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7547777 |
Penam crystals and process for producing the same
The present invention provides novel 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxy
lic acid benzhydryl ester (TMPB)-acetone crystals for use in the production of...
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7514553 |
Process for producing penicillanic acid compound
A process for preparing a penicillanic acid compound of the formula (2) comprising reacting a halogenated penicillanic acid compound of the formula (1), (a) in the presence of a metal bismuth or...
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7459551 |
Method for preparing cyclic compounds
The present invention provides a method for preparing a β-lactam compound of the following Formula (3), which comprises the step of reacting a compound of the following Formula (1) with a trialkyl...
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7358356 |
Processes for preparation of organic compounds
The present invention provides a method for preparing an organic compound, which comprises a dehydration step of distilling off water from a polar organic solvent solution containing the organic...
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7273935 |
Process for the preparation of 3-methylcepham derivatives
A process for the preparation of 3-methylcepham-4-carboxylate of the formula (I).
wherein R 2 and R 3 may be same or different and represent hydrogen, halogen, amino, alkyl, phenacetamido,...
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7125986 |
Penicillanic acid derivative compounds and methods of making
Compounds 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...
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7112582 |
Bicyclic 6-alkylidene-penems as β-lactamase inhibitors
The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
wherein...
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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...
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7022691 |
Inhibitors of serine and metallo-β-lactamases
Compounds 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...
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7018997 |
Tricyclic 6-alkylidene-penems as β-lactamase inhibitors
The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
wherein...
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6936711 |
Process for preparation of penam derivatives from cepham derivatives
The present invention relates to a process for preparing 2α-methyl-2β-substituted methyl penam derivatives from cepham derivatives, more particularly the present invention provides a novel...
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6770759 |
Penicillanic acid derivative compounds and methods of making
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...
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6660855 |
Crystals of penicillin and process for the production thereof
The crystal of the invention is crystal of diphenylmethyl 2-methyl-2-triazolylmethylpenam-3-carboxylate which is stable substantially without decomposition or degradation of properties even when...
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6600035 |
6-(substituted methylene) penems and intermediates
Compounds of formula (I) in which: R 1 is hydrogen or an organic substituent group; R 2 is a fused bicyclic heterocyclic ring system of general formula (a) wherein R 4 and R 5 are independently...
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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),...
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6437119 |
Compounds formed from two or three antibiotics and their processes of preparation
Processes for preparing compounds having two or three antibiotic functionalities using quinolone derivatives, β-lactams and vancomycin and the like as the starting materials and chloride linking...
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6395726 |
3,6-disubstituted penam sulfone derivatives
Compounds are provided having the following formulae I and II: wherein n is 0 or 1 and when n=1, R is a 5 or 6 membered heterocyclic ring, hydroxy, halogen, oxo, carbamoyl, alkoxy, or...
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6339152 |
Process for producing exo-methylenepenam compounds
The present invention is directed to a process for preparing an exo-methylenepenam compound wherein a cephem compound is reduced with a metal having a standard oxidation-reduction potential of up...
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6274730 |
Process for producing halogenated β-lactam compound
A process for preparing halogenated β-lactam compounds, characterized in that a β-lactam amino compound of the formula (1) is reacted with nitrous acid or nitrite in a slurry dispersion state in...
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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...
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6255479 |
Process for the preparation of α-oxolactams
A method for preparing an α-oxolactam comprising, reacting a corresponding α-diazolactam with an oxygen donor, in the presence of a transition metal catalyst, to yield the corresponding...
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6160112 |
Procedure for the preparation of dioxopenicillanic acid derivatives
Procedure for the preparation of dioxopenicillanic acid derivatives and its salts pharmaceutically acceptable with general formula I, where, R is hydrogen, alkyl group containing 1 to 5 Carbon...
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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...
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6150350 |
Antimicrobial compositions
The invention relates to antimicrobial compositions comprising a combination of (1) a therapeutically effective amount of a compound of formula I ##STR1## with (2) a second ingredient selected from...
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6043356 |
Process for preparing β-lactam compound
The present invention provides a process for preparing an exo-methylenepenam compound represented by the general formula (5) characterized in that a β-lactam halide compound represented by the...
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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...
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5886203 |
Metalorganic compounds
A process is provided for the production of metalorganic compounds by reacting a Grignard reagent with a Group II, Group III or Group V metal halide in a tertiary alkyl amine solvent to form a...
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5821362 |
Method of desilylating silylether compounds
Method of desilylating a silylether compound by reacting a silylether compound of the general formula (I): ##STR1## or a salt thereof with an amine hydrogen fluoride salt or a pyridine hydrogen...
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5801242 |
Process for making quinolonyl lactam antimicrobials and novel intermediate compounds
The present invention provides processes for making compounds of the structure (Q--L 1 )--L--(L 2 --B) wherein (I) Q is a quinolone moiety; (II) B is a lactam moiety; and (III) L, L 1 ,...
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5763603 |
Crystalline tazobactam, and its production and use
Crystalline sodium 2α-methyl-2β-(1,2,3-triazol-1-yl) -methylpenam-3α-carboxylate-1,1-dioxide monohydrate (crystalline tazobactam sodium monohydrate) obtainable by adding to a concentrated...
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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...
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5703231 |
Process for making antimicrobial compounds
The present invention provides a process for making a compound having a structure according to Formula (I) ##STR1## wherein A 1 , A 2 and A 3 are independently carbon or nitrogen and R 1 , R 3 ,...
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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...
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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...
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5681951 |
Metal catalyzed displacement process
A process for preparing a compound of formula (I'): ##STR1## comprising reacting a compound of formula (II'): ##STR2## with a compound of formula (III'): A'SH ...
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5644053 |
Penam derivatives
The present invention discloses compounds having the formula ##STR1## wherein one of R 1 and R 2 is --COR 4 , --CN, --CH 2 R 5 , halogen, --CHCHR 6 or Q and the other is hydrogen or lower...
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5625059 |
Process for the manufacture of 4-acetoxy-3-hydroxyethyl-azetidinone
The invention relates to a novel process for the manufacture of 4-acetoxy-3-hydroxyethyl-azetidinone of the formula ##STR1## especially 4(R)-acetoxy-3(R)-(1'(R)-hydroxyethyl)-2-azetidinone, from...
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5621096 |
Process for preparing penems
The invention provides a process for the preparation of the compound of formula I ##STR1## wherein R is carboxy group or a carboxylate anion, by enzymatic hydrolysis with a lipase or an acylase in...
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5599925 |
Penam derivatives
A penam derivative of the general formula ##STR1## wherein R 1 means hydrogen, halogen, amino or protected amino; R 2 means hydrogen, halogen, lower alkoxy, lower acyl, lower alkyl, hydroxy- or...
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5541317 |
Azetidinone compounds useful in the preparation of carbapenem antibiotics and process for preparing carbapenem and penem compounds
Compounds of formula (I): ##STR1## wherein: R 1 is hydrogen or a hydroxy-protecting group; R 2 is alkyl, alkoxy, halogen, optionally substituted phenyl or optionally substituted phenoxy; R 3 is...
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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...
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5539102 |
Production method for sulfamide
The method for producing a sulfamide according to the present invention includes the step of reacting an alcohol and an oxycarbonylsulfamide compound in the presence of a trivalent phosphorus...
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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...
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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...
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5488106 |
Process for preparing 6-[(isoxazolinyl)methyl]penicillanic acid 1,1-dioxide compounds
The invention provides a novel class of 6-(isoxazolinyl)methyl penicillanic acid 1,1-dioxide compounds having the formula: ##STR1## wherein M, X, R 2 , R 3 , R 4 and R 5 are described in the...
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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...
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5474993 |
Lactam inhibitors of cholesterol esterase
The present invention is related to compounds which inhibit pancreatic cholesterol esterase. The compounds have the formula: ##STR1## wherein R 1 is H or C 1 -6 alkyl; R 2 is H or C 1 -6...
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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...
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5457193 |
Hydroxy protecting group removal in penems
The present invention relates the removal of t-butyldimethylsilyl protecting groups in the preparation of penems which are useful antibiotics. The invention provides a process for preparing a...
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5442058 |
Conversion of penicillins and cephalosporins to 1-(S)-sulfoxides
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...
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