Boron Or Silicon Containing Patents (Class 544/69)
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Publication number: 20130129940Abstract: Described herein are organoaminosilane precursors which can be used to deposit silicon containing films which contain silicon and methods for making these precursors. Also disclosed herein are deposition methods for making silicon-containing films or silicon containing films using the organoaminosilane precursors described herein. Also disclosed herein are the vessels that comprise the organoaminosilane precursors or a composition thereof that can be used, for example, to deliver the precursor to a reactor in order to deposit a silicon-containing film.Type: ApplicationFiled: May 17, 2012Publication date: May 23, 2013Applicant: AIR PRODUCTS AND CHEMICALS, INC.Inventors: Manchao Xiao, Xinjian Lei, Bing Han, Mark Leonard O'Neill, Ronald Martin Pearlstein, Richard Ho, Haripin Chandra, Agnes Derecskei-Kovacs
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Publication number: 20130079303Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.Type: ApplicationFiled: November 19, 2012Publication date: March 28, 2013Applicant: AMGEN INC.Inventor: Amgen Inc.
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Publication number: 20130053529Abstract: A benzoxazine-bridged compound is provided. The compound has a low dielectric constant, a high mechanic strength and a high glass transition temperature. The compound has a highly cross-linked structure with a yellow-light photoluminescent emission. Characterization of the present disclosure has been conducted with Fourier transform infrared, nuclear magnetic resonance, molecular mass and elemental analysis.Type: ApplicationFiled: August 31, 2011Publication date: February 28, 2013Applicant: Chung-Shan Institute of Science and Technology, Armaments, Bureau, Ministry of National DefenseInventors: Wen-Chiung Su, Ying-Ling Liu
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Patent number: 8383670Abstract: Described herein are compounds of Formula (I): wherein A, J, Z, X, R1, and R4 are defined herein, and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: GrantFiled: March 17, 2011Date of Patent: February 26, 2013Assignee: Calcimedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20130040912Abstract: The invention relates to compounds of formula (I) R1 is methyl, n-hexyl, aminoethyl, methylaminoethyl, ethylaminoethyl, dimethylaminoethyl, acryloylaminoethyl, methacryloylaminoethyl, methoxyethyl, ethoxyethyl, d-C4-alkyl-sulfonyl, acryloyl, or methacryloyl; or R1 is aminoethyl, acryloyl or acryloylaminoethyl carrying a linker and a tag, and R2 and R3, independently of each other, are hydrogen or CrC4-alkyl, or R2 and R3 together form a methylene or an ethylene bridge; and tautomers, solvates and pharmaceutically acceptable salts thereof. These compounds are effective in preventing or treating a disease or disorder modulated by PI3 kinases and/or mTOR, in particular treating a hyperproliferative disorder.Type: ApplicationFiled: April 27, 2011Publication date: February 14, 2013Applicant: UNIVERSITY OF BASELInventors: Vladimir Cmiljanovic, Natasa Cmiljanovic, Bernd Giese, Matthias Wymann
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Patent number: 8362283Abstract: The present invention relates to methods for the synthesis of galanthamine, morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.Type: GrantFiled: May 12, 2010Date of Patent: January 29, 2013Assignee: Board of Regents, The University of Texas SystemInventors: Philip D. Magnus, Benjamin P. Fauber, Neeraj Sane
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Patent number: 8324204Abstract: A series of 5,6-dihydro-1-benzothiophen-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: GrantFiled: June 4, 2007Date of Patent: December 4, 2012Assignee: UCB Pharma SAInventors: Rikki Peter Alexander, Stuart Bailey, Stephen Brand, Daniel Christopher Brookings, Julien Alistair Brown, Alan Findlay Haughan, Natasha Kinsella, Christopher Lowe, Stephen Robert Mack, William Ross Pitt, Marianna Dilani Richard, Andrew Sharpe, Laura Jane Tait
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Publication number: 20120296087Abstract: Morpholino-based oligomers suitable as antisense agent comprising modifications of phosphorodiamidate backbone or modification with 5-substituted pyrimidines of morpholino compound that is soluble in culture medium and sufficient for cell penetration thereby eliminating the need for injecting into the cells. Monomers comprising the said oligomers and its method of manufacture, method of manufacture of the said oligomers and its dye, flurophore, drug, biomolecule conjugate wherein the said oligomers find different end use but not limited to regulation of gene expression, tissue culture with improved transfection efficiency and related studies on cellular transfection.Type: ApplicationFiled: August 10, 2010Publication date: November 22, 2012Applicant: INDIAN ASSOCIATION FOR THE CULTIVATION OF SCIENCEInventors: Surajit Sinha, Sankha Pattanayak, Sibasish Paul, Bappaditya Nandi
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Patent number: 8268818Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: September 4, 2007Date of Patent: September 18, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Tiansheng Wang, Jeremy Green, Brian Ledford, François Maltais, Andreas P. Termin, Mark Cornebise, Jonathan Parsons, Adam Tanner, James Westcott
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Publication number: 20120214765Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.Type: ApplicationFiled: September 19, 2011Publication date: August 23, 2012Applicant: Anacor Pharmaceuticals, Inc.Inventors: Tsutomu Akama, Yong-Kang Zhang, Charles Z. Ding, Jacob J. Plattner, Kirk R. Maples, Yvonne Freund, Virginia Sanders, Yi Xia, Stephen J. Baker, James A. Nieman, Xiaosong Lu, Marcelo Sales, Rashmi Sharma, Rajeshwar Singh, Robert T. Jacobs, Daitao Chen, Michael Richard Kevin Alley
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Publication number: 20120184508Abstract: Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.Type: ApplicationFiled: January 11, 2012Publication date: July 19, 2012Inventors: Wenjian Liu, Kin-Chun Luk, Xiaohu Zhang
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Patent number: 8217113Abstract: Condensation crosslinkable compositions based on organosilicon compounds contain at least one heterocyclic compound A[CR12SiRa(OR2)3-a]x which contains at least one heteroatom from main groups 3 or 5 and is bonded to CR12 through one of these heteroatoms.Type: GrantFiled: July 29, 2008Date of Patent: July 10, 2012Assignee: Wacker Chemie AGInventors: Uwe Scheim, Wolfram Schindler, Peter Schoeley, Volker Stanjek
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Publication number: 20120171116Abstract: The present invention includes arginase enzyme inhibitors, compositions comprising these arginase inhibitors, and methods of treating or diagnosing conditions characterized either by abnormally high arginase activity or abnormally low nitric oxide levels in a mammal, comprising administering compositions of the invention to the mammal.Type: ApplicationFiled: July 26, 2011Publication date: July 5, 2012Inventors: Bruce Edward Tomczuk, Gary Lee Olson, Richard Scott Pottorf, Jane Wang, Bhaskara Rao Nallaganchu
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Publication number: 20120107328Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).Type: ApplicationFiled: November 3, 2008Publication date: May 3, 2012Inventors: William J. Greenlee, Zhaoning Zhu, Theodros Asberom, Xianhai Huang, Hubert B. Josien
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Publication number: 20120108801Abstract: The invention relates to disubstituted-aminodifluorosulfinium salts represented by the formula (I). Processes for preparing same and methods of use as deoxofluorinating reagent is also provided.Type: ApplicationFiled: June 18, 2010Publication date: May 3, 2012Applicant: OMEGACHEM INCInventors: Michel A. Couturier, Alexandre L'Heureux
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Publication number: 20120101233Abstract: The present invention discloses new catalyst systems based on complexes of divalent metals supported by chelating phenoxy ligands for immortal ring-opening polymerisation of cyclic esters and cyclic carbonates.Type: ApplicationFiled: April 29, 2010Publication date: April 26, 2012Applicant: TOTAL PETROCHEMICALS RESEARCH FELUYInventors: Jean-François Carpentier, Yann Sarazin, Valentin Poirier, Marion Helou
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Publication number: 20120077801Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state.Type: ApplicationFiled: August 3, 2011Publication date: March 29, 2012Inventors: Roger Victor Bonnert, Rhona Jane Cox, Simon De Sousa, Mark Dickinson, Simon Fraser Hunt, Austen Pimm, Hitesh Jayantilal Sanganee, Frank Burkamp, Premji Meghani
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Publication number: 20120071650Abstract: The invention relates to a method (a) for producing aminoorganyltriorganylsilanes of the general formula (1) R?3-nR1nSi—R2—NR3R4 (1), a method (b) for producing cyclic aminosilanes of the general formula (4), and a method (III) for producing silylorganoamines of the general formula (7) R013-tR11tSi—R12—NR13—R14—SiR023-sR15s (7), wherein amines are reacted with halogen organylsilanes, wherein R?, R1, R2, R3, R4, R, R5, R6, R01, R02, R11, R12, R13, R14, R15, n, and s have the meanings specified in claims 1 to 3, wherein after the reaction, the ammonium halides of the amines produced as by-products are released by adding a base (B) to the reaction mixture, the amines are removed from the reaction mixture by distillation, two liquid phases are formed by further adding base (B) to the reaction mixture, wherein the one phase contains at least 90 wt % of the hydrohalide of the base (B) and said phase is separated.Type: ApplicationFiled: June 1, 2010Publication date: March 22, 2012Applicant: WACKER CHEMIE AGInventor: Michael STEPP
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Publication number: 20120041193Abstract: Disclosed herein are vinyl-bromides, vinyl-boronic acids and vinyl-boronic acid derivatives useful as synthetic intermediates for the preparation of therapeutic agents. Also disclosed are methods of synthesis of vinyl-bromides, vinyl-boronic acids and vinyl-boronic acid derivatives.Type: ApplicationFiled: August 10, 2011Publication date: February 16, 2012Applicant: Frontier Scientific, Inc.Inventors: Shivanand K. Math, Homayoun H. Mokri, James B. LaMunyon, Dustin R. Cefalo, Charles A. Testa
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Patent number: 8105504Abstract: Organic materials which possess outstanding stability to oxidative, thermal or light-induced degradation comprise as stabilizers at least one compound of the formula (I) wherein the general symbols are as defined in claim 1. The compounds of formula I are especially useful as stabilizers for protecting polymers and lubricants against oxidative, thermal or light-induced degradation and as scavengers for oxidized developer in color photographic material.Type: GrantFiled: August 22, 2005Date of Patent: January 31, 2012Assignee: BASF SEInventors: Michèle Gerster, Peter Nesvadba
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Publication number: 20120010403Abstract: A production method of a compound containing a primary, secondary, or tertiary aminomethyl aromatic ring of the present invention includes: using a fluoroboron compound or a dimer thereof, or solvates thereof, which are represented by a formula (I): Ra(Rb)N—CH2—BF3M??(I) as an aminomethylating agent for an aromatic ring; and reacting the aminomethylating agent with an aromatic ring-containing compound, which can react with the aminomethylating agent, under the presence of a metal catalyst such as a palladium compound so as to perform the direct aminomethylation of the aromatic ring.Type: ApplicationFiled: September 21, 2011Publication date: January 12, 2012Inventor: Keigo TANAKA
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Publication number: 20110275762Abstract: The invention relates to novel therapeutic agents and diagnostic probes. The invention also relates to phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitor triazine-, pyrimidine- and pyridine-based compounds? Formula (I), their stereoisomers, geometric isomers, tautomers, solvates, metabolites, N-oxide derivatives, pharmaceutically acceptable salts, and prodrugs thereof compositions of the new compounds; either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, for treating disorders mediated by lipid kinases. •Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: November 10, 2009Publication date: November 10, 2011Applicant: UNIVERSITY OF BASELInventors: Vladimir Cmiljanovic, Natasa Cmiljanovic, Bernd Giese, Matthias Wymann
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Patent number: 8049027Abstract: An organosilicon compound having an amino group is provided. This compound is represented by the following general formula (1): wherein R1 and R2 respectively represent an unsubstituted or substituted aliphatic monovalent hydrocarbon group containing 1 to 10 carbon atoms with the proviso that the R1 and R2 may together form a ring with the nitrogen atom to which they are bonded, and that R1 and R2 may contain a heteroatom; R3 and R4 independently represent an unsubstituted or substituted monovalent hydrocarbon group containing 1 to 10 carbon atoms; and n represents an integer of 0 to 2. Use of this compound enables production of a polymer product having excellent mechanical properties, high heat resistance, and high transparency. The solution of this compound is stable, and can be stored for a long time, and when used for a polymer modifying agent, it facilitates introduction of amino group and hydroxy group.Type: GrantFiled: October 20, 2009Date of Patent: November 1, 2011Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Takayuki Honma, Tohru Kubota, Ayumu Kiyomori
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Publication number: 20110245203Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.Type: ApplicationFiled: March 30, 2011Publication date: October 6, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Jing Li
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Publication number: 20110224366Abstract: Condensation crosslinkable compositions based on organosilicon compounds contain at least one heterocyclic compound A[CR12SiRa(OR2)3-a]x which contains at least one heteroatom from main groups 3 or 5 and is bonded to CR12 through one of these heteroatoms.Type: ApplicationFiled: July 29, 2008Publication date: September 15, 2011Applicant: WACKER CHEMIE AGInventors: Uwe Scheim, Wolfram Schindler, Peter Schoeley, Volker Stanjek
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Publication number: 20110207701Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.Type: ApplicationFiled: August 16, 2010Publication date: August 25, 2011Applicant: Anacor Pharmaceuticals, Inc.Inventors: Huchen Zhou, Dazhong Ding, Yasheen Zhou, Yong-Kang Zhang, Jacob J. Plattner
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Publication number: 20110190235Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.Type: ApplicationFiled: August 6, 2010Publication date: August 4, 2011Applicant: Anacor Pharmaceuticals, Inc.Inventors: Daitao Chen, Matthew Orr, Jessica Sligar, Robert Jacobs, Jacob J. Plattner
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Publication number: 20110190480Abstract: The present invention relates to dyes of the general formula CAT+ Y? (I), where Y? is an anion selected from the group of the cyanoborates, fluoroalkylphosphates, fluoroalkylborates or imidates and CAT+ is a cation selected from the group of the azine, xanthene, polymethine, styryl, azo, tetrazolium, pyrylium, benzopyrylium, thiopyrylium, benzothiopyrylium, thiazine, oxazine, triarylmethane, diarylmethane, methine, acridine, quinoline, isoquinoline or quaternary azafluorenone dyes, for colouring plastics and plastic fibres, for the preparation of flexographic printing inks, as ball-point pen pastes, as stamp ink, for colouring leather and paper, for use in data acquisition systems, reprography, in ink microfilters, in photogalvanics, laser technology and the photo industry.Type: ApplicationFiled: April 11, 2011Publication date: August 4, 2011Inventors: Nikolai (Mykola) IGNATYEV, Urs Welz-Biermann, Helge Willner, Maik Finze, Eduard Bernhardt, Andriy Kucheryna
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Publication number: 20110190455Abstract: A bi-photochromic molecule comprises two photochromic moieties linked via a polydialkylsiloxane oligomer. An ophthalmic lens comprises the bi-photochromic molecule. A polymeric host material comprises the bi-photochromic molecule.Type: ApplicationFiled: August 18, 2009Publication date: August 4, 2011Applicant: Vivimed Labs Europe Ltd.Inventor: Steven Michael Partington
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Publication number: 20110172417Abstract: This invention relates to a heterogeneous copper nanocatalyst composed of copper nanoparticles immobilized on a boehmite support, a method of preparing the same, and the use thereof. The copper nanocatalyst composed of the copper nanoparticles supported on boehmite exhibits excellent performance in a Huisgen cycloaddition reaction and an A3 coupling reaction of aldehyde, amine and alkyne. The copper nanocatalyst is able to be prepared in a large scale and shows superior reactivity even when used in a small amount under mild conditions without an additive in an organic reaction. This heterogeneous catalyst is easy to separate and reuse after the reaction.Type: ApplicationFiled: July 9, 2008Publication date: July 14, 2011Applicant: Postech Academy-Industry FoundationInventors: Jai Wook Park, In Soo Park
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Publication number: 20110147681Abstract: A photochromic polymer comprising at least one siloxane oligomer and at least two photochromic groups covalently linked to one or both terminuses of the siloxane oligomer and compositions containing photochromic siloxane polymers with narrow polydispersity. The photochromic polymer enhances switching speed in rigid host polymers.Type: ApplicationFiled: June 5, 2009Publication date: June 23, 2011Applicant: ADVANCED POLYMERIK PTY LTDInventors: Richard Alexander Evans, Nino Malic, Mark Robert York, Abdelselam Saeed Ali, Jonathan Andrew Campbell
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Patent number: 7947802Abstract: Benzoxazine monomers comprising at least one pendant group are described. (Co)Polymers comprising at least one benzoxazine monomer having at least one pendant group are also described. In a preferred embodiment, the pendant group is located in a side chain of the benzoxazine monomer or polymer. Methods for preparing the benzoxazine monomers and polymers are described. Compositions comprising the benzoxazine monomers and polymers have numerous uses including optical materials, and in electronic materials as electrically insulating materials, and as fireproof materials.Type: GrantFiled: September 6, 2007Date of Patent: May 24, 2011Assignee: Case Western Reserve UniversityInventors: Hatsuo Ishida, Pedro Velez-Herrera
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Publication number: 20110108781Abstract: The present invention relates to photochromic materials that include a photochromic compound that includes a photochromic substituent (e.g., an indeno-fused naphthopyran) and at least one pendent silane group, which is bonded to the photochromic substituent. The pendent silane groups are selected from certain pendent siloxy-silane groups and/or pendent alkoxy-silane groups represented by general formulas (I) and/or (II) as described in further detail herein. The present invention also relates to photochromic articles, such as photochromic optical elements (e.g., photochromic lenses), and photochromic coating compositions (e.g., curable photochromic coating compositions), that include the photochromic materials of the present invention. The photochromic materials of the present invention have improved compatibility with compositions into which they may be incorporated, for example, coating compositions, such as urethane coating compositions.Type: ApplicationFiled: October 26, 2010Publication date: May 12, 2011Applicant: TRANSITIONS OPTICAL, INC.Inventor: Massimiliano Tomasulo
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Patent number: 7915236Abstract: The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.Type: GrantFiled: July 1, 2009Date of Patent: March 29, 2011Assignee: Cephalon, Inc.Inventors: Raffaella Bernardini, Alberto Bernareggi, Paolo G. Cassara, Sankar Chatterjee, Germano D'Arasmo, Sergio De Munari, Edmondo Ferretti, Mohamed Iqbal, Ernesto Menta, Patricia A. Messina McLaughlin, Ambrogio Oliva
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Patent number: 7888356Abstract: The structure and preparation of antibiotics incorporating borinic acid complexes are disclosed, especially hydroxyquinoline, imidazole and picolinic acid derivatives, along with compositions of these antibiotics and methods of using the antibiotics and compositions as bactericidal and fungicidal agents as well as therapeutic agents for the treatment of diseases caused by bacteria and fungi.Type: GrantFiled: January 9, 2008Date of Patent: February 15, 2011Assignee: Anacor Pharmaceuticals, Inc.Inventors: Ving Lee, Stephen J. Benkovic, Stephen J. Baker, Kirk R. Maples, Tsutomu Akama, Yong-Kang Zhang, Rajesjwar Singh, Vittorio A. Sauro, Chetan Pandit, Zhuoyi Su, Zhixiang Yang
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Publication number: 20110031188Abstract: Humic derivatives are prepared and used to adhere to the surfaces of mineral media and other hydroxyl-carrying supports for cleaning the environment by selective sequestration of complex mixtures of contaminants possessing preferential affinity for natural or modified humic substances (HS). The sequestration of target components occurs as a result of their binding to dissolved humic derivatives that can be removed from the solution by adding any solid hydroxyl-carrying support (e.g., silica gel). Another method to sequester the target components from solution is their selective sorption onto humic derivatives immobilized onto solid support (e.g., silica gel). Yet another method involves using the humic derivatives to install a broad spectrum reactive barrier without excavation as an in situ passive remediation system.Type: ApplicationFiled: March 7, 2006Publication date: February 10, 2011Inventors: Irina Vasilyevna Perminova, Sergey Anatolievich Ponomarenko, Leonid Alexandrovich Karpiouk, Kirk Hatfield
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Publication number: 20100310466Abstract: The invention, relates to compounds of formula I (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including inhibition of kinase activity such as PI-3 kinase.Type: ApplicationFiled: January 23, 2009Publication date: December 9, 2010Inventors: Guillermo A. Morales, Kevin T. Weber, Jessica M. Newblom, Xiaodong Peng, Jingdong Su, Joseph R. Garlich
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Publication number: 20100305066Abstract: A series of 5,6-dihydro-1-benzothiophen-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: ApplicationFiled: June 4, 2007Publication date: December 2, 2010Applicant: UCB PHARMA S.A.Inventors: Rikki Peter Alexander, Stuart Bailey, Stephen Brand, Daniel Christopher Brookings, Julien Alistair Brown, Alan Findlay Haughan, Natasha Kinsella, Christopher Lowe, Stephen Robert Mack, William Ross Pitt, Marianna Dilani Richard, Andrew Sharpe, Laura Jane Tait
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Patent number: 7842823Abstract: The present invention provides a novel class of fluorogenic probes for reactive oxygen species. Exemplary probes of the invention utilize a boronate deprotection mechanism to provide high selectivity and optical dynamic range for detecting H2O2 in aqueous solution over similar reactive oxygen species (ROS) including superoxide, nitric oxide, tert-butyl hydroperoxide, and hydroxyl radical; Peroxyresorufin-1 (PR1), Peroxyfluor-1 (PF1), and Peroxyxanthone-1 (PX1) are first-generation probes that respond to H2O2 by an increase in red, green, and blue fluorescence, respectively. The boronate dyes are cell-permeable and can detect micromolar changes in H2O2 concentrations in living cells, including hippocampal neurons, using confocal and two-photon microscopy. The unique combination of ROS selectivity, membrane permeability, and a range of available excitation/emission colors establishes the potential value of PR1, PF1, PX1, and related probes for interrogating the physiology and pathology of cellular H2O2.Type: GrantFiled: October 27, 2006Date of Patent: November 30, 2010Assignee: The Regents of the University of CaliforniaInventor: Christopher J. Chang
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Publication number: 20100292185Abstract: Disclosed herein are ?-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising ?-aminoboronic acids and methods of use thereof.Type: ApplicationFiled: May 10, 2010Publication date: November 18, 2010Inventors: Christopher J. Burns, Rajesh Goswami, Randy W. Jackson, Thomas Lessen, Weiping Li, Daniel Pevear, Pavan Kumar Tirunahari, Hongyu Xu
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Publication number: 20100256092Abstract: This invention relates to, among other items, 6-substituted benzoxaborole compounds and their use for treating bacterial infections.Type: ApplicationFiled: May 12, 2009Publication date: October 7, 2010Applicants: Anacor Pharmaceuticals, Inc., GlaxoSmithKlineInventors: Yi Xia, Michael Richard Kevin Alley, Yasheen Zhou, Vincent S. Hernandez, Jacob J. Plattner, Charles Z. Ding, Kathy Cao, Yong-Kang Zhang, Andrew Benowitz, Tsutomu Akama, Jessica Sligar, Guofeng Jia, Ligong Ou, Neerja Saraswat, Sreekanth Ramachandran, Chris Diaper, Yanchen Zhang, Goverdhan Reddy Banda, James A. Nieman, Mehdi Keramane, Rahim Mohammed, Rajendra Subedi, Hong Liang, Rajeshwar Singh
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Publication number: 20100189658Abstract: The present invention relates to molecular probes of the formula (I) {L1-R1-L}n-A-CO—NH—R2-L2??(I) as defined herein that allow for the observation of the catalytic activity of a selected cathepsin in in vitro assays, in cells or in multicellular organisms, a method for their preparation and the use thereof.Type: ApplicationFiled: August 27, 2009Publication date: July 29, 2010Applicant: SANOFI-AVENTISInventors: Karl-Ulrich WENDT, Maik KINDERMANN, Anja GLOBISCH
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Publication number: 20100189644Abstract: The present invention is directed to arginase inhibitor compounds of formula IA or formula IB: or a pharmaceutically acceptable salt thereof, compositions containing these compounds, and methods of their use for the treatment and diagnosis of conditions characterized by upregulation of arginase, abnormally high arginase activity, or by abnormally low nitric oxide synthase activity.Type: ApplicationFiled: January 26, 2010Publication date: July 29, 2010Applicants: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA, ARGINETIX, INC.Inventors: DAVID W. CHRISTIANSON, Bruce Edward Tomczuk, Richard Scott Pottorf, Andrew Vargha Colasanti, Gary Lee Olson
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Patent number: 7723409Abstract: The invention describes a composition comprising a) a naturally occurring or synthetic elastomer susceptible to oxidative, thermal, dynamic, light-induced and/or ozone-induced degradation, b) a white reinforcing filler, and c) as coupling agent, at least one compound of the formula (I) wherein the general symbols are as defined in claim 1, or an oligomeric hydrolysis product of the compound of the formula (I).Type: GrantFiled: December 6, 2004Date of Patent: May 25, 2010Assignee: Ciba Specialty Chem. Corp.Inventors: Francesco Fuso, Michèle Gerster, Gerrit Knobloch, Pierre Rota-Graziosi
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Publication number: 20100120715Abstract: Disclosed herein are ?-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising ?-aminoboronic acids and methods of use thereof.Type: ApplicationFiled: May 12, 2009Publication date: May 13, 2010Inventors: Christopher J. Burns, Randy W. Jackson, Rajesh Goswami, Hongyu Xu
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Patent number: 7709635Abstract: One aspect of the present invention relates to “boronium” ions that are stable, hydrophobic, room-temperature ionic liquids. In certain embodiments, ionic liquids of the instant invention are represented by the formula [XnBY4?n]+(n?1)(n?1)Z?1, wherein X refers to a Lewis base, Y refers to a substituent covalently bonded to boron, Z?1 is a charge diffuse anion, and x is 2, 3 or 4. In certain embodiments, the ionic liquids of the instant invention are of the general type [X2BY2]+1Tf2N?1, wherein each X is independently a tertiary amine, a N-alkylimidazole or a pyridine; and each B—X bond is a B—N bond.Type: GrantFiled: May 19, 2006Date of Patent: May 4, 2010Assignee: University of South AlabamaInventor: James H. Davis, Jr.
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Publication number: 20100099866Abstract: An organosilicon compound having an amino group is provided. This compound is represented by the following general formula (1): wherein R1 and R2 respectively represent an unsubstituted or substituted aliphatic monovalent hydrocarbon group containing 1 to 10 carbon atoms with the proviso that the R1 and R2 may together form a ring with the nitrogen atom to which they are bonded, and that R1 and R2 may contain a heteroatom; R3 and R4 independently represent an unsubstituted or substituted monovalent hydrocarbon group containing 1 to 10 carbon atoms; and n represents an integer of 0 to 2. Use of this compound enables production of a polymer product having excellent mechanical properties, high heat resistance, and high transparency. The solution of this compound is stable, and can be stored for a long time, and when used for a polymer modifying agent, it facilitates introduction of amino group and hydroxy group.Type: ApplicationFiled: October 20, 2009Publication date: April 22, 2010Applicant: SHIN-ETSU CHEMICAL CO., LTD.Inventors: Takayuki Honma, Tohru Kubota, Ayumu Kiyomori
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Patent number: 7696347Abstract: The present invention provides compounds which are useful as safe substitutes for the organotin reagent used in coupling reaction for the oxymethylation of aromatic rings, such as alkoxymethylation or hydroxymethylation, with a palladium catalyst and which can dispense with chromatographic purification with silica gel in the production and are suitable for mass production; and compounds applicable even to the oxymethylation of aromatic ring substrates which do not permit coupling reaction by conventional technique or have low reactivity.Type: GrantFiled: March 13, 2006Date of Patent: April 13, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Keigo Tanaka, Satoshi Inoue, Daisuke Ito, Norio Murai, Yosuke Kaburagi, Shuji Shirotori, Shuichi Suzuki, Yoshiaki Ohashi
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Publication number: 20100081633Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.Type: ApplicationFiled: September 25, 2009Publication date: April 1, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Jing Li
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Patent number: 7687497Abstract: The novel C10-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW<600).Type: GrantFiled: October 16, 2007Date of Patent: March 30, 2010Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Kesavaram Narkunan, Xinghai Chen, Harry Kochat, Frederick Hausheer