Boron Or Silicon Containing Patents (Class 544/229)
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Publication number: 20130309170Abstract: This document relates to compounds useful for targeting PARP1. Also provided herein are methods for using such compounds to detect and image cancer cells.Type: ApplicationFiled: November 22, 2011Publication date: November 21, 2013Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Thomas Reiner, Edmund J. Keliher, Ralph Weissleder
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Patent number: 8569481Abstract: Capture compounds and collections thereof and methods using the compounds for the analysis of biomolecules are provided. In particular, collections, compounds and methods are provided for analyzing complex protein mixtures, such as the proteome. The compounds are multifunctional reagents that provide for the separation and isolation of complex protein mixtures. Each compound has the formula: wherein: Z is a trityl derivative; X, the reactivity function, covalently binds to amino acid side chains of proteins; Y, the selectivity function, modulates binding of X to the amino acid side chains in proteins such that X binds to fewer proteins when Y is present than in its absence; and Q permits separation or immobilization of the capture compound. Automated systems for performing the methods also are provided.Type: GrantFiled: November 2, 2010Date of Patent: October 29, 2013Assignee: Pharmaceuticals, Inc.Inventors: Hubert Köster, Suhaib Siddigi, Daniel P. Little
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Publication number: 20130280211Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: June 17, 2013Publication date: October 24, 2013Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. ST. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
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Publication number: 20130281402Abstract: The disclosure includes hydroxamic compounds of Formula I: (Formula I) wherein Z, L, R1, R2, and R3 are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.Type: ApplicationFiled: January 6, 2012Publication date: October 24, 2013Applicant: CRYSTAL BIOPHARMACEUTICAL LLCInventors: Yi Chen, Yu Chen
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Publication number: 20130274471Abstract: A compound for an organic photoelectric device, an organic photoelectric device including the same, and a display device including the same the compound being represented by the following Chemical Formula 1:Type: ApplicationFiled: June 12, 2013Publication date: October 17, 2013Inventors: Kyu-Yeon IN, Myeong-Soon KANG, Ho-Kuk JUNG, Nam-Soo KIM, Eui-Su KANG, Mi-Young CHAE, Jin-Seong PARK
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Publication number: 20130261081Abstract: A heterocyclic compound represented by the general formula (1) or a salt thereof: wherein m, l, and n respectively represent an integer of 1 or 2; X represents —O— or —CH2—; R1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R2 and R3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R2 and R3 are bonded to form a cyclo-C3-C8 alkyl group; and R4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).Type: ApplicationFiled: September 12, 2011Publication date: October 3, 2013Inventors: Nobuaki Ito, Hirofumi Sasaki, Kuninori Tai, Tomoichi Shinohara
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Patent number: 8546564Abstract: Provided herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof, or mixtures thereof, wherein Z1, Z2, X1, X2, X3, R1, R2 R3, m and n are defined herein. Also provided are pharmaceutically acceptable compositions that include a compound of formula I and a pharmaceutically acceptable excipient. Also provided are methods for treating FAAH-mediated disorders comprising administering to a subject in need thereof a therapeutically effective amount of a compound or composition of the present invention.Type: GrantFiled: April 7, 2010Date of Patent: October 1, 2013Assignee: Infinity Pharmaceuticals, Inc.Inventors: Alfredo C. Castro, Michael J. Grogan, Daniel A. Snyder
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Publication number: 20130252024Abstract: Disclosed are a compound that emits fluorescence, particularly in its solid state, and is suited to provide a color converting material with various improved performance properties over prior art and a light emitter, a color conversion filter, a color conversion device, and a photoelectric device each containing the compound; particularly a Schiff base type compound of formula (I) and a coloring material, a color conversion layer, a light absorbing layer, a color conversion filter, a light absorbing filter, a color-converting light-emitting device, and a photoelectric device each containing the compound. The definition of the symbols in formula (I) is the same as in the specification.Type: ApplicationFiled: May 9, 2013Publication date: September 26, 2013Applicant: ADEKA CORPORATIONInventors: Mitsuhiro OKADA, Koichi SHIGENO
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Publication number: 20130253191Abstract: The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.Type: ApplicationFiled: February 7, 2013Publication date: September 26, 2013Applicant: Incyte CorporationInventor: Jiacheng Zhou
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Publication number: 20130253190Abstract: The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.Type: ApplicationFiled: February 7, 2013Publication date: September 26, 2013Applicant: Incyte CorporationInventor: Jiacheng Zhou
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Publication number: 20130244448Abstract: Classes of liquid aminosilanes have been found which allow for the production of silicon carbo-nitride films of the general formula SixCyNz. These aminosilanes, in contrast, to some of the precursors employed heretofore, are liquid at room temperature and pressure allowing for convenient handling. In addition, the invention relates to a process for producing such films. The classes of compounds are generally represented by the formulas: and mixtures thereof, wherein R and R1 in the formulas represent aliphatic groups typically having from 2 to about 10 carbon atoms, e.g., alkyl, cycloalkyl with R and R1 in formula A also being combinable into a cyclic group, and R2 representing a single bond, (CH2)n, a ring, or SiH2.Type: ApplicationFiled: September 13, 2012Publication date: September 19, 2013Applicant: AIR PRODUCTS AND CHEMICALS, INC.Inventors: Manchao Xiao, Arthur Kenneth Hochberg
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Publication number: 20130237499Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: ApplicationFiled: March 1, 2013Publication date: September 12, 2013Applicant: Bristol-Myers Squibb CompanyInventors: Zhizhen Barbara Zheng, Stanley D'Andrea, David R. Langley, B. Narasimhulu Naidu
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Publication number: 20130225571Abstract: The invention relates to new crystalline forms of processes for manufacturing a compound of formula 5, or a stereoisomer, tautomer or a salt thereof, wherein the substituents are as defined in the specification. The invention further relates to new manufacturing processes for specific solid forms of Compound A and its salts, to such solid forms and to use of said solid forms for the therapeutic treatment of warm-blooded animals.Type: ApplicationFiled: September 29, 2011Publication date: August 29, 2013Applicant: NOVARTIS AGInventors: John Vincent Calienni, Marilyn De La Cruz, Dietmar Flubacher, Baoqing Gong, Prasad Koteswara Kapa, Piotr H. Karpinski, Hui Liu, Pascal Michel, Rasmus Mose, Maria Caterina Testa, Liladhar Murlidhar Waykole
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Patent number: 8513218Abstract: 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: GrantFiled: March 30, 2011Date of Patent: August 20, 2013Assignee: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Jing Li
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Publication number: 20130210158Abstract: Quaternary nitrogen heterocyclic boronic acid-containing compounds are described, which are sensitive to glucose and fructose, as well as a variety of other physiologically important analytes, such as aqueous chloride and iodide, and a method of using the compounds. Also disclosed is a contact lens doped with the quaternary nitrogen heterocyclic boronic acid-containing compound, and a method of using the doped contact lens to measure the concentration of analyte in tears under physiological conditions.Type: ApplicationFiled: December 24, 2012Publication date: August 15, 2013Inventors: CHRIS D. GEDDES, RAMACHANDRAM BADUGU, JOSEPH R. LAKOWICZ
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Publication number: 20130203675Abstract: Asymmetric bifunctional silyl (ABS) monomers comprising covalently linked pharmaceutical, chemical and biological agents are described. These agents can also be covalently bound via the silyl group to delivery vehicles for delivering the agents to desired targets or areas. Also described are delivery vehicles which contain ABS monomers comprising covalently linked agents and to vehicles that are covalently linked to the ABS monomers. The silyl modifications described herein can modify properties of the agents and vehicles, thereby providing desired solubility, stability, hydrophobicity and targeting.Type: ApplicationFiled: September 15, 2011Publication date: August 8, 2013Inventors: Joseph M. DeSimone, Matthew Finniss, Mary Napier, Ashish Pandya, Matthew Parrott
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Publication number: 20130203988Abstract: The invention relates to processes of making bortezomib of formula (1) enantiomers thereof and/or intermediates thereof, comprising at least one step of coupling a carboxylic acid with an amine, wherein the coupling step is performed in a presence of the compound of formula (8), wherein A is C1-C6 alkyl group, preferably wherein A is n-propyl group.Type: ApplicationFiled: October 14, 2010Publication date: August 8, 2013Applicant: Synthon BVInventors: Jakub Castulik, Miroslav Zabadal
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Publication number: 20130196362Abstract: Provided herein are improved fluorogenic compounds and probes that can be used as reagents for measuring, detecting and/or screening peroxynitrite. The fluorogenic compounds of the invention can produce fluorescence colors, such as green, yellow, red, or far-red. Also provided herein are fluorogenic compounds for selectively staining peroxynitrite in the mitochondria of living cells. Provided also herein are methods that can be used to measure, directly or indirectly, the presence and/or amount of peroxynitrite in chemical samples and biological samples such as cells and tissues in living organisms. Also provided are high-throughput screening methods for detecting or screening peroxynitrite or compounds that can increase or decrease the level of peroxynitrite in chemical and biological samples.Type: ApplicationFiled: January 30, 2013Publication date: August 1, 2013Applicant: THE UNIVERSITY OF HONG KONGInventor: THE UNIVERSITY OF HONG KONG
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Publication number: 20130165390Abstract: 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: November 2, 2012Publication date: June 27, 2013Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventor: Millennium Pharmaceuticals, Inc.
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Publication number: 20130150325Abstract: The present application relates to novel 3-(fluorovinyl)pyrazole derivatives, to processes for their preparation, to their use for treatment and/or prevention of diseases and to their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: July 17, 2012Publication date: June 13, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Michael HÄRTER, Hartmut BECK, Karl-Heinz THIERAUCH, Peter ELLINGHAUS, Susanne GRESCHAT, Joachim SCHUHMACHER
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Publication number: 20130150292Abstract: The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.Type: ApplicationFiled: September 14, 2012Publication date: June 13, 2013Applicant: Trustees of Tufts CollegeInventors: William W. Bachovchin, Hung-Sen Lai, Wengen Wu
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Publication number: 20130142807Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.Type: ApplicationFiled: January 25, 2013Publication date: June 6, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventor: Rigel Pharmaceuticals, Inc.
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Patent number: 8450301Abstract: The invention relates to the use of piperazine compounds of formula (I) or the agriculturally useful salts of piperazine compounds of formula (I) as herbicides, the variables in formula (I) being defined as cited in the claims and the description.Type: GrantFiled: December 29, 2006Date of Patent: May 28, 2013Assignee: BASF SEInventors: Eike Hupe, Cyrill Zagar, Matthias Witschel, Toralf Kühn, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Michael Puhl, Robert Reinhard, Bernd Sievernich, Klaus Groβmann, Thomas Ehrhardt, Michael Rack
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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: 20130115194Abstract: The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: November 2, 2012Publication date: May 9, 2013Inventors: Daniel D. LONG, Robert Murray MCKINNELL, Lan JIANG, Mandy LOO, Kassandra LEPACK, Lori Jean VAN ORDEN, Gavin OGAWA, Xiaojun HUANG, Weijiang ZHANG
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Patent number: 8436166Abstract: Vinylsilane compounds having a specific amino group, typically diethylaminopropyldimethylvinylsilane, N-methylpiperazinylpropyldimethylvinylsilane, and bistrimethylsilylaminopropyldimethylvinylsilane are novel and useful as a modifier for polymers.Type: GrantFiled: June 10, 2010Date of Patent: May 7, 2013Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Yoichi Tonomura, Tohru Kubota
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Publication number: 20130109653Abstract: The present invention provides a substituted pyridine compound or a pharmacologically acceptable salt thereof which has excellent CETP inhibition activity and is useful as a medicament. The present invention provides a compound represented by a general formula (I), wherein R1 is H, optionally substituted alkyl, OH, optionally substituted alkoxy, alkylsulfonyl, optionally substituted amino, carboxy, optionally substituted carbonyl, CN, halogeno, optionally substituted phenyl, optionally substituted aromatic heterocyclyl, optionally substituted saturated heterocyclyl, optionally substituted saturated heterocyclyloxy or optionally substituted saturated heterocyclylcarbonyl, etc., and the like.Type: ApplicationFiled: July 8, 2011Publication date: May 2, 2013Applicants: UBE INDUSTRIES, LTD., DAIICHI SANKYO COMPANY, LIMITEDInventors: Tsuyoshi Nakamura, Hidenori Namiki, Naoki Terasaka, Akiko Shima, Masahiko Hagihara, Noriaki Iwase, Katsunori Takata, Osamu Kikuchi, Kazunari Tsuboike, Hiroyuki Setoguchi, Kenji Yoneda, Hidetoshi Sunamoto, Koji Ito
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Patent number: 8426435Abstract: The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a compound represented by formula (1) or a pharmacologically acceptable salt thereof: wherein, R1, R3, R4, and R6 are each independently C1-3 alkyl; and R2 and R5 are each independently a hydrogen atom or C1-3 alkyl.Type: GrantFiled: October 22, 2012Date of Patent: April 23, 2013Assignee: Shiseido Company Ltd.Inventors: Naoto Hanyu, Tomoko Saito, Takako Shibata, Kiyoshi Sato, Kimihiro Ogino
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Patent number: 8415295Abstract: Dipeptidyl peptidase IV (DPP-IV)-inhibiting compounds are provided that have formula I: wherein n is 1 to 3; X is CH2; S; O; CF2 or C(CH3)2; Z is H; halogen; hydroxyl; (C1-6)alkoxy; (C1-12)alkyl; (C3-12)cycloalkyl; phenyl; or heteroaryl; where the phenyl and heteroaryl groups are optionally mono- or independently plurisubstituted with R7; optionally, X together with an adjacent ring carbon and Z form a fused cyclopropyl; and optionally, one of the bonds in the ring containing X is a double bond; and CriRii, R1, R1, R3, R4 and R5 are as described herein. Methods for preparing these compounds, and methods for treating diabetes, especially Type II diabetes, and other related diseases are described using the compounds of formula I in pharmaceutical compositions which contain these compounds. Pharmaceutical compositions which contain combinations of these compounds with other antidiabetic agents are also described herein.Type: GrantFiled: January 22, 2010Date of Patent: April 9, 2013Assignee: Phenomix CorporationInventors: David Alan Campbell, David T. Winn, Juan Manuel Betancort
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Publication number: 20130085277Abstract: The present invention relates to a process for the preparation of bortezomib (Formula I) and its intermediates.Type: ApplicationFiled: February 9, 2011Publication date: April 4, 2013Applicant: RANBAXY LABORATORIES LIMITEDInventors: Satish Kumar, Venugopal Venkatarama Durvasula, Parendu Dhirajlal Rathod, Ram Chander Aryan
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Publication number: 20130085278Abstract: The present invention provides methods for preparing 5-[2-[7-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]ethynyl]-2-pyridinamine (compound A), which is useful for the treatment of depression and other CNS disorders. The present methods are useful for preparing compound A on large scale in manufacturing facilities.Type: ApplicationFiled: September 27, 2012Publication date: April 4, 2013Applicant: Hoffmann-La Roche IncInventor: Hoffmann-La Roche Inc
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Publication number: 20130060026Abstract: This invention relates to processes and intermediates for making {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, useful in the treatment of diseases related to the activity of Janus kinases (JAK) including inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: ApplicationFiled: September 6, 2012Publication date: March 7, 2013Applicant: INCYTE CORPORATIONInventors: Jiacheng Zhou, Yongzhong Wu, Pingli Liu, Ganfeng Cao
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Publication number: 20130052281Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: August 22, 2012Publication date: February 28, 2013Applicant: Takeda Pharmaceutical Company LimitedInventors: William FARNABY, Charlotte FIELDHOUSE, Catrina KERR, Natasha KINSELLA, David LIVERMORE, Kevin MERCHANT, David MILLER, Katherine HAZEL
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Publication number: 20130053343Abstract: Compounds having the structures below that are TPH1 inhibitors are provided: The compounds are useful of, e.g., to increase bone mass. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis.Type: ApplicationFiled: November 2, 2010Publication date: February 28, 2013Applicant: The Trustees of Columbia University in th City ofInventors: Donald Landry, Shi-Xian Deng
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Publication number: 20130045948Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein A, W, X, G, R1, R2, R3, R4, m and n are as defined in the disclosure. Also disclosed are pharmaceutical compositions containing the compounds of Formula 1 and methods for treating a disease or condition mediated by fatty acid amide hydrolase activity comprising applying a therapeutically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: December 10, 2010Publication date: February 21, 2013Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: Mei H. Dung, Robert James Pasteris
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Publication number: 20130045497Abstract: The present invention provides compounds useful for detection of hydrogen peroxide and methods of using same.Type: ApplicationFiled: August 16, 2012Publication date: February 21, 2013Applicant: Promega CorporationInventors: Dieter Klaubert, John Shultz, James Unch, Michael P. Valley, Hui Wang, Wenhui Zhou
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Patent number: 8373159Abstract: The present invention relates to an organic light-emitting diode comprising an anode An and a cathode Ka and a light-emitting layer E which is arranged between the anode An and the cathode Ka and comprises at least one carbene complex and if appropriate at least one further layer, where the light-emitting layer E and/or the at least one further layer comprises at least one compound selected from disilylcarbazoles, disilyldibenzofurans, disilyldibenzothiophenes, disilyldibenzophospholes, disilyldibenzothiophene S-oxides and disilyldibenzothiophene S,S-dioxides, to a light-emitting layer comprising at least one of the aforementioned compounds and at least one carbene complex, to the use of the aforementioned compounds as matrix material, hole/exciton blocker material, electron/exciton blocker material, hole injection material, electron injection material, hole conductor material and/or electron conductor material, and to a device selected from the group consisting of stationary visual display units, mobile visuType: GrantFiled: June 25, 2008Date of Patent: February 12, 2013Assignee: BASF SEInventors: Nicolle Langer, Klaus Kahle, Christian Lennartz, Oliver Molt, Evelyn Fuchs, Jens Rudolph, Christian Schildknecht, Soichi Watanabe, Gerhard Wagenblast
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Publication number: 20130018065Abstract: The present invention relates in general to the field of organic chemistry and in particular to a process for the preparation of 5-((E)-2-((2S,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-methanesulfonylamino)pyrimidine (RSVL) as well as a process for preparing crystalline 5-((E)-2-((2S,4R)-4-(tert-butyldimethylsilyloxy)-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVLTBS) useful as key intermediates for the preparation of rosuvastatin or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: December 15, 2010Publication date: January 17, 2013Applicant: Lek Pharmaceuticals D.D.Inventors: Samo Andrensek, Jolanda Anzel, Marjeta Hocevar, Zdenko Casar
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Publication number: 20130005968Abstract: The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.Type: ApplicationFiled: September 14, 2012Publication date: January 3, 2013
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Publication number: 20130005687Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.Type: ApplicationFiled: September 12, 2012Publication date: January 3, 2013Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C. Rech, Wei Xiao
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Publication number: 20120328570Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: September 7, 2012Publication date: December 27, 2012Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
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Publication number: 20120322946Abstract: Organosilicon compounds are represented by the following formula: wherein R is a hydrolyzable group, R? is an alkyl having 1 to 4 carbon atoms, A is an alkylene having 1 to 6 carbon atoms, X is O or S, Y is —NH— or S, L1 and L2 are C or N, Z and M are —NH—, O or S, R1 to R11 are H, alkyl having 1 to 6 carbon atoms, alkoxy or fluoroalkyl, or amino, m is 1 to 3, and n is 0 to 3. R1 and R2 or R2 and R3 may bonded together. R5 and R6 or R9 and R10 may directly bond together. R4 and R7 or R8 and R11 may form a ring skeleton. Their production processes, pressure-sensitive adhesive compositions, self-adhesive polarizers and LCDs are also disclosed.Type: ApplicationFiled: August 30, 2012Publication date: December 20, 2012Applicant: SHIN-ETSU CHEMICAL CO., LTD.Inventor: Kazuhiro Tsuchida
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Publication number: 20120305851Abstract: The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices, and to electronic devices which contain these compounds.Type: ApplicationFiled: December 17, 2010Publication date: December 6, 2012Applicant: Merck Patent GmbHInventors: Junyou Pan, Herwig Buchholz, Teresa Mujica-Fernaud, Irina Martynova
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Publication number: 20120309714Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: ApplicationFiled: December 15, 2010Publication date: December 6, 2012Applicant: H. Lundbeck A/SInventors: Ask Püschl, Jacob Nielsen, Jan Kehler, John Paul Kilburn, Mauro Marigo, Morten Langgård
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Patent number: 8324234Abstract: The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a compound represented by formula (1) or a pharmacologically acceptable salt thereof: wherein, R1, R3, R4, and R6 are each independently C1-3 alkyl; and R2 and R5 are each independently a hydrogen atom or C1-3 alkyl.Type: GrantFiled: February 6, 2009Date of Patent: December 4, 2012Assignee: Shiseido Company Ltd.Inventors: Naoto Hanyu, Tomoko Saito, Takako Shibata, Kiyoshi Sato, Kimihiro Ogino
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Publication number: 20120302586Abstract: Inhibitors of parasitic dihydroorotate dehydrogenase enzyme (DHOD) are candidate therapeutics for treating malaria. Illustrative of such therapeutic agents include the compound: and a triazolopyrimidine class of compounds that conform to Formula IX: and their solvates, stereoisomers, tautomers and pharmaceutically acceptable salts.Type: ApplicationFiled: September 28, 2010Publication date: November 29, 2012Applicants: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM, MONASH UNIVERSITY, CLAYTON, GLAXOSMITHKLINE INVESTIGACION Y DESARROLLO, S.L, UNIVERSITY OF WASHINGTON, MEDICINES FOR MALARIA VENTUREInventors: Pradipsinh K. Rathod, David Floyd, Jeremy Burrows, Alka Marwaha, Ramesh Gujjar, Jose Coteron-Lopez, Margaret Phillips, Susan A. Charman, David Matthews
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Publication number: 20120295874Abstract: The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes one or more pharmacophores which potentially binds to a target molecule with a dissociation constant of less than 300 ?M and a linker element connected to the pharmacophore. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to the pharmacophore.Type: ApplicationFiled: October 7, 2010Publication date: November 22, 2012Applicants: CORNELL UNIVERSITY, COFERON, INC., PURDUE RESEARCH FOUNDATIONInventors: Francis Barany, Maneesh Pingle, Sarah Filippa Giardina, Donald Bergstrom, Lee Daniel Arnold
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Publication number: 20120289699Abstract: The present invention provides a synthetic process for producing bortezomib using a novel intermediate. The present invention also provides a process for purifying bortezomib anhydride, and a new crystalline polymorph of bortezomib anhydride.Type: ApplicationFiled: May 12, 2011Publication date: November 15, 2012Inventors: Julian Paul Henschke, Aiping Xie, Xin Yan Huang, Yung Fa Chen
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Patent number: 8309740Abstract: The present invention relates to a method for one-pot synthesis of ionic liquid with fluoroalkyl group, more particularly to a method for one-pot synthesis of ionic liquid with fluoroalkyl group represented by the following Chemical Formula 1 by adding and reacting a nitrogen-containing compound, a Brønsted acid of the formula YH and a fluoroolefin compound of the formula CFR1?CR2R3 in a single reactor: wherein represents a nitrogen-containing compound; Y? represents an anion of the Brønsted acid; and R1, R2 and R3, which may be same or different, represent hydrogen, fluorine, C1-C10 alkyl or C1-C10 fluoroalkyl having from 1 to 23 fluorine atoms.Type: GrantFiled: August 15, 2008Date of Patent: November 13, 2012Assignee: Korea Institute of Science and TechnologyInventors: Hyun Joo Lee, Dong Jin Suh, Byoung Sung Ahn, Hong Gon Kim, Chang Soo Kim, Hoon Sik Kim
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Publication number: 20120269797Abstract: Proteasome inhibitors (PI) are used for inhibiting the maturation of dendritic cells (DZ) and thus in the treatment or the prophylaxis of allergies, asthma, tissue or transplant rejection or autoimmune diseases. The concentration of the proteasome inhibitors lies preferably in the range of 10 nM to 10 ?M, based on the peripheral blood or the cytoplasm.Type: ApplicationFiled: July 15, 2010Publication date: October 25, 2012Inventors: Ulrich Schubert, Elisabeth Zinser, Alexander Steinkasserer