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WO/2001/055097A1 |
This invention relates to an improved synthesis of 5-(N-[(S)-N-{N,N-bis(2-chloroethyl)amino}phenoxycarbonyl)-$g
(g)-glutamyl]amino)isophthalic acid (also named ZD9063P), a prodrug used in Antibody Directed Enzyme Prodrug Therapy (ADEPT),...
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WO/2001/055060A2 |
The invention relates to chiral ionic liquids of the general formula [A]¿n??+¿[Y]?n-¿, wherein n = 1 or 2, the anion [Y]?n-¿ is the anion of an organic or inorganic protonic acid and the cation [A]?+¿ is an optically active organic ...
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WO/2001/055090A1 |
This invention provides a method of making (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid (pregabalin) or a salt thereof via an asymmetric hydrogenation synthesis. Pregabalin is useful for the treatment and prevention of seizure disorders...
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WO/2001/055175A2 |
The present invention relates to a process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalanin
amides of formula (I), in which the anions X are physiologically acceptable anions, and their analogs, which a...
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WO/2001/053241A1 |
A method is provided for catalytically transforming a functional group within a first reactant by reaction with a second reactant in the presence of a nonmetallic, organic catalyst composition composed of a heteroatom-containing activato...
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WO/2001/053269A1 |
Acid addition salts of imidazolidinones are provided as catalysts for transforming a functional group within a first reactant by reaction with a second reactant. Exemplary first reactants are $g(a),$g(b)-unsaturated carbonyl compounds su...
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WO/2001/049649A1 |
The invention relates to a process for the enantioselective preparation of tolterodine and analogues and salts thereof comprising the steps of: a) enantioselectively reducing the carbonyl function in a compound of formula (II), wherein R...
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WO/2001/049650A1 |
The invention concerns novel esters derived from (RR,SS)-2-hydroxybenzoate of 3-(2-dimethylaminomethyl-1-hydroxycyclocyclohexyl)phenyl, Tramadol analogs, method for obtaining said esters and to the utilization of said compounds for the p...
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WO/2001/047940A1 |
The invention concerns: (i) [4-(4-cyanobenzyl)phenyl]glycopyranosides of formula (I) wherein: the glycopyranosyl group R represents a $g(b)-D arabinopyranosyl, $g(b)-D-lyxopyranosyl, $g(b)-D-ribopyranosyl, $g(b)-D-mannopyranosyl, $g(b)-L...
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WO/2001/046131A1 |
The invention provides a method for making 24(S)-hydroxyvitamin D¿2? which is a stereospecific synthesis.
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WO/2001/045484A2 |
The present invention relates to an improved process for preparing simvastatin and more particularly, the improved process for preparing simvastatin expressed by formula 1 with high yield and high purity by performing the following seque...
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WO/2001/046098A1 |
A novel bisphosphine compound represented by formula (1): (wherein t-C¿8?H¿17? represents 1,1,3,3-tetramethylbutyl), which has asymmetric centers at the phosphorus atoms and is useful as the ligand of asymmetric catalysts for asymmetri...
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WO/2001/042173A2 |
Process for the preparation of a diastereomerically enriched phenylglycine amide derivative in which an enantiomerically enriched phenylglycine amide is converted into the corresponding Schiff base with the aid of compound R¿2?-C(O)-R¿...
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WO/2001/042190A1 |
The instant invention is a route to stereospecific 3-substituted 5-membered ring isomers of Formula (A). The final products are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegene...
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WO/2001/040153A1 |
The present invention provides a process for preparing optically active $g(a)-hydroxy acids and derivatives thereof by subjecting the alkylated 1,3-dioxolanones of formula (IV) wherein R¿1? and R¿2? are the same or different and are ea...
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WO/2001/039884A2 |
A chiral catalyst comprising a 3,4-disubstituted pyridine, or a salt, N functionalised derivative, dimer or oligomer thereof, wherein the 3-substituent is substantially hindered from rotation about the bond (sp?2¿-sp?2¿ biaryl axis) li...
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WO/2001/036359A1 |
A novel optically active binaphthol derivative with which a higher reaction yield and a higher optical yield (selectivity) can be attained in asymmetric synthesis and which is useful as an asymmetric catalyst, etc.; an asymmetric catalys...
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WO/2001/034612A2 |
Chiral ligands and transition metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The chiral ligands include (R,S,S,R)-DIOP*. The ruthenium complex reduces enamide to the corresponding amine with up...
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WO/2001/028990A2 |
A method of synthesizing pure enantiomers of acylanalides such as Casodex$m(3) (bicalutamide) and its derivatives includes contacting a compound having a ring structure that, when opened, provides a substituent having the structure of Fo...
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WO/2001/025183A1 |
Optically active 1-perfluoroalkylated alcohols can be prepared by subjecting a 1-perfluoroalkylated unsaturated ester to asymmetric hydrogenation with an optically active ruthenium complex catalyst to thereby obtain a carboxylic ester of...
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WO/2001/025215A2 |
The invention relates to a method for selectively dissociating cyclic carboxylic acid anhydrides of the formula (I), wherein R represents benzyl, alkyl having 1 to 6 carbon atoms or aryl, to give the corresponding semi-esters. According ...
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WO/2001/025188A1 |
The present invention relates to novel carbamates, ureas, and pharmaceutically acceptable salts thereof; compositions comprising the carbamate, urea, or a pharmaceutically acceptable salt thereof; and methods for treating or preventing c...
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WO/2001/025486A1 |
The present invention relates to methods of screening for compounds that bind RNA molecules. In particular, the methods of the invention comprise screening a library of test compounds, each of which is attached to a solid support, with a...
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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/2001/021559A1 |
The invention relates to a method for hydrogenating organic compounds containing at least one C-C double bond. According to the invention, the hydrogenation of the compound to be hydrogenated is carried out using a hydrogenation catalyst...
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WO/2001/021625A1 |
Chiral ligands and transition metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The chiral ligands include chiral C1-C6 TunaPhos ligands. The ruthenium TunaPhos complex reduces ketones to the corr...
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WO/2001/019833A1 |
The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D¿4? antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D¿4?...
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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/2001/019787A1 |
An aldehyde compound is reacted with an amine compound and hydrogen cyanide in the presence of a chiral zirconium catalyst obtained by mixing a zirconium alkoxide with an optically active binaphthol compound.
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WO/2001/017952A1 |
3,4-Disubstituted-1-cyclopentene compounds, in substantially enantiopure form, have the relative stereochemistry according to formula (1A) or (1B) including the opposite enantiomers thereof, wherein R?1¿ is either COOX, wherein X is alk...
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WO/2001/018012A1 |
A phosphino- or arsenoamidine of Formula (1) M is Phosphorus or Arsenic (P, As); X, Y, and Z can be independently selected from hydrogen, alkyl, aryl (pendant or fused), halogen, alkoxy (C1-C10), cyano, nitro, amino, alkylamino, dialkyla...
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WO/2001/014299A1 |
Chiral ligands and transition metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The chiral ligands include phospholanes, P, N ligands, N, N ligands, biphenols, and chelating phosphines. The ferroc...
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WO/2001/014287A1 |
A novel method for synthesizing absolute asymmetry through the irradiation with circular polarization light which comprises providing a photochemically reversible reaction system wherein the starting material is a mixture of enantiomers ...
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WO/2001/012583A1 |
This invention relates to an improved industrial scale production method for adrenaline or an addition salt thereof employing an asymmetric hydrogenation reaction as the key reaction step and a special sequence of subsequent steps, where...
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WO/2001/012574A1 |
A catalytic transfer hydrogenation process is provided. The process can be employed to transfer hydrogenate N-substituted imines and iminium salts, which are preferably prochiral. The catalyst employed in the process is preferably a meta...
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WO/2001/010822A1 |
This invention relates to a method for preparing certain acids of formula (I) via a chloroepoxy ester, which are useful as phosphodiesterase 4 inhibitors.
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WO/2001/010819A1 |
New carnitine derivatives of general formula (I) are described in racemic and/or optically active form, as well as the process for their preparation and their use as pharmaceutical anti-angina active ingredients for the treatment of isch...
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WO/2001/010814A1 |
A process for obtaining nitroxyalkylesters of the 2-(S)-(6-methoxy-2-naphthyl)-propanoic acid having an enantiomeric excess higher than or equal to 95 %, preferably higher than or equal to 98 %, characterized in that an halide of the 2-(...
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WO/2001/009120A1 |
Amine and amide derivatives of formula (A) which are ligands for the neuropeptide Y Y5 (NPY5) receptor, methods of preparation and pharmaceutical compositions containing amines and amides of formula (A) as the active ingredient are descr...
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WO/2001/009079A1 |
The invention relates to compounds of formula (I) provided in the form of racemates and enantiomers, preferably compounds of formula (Ia), wherein R¿4? represents C¿1?-C¿6? alkyl; Z represents chlorine, bromine or iodine, and; X repre...
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WO/2001/009147A1 |
The invention relates to novel chiral phosphorus ligands that can be easily produced on the basis of chinoline derivatives which represent inexpensive starting materials. The novel compounds have the general formula (I), wherein R?1¿, R...
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WO/2001/009077A1 |
The invention concerns the use of an optically active N-substituted norephedrine chiral derivative as ligand in an enantioselective reduction of unsaturated compounds bearing functional groups by a hydrogen transfer process. The inventio...
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WO/2001/009083A1 |
Compounds of formula (I), wherein; R¿5? represents C¿1?-C¿6? alkyl, C¿1?-C¿6? hydroxyalkyl, C¿1?-C¿6? alkoxy-C¿1?-C¿6? alkyl, C¿1?-C¿6? alkanoyloxy-C¿1?-C¿6? alkyl, C¿1?-C¿6? aminoalkyl, C¿1?-C¿6? alkylamino-C¿1?-C¿6? ...
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WO/2001/009080A1 |
The invention relates to a process for the cis-selective preparation of cyclic amines of the sertralin type by reductive alkylation of cyclic imines or their precursors and catalytic hydrogenation in the presence of copper-containing cat...
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WO/2001/007386A2 |
Disclosed are electronically perturbed asymmetric aromatic ligands. In one aspect, the ligands are polyfluorinated. The ligands may be nucleophilically substituted. The ligands have many useful applications including catalytic applicatio...
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WO/2001/005741A1 |
The invention relates to the production of amines, including chiral amines, by reacting aldehydes or ketones with ammonia or primary or secondary amines in the presence of hydrogen and in the presence of homogeneous metal catalysts, unde...
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WO/2001/005776A1 |
The invention concerns compounds of formula (I) wherein: R¿1?, R¿2?, R¿3?, R¿4?, R¿5?, R¿6? and R¿7? are as defined in Claim 1. Said compounds have an affinity for CRF receptors.
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WO/2001/004131A1 |
Chiral or nonchiral ditertiary diphosphines having solubilizing substituents, for example -NH-C(O)-NH-C(CH¿2?-O-CH¿2?CH¿2?CO¿2?H)¿3?, in the diphosphine framework are excellent ligands for d¿8? metal complexes which are soluble in ...
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WO/2001/002326A1 |
The present invention is concerned with a process for the preparation of (R)-1-(3,5-bis(trifluoromethyl)phenyl)ethanol by asymmetric transfer hydrogenation of 3,5-bis(trifluoromethyl)acetophenone using a rhodium of ruthenium catalyst and...
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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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