Hydroxy, Bonded Directly To Carbon, Or Ether Containing (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/158)
  • Patent number: 9475757
    Abstract: The present invention relates to an improved process for synthesis of anti-Parkinson compound of formula (I) from commercially available (R)-benzyl glycidyl ether, wherein the compound obtained has enantiopurity greater than >98%. Formula (I) wherein R1 and R2 are each independently selected from hydrogen or halogen.
    Type: Grant
    Filed: May 2, 2014
    Date of Patent: October 25, 2016
    Assignee: Council of Scientific & Industrial Research
    Inventors: Murugan Muthukrishnan, Mohammad Mujahid
  • Patent number: 9193672
    Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of retinoids and retinoid-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
    Type: Grant
    Filed: July 15, 2009
    Date of Patent: November 24, 2015
    Inventor: Chongxi Yu
  • Publication number: 20150133465
    Abstract: The invention provides compounds of formula (I): wherein R1-R3, n, and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 14, 2015
    Inventors: Edmond J. LaVoie, Ajit Parhi, Daniel S. Pilch, Yongzheng Zhang, Malvika Kaul
  • Publication number: 20150119426
    Abstract: Disclosed are modulators of the human relaxin receptor 1, for example, of formula (I), wherein A, R1, and R2 are as defined herein, that are useful in treating mammalian relaxin receptor 1 mediated facets of human health, e.g., cardiovascular disease. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the disclosure, and a method for therapeutic intervention in a facet of mammalian health that is mediated by a human relaxin receptor 1.
    Type: Application
    Filed: March 15, 2013
    Publication date: April 30, 2015
    Inventors: Juan Jose Marugan, Jingbo Xiao, Marc Ferrer-Alegre, Catherine Chen, Noel Southall, Wei Zheng, Alexander Agoulnik, Irina Agoulnik
  • Patent number: 9012687
    Abstract: The present invention provides a process for isolating kukoamine by solid phase extraction using a polyamide or a derivative thereof as an adsorbent. Said process is convenient, economical and environmental-friendly, and obtains highly purified kukoamines with a high yield.
    Type: Grant
    Filed: April 24, 2014
    Date of Patent: April 21, 2015
    Assignee: City University of Hong Kong
    Inventors: Hon-Yeung Cheung, Yuan-Yuan Li, Rui Di
  • Publication number: 20150080472
    Abstract: The invention provides methods of treating Friedreich's ataxia using histone deacetylase inhibitors.
    Type: Application
    Filed: September 9, 2014
    Publication date: March 19, 2015
    Inventors: JOEL M. GOTTESFELD, ANN-KRISTIN JENSSEN, DAVID M. HERMAN, RYAN BURNETT, C. JAMES CHOU
  • Patent number: 8981149
    Abstract: The invention relates to compounds of formula (I), and the use thereof as a drug, particularly for the treatment of tumors associated with hyperactivation of the hedgehog protein signaling pathway, treatment of neurodegenerative diseases, treatment of diseases related to cerebral development (holoprosencephaly), for stem cell monitoring treatment of cerebrovascular accidents and cardiovascular accidents, treatment of diseases involving oligodendrocytes and diseases involving neurolemmocytes, for application thereof in vitro for modulating human or animal stem cell renewal, and for the treatment of diabetes. The invention also relates to pharmaceutical compositions having a compound of formula (I).
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: March 17, 2015
    Assignees: Centre National de la Recherche Scientifique, Universite de Strasbourg
    Inventors: Martial Ruat, Hélène Faure, Hermine Roudaut, Lucile Hoch, Angèle Schoenfelder, Maurizio Taddei, André Mann
  • Publication number: 20150065497
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: August 5, 2014
    Publication date: March 5, 2015
    Inventors: Sara S. Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D.J. Grootenhuis
  • Patent number: 8969620
    Abstract: The present invention relates to a process of manufacture of compounds of formula (B) wherein R1, R2 and R3 are as defined for compounds of formula (A), which process comprises hydrogenation of compounds of general formula (A). In particular, the present invention relates to an improved process for the manufacture of Lacosamide (LCM), (R)-2-acetamido-N-benzyl-3-methoxypropion-amide (B1), which is useful as an anticonvulsive drug.
    Type: Grant
    Filed: September 29, 2011
    Date of Patent: March 3, 2015
    Assignee: UCB Pharma GmbH
    Inventors: Alain Merschaert, Didier Bouvy, David Vasselin, Nicolas Carly
  • Patent number: 8957252
    Abstract: The present invention discloses novel process for the preparation of (2R)-2-acetamido-N- benzyl-3-methoxypropanamide of Formula I involving novel intermediates of Formula-XIX and Formula-XX.
    Type: Grant
    Filed: July 26, 2011
    Date of Patent: February 17, 2015
    Assignee: Indoco Remedies Limited
    Inventors: Mangesh Narayan Rajadhyaksha, Ranjeet Nair, Nilesh Balkrishna Shrigadi, Aditi Milind Panandikar
  • Patent number: 8946476
    Abstract: The present patent application relates to an alternative process for the preparation of amino derivatives. In particular, the present application relates to an improved process for the manufacture of Lacosamide (LCM), (R)-2-acetamido-N-benzyl-3-methoxypropion-amide, which is useful as an anticonvulsive drug. In a particular aspect, the present invention relates to a process of manufacture of optically enriched (R)-2-acetamido-N-benzyl-3-methoxypropion-amide (I) comprising resolution of 2-acetamido-N-benzyl-3-methoxypropion-amide (II).
    Type: Grant
    Filed: November 6, 2009
    Date of Patent: February 3, 2015
    Assignee: UCB Pharma GmbH
    Inventors: Didier Bouvy, Alain Merschaert, Véronique Pinilla, Joerg Hamann, Ralf Kanzler, Antoine Thomas
  • Patent number: 8946477
    Abstract: The invention relates to solid forms of the anti-epileptic agent lacosamide (I). The invention also relates to mixtures of solid forms of lacosamide. The invention further relates to mixtures of lacosamide enantiomers crystallized in a conglomerate Form and the use thereof in providing enantiomerically enriched lacosamide, preferably lacosamide enriched with the (R)-enantiomer of lacosamide.
    Type: Grant
    Filed: April 12, 2013
    Date of Patent: February 3, 2015
    Assignee: Medichem, S.A.
    Inventors: Ernesto Duran Lopez, Monica Benito Velez, Jordi Bosch i Lladó
  • Publication number: 20150031892
    Abstract: Sphingolipid metabolite mimetics and methods of synthesizing them are provided. The sphingolipid metabolite mimetics are shown to be effective at inducing apoptosis in various types of tumor cells. Further, the sphingolipid metabolite mimetics are shown to be effective at sensitizing multiple types of tumor cells to TRAIL-induced apoptosis. Formulations containing one or more sphingolipid metabolite mimetics and, optionally, one or more cell death receptor agonists are provided. Methods of treating cancer in a subject in need thereof are provided using one or more sphingolipid metabolite mimetics.
    Type: Application
    Filed: October 10, 2014
    Publication date: January 29, 2015
    Inventors: Feiyan Liu, Kebin Liu, Zhizhen Huang, Ping Wu
  • Patent number: 8933065
    Abstract: A first aspect of the invention is a compound (sometimes also referred to herein as an “active agent” or “active compound”) of Formula I or Ia: or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: January 13, 2015
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Harold L. Kohn, Christophe Salomé, Ki Duk Park, Elise Salomé-Grosjean
  • Publication number: 20150011621
    Abstract: Formylated xanthocillin analogs can be used in the treatment of neurodegenerative diseases. The analogs can be prepared synthetically, and at least some of the analogs can be obtained from a microorganism strain of the Penicillium chrysogenum species.
    Type: Application
    Filed: February 2, 2013
    Publication date: January 8, 2015
    Inventors: Maria del Carmen Ramos Martin, Sonia Campoy García, Javier Santos Burgos Muñoz, José Luis Adrio Fondevila, Javier Velasco Alvarez
  • Patent number: 8907132
    Abstract: Processes for preparing and purifying (R)-2-acetamido-N-benzyl-3-methoxy-propionamide of formula-1 and intermediates thereof are provided.
    Type: Grant
    Filed: February 9, 2011
    Date of Patent: December 9, 2014
    Assignee: MSN Laboratories Private Limited
    Inventors: Manne Satyanarayana Reddy, Sajja Eswaraiah, Aluru Srinivas, Revu Satyanarayana
  • Publication number: 20140357628
    Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof, with the proviso that the compound is no Tranilast.
    Type: Application
    Filed: June 27, 2014
    Publication date: December 4, 2014
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, David Stapleton, Steven Zammit, Darren James Kelly, Richard Ernest Gilbert, Henry Krum
  • Publication number: 20140350113
    Abstract: Described herein are small-molecule mimics of CD4, which both enter the Phe43 cavity and target Asp368 of gp120, the HIV-1 envelope protein. Also described herein are methods of using these compounds to inhibit the transmission or progression of HIV infection. These compounds exhibit antiviral potency greater than that of a known antiviral, NBD-556, with 100% breadth against clade B and C viruses. Importantly, the compounds do not activate HIV infection of CD4-negative, CCR5-positive cells, in contrast to NBD-556.
    Type: Application
    Filed: December 14, 2012
    Publication date: November 27, 2014
    Inventors: Joseph Sodroski, Judith M. LaLonde, Amos B. Smith, III, Peter D. Kwong, Young Do Kwon, David M. Jones, Alexander W. Sun, Joel R. Courter, Takahiro Soeta, Toyoharu Kobayashi, Amy M. Princiotto, Xueling Wu, John R. Mascola, Ame Schon, Emesto Freire, Navid Madani, Matthew Le-Khac, Wayne A. Hendrickson
  • Publication number: 20140342989
    Abstract: A first aspect of the invention is a compound (sometimes also referred to herein as an “active agent” or “active compound”) of Formula Ia, or more particularly Formula Ib: or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.
    Type: Application
    Filed: July 31, 2014
    Publication date: November 20, 2014
    Inventors: Harold L. Kohn, Christophe Salome, Elise Salome-Grosjean
  • Publication number: 20140323568
    Abstract: The present invention includes bis- and tris-benzamide compounds that block AR signaling and have activity against prostate cancer. Uses for these compounds, and pharmaceutical compositions containing the same, also are provided.
    Type: Application
    Filed: April 23, 2014
    Publication date: October 30, 2014
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Jung-Mo AHN, Ganesh RAJ
  • Publication number: 20140303384
    Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical compositions containing these novel compounds, and methods for the preparation of these compounds.
    Type: Application
    Filed: October 5, 2012
    Publication date: October 9, 2014
    Inventors: Brian A. Duclos, Richard Andrew Ewin, Paul D. Johnson, Timothy Allan Johnson, Graham M. Kyne, Derek James Sheehan, Susan Mary Kult Sheehan, Donald James Skalitzky, Rajendran Vairagoundar
  • Patent number: 8853439
    Abstract: The invention relates to improved processes for the preparation of lacosamide. The invention also relates to a novel intermediate useful in the preparation of lacosamide. The invention also relates to process for the purification of lacosamide.
    Type: Grant
    Filed: September 23, 2010
    Date of Patent: October 7, 2014
    Assignee: Cadila Healthcare Limited
    Inventors: Bipin Pandey, Kalpesh Shah
  • Patent number: 8853453
    Abstract: The present invention relates to processes for reducing impurities in lacosamide during the preparation of lacosamide. The invention provides processes for minimizing or removing impurities such as (2R)-2-(acetylamino)-3-(benzylamino)-3-oxopropyl acetate of Formula II or (2R)-2-propanoylamino-N-benzyl-3-methoxypropionamide of Formula III in lacosamide.
    Type: Grant
    Filed: January 31, 2011
    Date of Patent: October 7, 2014
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Hari Mohan Sriram, Mukesh Kumar Madhra, Mukesh Kumar Sharma
  • Patent number: 8853452
    Abstract: Compounds and their syntheses are disclosed herein. Compositions and pharmaceutical compositions comprising a compound are also described, and include compositions also comprising liposomes. Methods for the treatment of cancer in animals comprising administering a compound or a composition comprising a compound are also described.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: October 7, 2014
    Assignee: The Administrators of the Tulane Educational Fund
    Inventors: Barbara S. Beckman, Maryam Foroozesh, Jiawang Liu
  • Publication number: 20140296354
    Abstract: Described herein are the one-pot synthesis and characterization of a library of low molecular weight peptoid compounds that are able to form gels at room temperature. The compounds are synthesized from biologically-based starting materials, are biocompatible, and are resistant to degradation by proteases and peptidases.
    Type: Application
    Filed: April 1, 2014
    Publication date: October 2, 2014
    Applicant: OLD DOMINION UNIVERSITY RESEARCH FOUNDATION
    Inventors: Guijun WANG, Hari P. R. MANGUNURU
  • Publication number: 20140296572
    Abstract: The invention relates to improved processes for the preparation of lacosamide. The invention also relates to a novel intermediate useful in the preparation of lacosamide. The invention also relates to process for the purification of lacosamide.
    Type: Application
    Filed: June 12, 2014
    Publication date: October 2, 2014
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Bipin PANDEY, Kalpesh SHAH
  • Publication number: 20140288183
    Abstract: This invention relates to the use of bis- and tris-dihydroxyaryl compounds as well as sulfonamides, heteroaryls, tricycloalkyl and their analogs and pharmaceutically acceptable salts, for modulating tau aggregation and alleviating tauopathies, such as Alzheimer's disease (AD), Pick's disease (PiD), progressive supranuclear palsy (PSP), corticobasal degeneration (CBD) and familial frontotemporal dementia/Parkinsonism linked to chromosome 17 (FTDP-17), amyotrophic lateral sclerosis/Parkinsonism-dementia complex, argyrophilic grain dementia, dementia pugilistic, diffuse neurofibrillary tangles with calcification, progressive subcortical gliosis and tangle only dementia.
    Type: Application
    Filed: June 10, 2014
    Publication date: September 25, 2014
    Inventors: Alan D. Snow, Qubai Hu, Thomas Lake, Judy Cam
  • Publication number: 20140275269
    Abstract: Disclosed are 5-nitrobenzoate derivatives of Formula I, and the preparation method therefor, wherein R is referred to hydrogen (H), unsubstituted, mono-substituted, di-substituted or tri-substituted benzoyl moiety. 5-Nitrobenzoare derivatives of Formula I do not affect the platelet aggregation, possesses the inhibitory activity related to the tumor cell-induced platelet aggregation (TCIPA), and further specifically inhibits podoplanin-induced platelet aggregation. Therefore, 5-nitrobenzoates of the invention are applicable in its therapeutic use as the novel therapeutic agent in preventing tumor metastasis.
    Type: Application
    Filed: May 27, 2014
    Publication date: September 18, 2014
    Applicant: CHANG GUNG UNIVERSITY
    Inventors: Ching-Ping TSENG, Pei-Wen HSIEH, Yao-Wen CHANG
  • Publication number: 20140256817
    Abstract: Small-molecule scaffolds based on 1,2-diphenylacetylene that accurately replicate the spatial and angular projections of several side chains on both faces of an ?-helix, specifically the i and i+7 side chains on one face, and the i and i+2 side chains on the other. The amphipathic ?-helix mimetic can be used to disrupt disease-promoting protein-protein interactions that are mediated by ?-helices.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 11, 2014
    Applicant: UNIVERSITY OF MARYLAND, BALTIMORE
    Inventor: Steven FLETCHER
  • Patent number: 8829241
    Abstract: The invention describes a process for the purification of iodinated aryl compounds where the purification is performed by continuous crystallization of a crude product in a solvent with addition of anti-solvent. The continuous crystallization process is performed in one or more crystallizers at a temperature up to the boiling point of the content of the crystallizer.
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: September 9, 2014
    Assignee: GE Healthcare AS
    Inventors: Jan Cervenka, Khalid Hussain, Arne W. Aabye
  • Patent number: 8829033
    Abstract: A first aspect of the invention is a compound (sometimes also referred to herein as an “active agent” or “active compound”) of Formula Ia, or more particularly Formula Ib, or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: September 9, 2014
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Harold L. Kohn, Christophe Salomé, Elise Salomé-Grosjean
  • Publication number: 20140228441
    Abstract: The invention relates to compounds of formula (I), and the use thereof as a drug, particularly for the treatment of tumors associated with hyperactivation of the hedgehog protein signaling pathway, treatment of neurodegenerative diseases, treatment of diseases related to cerebral development (holoprosencephaly), for stem cell monitoring treatment of cerebrovascular accidents and cardiovascular accidents, treatment of diseases involving oligodendrocytes and diseases involving neurolemmocytes, for application thereof in vitro for modulating human or animal stem cell renewal, and for the treatment of diabetes. The invention also relates to pharmaceutical compositions having a compound of formula (I).
    Type: Application
    Filed: September 21, 2012
    Publication date: August 14, 2014
    Applicants: Centre National De La Recherche Scientifique, Universite De Strasbourg
    Inventors: Martial Ruat, Hélène Faure, Hermine Roudaut, Lucile Hoch, Angèle Schoenfelder, Maurizio Taddei, André Mann
  • Publication number: 20140221492
    Abstract: This invention relates to novel 2-amino-3-hydroxypropanoic acid derivatives and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an NMDA glycine-site antagonist.
    Type: Application
    Filed: March 20, 2014
    Publication date: August 7, 2014
    Inventor: Craig E. Masse
  • Patent number: 8796488
    Abstract: A novel process for the synthesis of Lacosamide using D,L-serine as starting material is described, where the methylation reaction of hydroxyl is carried out using an inexpensive base such as NaOH and an inexpensive alkylating agent, non-toxic and non-carcinogenic, such as methyl p-toluenesulfonate; the R enantiomer is isolated from the racemic mixture of Lacosamide after selective hydrolysis of the acetamide, salification of the racemic mixture with a chiral acid (HX*) in an organic solvent, resolution of the diastereoisomeric mixture, preferably by precipitation of the R enantiomer, and subsequent acetylation of the optically pure intermediate.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: August 5, 2014
    Assignee: Euticals S.p.A.
    Inventors: Alberto Bologna, Patrizia Castoldi, Domenico Vergani, Giorgio Bertolini
  • Patent number: 8772296
    Abstract: Benzamide derivatives of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, and n are as defined herein.
    Type: Grant
    Filed: May 31, 2007
    Date of Patent: July 8, 2014
    Assignee: Amgen Inc.
    Inventors: Jay P. Powers, Michael Degraffenreid, Lisa Julian, Jacob Kaizerman, Dustin McMinn, Yosup Rew, Daqing Sun, Xuelei Yan, Zhulun Wang, Felix Gonzalez Lopez De Turiso
  • Patent number: 8759582
    Abstract: Present invention relates to an improved and commercial process for the preparation of lacosamide ((R)-2-acetamido-N-benzyl-3-methoxypropanamide) of formula (I). Present process utilizes high purity crystalline solids of formulae (XXXII) and (XIII) as key intermediates. Lacosamide is indicated for the adjunctive treatment of partial onset seizures in patients aged at least 17 years.
    Type: Grant
    Filed: February 4, 2011
    Date of Patent: June 24, 2014
    Assignee: Natco Pharma Limited
    Inventors: Pulla Reddy Muddasani, Veerababu Madalapu, Venkaiah Chowdary Nannapaneni
  • Patent number: 8754259
    Abstract: The present invention provides synthetic routes for preparing various isomers of cyclohexane-based coolants, such as menthyl esters and menthanecarboxamide derivatives, in particular those substituted at the amide nitrogen, for example with an aromatic ring or aryl moiety. Such structures have high cooling potency and long lasting sensory effect, which make them useful in a wide variety of consumer products. One synthetic route involves a copper catalyzed coupling of a primary menthanecarboxamide with an aryl halide, such reaction working best in the presence of potassium phosphate and water. Using this synthetic route, specific isomers can be prepared including the menthanecarboxamide isomer having the same configuration as l-menthol and new isomers such as a neoisomer having opposite stereochemistry at the carboxamide (C-1) position. The neoisomer unexpectedly has potent and long lasting cooling effect.
    Type: Grant
    Filed: March 20, 2013
    Date of Patent: June 17, 2014
    Assignee: The Procter & Gamble Company
    Inventors: Kenneth Edward Yelm, Gregory Mark Bunke, John Christian Haught
  • Patent number: 8754124
    Abstract: The present invention includes bis- and tris-benzamide compounds that block AR signaling and have activity against prostate cancer. Uses for these compounds, and pharmaceutical compositions containing the same, also are provided.
    Type: Grant
    Filed: November 21, 2012
    Date of Patent: June 17, 2014
    Assignee: Board of Regents, The University of Texas System
    Inventors: Jung-Mo Ahn, Ganesh Raj
  • Patent number: 8748660
    Abstract: The present invention relates to the improved and efficient process for the synthesis of antiepileptic drug Lacosamide in high enantiopurity (>98% ee) and better yield. More particularly, the present invention relates to improved and efficient, cost effective process for synthesis of desired (R) isomer of Lacosamide starting from commercially available (S)-benzyl glycidyl ether.
    Type: Grant
    Filed: August 20, 2012
    Date of Patent: June 10, 2014
    Assignee: Council of Scientific & Industrial Research
    Inventors: Muthukrishnan Murugan, Mohammad Mujahid, Prashant Pramod Majumdar
  • Publication number: 20140142117
    Abstract: The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.
    Type: Application
    Filed: November 11, 2013
    Publication date: May 22, 2014
    Inventors: John H. van Duzer, Ralph Mazitschek, Walter Ogier, James E. Bradner, Guoxiang Huang, Dejian Xie, Nan Yu
  • Patent number: 8722881
    Abstract: A tetradendate amide based macrocyclic ligand and its Fe(III) complex which act as activators of hydrogen peroxide. The synthetic methodology to develop the ligands is new, simple and provides better yield for each step of the ligand synthesis. The Fe(III)-complexes and hydrogen peroxide together are can perform several environmentally benign oxidation reactions. Organic dye bleaching, bleaching of pulp and paper effluent and N-oxide synthesis may be performed using the newly developed catalyst and hydrogen peroxide. Alcohol oxidation and alkene epoxidation may also be performed using the catalysts and hydrogen peroxide.
    Type: Grant
    Filed: October 13, 2010
    Date of Patent: May 13, 2014
    Assignee: Board of Trustees of the University of Arkansas
    Inventors: Anindya Ghosh, Shane Z. Sullivan, Samuel L. Collom, Sharon Pulla
  • Publication number: 20140128463
    Abstract: Disclosed are amide compounds, preparation method and uses thereof, specifically, the compounds represented by formula I or pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, Q, X and n are defined as in the description. Also disclosed are a method for preparing the compounds of formula I, a composition containing the compounds, and the uses of the same in the preparation of medicaments for regulating blood lipid and/or preventing gallstone. The compounds of formula I disclosed in the present invention have stability in vitro, good solubility in the pharmaceutical organic solvents and favorable bioavailability in animals.
    Type: Application
    Filed: June 25, 2012
    Publication date: May 8, 2014
    Applicants: China State Institute of Pharmaceutic Industry, Shanghai Institute of Pharmaceutical Industry
    Inventors: Zhenpeng Yu, Gouping Wang, Zhen Zhang, Minyu Liu, Xiaoling Huang, Ying Liu, Lin Xiao, Li Cai, Xuejun Wu, Yifang Deng, Mianli Pan, Renhai Chen, Shenrong Tang, Quanhai Liu
  • Patent number: 8710264
    Abstract: A compound of general formula (I) wherein, R11, R12, R13, R14, R15, W, Y, R1, R2, R3, R4, R5, and R6 take various meanings for use in the treatment of cancer.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: April 29, 2014
    Assignee: Pharma Mar, S.A.
    Inventors: Alberto Rodríguez Vicente, Maria Garranzo García-Ibarrola, Carmen Murcia Pérez, Francisco Sánchez Sancho, Maria del Carmen Cuevas Marchante, Cristina Mateo Urbano, Isabel Digón Juárez
  • Patent number: 8704001
    Abstract: This invention relates to novel 2-amino-3-hydroxypropanoic acid derivatives and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an NMDA glycine-site antagonist.
    Type: Grant
    Filed: September 15, 2009
    Date of Patent: April 22, 2014
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Craig E. Masse
  • Publication number: 20140094521
    Abstract: The objective of the present invention is to provide a new compound which is effective in treating blood cancer, particularly multiple myeloma, and which is also effective in suppressing an SP cell, i.e. Side Population Cell, which is a cause of recurrence of cancer. The compound according to the present invention is a novel compound which has the specific benzylamine structure.
    Type: Application
    Filed: May 23, 2012
    Publication date: April 3, 2014
    Applicant: THE UNIVERSITY OF TOKUSHIMA
    Inventors: Daisuke Tsuji, Kohji Itoh, Akira Otaka, Akira Shigenaga, Masahiro Abe, Masahiro Hiasa
  • Publication number: 20140051678
    Abstract: The present invention relates to compounds which are inhibitors of the activity of Complex III of the mitochondrial electron transport chain and pharmaceutical compositions comprising said compounds alone or in combination with other active agents. The present invention further relates to use of the compounds of the invention as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit. More particularly the present invention relates to the use of the compounds of the invention in a method of treating and/or preventing cancers presenting tumor-initiating cells.
    Type: Application
    Filed: November 24, 2011
    Publication date: February 20, 2014
    Applicant: STEMERGIE BIOTECHNOLOGY SA
    Inventors: Virginie Clement-Schatlo, Thomas Fessard, Riccardo Cribiu
  • Publication number: 20140039059
    Abstract: The use of substances capable of inhibiting one or more enzymes of the histone deacetylase family (histone deacetylase inhibitors) for the therapeutic treatment of Philadelphia-negative myeloproliferative syndromes (polycythemia vera, essential thrombocythemia or idiopathic myelofibrosis) is described. The dosage of the above-mentioned substances is significantly lower than that normally used for the care of other tumour syndromes and may be from 10 to 150 mg/day/patient.
    Type: Application
    Filed: October 7, 2013
    Publication date: February 6, 2014
    Applicant: ITALFARMACO SPA
    Inventors: Tiziano Oldoni, Paolo Mascagni, Alessandro Rambaldi, Tiziano Barbui
  • Patent number: 8633228
    Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(?G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: January 21, 2014
    Assignee: Mitsui Chemicals Agro, Inc.
    Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
  • Publication number: 20140018549
    Abstract: Compounds of Formula I are useful for the treatment of anxiety disorders such as generalized anxiety disorder (GAD), panic attack, post traumatic stress disorder (PTSD), obsessive compulsive disorder (OCD) and social phobias, wherein: A is chosen from: aryl or heteroaryl, A being optionally substituted with up to 5 independently-selected groups R8; R1 is chosen from: alkyl or haloalkyl; R2 is chosen from: H, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7; R3, R4 and R5 are independently chosen from: H or alkyl; R6 and R7 are independently chosen from: H or alkyl; and R8 is chosen from: OH, CN, halo, alkyl, alkoxy, haloalkyl, haloalkoxy, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7.
    Type: Application
    Filed: April 25, 2013
    Publication date: January 16, 2014
    Applicant: NPS Pharmaceuticals, Inc.
    Inventor: NPS Pharmaceuticals, Inc.
  • Publication number: 20140011882
    Abstract: Disclosed are 5-nitrobenzoate derivatives of Formula I, and the preparation method therefor, wherein R is referred to hydrogen (H), unsubstituted, mono-substituted, di-substituted or tri-substituted benzoyl moiety. 5-Nitrobenzoate derivatives of Formula I do not affect the platelet aggregation, possesses the inhibitory activity related to the tumor cell-induced platelet aggregation (TCIPA), and further specifically inhibits podoplanin-induced platelet aggregation. Therefore, 5-nitrobenzoates of the invention are applicable in its therapeutic use as the novel therapeutic agent in preventing tumor metastasis.
    Type: Application
    Filed: November 28, 2012
    Publication date: January 9, 2014
    Applicant: CHANG GUNG UNIVERSITY
    Inventors: CHING-PING TSENG, PEI-WEN HSIEH, YAO-WEN CHANG