Boron Or Silicon Containing Patents (Class 544/229)
-
Publication number: 20090221762Abstract: The invention concerns compounds, oligomers, and polymers that contain: (I), (II), (III), or (IV) groups; where “-” indicates points of attachment.Type: ApplicationFiled: January 10, 2007Publication date: September 3, 2009Applicant: THE TRUSSTEES OF THE UNIVERSITY OF PENNSYLVANIAInventors: Michael J. Therien, Kimihiro Susumu
-
Publication number: 20090221818Abstract: Disclosed are peptide-based compounds that include boronic acid or cyano functionality, which efficiently and selectively inhibit fibroblast activation protein alpha. Among other therapeutic utilities, the peptide-based compounds may be useful for the treatment of cancer.Type: ApplicationFiled: July 5, 2006Publication date: September 3, 2009Applicant: Trustees of Tufts CollegeInventors: William W. Bachovchin, Hung-Sen Lai
-
Publication number: 20090215724Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1 and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: February 20, 2009Publication date: August 27, 2009Inventors: Daisy Joe DuBois, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Yan Lou, Timothy D. Owens, Calvin Wesley Yee
-
Patent number: 7576201Abstract: A compound for electrochromic devices. One such compound of the invention is dihydro-disubstituted phenazine (VI): wherein R9 is and n=1-10.Type: GrantFiled: February 28, 2008Date of Patent: August 18, 2009Assignee: Ntera LimitedInventors: Donald Fitzmaurice, David Cummins, David Corr, S. Nagaraja Rao, Gerrit Boschloo
-
Patent number: 7566781Abstract: The present invention provides an imidazopyridine compound represented by formula (I), wherein R1 and R2 each independently represent a C1-6 alkyl group et al; R3 and R4 each independently represent a hydrogen atom, a methyl et al; Ar1 is a divalent substituent representing a monocyclic or bicyclic, 3- to 8-membered aromatic or aliphatic heterocyclic group et al; Ar2 represents an aromatic carbocyclic group, or an aromatic heterocyclic group; W represents —(CH2)m et al, and m indicates an integer of from 0 to 10. This compound acts as a melanin concentrating hormone receptor antagonist, and is useful as treating agents for obesity.Type: GrantFiled: May 9, 2005Date of Patent: July 28, 2009Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Shunji Sakuraba, Minoru Moriya, Hidekazu Takahashi, Hiroyuki Kishino, Makoto Jitsuoka, Minoru Kameda, Akio Kanatani
-
Patent number: 7560550Abstract: Glycosylation of 2,6-diaminopurines or silyl derivatives thereof with a compound of the structure is facilitated by the presence of an optionally silylated 1,3-dicarbonyl compound during glycosylation. Byproducts are minimized, while stereoselectivity may be altered by choice of Lewis acid and other reaction condictions.Type: GrantFiled: July 22, 2004Date of Patent: July 14, 2009Assignee: RFS Pharma, LLCInventors: Wolfgang Döring, Hermann Petersen
-
Publication number: 20090176893Abstract: The present invention provides for a composition comprising a siloxane having the formula: M1DM2 wherein M1=(R1)(R2)(R3)SiO1/2; M2=(R4)(R5)(R6)SiO1/2 and D=(R7)(Z)SiO2/2 where R1, R2, R3, R4, R5, R6 and R7 are each independently selected from the group consisting of 1 to 4 carbon monovalent hydrocarbon radicals, aryl, and a hydrocarbon group of 4 to 9 carbons containing an aryl group; Z is a pendant hydrophilic ionic group selected from the group consisting of R8—RA, R9—RC, and R10—RZ; RA being an anionic substituent, RC a cationic substituent or RZ a zwitterionic substituent on the D group wherein the composition is resistant to hydrolysis under either basic or acidic conditions.Type: ApplicationFiled: December 26, 2007Publication date: July 9, 2009Applicant: MOMENTIVE PERFORMANCE MATERIALS INC.Inventors: Mark D. Leatherman, George A. Policello, Wenqing N. Peng, Liping Zheng, Roland Wagner, Suresh K. Rajaraman, Zijun Xia
-
Publication number: 20090163513Abstract: The present invention relates to a novel process for the preparation of high purity ziprasidone and pharmaceutically acceptable acid addition salts of ziprasidone; and solvates and hydrates thereof using novel intermediates and a purification method for ziprasidone and pharmaceutically acceptable acid addition salts of ziprasidone; and solvates and hydrates thereof. Thus, 1-(1,2-benzisothiazol-3-yl)piperazine is silylated with trimethylsilylchloride in methylene chloride in the presence of triethylamine and the solvent is distilled off to obtain silylated 1-(1,2-benzisothiazol-3-yl)piperazine. The silylated compound is reacted with 5-(2-chloroethyl)-6-chloro-oxindole in the presence of sodium carbonate to obtain ziprasidone.Type: ApplicationFiled: January 27, 2005Publication date: June 25, 2009Applicant: HETERO DRUGS LIMITEDInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Itiyala Srinivas Reddy
-
Publication number: 20090156553Abstract: 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: ApplicationFiled: December 29, 2006Publication date: June 18, 2009Applicant: BASF SEInventors: Eike Hupe, Cyrill Zagar, Matthias Witschel, Toralf Kuhn, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Michael Puhl, Robert Reinhard, Bernd Sievernich, Klaus Grossmann, Thomas Ehrhardt, Michael Rack
-
Publication number: 20090143578Abstract: Processes for preparing entecavir and novel intermediates thereof using carbon-silicon oxidation.Type: ApplicationFiled: February 4, 2009Publication date: June 4, 2009Inventors: Maotang X. Zhou, Emily A. Reiff, Purushotham Vemishetti, Yadagiri R. Pendri, Ambarish K. Singh, Siva Josyula Prasad, Ulhas P. Dhokte, Xinhua Qian, Pia Mountford, Kerry B. Hartung, Helen Sailes
-
Publication number: 20090124559Abstract: 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: December 15, 2006Publication date: May 14, 2009Applicant: Trustees of Tufts College Office of Technology and Industry CollaborationInventors: William W. Bachovchin, Hung-Sen Lai, Wengen Wu
-
Patent number: 7531526Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.Type: GrantFiled: January 2, 2008Date of Patent: May 12, 2009Assignee: Millennium Pharmaceuticals, Inc.Inventors: Julian Adams, Yu-Ting Ma, Ross L. Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
-
Publication number: 20090099132Abstract: 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: October 16, 2007Publication date: April 16, 2009Applicant: Millennium Pharmaceuticals, Inc.Inventors: Edward J. Olhava, Mihaela Diana Danca
-
Publication number: 20090082561Abstract: The present invention provides methods for preparing complexed diaryl boronic acids from alkyl diarylborinates.Type: ApplicationFiled: July 18, 2008Publication date: March 26, 2009Inventors: Ali Tavassoli, Stephen J. Benkovic
-
Publication number: 20090041786Abstract: 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: August 18, 2008Publication date: February 12, 2009Inventors: Hui Li, Sambaiah Thota, David Carroll, Ankush Argade, Kin Tso, Arvinder Sran, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Vanessa Taylor, Robin Cooper, Rajinder Singh, Brian Wong
-
Publication number: 20090005557Abstract: The present invention provides a ?-electron-conjugated organice silane compound that give an organic thin film superior in peeling restance, orientation, crystallinity and eletroconductive properties, and a production method thereof. A ?-electron-conjugated organice silane compound represented by General Formula: R1-SiX1X2X3 (R1 represents an organic group having a particular monocyclic heterocyclic unit; and X1 to X3 are a group giving a hydroxyl group by hydrolysis). A method of producing the organic silane compound, comprising allowing a compound represented by General Formula: R1-Li (R1 is the same as above) or a compound represented by General Formula: R1-MgX5 (R1 is the same as above; and X5 represents a halogen atom) with a compound represented by General Formula: X4-SiX1X2X3 (X1 to X3 are the same as above; and X4 represents a hydrogen or halogen atom or a lower alkoxy group).Type: ApplicationFiled: July 4, 2005Publication date: January 1, 2009Inventors: Masatoshi Nakagawa, Hiroyuki Hanato, Toshihiro Tamura
-
Publication number: 20080318899Abstract: The invention relates to novel chemical compounds and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.Type: ApplicationFiled: November 2, 2005Publication date: December 25, 2008Inventors: Martin Watterson, Linda Van Eldik, Jacques Haiech, Marcel Hibert, Jean-Jacques Bourguignon, Anastasia Velentza, Wenhui Hu, Magdelena Zasadzki
-
Publication number: 20080312183Abstract: Deoxyuridine derivatives of the formula (I) where R1 is H or various substituents; D is —NHCO—, —CONH—, -0-, —C(?O)—, —CH?CH, —C?C—, —NR5—; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl or a stable monocyclic, bicyclic or tricyclic ring system; G is —O—, —S—, —CHR10—, —C(?O)—; J is —CH2—, or when G is CHR10 may also be —O— or —NH—; R10 is H, F, —CH3, —CH2NH2, —CH2OH; —OHR11 is H, F, —CH3, —CH2NH2, —CH2OH, —CH(OH)CH3, CH(NH3)CH3; or R10 and R11 together define an olefinic bond, or together form a —CH2-group, thereby defining a cis or trans cyclopropyl group; have utility in the prophylaxis or treatment of protozoal diseases such as malaria.Type: ApplicationFiled: January 6, 2005Publication date: December 18, 2008Inventors: Ian Gilbert, Corinne Nguyen, Gian Filippo Ruda, Alessandro Schipani, Ganasan Kasinathan, Nils-Gunnar Johansson, Dolores Gonzalez Pacanowska
-
Publication number: 20080303003Abstract: The present invention relates to anthracene derivatives, to the use thereof in organic electroluminescent devices, and to organic electroluminescent devices comprising these compounds.Type: ApplicationFiled: November 17, 2006Publication date: December 11, 2008Applicant: MERCK PATENT GMBHInventors: Holger Heil, Philipp Stoessel, Amir Parham, Horst Vestweber
-
Patent number: 7462404Abstract: Novel boron complexes are blue emissive electroluminescent compounds.Type: GrantFiled: March 12, 2004Date of Patent: December 9, 2008Assignee: Merck Patent GmbHInventors: Poopathy Kathirgamanathan, Matthew Samuel Kirkham, Alexander Kit Lay, Subramaniam Ganeshamurugan, Gnanamoly Paramaswara, Muttulingam Kumaraverl, Arumugam Partheepan, Selvadurai Selvaranjan, Juan Antipan-Lara, Richard Price, Sivagnanasundram Surendrakumar
-
Patent number: 7456195Abstract: The present invention provides novel phenylglycinamide derivatives of Formula (I) or (IV): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables W, W1, Y, Z, R7, R8, R9, and R11 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.Type: GrantFiled: June 22, 2006Date of Patent: November 25, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Xiaojun Zhang, Alexandra A. Nirschl, Yan Zou, Eldon Scott Priestley
-
Publication number: 20080287394Abstract: Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: May 3, 2005Publication date: November 20, 2008Applicant: MERCK & CO., INC.Inventors: John S. Wai, Joseph P. Vacca, Linghang Zhuang, Boyoung Kim, Terry A. Lyle, Catherine M. Wiscount, Melissa S. Egbertson, Lou Anne Neilson, Mark Embrey, Thorsten E. Fisher, Donnette D. Staas
-
Publication number: 20080287578Abstract: 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: ApplicationFiled: December 6, 2004Publication date: November 20, 2008Inventors: Francesco Fuso, Michele Gerster, Gerrit Knobloch, Pierre Rota-Graziosi
-
Publication number: 20080261918Abstract: A compound of any of formulas (I) to (V): wherein at least one of Y and Z includes a Si atom, is of utility in therapy.Type: ApplicationFiled: December 16, 2003Publication date: October 23, 2008Inventors: Graham Andrew Showell, Louise Marie Walsh, Ajay Kumar Mandal, David John Miller
-
Publication number: 20080242859Abstract: 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: ApplicationFiled: March 13, 2006Publication date: October 2, 2008Applicant: Eisai R&D Management Co., LtdInventors: Keigo Tanaka, Satoshi Inoue, Daisuke Ito, Norio Murai, Yosuke Kaburagi, Shuji Shirotori, Shuichi Suzuki, Yoshiaki Ohashi
-
Publication number: 20080230745Abstract: A liquid crystal compound represented by the following formula is provided to enhance the contrast of a liquid crystal device using ferroeloctric liquid crystal: R1 is an alkyl group having 4 to 6 carbon atoms. R2 is an alkyl group having 6 to 18 carbon atoms or an alkoxy group having 6 to 18 carbon atoms. X1 and X2 are each independently hydrogen ox fluorine.Type: ApplicationFiled: March 23, 2007Publication date: September 25, 2008Inventor: Michael Wand
-
Publication number: 20080214501Abstract: Described herein are probes for Bruton's tyrosine kinase (Btk). Such probes are used to characterize and develop Btk-selective inhibitors intended for therapeutic use.Type: ApplicationFiled: November 5, 2007Publication date: September 4, 2008Applicant: PHARMACYCLICS, INC.Inventors: Zhengying PAN, Shyr Jiann Li, Heleen SCHEERENS, Lee HONIGBERG, Erik VERNER
-
Publication number: 20080194520Abstract: The present invention is related to derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: ApplicationFiled: December 19, 2005Publication date: August 14, 2008Inventors: Dominique Swinnen, Agnes Bombrun, Patrick Gerber, Catherine Jorand-Lebrun
-
Publication number: 20080167389Abstract: The present invention provides for a composition comprising a silane having the formula: (R1)(R2)(R3)Si—R4—Si(R5)(R6)(R7) wherein R1, R2, R3, R5, and R6 are each independently selected from the group consisting of 1 to 6 monovalent hydrocarbon radicals, aryl, and a hydrocarbon group of 7 to 10 carbons containing an aryl group; R4 is a hydrocarbon group of 1 to 3 carbons; R7 comprises an anionic, cationic or zwitterionic substituent. The silanes of the present invention exhibit resistance to hydrolysis over a wide pH range.Type: ApplicationFiled: December 10, 2007Publication date: July 10, 2008Applicant: MOMENTIVE PERFORMANCE MATERIALS INC.Inventors: Mark D. Leatherman, George A. Policello, Wenqing Peng, Liping Zheng, Roland Wagner, Suresh K. Rajaraman, Zijun Xia
-
Publication number: 20080161269Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: December 19, 2007Publication date: July 3, 2008Applicants: ASTRAZENECA AB, ASTEX THERAPEUTICS LIMITEDInventors: Stefan Berg, Sofia Karlstrom, Karin Kolmodin, Johan Lindstrom, Jan-Erik Nystrom, Fernando Sehgelmeble, Peter Soderman
-
Publication number: 20080119468Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: September 4, 2007Publication date: May 22, 2008Applicant: Amgen Inc.Inventors: Andrew Tasker, Dawei Zhang, Liping H. Pettus, Rob M. Rzasa, Kelvin K.C. Sham, Shimin Xu, Partha Chakrabarti
-
Patent number: 7365198Abstract: Provided is an organic light emitting device capable of emitting light with high efficiency by incorporating a silyl compound in which a silyl group is directly bonded to an anthracene ring particularly into its light emitting layer.Type: GrantFiled: February 22, 2007Date of Patent: April 29, 2008Assignee: Canon Kabushiki KaishaInventors: Akihito Saitoh, Masataka Yashima
-
Publication number: 20080070864Abstract: Compounds, pharmaceutical compositions and methods for modulating the activity of nuclear receptors are provided. In particular, quinazolinones are provided for modulating the activity of farnesoid X receptor (FXR) and/or orphan nuclear receptors.Type: ApplicationFiled: March 4, 2003Publication date: March 20, 2008Applicant: X-Ceptor Therapeutics, Inc.Inventors: Richard Martin, Jeffrey D. Kahl, Brenton T. Flatt, Ronald Griffith
-
Publication number: 20080038191Abstract: Positron emitting compounds and methods of their production are provided. The compounds have the formula: (F)m G (R)n wherein each R is a group comprising at least one carbon, nitrogen, phosphorus or sulfur atom and G is joined to R through said carbon, nitrogen, phosphorus or sulfur atom; G is silicon or boron; m is 2 to 5 and n is 1 to 3 with m+n=3 to 6 when G is silicon; m is 1 to 3 and n is 1 to 3 with m+n=3 to 4 when G is boron; and wherein the compound further comprises one or more counterions when the above formula is charged; and wherein at least one F is 18 F.Type: ApplicationFiled: February 14, 2005Publication date: February 14, 2008Inventors: David M. Perrin, Richard Ting
-
Patent number: 7329659Abstract: The present invention provides a compound of formula (I): in which Ar and R1 are phenyl or a heteroaromatic group, R2 is generally hydrogen, R3 is hydrogen or alkyl and X, Y and Z are generally CH or N as VR-1 antagonists; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; use of it to manufacture medicaments to treat pain or inflammation; and methods of treating pain or inflammationType: GrantFiled: April 5, 2004Date of Patent: February 12, 2008Assignee: Merck Sharp & Dohme LimitedInventors: Peter Blurton, Frank Burkamp, Stephen Robert Fletcher, A. Brian Jones, Edward Giles McIver
-
Publication number: 20070205715Abstract: Provided is an organic light emitting device capable of emitting light with high efficiency by incorporating a silyl compound in which a silyl group is directly bonded to an anthracene ring particularly into its light emitting layer. In the organic light emitting device including: a pair of electrodes formed of an anode and a cathode, at least one of which being transparent or semi-transparent; and one or more layers containing an organic compound layer interposed between the pair of electrodes, at least one of the layer containing the organic compound contains the following silyl compound, and a layer containing at least one kind of the silyl compound is a light emitting layer.Type: ApplicationFiled: February 22, 2007Publication date: September 6, 2007Applicant: CANON KABUSHIKI KAISHAInventors: Akihito Saitoh, Masataka Yashima
-
Publication number: 20070185058Abstract: Compounds of formula I wherein R1, R2, R4, R5, A, B, D and n are as defined, and pharmaceutically acceptable salts thereof, processes for their preparation, their use as pharmaceuticals and pharmaceutical compositions comprising them.Type: ApplicationFiled: January 25, 2007Publication date: August 9, 2007Inventors: Aurelia Conte, Holger Kuehne, Thomas Luebbers, Patrizio Mattei, Cyrille Maugeais, Werner Mueller, Philippe Pflieger
-
Patent number: 7245073Abstract: It is an object to provide an organic compound that has a bipolar property and also a light emitting property, and further has heat resistance. A quinoxaline derivative represented by a general formula (1) is provided. In the formula, A represents any one of an alkylene chain, silicon (Si), oxygen (O), nitrogen (N), and sulfur (S). R1 to R8, which may be identical or different, individually represent any one of a lower alkyl group, an aryl group, and a heterocyclic group.Type: GrantFiled: July 28, 2004Date of Patent: July 17, 2007Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Satoko Shitagaki, Hiroko Abe, Satoshi Seo
-
Patent number: 7198958Abstract: A fluorescent label compound of formula where Z is a reactive group that can be used for covalent coupling of the fluorescent label compound to other molecule. Either the fluorophore is a dipyrrometheneboron difluoride dye and Y is a water-solubilizing moiety, or Y is —CH2CH2SO3? X+ where X+ is a cation. The use of the compounds in bianalytical assays and cytological or histological staining methods, and a method for increasing the hydrophilicity of fluorescent compounds, are also disclosed.Type: GrantFiled: July 1, 2002Date of Patent: April 3, 2007Assignee: Arctic Diagnostics OyInventors: Niko Meltola, Aleksi Soini
-
Patent number: 7179804Abstract: The present invention relates to selective NK-1 receptor antagonists of Formula (I); or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykininsType: GrantFiled: April 22, 2003Date of Patent: February 20, 2007Assignee: Eli Lilly and CompanyInventors: Albert Kudzovi Amegadzie, Kevin Matthew Gardinier, Erik James Hembre, Jian Eric Hong, Louis Nickolaus Jungheim, Michael Alan Robertson, Kenneth Allen Savin
-
Patent number: 7164018Abstract: The present invention relates to polymers characterized by novel silicon linkers based on the carbamyl piperazine moiety, methods of preparing these polymers and their use in the solid phase synthesis of compounds or libraries of compounds embracing a phenyl ring in their structure.Type: GrantFiled: January 29, 2004Date of Patent: January 16, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Enzo Cereda, Carlo Maria Pellegrini, Monica Quai, Walter Barbaglia
-
Patent number: 7135475Abstract: The present invention is a 1,3,8 substituted xanthine derivative of formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specification. Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.Type: GrantFiled: June 12, 2003Date of Patent: November 14, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Peter W. Dunten, Louise H. Foley, Nicholas J. S. Huby, Sherrie L. Pietranico-Cole, Weiya Yun
-
Patent number: 7119080Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.Type: GrantFiled: December 8, 2003Date of Patent: October 10, 2006Assignee: Millennium Pharmaceuticals, Inc.Inventors: Julian Adams, Yu-Ting Ma, Ross L. Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
-
Patent number: 7109323Abstract: The invention relates to the formulation of pharmaceutical compounds. More particularly, the invention provides stable, pharmaceutically acceptable compositions prepared from boronic acid compounds and methods for preparing the compositions. The invention also provides novel boronate ester compounds. The invention further provides boronic acid anhydride compounds useful in the methods of the invention.Type: GrantFiled: December 23, 2003Date of Patent: September 19, 2006Assignees: The United States of America as represented by the Department of Health and Human Services, Millennium Pharmaceutical, Inc.Inventors: Louis Plamondon, Louis Grenier, Julian Adams, Shanker Lal Gupta
-
Patent number: 7094897Abstract: The present invention describes novel organometallic compounds which are phosphorescence emitters. Such compounds can be used as active components (=functional materials) in a series of different types of application which can be classed within the electronics industry in the broadest sense. The compounds according to the invention are described by the formulae (I), (Ia), (II) and (IIa).Type: GrantFiled: April 3, 2002Date of Patent: August 22, 2006Assignee: Covion Organic Semiconductors GmbHInventors: Philipp Stossel, Hubert Spreitzer, Heinrich Becker
-
Patent number: 7034152Abstract: Processes are disclosed for preparing the antiviral agent entecavir. A resin adsorption process for the isolation and purification of entecavir is also disclosed. Various intermediates useful in the preparation of entecavir are also disclosed.Type: GrantFiled: December 11, 2003Date of Patent: April 25, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Yadagiri R. Pendri, Chung-Pin H. Chen, Sunil S. Patel, Jeffrey M. Evans, Jing Liang, David R. Kronenthal, Gerald L. Powers, Siva Josyula Prasad, Jeffrey T. Bien, Zhongping Shi, Ramesh N. Patel, Amit Banerjee, Yeung Yu Chan, Sushil K. Rijhwani, Ambarish K. Singh, Shaopeng Wang, Milan Stojanovic, David J. Kucera, Richard P. Polniaszek, Charles Lewis, John Thottathil, Dhileepkumar Krishnamurty, Maotang X. Zhou, Purushotham Vemishetti
-
Patent number: 6998484Abstract: The present invention relates to a new method for the synthesis of purine LNA (Locked Nucleic Acid) analogues which provides a higher overall yield. The method comprising a regioselective 9-N purine glycosylation reaction followed by a one-pot nucleophilic aromatic substitution reaction of the 6-substituent in the purine ring and simultaneous nucleophile-induced intramolecular ring closure of the C-branched carbohydrate to form novel purine LNA analogues. The novel strategy is illustrated by the synthesis of the novel compound (1S,3R,4R,7S)-7-benzyloxy-1-methanesulfonylmethyl-3-(guanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane which is easily converted into (1S,3R,4R,7S)-7-hydroxy-1-hydroxymethyl-3-((2-N-isobutyrylguanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane after isobutyryl protection of the 2-amino purine group and subsequent substitution of 1-methanesulfonyl with benzoate, debenzoylation and debenzylation.Type: GrantFiled: October 4, 2001Date of Patent: February 14, 2006Assignee: Santaris Pharma A/SInventors: Troels Koch, Flemming Ressig Jensen
-
Patent number: 6992189Abstract: In its several embodiments, this invention discloses novel processes to prepare the compounds of formula II and formula IV:Type: GrantFiled: March 27, 2003Date of Patent: January 31, 2006Assignee: Schering CorporationInventors: William Leong, Minzhang Chen, Bosco A. D'sa, Man Zhu, Tong Xiao, Xiongwei Shi, Suhan Tang, Dinesh Gala, Andrew J. Goodman, Christopher M. Nielsen, Gary M. Lee, Juan A. Gamboa, Andrew D. Jones
-
Patent number: 6964966Abstract: This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.Type: GrantFiled: April 23, 2002Date of Patent: November 15, 2005Assignee: Wockhardt LimitedInventors: Noel John De Souza, Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Shiv Kumar Agarwal, Shrikant V. Gupte, Dilip J. Upadhyay, Satish B. Bhawsar, Rupinder K. Beri, Kandepu Sreenivas, Sheela Chandrasekharan Nair, Milind Chintaman Shukla, Yati Chugh, Nitin Shetty, Ravindra D. Yeole, M. Madhav Reddy
-
Patent number: 6958319Abstract: The present invention provides stable compounds prepared from boronic acid and lyophilized compounds thereof of the formula (1): in which Z1 and Z2 are moieties derived from sugar. The invention also provides methods for preparing such compounds. Lyophilizing a mixture comprising a boronic acid compound and a moiety derived from sugar produces a stable composition that readily releases the boronic acid compound upon reconstitution in aqueous media.Type: GrantFiled: September 18, 2003Date of Patent: October 25, 2005Assignee: The United States of America as represented by the Department of Health and Human ServicesInventor: Shanker Lal Gupta
