Abstract: The present invention is concerned with derivatives of 3,5-diphenyl-diazole compounds, which are effective therapeutic agents for use in treating diseases linked to protein aggregation and/or neurodegenerative diseases such as Alzheimer's disease (AD), Parkinson's disease (PD), and Transmissible spongiform encephalopathies (TSEs) such as Creutzfeldt-Jakob disease (CJD). The therapeutic effect is caused by the inhibition of the protein aggregation in the affected tissue, such as the brain. 3,5-Diphenyl-diazole derivatives have been shown to be effective in inhibiting aggregation of proteins but are also characterized by their poor solubility in aqueous solutions. The prodrugs of the invention are modified 3,5-diphenyl-diazole derivatives, which are characterized by their improved solubility in aqueous solutions, and by their increased bioavailability.
Type:
Grant
Filed:
December 14, 2016
Date of Patent:
June 4, 2019
Assignee:
Max-Planck-Gesellschaft zur Forderung
Inventors:
Armin Giese, Felix Schmidt, Christian Griesinger, Andrei Leonov, Sergey Ryazanov
Abstract: Flame resistant fabrics and garments that have improved resistance to pilling and/or abrasion are disclosed. The fabrics, the fibers or yarns that make up the fabrics, or garments made from the fabrics are treated with a finish composition that is applied to the fibers, yarns, fabrics, or garments and then cured. The finish composition increases the resistance to pilling and/or abrasion of the fibers, yarns, fabrics, or garments. The finish composition includes a polymeric abrasion resistance aid, an alkylfluoropolymer, a polyethylene, and a wetting agent.
Abstract: Ion conductive organic-inorganic composite particles are particles that have an organic group on the surface of inorganic particles and have at least a configuration that does not allow the inorganic particles to contact with each other by steric hindrance of the organic group, the organic group containing an ion conductive group.
Abstract: Preparation and in vitro and in vivo characterization of novel forms of active pharmaceutical ingredients, suitable for pharmaceutical compositions in drug delivery systems for humans.
Type:
Grant
Filed:
August 6, 2012
Date of Patent:
October 27, 2015
Assignee:
THAR PHARMACEUTICALS, INC.
Inventors:
Mazen Hanna, Ning Shan, Miranda L. Cheney, David R. Weyna, Raymond Houck
Abstract: A process for imparting flame resistance and the flame resistant fabrics produced by such process are provided. The process for imparting flame resistant properties involves treating a target fabric with one or more flame retardant chemicals (and, preferably, a softening agent) and then curing the treated fabric to durably affix the flame retardant to the fabric. In many cases, it may be desirable to subject the treated fabric to mechanical face finishing to increase softness. Optionally, stain release agents, soil repellent agents, permanent press resins, and the like may be added to the bath of flame retardant chemicals, eliminating the need for one or more additional manufacturing processes. Alternately, soil repellent agents may be applied to only one side of the treated fabric after the application of the flame retardant chemicals. The present fabrics exhibit improved performance and tear strength, even after repeated launderings, as compared to conventionally treated fabrics.
Abstract: A reactive ionic liquid to be used as an ionic component that is contained in an ion-containing layer in a transducer arranged in contact with a high-resistance layer as a dielectric layer of the transducer, and is restrained from migrating from the ion-containing layer to the high-resistance layer on application of a voltage is provided. The reactive ionic liquid comprises an ion pair that consists of an anion and a cation. (a) The cation (a1) is an imidazolium or quaternary ammonium cation, and (a2) comprises a reactive group that consists of an alkoxysilyl or phosphonate group. (b) The anion (b1) is a sulfonate, sulfonylimide, or nitrobenzoate anion.
Type:
Application
Filed:
December 17, 2014
Publication date:
May 21, 2015
Applicants:
SUMITOMO RIKO COMPANY LIMITED, KYUSHU UNIVERSITY
Abstract: The present invention relates to a radiotracer precursor for imaging of hypoxic tissues, a radiotracer and a method for preparing the same. The radiotracer precursor, BANI, includes a nitroimidazole functional group with a feature of retention in hypoxic tissues and a bifunctional ligand able to complex with radioisotopes. Thus BANI can be used to produce radiotracers retained in hypoxic tissues and the radiotracers are applied to medical imaging of malignant tumor with hypoxic layer.
Type:
Grant
Filed:
July 22, 2013
Date of Patent:
May 5, 2015
Assignee:
Atomic Energy Council—Institute of Nuclear Energy Research
Abstract: Biocidally active cationic analogs of N-halamine having two biocidally active groups covalently bonded together in a single molecule and having general Formula (I). Compounds of Formula (I), and precursors thereof, can be in solution form immobilized onto a substrate via physical coating or covalent chemical bonding to functionalize surfaces or added into materials as additives so as to render them biocidal. The biocidal solutions and substrates comprising the compounds or precursors of the present invention can then be used to inactivate pathogenic microorganisms.
Abstract: Provided is a two-photon fluorescent probe, and more particularly, a two-photon fluorescent probe which is one or more selected from compounds represented by Formulae 1 and 2, a method for manufacturing the same, and an imaging method of zinc ions within the mitochondrion using the same. Since two probes are introduced into one molecule, the two-photon fluorescent probe of the present invention can selectively dye the mitochondria, simultaneously with reacting with zinc ions, thereby generating intense fluorescence. Thus, the two-photon fluorescent probe of the present invention can be used for the imaging of zinc ion distribution and activation within the mitochondrion in living cells or intact biological tissues.
Type:
Grant
Filed:
October 18, 2011
Date of Patent:
April 14, 2015
Assignee:
AJOU University Industry-Academic Cooperation Foundation
Abstract: Novel solution complexes of zoledronic acid are described which give rise to improved properties of zoledronic acid. The invention includes aqueous solution and molecular complexes of zoledronic acid with and optical isomers of asparagine, histidine, arginine and proline as well as pharmaceutical complexes containing them and methods of treatment using them.
Type:
Grant
Filed:
July 30, 2010
Date of Patent:
March 17, 2015
Assignee:
Thar Pharmaceuticals, Inc.
Inventors:
Mazen Hanna, Ning Shan, Miranda Cheney, David Weyna
Abstract: The present invention discloses compounds according to Formula I: wherein R1 is as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment cystic fibrosis by administering a compound of the invention.
Type:
Application
Filed:
August 5, 2014
Publication date:
February 12, 2015
Inventors:
Steven Emiel VAN DER PLAS, Hans KELGTERMANS, Sébastien Jean Jacques Cédric DROPSIT MONTOVER, Sébastien Laurent Xavier MARTINA, Martin James Inglis ANDREWS
Abstract: A new crystalline form of the Zoledronic acid, characterized by its X-rays diffractogram as well as by its spatial atomic distribution in the red crystalline and its curves of thermal analysis. There is also included a method to obtain this crystalline form, which includes the synthesis of the corresponding acid and the pharmaceutical composition this crystalline form comprises.
Type:
Grant
Filed:
February 4, 2010
Date of Patent:
February 10, 2015
Assignee:
Gador S.A.
Inventors:
Rafael Alberto Labriola, Dora Graciela Tombari, Adriana Vechhioli
Abstract: Therapeutic compositions comprising at least two substituted imidazole or imidazolium compounds may be used for a number of medical purposes, such as treatment of undesirable conditions or diseases, including disease or conditions related to bone, cancer, and/or pain.
Abstract: The present disclosure relates to therapeutic compositions comprising substituted imidazoliums having multiple acidic groups. The compounds may be used to treat diseases or conditions such as those associated with bone, cancer, or pain. Compositions, dosage forms, methods of treating diseases or conditions, methods of preparation, and other related embodiments related to the substituted imidazoliums are also described herein.
Abstract: Provided is a highly safe and effective compound represented by the following general formula (1) or a salt thereof which acts on tubulin and has an anticancer effect, wherein Ar represents an aryl group or a heteroaryl group; Z1, Z2, Z3, and Z4 each independently represent CH, a nitrogen atom, an oxygen atom, or a sulfur atom; R1 represents a hydrogen atom, a halogen atom, an alkyl group, or the like; R2 and R3 are the same or different and each represent a hydrogen atom, a halogen atom, a carboxyl group, or the like; n units of R4 are the same or different and each represent a hydrogen atom, an alkyl group, or the like; and n represents a number of 0 to 4.
Abstract: Therapeutic compositions comprising at least two substituted imidazole or imidazolium compounds may be used for a number of medical purposes, such as treatment of undesirable conditions or diseases, including disease or conditions related to bone, cancer, and/or pain.
Abstract: The disclosure is directed to: (a) phosphacycle ligands; (b) methods of using such phosphacycle ligands in bond forming reactions; and (c) methods of preparing phosphacycle ligands.
Type:
Grant
Filed:
July 15, 2011
Date of Patent:
September 23, 2014
Assignee:
AbbVie Inc.
Inventors:
Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
Type:
Grant
Filed:
March 18, 2014
Date of Patent:
September 9, 2014
Assignee:
Allergan, Inc.
Inventors:
Phong X. Nguyen, Todd M. Heidelbaugh, John R. Cappiello
Abstract: The technology of this invention concerns a method for the manufacture of hydroxy diphosphonic acids containing an amino moiety. The method specifically involves reacting a liquid P4O6 with an aminocarboxylic acid in the presence of a sulfonic acid. The aminocarboxylic acid is selected from 3 structurally different compounds. The amino hydroxy diphosphonic acids can be synthesized with high selectivity and purity and the unreacted starting raw materials can easily and conveniently be recirculated.
Type:
Grant
Filed:
October 4, 2010
Date of Patent:
July 15, 2014
Assignee:
Straitmark Holding AG
Inventors:
Samuel Corentin Cogels, David Lemin, Patrick Notté
Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
Type:
Grant
Filed:
February 11, 2013
Date of Patent:
June 3, 2014
Assignee:
Allergan, Inc.
Inventors:
Todd M. Heidelbaugh, Phong X. Nguyen, John Cappiello
Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
Type:
Grant
Filed:
November 10, 2005
Date of Patent:
May 6, 2014
Assignee:
Bristol-Myers Squibb Company
Inventors:
Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek J. Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
Abstract: The present invention relates to a method for the diagnosis or the prognosis of metastasis in prostate cancer which comprises determining if the c-MAF gene is amplified in a primary tumor sample. Likewise, the invention also relates to a method for the diagnosis or the prognosis of metastasis in prostate cancer, as well as to a method for determining the tendency to develop bone metastasis with respect to metastasis in other organs, which comprise determining the c-MAF expression level. Finally, the invention relates to the use of a c-MAF inhibitor as therapeutic target for treating the prostate cancer.
Abstract: Preparation, in-vitro and in vivo characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl)phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.
Abstract: Preparation, in-vitro and in vivo characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl)phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.
Abstract: The present invention relates to a method for the diagnosis or the prognosis of metastasis in breast cancer which comprises determining if the c-MAF gene is amplified in a primary tumor sample. Likewise, the invention also relates to a method for the diagnosis or the prognosis of metastasis in ER? breast cancer, as well as to a method for determining the tendency to develop bone metastasis with respect to metastasis in other organs, which comprise determining the c-MAF gene expression level. Finally, the invention relates to the use of a c-MAF inhibitor as therapeutic target for treating the ER? breast cancer metastasis.
Type:
Application
Filed:
October 5, 2011
Publication date:
February 27, 2014
Applicants:
Fundació Privada Institució Catalana De Recerca I Estudis Avançats, Fundació Privada Institut De Recerca Biomèdica
Inventors:
Roger Gomis, Maria Tarragona, Anna Arnal, Milica Pavlovic
Abstract: The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.
Type:
Grant
Filed:
November 22, 2006
Date of Patent:
February 4, 2014
Assignee:
University of South Florida
Inventors:
Said M. Sebti, Srikumar Chellappan, Nicholas James Lawrence
Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.
Type:
Application
Filed:
August 16, 2013
Publication date:
December 19, 2013
Applicants:
Icagen, Inc., Pfizer Limited
Inventors:
Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
Abstract: In one aspect, the invention relates to compounds having the formula XII: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
Abstract: The invention relates to the use of cyclovinyl phosphine compounds in the form of complexes with copper, as catalysts for reactions leading to the formation of carbon-carbon and carbon-heteroatom bonds. The invention also relates to complexes of copper with at least one cyclovinyl phosphine, as well as to the method for creating a carbon-carbon or a carbon-heteroatom bond catalysed by a cyclovinyl phosphine/copper complex.
Type:
Grant
Filed:
September 26, 2008
Date of Patent:
December 10, 2013
Assignee:
Centre National de Recherche Scientifique (C.N.R.S.)
Inventors:
Marc Taillefer, Hamid Kaddouri, Fouad Ouazzani
Abstract: Preparation and characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl) phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.
Type:
Application
Filed:
November 23, 2011
Publication date:
November 28, 2013
Applicant:
THAR PHARMACEUTICALS, INC.
Inventors:
Mazen Hanna, Ning Shan, Miranda L. Cheney, David R. Weyna, Paul K. Isbester, Xufeng Sun
Abstract: The invention relates to a process for modifying an inorganic substrate, directed toward giving it antimicrobial properties, said process consisting in grafting in one or more steps onto a surface of said substrate groups with intrinsic antimicrobial properties or groups capable of releasing species with antimicrobial properties. The grafting is performed by means of an organophosphorus coupling agent. A subject of the invention is similarly a substrate obtained by this process, as well as diverse uses of such a substrate.
Type:
Grant
Filed:
December 21, 2006
Date of Patent:
November 19, 2013
Assignees:
Centre National de la Recherche Scientifique, Universite Montpellier II Sciences et Techniques du Languedoc
Abstract: Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions. Although an oral dosage form with enhanced bioavailability with respect to the bisphosphonate compound can be used, the treatment can also be effective using an oral dosage form that includes a bisphosphonate compound, such as zoledronic acid, wherein the bioavailability of the bisphosphonate is unenhanced, or is substantially unenhanced.
Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.
Abstract: Provided are a nanoparticle/dispersant complex having excellent dispersibility and long-term stability in a dispersion medium, a production method therefor, and a nanoparticle dispersion liquid and a nanoparticle/matrix-material complex which are colorless and transparent even at high concentrations. In the nanoparticle/dispersant complex, a nanoparticle is covered with a dispersant containing a heterocyclic cationic group and one of an oxo acid group containing a sulfur atom or a phosphorus atom and an anion moiety of the oxo acid group; in the nanoparticle dispersion liquid, the nanoparticle/dispersant complex is dispersed into a dispersion medium; in the nanoparticle/matrix-material complex, the nanoparticle/dispersant complex is dispersed into a matrix material; and the production method for a nanoparticle/dispersant complex comprises forming, under a presence of the dispersant, a nanoparticle covered with the dispersant from a nanoparticle precursor.
Abstract: A process for the preparation of [1-hydroxy-2-(1H-imidazol-1-yl)-ethylidene]bisphosphonic acid consists of the reaction of aqueous solution of 1H-imidazole-1-acetic acid hydrochloride with phosphorus trichloride followed by removal of the excess of phosphorus trichloride, addition of water and hydrolysis of the reaction products. In order to isolate the product the post-reaction mixture is filtered and the anti-solvent is added to the aqueous filtrate in order to crystallize out [1-hydroxy-2-(1H-imidazol-1-yl)-ethylidene]bisphosphonic acid monohydrate.
Type:
Grant
Filed:
October 17, 2009
Date of Patent:
September 3, 2013
Assignee:
Zaklady Farmaceutyczne Polpharma SA
Inventors:
Leszek Dembkowski, Mariusz Krzyzanowski, Robert Rynkiewicz, Roman Szramka, Zdzislaw Roznerski, Daniel Zyla, Janusz Rachon, Slawomir Makowiec
Abstract: This invention relates to biomaterials, said biomaterials for use in methods to control and/or induce bone growth. Particularly, the invention relates to macroporous calcium phosphate biomaterials pre-loaded with certain amounts of osteoclastic activity inhibitors for use in methods to control and/or induce bone growth in primates.
Type:
Application
Filed:
March 18, 2013
Publication date:
August 22, 2013
Applicants:
UNIVERSITY OF WITWATERSRAND, JOHANNESBURG, MEDICAL RESEARCH COUNCIL OF SOUTH AFRICA
Inventors:
Medical Research Council of South Africa, University of Witwatersrand, Johannesburg
Abstract: The invention provides in part, conjugate compounds. The invention also provides synthesis methods for making the compounds, and uses of the compounds.
Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
Abstract: The present invention relates to drug derivatives and linkers. The invention specifically relates to compounds and methods of phosphonates and linkers, that are useful as carriers for imaging agents and useful in the treatment of various bone diseases.
Type:
Grant
Filed:
April 16, 2008
Date of Patent:
April 30, 2013
Assignee:
University of Southern California
Inventors:
Charles E. McKenna, Boris A. Kashemirov, Joy Lynn F. Bala
Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
Abstract: The present invention relates to amide compounds, processes for their preparation, pharmaceutical compositions containing these compounds and to their use in the treatment of disorders, conditions or disorders such as allergic disorders, inflammatory disorders and disorders of the immune system.
Type:
Grant
Filed:
April 22, 2010
Date of Patent:
March 19, 2013
Assignee:
Glaxo Group Limited
Inventors:
David George Allen, Diane Mary Coe, Anthony William James Cooper, Paul Martin Gore, David House, Stefan Senger, Steven Leslie Sollis, Sadie Vile, Caroline Wilson
Abstract: Preparation and in vitro and in vivo characterization of novel forms of active pharmaceutical ingredients, suitable for pharmaceutical compositions in drug delivery systems for humans.
Type:
Application
Filed:
August 6, 2012
Publication date:
February 7, 2013
Inventors:
Mazen HANNA, Ning SHAN, Miranda L. CHENEY, David R. WEYNA, Raymond HOUCK
Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.
Type:
Grant
Filed:
March 24, 2011
Date of Patent:
December 18, 2012
Assignee:
Bayer Aktiengesellshaft
Inventors:
Michael Ruther, Hermann Hagemann, Udo Schneider, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Thomas Bretschneider, Christophe Erdelen, Mark Wilhelm Drewes, Dieter Feucht, Folker Lieb