Abstract: Methods for separating oligonucleotides are described. The oligonucleotides to be separated include separation tags attached to each end of the oligonucleotides.
Abstract: Methods and compounds useful for the purification of oligonucleotides and their analogs are provided wherein the oligonucleotides are contaminated with at least one oligonucleotide having at least one abasic site by the formation of imines at the aldehyde moiety of the abasic site and subsequent separation based on extractions, precipitations or chromatography.
Abstract: Methods for the preparation of oligonucleotides having bioreversible phosphate blocking groups are disclosed. The oligonucleotides are prepared utilizing amidite type chemistry wherein the bioreversible phosphorus protecting group is formed as an integral part of the amidite reagent.
Abstract: The present invention comprises 7-deaza L-nucleosides having unexpectedly high inhibitory activity against the hepatitis B virus. The invention further comprises pharmaceutical compositions comprising such compounds as well as methods of treating mammals, particularly humans, infected with HBV and other viral infections.
Type:
Application
Filed:
December 20, 2002
Publication date:
August 14, 2003
Applicant:
Micrologix Biotech Inc.
Inventors:
Khalid Mekouar, Robert Deziel, Samir Mounir, Radhakrishnan P. Iyer
Abstract: A process for efficiently producing a nucleic acid derivative by condensing a specific nitrogen-containing heterocyclic compound such as a dinitrogen 6-membered heterocyclic compound or a trinitrogen 5-membered heterocyclic compound with a pentose using a less expensive and safe reagent. Namely, a process for producing a nucleic acid derivative by condensing a dinitrogen 6-membered heterocyclic compound or a trinitrogen 5-membered heterocyclic compound with a pentose in the presence of an iron halide.
Abstract: An efficient method for producing high quality beta glucan enriched soluble dietary fiber products is described. An aqueous extraction slurry of beta glucan-containing grain material is homogenized, acidified and enzymatically digested to reduce viscosity and optimize separation of insolubles from the aqueous extract solution. The resulting extract is heat processed to precipitate denatured protein components and subsequently dried or otherwise processed to provide the products for use as food additives or dietary supplements.
Type:
Application
Filed:
February 4, 2002
Publication date:
August 14, 2003
Inventors:
Bernhard H. Van Lengerich, Olaf Gruess, Friedrich P. Meuser
Abstract: The present invention relates to the dibenzoazulene compounds represented by formula I as well as to their pharmaceutical preparations for the inhibition of tumor necrosis factor alpha (TNF-&agr;) and interleukine 1 (IL-1) in mammals at all diseases and conditions where these mediators are excessively secreted. The compounds of the present invention also demonstrate an analgetic action and can be used to relieve pain.
Abstract: Novel compounds are disclosed which inhibit the activity of phospholipase enzymes in a mammal, particularly cytosolic phospholipase A2. Pharmaceutical compositions comprising such compounds and methods of treatment using such compositions are also disclosed.
Type:
Application
Filed:
May 8, 2002
Publication date:
August 14, 2003
Applicant:
American Home Products Corporation
Inventors:
Jasbir S. Seehra, Neelu Kaila, John C. McKew, Frank Lovering, Jean E. Bemis, YiBin Xiang
Abstract: (2R)-1-[3,5-bis(trifluoromethyl)benzoyl]-4-[2-[(2S)-2-(methoxymethyl)morpholino]ethyl]-2-(3-hydroxy-4-methylbenzyl)piperazine dihydrochloride is obtained by debenzylating (2R)-4-benzyl-1-[3,5-bis(trifluoromethyl)-benzoyl]-2-(3-hydroxy-4-methylbenzyl)piperazine, then N-alkylating and converting to hydrochloride.
Abstract: Fused bicyclic amines of formula (1) are described wherein Ar is an aryl or heteroaryl group; Y is a —S(O2)— or —C(O)— group; R1 is a hydrogen or halogen atom or an alkyl, haloalkyl, alkoxy, haloalkoxy or cyano group; X is a nitrogen atom or a C(R1a) group where R1a is as defined for R1 and may be the same or different; W and Z are each a carbon atom and together with U form an optionally substituted five- or six-membered monocyclic aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the activity of Class I receptor tyrosine kinases and are of use in the prophylaxis and treatment of hyperproliferative disorders such as cancer, psoriasis, restenosis, atherosclerosis and fibrosis.
Type:
Application
Filed:
February 4, 2003
Publication date:
August 14, 2003
Inventors:
David Festus Charles Moffat, Peter David Davis
Abstract: The invention relates to pyrimido[5,4-e][1,2,4]triazine-5,7-diamine compounds which are useful for inhibiting protein tyrosine phosphatases, particularly PTP1B.
Type:
Application
Filed:
December 10, 2002
Publication date:
August 14, 2003
Inventors:
Kevin Richard Guertin, Lina Quattrocchio Setti
Abstract: The present invention relates to protected valacyclovir, N-tert-butoxycarbonyl-L-valine 2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy] ethyl ester, and a method of making it. The present invention further relates to a method of making valacyclovir including the steps of coupling an amine protected valine selected from N-t-butoxycarbonyl valine and N-formyl valine with acyclovir using a coupling agent to form a protected valacyclovir, and deprotecting the protected valacyclovir to form valacyclovir or a pharmaceutically acceptable salt thereof. The present invention further relates to valacyclovir in pure form, a method of making pure valacyclovir, and to compositions containing pure valacyclovir.
Type:
Application
Filed:
November 13, 2002
Publication date:
August 14, 2003
Inventors:
Marina Yu Etinger, Lev M. Yudovich, Michael Yuzefovich, Gennady A. Nisnevich, Ben Zion Dolitzky, Boris Pertsikov, Boris Tishin, Dina Blasberger
Abstract: The present invention is concerned with novel processes for the preparation of (R)-1-(3,5-bis(trifluoromethyl)phenyl)ethan-1-ol. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
Abstract: A process for preparing 1H-imidazo[4,5-c]quinolin-4-amines is disclosed. The process involves reacting a 6H-imidazo[4,5-c]tetrazolo[1,5-a]quinoline with triphenylphosphine and hydrolyzing the product thereof.
Abstract: The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof, 1,2,3,4-tetrahydroisoquinolinyl, benz[cd]indolinyl and 5,6-dihydrophenanthridinyl compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.
Type:
Application
Filed:
December 17, 2002
Publication date:
August 14, 2003
Inventors:
N. Laxma Reddy, Michael Maillard, David Berlove, Sharad Magar, Graham J. Durant
Abstract: The present invention provides a process for preparing N-protected-4-substituted piperidines of formula (I) wherein Pg represents a suitable nitrogen protecting group; X represents a heterocycle, substituted heterocycle, substituted alkenyl or substituted aryl wherein the substituted heterocycle, substituted alkenyl or substituted aryl are substituted with from 1 to 3 suitable activating groups; and R1, R2, R3, R4, R5, R6, R7, and R8 each independently represent an alkyl, alkenyl, cycloalkyl, aryl, substituted aryl, heterocycle, or substituted heterocycle, comprising treating a compound of formula (II) wherein the substituents are defined as above, with triethylsilane and trifluoroacetic acid.
Type:
Application
Filed:
May 28, 2002
Publication date:
August 14, 2003
Inventors:
Alexander Glenn Godfrey, Steven Wayne Pedersen
Abstract: Provided is a method of hydrogenating the exocyclic double bond of a thiazolidinedione precursor in a method of making a thiazolidinedione antihyperglycemic, for example pioglitazone, including work-up steps to afford pure thiazolidinedione antihyperglycemic.
Abstract: The present invention relates to a production method of a crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]benzimidazole.n′H2O (wherein n′ is about 0 to about 0.1) or a salt thereof, which characteristically includes crystallization from an organic solvent solution or suspension in which (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]-benzimidazole.nH2O (wherein n is about 0.1 to about 1.0) or a salt thereof has been dissolved or suspended, and the like, and provides a convenient method for efficiently producing an optically active sulfoxide derivative having an extremely high enantiomer excess in high yield at an industrial large scale.
Abstract: A process for the preparation of 2-chloro-5-chloromethyl-1,3-thiazole, in which allyl isothiocyanate of formula CH2═CH—CH2-NCS is reacted at from −40° C. to +30° C., in a solvent that is inert under the reaction conditions, with from 1 to 2 mol of a chlorinating agent per mol of allyl isothiocyanate; to the reaction mixture so obtained there is added, at a reaction temperature of from 0° C. to the boiling temperature of the solvent used, from 1 to 5 mol of oxidising agent per mol of allyl isothiocyanate, and then 2-chloro-5-chloromethyl-1,3-thiazole is isolated from the reaction mixture and is optionally converted by crystallisation into high-purity 2-chloro-5-chloromethyl-1,3-thiazole.
Type:
Application
Filed:
March 27, 2003
Publication date:
August 14, 2003
Inventors:
Sylvia Krich, Christian Burger, Johann Altreiter, Birgit Zwolfer
Abstract: The present invention provides a process for preparing an imidazole derivative or its salt which comprises reacting a tetrahydrofuran or tetrahydropyran derivative with formamidine or its salt in the presence of a base.
Abstract: A class of novel indole is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.
Abstract: The invention concerns a novel method for preparing vitamin E. More particularly, it concerns a novel method for the condensation of Arimethylhydroquinone and isophytol.
Abstract: A process for producing an oxirane compound from ethylbenzene hydroperoxide and an olefin in the presence of an immobilized catalyst bed, wherein the process satisfies the following conditions (1) to (4):
Abstract: The invention relates to an improved process for obtaining pure crystalline betulin which is substantially free from betulinic acid, from an extract of birch bark.
Type:
Application
Filed:
January 31, 2003
Publication date:
August 14, 2003
Applicant:
Boehringer Ingelheim Pharma GmbH & Co. KG
Abstract: Disclosed are compounds produced by a process comprising the step of reacting an amine reactant with an epoxide reactant to form a hydrolytically stable carbon-nitrogen bond therebetween, wherein at least one of the amine or epoxide reactants comprises a terminal alkoxysiyl group. Also disclosed are curable compositions comprising the compounds of the present invention and the cured products derived therefrom.
Abstract: An efficient method is disclosed for the preparation of trifluoromethyl- and difluoromethylsilanes using magnesium metal mediated reductive tri- and difluoromethylation of chlorosilanes with tri- and difluoromethyl sulfides, sulfoxides, and sulfones. One byproduct of the process is diphenyl disulfide. Since phenyl trifluoromethyl sulfone, sulfoxide and sulfide are readily prepared from readily available trifluoromethane and diphenyl disulfide, the method can be considered “pseudo-catalytic” for the preparation of (trifluoromethyl)trimethylsilane from environmentally benign trifluoromethane.
Type:
Application
Filed:
November 27, 2002
Publication date:
August 14, 2003
Inventors:
G.K. Surya Prakash, Jinbo Hu, George A. Olah
Abstract: A process for the removal and recovery of quaternary salt (A) and base (D) from a reaction mixture is disclosed. The reaction mixture resulting from oxidative direct carbonylation contains in addition to (A) and (D), at least one hydroxyaromatic compound (B) and at least one reaction product (C) and optionally a solvent, and the process entails a) adding acid to the reaction mixture to cause conversion of (D) into a hydroxyaromatic compound (B2) b) separating the reaction mixture into b1.) that contains (C) and optionally (B) and/or (B2) and b2.) that contains (A) and optionally (B) and/or (B2), and c) reacting b1.) with a base (E) to re-form (D).
Type:
Application
Filed:
December 16, 2002
Publication date:
August 14, 2003
Inventors:
Peter Fischer, Sven Michael Hansen, Claus-Peter Reisinger
Abstract: Perfluoroalkyl-substituted amines, acids, amino acids and thioether acid compounds containing a perfluoroalkyl-iodoalkyl or perfluoroalkyl-alkene group as well as derivatives thereof, are described. They are useful as surfactants in a variety of applications where low surface tensions are required, including coating formulations for glass, wood, metal, cement, paper, textiles, as foam control agents in polyurethane foams and especially in aqueous fire-fighting formulations.
Type:
Application
Filed:
July 24, 2002
Publication date:
August 14, 2003
Inventors:
Marlon Haniff, Ted Deisenroth, John Jennings, Karl Friedrich Mueller
Abstract: The present invention discloses aminothiol compounds and acylated derivatives thereof, which respectively have general formula I and formula II wherein R1-R6 are substitutable ligands. Such compounds can perform as superior catalysts in asymmetric addition reactions of organic zinc and aldehyde. According to the present invention, the compounds is needed only less than 0.02% of main reactants to obtain enantioselectivity higher than 99% enantiomeric excess, whereby the asymmetric reactions can become very economic.
Abstract: Unexpected corrosion of downstream sections of a dialkyl carbonate manufacturing apparatus has been traced to alkyl chloroformate impurities, which slowly decompose to yield hydrochloric acid. An improved process and apparatus for dialkyl carbonate synthesis reduce corrosion by physically removing or chemically decomposing the alkyl chloroformate impurities within the corrosion-resistant upstream sections of the apparatus. The alkyl chloroformate may be decomposed by passing it through a passageway at a temperature of about 30° C. to about 130° C. for a time of about 0.5 hour to about 10 hours. The passageway may include one or more holding vessels or a tubular section that promotes plug flow.
Type:
Application
Filed:
August 23, 2002
Publication date:
August 14, 2003
Inventors:
Eugene Pauling Boden, Ganesh Kailasam, Larry Neil Lewis, Alberto Nisoli, John Yaw Ofori, Angel Sanchez Gonzalez, Ignacio Vic Fernandez
Abstract: A process is described for the preparation of R or S aminocarnitine, R or S phosphonium aminocarnitine and R and S 3,4 diaminobutanoic acid, and their derivatives with the following formula: 1
Abstract: A process is described for the preparation of R or S aminocarnitine, R or S phosphonium aminocarnitine and R and S 3,4 diaminobutanoic acid, and their derivatives with the following formula: 1
Type:
Application
Filed:
February 25, 2003
Publication date:
August 14, 2003
Inventors:
Fabio Giannessi, Natalina Dell'uomo, Maria Ornella Tinti, Francesco De Angelis
Abstract: A method of improving the stability of a quaternary ammonium salt and a method of efficiently preparing the quaternary ammonium salt having improved stability.
Abstract: Compounds of the formula R2.[(AO)n.R3]m, where R2 is a residue of a group having at least m active hydrogen atoms derived from hydroxyl and/or amino and/or amido groups, AO is alkyleneoxy, n is 2 to 200; R3 includes residue(s) of alkenyl succinic acids and optionally other acids, and m is 2 to 10, but when m is 2 there are other restrictions in the definitions, are disclosed as useful thickeners and/or dispersants in aqueous systems. The use of such materials as thickeners is also disclosed.
Type:
Application
Filed:
December 10, 2002
Publication date:
August 14, 2003
Applicant:
Imperial Chemical Industries PLC
Inventors:
Neil Michael Carpenter, Steven John Anderson, Richard Robert Tenore, Peter Glynn Hibbert
Abstract: The present invention is to provide manufacturing intermediates which can be led to useful &agr;-ketoamide compounds having protease-inhibiting activity extremely economically and stereoselectively, and to provide epoxycarboxamide compounds, azide compounds and amino alcohol compounds represented by the following formulae: 1
Abstract: The present invention is directed to labeled compounds, [2H1, 13C], [2H2, 13C] and [2H3, 13C]methyl aryl sulfides wherein the 13C methyl group attached to the sulfur of the sulfide includes exactly one, two or three deuterium atoms and the aryl group is selected from the group consisting of 1-naphthyl, substituted 1-naphthyl, 2-naphthyl, substituted 2-naphthyl, and phenyl groups with the structure 1
Type:
Application
Filed:
January 14, 2003
Publication date:
August 14, 2003
Inventors:
Rodolfo A. Martinez, Marc A. Alvarez, Louis A. Silks, Clifford J. Unkefer
Abstract: The present invention relates to a novel process for the preparation of 1-(2,6,6-trimethyl-2-cyclohexene-1-yl)-2-but-2-ene-1-one commonly known as &agr;-Damascone, by acylation of unsaturated cyclic hydrocarbon 2,6,6-trimethyl-1-cyclohexene followed by work up and its purification by vacuum distillation.