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WO/2003/095466A1 |
The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comp...
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WO/2003/093285A1 |
The invention relates to ferrocenyl ligands of general formula (II), the Sfc,S-enantiomer or the Rfc,R-enantiomer of the ferrocenyl ligands of formula (II) being enriched, and a method for producing such ligands.
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WO/2003/093222A1 |
Novel polymorph Form C of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine is produced having different infra red spectrum and X-ray diffraction patterns from previously known forms of the compound.
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WO/2003/092578A2 |
The present invention relates to improved methods for synthesising cyproterone acetate (17&agr -Acetoxy-6-chloro-1&agr , 2&agr -methylene-4,6-pregnadiene-3,20-dione) from solasodine. The methods of the invention are shorter as those of t...
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WO/2003/093292A1 |
The invention relates to compounds of general formula I and the pharmaceutically compatible salts thereof, wherein R1 represents hydrogen, C1- to C6-alkyl, COR4, COOR4, COSR4 or CONHR5, wherein R4 represents C1- to C6-alkyl or unsubstitu...
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WO/2003/091196A1 |
The invention relates to a novel process for synthesizing organic compounds of general Formula (I). The said process may be carried out on an industrial scale and makes it possible to obtain from a mixture of racemic alcohols of formula ...
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WO/2003/091207A2 |
This invention provides a method of preparing amine stereoisomers, which comprises stereoselectively reducing a sulfinylimine that bears on the sulfmyl group a residue of an alcohol, thiol or amine, or reacting a sulfmylimine stereoisome...
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WO/2003/087026A1 |
Compounds of the general formula (I) are valuable therapeutics for the treatment of cancer and cancer related diseases.
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WO/2003/086605A2 |
One aspect of the present invention relates to ionic liquids comprising a pendant Bronsted-acid group, e.g., a sulfonic acid group. Another aspect of the present invention relates to the use of an ionic liquid comprising a pendant Bronst...
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WO/2003/084933A2 |
The invention relates to a method for producing chiral imidazolidin-2-ones of general formula (I), in which R1 represents C1-C8-alkyl, cyclohexyl-, phenyl-, a phenyl radical substituted with C1-C6-alkyl-, halo-, nitro-, C1-C6-alkoxy-, C1...
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WO/2003/084971A1 |
The present invention relates to ligands of the general formula (I). In addition, a process for the production thereof and the use thereof are demonstrated.
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WO/2003/084942A2 |
The present invention describes the synthesis of the following compounds in high stereochemical purity by a novel stereoselective alkylation of 2-methyl-4-protected piperazines using an inorganic base. (I)
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WO/2003/082812A2 |
A process for the preparation of a compound of formula (I); in which R represents H or an acid protecting group which comprises reacting a compound of formula (II); in which R is as previously defined with a compound of formula (III); wh...
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WO/2003/080855A2 |
The present invention relates to a method for the deracemisation or chiral inversion of chiral amines by enzymatic treatment. The method employs a stereoselective enzymatic conversion and either a non-selective or partially selective che...
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WO/2003/079975A2 |
The present invention relates generally to processes for the efficient production optically active 3-substituted lactams of formula (I) [Insert chemical formula here] process, comprising: contacting a compound of formula (II): [Insert ch...
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WO/2003/078420A2 |
A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula (I) wherein R, Ar, and Q are defined as set forth herein, and inter...
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WO/2003/078399A1 |
The asymmetrical hydrogenation of 1-(4-methoxybenzyl)-3,4,5,6,7,8-hexahydroisoquinolinium salts to yield (S) or (R)-1-(4-methoxybenzyl)-1,2,3,4,5,6,7,8-hexahydroisoquinolin
ium salts can be effected with superior optical yield by the use...
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WO/2003/076451A1 |
The invention relates to bidentate organophosphorous ferrocenyl ligands containing ligands of formula (I), to their complex compounds and to their utilization in catalytic processes.
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WO/2003/076072A1 |
A practical chiral zirconium catalyst, characterized in that a chiral zirconium catalyst is fixed on a zeolite. The practical chiral zirconium catalyst can maintain high catalyst activity after the storage for a long period of time, is s...
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WO/2003/074487A1 |
A process for the production of optically active β-hydroxy esters represented by the general formula (&Verbar &Verbar &Verbar ): (&Verbar &Verbar &Verbar ) [wherein R1 is optionally substituted hydrocarbyl or the like; R2 is different f...
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WO/2003/074169A2 |
Metallic catalysts of the general formula (I) and their precursors, suitable for chemo- regio- and stereoselective reactions, derived from ortho- bis(1-phospholanyl)-heteroarenes. The new catalysts are characterized by the presence of tw...
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WO/2003/074717A1 |
A process for preparation of optically active allenes represented by the general formula (1): (1) [wherein R2 and R3 are different from each other and each hydrogen, optionally substituted C1−20 alkyl, or optionally substituted C6−20...
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WO/2003/072559A1 |
The invention relates to methods for producing enantiomer-pure 3-amidinophenylalanine derivatives, based on 3-cyanophenylalanine derivatives, which are used as pharmaceutically active urokinase inhibitors. The inventive production method...
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WO/2003/072576A2 |
Compounds of the formula (I), or a pharmaceutically−acceptable salt, or an in−vivo−hydrolysable ester thereof, wherein −N−HET is, for example, formula (Ic) or (If) wherein R1 is, for example, halogen or a (1−4C)alkyl group wh...
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WO/2003/070720A1 |
A novel route is described for the synthesis of N-methyl-3-hydroxy-3-(2-thienyl)propylamine IV, which can be used as a starting compound for the preparation of duloxetine. N-methyl-3-hydroxy-3-(2-thienyl)propylamine is synthesized via no...
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WO/2003/070676A1 |
A process for easily producing from an inexpensive material an optically active 3-halo-1,2-propanediol derivative useful as an intermediate for medicines. The process comprises reacting 2-chloroallyl alcohol, which is easily available at...
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WO/2003/066578A1 |
A pinene derivative represented by the general formula (I) or a salt thereof; and a process for producing the derivative or salt or a process for producing from the derivative or salt an optionally active 2-(t-butoxycarbonyl)amino-3-hydr...
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WO/2003/064392A1 |
The invention relates to a process for the manufacture of a compound of formula (I) or a salt, especially a pharmaceutically acceptable salt with a base, thereof or a lactone thereof wherein the element (II) represents -CH2-CH2- or -CH=C...
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WO/2003/064382A2 |
A method for preparing an alkali metal salt comprising: (a) condensing a disilyloxydiene with an aldehyde in the presence of a titanium (IV) catalyst in an inert solvent to form a 5(S)Âhydroxy−3−ketoester&semi (b) reducing the 5(S)â...
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WO/2003/063852A1 |
A preventive and/or therapeutic agent for urinary incontinence which contains as an active ingredient an N-aminoalkylglycinamide derivative represented by the following formula (I), an optical isomer thereof, or a pharmaceutically accept...
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WO/2003/061825A1 |
The present invention provides a catalyst system and a process for the preparation of a nonracemic chiral alcohol by hydrogenation of a ketone using the catalyst system, wherein the catalyst system comprises ruthenium, a nonracemic nonat...
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WO/2003/062181A1 |
the present invention provides a process for the preparation of a nonracemic diastereorner of 1-(4-benezoxy-phenyl)-2-(4-hydroxy-4-phenyl-piperidin-1-yl)-
1-propanol by hydrogenation of a corresponding noracemic 1-(4-benzoxy-phenyl)-2-(4...
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WO/2003/061826A1 |
The present invention provides a catalyst system and a process for the preparation of a nonracemic chiral alcohol by hydrogenation of a ketone using the catalyst system, wherein the catalyst system comprises ruthenium, a nonracemic chira...
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WO/2003/061660A1 |
The present invention relates to melanocortin receptor agonist of the formula (I): which is useful in the treatment for obesity, diabetes, and male and/or female sexual dysfunction.
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WO/2003/062180A1 |
The present invention provides a process for the preparation of a nonracemic diastereomer of 1−(4−benzoxy−phenyl)−2−(4−hydroxy−4−phenylâˆ
’piperidin−1Âyl)−1−propanol by hydrogenation of a corresponding nonracemic 1...
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WO/2003/061824A1 |
The present invention provides a catalyst system and a process for the preparation of a nonracemic chiral alcohol by hydrogenation of a ketone using the catalyst system, wherein the catalyst system comprises ruthenium, a nonracemic chira...
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WO/2003/059335A1 |
The invention relates to the phenyl sulfoxides and phenyl sulfones of formula (I) and to methods for producing the same as well as to their use in the production of drugs for the treatment and/or prophylaxis of diseases, especially Alzhe...
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WO/2003/059902A1 |
The invention relates to a method for producing pure racemic R- or S-thioctic acid or the mixtures thereof by transesterification of 6,8-disubstituted octanoic acids, to the salts or esters thereof with sulfides, sulfur and sulfites. In ...
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WO/2003/059512A1 |
The invention concerns a catalyst immobilized on silica for heterogeneous catalysis, in the form of silica particles of average grain size distribution ranging between 15 $g(m)m and 2 mm comprising a ligand bound to the particles by a co...
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WO/2003/057649A2 |
An ammonium selective ionophore for use in ion selective electrodes. The electrodes can be used to measure ammonium chloride, for example, at different concentrations (curves 1-6 in Figure 1).
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WO/2003/053176A2 |
The present invention relates to smoking articles such as cigarettes, and in particular to a method and composition for providing a cooling effect to cigarettes. The tobacco rod of the cigarette contains a cyclic alpha-keto enamine that ...
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WO/2003/053886A1 |
The present invention relates to a process and a device for the gassing of a liquid phase with hydrogen. The process and the device are characterised by the form of the gassing of the solution with hydrogen. This is metered in without bu...
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WO/2003/053916A1 |
The invention concerns a new process for preparing (S)-(+)-2-(substituted phenyl)-2-hydroxy-ethyl carbamates and to novel intermediates used in this process. It further relates to polymorphic forms of said carbamates and to processes for...
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WO/2003/051827A1 |
The invention relates to a process for the preparation of an enantiomerically enriched compound of formula (1) or a salt thereof, in which R?1¿ and R?2¿ each independently represent an (hetero)alkyl or (hetero)aryl group, wherein R?1¿...
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WO/2003/050062A2 |
Methods for production of chirally pure $g(a)-amino acids and N-sulfonyl $g(a)-amino acids are described. An aldehyde and a cyanide salt are reacted with an $g(a)-methylbenzylamine to afford a product. The product reacts with a strong ac...
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WO/2003/050063A2 |
A process is provided for preparing chirally pure S-enantiomers of $g(a)-amino acids comprising the steps of: a) preparing an organometallic reagent from an alkyl halide of the Formula (R)¿2?CH(CH¿2?)¿n?CH¿2?X; b) adding the organome...
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WO/2003/049681A2 |
A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds are useful as factor Xa inhibitors.
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WO/2003/048117A2 |
The invention concerns compounds of formula (I), wherein A is a group of formula (a) or (b), wherein: R represents a hydrogen or halogen atom, a -S(O)z(C1-C4)Alk wherein z is 0, 1 or 2, a -NHSO2(C1-C4)Alk, -SO2NH(C1-C4)Alk, -NHSO2-(C1-C4...
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WO/2003/048102A1 |
The invention relates to a method for the production of dihydroxycarboxylate esters and a total synthesis for the production of R-(+)-&agr lipoic acid.
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WO/2003/048173A1 |
The present invention is based around the discoveries that novel ligands of formula (4), and the opposite enantiomers thereof, (i) have utility as components of catalysts for asymmetric hydrogenation and (ii) are readily accessible by an...
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