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WO/2001/038292A2 |
The invention relates to a method for producing optically active amines. The invention also relates to a method for producing racemic amines, which can be racemically split using optically active carboxylic acids or enzymes. The inventio...
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WO/2001/034563A1 |
A method of preparing a substantially pure enantiomer of an acylanilide such as Casodex$m(3) (bicalutamide) and/or its derivatives includes resolving an intermediate compound having the structure of Formula (I), wherein: R?1¿ is alkyl o...
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WO/2001/034160A1 |
This invention relates to the compound of Formula (I) or a pharmaceutical acceptable salt, hydrate or solvate thereof, which is an inhibitor of cystein proteases, particularly cathepsin K, and is useful in the treatment of diseases in wh...
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WO/2001/034159A1 |
This invention relates to the compound of Formula (I) or a pharmaceutically acceptable salt, hydrate or solvate thereof, which is an inhibitor of cysteine proteases, particularly cathepsin K, and is useful in the treatment of diseases in...
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WO/2001/032691A1 |
Compounds of formula (I) and pharmaceutically acceptable salts and esters thereof are active as inhibitors of hepatitis C virus NS3 protease. Consequently they are potentially useful in the treatment and prevention of hepatitis C virus i...
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WO/2001/023088A1 |
The invention relates to a catalyst for asymmetrical transfer hydrogenation on the basis of a transition metal compound and a nitrogen-containing enantiomerically enriched ligand. The invention also relates to various processes for the p...
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WO/2001/019761A2 |
One aspect of the present invention relates to methods for the transition-metal-catalyzed asymmetric 1,4-addition of a nucleophile, e.g., hydride, to cyclic and acyclic enoates and enones. In certain embodiments of the methods of the pre...
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WO/2001/019782A1 |
The invention relates to cyclopropane carboxylic acid amides of general formula (I), wherein the substituents have the following meaning: R?1¿ represents substituted or unsubstituted C¿1?-C¿6? alkyl or C¿2?-C¿6? alkenyl groups, R?2Â...
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WO/2001/016090A1 |
The present invention provides a compound having the formula (I) or (II): wherein R?1¿ is selected from halogen and organic moieties; R?2¿ and R?3¿ are independently selected from hydrogen and organic moieties having a mass greater th...
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WO/2001/014288A1 |
An optical resolver comprising an optically active substance obtained from tris(2,3-epoxypropyl) isocyanurate. The substance is an optically active tris(epoxyalkyl) isocyanurate, a derivative thereof, or an optically active derivative of...
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WO/2001/014327A1 |
The invention relates to 1,3-disubstituted-3-oxopropane-1-sulphonic acids and sulphonates and pure enantiomers thereof. The invention further relates to the use of enantiomerically enriched 1,3-disubstituted-3-oxopropane-1-sulphonic acid...
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WO/2001/001569A2 |
The invention relates to a process for preparing (-)-(1S,4R) N protected 4-amino-2-cylcopentene-1-carboxylate esters represented by formula (I) wherein R¿1? and R¿2? are as described within the specification.
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WO/2000/076991A1 |
A process is provided for preparing chiral cyclopropane carboxylic acids, preferably of structure (I) which are intermediates used in preparing acyl guanidine sodium/proton exchange (NHE) inhibitors.
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WO/2000/063188A1 |
The invention relates to a novel (-)- enantiomer of the 2- [2-(1- chlorocyclopropyl) -3-(2- chlorophenyl) -2-hydroxypropyl] -2,4- dihydro- [1,2,4]- triazole-3- thione, of formula (I), a method for producing this novel active ingredient a...
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WO/2000/063255A1 |
A process for producing a chitin derivative having the high ability to asymmetrically identify; and a separatory agent for optical isomers which comprises the chitin derivative as an agent for asymmetric identification. The process for p...
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WO/2000/063175A2 |
The invention relates to a novel process for the preparation of certain pharmaceutically active pyridyl compounds.
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WO/2000/061540A1 |
The present invention provides processes for the preparation of 3-aryloxy-3-arylpropylamines and intermediates thereof using an nucleophilic aromatic displacement in 1,3-dimethyl-2-imidazolidinone or N-methylpyrrolidinone.
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WO/2000/056693A1 |
The present invention relates to a method of industrial-scale purification of lactic acid, the method comprising the steps of: (a) reduced-pressure distillation of a concentrated lactic acid solution having a total acid content of at lea...
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WO/2000/053283A1 |
A process for isolating enantiomer components from a mixture of enantiomers through co-crystallization is disclosed, comprising the steps of (a) forming a solution comprising the mixture of enantiomers (R) and (S) and co-crystallization ...
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WO/2000/050378A2 |
The present invention relates to a method of preparing a 1-nitro-3-substituted-3-amino-2-propanol diastereomer represented by Structural Formula (I): In Structural Formula (I), R is an amine protecting group, and R?1¿ is an amino acid s...
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WO/2000/048987A1 |
The invention relates to novel substituted 3-phenoxy or 3-phenylalkyloxy-2-phenyl-propylamines of general formula (1), to methods for producing them and to their use as medicaments.
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WO/2000/047546A1 |
The invention relates to a method for the racemization of optically active amines by reacting the optically active amine in the presence of hydrogen and of a hydrogenation or dehydrogenation catalyst at an elevated temperature. According...
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WO/2000/047545A1 |
The invention relates to a method for producing racemic amines of formula (I), in which R?1¿ and R?2¿ are not the same and R?1¿, R?2¿, R?3¿ are alkyl-, cycloalkyl-, arylalkyl-, aryl-, heteroaryl rests and heterocyclic rests and R?3Â...
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WO/2000/040539A1 |
Novel 4-Biarylbutyric and 5-Biarylpentanoic Acid Derivatives, use of substituted 4-Biarylbutyric and 5-Biarylpentanoic Acid Derivatives as Matrix Metalloprotease Inhibitors for the Treatment of Respiratory Diseases, pharmaceutical compos...
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WO/2000/032638A1 |
The invention concerns chiral esters of polysaccharides, preferably of cellulose, amylose, $g(b)-cyclodextrin or amylopectin, obtained by reacting, in a basic medium, polysaccharides (polyhydroxy compounds) with racemic or enriched acid ...
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WO/2000/032556A1 |
Methods of preparing, and compositions comprising, derivatives of (-)-venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depr...
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WO/2000/032555A1 |
Methods of preparing and compositions comprising, derivatives of (+)-venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depre...
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WO/2000/032554A1 |
A process for preparing a substantially single enantiomer of tramadol, or a pharmaceutically-acceptable salt thereof, proceeds by means of a classical salt resolution using a substantially single enantiomer of $i(o,o)-di-$i(p)-toluoyltar...
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WO/2000/027778A1 |
The invention concerns a resolution method for a racemic mixture of aldehyde of formula (I) wherein: R¿1?, R¿2?, R¿3?, R¿4?, R¿5?, R¿6? Z and n are as defined in Claim (1). The aldehydes of formula I are useful in their enantiomeri...
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WO/2000/025885A1 |
The invention concerns a method for separating at least a constituent of a mixture in a set of looping chromatographic columns, the loop comprising at least a point for injecting a load, a point for drawing off the raffinate, a point for...
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WO/2000/026170A1 |
The invention relates to racemate splitting of 2-hydroxypropionic acids by reacting racemic acid with an optically active base and subsequently separating a diastereomeric salt from the acid and the base. The invention is characterized i...
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WO/2000/024711A1 |
This invention encompasses a novel process for synthesizing compounds represented by formula (A). These compounds are intermediates useful in the preparation of certain agents that are selective COX-2 inhibitors.
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WO/2000/023414A2 |
A process for the preparation of optically active cyclohexylglycolate esters is described. The process utilizes carboxylic acid activation to couple $i((R))- or $i((S))-cyclohexylphenylglycolic acid (CHPGA) with 4-$i(N,N)-diethylamino bu...
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WO/2000/018724A1 |
The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, ...
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WO/2000/018721A1 |
The invention relates to substituted polycyclic aryl and heteroaryl $i(tertiary)-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions an...
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WO/2000/017153A1 |
According to the invention, (+/-)-$g(a)-(difluoromethyl)ornithine is cleaved into its isomers by means of (-)-O, O'-di-p -toluyol -L-tartaric acid. (+/-) -$g(a)- (difluoromethyl)ornithine -monohydroch loride monohydrate and notably its (...
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WO/2000/017133A2 |
The invention concerns LTA¿4? hydrolase inhibiting compounds of formula (I). It also concerns their therapeutic, in particular anti-inflammatory, applications.
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WO/2000/010968A2 |
The present invention relates to novel aryl sulphonamide amino acid esters and analogues, methods for the production and use thereof in the prophylaxis and treatment of neurodegenerative diseases, especially in the treatment of apoplexia...
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WO/2000/009463A1 |
The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile, selected from the group consisting of water, alcohols, carboxylic acids, and thiols, an...
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WO/2000/009493A1 |
A short practical commercial process for the efficient enantioselective synthesis of the non-steroidal antiestrogen of formula (I) or (XIV) or a pharmaceutically acceptable salt thereof.
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WO/2000/008012A1 |
The invention relates to enantiomer-free crystalline (R) or (S) lipoic acid, where the reflection line at 2 $g(U) = 23° is the most intensive one in the 13° to 30° range in the 2 $g(U) diffractogram.
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WO/2000/005196A1 |
The present invention relates to $g(a)-amino acid phenyl ester derivatives having general formula (I) wherein R¿1? is (C¿1-3?)alkyloxy; R¿2? is (C¿1-3?)alkyl, (C¿1-3?)alkyloxy or (C¿2-3?)alkenyl; R¿3? is hydrogen, (C¿1-3?)alkyl, ...
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WO/2000/002834A1 |
A composition and method for the catalytic conversion of a racemic mixture of dienes to a cyclic olefin by a ring-closing metathesis (RCM) reaction are disclosed. The composition, a transition metal complex with an M=C reaction site, con...
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WO/2000/001689A1 |
A process for producing compounds of formula (1.0) is disclosed. The compound of formula (1.0) is produced by: (1) separating the atropisomers of (2.0) to obtain the atropisomers (2.0A) and (2.0B); (2) heating the atropisomer of formula ...
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WO/2000/001642A1 |
A new polymeric material, a process for forming the material and method of using the material to separate enantiomers of chiral compounds, particularly amino acids and pharmaceuticals are disclosed. A polymeric material can be formed fro...
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WO/2000/000464A1 |
The present invention describes new chiral stationary phases and optically active compounds therein contained. The optically active compounds contained in the stationary phases are represented by the formula of structure (I), containing ...
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WO/1999/058532A1 |
The invention relates to a method for producing (S,S)-8-benzyl-2,8-diazabicyclo[4.3.0]nonane.
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WO/1999/056699A2 |
The present invention relates to a method and catalysts for the stereoselective addition of a nucleophile to a reactive $g(p)-bond of a substrate. The chiral, non-racemic catalysts of the present invention constitute the first examples o...
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WO/1999/057089A1 |
A process for the production of enantiomerically pure or optically enriched sertraline-tetralone from a mixture containing two enantiomers using continuous chromatography. The chromatography comprises a liquid mobile phase comprising at ...
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WO/1999/052886A1 |
A method for kinetically resolving a stereoisomer mixture of compounds using asymmetric epoxidation is provided. Compounds contain an olefin moiety providing one stereoisomer to be epoxidized at a higher rate than the other stereoisomer ...
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