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WO/1995/022966A1 |
This disclosure relates to a novel class of hydroxamic and carboxylic acid based matrix metalloproteinase inhibitor derivatives. The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of su...
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WO/1995/022520A1 |
A compound of structure (I), wherein, when R8 = H: R1 = alkyl, cycloalkyl, arylalkyl, aryl; R2 = cycloalkyl, aryl, C3-C10 alkyl; X, Y = O, S(O)n, NH; Z = CH2OH, NHSO2R3, CHO, CO2R3, CONHR4R5, CN, COR6, H, halo, NHCN, NHCONR4R5, CONR4OR5,...
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WO/1995/021153A1 |
Phenyl acetic acid derivatives of formula (I) in which the components and index have the following meanings: X is NOCH3, CHOCH3 CHCH3 and CHCH2CH3; R1 is hydrogen and alkyl; R2 is cyano, nitro, trifluoro methyl, halogen, alkyl and alkoxy...
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WO/1995/021174A1 |
Compounds of formula (I): wherein R is C1-C6alkyl, C1-C6haloalkyl, C3-C6alkenyl, C3-C6alkynyl, C1-C4alkoxy or C3-C6cycloalkyl; R1 is halogen; R2 and R3 are each independently of the other C1-C4alkyl; R4 is halogen or a group of the formu...
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WO/1995/020570A1 |
The invention concerns hydroxamic-acid derivatives of general formula (I) in which A is hydrogen or a grouping which can be easily splitt off, A1 is hydrogen or alkyl, Ar is an optionally substituted arylene or hetero-arylene group, E is...
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WO/1995/019957A1 |
The following compounds: 2S-Hydroxy-3R-[1S-(tert-butylcarbamoyl)-2,2-dimethyl-propylc
arbamoyl]-5-methyl-hexanohydroxamic acid, 2S-Hydroxy-3R-[1S-(N,N-dimethylcarbamoyl)-2,2-dimethyl-propy
l-carbamoyl]-5-methyl-hexanohydroxamic acid, 2S-...
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WO/1995/019956A1 |
Matrix metalloproteinase inhibiting compounds of formula (I), wherein X is a -CO2H or -CONHOH group; R4 is a phenyl or 5- or 6-membered heteroaryl ring wherein any ring nitrogen atom may be oxidised as an N-oxide, which may be optionally...
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WO/1995/019965A1 |
Synthetic mammalian matrix metalloprotease inhibitors are disclosed that are useful for treating or preventing diseases wherein said diseases are caused by unwanted mammalian matrix metalloprotease activity and include skin disorders, ke...
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WO/1995/019961A1 |
Matrix metalloproteinase inhibiting compounds of formula (I), wherein X is a -CO2H or -CONHOH group; and one of the groups proximate to the amide bonds is a steric bulky group, showing enhanced oral absorption.
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WO/1995/017376A1 |
The invention relates to novel aryl acetic acid derivatives of formula (I) in which Ar, E, G, Q1, Q2 and Z have the meanings given in the description, processes for their production and their use as fungicides.
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WO/1995/016667A1 |
Process for the preparation of N-alkyl-N,O-diacetyl hydroxylamine, for instance N-methyl-N,O-diacetyl hydroxylamine, by catalytic reduction of a nitroalkane, for instance nitromethane, in the presence of acetic anhydride. As catalyst pre...
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WO/1995/013264A1 |
A hydroxamic acid derivative represented by general formula (1) and a medicinal preparation containing the same, having the effect of suppressing smooth muscle fiber growth and being usable as a vascular wall thickening preventive, a pos...
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WO/1995/012572A1 |
The present invention provides a compound of formula (I) processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and a method of treating disor...
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WO/1995/012603A1 |
This invention is directed to compounds of formula (I): wherein R1 is mercapto, acetylthio, carboxy, hydroxycarbamoyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, benzyloxycarbamoyl or (i) (where R6 is optionally substituted aryl,...
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WO/1995/010503A1 |
Amidoxime derivatives represented by general formula [I] and a flowering accelerator containing at least one of them as the active ingredient, wherein R1 represents halogen, alkynyloxy, haloalkyl, alkoxy, alkyl or methylenedioxy, and n r...
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WO/1995/007076A1 |
There are disclosed novel inclusion complexes of racemic ibuproxam and of optically active S-(+)-ibuproxam with hydrophilic and hydrophobic cyclodextrin derivatives and, in the case of optically active S-(+)-ibuproxam, also with 'beta'-c...
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WO/1995/006031A1 |
Compounds and methods are disclosed that are useful in inhibiting the TNF-'alpha' converting enzyme (TACE) responsible for cleavage of TNF-'alpha' precursor to provide biologically active TNF-'alpha'. The compounds employed in the invent...
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WO/1995/005358A1 |
Phenols and phenol derivatives having the general structural formula (I) are used to produce medicaments with fibrinogen-reducing effect. Also disclosed are new phenols and phenol derivatives, a process for producing the same and medicam...
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WO/1995/004715A1 |
An acylphenylglycine derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, and a preventive and remedy for diseases caused by an increased collagenase activity containing the same as the active ingr...
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WO/1995/004033A1 |
Compounds of formula (1) are described, wherein R1 represents (a), where R3 is a hydrogen or halogen atom or a methyl, trifluoromethyl or methoxy group; R2 represents a hydrogen atom or a methyl group; and the salts, solvates, hydrates a...
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WO/1995/003271A1 |
Use in the prevention and/or in the treatment of neurodegenerative diseases of 2-amino-4-phenyl-4-oxobutyric acid derivatives (I) which act as kynureninase enzyme inhibitors and/or kynurenine-3-hydroxylase enzyme inhibitors. In formula (...
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WO/1995/002575A1 |
Hydroxyurea compounds comprising halo substituted 1, 2, 3, 4-tetrahydronaphthalene, and indane derivatives, pharmaceutical compositions and their use as OPUFA and 5-lipoxygenase pathway inhibitors.
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WO/1995/001168A2 |
A novel pharmaceutical preparation contains an active principle with at least one pharmaceutically active amidin group which may be orally absorbed. The amidin group is a compound selected from the group (a), (b) and (c), in which R7 sta...
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WO/1995/000480A1 |
The present invention is related to novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of formula (I) wherein W represents -C(=O)- or -CH(OH)-; R1 represents hydrogen or...
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WO/1995/000140A1 |
A pharmaceutical composition comprises a gallium complex of desferrioxamine or penicillamine as active ingredient therein, in combination with a pharmacologically acceptable carrier. The gallium desferrioxamine or gallium penicillamine c...
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WO/1994/027965A1 |
The present invention relates to novel 5-HT4 receptor ligands which are 1-(5-halo-4-aminophenyl) (C2-6)alkan-1-one derivatives in which the 5-halo-4-aminophenyl group is substituted at its 2-position with (C1-4)alkyloxy or phenyl(C1-4)al...
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WO/1994/027947A1 |
This invention relates to substituted phenylcyclopropane derivatives, which carry various substituents on the cyclopropane ring, to processes for their preparation, to pharmaceutical compositions containing them, and to methods for their...
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WO/1994/027955A1 |
Intermediates and a stereoselective process for preparing hydroxyethylene dipeptide isosteres and lactone compounds which process comprises, as an essential step, the stereoselective reduction of the keto group in a 5S-4-keto-5-dibenzyla...
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WO/1994/026693A1 |
Novel compounds of formula (I) together with their salts and solvates have a number of uses in medicine, in particular as central muscle relaxants.
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WO/1994/026700A1 |
Compounds of formula (I) in which Y is hydrogen, C1-C4alkyl, C1-C4alkoxy, OH, CN, NO2, Si(CH3)3, CF3 or halogen, Z is a group (a) or (b) and R1 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4-alkynyl, C3-C6cycloalkyl, phenyl which is unsubs...
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WO/1994/026692A1 |
The present invention relates to amide and thioamide compounds of formula (I), synthesis thereof, intermediates, salts, solvates and physiologically functional derivatives thereof, pharmaceutical compositions containing them and to the u...
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WO/1994/025435A1 |
Compounds of formula (1), wherein R represents a -CONHOR6 [where R6 is a hydrogen atom or an acyl group], carboxyl (-CO2H), esterified carboxyl, -SR6 or -P(O)(X1R7)-X2R8 group, where X1 and X2, which may be the same or different, is each...
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WO/1994/025434A1 |
Compounds of formula (1) are described where R represents a -CONHOR6 [where R6 is a hydrogen atom or an acyl group], carboxyl (-CO2H), esterified carboxyl, -SR6 or -P(O)(X1R7)- -X2R8 group, where X1 and X2, which may be the same or diffe...
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WO/1994/025430A1 |
The present invention is concerned with novel hydroxamic acid derivatives of formula (I) and their use in medical therapy, particularly in the prophylaxis or treatment of clinical conditions for which an inhibitor of the lipoxygenase or ...
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WO/1994/025431A1 |
The present invention is concerned with novel hydroxamic acid derivatives of formula (I) and their use in medical therapy, particularly in the prophylaxis or treatment of clinical conditions for which an inhibitor of the lipoxygenase or ...
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WO/1994/024095A1 |
Compounds having a formula selected from the group consisting of (I), (a) and (III) and the respective pharmaceutically acceptable salts, esters and prodrugs thereof, wherein E is selected from the group consisting of -R14, -NR14R15, -SR...
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WO/1994/024096A1 |
Hydroxamic acids and hydroxamic acid ethers have formulae (I) and (II), in which Z1 and Z2 stand for the groups -NH-OY, -NR1-OY or -OX, at least one of the residues Z1 or Z2 in (I) or the residue Z1 in (II) being -NH-OY or -NR1-OY; R1 st...
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WO/1994/022309A1 |
Methods and compositions are disclosed that are useful for treating or preventing diseases wherein said diseases include skin disorders, keratoconus, restenosis, and wounds and the compositions include synthetic mammalian matrix metallop...
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WO/1994/021625A1 |
Compounds of formula (I), wherein R2 represents a C2-C6 alkyl group which may contain an ether or thioether linkage; R3 represents (a) the side chain of a naturally occurring alpha-amino acid in which any carboxylic acid group may be est...
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WO/1994/018158A1 |
The present invention provides novel N-hydroxyurea and hydroxamic acid derivatives of chemical formula (I), wherein R is C1-C4 alkyl or -NR1R2; R1 and R2 are each, independently, hydrogen or C1-C4 alkyl; M is hydrogen or pharmaceutically...
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WO/1994/017035A1 |
New aminoacid derivates have the general formula: T-Z-NR1-(R2CR3)-CO-Y-(CH2)n-R, in which R, R1 to R3, T, Z, Y and n are defined as in the first claim. They represent valuable NPY-antagonistic active substances. Also disclosed are their ...
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WO/1994/015908A1 |
A propionamide derivative represented by general formula (I) and a salt thereof, wherein R1 and R2 represent each hydrogen, etc.; R3 and R4 are combined together to represent optionally substituted C2-C7 alkylene, etc.; R5 represents hyd...
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WO/1994/014322A1 |
A compound having formula (I) wherein R1 is hydrogen, C1-4 alkyl, C1-4 haloalkyl, C2-4 alkenyl, C2-4 alkynyl, C3-6 cycloalkyl, aryl or aryl(C1-4)alkyl; R2 is hydrogen, C1-4 alkyl, C1-4 haloalkyl or C3-6 cycloalkyl; W is CH3O.CH = CCO2CH3...
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WO/1994/014755A1 |
A novel anti-active-oxygen agent which inhibits the generation of active oxygen species, is highly safe, can be preparated at a rather low cost, and contains an amino acid derivative represented by general formula (I) or a salt thereof a...
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WO/1994/014757A1 |
In order to prepare hydroxylamine-ethers having formula (I), in which X stands for NO2, CN, halogen, alkyl and halogen alkyl; Y stands for H, NO2, CN, halogen, alkyl and halogen alkyl; n equals 0 to 2 or 1 to 4 when Y and all X's stand f...
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WO/1994/014761A1 |
A compound having general formula (I), wherein R1 and R2 are independently hydrogen, C1-4 alkyl, C1-4 haloalkyl, C2-4 alkenyl, C2-4 alkynyl, C3-6 cycloalkyl, aryl or aryl(C1-4)alkyl; R3 is hydrogen, C1-4 alkyl, C1-4 haloalkyl or C3-6 cyc...
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WO/1994/012461A1 |
This invention relates to 4-substituted catechol diether compounds which are selective inhibitors of phosphodiesterase (PDE) type IV. The compounds of the present invention are useful in inhibiting PDEIV and in the treatment of AIDS, ast...
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WO/1994/011339A1 |
The invention provides as new compounds cis-cis-cis-tetrasubstituted cyclopentane compounds which are expected to be useful as chelating agents for alkaline earths, transition, lanthanide and actinide metal ions. The compounds have formu...
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WO/1994/011334A1 |
Compounds of general formula (I) in which the index and the constituents have the meanings below: n: 0, 1, 2, 3 or 4; X: CHOCH3, CHCH3 or NOCH3; Y: O or NH; R1: nitro, cyano, halogen, alkyl, alkyl halide, alkoxy, alkoxy halide, alkylthio...
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WO/1994/010148A1 |
The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein W is selected from optionally substituted pyridyl, naphthyl, and quinolyl; which inhibits lipoxygenase enzyme activity and l...
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