The Aryl Ring Or Ring System And Amino Nitrogen Are Bonded Directly To The Same Acyclic Carbon, Which Carbon Additionally Has Only Hydrogen Or Acyclic Hydrocarbyl Substituents Bonded Directly Thereto Patents (Class 564/384)
  • Patent number: 10464879
    Abstract: Disclosed is a process for performing a reductive amination of a first functional group in an organic feed substrate, which feed substrate comprises at least one further functional group containing a halogen atom, in the presence of hydrogen, a nitrogen-containing compound, and a catalyst, wherein the presence of the nitrogen-containing compound, expressed in a molar ratio relative to the first functional group in the organic feed substrate, at least during the reaction as long as the conversion of the organic feed substrate has not yet reached 80%, is maintained below a level of 1.3. Further disclosed is a composition of the invention comprising at least 98.0% wt of 2-chloro-benzyl-dimethylamine, at most 0.60% wt of the meso-o-Cl-BDMA dimer and at least 1 ppm wt of the (+/?)-o-Cl-BDMA dimer and any use therefor.
    Type: Grant
    Filed: November 7, 2016
    Date of Patent: November 5, 2019
    Assignee: Taminco BVBA
    Inventors: Kristof Moonen, Kim Dumoleijn, Kristof Weyne, Jerome Leonard Stavinoha, Jr., Zhufang Liu
  • Patent number: 10231939
    Abstract: Compositions comprising hydroxytyrosol-containing formulations and treatment regiments comprising hydroxytyrosol and/or oleuropein and chemotherapeutic agents are disclosed. Compositions and/or regiments may optionally include the administration of vitamins, minerals, and anti-oxidants. Methods for using these compositions and treatment regimens for treating subjects for diseases, such as a malignancy, and for inducing or enhancing angiogenesis, treating or preventing oxidative stress, for treating or preventing high glucose-induced dysfunction, treating or preventing chemotherapy-induced dysfunction, and for improving cell viability are provided. Various methods for use of the hydroxytyrosol compositions for inhibition of lysine specific demethylase 1 (LSD1) in various cancers are also provided.
    Type: Grant
    Filed: April 25, 2017
    Date of Patent: March 19, 2019
    Inventor: Darlene E. McCord
  • Patent number: 10035755
    Abstract: The invention relates to a method for producing halogen-N,N-dimethylbenzylamines wherein halogen=chlorine or bromine, preferably chloro-N,N-dimethylbenzylamines, preferably ortho-chloro-N,N-dimethylbenzylamine (o-Cl-DMBA), by reductive amination in the absence of sulfur.
    Type: Grant
    Filed: March 4, 2014
    Date of Patent: July 31, 2018
    Assignee: LANXESS Deutschland GmbH
    Inventors: Lars Peters, Andreas Schulze Tilling, Wolfgang Stirner
  • Publication number: 20150119461
    Abstract: The present application provides novel tetrahydro-isohumulone (THIAA) derivatives and substantially enantiomerically pure compositions and pharmaceutical formulations thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPAR?, inhibit inflammation, and treat conditions associated with inflammation and conditions responsive to PPAR? modulation such as diabetes.
    Type: Application
    Filed: January 9, 2015
    Publication date: April 30, 2015
    Inventors: Veera KONDA, Jan URBAN, Anuradha DESAI, Clinton J. DAHLBERG, Brian J. CARROLL
  • Publication number: 20150094492
    Abstract: The present invention relates to a process for preparing N-(5-chloro-2-isopropylbenzyl)cyclopropanamine by hydrogenation of N-[(5-chloro-2-isopropylphenyl)methylene]cyclopropanamine over specific platinum catalysts.
    Type: Application
    Filed: April 25, 2013
    Publication date: April 2, 2015
    Inventors: Thomas Himmler, Sandra Lehmann, Thomas Norbert Muller, Mathias Riedrich, Lars Rodefeld, Frank Volz, Sascha Von Morgenstern
  • Patent number: 8993808
    Abstract: The present invention relates to phenylcyclopropylamine derivatives. In particular, pharmaceutical compositions comprising phenylcyclopropylamine derivatives are provided. The compounds of this invention can, inter alia, be used for the treatment and the prevention of cancer as well as neurodegenerative diseases or disorders.
    Type: Grant
    Filed: January 21, 2010
    Date of Patent: March 31, 2015
    Assignee: Oryzon Genomics, S.A.
    Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria
  • Patent number: 8962657
    Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.
    Type: Grant
    Filed: November 8, 2013
    Date of Patent: February 24, 2015
    Assignee: Jacobus Pharmaceutical Company, Inc.
    Inventors: Gavin David Heffernan, David Penman Jacobus, Guy Alan Schiehser, Hong-Ming Shieh, Wenyi Zhao
  • Publication number: 20150038651
    Abstract: Provided are novel dinuclear indium catalysts of formula (A) that are capable of living and immortal ring opening polymerization and copolymerization of cyclic ester monomers for the preparation of biodegradable polymers and copolymers, in particular polyesters. Also disclosed are polymerization methods and polymer products. These dinuclear indium catalysts allow less costly, highly reactive living polymerization of cyclic ester monomers with possible high turn over rates and/or substantial stereo chemical and microstructure control.
    Type: Application
    Filed: May 18, 2012
    Publication date: February 5, 2015
    Applicant: University of British Columbia
    Inventors: Parisa Mehrkhodavandi, Insun Yu, J. Alberto Acosta-Ramirez
  • Patent number: 8927758
    Abstract: Process for the optical resolution of the compound of formula (I): by chiral chromatography. Application in the synthesis of ivabradine, of its addition salts with a pharmaceutically acceptable acid and of their hydrates.
    Type: Grant
    Filed: March 26, 2013
    Date of Patent: January 6, 2015
    Assignee: Les Laboratories Servier
    Inventors: Jean-Michel Lerestif, Jean-Pierre Lecouve, Daniel Dron, Eric Gojon, Maryse Phan
  • Publication number: 20140288247
    Abstract: The invention relates to hardeners for epoxy resin containing secondary amino groups having dialkyl amino phenyl groups. The hardeners have a surprisingly low viscosity and harden surprisingly fast together with the epoxy resins, even in moist, cold conditions, and without blushing to form films with high hardness and stability. They are suitable, in particular, for low-emission coatings.
    Type: Application
    Filed: November 8, 2012
    Publication date: September 25, 2014
    Inventors: Urs Burckhardt, Edis Kasemi
  • Publication number: 20140275446
    Abstract: The present invention relates to hardeners for epoxy resins, which contain secondary aliphatic and primary aromatic amino groups. They harden surprisingly quickly together with epoxy resins even under cold and humid conditions and without blushing effects to give films with a high degree of hardness. They are especially suitable for coatings with high resistance requirements.
    Type: Application
    Filed: November 8, 2012
    Publication date: September 18, 2014
    Applicant: Sika Technology AG
    Inventors: Andreas Kramer, Edis Kasem
  • Patent number: 8742175
    Abstract: The present invention discloses novel aromatic ketone compounds with functional substitution groups at para- or meta positions which can be used as photo-initiators or effective components of photo-initiator mixtures for the photopolymerizations of ethylenically unsaturated systems. The preparation of these compounds is also disclosed.
    Type: Grant
    Filed: November 4, 2011
    Date of Patent: June 3, 2014
    Assignee: Shenzhen UV-Chemtech Co., Ltd.
    Inventors: Yongbo Zhang, Yanchao Wang, Yapeng Wang, Huaihai Song, Zhigang Wang
  • Publication number: 20140142304
    Abstract: There is provided a process for producing an aminopropyne or an enaminone comprising the step of reacting a metal acetylide, an amine and a carbonyl-containing compound in the presence of a transition metal catalyst. There is also provided a process for producing an aminopropyne comprising the step of reacting a metal acetylide, an amine and a halide-containing compound in the presence of a transition metal catalyst at a reaction temperature of 50° C. to 150° C. There are also provided processes to further synthesize the aminopropyne produced to obtain a butyneamine, another aminopropyne or a triazol.
    Type: Application
    Filed: July 6, 2012
    Publication date: May 22, 2014
    Applicant: Agency for Science, Technology and Research
    Inventors: Yugen Zhang, Dingyi Yu, Zhewang Lin
  • Publication number: 20140083853
    Abstract: An electrode for use in a electrochemical sensor comprises carbon modified with a chemically sensitive redox-active compound, excluding an electrode based on carbon having derivatised thereron two redox-active species wherein at least one of said species is selected from anthraquinone, phenanthrenequinone and N,N?-diphenyl-p-phenylenediamine (DPPD). The invention further provides a pH sensor comprising: a working electrode comprising carbon modified with a chemically sensitive redox active material; and a counter electrode, wherein the ratio of the surface area of the working electrode to the surface area of the counter electrode is from 1:10 to 10:1. Also provided is a pH sensor comprising: a working electrode comprising carbon modified with a chemically sensitive redox active material, and a counter electrode, wherein the area of the working electrode is from 500 ?m2 to 0.1 m2. The uses of these electrodes and sensors are also described.
    Type: Application
    Filed: September 23, 2013
    Publication date: March 27, 2014
    Applicant: ISIS INNOVATION LTD.
    Inventors: Sean P. McCormack, Richard G. Compton, Gregory George Wildgoose, Nathan Scott Lawrence
  • Publication number: 20140073815
    Abstract: This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid ? protein.
    Type: Application
    Filed: May 6, 2013
    Publication date: March 13, 2014
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Yuusuki TAMURA, Shinji SUZUKI, Yukio TADA, Shuji YONEZAWA, Chiaki FUJIKOSHI, Sae MATSUMOTO, Yuuji KOORIYAMA, Tatsuhiko UENO
  • Publication number: 20130289076
    Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I) as described and defined herein, and their use in therapy, including, e.g., the treatment or prevention of cancer.
    Type: Application
    Filed: October 7, 2011
    Publication date: October 31, 2013
    Inventors: Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe, Marc Murtinell Pedemonte, Alberto Ortega Muñoz, Núrla Valls Vidal
  • Patent number: 8557147
    Abstract: The present disclosure provides a chemiluminescent composition where the chemiluminescent substrate is 1,2-dioxetane, which contains 1,2-dioxetane and an alkyl dimethyl benzyl quaternary ammonium salt having the structure of general formula I. The present disclosure also provides an enhancing reagent and methods for enhancing chemiluminescence of 1,2-dioxetane, where the enhancing reagent contains an alkyl dimethyl benzyl quaternary ammonium salt having the structure of general formula I.
    Type: Grant
    Filed: June 29, 2011
    Date of Patent: October 15, 2013
    Assignee: Shenzhen Mindray Bio-Medical Electronics Co., Ltd.
    Inventors: Chungen Qian, Yuping Zhang
  • Publication number: 20130245276
    Abstract: The present invention relates to a process for preparing primary amines comprising the process steps A) provision of a solution of a primary alcohol in a fluid, nongaseous phase, B) contacting of the phase with free ammonia and/or at least one ammonia-releasing compound and a homogeneous catalyst and optionally C) isolation of the primary amine formed in process step B), characterized in that the volume ratio of the volume of the liquid phase to the volume of the gas phase in process step B is greater than 0.05 and/or in that process step B is carried out at pressures greater than 10 bar.
    Type: Application
    Filed: December 7, 2011
    Publication date: September 19, 2013
    Applicant: Evonik Degussa GmbH
    Inventors: Florian Klasovsky, Jan Christoph Pfeffer, Thomas Tacke, Thomas Haas, Matthias Beller, Angela Koeckritz, Jens Deutsch, Andreas Martin, Sebastian Imm
  • Publication number: 20130217910
    Abstract: The present invention relates to a process for the preparation of substituted N-(benzyl)cyclopropanamines of the general formula (II) starting from N-[(aryl)methylene]cyclopropanamine derivatives. The present invention further provides the N-[(arypmethylene]cyclopropanamine derivatives used as starting compounds in this process according to the invention, and their use for the preparation of substituted N (benzyl)cyclopropanamines.
    Type: Application
    Filed: November 4, 2011
    Publication date: August 22, 2013
    Inventors: Norbert Lui, Wahed Ahmed Moradi, Thomas Norbert Muller
  • Publication number: 20130217877
    Abstract: The present invention discloses novel aromatic ketone compounds with functional substiution groups at para- or meta positions which can be used as photo-initiators or effective components of photo-initiator mixtures for the photopolymerizations of ethylenically unsaturated systems. The preparation of these compounds is also disclosed.
    Type: Application
    Filed: November 4, 2011
    Publication date: August 22, 2013
    Applicant: SHENZHEN UV-CHEMTECH CO., LTD
    Inventors: Yongbo Zhang, Yanchao Wang, Yapeng Wang, Huaihai Song, Zhigang Wang
  • Patent number: 8450528
    Abstract: Process for the preparation of 2,2-difluoroethylamine of the formula (I) CHF2CH2NH2??(I) comprising the stages (i) and (ii): stage (i): reaction of 2,2-difluoro-1-haloethane of the general formula (II) CHF2—CH2Hal??(II), with a benzylamine compound of the formula (III) in the presence of an acid scavenger, in which, in formula (II), Hal is chlorine, bromine or iodine, and, in the formulae (III), R1 is hydrogen or C1-C12-alkyl, and R2 is hydrogen, halogen, C1-C12-alkyl or C1-C6-alkoxy; stage (ii): catalytic hydrogenation of the N-benzyl-2,2-difluoroethanamine compound obtained in the stage (i) to give 2,2-difluoroethylamine of the formula (I) or a salt thereof.
    Type: Grant
    Filed: November 9, 2011
    Date of Patent: May 28, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Norbert Lui, Jens-Dietmar Heinrich, Christian Funke, Günter Schlegel, Thomas Norbert Müller
  • Patent number: 8445722
    Abstract: The present invention relates to a method for screening an anticancer compound and an anticancer compound screened using the method, and more particularly, to a method for screening an anticancer compound, the method comprising: culturing cancer cells expressing the oncogenic protein transmembrane 4 L6 family member 5 (TM4SF5), expressed as the polypeptide of SEQ ID NO: 2, treating the cancer cells with an anticancer candidate, and determining that the anticancer candidate is an anticancer substance when the candidate exhibits antagonistic activity against tumor formation and metastasis based on several events through the molecular mechanism of TM4SF5. The present invention also relates to chalcone compounds screened to have anticancer activity using the method, and an anticancer composition comprising the compound as an effective ingredient.
    Type: Grant
    Filed: December 7, 2007
    Date of Patent: May 21, 2013
    Assignees: Industry-Academic Cooperation Foundation Gyeongsang National University, Seoul National University Industry Foundation
    Inventors: Ki Hun Park, Jung Weon Lee, Young Bae Ryu, Hyung Won Ryu, Sin-Ae Lee
  • Patent number: 8425885
    Abstract: Certain novel substituted 3-(phenoxymethyl) benzyl amines and personal care compositions comprising such, which are particularly beneficial for skin lightening and achieving evenness of color, especially for face and underarm skin.
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: April 23, 2013
    Assignee: Conopco, Inc.
    Inventors: Jose Guillermo Rosa, Bijan Harichian, John Steven Bajor, Carol Annette Bosko, Diana Jean Drennan, John Chun-Sing Nip
  • Patent number: 8383859
    Abstract: The present application relates to novel methods for the preparation of primary, secondary and tertiary carbinamine compounds, particularly the preparation of compounds of formulae I, IV and VI, from a carbonyl compound of formula II in the presence of ammonia or an ammonium equivalent of the formula NH4+X?, by way of allylation, crotylation, arylation, reductive amination and catalytic hydrogenation.
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: February 26, 2013
    Inventors: Avinash N. Thadani, Bhartesh Dhudshia
  • Publication number: 20120329800
    Abstract: Administration of a monoamine oxidase inhibitor is useful in the prevention and treatment of muscle dystrophy. Methods and compositions for inhibiting the production of reactive oxygen species in a muscle cell overproducing reactive oxygen species are provided herein.
    Type: Application
    Filed: June 22, 2011
    Publication date: December 27, 2012
    Inventors: Paolo Bonaldo, Marcella Canton, Fabio DiLisa, Sara Menazza
  • Patent number: 8324429
    Abstract: The present invention provides N-methylethylcarbamino-3-[(S)-1-(methyl-[(S)-1-phenylethyl]amino)ethyl]phenyl ester represented by formula (II) and its preparation method. The present invention also provides (S)-1-(3-methoxyphenyl)-N-methyl-N—[(S)-1-phenylethyl]ethylamine and 3-[(S)-1-(methyl-[(S)-1-phenylethyl]amino)ethyl]phenol as intermediates of the compound represented by formula (II), and the use of the compound represented by formula (II) for preparing rivastigmine used for treating Alzheimer disease.
    Type: Grant
    Filed: January 10, 2008
    Date of Patent: December 4, 2012
    Assignees: Shanghai Institute of Pharmaceutical Industry, Zhejian Hisun Pharmaceutical Co., Ltd.
    Inventors: Fuli Zhang, Meng Hu, Meihua Xie, Anping Lai, Rentong Sun, Daoxin Chen, Rusheng Bao, Hua Bai
  • Publication number: 20120283249
    Abstract: The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.
    Type: Application
    Filed: June 17, 2009
    Publication date: November 8, 2012
    Inventors: Roman Lopez, Séverine Hebbe, Daniel Gillet, Julien Barbier
  • Publication number: 20120251492
    Abstract: Provided are a triterpene derivative represented by a general formula (I), a pharmaceutically acceptable salt thereof, and an agent for preventing or treating chronic hepatitis C comprising the triterpene derivative or the salt as an active ingredient: [in the formula (I), R1 represents a carboxyl group, a hydroxymethyl group, —CH2OSO3H, or and R2 represents —OR3 or —O— (CH2) m-OR4, where R3 represents a benzyl group which may be substituted with a hydroxymethyl group, a dimethylaminomethyl group, a phenylaminomethyl group, a morpholinomethyl group, a carboxyl group, or a formyl group, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or a hydroxy C1-6 alkyl group, R4 represents a phenyl group which may be substituted with a carboxyl group, and m represents an integer of 1 to 3, with the proviso that a case where R1 is —CH2OH, and R3 is a C1-6 alkyl group, a C2-6 alkenyl group, or a benzyl group is excluded].
    Type: Application
    Filed: December 15, 2010
    Publication date: October 4, 2012
    Applicant: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Makoto Ishikawa, Shigeki Suzuki, Makoto Aoki, Nobuto Minowa, Kokichi Suzuki
  • Patent number: 8242264
    Abstract: The present invention relates to a process for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine and the intermediates thereof. The present invention provides a compound represented by formula I and a compound represented by formula II, and processes for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine by using the compound represented by formula I, the compound represented by formula II and o-nitrobenzaldehyde. The invention has the advantages of the shorter synthesis steps, easily available raw materials and simple operation. Moreover, the process is economic and safe by avoiding the use of expensive and dangerous lithium aluminum hydride.
    Type: Grant
    Filed: May 22, 2008
    Date of Patent: August 14, 2012
    Assignees: Topharman Shanghai Co., Ltd., Weifang Tehua Chemical Co., Ltd.
    Inventors: Fuqiang Zhu, Haihong Li, Wenzhong Wang, Hui Zhang, Jingshan Shen
  • Publication number: 20120196819
    Abstract: Compositions and methods for the treatment and control of various conditions in an animal which comprises administering to said animal an effective amount of a immediate release composition of about 0.5% to 50% wt/wt of active ingredient together with excipients to a total of about 100%, wherein said compositon dissolves in a relatively short period of time, e.g., 75 seconds or less, 5 seconds or less, or 3 seconds or less, upon administration to said animal.
    Type: Application
    Filed: January 4, 2012
    Publication date: August 2, 2012
    Applicant: NEWMARKET PHARMACEUTICALS LLC
    Inventors: David ROCK, Mark RIDALL
  • Patent number: 8227643
    Abstract: This invention relates to bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable salts and their use in the modulation of Sirtuin 1 (Sirt1) and there use in neuroprotection for subject suffering from neurodegenerative diseases such as Alzheimer's disease, Huntington's disease, Amyotrophic lateral sclerosis, frontotemporal dementia, Parkinson's disease, including Parkinson's plus diseases such as multiple system atrophy, progressive supranuclear palsy, corticobasal degeneration and dementia with Lewy bodies, and in the manufacture of medicaments for such Sirt1 modulation and neuroprotection.
    Type: Grant
    Filed: January 12, 2010
    Date of Patent: July 24, 2012
    Assignee: ProteoTech, Inc.
    Inventors: Alan D. Snow, Qubai Hu, Judy A. Cam
  • Patent number: 8143451
    Abstract: The present invention relates to a method for the preparation of tertiary carbinamine compounds from diastereoselective allylation and crotylation of N-unsubstituted imines derived from ketones.
    Type: Grant
    Filed: October 4, 2007
    Date of Patent: March 27, 2012
    Assignee: Kanata Chemical Technologies Inc.
    Inventors: Avinash N. Thadani, Bhartesh Dhudshia
  • Publication number: 20120059179
    Abstract: A new method of ortho-fluorination where an aryl C—H bond is directly replaced by an aryl C-F bond in a palladium-catalyzed reaction is provided. The method includes the ortho-fluorination of a triflamide protected benzylamine, a palladium catalyst, such as Pd(OTf)2, a fluorinating reagent such as N-fluoro-2,4,6-trimethylpyridinium triflate, and a ligand to promote the reaction such as N-methylpyrrolidinone (NMP).
    Type: Application
    Filed: April 2, 2010
    Publication date: March 8, 2012
    Applicant: The Scripps Research Insitiute
    Inventor: Jin-Quan Yu
  • Publication number: 20120001136
    Abstract: The present disclosure provides a chemiluminescent composition where the chemiluminescent substrate is 1,2-dioxetane, which contains 1,2-dioxetane and an alkyl dimethyl benzyl quaternary ammonium salt having the structure of general formula I. The present disclosure also provides an enhancing reagent and methods for enhancing chemiluminescence of 1,2-dioxetane, where the enhancing reagent contains an alkyl dimethyl benzyl quaternary ammonium salt having the structure of general formula I.
    Type: Application
    Filed: June 29, 2011
    Publication date: January 5, 2012
    Applicant: Shenzhen Mindray Bio-Medical Electronics Co., Ltd.
    Inventors: Chungen Qian, Yuping Zhang
  • Patent number: 8088955
    Abstract: This invention relates to novel alpha-substituted ?,?-unsaturated E- or Z-aldehydes, or isomer mixture thereof, of the formula (I) in which R1 and R2 may be identical or different and are each H or a hydrocarbon, in which the hydrocarbon may have one or more heteroatoms and R3 and R4 may be identical or different and are each a hydrocarbon, in which the hydrocarbon may have one or more heteroatoms, and R5 may be identical or different and is H or a hydrocarbon, in which the hydrocarbon may have one or more heteroatoms, to the use thereof, and to processes for their preparation. The invention further relates to the preparation of further intermediates for pharmaceuticals and to the preparation of the pharmaceuticals.
    Type: Grant
    Filed: July 11, 2008
    Date of Patent: January 3, 2012
    Assignee: DSM Fine Chemicals Austria NFG GmbH & Co. KG
    Inventors: Gerhard Steinbauer, Martina Kotthaus, Klaus Edegger, Stefaan Marie Andre De Wildeman, Henricus Martinus Maria Gerardus Straatman, Anna Maria Cornelia Francisca Castelijns, Andreas Hendrikus Maria De Vries
  • Patent number: 8084646
    Abstract: Disclosed is a process for producing 1-hydroxy-4-aminoadamantane.
    Type: Grant
    Filed: September 28, 2007
    Date of Patent: December 27, 2011
    Assignee: Shionogi & Co., Ltd.
    Inventor: Hideaki Watanabe
  • Publication number: 20110257334
    Abstract: A solvent that reversibly converts from a hydrophobic liquid form to hydrophilic liquid form upon contact with water and a selected trigger, e.g., contact with CO2, is described. The hydrophilic liquid form is readily converted back to the hydrophobic liquid form and water. The hydrophobic liquid is an amidine or amine. The hydrophilic liquid form comprises an amidinium salt or an ammonium salt.
    Type: Application
    Filed: October 28, 2010
    Publication date: October 20, 2011
    Inventors: Philip G. Jessop, Lam N. Phan, Andrew J. Carrier, Rui Resendes, Dominik Wechsler
  • Publication number: 20110230465
    Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
    Type: Application
    Filed: September 16, 2010
    Publication date: September 22, 2011
    Applicant: BOEHRINGER INGLEHEIM INTERNATIONAL GMBH
    Inventors: Timothy STAMMERS, Xavier BARBEAU, Pierre BEAULIEU, Megan BERTRAND-LAPERLE, Christian BROCHU, Paul J. EDWARDS, Pasquale FORGIONE, Cédrickx GODBOUT, Oliver HUCKE, Marc-André JOLY, Serge LANDRY, Olivier LEPAGE, Julie NAUD, Marc PESANT, Martin POIRIER, Maude POIRIER, Bounkham THAVONEKHAM
  • Publication number: 20110184174
    Abstract: The present invention provides a compound of formula (IV) wherein R is Cl, Br, NO2, OH or OR?, and R? is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (?)-1-[(4-chlorophenyl)-phenylmethyl]piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).
    Type: Application
    Filed: June 2, 2009
    Publication date: July 28, 2011
    Applicant: CIPLA LIMITED
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Maruti Ghagare, Sandip Vasant Chikhalikar
  • Publication number: 20110092739
    Abstract: The present invention relates to novel cationic lipids, transfection agents, microparticles, nanoparticles, and short interfering nucleic acid (siNA) molecules. The invention also features compositions, and methods of use for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity in a subject or organism. Specifically, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver biologically active molecules, such as antibodies (e.g., monoclonal, chimeric, humanized etc.
    Type: Application
    Filed: December 20, 2010
    Publication date: April 21, 2011
    Applicant: Sima Therapeutics, Inc.
    Inventors: Tongqian Chen, Chandra Vargeese, Kurt Vagle, Weimin Wang, Ye Zhang
  • Publication number: 20110065760
    Abstract: The present invention is related to a compound of the formula (I), (II), (III), (IV), (V): wherein Z1, Z2, Z3 and Z4 are each and independently selected from the group comprising C(O)—, —C(S)—, —C(O)—NR10—, —C(S)—NR11—, —C(N—CN)—NR12—, —S(O)—, —S(O2)—, —S(O)—NR13—, and S(O2)—NR14—, —O—, —S— or are each and individually absent; X is a spacer and is independently selected from the group comprising -M1-L1-K-L2-M2-, wherein Y.
    Type: Application
    Filed: November 23, 2009
    Publication date: March 17, 2011
    Applicant: Jerini AG
    Inventors: Jochen KNOLLE, Mike Schutkowski, Gerd Hummel, Thomas Tradler, Laurence Jobron, Claudia Christner, Dirk Scharn, Roland Stragies, Christoph Gibson, Frank Osterkamp
  • Patent number: 7893302
    Abstract: The present invention relates to novel cationic lipids, transfection agents, microparticles, nanoparticles, and short interfering nucleic acid (siNA) molecules. The invention also features compositions, and methods of use for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity in a subject or organism. Specifically, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver biologically active molecules.
    Type: Grant
    Filed: November 12, 2009
    Date of Patent: February 22, 2011
    Assignee: Sirna Therapeutics, Inc.
    Inventors: Tongqian Chen, Chandra Vargeese, Kurt Vagle, Weimin Wang, Ye Zhang
  • Publication number: 20110015240
    Abstract: The invention provides a thiazole derivative useful as a VAP-1 inhibitor, as well as a pharmaceutical agent for the prophylaxis or treatment of VAP-1 associated diseases and the like, a method of inhibiting VAP-1 in a subject, and a method for the prophylaxis or treatment of VAP-1 associated disease in a subject. The thiazole derivative is a compound represented by the formula (I): R1—NH—X—Y—Z wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: January 30, 2009
    Publication date: January 20, 2011
    Applicant: R-TECH UENO, LTD.
    Inventors: Tatsuya Matsukawa, Kazuhiro Masuzaki, Yosuke Kawai, Akiko Kawasaki, Akiko Akasaka, Makoto Takewaki
  • Publication number: 20100324064
    Abstract: The present invention relates to novel analogs of choline and methods of use or treatment of neurodegenerative disorders and/or conditions such as Parkinson's disease, Huntington disease, Alzheimer's disease and related disorders such as amyotrophic lateral sclerosis, spinal muscular atrophy, Friedrich's ataxia, Pick's disease, Bassen-Kornzweig syndrome, Refsom's disease, retinal degeneration, Cruetzfelt-Jacob syndrome or prion disease (mad cow disease), dementia with Lewy bodies, schizophrenia, paraneoplastic cerebellar degeneration and neurodegenerative conditions caused by stroke. The present compounds are effective to treat any neurological condition where acetylcholine transmission neurons and their target cells are affected.
    Type: Application
    Filed: July 22, 2010
    Publication date: December 23, 2010
    Applicants: Medical College of Georgia Research Institute, Universtiy of Georgia Research Foundation
    Inventors: Jerry J. BUCCAFUSCO, Alvin V. Terry, J. Warren Beach, Rammamohanna R. Jonnala
  • Patent number: 7851654
    Abstract: Disclosed relates to a novel chalcone derivative, pharmaceutically acceptable salt thereof, a method for preparing the same and uses thereof, the chalcone derivative being readily obtained through the steps of: reacting aminoacetophenone with sulfonylchloride under the presence of an appropriate salt; and reacting the compound prepared in the above step with hydroxybenzaldehide under the presence of an appropriate catalyst. The chalcone derivative of formula 1 in accordance with the present invention having strong enzyme inhibitory activities for glycosidase can be effectively used in preventing and treating various diseases induced by glycosidase, and the chalcone derivative of the invention having tyrosinase and melanin synthesis inhibitory activities can be effectively used as a skin-whitening compound.
    Type: Grant
    Filed: April 3, 2006
    Date of Patent: December 14, 2010
    Assignee: Industry-Academic Cooperation Foundation Gyeongsang National University
    Inventors: Ki Hun Park, Jin Hyo Kim, Woo Duck Seo, Young Bae Ryu, Hyung Won Ryu, Woo Song Lee, Sang Wan Gal
  • Publication number: 20100260750
    Abstract: Novel serotonin reuptake inhibitor compounds which are designed to exert serotonin uptake inhibitory activity in the peripheral system while being devoid of CNS activity, and a process of preparing same are disclosed. Further disclosed are pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with peripheral serotonin levels and/or activity, and/or platelet aggregation.
    Type: Application
    Filed: June 21, 2007
    Publication date: October 14, 2010
    Applicant: Ramot At Tel Aviv University Ltd
    Inventors: Moshe Rehavi, David Gurwitz
  • Publication number: 20100256358
    Abstract: The present invention relates to a process for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine and the intermediates thereof. The present invention provides a compound represented by formula I and a compound represented by formula II, and processes for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine by using the compound represented by formula I, the compound represented by formula II and o-nitrobenzaldehyde. The invention has the advantages of the shorter synthesis steps, easily available raw materials and simple operation. Moreover, the process is economic and safe by avoiding the use of expensive and dangerous lithium aluminum hydride.
    Type: Application
    Filed: May 22, 2008
    Publication date: October 7, 2010
    Applicants: TOPHARMAN SHANGHAI CO., LTD., WEIFANG TEHUA CHEMICAL CO., LTD.
    Inventors: Fuqiang Zhu, Haihong Li, Wenzhong Wang, Hui Zhang, Jingshan Shen
  • Publication number: 20100249024
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula 1, A1 and A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring.
    Type: Application
    Filed: June 14, 2010
    Publication date: September 30, 2010
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Joann Bohn, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Nazia Quraishi
  • Publication number: 20100234630
    Abstract: This invention relates to novel alpha-substituted ?,?-unsaturated E- or Z-aldehydes, or isomer mixture thereof, of the formula (I) in which R1 and R2 may be identical or different and are each H or a hydrocarbon, in which the hydrocarbon may have one or more heteroatoms and R3 and R4 may be identical or different and are each a hydrocarbon, in which the hydrocarbon may have one or more heteroatoms, and R5 may be identical or different and is H or a hydrocarbon, in which the hydrocarbon may have one or more heteroatoms, to the use thereof, and to processes for their preparation. The invention further relates to the preparation of further intermediates for pharmaceuticals and to the preparation of the pharmaceuticals.
    Type: Application
    Filed: July 11, 2008
    Publication date: September 16, 2010
    Inventors: Gerhard Steinbauer, Martina Kotthaus, Klaus Edegger, Stefaan Marie Andre De Wildeman, Henricus Martinus Maria Gerardus Straatman, Andreas Hendrikus Maria De Vries
  • Patent number: 7750193
    Abstract: The present invention relates to a process for preparing 2-alkylpolyisobutenylphenols and their Mannich adducts, to compositions obtainable by this process and to their use.
    Type: Grant
    Filed: February 1, 2005
    Date of Patent: July 6, 2010
    Assignee: BASF Aktiengesellschaft
    Inventors: Arno Lange, Helmut Mach, Hans Peter Rath, Dietmar Posselt, Anja Vinckier