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WO/2001/000545A1 |
Process for the heterogeneous and enantioselective hydrogenation of prochiral organic $g(a)-keto compounds with platinum as the catalyst in the presence of a soluble or immobilised chiral aromatic nitrogen base with at least one basic ni...
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WO/2000/076942A1 |
The invention concerns mainly novel diamine derivatives or the like of general formula (I) particularly useful, in their optically active form, as ligand of metal complexes. The invention also concerns the complexes, the method for prepa...
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WO/2000/075104A1 |
The invention concerns a novel method for preparing optically active $g(a)-aminonitriles of formula (I) by enantioselective hydrocyanation using a hydrocyanation agent, in the presence of a chiral or chirality inducing metal complex acti...
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WO/2000/073274A2 |
The invention relates to substituted phenylcyclohexane carboxylic acid amides of the formula (I), to methods for producing said amides and to their use in medicaments, especially for treating cardiovascular diseases.
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WO/2000/071541A1 |
The present invention relates to optically active quinoline carboxylic acid derivatives, pharmaceutically acceptable salts thereof, solvates thereof, and a process for preparation thereof. More particularly, the present invention relates...
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WO/2000/071503A1 |
Novel 4-cyano-3-hydroxybutanoyl hydrazides (10), particularly R-chiral intermediates are described. The intermediates are useful in preparing (R)-3-hydroxy-4-trimethylaminobutyric acid (L-carnitine) and R-4-amino-3-hydroxybutyric acid (G...
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WO/2000/069808A1 |
A process for the preparation of L-carnitine inner salt comprising the reduction, with a suitable reducing agent, of a compound of formula (I): where X¿1? and X¿2?, which may be the same or different, are hydroxy, C¿1?-C¿4? alkoxy, p...
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WO/2000/069777A1 |
In a method of performing a chemical reaction using a Lewis acid, after the reaction is complete, the Lewis acid is extracted from the reaction product in the form of an aqueous solution, followed by drying of the aqueous solution of the...
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WO/2000/068181A2 |
The invention relates to a process for preparing (1R,2S,4R) -(-)-2-[(2'- {N,N-dimethylamino} -ethoxy)] -2-[phenyl] -1,7,7-tri- [methyl] -bicyclo [2.2.1] heptane and pharmaceutically acceptable acid addition salts thereof with higher yiel...
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WO/2000/068183A2 |
The invention relates to high purity (1R,2S,4R)-(-)-2- [(2'-{N,N- dimethylamino} -ethoxy)] -2-[phenyl] -1,7,7-tri-[methyl] -bicyclo[2.2.1] heptane and pharmaceutically acceptable acid addition salts thereof containing not more than 0.2 %...
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WO/2000/066519A1 |
The invention concerns a method for stereospecific preparation of 4-hydroxyalk-1-ene compounds of configuration $i((R)) or $i((S)) of general formula (I) wherein: X represents an oxygen atom, and in such case R is selected among an alkyl...
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WO/2000/066545A1 |
The invention concerns compounds of general formula (I) wherein: R¿1? represents either a hydrogen atom, or an amino group, or a C¿1?-C¿4? alkyl group, or a C¿1?-C¿6? alkoxycarbonyl group, or a -OH group; R¿2? represents either a C...
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WO/2000/064914A1 |
The invention relates to modular, unsymmetrical bidentate organophosphorous ligands of the general formula (I) that have a trivalent phosphine functionality and a second trivalent phosphorous group that is bound to a chiral ligand struct...
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WO/2000/064583A1 |
Compounds having formula (A) are disclosed. M?1¿ and M?2¿ are the same or different and are transition metal atoms or ions; Z?2¿ and Z?3¿, independtly, are the atoms necessary to complete a 3-12 membered heterocyclic ring; Z?1¿ is a...
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WO/2000/064844A1 |
The invention relates to a method for the asymmetric dihydroxylation of olefins, using osmium catalysts for producing monofunctional, bifunctional and/or polyfunctional chiral 1,2 diols of formula (I): R?1¿R?2¿C(OH)-C(OH)R?3¿R?4¿. Ac...
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WO/2000/064882A2 |
An improved process for the preparation of single enantiomers of formula (I), and novel intermediates and processes thereto.
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WO/2000/061526A1 |
The invention relates to a method for carrying out the transition metal-catalyzed dimerization or codimerization of alkenes. The inventive method is characterized in that the dimerization or codimerization is carried out in compressed ca...
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WO2000040547B1 |
Methods for stereoselective substitution in which a (mono or un)- alpha -substituted unprotected beta -amino ester compound or salt thereof is reacted with an aliphatic electrophile in the presence of a base selected from alkyl lithium c...
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WO/2000/059513A1 |
Novel sulfur-containing analogs of 1$g(a),25- dihydroxyvitamin D¿3? are provided. These analogs are synthesized in a convergent manner by joining A-ring and C,D ring fragments. Each analog with 1$g(a),3$g(b)-substituent stereochemistry ...
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WO/2000/058253A1 |
A process for the preparation of carvone comprises hydrogenating carvoxime in the presence of a selectively poisoned catalyst. Preferred catalysts include noble metals supported on inorganic materials poisoned with a catalyst modifier. I...
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WO/2000/056701A1 |
An improved process for the preparation of non-hygroscopic salts of L(-)-carnitine, in which the characterizing step comprises heating a mixture comprising L(-)-carnitine inner salt and a fumaric acid or tartaric acid.
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WO/2000/056696A1 |
The present invention provides a method for producing an $g(a)-acyloxy carbonyl compound from an enol ester epoxide stereoselectively using an acid catalyst which is capable of affecting rearrangement of the enol ester epoxide with inver...
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WO/2000/056699A1 |
The invention relates to a method for hydrolyzing optically active amides to carboxylic acids and optically active amines with retention of the center of chirality. The hydrolysis of the amides is carried out with an alkali or alkaline e...
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WO/2000/055124A2 |
The present invention relates to novel cysteine protease inhibitors; the pharmaceutically acceptable salts and $i(N)-oxides thereof; their uses as therapeutic agents and the methods of their making.
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WO/2000/053305A1 |
Polymer enlarged catalysts and precatalysts for catalytic organic synthesis characterized in that the polymer enlargement has polymers based on isoprene or butadiene. The invention also relates to a method for the production and to the u...
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WO/2000/053614A1 |
The invention relates to a method for producing glyco-conjugates of 20(S)-camptothecin in which a 3-O-methylated $g(b)-L-fucose building block is linked to the 20 hydroxyl group of a camptothecin derivative via thiourea-modified peptide ...
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WO/2000/051979A1 |
The invention provides novel PGF analogs. In particular, the present invention relates to compounds having a structure according to formula (I) wherein R¿1?, X, and Z are defined below. This invention also includes optical isomers, dias...
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WO/2000/050430A1 |
The application relates to diazaphospholidine compounds of Formula (1) and Formula (2) where A and B are independently selected from C(R¿22?R¿23?) and C(R¿22?R¿23?)C(R¿24?R¿25?); R¿1?, R¿2?, R¿3?, R¿4?, R¿18?, R¿19?, R¿20?, ...
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WO/2000/050365A1 |
The present invention relates to a process for stereoselective cycloaddition reactions which generally comprises a cycloaddition reaction between a pair of substrates, each either chiral or prochiral, that contain reactive $g(p)-systems,...
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WO/2000/048988A1 |
Compounds of formula (1) and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined in the specification, are effective inhibitors of the binding of VCAM-1 to VLA-4 $i(in vivo) and are useful in treating ...
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WO/2000/049028A1 |
The invention concerns a method for preparing a compound of formula (I) wherein: A represents naphthyl or phenyl optionally substituted; and Ar¿1?, Ar¿2? independently represent a saturated or aromatic carbocyclic group, optionally sub...
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WO/2000/047551A2 |
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural an...
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WO/2000/047591A1 |
The present invention relates to analogs of (1R, cis)-4-(6-amino-9H-purin-9-yl)-2-cyclopentene-1-methanol, processes for their preparation, and their use in treating viral infections.
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WO/2000/046175A1 |
The present invention relates to a new microbial process for the preparation of compound formula (I) from a compound of general formula (II) wherein R stands for an alkali metal or ammonium ion, by the submerged cultivation of a mold str...
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WO/2000/046186A1 |
The present invention relates to a process for preparing (R)-4-cyano-3-hydroxybutyric acid ester derivatives and more particularly, to a process for preparing optically pure (R)-4-cyano-3-hydroxybutyric acid ester derivatives expressed b...
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WO/2000/044716A1 |
Compounds of formula (B): (1a), or (1b), (1c) are provided wherein the variables are as defined herein which are useful in disease conditions mediated by TNF-$g(a), such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative c...
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WO/2000/044717A2 |
Facile methods for preparing diketide and triketide thioesters are disclosed. The resulting thioesters may be used as intermediates in the synthesis of desired polyketides, and may contain functional groups which ultimately reside in sid...
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WO/2000/043345A1 |
The invention relates to an improved method for the industrial-scale production of L-phenylephrine hydrochloride 3 by asymmetric hydrogenation as key step and a special series of subsequent steps. According to the invention [Rh(COD)Cl]¿...
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WO2000001687A9 |
Novel benzothiepines, derivatives, and analogs thereof; methods of preparing such compounds; pharmaceutical compositions containing such compounds; and methods of using these compounds and compositions in the preparation of a medicament,...
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WO/2000/040545A1 |
The invention concerns a novel method for preparing chiral amino acids of formula (I) characterised in that it consists in contacting a racemic hydantoin of formula (II) with an enantiomeric splitting agent.
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WO/2000/040529A1 |
The invention relates to the use of compounds of formula (I): wherein X is -C(O)-, -C(S)-, -C=NOH, or -CH(R?7¿)- wherein R?7¿ is hydrogen, hydroxy, C¿1-7?alkoxy, -OR?8¿ or -NR?8¿R?9¿ (wherein R?8¿ is a group -Y?1¿R?10¿ (wherein ...
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WO/2000/040552A1 |
The present application relates to novel aminomalonamides of formula (1) and pharmaceutical composition thereof which are useful for inhibiting matrix metallo-proteinases.
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WO/2000/040548A1 |
The present invention relates to new compounds for the inhibition of blood clotting proteins, and more particularly, to arylalkanoyl derivatives of formula (I), wherein R(1), R(2), R(3), R(4), R(5), R(6a) and R(6b) have the meanings indi...
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WO/2000/039068A1 |
The invention relates to a method for producing glyoxylic acid esters from glyoxylic acid ester hemiacetals which a) are directly transesterified with an alcohol in the presence of a catalyst; or b) are firstly converted into the corresp...
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WO/2000/039324A2 |
The invention relates to a new method for producing enantiomer-enriched 1-amino-4-(hydroxymethyl)-cyclopent-2-ene derivatives of the general formulae (I) and (II) in which R?1¿ is hydrogen or a possibly substituted C¿1-8? alkyl rest, a...
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WO/2000/037438A1 |
The present invention relates to novel thio-aminotetralin compounds of formula (I) wherein Z, X, R¿1?, R¿2?, R¿3?, R¿4?, R¿5?, and R¿6? are defined herein. The compounds are useful in pain management.
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WO/2000/037445A1 |
The invention concerns a lower alkyl ester of formula (I) and its optically pure isomer; the latter is obtained either by enantioselective enzymatic hydrolysis, or by cyclisation of a compound of formula (VI).
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WO/2000/037478A1 |
The invention relates to novel ligands and complexes for the homogeneous catalytic enantioselective hydrogenation. The invention specifically concerns the ligands of general formula (I). Another aspect of the invention relates to the com...
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WO/2000/037436A1 |
This invention relates to sulfonamide derivatives of formula (Ia) (in which R is -CH(R?2¿)Ar?1¿ or -CH(R?2¿)CH=CHAr?1¿, and the other variables are as defined in the claims) that are inhibitors of procollagen C-proteinase, pharmacolo...
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WO/2000/037426A1 |
The present invention relates to novel oxo-aminotetralin compounds of formula (I), wherein X, R¿1?, R¿2?, R¿3?, R¿4?, R¿5?, and R¿6? are defined herein. The compounds of formula (I) are useful in pain management.
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