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WO/2000/055125A2 |
The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
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WO/2000/053544A1 |
A process for producing a carboxylic acid derivative characterized by mixing a quaternary ammonium salt having a specific triazine ring in the molecule, a carboxylic acid compound, and a compound having a nucleophilic functional group to...
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WO/2000/050377A1 |
A method for selective mono-N-alkylation of primary amines to produce secondary amines that are substantially free of overalkylated tertiary amines and quaternary ammonium salts, under mild reaction conditions without the necessity of pr...
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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 $i(in vivo) and are useful in treating ...
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WO/2000/047031A2 |
The present invention is directed to partitioning agents and methods of using same to effectuate separation of a reactant, intermediate product, and/or final product from a reaction mixture while minimizing the need for traditional separ...
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WO/2000/047555A1 |
Disclosed is a composition of (1) a substituted benzaldehyde having general formula (I) where X is a leaving group in the ortho or para position, (2) a mercaptide having the general formula MSR' in an amount about stoichiometric to about...
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WO/2000/046190A1 |
A process for producing 2-hydroxy-4-methylthiobutanoic acid is provided wherein 2-hydroxy-4-methylthiobutyronitrile is converted to 2-hydroxy-4-methylthiobutanamide by using sulfuric acid, then adding an aqueous solution containing ammon...
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WO/2000/044716A1 |
Compounds of formula (B): (1a), or (1b), (1c) are provided wherein the variables are as defined herein which are useful in disease conditions mediated by TNF-$g(a), such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative c...
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WO/2000/044706A1 |
A process which comprises converting a $g(a)-amino acid ester into the corresponding imine to thereby protect the amino group of the ester, reacting the imine with a halomethyllithium to form an N-protected $g(a)-amino halomethyl ketone,...
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WO/2000/044709A2 |
Compound of the formula (B) are useful in treating disease conditions mediated by TNF-$g(a), such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage l...
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WO/2000/044713A1 |
The invention concerns compounds of formula (I) which are useful in treating disease conditions mediated by TNF-$g(a), such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease an...
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WO/2000/043360A1 |
High-quality N-protected S-phenylcysteine compounds represented by general formula (1) are easily, simply and efficiently isolated in high yield by salting out the compounds as salts thereof with bases in the presence of water. In said f...
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WO/2000/043359A1 |
A process for producing an organic polysulfide compound comprises contacting, in th presence of a catalyst, a mercaptan with elemental sulfur to produce a product medium and contacting the product medium with a material comprising carbon...
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WO/2000/041998A1 |
Propargylether derivatives of formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R¿1? is hydrogen, alkyl, cycloalkyl or optionally substituted aryl, R¿2? and R¿3? are each independently hydrogen or...
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WO/2000/041990A1 |
The invention relates to novel compounds of formula (I), wherein R stands for phenyl, phenyl which has been substituted by C¿1-4?alkyl, C¿1-4?alkoxy or halogen, naphthyl or an aromatic ring with heteroatoms; X means O, S, SO oder SO¿2...
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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/2000/039078A1 |
The present invention relates to methods for production of sulfurized diphenyloxides wherein a diphenyloxide is reacted with elemental sulfur in the presence of solid acid catalyst. The solid acid catalyst can be a zeolite or a catalytic...
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WO/2000/039079A1 |
The invention concerns a method for preparing aromatic diphenyl thioethers. More particularly the invention concerns the preparation of 4-chloro-4'-thiomethyldiphenylether. The inventive method for preparing an aromatic diphenyl thioethe...
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WO/2000/037440A1 |
Optionally fluorine-substituted alkyl or alkenyl poly(ethylene oxides) the compounds of general formula (1) in which R is an alkyl group with 10-20 carbon atoms, an alkenyl group with 10-20 carbon atoms or a fluoroalkyl or fluoroalkenyl ...
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WO/2000/037439A1 |
A method for the preparation of aromatic hydroxythiols including oxidizing an aromatic aminothiol to form an aminodisulfide compound; forming a bis-diazonium salt of the aminodisulfide compound; and reacting the bis-diazonium salt with w...
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WO/2000/035866A2 |
A method for the preparation of hydroxythiol compounds by reacting a hydroxyl-protected halide compound having the structure: X-R-OPg with magnesium in a Grignard-suitable solvent to form a hydroxyl-protected magnesium halide compound, w...
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WO/2000/034235A1 |
A process which can be used to produce an organic disulfide is provided. The process comprises contacting a mercaptan in the presence of an oxygen-containing fluid, a catalyst, optionally a cocatalyst, and further optionally a solvent or...
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WO/2000/031029A1 |
The invention relates to a method of producing organic disulfides by oxidizing mercaptans with sulfur which is dissolved in an organic disulfide and using an amine as the catalyst. Said mercaptans are used as 'crude mercaptan flow' from ...
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WO/2000/029394A1 |
Disclosed is a method for the production of isoxazols of formula (I), wherein the substituents have the following meanings: R?1¿ hydrogen, C¿1?-C¿6?-alkyl, R?2¿ hydrogen, C¿1?-C¿6?-alkyl, R?3¿, R?4¿, R?5¿ hydrogen, C¿1?-C¿6?-a...
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WO/2000/027809A1 |
The invention concerns a method for preparing methionine aminoamide. The invention also concerns the preparation of methionine without co-production of salts, from an aqueous solution containing essentially methionine aminonitrile by pro...
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WO/2000/027810A1 |
The present invention provides valuable intermediates which can be used in the synthesis of a compound having polyene chain structure, processes for preparing the same, and a process for preparing $g(b)-carotene by using said intermediat...
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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/2000/024697A1 |
Aldehyde derivatives of polyethylene glycols and methods of making thereof are disclosed. These aldehyde derivatives can be used to make polyethylene glycol-hydrazines, polyethylene glycol-thiols, polyethylene glycol amines, and branched...
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WO/2000/023409A1 |
A method is provided for synthesizing diaryl-substituted heterocyclic compounds, particularly 2,5-diaryl-substituted tetrahydrofurans and tetrahydrothiophenes. Methods for synthesizing starting materials and intermediates are provided as...
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WO/2000/021924A1 |
The invention relates to benzocyclohexandiones of general formula (I), a method for the production and use thereof as herbicides and plant growth regulators. In said general formula (I), R?1¿, R?2¿, R?3¿, R?4¿, R?5¿, R?6¿ and R?7¿...
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WO/2000/021920A1 |
Compounds of the formula (1a), wherein R1 is a group of the formula (2) where R1, R2, A, B, U, V, W, X, Y, Z, k and n have the significance given in the specification, are useful to treat rheumatoid arthritis, psoriasis, multiple scleros...
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WO/2000/020389A1 |
A compound having formula (I) wherein R?1¿ is oxo, -OR?a¿, -OC(=O)R?b¿; or (A); R?2¿ is H; or R?1¿ is -OR?c¿ and R?2¿ is -OR?d¿; or R?1¿ and R?2¿ together form -O(CH¿2?)¿m?O-; and any pharmaceutically-acceptable salt thereof ...
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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/2000/015614A1 |
The invention relates to novel pyridyl derivatives (I), their use as medicaments, pharmaceutical formulations including them and methods for their preparation.
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WO/2000/015585A1 |
The invention concerns a method for the condensation of aromatic derivative(s) or a sulphinic derivative by a perhalogenated, advantageously perfluorinated, carbon atom. Said method is characterised in that it consists in subjecting said...
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WO/2000/015625A2 |
The present invention relates to methods of making dihydropyrone HIV protease inhibitors.
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WO/2000/014060A1 |
A process for the preparation of aromatic thiols represented by the general formula (I): Y¿n?-Ar-(SH)¿m? (wherein Ar is an aromatic hydrocarbon residue; Y is at least one kind of substituent bonded to a carbon atom constituting the aro...
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WO/2000/014059A1 |
The invention relates to a method for producing derivatives of 4-alkylsulfinyl methylarylene methanols. Derivatives of 4-alkylsulfinyl methylarylene methanols are valuable monomers in the production of conjugated polymers, which are suit...
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WO/2000/008033A1 |
The present invention is directed to novel water-soluble prodrugs of aliphatic or aromatic hindered hydroxyl group containing pharmaceuticals.
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WO/2000/006555A1 |
This invention provides a process for preparing compounds of formula (1) wherein: X is phenyl optionally substituted with one or more substituents selected from the group consisting of halogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 ca...
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WO/2000/002852A1 |
The invention concerns a novel method for preparing hydroxymethylthiobutyric acid by sulphuric hydrolysis of hydroxymethylthiobutyronitrile.
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WO/2000/002853A1 |
The invention concerns an improved method for separating hydroxymethylthiobutyric acid by neutralising hydroxymethylthiobutyronitrile sulphuric hydrolysate, decanting and treating each phase with an organic solvent.
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WO/2000/001669A2 |
The present invention relates to 2-nitro-5-(phenylthio)-anilines which are obtained by reacting 5-chlorine-2-nitroanilines with thiophenols and ammonia in a solvent.
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WO/1999/067208A1 |
Derivatives of hydroxyphenylsulfanylbenzoic and hydroxyphenylsulfanylarylacetic acids of formula (I), wherein X is H, halogen or NO¿2? group, a is 0 or 1, and m is 2 to 4 if Z is either 4-acetyl-3-hydroxy-2-propylphenoxy of formula (II)...
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WO/1999/065878A1 |
A process for preparing intermediates and benzoquinolin-3-one pharmaceuticals, such pharmaceuticals are effective in treating conditions consequent on 5$g(a)-reductase.
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WO/1999/064385A1 |
The present invention relates to a method for condensing at least one carbonyl compound on an electroattractor radical on a carbocyclic aromatic thioether or ether, characterised in that the electroattractor radical present on said carbo...
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WO/1999/062871A1 |
Novel 3-aryl proprionic acid derivatives and analogs, having general formula (I) and stereo- and optical isomers and racemates thereof as well as pharmaceutically acceptable salts, solvates and crystalline forms thereof, process for thei...
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WO/1999/062874A1 |
A process for producing highly pure trifluoro methylthiomethyl benzene derivatives, which are useful as intermediates in synthesizing drugs and pesticides, at a high yield by using readily available materials without resort to flon. This...
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WO/1999/059947A1 |
This invention relates to a process for the synthesis of ethers or esters comprising reacting an alcohol or carboxylic acid with an organic halide to produce an ether or ester respectively and a hydrogen halide, wherein further organic h...
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