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RE40794 |
Crystalline forms of carbapenem antibiotics and methods of preparation
A process for preparing a crystalline, carbapenem monosodium salt of formula IIa:
characterized by the steps a) adding about 10 to 30% of an organic solvent to an aqueous solution of the...
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7534782 |
Crystal of 1-methylcarbapenem solvate
A 1-methylcarbapenem compound ethanolate of the formula (I-1) in the crystalline form that shows main peaks at interplanar spacings d=7.60, 6.69, 6.33, 6.14, 5.15, 4.58 and 4.48 in the X-ray powder...
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7524952 |
Process for producing carbapenem compound for oral administration
The present invention provides a process for efficiently producing a 1β-methylcarbapenem compound for oral administration. The process, which is for producing a 1β-methylcarbapenem compound...
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7507814 |
Process for preparation of imipenem
The invention provides a novel compound of Formula II which is useful in the preparation of imipenem monohydrate of Formula I, wherein R1 is a p-nitrobenzyl or p-methoxybenzyl group; and R2 and R3...
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7479362 |
UV decomposable molecules and a photopatternable monomolecular film formed therefrom
Aspects of the invention provide a method of controlling the solid-state property of the solid-phase surface or controlling forming reactive region. The method can be attained by using a device for...
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7462712 |
Process for the preparation of imipenem
The present invention relates to an improved process for the preparation of imipenem comprising reacting a bicyclo ketone precursor of the Formula II,
wherein R is a protecting group, with a...
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7381724 |
Optically active 5H-pyrrolo[3,4-b]pyrazine derivative, its preparation and pharmaceutical compositions containing same
Dextrorotatory isomer of 6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonylox
y]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine, its preparation and pharmaceutical compositions containing it...
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7332600 |
Process for the preparation of crystalline imipenem
The present invention relates to a cost effective and industrially advantageous process for the preparation of imipenem of high purity, which comprises dissolving crude imipenerm in warm water to...
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7241885 |
Process for the isolation of crystalline imipenem
The present invention relates to a cost effective and industrially advantageous process for the preparation of imipenem of high purity comprising the steps of treating an aqueous solution...
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7163936 |
β-lactam compounds and process for producing the same
1. A β-lactam compound of the formula [1];
wherein R 1 is a lower alkyl, a lower alkyl substituted by a hydroxy; R 2 is a hydrogen, a lower alkyl; X is O, S, NH; m and n are 0 to 4, Y 1 is...
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7084268 |
Carbapenem compound crystals and interjection preparations
The present invention provides carbapenem hydrochloride trihydrate crystals, which are chemically stable, easily purified and useful as antimicrobial agents, a process for producing them, and a...
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7071330 |
Process for carbapenem synthesis
A process for synthesizing a compound represented by formula I:
or a pharmaceutically acceptable salt thereof, wherein deprotection is conducted using a prereduced metal catalyst is disclosed.
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7041836 |
Antibiotic compounds
The present invention relates to carbapenems and provides a compound of the formula (I):
or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein:
R 1 is...
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7041660 |
Crystalline 1-methylcarbapenem derivatives
This invention provides crystalline forms of a 1-methylcarbapenem derivative of formula (I-1), (I-2) or (I-3)
The crystalline forms of the 1-methylcarbapenem derivative exhibit excellent...
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7034150 |
Processes for the preparation of carbapenem-type antibacterial agents
A process for the preparation of a carbapenem antibacterial compound of the following formula (4) having a 1-alkylpyrrolidine structure or a salt thereof, a useful synthetic intermediate of the...
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7022841 |
Process for making carbapenem compounds
The present invention relates to a process for reducing the levels of organic solvents to pharmaceutically acceptable levels in thermally unstable crystalline carbapenem solids represented by...
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7001897 |
1-methylcarbapenem derivatives
A 1-methylcarbapenem compound represented by the formula (I):
having antibacterial activity, pharmacologically acceptable esters or salts thereof and pharmaceutical compositions (particularly...
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6649756 |
PROCESS IMPROVEMENT IN THE PREPARATION OF (4R, 5S, 6S)-3-&lsqb &lsqb (2R,3R)-2-&lsqb &lsqb &lsqb (S)-2-AMINO-3-METHYL-1-OXOBUTYL&rsqb AMINO&rsqb METHYL&rsqb TETRAHYDRO-3-FURANYL&rsqb THIO&rsqb -6-&lsqb (R)-1-HYDROXYETHYL&rsqb -4-METHYL-7-OXO-1-AZABICYCLO&lsqb 3.2.0&rsqb HEPT-2-ENE-2-CARBOXYLIC ACID
The invention is a process improvement for producing the carbapenem antibacterial agent (4R, 5S,...
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6642377 |
Process for the preparation of basic antibiotic-inorganic acid addition salts and intermediate oxalates
A production process which comprises subjecting a basic antibiotic.oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid: wherein the ring A means the basic...
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6589952 |
Imidazo&lsqb 1,2-a&rsqb pyrazines for the treatment of neurological disorders
Provided herein are novel imidazo[1,2-a]pyrazines of Formula I: wherein: X is CHR 5 , NR 5 , O, S, S(O) n or a single bond, wherein n is equal to 0, 1 or 2; D is aryl or heteroaryl attached...
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6548492 |
Process for formulation of carbapenem antibiotic compositions
A novel process for preparing a stabilized, lyophilized carbapenem, antibiotic formulation suitable for intravenous administration to patients in need thereof, wherein the active ingredient is of...
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6531594 |
Process for producing 1H-3-aminopyrrolidine and derivatives thereof
A process for producing 1H-3-aminopyrrolidine and derivatives thereof is disclosed. The process is especially useful for producing optically active 1H-3-aminopyrrolidine and derivatives thereof and...
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6504027 |
Decarboxylation process for synthesizing carbapenem antibiotics
A process for the direct crystallization of a compound of the formula I: or a pharmaceutically acceptable salt thereof, is disclosed, wherein R 1 and R 2 represent H, C 1-10 alkyl, aryl or...
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6486150 |
Process for formulation of antibiotic compounds
The present invention involves a process for preparing a stable final formulation product of a compound of formula I, or its pharmaceutically acceptable salt, hydrate or solvate by incorporating...
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6482818 |
C-2 S/O-and S/N formaldehyde acetal derivatives of carbapenem-3-carboxylic acids and their use as antibiotics and β-lactamase inhibitors
The compounds of the general formula I wherein R 1 denotes hydrogen, hydroxymethyl or 1-hydroxyethyl, R 2 denotes hydrogen or methyl and R 3 denotes a pharmaceutically acceptable group which...
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6479478 |
Carbapenem compounds
It is provided carbapenem compounds represented by the following formula (I): wherein R is hydrogen atom, or substituted or unsubstituted lower alkyl group; and, n is an integer of 1 or 2, or a...
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6444673 |
Optically active 5H-pyrrolo&lsqb 3,4-b&rsqb pyrazine derivative, its preparation and pharmaceutical compositions containing it
Dextrorotatory isomer of 6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonylox
y]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine, its preparation and pharmaceutical compositions containing it...
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6436921 |
Carbapenem derivatives and a preparation method thereof
The present invention relates to carbapenem derivatives of Formula I, wherein X is carbonyl or sulfonyl, and a preparation method thereof. The carbapenem derivatives of the invention have excellent...
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6410525 |
Carbapenem derivatives, utilization thereof and intermediate compounds of the same
A carbapenem compound of the formula (I) wherein R 1 is a group hydrolyzable in the living body, R 2 and R 3 are the same or different and each is a lower alkyl, R is a group of the formula...
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6342494 |
Carbapenem compounds, use thereof, and intermediate compounds of the same
A carbapenem compound of the formula (I) wherein R 1 is a group hydrolyzable in the body, R 2 is selected from the group consisting of aryl groups optionally substituted by 1-3 alkyl groups...
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6297231 |
Stabilized carbapenem antibiotic compositions and method of making
The present invention relates to a novel stabilized form of carbapenem antibiotics of formula II: ##STR1## compositions and methods thereof wherein the antibiotics and compositions are stabilized...
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6265396 |
β-lactam compounds and process for preparing the same
A β-lactam compound of the formula: ##STR1## wherein R 1 is lower alkyl or OH-substituted lower alkyl, R 2 is H or lower alkyl, X is O, S or NH, n is 1 to 3, R 3 is --C(R a )NH (R a is H,...
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6251891 |
Carbapenem derivatives
A compound represented by the general formula ##STR1## wherein R 1 either represents a hydrogen atom or a lower alkyl group, R 2 represents a hydrogen atom, an ester residue, an alkali metal or...
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6180783 |
Stabilized carbapenem intermediates and improved process for carbapenem synthesis
A stabilized carbapenem intermediate compound represented by the formula 1: ##STR1## or a salt thereof is disclosed, wherein P represents a carboxyl protecting group and X represents a charge...
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6180622 |
Imidazo[5,1-b]thiazol-3-yl carbapenem antimicrobials
Compounds of formula (I) and compounds of formula (II) which have potent antimicrobial activity against a wide range of bacteria including Gram-positive bacteria and Gram-negative bacteria as well...
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6174877 |
Carbapenem compound, their production and use
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6111098 |
Crystal of pyrrolidylthiocarbapenem derivative, lyophilized preparation containing said crystal, and process for producing the same
The present invention provides a crystal of (1R,5S,6S)-6-[(1R)-1-hydroxyethyl]-2-[(3S,5S)-5-sulfamoylami
nomethyl-1-pyr rolidin-3-yl]thio-1-methyl-1-carba-2-penem-3-carboxylic acid represented by...
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6090802 |
1- Methylcarbapenem derivatives
A 1-methylcarbapenem compound represented by the following formula (I): ##STR1## wherein R 1 represents hydrogen or C 1 -C 4 alkyl; R 2 represents hydrogen or an ester residue; and A represents...
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6051569 |
1'S, 5R, 6R-carbapenem derivatives and antimicrobial agents comprising the same
A carbapenem derivative represented by the following formula (I), ##STR1## wherein R 1 represents a hydrogen atom, a substituted or unsubstituted aryl group, or a substituted or unsubstituted...
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6037341 |
Carbapenem derivatives
Compounds having potent antimicrobial effects over Gram-positive bacteria and Gram-negative bacteria, a high stability to β-lactamases and DHP-I and a high safety for the human body and a process...
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5998612 |
Antibiotic synthesis
A method of preparing intermediates for carbapenem antibiotics characterized by treating a N-deprotected acetoxy conpound of the formula: ##STR1## in the presence of a Lewis acid or a silylating...
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5977097 |
1-methylcarbapenem derivatives
A 1-methylcarbapenem compound represented by the following formula: ##STR1## [wherein R 1 represents a hydrogen atom or a lower alkyl group, R 2 represents a hydrogen atom or a lower alkyl group,...
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5952323 |
Carbapenem antibiotic
A pharmaceutical composition is disclosed which contains a compound of formula I: ##STR1## or a pharmaceutically acceptable salt, prodrug or hydrate thereof, in the stabilized form and/or in...
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5886172 |
Carbapenem-3-carboxylic acid ester derivatives
Disclosed are carbapenem-3-carboxylic acid ester derivatives of formula (I), wherein R 1 is a hydrogen atom or a lower alkyl group, R 2 is an alkyl group which may be substituted by a cycloalkyl...
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5872250 |
Process for synthesizing carbapenem antibiotics
A process for synthesizing a compound of the formula I: ##STR1## or a pharmaceutically acceptable salt or ester thereof, wherein each P independently represents H or a protecting group, and R 1 ...
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5866564 |
Carbapenem derivatives, their preparation and their use as antibiotics
Compound of formula (I): ##STR1## wherein R 1 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl or --C(NH)R 0 where R 0 is hydrogen or C 1 -C 6 alkyl; A is ##STR2## R...
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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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5750686 |
Carbapenem compounds and process for producing the same
A novel β-lactam compound of the formula 1!: ##STR1## or a pharmaceutically acceptable salt thereof, which shows an excellent antibacterial activity against Gram-positive bacteria, especially...
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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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5679790 |
2- 1-(1,3-thiazolin-2-yl)azetidin-3-yl!thio-carbapenem derivatives
Novel carbapenem compounds, (1R,5S,6S)-2- 1-(1,3-thiazolin-2-yl)azetidin-3-yl!thio-6- (R)-1-hydroxyeth yl!-1-methyl-carbapen-2-em-3-carboxyic acid derivatives. These carbapenem compounds are...
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