photoinitiators in the formulation of printing inks and other energy curable coatings.
    Type: Grant
    Filed: January 28, 2005
    Date of Patent: September 20, 2011
    Assignee: Sun Chemical Corporation
    Inventors: Shaun Lawrence Herlihy, Brian Rowatt
  • Patent number: 8017613
    Abstract: The present invention relates to new compounds, ligands of the beta-3 adrenergic receptor, their preparation and their use in therapy or as research tools for said receptor; the invention also relates to a process for the preparation of the compounds of the invention and the use of inverse agonists of the beta-3 adrenergic receptor as medicaments.
    Type: Grant
    Filed: August 3, 2007
    Date of Patent: September 13, 2011
    Assignee: Universita' Degli Studi Di Bari
    Inventors: Antonio Scilimati, Maria Grazia Perrone, Ernesto Santandrea
  • Patent number: 8013152
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: April 14, 2010
    Date of Patent: September 6, 2011
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Mathai Mammen, Craig Husfeld, Li Li, YongQi Mu, Aaron Kushner, Eric Stangeland, Trevor Mischki, Adam Hughes, Sarah Dunham
  • 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
  • Patent number: 7989454
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, COPD.
    Type: Grant
    Filed: December 2, 2008
    Date of Patent: August 2, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Romyr Dominique, Robert Alan Goodnow, Jr., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
  • Publication number: 20110182799
    Abstract: A method of sequestering a multi-element gas emitted by an industrial plant is described herein, the method comprising: contacting a solution, including a first reactant comprising a multi-element gas emitted by an industrial plant and at least one gas absorber comprising nitrogen, for example ammonia or an amine, with a solid, including a second reactant, under conditions that promote a reaction between the first reactant and the second reactant to provide a first product, which incorporates one or more elements of the multi-element gas, thereby sequestering the multi-element gas.
    Type: Application
    Filed: January 18, 2011
    Publication date: July 28, 2011
    Applicant: Rutgers, The State University of New Jersey
    Inventors: Richard E. RIMAN, Qinghua Li
  • Patent number: RE43688
    Abstract: Contemplated substituted arylpiperazinyl compounds, and most preferably 18F-Mefway, exhibit desirable in vitro and in vivo binding characteristics to the 5-HT1A receptor. Among other advantageous parameters, contemplated compounds retain high binding affinity, display optimal lipophilicity, and are radiolabeled efficiently with 18F-fluorine in a single step. Still further, contemplated compounds exhibit high target to non-target ratios in receptor-rich regions both in vitro and in vivo, and selected compounds can be effectively and sensitively displaced by serotonin, thus providing a quantitative tool for measuring 5-HT1A receptors and serotonin concentration changes in the living brain.
    Type: Grant
    Filed: July 21, 2011
    Date of Patent: September 25, 2012
    Assignee: The Regents of the University of California
    Inventors: Jogeshwar Mukherjee, Neil Saigal, Harsh Saigal, legal representative