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7094431 Method of healing skin wounds in mammals and a composition therefor  
This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or...
7091197 Beta-lactamase inhibitor prodrug  
Prodrugs of 6-β-hydroxymethylpenicillanic acid sulfone having the structure wherein R is H or methyl, and solvates thereof, are disclosed. Also disclosed are pharmaceutical compositions...
6495539 B-lactam-like chaperone inhibitors  
Compounds of the formula and the salts, esters and amides thereof wherein Z is S, SO, SO 2 or O; each of R 1 , R 2 and R 3 is independently H or substituted or unsubstituted alkyl (1-10C),...
6436398 2 β-substituted-6-alkylidene penicillanic acid derivatives as β-lactamase inhibitors  
Compound of formula I: wherein R 1 , R 2 , R 3 , R 4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting...
6271222 Penem antibacterial compounds, compositions and methods of treatment  
The present invention relates to penem antibacterial agents in which the releaseable liphophilic aromatic side-chain, tethered to the carbapenem nucleus via a methylene linker, necessary for...
6156745 2β-substituted-6-alkylidene penicillanic acid derivatives as β-lactamase inhibitors  
Compounds of formula I: ##STR1## wherein R 1 , R 2 , R 3 , R 4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting...
5994340 Azetidinone derivatives as β-lactamase inhibitors  
New 2-oxo-1-azetidine sulfonic acid derivatives with an aminoalkyl substituted "anti" (E-isomer) oxyimino group in the acylamino substituent at the 3 position of the monobactam ring. These...
5885981 Antibacterial penem esters derivatives  
Antibiotic penem compounds are represented by the following formula: ##STR1## wherein R represents a group of the general formula: ##STR2## in which R 1 is a hydrogen atom or linear or branched C...
5747483 Penem derivatives, their preparation and pharmaceutical compositions containing them  
Penem derivatives of general formula (I), below, and pharmaceutically acceptable salts thereof are disclosed. ##STR1## wherein: R 1 is H, C 1 -C 6 alkoxy, C 3 -C 7 cycloalkyl, or an optionally...
5703068 Penem compounds  
Antibiotic penem compounds are represented by the following formula: ##STR1## wherein R represents a group of the following formula: ##STR2## in which R 1 is a linear or branched, C 1 -C 6 alkyl...
5686441 Penam sulfones as β-lactamase inhibitors  
Novel 3-(substituted)-3-methyl-4-thia-1-azabicyclo 3.2.0!heptane-2-carboxylate, 4,4-dioxides which are of value for use in combination with β-lactam antibiotics to increase the effectiveness of...
5650394 Use of urinastatin-like compounds to prevent premature delivery  
The present invention provides a method of diagnosing and treating a pregnant female at risk for impending preterm delivery. The method comprises the step of diagnosing imminent preterm delivery by...
5538962 Antibiotic penem compounds  
The present invention provides a compound of the formula (I) ##STR1## wherein: R 1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R 2 is hydrogen or C 1 -4 alkyl; Z is carboxy, sufonic...
5506225 Antibacterial penem compounds  
Antibiotic penem compounds are represented by the following formula: ##STR1## wherein R represents a physiological-hydrolyzable, ester-forming group. The physiologically hydrolyzable, ester-forming...
5492903 Crystalline esters of (+)-(5R, 6S)-6-[(R)-1-hydroxyethyl]-3-(3-pyridyl)-7-oxo-4-thia-1-azabicyclo[3.2.0]h e  
Crystalline acetoxymethyl and pivaloyloxymethyl esters of (+)-(5R, 6S)-6-[(R)-1-hydroxyethyl]-3-(3-pyridyl)-7-oxo-4-thia-1-azab icyclo-[3.2.0] hept-2-ene-carboxylic acid can be obtained by adding a...
5480880 Penem derivatives  
The invention provides compounds of the general formula I ##STR1## wherein R 1 is a hydrogen atom, a negative charge or an ester residue; R is: a) --(CH 2 ) n --A--CO 2 H, --(CH 2 )n--A--SO 3...
5464616 6β-substituted penicillanic acids as beta-lactamase inhibitors  
A 6β-substituted penicillanic acid of the formula XII: ##STR1## or a pharmaceutically acceptable salt or ester thereof, wherein A and B are each hydrogen wherein the carbon atoms to which A and...
5200403 Inhibition of βlactamase with 6 β-(substituted methyl)-penicillanic acid derivatives  
Compounds of the formula I ##STR1## wherein R' is a free or esterified carboxy group or a carboxylate anion and R 2 is an organic group have beta-lactamase inhibition activity. A process for the...
5126335 Penicillins containing an acrylamide side chain  
Compounds of formula (I) and pharmaceutically acceptable salts and in-vivo hydrolysable esters thereof: ##STR1## wherein X is hydrogen or a group NHR 1 , wherein R 1 is hydrogen or an amino...
5116832 Penem derivatives production and use thereof  
Novel penem compounds of the formula, ##STR1## wherein R is hydrogen or allyl, and A is an aliphatic 5- or 6-membered heterocyclic group having one or two oxygens in the ring and their...
5089489 6-substituted penem esters as anti-inflammatory and anti-degenerative agents  
6-substituted penem esters of formula (I): ##STR1## wherein R 1 is halogen or a C 1 -C 4 alkyl, C 1 -C 4 alkoxy, phenyl, phenoxy, benzyl or sulphonyloxy group; R 2 is a C 1 -C 4 alkyl,...
5051416 Oral antibacterial method  
A method is provided for treating a warm-blooded animal having a susceptible bacterial infection which comprises administering orally to said animal a non-toxic, antibacterially effective amount of...
5036063 Penem derivatives  
Penem derivatives of the formula ##STR1## having R 1 equal to 3-oxocyclobutyl and R 2 equal to H or an ester-forming group, pharmaceutical preparations active against bacterial infections and...
5015473 6-(substituted)methylenepenicillanic and 6-(substituted)hydroxymethylpenicillanic acids and derivatives thereof  
Beta-lactamase inhibiting compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition or carboxylate salt thereof; where n is zero, 1 or 2; X 3 is H or Br, R 1 is H, the...
5004738 1,1-dioxopenicillanoyl oxymethyl D-6-(α-(methyleneamino) phenylacetamido)-penicillanate and a process for the preparation thereof  
A pharmaceutical compound which comprises reacting the sodium penicillanic acid 1,1-dioxides with chloroiodomethane in the presence of a solvent to produce chloromethylpenicillanate 1,1-dioxides,...
4997829 Penem compounds, and use thereof  
A penem compound represented by the general formula: ##STR1## (wherein R denotes hydrogen or allyl group, A denotes oxygen atom or methylene group and B denotes methylene, ethylene or carbonyl...
4994260 Pharmaceutical mixture  
A pharmaceutical mixture with controlled release of actice substance which includes masking of bad taste and stability increasing of active substance characterized in that an encapsulated active...
4965260 Bicyclic beta-lactam carboxylic acids  
Compounds of the formula ##STR1## in which R 1 is lower alkyl substituted by hydroxy or by protected hydroxy, R 2 represents carboxy or functionally modified carboxy, R 3 is hydrogen, amino,...
4958020 Process for producing β-lactamase inhibitor  
A process for producing the compound [2S-(2α,3β,5α)]-3-methyl-7-oxo-3-(1H-1,2,3-triazol-1-yl-m ethyl)-4-thia-1-azabicyclo[3 2 0]-heptane-2-carboxylic acid, (4-nitrophenyl)methyl ester,...
4954489 Penicillins having a substituted acrylamido side chain  
Compounds of formula (I) and their salts and esters: ##STR1## wherein X is hydrogen or a group NHR 1 , wherein R 1 is hydrogen or an amino protecting group, and R is optionally substituted C 5 -8...
4952577 Methoxymethyl penem compounds  
A substantially (≥95%) optically pure (5R,6S,1'R) penem of formula ##STR1## and the pharmaceutically acceptable salts and the ester prodrugs thereof, are endowed with antibacterial activity.
4931434 Penem compounds  
Compounds of the general formula (II): ##STR1## in which N + denotes an unsubstituted or substituted nitrogen-containing heterocyclyl ring bonded to the remainder of the molecule through a ring...
4918067 Heterocyclic substituted penicillin antibiotics  
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt or in-vivo hydrolysable ester thereof: ##STR1## wherein R 1 is a 5 or 6 membered sulphur and/or...
4891369 2β-Substituted-methylpenicillanic acid derivatives, and salts and esters thereof  
Disclosed are 2β-substituted-methylpenicillanic acid compounds of the formula ##STR1## wherein n is 0, 1 or 2; and ##STR2## is monocyclic or bicyclic heterocyclic ring group which has 2 to 4...
4886793 Penem derivatives  
There are provided compounds of formula I: ##STR1## wherein R 1 is hydrogen or a C 1 -C 4 alkyl group either unsubstituted or substituted by one or more substituents chosen from a free or...
4882325 Crystalline 1,1-dioxopenicillanoyloxymethyl 6-(d-amino-phenylacetamido)penicillanate napsylate and method of using the same  
Crystalline 1,1-dioxopenicillanoyloxymethyl 6-(D-α-amino-α-phenylacetamido)penicillanate napsylate. The product may be prepared by reacting 1,1-dioxopenicillanoyloxymethyl...
4861768 2 β-substituted thiomethylpenicillin derivatives and their preparation and use  
Disclosed is a penicillin derivative of the formula: ##STR1## wherein n is an integer of 0, 1 or 2; Y is a cyano group, a lower acyl group, a mono- or di-lower alkylthiocarbamoyl group, ##STR2##...
4849419 7-oxo-4-thia-azabicyclo[3,2,0]hept-2-ene derivatives  
A compound of formula I ##STR1## with R 1 being an alkyl group substituted by one or more substituents and esters thereof at the 2-carboxy group or at the 8-hydroxy group or both; and salts...
4847266 Method for preparing 6-β-halopenicillanic acids  
The present invention relates to a new and improved method for the preparation of a compound of the formula I ##STR1## in which R stands for halogen, giving rise to high yields of substantially...
4847247 Penicillin derivatives as anti-inflammatory and antidegenerative agents  
Derivatives of Penicillin, their sulfoxides and sulfones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.
4840944 Antibacterial beta-lactams, pharmaceuticals thereof and methods of using them  
The present invention relates to hitherto unknown compounds of the general formula I: ##STR1## in which R 1 stands for a phenyl, 4-hydroxyphenyl, 1,4-cyclohexadienyl or a 3-thienyl group; R 2 ...
4831025 Crystalline penicillin derivative tosylate hydrates  
The present invention relates to a crystalline hydrate of a salt of the antimicrobial agent 1,1-dioxopenicillanoyloxymethyl 6-(D-α-amino-α-phenylacetamido)penicillanate with p-toluenesulfonic...
4826832 Penen compounds  
Compounds of the formula ##STR1## in which R 1 represents lower alkyl substituted by hydroxy or by protected hydroxy, R 2 represents carboxy or functionally modified carboxy, and R 3 represents...
4798828 Heterocyclic-methylene-penems  
Compounds of the general formula I: ##STR1## and their pharmaceutically acceptable salts and in vivo hydrolyzable esters, in which one of R 1 and R 2 denotes hydrogen, the other of R 1 and...
4797396 β-Lactam derivatives as anti-inflammatory and antidegenerative agents  
β-Lactam derivatives and analogs are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.
4795748 Antibacterial 7-oxo-4-thia-1-azabicyclo[3,2,0]hept-2-ene derivatives  
A compound of the formula I ##STR1## in which R 1 represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms, the --CONHR 1 group being present at the 3- or 4-position on the...
4794109 6-hydroxy-lower alkylpenem compounds, pharmaceutical preparations that contain these compounds, and the use of the latter  
2-Heterocyclyl-lower alkyl-6-hydroxy-lower alkyl-2-penem compounds of the formula ##STR1## in which R 1 represents lower alkyl substituted by hydroxy or protected hydroxy, R 2 represents carboxy...
4774238 Heterocyclic-methylene-penems  
(5R) (Z)-6-(1-methyl,1,2,3-triazol-4-yl-methylene)-penem-3-carbox ylic acid and its salts are provided in analytically pure crystalline form, and the salts in hydrated form, for example (5R) sodium...
4772597 2-azacycloalkylthiopenem derivatives  
Certain 2-azacycloalkylthio-2-penem-3-carboxylic acid compounds are useful as antibacterials for treating mammals and have the formula ##STR1## or a pharmaceutically acceptable salt thereof,...
4762827 (5R,6S,8R )-6-(1-hydroxyethyl)-2-(3R-pyrrolidin-2-one-3-yl)thiopenem-3-carboxylic acid  
There is disclosed the compound (5R,6S,8R)-6-(1-hydroxyethyl)-2-(3R-pyrrolidin-2-one-3-yl)th iopenem-3-carb oxylic acid, and pharmaceutically acceptable salts and esters as well as compositions...
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