Phosphorus Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/22)
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Patent number: 8710215Abstract: Novel bisphosphonate cyclic acetal compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating bone metabolism disorders, such as abnormal calcium and phosphate metabolism.Type: GrantFiled: October 12, 2012Date of Patent: April 29, 2014Assignee: Warner Chilcott Company, LLCInventors: Frank Hallock Ebetino, Adam Wieslaw Mazur, Roy Lee Martin Dobson
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Patent number: 8703437Abstract: The present invention provides fluorogenic substrates and methods of use in detecting and analyzing phospholipase C isozyme (PLC) activity.Type: GrantFiled: June 7, 2011Date of Patent: April 22, 2014Assignee: The University of North Carolina at Chapel HillInventors: Qisheng Zhang, Wei Gang Huang, John Sondek, Stephanie Hicks
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Patent number: 8703745Abstract: 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: GrantFiled: February 21, 2013Date of Patent: April 22, 2014Assignee: Allergan, Inc.Inventors: Todd M. Heidelbaugh, Phong X. Nguyen
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Publication number: 20140107073Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.Type: ApplicationFiled: October 4, 2013Publication date: April 17, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
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Publication number: 20140093935Abstract: Mitigation of photo-induced damage in excitation illuminated reactions and analyses utilizing such reactions results in an enhanced performance for the reactions and the analyses. There is provided a novel class of triplet-state quenchers for mitigating photo-induced damage which are both simple in structure and effective at preventing and/or reducing photo-induced damage to reaction components of excitation illuminated reaction mixtures. Also provided are methods of using the compounds of the invention, devices and kits incorporating the compounds of the invention.Type: ApplicationFiled: September 27, 2013Publication date: April 3, 2014Applicant: Pacific Biosciences of California, Inc.Inventors: Gene Shen, Andrei Fedorov, Wei-Chuan Sun, Stephen Yue
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Publication number: 20140088303Abstract: Disclosed is a method for highly efficiently obtaining an optically active alcohol from a carbonyl compound highly enantioselectively. Also disclosed is a ligand used in such a method. Specifically, an optically active alcohol is obtained by reacting a carbonyl compound and an organozinc compound by using a ligand (L) shown below.Type: ApplicationFiled: November 27, 2013Publication date: March 27, 2014Applicants: Sekisui Medical Co., Ltd., National University Corporation Nagoya UniversityInventors: Kazuaki ISHIHARA, Manabu HATANO, Takashi MIYAMOTO
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Publication number: 20140088046Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.Type: ApplicationFiled: September 5, 2013Publication date: March 27, 2014Applicant: ZOETIS LLCInventors: Denis Billen, Michael Curtis, Richard Andrew Ewin, Richard M. Goodwin, Paul D. Johnson, Timothy Allan Johnson, Graham M. Kyne, Todd M. Maddux, Susan Mary Kult Sheehan, Rajendran Vairagoundar
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Patent number: 8674102Abstract: The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins, nucleic acids and cellular organelles. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes are also provided that comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been modified to provide beneficial properties.Type: GrantFiled: January 3, 2013Date of Patent: March 18, 2014Assignee: Enzo Life Sciences, Inc.Inventors: Praveen Pande, Zaiguo Li, Maciej Szczepanik, Wayne Forrest Patton
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Publication number: 20140051080Abstract: Compounds of general formula I are used as labels in an electrochemical assay: (I) in which: Fc and Fc? are substituted or unsubstituted ferrocenyl moieties, X is a C1 to C6 alkylene chain which is optionally interrupted by —O— or —NH—; Y is a C1 to C6 alkylene chain which is optionally interrupted by —O— or —NH—; Z is a C1 to C12 alkylene chain which may optionally be substituted and/or may optionally be interrupted by —O—, —S—, cycloalkyl, —CO—, —CON R1—, —NR1CO— or —NR1— in which R1 represents hydrogen or C1 to C4 alkyl; and R is a linker group. Compounds I are used to make labelled substrates, as well as functionalised compounds for making the labelled substrates.Type: ApplicationFiled: December 22, 2011Publication date: February 20, 2014Inventors: Jonathan Sharp, Stephen Flower, Christopher Frost
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Publication number: 20140024621Abstract: The invention generally relates to aminopyridines and methods of use thereof. In certain embodiments, the invention provides an aminopyridine or a pharmaceutically-acceptable salt thereof, in which the aminopyridine or the salt thereof includes a cleavable functional group that substantially prevents extra-hepatic hydrolysis.Type: ApplicationFiled: July 23, 2012Publication date: January 23, 2014Applicant: MS THERAPEUTICS LIMITEDInventors: Michael J. Hudson, Alan Palmer, Richard Todd, Patrick Camilleri
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Publication number: 20140010758Abstract: Compounds of the formulae, (I), wherein each variable is as defined herein are provided which are useful in (i) diagnostic methods for detecting and/or identifying cells presenting PSMA; (2) compositions comprising a compound of the invention together with a pharmaceutically acceptable carrier, excipient, and/or diluent; (3) methods for inhibiting or treating prostrate cancer; and (4) methods for blocking or destabilizing neovasculature of a tumor.Type: ApplicationFiled: November 10, 2011Publication date: January 9, 2014Applicants: THE REGEANTS OF THE UNIVERSITY OF CALIFORNIA, WASHINGTON STATE UNIVERSITYInventors: Clifford E. Berkmam, Henry F. Vanbrocklin
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Patent number: 8624024Abstract: Disclosed is a method for highly efficiently obtaining an optically active alcohol from a carbonyl compound highly enantioselectively. Also disclosed is a ligand used in such a method. Specifically, an optically active alcohol is obtained by reacting a carbonyl compound and an organozinc compound by using a ligand (L) shown below.Type: GrantFiled: April 27, 2012Date of Patent: January 7, 2014Assignees: National University Corporation Nagoya University, Sekisui Medical Co., Ltd.Inventors: Kazuaki Ishihara, Manabu Hatano, Takashi Miyamoto
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Publication number: 20130338110Abstract: The inventions disclosed include methods of treating cancers and related neoplasias, especially prostate cancer, with pharmaceutically acceptable salts comprising lipophilic cation moieties linked to nitroxide or linked to hydroxylamine anti-oxidant groups.Type: ApplicationFiled: May 20, 2013Publication date: December 19, 2013Inventors: David A. ZARLING, Hirak S. BASU, Balaraman KALYANARAMAN, Joy JOSEPH
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Publication number: 20130336965Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: May 20, 2013Publication date: December 19, 2013Applicant: Novartis AGInventors: Matthew Burger, Joseph E. Drumm, III, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Benjamin Taft, Huw Tanner
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Patent number: 8609638Abstract: The invention provides compounds, compositions, and methods for studying the Rohmer pathway and for treating bacterial infections or parasitic infections. The parasitic infection can be a protozoan infection, such as malaria. The compounds and compositions can also be used as antibiotics, for example, to kill bacteria or parasites, or to inhibit bacterial or parasite growth. The invention further provides inhibitors of isoprenoid biosynthesis enzymes, and methods of inhibiting the activity of isoprenoid biosynthesis enzymes. The compounds can be, for example, alkynes or allenes that bind to a unique Fe of an Fe4S4 cluster of an isoprenoid biosynthesis enzyme.Type: GrantFiled: October 8, 2010Date of Patent: December 17, 2013Assignee: The Board of Trustees of the University of IllinoisInventors: Eric Oldfield, Ke Wang, Weixue Wang, Yonghui Zhang
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Patent number: 8604201Abstract: 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: GrantFiled: September 26, 2008Date of Patent: December 10, 2013Assignee: Centre National de Recherche Scientifique (C.N.R.S.)Inventors: Marc Taillefer, Hamid Kaddouri, Fouad Ouazzani
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Patent number: 8598351Abstract: The present invention provides phospho-amino pincer-type ligands, metal complexes thereof, and catalytic methods comprising such metal complexes.Type: GrantFiled: June 20, 2012Date of Patent: December 3, 2013Assignee: King Abdullah University of Science and TechnologyInventors: Kuo-Wei Huang, Tao Chen, Lipeng He, Dirong Gong, Weiguo Jia, Liangfeng Yao
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Patent number: 8592585Abstract: The present invention discloses a phosphorescent tris-chelated transition metal complex comprising i) two identical non-conjugated cyclometalated ligands being incorporated into a coordination sphere thereof with a transition metal, and one ligated chromophore being incorporated into the coordination sphere; or ii) one non-conjugated cyclometalated ligand forming a coordination sphere thereof with a transition metal, and two ligated chromophores being incorporated into the coordination sphere, wherein the metal is iridium, platinum, osmium or ruthenium, and the ligated chromophore possesses a relatively lower energy gap in comparison with that of the non-conjugated cyclometalated ligand, the latter afforded an effective barrier for inhibiting the ligand-to-ligand charge transfer process, so that a subsequent radiative decay from an excited state of these transition complexes will be confined to the single ligated chromophore.Type: GrantFiled: August 29, 2011Date of Patent: November 26, 2013Assignee: National Tsing Hua UniversityInventors: Yun Chi, Pi-Tai Chou, Yi-Hwa Song, Yuan-Chieh Chiu, Chiung-Fang Chang
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Publication number: 20130310343Abstract: A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the crystalline form may be used in antibiotics.Type: ApplicationFiled: April 22, 2013Publication date: November 21, 2013Applicant: Trius Therapeutics, Inc.Inventors: Katharina Reichenbacher, Robert J. Duguid, Jacqueline A. Ware, Douglas Phillipson
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Publication number: 20130310344Abstract: The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.Type: ApplicationFiled: August 5, 2011Publication date: November 21, 2013Applicant: ASTRAZENECA ABInventors: Robert Bruce Diebold, Thomas Gero, Paul Grover, Shan Huang, Stephanos Ioannidis, Claude Afona Ogoe, Jamal Carlos Saeh, Jeffrey Gilbert Varnes
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Publication number: 20130310395Abstract: The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.Type: ApplicationFiled: May 13, 2013Publication date: November 21, 2013Applicant: NOVARTIS AGInventors: Stephanie Kay DODD, Pascal FURET, Robert Martin GROTZFELD, Darryl Brynley JONES, Paul William MANLEY, Andreas MARZINZIK, Xavier Francois Andre PELLE, Bahaa SALEM, Joseph SCHOEPFER
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Patent number: 8586743Abstract: The present disclosure is directed to a reactive ester agent capable of conjugating a reporter molecule to a carrier molecule or solid support. The reactive ester agent has the general formula: wherein the variables are described throughout the application.Type: GrantFiled: January 30, 2008Date of Patent: November 19, 2013Assignee: Life Technologies CorporationInventors: Kyle Gee, Aleksey Rukavishnikov, Diane M. Witczak
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Publication number: 20130302280Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: ApplicationFiled: June 26, 2013Publication date: November 14, 2013Inventors: Aesop Cho, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Choung U. Kim, Qi Liu, William J. Watkins, Jennifer R. Zhang
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Publication number: 20130303768Abstract: A method for the synthesis of N-substituted 3-acylated pyridinium compounds by reacting a pentamethine precursor with a primary amine.Type: ApplicationFiled: July 18, 2013Publication date: November 14, 2013Applicant: ROCHE DIAGNOSTICS OPERATIONS, INC.Inventors: Peter Gebauer, Dieter Heindl, Carina Horn
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Patent number: 8580767Abstract: Dosage forms or pharmaceutical compositions comprise a compound having the structure of Formula IV: wherein n is a non-negative integer; wherein each Z is an oxazolidinone-containing moiety having antibiotic activity in vivo upon cleaving, wherein M is independently OR1 or NR1R2; wherein R1 and R2 are independently selected from the group consisting of H, an optionally-substituted hydrocarbyl residue or a pharmaceutically acceptable cation; wherein the compound in the dosage form or a pharmaceutical composition is present in an amount effective for treating or preventing an antibacterial infection in a mammalian subject. Methods of preparing and using these dosage forms or pharmaceutical compositions are also disclosed.Type: GrantFiled: May 25, 2010Date of Patent: November 12, 2013Assignee: Trius Therapeutics, Inc.Inventors: D. Keith Hester, II, Robert J. Duguid, John Finn
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Publication number: 20130296276Abstract: The present invention provides a compound having a muscle cell or adipocyte differentiation regulating action, useful for the prophylaxis or treatment of diseases such as diabetes, obesity, dyslipidemia and the like, and the like, and having superior efficacy. The present invention provides a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof.Type: ApplicationFiled: July 14, 2011Publication date: November 7, 2013Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Osamu UJIKAWA, Kazuaki TAKAMI, Nobuyuki TAKAKURA, Nozomu SAKAI
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Publication number: 20130295599Abstract: 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: ApplicationFiled: October 18, 2011Publication date: November 7, 2013Applicant: Ajou University Industry-Academic Cooperation FoundationInventor: Hwan Myung Kim
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Publication number: 20130281407Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.Type: ApplicationFiled: June 19, 2013Publication date: October 24, 2013Inventors: Michael N. Greco, Harold R. Almond, Michael J. Hawkins, Eugene Powell
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Publication number: 20130281664Abstract: The present invention relates to novel Ruthenium catalysts and related borohydride complexes, and the use of such catalysts, inter alia, for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e.Type: ApplicationFiled: October 11, 2011Publication date: October 24, 2013Inventors: David Milstein, Ekambaram Balaraman, Chidambaram Gunanathan, Boopathy Gnanaprakasam, Jing Zhang
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Publication number: 20130253185Abstract: The present invention provides novel compounds and ligands that are useful in transition metal catalyzed cross-coupling reactions. For example, the compounds and ligands of the present invention are useful in palladium or gold catalyzed cross-coupling reactions.Type: ApplicationFiled: November 17, 2011Publication date: September 26, 2013Applicant: Dalhousie UniversityInventors: Rylan J. Lundgren, Mark Stradiotto
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Publication number: 20130237502Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.Type: ApplicationFiled: March 5, 2013Publication date: September 12, 2013Inventors: Michael Curtis, Brian A. Duclos, Richard A. Ewin, Paul D. Johnson, Timothy Allen Johnson, Rajendran Vairagoundar, Denis Billen, Richard M. Goodwin, Andrea K. Haber-Stuk, Graham M. Kyne, Susan M. K. Sheehan
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Publication number: 20130225527Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 15, 2013Publication date: August 29, 2013Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: ARIAD PHARMACEUTICALS, INC.
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Publication number: 20130225822Abstract: The present invention relates to a chiral spiro-pyridylamidophosphine ligand compound, synthesis method therefor and application thereof. The chiral spiro-pyridylamidophosphine compound is a compound having a structure of Formula (I), a racemate or optical isomer thereof, or a catalytically acceptable salt thereof, and is mainly characterized by having a chiral spiro-dihydro-indene skeleton in its structure. The chiral spiro-pyridylamidophosphine compound may be synthesized with optical active 7-diaryl/alkylphosphino-7?-amino-1,1?-spiro-dihydro-indene or substituted 7-diaryl/alkylphosphino-7?-amino-1,1?-spiro-dihydro-indene having a spiro-skeleton as chiral starting material. The chiral spiro-pyridylamidophosphine compound may be used as a chiral ligand in asymmetric hydrogenation of a carbonyl compound catalyzed by iridium, in which the reaction activity is very high, the amount of the catalyst may be 0.0001 mol %, and the enantioselectivity of the reaction is up to 99.9% ee.Type: ApplicationFiled: November 18, 2011Publication date: August 29, 2013Inventors: Qilin Zhou, Jianhua Xie, Xiaoyan Liu, Jianbo Xie, Lixin Wang
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Publication number: 20130225528Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 15, 2013Publication date: August 29, 2013Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: ARIAD Pharmaceuticals, Inc.
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Publication number: 20130209994Abstract: The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins, nucleic acids and cellular organelles. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes are also provided that comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been modified to provide beneficial properties.Type: ApplicationFiled: January 3, 2013Publication date: August 15, 2013Applicant: ENZO LIFE SCIENCES, INC.Inventor: ENZO LIFE SCIENCES, INC.
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Patent number: 8507530Abstract: Anti-fungal agent having excellent anti-fungal action physicochemical properties including safety and water solubility.Type: GrantFiled: April 25, 2008Date of Patent: August 13, 2013Assignee: Eisai R&D Management Co., Ltd.Inventors: Keigo Tanaka, Eiichi Yamamoto, Naoaki Watanabe
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Publication number: 20130203702Abstract: The present invention relates to novel compounds, compositions containing same and methods for inhibiting human farnesyl pyrophosphate synthase or for the treatment or prevention of disease conditions using said compounds;Type: ApplicationFiled: May 27, 2011Publication date: August 8, 2013Applicant: The Royal Institution for the Advancement of Learning/McGill UniversityInventors: Youla S. Tsantrizos, Joris Wim De Schutter, Yih-Shyan Lin
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Publication number: 20130203998Abstract: 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: ApplicationFiled: March 14, 2013Publication date: August 8, 2013Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventor: UNIVERSITY OF SOUTHERN CALIFORNIA
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Patent number: 8501714Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: GrantFiled: September 7, 2010Date of Patent: August 6, 2013Assignee: Gilead Sciences, Inc.Inventors: Aesop Cho, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Choung U. Kim, Qi Liu, William J. Watkins, Jennifer R. Zhang
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Publication number: 20130165412Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor.Type: ApplicationFiled: September 14, 2012Publication date: June 27, 2013Inventors: Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
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Publication number: 20130135703Abstract: An electrochromic compound represented by the following General Formula (1) wherein E represents at least one of O, S, Se, and N—R; R represents at least one of a hydrogen atom, a substitutive aliphatic hydrocarbon group, and a substitutive aromatic hydrocarbon group; X1-X10 may be the same or different and each represent at least one of a hydrogen atom and a monovalent substituent; L1 and L2 may be the same or different and each represent a monovalent substituent; and A? and B? may be the same or different and each represent a monovalent anion.Type: ApplicationFiled: November 14, 2012Publication date: May 30, 2013Applicant: RICOH COMPANY, LTD.Inventors: Takashi Okada, Shigenobu Hirano, Tsutomu Sato
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Patent number: 8450488Abstract: The invention relates to a novel process for the preparation of [1-hydroxy-2-(3-pyridinyl)ethylidene]bisphosphonic acid and hemipentahydrate monosodium salt thereof comprising (a) reacting an aqueous solution of 3-pyridyl acetic acid hydrochloride with phosphorus trichloride; (b) removing unreacted phosphorus trichloride; (c) adding water and hydrolyzing; (d) isolating crystalline [1-hydroxy-2-(3-pyridinyl)ethylidene]bisphosphonic acid; (e) suspending said crystalline [1-hydroxy-2-(3-pyridinyl)ethylidene]bisphosphonic acid in water; (f) adding sodium hydroxide, filtering off, and washing; and (g) drying obtained hemipentahydrate monosodium salt of 1-hydroxy-2-(3-pyridinyl)ethylidene]bisphosphonic acid.Type: GrantFiled: December 28, 2005Date of Patent: May 28, 2013Assignee: Zaklady Farmaceutyczne Polpharma S.A.Inventors: Leszek Dembkowski, Robert Rynkiewicz, Janusz Rachoń, Slawomir Makowiec, Witold Przychodzeń, Dariusz Witt
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Patent number: 8440644Abstract: 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: GrantFiled: May 20, 2011Date of Patent: May 14, 2013Assignee: Allergan, Inc.Inventors: Phong X. Nguyen, Todd M. Heidelbaugh
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Publication number: 20130116214Abstract: The present invention provides a compound having a muscle cell or adipocyte differentiation regulating action, useful for the prophylaxis or treatment of diseases such as diabetes, obesity, dyslipidemia and the like, and the like, and having superior efficacy. The present invention provides a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof.Type: ApplicationFiled: July 14, 2011Publication date: May 9, 2013Inventors: Osamu Ujikawa, Kazuaki Takami, Nobuyuki Takakura, Nozomu Sakai
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Patent number: 8431714Abstract: 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: GrantFiled: April 16, 2008Date of Patent: April 30, 2013Assignee: University of Southern CaliforniaInventors: Charles E. McKenna, Boris A. Kashemirov, Joy Lynn F. Bala
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Patent number: 8426388Abstract: A compound of the formula is disclosed as a prodrug of an HIV protease inhibitor. Methods and compositions for inhibiting HIV protease activity and treating HIV infection are also disclosed.Type: GrantFiled: April 7, 2010Date of Patent: April 23, 2013Assignee: AbbVie Inc.Inventors: David A. DeGoey, William J. Flosi, David J. Grampovnik, Larry L. Klein, Dale J. Kempf, Xiu C. Wang
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Patent number: 8426389Abstract: A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi , anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the crystalline form may be used in antibiotics.Type: GrantFiled: February 3, 2010Date of Patent: April 23, 2013Assignee: Trius Therapeutics, Inc.Inventors: Katharina Reichenbächer, Robert J. Duguid, Jacqueline A. Ware, Douglas Phillipson
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Publication number: 20130089793Abstract: An ionic liquid including a phosphazene compound that has a plurality of phosphorus-nitrogen units and at least one pendant group bonded to each phosphorus atom of the plurality of phosphorus-nitrogen units. One pendant group of the at least one pendant group comprises a positively charged pendant group. Additional embodiments of ionic liquids are disclosed, as are electrolyte solutions and energy storage devices including the embodiments of the ionic liquid.Type: ApplicationFiled: October 5, 2011Publication date: April 11, 2013Applicant: BATTELLE ENERGY ALLIANCE, LLCInventors: Kevin L. Gering, Mason K. Harrup, Harry W. Rollins
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Publication number: 20130090309Abstract: The invention provides certain amino-pyridine-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and n are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: April 30, 2012Publication date: April 11, 2013Inventors: Eric Thomas Romeo, Michelle R. Machacek, Benjamin Wesley Trotter, Thomas Allen Miller, Brian Michael Andresen, Neville John Anthony, Brandon M. Taoka, Yuan Liu
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Patent number: 8410269Abstract: The present invention discloses a phosphorescent tris-chelated transition metal complex comprising i) two identical non-conjugated cyclometalated ligands being incorporated into a coordination sphere thereof with a transition metal, and one ligated chromophore being incorporated into the coordination sphere; or ii) one non-conjugated cyclometalated ligand forming a coordination sphere thereof with a transition metal, and two ligated chromophores being incorporated into the coordination sphere, wherein the metal is iridium, platinum, osmium or ruthenium, and the ligated chromophore possesses a relatively lower energy gap in comparison with that of the non-conjugated cyclometalated ligand, the latter afforded an effective barrier for inhibiting the ligand-to-ligand charge transfer process, so that a subsequent radiative decay from an excited state of these transition complexes will be confined to the single ligated chromophore.Type: GrantFiled: August 29, 2011Date of Patent: April 2, 2013Assignee: National Tsing Hua UniversityInventors: Yun Chi, Pi-Tai Chou, Yi-Hwa Song, Yuan-Chieh Chiu, Chiung-Fang Chang