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WO/1993/025523A1 |
There is provided a process for preparing a compound of formula (I), wherein R is H or a hydroxy protecting group, R¿2? is an organic residue and R¿3? is H or a nitrogen protecting group, which process comprises reacting together a com...
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WO/1993/023406A1 |
The present invention relates to removal of t-butyldimethylsilyl protecting groups in the preparation of penems which are useful antibiotics. The invention provides a process for preparing a compound of formula (I), wherein R is a free o...
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WO/1993/008196A1 |
A compound represented by general formula (I) and a preventive or curative agent for fish diseases containing the same as an active ingredient, wherein A represents a single bond and R?1¿ represents (a), lower alkenoyl, cyclopropylcarbo...
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WO/1993/007154A1 |
The present invention provides methods of making compounds of the structure [Q - L1] - L - [L2 - B], wherein Q is a quinolone moiety; B is a beta-lactam moiety; L, L1, and L2 together comprise a carbamate-containing linking moiety, compr...
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WO/1993/004070A1 |
beta-lactam antibiotics of formula (I) or a salt thereof: wherein X is hydrogen or a group NHR1, wherein R1 is hydrogen or an amino protecting group, and R is an optionally substituted spiro, fused or bridged bicyclic or tricyclic group ...
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WO/1993/003042A1 |
A compound of formula (I), wherein R1, R2 and R3 may be various substituents, and R4 may be hydrogen or a salt or ester-forming group and =|= indicates that the =CR1R2 side chain may be present as either (a) or (b) isomeric forms, or as ...
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WO/1993/001174A1 |
The present invention provides compounds of formula (I), wherein R?1¿ is hydrogen, alkyl or CH¿2?alkyl where the alkyl portion is substituted by OH; A represents either a group CHR?21¿CHR?22¿OH or a group (II), where R?21¿ is hydrog...
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WO/1993/000345A1 |
The invention provides compounds of general formula (I) wherein R1 is a hydrogen atom, a negative charge or an ester residue; R is: a) -(CH2)n-A-CO2H, -(CH2)n-A-SO3H or -(CH2)n-A-PO3H2, wherein n is either zero, one or two and A is a gro...
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WO/1992/020665A1 |
The present invention provides compounds of formula (I), wherein x is zero, 1 or 2; R1 and R6 are each independently hydrogen, C1-4alkyl or CH2C1-3alkyl where the C1-3alkyl portion is substituted by OH; R2, R3, R4 and R5 are each indepen...
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WO/1992/020689A1 |
Penem compounds of formula (I) or esters or pharmaceutically acceptable salts thereof, in which one of R1, R2 or R3 is a heterocyclic group having up to 5 ring atoms, the remainder of R1, R2 and R3 being hydrogen, optionally substituted ...
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WO/1992/010502A1 |
Heterocyclic carboxylic esters or derivatives thereof, comprising a beta-lactam moiety linked by a carboxylic acid bridge to an imidazole moiety for use as antimicrobial agents are provided. Also methods for the preparation of these este...
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WO/1992/003444A1 |
Antibiotic penem compounds are represented by formula (I), wherein R represents a group of formulae (II) or (III) in which R1 is a linear or branched, C1-C6 alkyl group, R2 is a particular substituted or unsubstituted alkyl, aryl or aral...
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WO/1992/003443A1 |
Antibiotic penem coumpounds are represented by formula (I), wherein R represents a physiologically-hydrolyzable, ester-forming group. The physiologically hydrolyzable, ester-forming group useful in the penem compound of the present inven...
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WO/1992/003442A1 |
Antibiotic penem compounds are represented by formula (I), wherein R represents a group of general formulae (II), (III), or -CH2-Z, in which R1 is a linear or branched C1-C6 alkyl group, R2 is a particular substituted or unsubstituted al...
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WO/1992/001061A1 |
beta-Lactam derivatives are synthesized by an enzymatic reaction of the parent amino beta-lactam with the corresponding acylating agent, the concentration of the acylating agent plus the concentration of beta-lactam derivative in the rea...
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WO/1991/017995A1 |
A compound of general formula (I), wherein R�1? is a hydrogen atom, C�1?-C�6? alkyl, C�1?-C�6? alkoxy, cycloakyl or hydroxyalkyl, the alcoholic function of the hydroxyalkyl being free or protected; R�2? is a free or esterifie...
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WO/1991/016310A1 |
Antimicrobial quinolone thiourea compounds of general formula (I), wherein (1) A1, A2, A3, R1, R3, R4, and R6 form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial ...
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WO/1991/016327A1 |
Antimicrobial quinolonyl lactam compounds comprising a lactam-containing moiety linked to a quinolone moiety, of formula (I), wherein (1) A1, A2, A3, R1, and R4 generally form any of a variety of quinolone, naphthyridine or related cycli...
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WO/1991/016326A1 |
A simplified method for making the chloromethyl ester of sulbactam in which the tetraalkylammonium sulbactam salt is not dried and isolated prior to alkylation. The method comprises reacting a tetraalkylammonium salt and a sulbactam salt...
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WO/1991/014691A1 |
There is provided a process for preparing penem esters having antibacterial activity, starting from a compound of formula (II) wherein R1 is H or a hydroxy protecting group and Z is a C1-C10 alkyl or an aryl group which is reacted with a...
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WO/1991/005788A1 |
The present application discloses a process for the conversion of penicillin-1-(R)-sulfoxide(s) and/or cephalosporin-1-(R)-sulfoxides in solution, to their corresponding 1-(S)-sulfoxides comprising the step of treating said 1-(R)-sulfoxi...
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WO/1991/000283A1 |
There is provided a process for the preparation of compounds of formula (I) useful as antibacterials, wherein R represents hydrogen atom or a hydroxy protecting group, which process comprises reacting a compound of formula (II) wherein R...
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WO/1990/011782A2 |
A drug delivery system is described in which an immunoconjugate and a prodrug are used in association with each other to deliver a drug to a host target site such as a tumour. The immunoconjugate comprises an antibody or antibody fragmen...
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WO/1990/008764A1 |
The asymmetrical ureas have the formula (I) wherein R2 and R3, similar or different, represent a hydrogen atom or a structural fraction susceptible of being bonded to a nitrogen atom, appropriate for forming part of a ring wherein the ni...
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WO/1990/006928A1 |
6-(1-Carbamoyl-1-hydroxymethyl)penicillanic acid derivatives are useful as antibacterials and/or betalactamase inhibitors.
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WO/1990/004594A1 |
Antimicrobial quinolonyl lactam esters comprising a lactam-containing moiety linked, by an ester group, to the 3-carboxy group of a quinolone moiety. These compounds are of formula (I), wherein (1) R3, R4, and R5, together with bonds ''a...
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WO/1990/004591A1 |
Antimicrobial dithiocarbamoyl quinolone compounds of general formula (I), wherein A1, A2, A3, R1, R3, R4, and R6 form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobi...
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WO/1990/001484A1 |
A crystalline form of (5R,6S)-2-carbamoyloxymethyl-6-[(1R)-hydroxyethyl]-2-penem-3
-carboxylic acid incorporates two molecules of water per molecule of the acid and is useful as an antibacterial agent.
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WO/1988/010256A1 |
The present invention relates to a method for producing novel 4-[1-oxoalkyl]-2,5-oxazolidinediones, (4-1 OOD), and their use in a stereoselective method of producing beta-lactam-containing compounds which include several biologically act...
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WO/1988/008845A1 |
Diastereomeric 5R,6S-6-(1R-hydroxyethyl)-2-(1S-oxo-3R-thiolanylthio)-2-pene
m-3-carboxylic acid and 5R,6S-6-(1R-hydroxyethyl)-2-(1R-oxo-3S-thiolanylthio)-2-pene
m-3-carboxylic acid, and pharmaceutically-acceptable salts and in vivo hydro...
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WO/1988/007534A1 |
Certain beta-lactam epoxides have been found to be irreversible inhibitors of beta-lactamase enzymes, thus making them alternatives to clavulanic acid and sulbactam, and others are useful intermediates in the preparation of such compound...
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WO/1988/001615A1 |
Novel ester derivatives of carboxylic acid medicaments of formula (I), wherein R-COO - represents the acyloxy residue of a carboxylic acid drug or medicament, n is an integer from 1 to 3, and R1 and R2 are the same or different and are s...
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WO/1988/000186A1 |
A composition comprising an aqueous preparation on the basis of keratin softening, which contains as a swelling and penetration agent, an N-alkyl pyrrolidone wherein the alkyl group contains between 8 and 22 carbon atoms.
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WO/1988/000203A1 |
The extraction of water soluble antibiotics containing a phenolic or carboxylic group from an aqueous solution or fermentation broth using a N-C8-C14 alkyl pyrrolidone extractant and the process involving the extraction of said antibiotic.
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WO/1988/000185A1 |
A permanent hair color altering composition comprising an aqueous preparation on the basis of melanin dissolution and/or oxidation of a hair colorant dye intermediate, which contains as a swelling and penetration agent, an N-alkyl pyrrol...
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WO/1987/006231A1 |
Crystalline anhydrous amoxycillin is prepared by removing bound solvent molecules from a crystalline solvate (other than the trihydrate) of amoxycillin. A preferred crystalline solvate is the monomethanolate.
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WO/1987/006230A1 |
New process for the debromination and/or deiodination of 6,6-dihalo- and 6-monohalopenicillanic acids or derivatives thereof by treatment with dialkyl, trialkyl or diaralkyl phosphite, the desired compounds being obtained in good to exce...
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WO/1987/001371A1 |
New and improved method for the preparation of a compound of formula (I), in which R stands for halogen, giving rise to high yields of substantially pure 6beta-halopenicillanic acids, obtained in one step.
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WO/1987/000525A1 |
Compounds of general formula (I), and their pharmaceutically acceptable salts and in vivo hydrolysable esters, in which one of R1 and R2 denotes hydrogen, the other of R1 and R2 denotes an unsubstituted or substituted fused bicyclic hete...
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WO/1986/006723A1 |
A process for producing beta-lactam derivatives, which comprises reacting a beta-lactam derivative wherein the carboxyl group is protected and which is represented by the general formula: A-COO-X (wherein A represents a beta-lactam deriv...
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WO/1986/005182A1 |
beta-Lactam compounds, which are represented by formula (I) wherein R1 represents a hydrogen atom or a protective group for an amino group, and W represents (II) ou (III) wherein R2 represents a hydrogen atom, a salt-forming cation, a pr...
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WO/1986/000615A1 |
New 2-oxoazetidines having the formula (I) and (Ia) wherein R1 is a lower fluoralkyl group or a lower hydroxy alkyl group optionally protected, R2 is chlorine, bromine, iodine, fluorine, a group of formula (A) wherein n is 0, 1 or 2 and ...
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WO/1985/004878A1 |
Compounds of general formula (I), their pharmaceutically acceptable salts and in-vivo hydrolysable esters are antibacterial agents; in which R1 is optionally substituted phenyl or optionally substituted 5 or 6-membered heterocyclyl; R2 i...
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WO/1985/003937A1 |
The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are compounds of the formula (I), and the non-toxic pharmaceutically acceptable salts thereof, wherein D is ...
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WO/1985/003294A1 |
A process for the preparation of Penicillin V $(b)-sulfoxide by oxidation of Penicillin V in a two-phase liquid system comprising hydrogen peroxide aqueous solution and an organic solvent or mixture of organic solvents. The process is ch...
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WO/1985/002403A1 |
Penems of general formula (I), n is 1, 2 or 3; m is 1, 2 or 3; Z represents -COOH, -SO3H, or formula (III), R, R1, R2 and R3 independently represent hydrogen, lower alkyl, hydroxy lower alkyl, amino lower alkyl, carboxy lower alkyl, thio...
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WO/1984/002911A1 |
A compound of formula (I) or a salt thereof, wherein R1 and R3 are independently an in vivo hydrolysable group, or R1 and R3 together form an in vivo hydrolysable group, provided that R1 and R3 are not both C1-6 alkylcarbonyl; R7 is a hy...
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WO/1984/001776A1 |
A compound of formula (I): R1 is C1-6 alkyl, C3-6 cycloalkyl, C5-8 cyclo-alkenyl or an aromatic group; R2 is primary amino or an acid addition salt thereof, or a carboxy group or an ester thereof; R3 is hydrogen or a hydrocarbon moeity; ...
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WO/1984/000547A1 |
Compounds of formula (I), wherein, R1 represents hydrogen or methyl and R2 represents hydrogen or lower alkyl, lower alkenyl or cycloalkyl each of which may be unsubstituted or mono- or polysubstituted by amino, mono- or di-(lower)-alkyl...
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WO/1983/003968A1 |
The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are: (a) compounds of the formula: ADD-DHC BD (I), wherein ADD BD is a centrally acting drug species, and AD...
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