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WO/1998/021205A1 |
A method of preparation of optically pure isomers of hydroxyitraconazole, in particular the two $i(cis) dioxolane diastereomers of the $i(sec)-butyl $i(R,R)-isomer, and to phosphate and sulfate derivatives thereof is disclosed. Pharmaceu...
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WO/1998/021203A1 |
A method of preparation of optically pure isomers of hydroxyitraconazole, in particular the two $i(cis) dioxolane diastereomers of the $i(sec)-butyl (S,R)-isomer, and to phosphate and sulfate derivatives thereof is disclosed. Pharmaceuti...
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WO/1998/021199A2 |
Compounds of formula (I) in which A is =N- or (a); W is a group (W1), (W2) or (W3); R�11? is hydrogen, fluorine, chlorine, bromine or methyl; and R�1? to R�5?, R�13?,n�1? and n�13? are as defined in claim 1, and the pyrazole ...
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WO/1998/021213A2 |
A substantially pure single enantiomer of a compound of formula (1), wherein X?1¿ and X?2¿ are independently chlorine or fluorine and R is hydrogen, -P(O)(OH)¿2? or -SO¿3?H, or a salt thereof. A method of preparation of optically pur...
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WO/1998/017631A2 |
The invention relates to novel pesticidally active compounds of formula (1) and to their possible isomers and mixtures of isomers, wherein: R�1? is hydrogen, C�1?-C�5?alkyl, C�3?-C�6?alkenyl, C�3?-C�6?alkynyl, or Ar-C�1?-...
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WO/1998/017643A1 |
The present invention is directed to compound of formula (I), wherein R�1?, R�2?, R�3?, R�4?, R�5?, X, Y and (Ia) are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contactin...
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WO/1998/017267A1 |
Compounds containing two aromatic systems covalently linked through a linker containing one or more atoms, or 'linker' defined as including a covalent bond $i(per se) so as to space the aromatic systems at a distance 1.5-15�, are effec...
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WO/1998/015274A1 |
This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
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WO/1998/013350A1 |
The invention relates to the use of compounds of formula (I) wherein: R?2� represents hydroxy, halogeno, C�1-3?alkyl, C�1-3?alkoxy, C�1-3?alkanoyloxy, trifluoromethyl, cyano, amino or nitro; n is an integer from 0 to 5; Z represe...
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WO/1998/011091A2 |
Novel tricyclic compounds of formula (1.0) are disclosed. Compounds of formula (1.0) are represented by the compounds of formulas (1.4) or (1.5) wherein R?1�, R?3� and R?4� are each independently selected from halo. Also disclosed ...
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WO/1998/010761A1 |
The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH�2? group. The naphthosultam is further substituted with various ...
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WO/1998/007702A1 |
Diamide derivatives represented by general formula (1), wherein A represents optionally substituted phenyl, etc.; B represents -CH=CH-, -C$m(Z)C-, -(CH=CH)�2?-, -C$m(Z)C-CH=CH-, -CH=CH-C$m(Z)C-, phenylene, etc.; and W represents (a) or...
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WO/1998/006725A1 |
We have found that 2-unsubstituted indoles of structural formula (IV) can be cost-effectively synthesized in high yield by the palladium-catalyzed coupling/ring closure of a 2-halo or 2-trifluoromethylsulfonyloxy aniline (I) and an acyl ...
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WO/1998/006399A1 |
This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
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WO/1998/005607A2 |
The use of anorganic or organic polyacids to treat mineral fertilizers, in particular the use of polyacids as a mixture with at least one nitrification inhibitor to treat mineral fertilizers. The invention also concerns the use of select...
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WO/1998/005646A1 |
This invention provides compounds of formula (1) wherein X is CR?5�, where R?5� is H, Cl or CH�3?; Y is CR?5'� where R?5'� is H, Cl, or Br; Z is O, S, SO, SO�2?, CH�2?, CH�2?CH�2?, NR?6�; B is (i, ii, iii, iv, or v) w...
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WO/1998/005648A1 |
Novel isoquinoline derivatives represented by general formula (I) or pharmaceutically acceptable acid-addition salts thereof, prepared by aiming at providing novel compounds which have an inhibitory activity on nerve cell death of the ap...
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WO/1998/004545A1 |
Novel tricyclic N-cyanoimine compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl-protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abn...
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WO/1998/004528A2 |
Substituted pyridines of formula (IA) are produced by reaction of suitably substituted pyridylaldehydes with Grignard or Witting reagents, and the resulting products are appropriately reduced. The pyridines of formula (IA) are suitable a...
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WO/1998/003476A1 |
The invention relates to compounds of formula (I), in which R�1? and R�2? are, independently of each other, lower alkyl or lower alkoxy-lower alkyl; R�3? and R�4? are, independently of each other, sec-lower alkyl or tert-lower al...
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WO/1998/003504A1 |
A class of substituted aminocyclohexane derivatives are selective agonists of 5-HT�1?-like receptors, being potent agonists of the human 5-HT�1D$g(a)? receptor subtype whilst possessing at least a 10-fold selective affinity for the 5...
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WO/1998/003505A2 |
Heterocyclic compounds represented by general formula (I) wherein R stands for an optionally substituted aromatic heterocyclic group; X stands for oxygen atom, an optionally oxidated sulfur atom, -C(=O)- or -CH(OH)-; Y stands for CH or N...
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WO/1998/003506A1 |
The invention concerns novel substituted pyrazole derivatives of general formula (I) in which R?1� - R?6� have the meanings given in the description. The invention also concerns a process for their preparation and their use as agents...
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WO/1998/002415A2 |
The invention relates to the use of at least one compound of general formula (I), in which R�1?, R�2? and R�3? independently of one another represent a hydrogen atom or an alkyl or alkenyl radical; R�4? represents an alkyl or alk...
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WO/1998/002422A1 |
New substituted aromatic carbonyl compounds and their derivatives have the general formula (I), in which Q stands for oxygen, sulphur or imino (NH); R?1� stands for hydrogen or halogen; and R?2� stands for the group -A?1�-A?2�-A?...
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WO/1998/000420A1 |
Thiophene derivatives of general formula (I) and pharmaceutically acceptable salts thereof. These compounds act as an anti-PCP agonist, thus being useful as psychotropic or antischizophrenic agents and so on. In said formula R�1? is -A...
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WO/1998/000408A1 |
Compounds of the formula (I), in which -A- is a group (A�1?), (A�2?) or (A�3?) where the bonding of -A- to the nitrogen atom takes place via the carbon atom; R�1? is halogen, C�1?-C�4?alkyl, C�1?-C�4?haloalkyl, C�1?-Cï¿...
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WO/1998/000389A1 |
This invention relates to a novel 2-hydroxypropionic acid derivative and its manufacturing method. Based on its mechanism to inhibit the CPT I, 2-hydroxypropionic acid derivative of this invention has blood glucose lowering effects so th...
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WO/1998/000430A1 |
Compounds having the formulas (I) and (Ia) are disclosed, as well as their preparation and use in medicaments.
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WO/1998/000399A1 |
A process for producing unsaturated nitrogen containing compounds such as enamides, enamines and aryl amines/amides is disclosed. A vinyl halide or aryl halide is reacted with an -NH- containing compound in the presence of a catalytic am...
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WO/1997/049399A1 |
This invention relates to the use of phenyl ureas of formula (I) in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8). The variables of formula (I) are defined herein.
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WO/1997/049704A1 |
The present invention is concerned with compounds of formula (I), the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hyd...
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WO/1997/048676A1 |
The invention relates to triphenylalkyl antibacterial compounds of general formula (1) pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action...
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WO/1997/047608A1 |
A novel process for producing 2-(1H-1,2,4-triazol-1-yl)acetophenones of general formula (I) which are useful as the starting materials in the production of antifungal agents and pesticides wherein R1 and R2 are the same or different and ...
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WO/1997/046555A1 |
Substituted imidazolylquinoxalinedione derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof and medicinal compositions comprising these compounds or salts thereof and pharmaceutically acceptable car...
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WO/1997/045425A1 |
A compound of formula (I) wherein R1 is indolyl or benzofuranyl; R2 is hydrogen, lower alkylthio(lower)alkyl or a group of formula (1) in which R5 is hydrogen, lower alkoxy or halogen; R3 is hydrogen, quinolyl or phenyl which may have a ...
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WO/1997/045402A1 |
Phenylsulfonylamide derivatives represented by general formula (I) and salts thereof, (wherein R1 is hydrogen or alkyl; R2 is COOR3 or CONHOR4; E is vinylene or ethylene; A is hydrogen, alkyl, carbocycle or heterocycle; J is single bond ...
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WO/1997/044323A1 |
The invention concerns novel mercapto-imidazolyl derivatives of formula (I), in which R and R1 have the meanings given in the description, as well as their acid addition salts and metallic salt complexes. The invention further concerns a...
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WO/1997/044332A1 |
The invention concerns sulphonyl-mercapto-triazolyl derivatives of formula (I-'alpha') or (I-'beta') in which R stands for alkyl, optionally substituted aralkyl and optionally substituted aryl, and R1 stands for various groups, as well a...
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WO/1997/044330A1 |
There is disclosed a process for the preparation of fluconazol which is a well-known antifungic agent, as well as pharmaceutically acceptable salts thereof, wherein a new compound having the formula (IV) in which R is H, benzyl, tripheny...
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WO/1997/042822A1 |
The invention relates to compounds of the formula (I) and the salts thereof, in which formula A is a (hetero)aromatic or heterocyclic bridge which is connected to the group SO2 via a direct bond or O, S, NH, CH2, or via alkylated NH or a...
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WO/1997/042956A1 |
This invention is directed to dihydropyrimidine compounds which are selective antagonists for human 'alpha'1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol ...
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WO/1997/043248A1 |
Compounds of general formula (I); salts of the compounds; and hydrates of them, wherein R1 is an optionally substituted heterocyclic group, CO2R6 (wherein R6 is alkyl) or CONR7R8 (wherein R7 and R8 are each independently hydrogen or alky...
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WO/1997/043269A1 |
The invention relates to novel triazolyl disulphides of formula (I), in which R1 has the meanings given in the description. It also relates to the acid addition salts and metal salt complexes of said triazolyl disulphides, a process for ...
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WO/1997/042178A1 |
The invention relates to acyl mercapto-triazolyl derivatives of the formula (I) in which R is alkyl, alkyl halide, optionally substituted aryl, optionally substituted aralkyl, alkoxy, alkylamino or optionally substituted arylamino, and R...
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WO/1997/042189A1 |
A class of compounds of formula (I) wherein Z, E, Q, T, U, V, W, M, R1, R7 and R8 are as defined herein; are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1D'alpha' receptor subtype whilst possessing ...
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WO/1997/042175A1 |
The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein ageing). Accordingly, compositions are disclosed which comprise substituted imidazolium compounds capable of inhib...
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WO/1997/042187A1 |
The invention relates to compounds of formula (I), wherein: R2 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino, nitro, C2-4alkanoyl, C1-4alkanoylamino, C1-4alkoxycarbonyl, C1-4alkylthio...
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WO/1997/041104A1 |
This invention relates to a compound of formula (I) wherein R1 is lower alkyl, R2 is heterocyclic group, etc., R3 is hydrogen, lower alkyl or halogen, R4 is lower alkyl or halogen, R5 is amino substituted with substituent(s) selected fro...
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WO/1997/041112A1 |
Compounds of formula (I), wherein R1 is hydrogen, methyl or trifluoromethyl, R2 is methyl or methoxy, A is C1-C4-haloalkyl, M is an alkali metal or alkaline earth metal atom and n is 1 or 2, are suitable for use as herbicides.
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