Abstract: A method for purification of the antibiotic mupirocin (pseudomonic acid A) which comprises: a) Causing or allowing precipitation of mupirocin from an aqueous solution thereof; b) Recovering the precipitate; c) Dissolving the recovered precipitate in an organic solvent.
Type:
Grant
Filed:
February 21, 2006
Date of Patent:
November 17, 2009
Assignee:
Axellia Pharmaceuticals ApS
Inventors:
Marc Antonius Theodorus Bisschops, Tiemen Geert Pieter Reijns, Anita Mathiesen, Lene Aassveen
Abstract: Is disclosed a cycloaliphatic polyepoxy compound represented by following Formula (1): wherein Y represents a linkage group or a single bond; and HAs each represent hydrogen atom at the junction between cyclohexane ring and oxirane ring, and the cyclohexane rings may each further have one or more substituents in addition to the groups shown in the formula. The cycloaliphatic polyepoxy compound contains stereoisomers in such proportions as to have a ratio A/B of 1.8 or more, wherein “A” and “B” are integrated intensities of signals of protons at the junction between cyclohexane ring and oxirane ring as determined by 1H-NMR spectroscopy of the compound, in which “A” represents the integrated intensity of a signal observed at a lower magnetic field, and “B” represents the integrated intensity of a signal observed at a higher magnetic field.
Abstract: The present invention is directed to a process for preparing ?-amino-?-hydroxycarboxamides. The process works with epoxycarboxamides of the formula 2 which are reacted with ammonia or other amines.
Abstract: The present disclosure provides the asymmetric cyanine fluorescent dyes of formula I in which X, n, R1, R2, R3, R4, R5 and Y? are as defined in the specification. The present disclosure also provides conjugates of the fluorescent dyes, methods for preparation thereof, compositions comprising the fluorescent dyes, and methods for staining biological samples using the fluorescent dyes and compositions thereof.
Abstract: 3-cyanonaphthalene-1-carboxylic acid perhydroxyalkylmethyl-piperazine compounds of formula I which are antagonistic to tachykinin receptors, pharmaceutical compositions containing such compounds, methods of using such compounds for the treatment and/or inhibition of various diseases and disorders, processes for preparing such piperazine compounds, and intermediate products of these processes.
Type:
Grant
Filed:
November 30, 2006
Date of Patent:
September 22, 2009
Assignee:
Solvay Pharmaceuticals GmbH
Inventors:
Jochen Antel, Daniel Jasserand, Uwe Schoen, Michael Firnges, Holger Sann, Reinhard Brueckner, Dania Reiche
Abstract: The present invention relates to a process for preparing optionally substituted aromatic or heteroaromatic nitriles starting from haloaromatics. These are reacted in a copper-catalysed reaction with potassium hexacyanoferrate(II) or potassium hexacyanoferrate(III) in the presence of heteroaromatic amines.
Type:
Grant
Filed:
August 27, 2007
Date of Patent:
September 22, 2009
Assignee:
SaltigoGmbH
Inventors:
Nikolaus Müller, Wolfgang Mägerlein, Matthias Beller, Thomas Schareina, Alexander Zapf
Abstract: The present invention provides a chiral ligand, represented by a formula or its enantiomer: X and X? can be independently O, NH, NR, NCOR or S; each of Z1-Z7 and Z1?-Z7? can be independently H, alkyl, aryl, substituted alkyl, substituted aryl, alkoxyl, aryloxyl, nitro, amide, aryloxide, halide, hydroxyl, carboxylate, heteroaryl, or a cyclic alkene, fused aryl, or cyclic ether group formed from any two adjacent Z groups or any two adjacent Z? groups; Y and Y? can be independently OH, OR, NH2, NHR, NR2, SH, PR2, OPR2, NHPR2, OP(OR)2, COOH, COOR, CONHR, or a linking group formed from Y and Y? groups together. Processes of preparing these ligands, catalysts that employ them and methods of using the catalysts are also provided.
Abstract: There is disclosed a process for producing an olefin oxide, which is characterized by reacting an olefin with oxygen in the presence of a silver catalyst and 0.2 mole or more of water per mol of the olefin.
Abstract: The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet): 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm?1.
Abstract: The invention relates to a method of separating and isolating an acylated derivative of 4-[(S)-4-dimethylamino-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile by reaction of a mixture of the 4-[(S)-4-dimethylamino-1-(4-fluorophenyl)-1-hydroxy-butyl]-3-hydroxymethylbenzonitrile and an acylated derivative thereof with a compound which form a derivative of the 4-[(S)-4-dimethylamino-1-(4-fluorophenyl)-1-hydroxy-butyl]-3-hydroxymethylbenzonitrile containing a carboxylic acid group. The acylated derivative containing a carboxylic acid group precipitates once it is formed and may easily be separated from the reaction mixture.
Abstract: An ester compound represented by the formula (I): has excellent pest controlling activity and is useful as an active ingredient for a pest controlling agent.
Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4,R5, R6, R7, R8a, R8b, W, a, b, c and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Accordingly, such compounds are expected to be useful as therapeutic agents for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
Type:
Grant
Filed:
August 15, 2005
Date of Patent:
August 4, 2009
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, Trevor Mischki, Adam Hughes, Yu-Hua Ji
Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).
Type:
Grant
Filed:
December 12, 2003
Date of Patent:
August 4, 2009
Assignee:
SmithKline Beecham Corporation
Inventors:
Jennifer Poole Peckham, Christopher Joseph Aquino, Wieslaw Mieczyslaw Kazmierski
Abstract: This invention provides a process for producing an epoxytriazole derivative represented by formula (2): (wherein R and Ar are defined below), which comprises a step including a reaction of an epoxy derivative represented by formula (1?): (wherein R represents a hydrogen atom or C1-12 alkyl group and Ar represents an aromatic group optionally substituted by a halogen atom(s) or trifluoromethyl group(s), and X? represents a hydroxy group or leaving group), with 1,2,4-triazole in the presence of a base and water.
Abstract: A process is provided for preparing a carrier which process comprises incorporating into the carrier at any stage of the carrier preparation a strength-enhancing additive. Also provided is the resultant carrier having incorporated therein a strength-enhancing additive and a catalyst comprising the carrier. Also provided is a process for the epoxidation of an olefin employing the catalyst. Also provided is a method of using the olefin oxide so produced for making a 1,2-diol, a 1,2-diol ether or an alkanolamine.
Type:
Grant
Filed:
August 30, 2005
Date of Patent:
July 14, 2009
Assignee:
Shell Oil Company
Inventors:
Randall Clayton Yeates, John Robert Lockemeyer, Marek Matusz
Abstract: A catalyst that enables to produce ethylene oxide in a high selectivity and a method for the production of ethylene oxide using the catalyst are provided. In the catalyst for the production of ethylene oxide, wherein the catalyst component is supported by a carrier, a carrier containing ?-alumina as the main component which has at least two peaks in the range of pore diameter of 0.01-100 ?m and at least one peak of the above peaks is present in the range of pore diameter of 0.01-1.0 ?m in the pore distribution measured by mercury porosimetry is adopted as said carrier.
Abstract: Processes for preparing hexafluoroisobutene epoxide (HFIBO) from CH2?C(CF3)2 (HFIB) are provided. The processes can be carried out in substantial absence of oxidation catalysts.
Abstract: To provide an efficient method for recovering and producing lactide having high optical purity by depolymerizing a polylactic acid or derivative thereof in order to carry out chemical recycling of the polylactic acid or derivative thereof or of a resin composition comprising same, wherein a mixture of a polylactic acid or derivative thereof and aluminum hydroxide is thermally decomposed at a temperature in a range from at least the melting temperature of the polylactic acid or derivative thereof to no greater than 320° C., thus recovering lactide.
Type:
Grant
Filed:
April 25, 2005
Date of Patent:
July 7, 2009
Assignees:
Kyushu Institute of Technology, Kitakyushu Foundation for the Advancement of Industry, Science and Technology
Abstract: A process for initiating a highly selective ethylene oxide catalyst is provided in which the highly selective ethylene oxide catalyst is operated first as a ‘standard’ Ag-based catalyst (e.g., a catalyst that contains only silver and alkali metal, especially cesium). Moreover, the inventive initiation procedure is more efficient when the concentration of carbon dioxide in the feed is higher than 6 vol. %, and even more efficient when the concentration of carbon dioxide in the feed is higher than 10 vol. %, of the feed mixture during the initiation period.
Type:
Grant
Filed:
September 26, 2007
Date of Patent:
June 30, 2009
Assignee:
SD Lizenzverwertungsgesellschaft mbH & Co. KG
Inventors:
Nabil Rizkalla, Barry Jay Billig, Norma B. Castagnola
Abstract: The invention relates to a process for the preparation of duloxetine (1a), comprising the reaction between 1-fluoronaphthalene and 3-N,N-dimethylamino-1-(2-thienyl)-propan-1-ol in the presence of 1,3-dimethyl-2-oxo-hexahydropyrimidine (DMPU) as the solvent; a method for the identification of duloxetine enantiomers and for the determination of its optical purity is also disclosed.
Type:
Grant
Filed:
October 13, 2006
Date of Patent:
June 30, 2009
Assignee:
Solmag S.p.A.
Inventors:
Samuele Frigoli, Claudio Fuganti, Roberta Pizzocaro