Piperazines (i.e., Fully Hydrogenated 1,4-diazines) Patents (Class 544/358)
  • Patent number: 10968164
    Abstract: A process to convert the cyclic monourea of ethylene amine compounds (U-EA) into ethylene amine compound (EA) is provided. The process may include performing a reactive separation step using a reaction mixture containing the cyclic monourea, wherein one cyclic monourea (U-EA) reacts with another cyclic monourea (U-EA) to transfer its urea unit thereto. The process may further include separating the obtained ethylene amine compound (EA) without urea unit from the reaction mixture.
    Type: Grant
    Filed: August 7, 2018
    Date of Patent: April 6, 2021
    Assignee: NOURYON CHEMICALS INTERNATIONAL B.V.
    Inventors: Michiel Jozef Thomas Raaijmakers, Antoon Jacob Berend Ten Kate, Eike Nicolas Kantzer, Rens Veneman, Slavisa Jovic, Rolf Krister Edvinsson, Karl Fredrik Lake, Hendrik Van Dam, Ina Ehlers, Sara Erika Tönnerfors
  • Patent number: 10099172
    Abstract: The present invention relates to a carbon dioxide absorbent comprising a triamine, a diamine and a dialkylene glycol dialkyl ether or trialkylene glycol dialkyl ether. The carbon dioxide absorbent according to the present invention can improve the carbon dioxide absorption capacity, absorption rate, and regeneration performance thereof simultaneously by using the triamine as a main absorbent, the diamine as a rate enhancer, the dialkylene glycol dialkyl ether or trialkylene glycol dialkyl ether as a fine disproportionation agent and a regeneration promoter.
    Type: Grant
    Filed: October 16, 2015
    Date of Patent: October 16, 2018
    Assignee: UNIVERSITY-INDUSTRY COOPERATION GROUP OF KYUNG HEE UNIVERSITY
    Inventors: Sung Yun Hong, Hoon Sik Kim
  • Patent number: 9814704
    Abstract: Provided are compounds having an inhibitory effect on Mixed Lineage Kinases. The compounds include substituted pyrrolo[2,3-b]pyridines having Formula IX Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment neuropsychiatric disorders which comprise the inhibition of Mixed Lineage Kinases.
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: November 14, 2017
    Assignee: The University of Rochester
    Inventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Colin J. Loweth, Torsten Wiemann
  • Patent number: 9688634
    Abstract: Objects of the present invention are to provide a compound which is highly active against pests, to provide a pest control agent comprising the compound, and to provide a method for controlling a pest by applying the compound. The present invention provides a 4-(arylethynyl)pyridine or a salt thereof, a pest control agent which comprises the 4-(arylethynyl)pyridine or salt thereof as an active ingredient, and a method for controlling a pest by applying the 4-(arylethynyl)pyridine or salt thereof in an effective amount.
    Type: Grant
    Filed: December 19, 2013
    Date of Patent: June 27, 2017
    Assignee: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Kazuhisa Kiriyama, Masahiro Matsumoto, Kotaro Yoshida, DamdinSuren Boldbaatar, Tatsuya Jukurogi, Nao Umemoto, Tatsuya Kani, Yoko Matsuda, Kumiko Tanaka, Michiko Kanuma, Tatsuya Shimada
  • Patent number: 9512105
    Abstract: Provided are compounds represented by the formula: where R, Y3, R1, R2, R3, R4, R6, G, R7, E1, E2, A, B, W, X, Y and Z are as defined herein.
    Type: Grant
    Filed: December 10, 2012
    Date of Patent: December 6, 2016
    Assignee: RESEARCH TRIANGLE INSTITUTE
    Inventors: Frank I. Carroll, James B. Thomas, Hernan A. Navarro, S. Wayne Mascarella, Scott P. Runyon, Chunyang Jin, Chad M. Kormos
  • Patent number: 9492560
    Abstract: Compounds are provided herein which are emetine derivatives that can be used as prodrugs which selectively undergo activation to release emetine in specific cellular conditions. In one aspect, a blocking group is incorporated onto the emetine molecule by the derivization of the N2?-position with moieties that can be selectively removed by hydrolysis in the cancer/tumor microenvironment. Such compounds are less cytotoxic than emetine and are substantially inactive in non-cancerous cells. In one aspect, the compounds described herein can be used for the treatment of metastatic and non-metastatic cancers, including, for example, breast cancer, prostate cancer, lung cancer, and leukemia.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: November 15, 2016
    Inventors: Oladapo Bakare, Samuel Ray Denmeade, Emmanuel S. Akinboye
  • Patent number: 9359327
    Abstract: The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.
    Type: Grant
    Filed: November 13, 2013
    Date of Patent: June 7, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: Sergio Cesco-Cancian, Hongfeng Chen, Jeffrey S. Grimm, Neelakandha S. Mani, Christopher M. Mapes, David C. Palmer, Daniel J. Pippel, Kirk L. Sorgi, Tong Xiao
  • Patent number: 9321749
    Abstract: Disclosed herein are novel heterocyclic compounds, their salts, pharmaceutical compositions comprising such compounds and salts, and their uses in modulating protein-protein interactions and for treating diseases resulting from aberrant protein-protein interactions.
    Type: Grant
    Filed: July 25, 2013
    Date of Patent: April 26, 2016
    Assignee: GLOBAVIR BIOSCIENCES, INC.
    Inventors: Chenera Balan, Usha Nagavarapu
  • Patent number: 9062015
    Abstract: The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, M4, Y1, Y2, V, W, n, m and o have the meanings given in Claim 1, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: June 23, 2015
    Assignee: Merck Patent GmbH
    Inventors: Frank Stieber, Dirk Wienke
  • Patent number: 9040539
    Abstract: A process for the preparation of a chiral compound, in particular posaconazole, wherein the process comprises mixing and reacting the compounds of formula (I) Y3—NH2; of formula (IIa) 0=C?N—Y0 and/or of formula (IIb) and of formula (III) in a solvent in any order to obtain a reaction mixture containing a chiral compound of formula (IV) and/or formula (V).
    Type: Grant
    Filed: May 18, 2011
    Date of Patent: May 26, 2015
    Assignee: SANDOZ AG
    Inventors: Michael Oberhuber, Joerg Salchenegger, Dominic De Souza, Martin Albert, Thorsten Wilhelm, Martin Langner, Hubert Sturm, Hans-Peter Spitzenstaetter
  • Patent number: 8993759
    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: Grant
    Filed: October 20, 2011
    Date of Patent: March 31, 2015
    Assignee: DOW Global Technologies LLC
    Inventor: Stephen W. King
  • Publication number: 20150083223
    Abstract: A fullerene derivative represented by the following formula (1): wherein “FLN” represents a fullerene core, R1 represents an optionally substituted C1-C24 alkyl group or an optionally substituted C7-C24 aralkyl group, R2 and R3 independently represent a hydrogen atom or an optionally substituted C1-C24 hydrocarbon group but excluding a case where both of R2 and R3 are hydrogen atoms, and R2 and R3 may combine together to form a ring.
    Type: Application
    Filed: September 25, 2013
    Publication date: March 26, 2015
    Applicants: Tohoku University, Showa Denko K.K.
    Inventors: Tienan JIN, Weili Si, Yoshinori Yamamoto, Takeshi Igarashi
  • Patent number: 8981093
    Abstract: Process for preparing piperazine of the formula I by reacting diethanolamine (DEOA) of the formula II with ammonia in the presence of hydrogen and a supported, metal-containing catalyst has been found, wherein the catalytically active mass of the catalyst, prior to its reduction with hydrogen, comprises oxygen-containing compounds of aluminum, copper, nickel and cobalt and in the range from 0.2 to 5.0% by weight of oxygen-containing compounds of tin, calculated as SnO, and the reaction is carried out in the liquid phase at an absolute pressure in the range from 160 to 220 bar, a temperature in the range from 180 to 220° C., using ammonia in a molar ratio to DEOA used of from 5 to 25 and in the presence of 0.2 to 9.0% by weight of hydrogen, based on the total amount of DEOA used and ammonia.
    Type: Grant
    Filed: June 5, 2013
    Date of Patent: March 17, 2015
    Assignee: BASF SE
    Inventors: Roland Bou Chedid, Johann-Peter Melder, Ulrich Abel, Roman Dostalek, Nina Challand, Bernd Stein, Michael Jödecke
  • Patent number: 8969353
    Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
    Type: Grant
    Filed: November 6, 2009
    Date of Patent: March 3, 2015
    Assignee: Massachusetts Institute of Technology
    Inventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
  • Patent number: 8962022
    Abstract: The present invention is directed to compositions of taste-masked microparticles comprising a substituted benzhydrylpiperazine coated and a taste-masking layer comprising a water-insoluble polymer and a gastrosoluble polymer, and methods of making such taste-masked microparticles. The present invention is also directed to stable orally disintegrating compositions comprising taste-masked microparticles of a substituted benzhydrylpiperazine and rapidly dispersing granules, and methods of making such orally disintegrating compositions.
    Type: Grant
    Filed: March 27, 2008
    Date of Patent: February 24, 2015
    Assignee: Aptalis Pharmatech, Inc.
    Inventor: Gopi Venkatesh
  • Patent number: 8952156
    Abstract: A process is disclosed for separating the output from the reaction of EDDN or EDMN with hydrogen in the presence of THF, a catalyst, TETA or DETA, water, and optionally organic compounds having higher and lower boiling points than TETA or DETA. Hydrogen is removed, and the output is supplied to a distillation column DK1 in which an azeotrope, optionally comprising organic compounds with a boiling point lower than TETA or DETA, is removed from the top. A product comprising TETA or DETA is removed from the bottom and passed into a distillation column DK2, removing THF. A stream comprising TETA or DETA passes from the bottom of DK2. The DK1 azeotrope is condensed. Phase separation is induced by the addition of an organic solvent essentially immiscible with water, and the mixture is separated. The organic phase is recycled into DK1 and the water phase is discharged.
    Type: Grant
    Filed: August 30, 2012
    Date of Patent: February 10, 2015
    Assignee: BASF SE
    Inventors: Hermann Luyken, Sebastian Ahrens, Gordon Brasche, Jens Baldamus, Robert Baumann, Randolf Hugo, Stephanie Jaegli, Johann-Peter Melder, Jörg Pastre, Boris Buschhaus
  • Patent number: 8952157
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Grant
    Filed: July 26, 2013
    Date of Patent: February 10, 2015
    Assignees: AbbVie Inc., The Walter and Eliza Hall Institute of Medical Research
    Inventors: Hong Ding, George A. Doherty, Steven W. Elmore, Laura Hexamer, Aaron R. Kunzer, Cheol-Min Park, Xiahong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Le Wang, Michael D. Wendt, Peter Edward Czabotar, Guillaume Laurent Lessene, Peter Malcolm Colman
  • Patent number: 8952198
    Abstract: Disclosed is a process for the preparation of an amine (particularly diamines and polyamines) by reacting an alkanolamine or a polyol with ammonia in the presence of a catalyst composed of two active metals from the group of transition metals, namely nickel and chromium supported on a microporous refractory substrate, in a hydrogenated, trickle bed reactor.
    Type: Grant
    Filed: January 30, 2013
    Date of Patent: February 10, 2015
    Inventors: Ian Williams, John Christopher Williams, German Maya Maya-Hernandez, Lilia Patricia Hernandez Salas, Miguel Angel Lopez Guerrero
  • Publication number: 20140371452
    Abstract: The invention provides a method for the reductive amination of diethanolamine to form a product composition that includes piperazine (PIP) and aminoethylethanolamine (AEEA). A catalyst with a transitional alumina/second metal oxide support and a mixture of catalytic metals is used for the reaction which results in low levels of non-PIP and non-AEEA side products.
    Type: Application
    Filed: November 14, 2012
    Publication date: December 18, 2014
    Inventors: Stephen W. King, Sadeka Onam, Thomas Z. Srnak
  • Patent number: 8912361
    Abstract: Process for preparing primary amines which have at least one functional group of the formula (—CH2—NH2) and at least one further primary amino group by alcohol amination of starting materials having at least one functional group of the formula (—CH2—OH) and at least one further functional group (—X), where (—X) is selected from among hydroxyl groups and primary amino groups, by means of ammonia with elimination of water, wherein the reaction is carried out homogeneously catalyzed in the presence of at least one complex catalyst comprising at least one element selected from groups 8, 9 and 10 of the Periodic Table and also at least one donor ligand.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: December 16, 2014
    Assignee: BASF SE
    Inventors: Thomas Schaub, Boris Buschhaus, Marion Kristina Brinks, Mathias Schelwies, Rocco Paciello, Johann-Peter Melder, Martin Merger
  • Publication number: 20140309114
    Abstract: Amine salts of certain herbicides that in free acid form include at least one carboxylic acid moiety are described. Herbicide salts comprising the cation of various imidazole, piperazine, piperidine, and morpholine compounds are provided. The herbicide amine salts described are suitable for formulation into herbicidal application mixtures and/or stable concentration compositions that exhibit acceptable volatility characteristics upon application.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Applicant: MONSANTO TECHNOLOGY LLC
    Inventors: Junhua Zhang, Daniel R. Wright, William Abraham
  • Patent number: 8858828
    Abstract: The present disclosure provides a scrubbing composition containing an aqueous solution of 2-(3-aminopropoxy)ethan-1-ol. The scrubbing composition is especially suited for use in removing acid gases, such as carbon dioxide and hydrogen sulfide, from gas streams.
    Type: Grant
    Filed: October 18, 2011
    Date of Patent: October 14, 2014
    Assignee: Huntsman Petrochemical LLC
    Inventors: Howard P. Klein, Robert A. Grigsby, Jr., Jingjun Zhou, Patrick Holub, Attila Gaspar, Zsolt Gaspar
  • Patent number: 8853243
    Abstract: The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.
    Type: Grant
    Filed: May 19, 2011
    Date of Patent: October 7, 2014
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, Jincong Zhuo, David Burns, Wenqing Yao, Ravi Kumar Jalluri
  • Patent number: 8816078
    Abstract: Compositions and methods related to the removal of acidic gas. In one embodiment, compositions and methods are provided for the removal of acidic gas from a gas mixture using an aqueous amine solvent comprising water, a first amine, and a second amine, wherein the first amine contributes at least 50% by weight of the solvent's total amine concentration.
    Type: Grant
    Filed: January 11, 2011
    Date of Patent: August 26, 2014
    Assignee: Board of Regents, The University of Texas System
    Inventors: Gary Rochelle, Stephanie Freeman, Xi Chen, Thu Nguyen, Alexander Voice, Humera Rafique
  • Patent number: 8796274
    Abstract: The use of a compound of formula I wherein Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; the ring is a 6-membered aromatic or is a 5 or 6 membered heteroaromatic ring; Ra, R1, R2, R4 and R8 are specified organic groups; n and p are independently 0-4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: August 5, 2014
    Assignee: Syngenta Crop Protection LLC
    Inventors: Jerome Cassayre, Louis-Pierre Molleyres, Peter Maienfisch, Fredrik Cederbaum, Camilla Corsi, Thomas Pitterna
  • Patent number: 8785693
    Abstract: Process for the preparation of primary amines which have at least one functional group of the formula (—CH2—NH2) by alcohol amination of starting materials which have at least one functional group of the formula (—CH2—OH), with ammonia, with the elimination of water, where the alcohol amination is carried out under homogeneous catalysis in the presence of at least one complex catalyst which comprises at least one element selected from groups 8 and 9 of the Periodic Table of the Elements, and also at least one phosphorus donor ligand of the general formula (I).
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: July 22, 2014
    Assignee: BASF SE
    Inventors: Thomas Schaub, Boris Buschhaus, Marion Kristina Brinks, Mathias Schelwies, Rocco Paciello, Johann-Peter Melder, Martin Merger
  • Patent number: 8765083
    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 SO.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: July 1, 2014
    Assignee: Nalco Company
    Inventors: Alan M. Blair, Keith N. Garside, William J. Andrews, Kailas B. Sawant
  • Patent number: 8765951
    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 SO.
    Type: Grant
    Filed: May 1, 2013
    Date of Patent: July 1, 2014
    Assignee: Nalco Company
    Inventors: Alan M. Blair, Keith N. Garside, William J. Andrews, Kailas B. Sawant
  • Patent number: 8759520
    Abstract: Compounds of general formula (I): wherein R1, R2, R3, R4, R5, R6, X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterized by abnormal cell growth and/or dysregulated apoptosis.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: June 24, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Stephen Peter East, Mark Whittaker, Osamu Ichihara, Adrian Kotei Kotey, Smantha Jayne Bamford
  • Patent number: 8748598
    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: Grant
    Filed: September 30, 2011
    Date of Patent: June 10, 2014
    Assignee: Laila Nutraceuticals
    Inventors: Ganga Raju Gokaraju, Rama Raju Gokaraju, Venkata Subbaraju Gottumukkala, Trimurtulu Golakoti, Krishanu Sengupta
  • Patent number: 8735397
    Abstract: The invention relates to a method for treating schizophrenia and/or related diseases comprising administering lurasidone and a mGluR2 ligand to a mammal in need thereof.
    Type: Grant
    Filed: March 28, 2011
    Date of Patent: May 27, 2014
    Assignees: Vanderbilt University, Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Herbert Y. Meltzer, Masakuni Horiguchi
  • Patent number: 8710059
    Abstract: The present invention relates to N-Phenyl-(homo)piperazinyl-benzenesulfonyl or benzenesulfonamide compounds of formula I wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.
    Type: Grant
    Filed: November 1, 2011
    Date of Patent: April 29, 2014
    Assignees: Abbott Laboratories, AbbVie Deutschland GmbH & Co. KG
    Inventors: Andreas Haupt, Frauke Pohlki, Liliane Unger, Ana Lucia Relo, Karsten Wicke, Min Zhang
  • Patent number: 8710062
    Abstract: This invention relates to piperazinedione compounds shown in the specification. These compounds are tyrosine kinase inhibitors and can be used to treat cancer.
    Type: Grant
    Filed: February 24, 2012
    Date of Patent: April 29, 2014
    Assignee: Taipei Medical University
    Inventors: Hui-po Wang, Che-Ming Teng, Chun-Li Wang, Jih-hwa Guh, Shiow-Lin Pan, Yuan-Yi Wang, Jang-Feng Lian
  • Patent number: 8686008
    Abstract: Compounds having the general formula II, III, or IV wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: 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: May 21, 2010
    Date of Patent: April 1, 2014
    Assignees: The University of Mississippi, L'Universite Catholique de Louvain
    Inventors: Christopher R. McCurdy, Christophe Mesangeau, Rae Reiko Matsumoto, Jacques Henri Poupaert, Bonnie Ann Avery, Ahmed Hassan Amin Abdelazeem
  • Patent number: 8685979
    Abstract: The invention relates to (among other things) oligomer-diarylpiperazine conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated diarylpiperazine compounds.
    Type: Grant
    Filed: January 22, 2009
    Date of Patent: April 1, 2014
    Assignee: Nektar Therapeutics
    Inventors: Zhongxu Ren, Jennifer Riggs-Sauthier
  • Publication number: 20140088106
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: October 14, 2013
    Publication date: March 27, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Yujia Dai, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Todd M. Hansen
  • Patent number: 8680102
    Abstract: The subject of the invention is compounds of formula (I): in which R1-R10 are as defined within, the method of preparation and therapeutic application as cannabinoid CB1 receptor antagonists.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: March 25, 2014
    Assignee: Sanofi
    Inventors: Francis Barth, Daniel Bichon, Murielle Rinaldi-Carmona, Christian Congy
  • Patent number: 8680273
    Abstract: The present invention is directed to a novel process for the preparation of piperazinyl and diazepanyl benzamide derivatives, useful for the treatment of disorders and conditions mediated by a histamine receptor, preferably the H3 receptor.
    Type: Grant
    Filed: January 10, 2011
    Date of Patent: March 25, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Anusuya Choudhury, Jeffrey S. Grimm, Kirk L. Sorgi, David Palmer, Jing Liu
  • Patent number: 8679773
    Abstract: This invention pertains to methods, kits and/or compositions for the determination of analytes by mass analysis using unique labeling reagents or sets of unique labeling reagents. The labeling reagents can be isomeric or isobaric and can be used to produce mixtures suitable for multiplex analysis of the labeled analytes.
    Type: Grant
    Filed: January 16, 2007
    Date of Patent: March 25, 2014
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Darryl J. C. Pappin, Michael Bartlett-Jones
  • Patent number: 8658647
    Abstract: A number of compounds and use of the compounds in a method for treating or preventing cancer in a subject by administering to the subject a pharmaceutical composition including a compound of formula I or a pharmaceutically acceptable salt thereof are described. The compounds can also be used to inhibit integrin-linked kinase in a cell, which has an effect on the Akt signaling pathway.
    Type: Grant
    Filed: November 21, 2011
    Date of Patent: February 25, 2014
    Assignee: The Ohio State University Research Foundation
    Inventors: Ching-Shih Chen, Su-Lin Lee, Samuel K. Kulp
  • Patent number: 8653081
    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: March 29, 2013
    Date of Patent: February 18, 2014
    Assignee: Cytokinetics, Inc.
    Inventors: Bradley P. Morgan, Erica A. Kraynack, Pu-Ping Lu, Alex Muci, David J. Morgans
  • Patent number: 8642596
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Grant
    Filed: December 6, 2005
    Date of Patent: February 4, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Yijun Deng, Theodore J. Nitz, Thomas R. Bailey, Yuanming Zhang, Sylvie Laquerre
  • Patent number: 8637520
    Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
    Type: Grant
    Filed: July 1, 2010
    Date of Patent: January 28, 2014
    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
  • Patent number: 8637709
    Abstract: Preparing a primary amine by alcohol amination of alcohol with ammonia and elimination of water includes reacting, in a homogeneously catalyzed reaction, a mixture of alcohol, ammonia, nonpolar solvent, and catalyst, in a liquid phase, to obtain a product mixture. The process then includes phase separating the product mixture into a polar product phase and a nonpolar product phase, and separating off the nonpolar product phase. At least some of the nonpolar phase returns to the homogenously catalyzed reaction. The process further includes separating off amination product from the polar product phase. At least some of the catalyst is in the nonpolar phase, and the catalyst accumulates in the nonpolar phase.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: January 28, 2014
    Assignee: BASF SE
    Inventors: Thomas Schaub, Boris Buschhaus, Marion Kristina Brinks, Mathias Schelwies, Rocco Paciello, Johann-Peter Melder, Martin Merger
  • Publication number: 20140011814
    Abstract: Provided herein are diamine salts of eicosapentaenoic acid and docosahexaenoic acid, processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and the uses of such compounds as agents for treating dyslipidemia, cardiovascular diseases such as cardiac arrhythmia, cardiac ischemia, myocardial infarction, cardiomyopathy, and stroke and obesity.
    Type: Application
    Filed: March 15, 2013
    Publication date: January 9, 2014
    Applicant: THETIS PHARMACEUTICALS LLC
    Inventors: Banavara L. MYLARI, Frank C. SCIAVOLINO
  • Patent number: 8624027
    Abstract: The present disclosure relates to a combination of therapeutic agents for use in treating a patient a subject suffering from cancer. In addition, the present disclosure also relates to diagnostic assays useful in classification of patients for treatment with one or more therapeutic agents.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: January 7, 2014
    Assignee: AbbVie Inc.
    Inventors: Omar Jameel Shah, Yu Shen, Xiaoyu Lin, Mark Anderson, Xiaoli Huang, Junling Li, Leiming Li
  • Publication number: 20140005384
    Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.
    Type: Application
    Filed: September 3, 2013
    Publication date: January 2, 2014
    Applicant: Pfizer Inc.
    Inventors: Anthony Michael Campeta, Joseph Francis Krzyzaniak, Jason Albert Leonard
  • Publication number: 20130331573
    Abstract: Process for preparing piperazine of the formula I by reacting diethanolamine (DEOA) of the formula II with ammonia in the presence of hydrogen and a supported, metal-containing catalyst has been found, wherein the catalytically active mass of the catalyst, prior to its reduction with hydrogen, comprises oxygen-containing compounds of aluminum, copper, nickel and cobalt and in the range from 0.2 to 5.0% by weight of oxygen-containing compounds of tin, calculated as SnO, and the reaction is carried out in the liquid phase at an absolute pressure in the range from 160 to 220 bar, a temperature in the range from 180 to 220° C., using ammonia in a molar ratio to DEOA used of from 5 to 25 and in the presence of 0.2 to 9.0% by weight of hydrogen, based on the total amount of DEOA used and ammonia.
    Type: Application
    Filed: June 5, 2013
    Publication date: December 12, 2013
    Inventors: Roland Bou Chedid, Johann-Peter Melder, Ulrich Abel, Roman Dostalek, Nina Challand, Bernd Stein, Michael Jödecke
  • Publication number: 20130331574
    Abstract: Process for preparing piperazine of the formula I by reacting diethanolamine (DEOA) of the formula II with ammonia (NH3) in the presence of hydrogen and a supported, metal-containing catalyst, wherein the catalytically active mass of the catalyst, prior to its reduction with hydrogen, comprises 20 to 85% by weight of oxygen-containing compounds of zirconium, calculated as ZrO2, 1 to 30% by weight of oxygen-containing compounds of copper, calculated as CuO, 14 to 70% by weight of oxygen-containing compounds of nickel, calculated as NiO, and 0 to 5% by weight of oxygen-containing compounds of molybdenum, calculated as MoO3, and the reaction is carried out in the liquid phase at an absolute pressure in the range from 160 to 220 bar, a temperature in the range from 180 to 220° C., using ammonia in a molar ratio to DEOA used of from 5 to 20 and in the presence of 0.2 to 9.0% by weight of hydrogen, based on the total amount of DEOA used and ammonia.
    Type: Application
    Filed: June 5, 2013
    Publication date: December 12, 2013
    Inventors: Roland Bou Chedid, Johann-Peter Melder, Ulrich Abel, Roman Dostalek, Nina Challand, Bernd Stein, Michael Jodecke
  • 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