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WO/2000/015599A1 |
The present invention relates to producing stereoselective nitro compounds by reacting a dicarbonyl compound with a nitrostyrene compound in the presence of a catalyst complex and a base.
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WO/2000/009472A1 |
N-Cyclopropyl-2-difluoromethoxy-3-halogenoanilines which serve as important intermediates in the preparation of quinolonecarboxylic acids useful as synthetic antimicrobial agents from industrially inexpensive and easily available raw mat...
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WO/2000/008495A2 |
The present invention provides a compound selected from the group consisting of (I), (II), and (III), wherein R?1¿ and R?4¿ are the same or different and are each H, C¿1?-C¿3? alkyl, phosphate, or C¿1?-C¿3? alkyl carboxylate; R?2¿...
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WO/2000/006527A1 |
The 3- and 4-methylcatechols are converted to the corresponding benzaldehyde by first alkylating the hydroxyl groups to form an alkylated methylcatechol. The methyl group is then converted to a methyl dibromide group using 1,3-dibromo-5,...
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WO/2000/005197A1 |
A substrate for solid phase synthesis comprising a solid phase-linker combination of formula (I) is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediate useful therein. Among the novel intermediat...
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WO/2000/003971A1 |
A process for selectively eliminating a compound of general formula (II) from a mixture of a compound of general formula (I) with the compound of general formula (II). This process comprises reacting the compound of general formula (II) ...
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WO/2000/002837A1 |
The invention relates to a method of oxidizing an alcohol to form an aldehyde or ketone using a ruthenium ion and oxygen in the presence of a substantially stable N-O free radical compound, wherein two atoms bound to the nitrogen atom ar...
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WO/1999/061410A1 |
This invention provides compounds of Formula (I) having structure (I) wherein: B and D are each, independently, hydrogen, halogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, aryl, heteroaryl, aralkyl of 6-12 carbon atoms,...
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WO/1999/061403A1 |
Compounds represented by general formula (I) and salts thereof, which are useful as glaucoma remedies, wherein R?1¿ is H, lower alkyl or phenyl, the phenyl being optionally substituted with lower alkyl, hydroxyl, lower alkoxy, halogeno,...
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WO/1999/059967A1 |
The invention relates to novel 2-(2-methylphenyl)-3,4-dihydro-2H-pyrrol derivatives of formula (I) in which Ar represents a substituted phenyl. The invention also relates to a number of methods for producing said derivatives and to their...
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WO/1999/059968A1 |
The invention relates to novel 2-(2-chlorophenyl)-3,4-dihydro-2H-pyrrol derivatives of formula (I) in which Ar represents substituted phenyl. The invention also relates to a number of methods for producing said derivatives and to their u...
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WO/1999/058509A1 |
The invention relates to a method for producing isoxazolene of the formula (I), where the substituents have the following meanings: R?1¿ is hydrogen, C¿1?-C¿6? alkyl, R?2¿ is C¿1?-C¿6? alkyl, R?3¿, R?4¿, R?5¿ are hydrogen, C¿1?...
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WO/1999/052850A1 |
The present invention relates to an oxidation which converts a primary or secondary alcohol of Formula (II) to an acid or ketone of Formula (I) with periodic acid and a catalytic amount of a chromium reagent.
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WO/1999/052849A1 |
The present invention relates to the oxidation of a primary alcohol of Formula (II) to the carboxylic acid of Formula (I): R?1¿CH¿2?OH$m(7)R?1¿CO¿2?H.
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WO/1999/051561A1 |
Process for the preparation of 3-bromoanisole comprising methoxydenitrating 3-bromonitrobenzene in the presence of a phase-transfer catalyst (PTC), and the preparation of 3-bromonitrobenzene by the bromination of nitrobenzene with bromin...
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WO/1999/047474A1 |
This invention relates to a novel, inventive process for the preparation of biphenyls or aromatic olefins by coupling reactions of the Suzuki coupling and Heck coupling type, using allylpalladium catalysts of the $g(m)-halo(triisopropylp...
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WO/1999/042433A1 |
Disclosed is a process for the nitration of aromatic compounds using oxygen activated by an inorganic catalyst and nitrogen dioxide. Since the present invention does not use concentrated nitric acid nor concentrated sulfuric acid used in...
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WO/1999/040052A1 |
It has been found possible to separate catalytically-active aminophosphonium catalysts from mixtures composed predominately of aminophosphonium catalyst residue(s) and heavy ends form a halogen exchange reaction conducted in an aprotic s...
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WO/1999/040056A1 |
The present invention concerns enzymatic aromatic hydroxylation-activated prodrugs, particularly anti-tumour prodrugs and those which are specifically activated by the hydroxylation activity of the enzyme CYP1B1.
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WO/1999/038829A1 |
A compound represented by formula (1) wherein each of ring A, ring B and ring C is independently a substituted or unsubstituted aromatic ring or a substituted or unsubstituted five or six-membered heterocycle which may be condensed with ...
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WO/1999/035117A1 |
The subject invention involves processes for making 2,4-difluoro-3-Q1-benzoic acid, wherein Q1 is derived from an electrophilic reagent, comprising the steps of: (a) treating 1-bromo-2,4-difluorobenzene with a strong, non-nucleophilic ba...
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WO/1999/035115A1 |
A benzyl or benzylidene tetralin or a pharmaceutically acceptable salt of benzyl or benzylidene tetralin represented by general formula (I) in which: a) R?1¿ completes a carbon-carbon double bond with the carbon at position 2, when x is...
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WO/1999/032463A1 |
This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.
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WO/1999/031265A1 |
Compounds having molecular weights of less than 1500 daltons that non-covalently interact with target proteins and covalently bond to target proteins at amino acid side chains that are not part of enzyme active sites, in which covalently...
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WO/1999/030680A1 |
Disclosed are $g(a)-amides of $i(L)-amino acids that produce fragrance or attenuate or mask malodor. In particular, glutamine and asparagine amides can be used in the invention. Such $g(a)-amides of $i(L)-amino acids are useful for gener...
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WO/1999/031030A1 |
The invention concerns a method for O-alkylation of phenol compounds comprising at least an acid, ester, aldehyde, amide or nitrile functional group, which consists in reacting said phenol compound with a halogenated aliphatic hydrocarbo...
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WO/1999/029666A1 |
The invention relates to compounds of formula (I) or a salt thereof in which R?a¿ represents the group (1) in which the ring A is 5, 6 or 7-membered carbocyclic ring optionally substituted by one or more C¿1-6?alkyl groups, fused at th...
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WO/1999/028282A1 |
A process for preparing a compound of Formula (I); where Q completes an optionally substituted 5- or 6-member saturated carbocyclic ring and R is optionally substituted phenyl or optionally substituted C¿3?-C¿6? cycloalkyl which proces...
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WO/1999/025335A1 |
A new family of inadone and tetralone tubulin-binding compounds (TBs) is disclosed. Unlike classical TBs, which inhibit mitosis among affected dividing cells, the TBs of the invention possess two unique properties: (1) they induce apopto...
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WO/1999/022858A1 |
A method of reacting an aromatic compound with an immiscible reacting agent involves the passage of the reactant along a flow path having a width of from 10 to 1000 $g(m)m in such a way that essentially laminar flow of the reactant takes...
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WO/1999/023061A1 |
According to the invention, a quantity of 0.5 to 20,000 ppm of one or more surface active substances from the group of anionic, cationic, zwitterionic or non-ionic is added to the reaction mixture during the conversion of aromatic compou...
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WO/1999/021824A1 |
The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorder...
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WO/1999/019291A1 |
Compounds represented by general formula (I) or salts thereof, wherein n is an integer of 2 or 3; R represents a straight-chain or branched saturated alkyl group having 4 or 5 carbon atoms, a cyclopentyl group, a cyclohexyl group or the ...
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WO/1999/019275A1 |
A process for electrophilic substitution of an aromatic compound, comprising contacting said aromatic compound, a precursor of the desired substituent and an aqueous reagent containing zinc halide, at an elevated temperature.
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WO/1999/016770A1 |
Tricyclic triazolobenzazepine derivatives in the form of a prodrug. The compounds are ones represented by general formula (I) and pharmacologically acceptable salts and solvates thereof. They are useful as an antiallergic and have excell...
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WO/1999/012886A1 |
The invention relates to a method for producing a dinitronaphthalene-isomer mixture by nitration of nitronaphthalene. According to said method, nitronaphthalene is reacted in a solvent of formula (I), wherein X represents nitrogen or sul...
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WO/1999/012919A1 |
Disclosed is a novel process and novel intermediates to prepare [R-(R*,R*) ]-N-[3-[1-[5, 6-dihydro-4-hydroxy -2-oxo-6-(2-phenylethyl) -6-propyl-2H-pyran-3- yl]propyl]phenyl]-5- (trifluoromethyl)-2- pyridinesulfonamide (XIX) which is a pr...
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WO/1999/012873A1 |
Active hydrogen atoms contained in an active hydrogen compound are activated by using as the activation catalyst a polymer gel having a three-dimensional network structure holding a solvent therein and bearing active sites inside the net...
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WO/1999/012887A1 |
The invention relates to a method for producing a dinitronaphthalene-isomer mixture by nitrating nitronaphthalene. The invention is characterized in that nitronaphthalene is optionally reacted in an inert organic solvent with 1 to 20 tim...
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WO/1999/010527A2 |
The invention relates to a method for isolating anionic organic substances from aqueous systems using polymer nanoparticles with cationic pH-sensitive surface groups. Extraction can be carried out directly from diluted solutions, biologi...
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WO/1999/006339A1 |
The invention concerns a method for preparing substituted benzyl bromides of general formula (I), wherein at least one substituent R?1-5¿ represents an electroattractive group, such as fluorine, chlorine, bromine, C¿1?-C¿4? alkoxycarb...
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WO/1999/006392A1 |
The invention concerns a method for preparing compounds of formula (I) in which R¿1? to R¿5?, n, Y are as defined in claim 1, comprising a step consisting in reacting a phenolic derivative of formula (II) in which R¿1? to R¿4? are as...
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WO/1999/006373A1 |
The invention relates to a method for producing 2-(3-pyrazolyl-oxymethylene) nitrobenzene derivatives of formula (I), wherein the substituents and indices have the meaning given in the Description, by bromination of an o-nitrotoluene of ...
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WO/1999/005087A1 |
A process for the preparation of a compound of general formula (I), wherein R?1¿ is hydrogen or C¿1?-C¿6? alkyl, C¿2?-C¿6? alkenyl or C¿2?-C¿6? alkynyl, any of which may optionally be substituted with one or more substituents sele...
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WO/1999/003802A1 |
The present invention provides a method of substituting a carbonyl compound with fluorine at the $g(a)-position, comprising reacting the carbonyl compound with a fluorinating agent in the present of a metal-containing catalyst. The react...
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WO/1999/002526A1 |
New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8-carbo and 8-oxy tropanes having 6- or 7-substituents. The compounds of the present invention can be racemic, pure $i(R)-enantiomers, or pure $i...
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WO/1999/000356A1 |
This invention relates to compounds of formula (I) which inhibit Factor Xa, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of patients suffering from conditions which can be ame...
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WO/1999/000114A2 |
The invention relates to the use of 1,3-bis-aromatic-prop-2-en-1-ones (chalcones), 1,3-bis-aromatic-propan-1-ones (dihydrochalcones), and 1,3-bis-aromatic-prop-2-yn-1-ones for the preparation of pharmaceutical compositions for the treatm...
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WO/1998/055437A1 |
The preparation of carbonyl compounds by oxidizing a nitro functional group of an organic compound is described. Oxidation is accomplished under catalyzed oxidative Nef reaction conditions.
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WO/1998/055446A1 |
The preparation of aromatic ketones substituted with a thioether group at the ortho position is accomplished by the initial reaction of an aromatic nucleus substituted with a halide and an ortho nitro group with a nitroalkane in the pres...
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