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WO/1990/011284A1 |
Antibacterial compounds of formula (I), wherein n is O or 1, R is hydrogen or a radical forming an ester hydrolyzable under physiological conditions, and R1 is hydrogen or methyl; the pharmaceutically-acceptable cationic salts thereof wh...
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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/1990/000170A1 |
New antibacterial 6-amido-1-methylcarbapenems and process for their synthesis involving new azetidinone intermediates.
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WO/1985/001502A1 |
Compounds represented by formula (I), (wherein X represents a lower alkenylene or lower alkylene group optionally containing a hydroxy group, Y represents (1) a lower alkyl group, (2) a C3-8 cycloalkyl group, (3) a lower alkenyl group, (...
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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/1983/002614A1 |
5,6-cis-Carbapenem-3-carboxylic acid derivatives represented by the following general formula:$(8,)$(wherein R1 represents a hydrocarbyl group or a heterocyclic group, R2 represents a hydrogen atom or a hydroxyl-protecting group, and n r...
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WO/1983/000867A1 |
5,6-cis-Carbapenem-3-carboxylic acid derivatives represented by the following formula:$(8,)$(wherein R1 represents a hydrocarbyl group or a heterocyclic group, R2 represents a hydrogen atom or a hydroxy-protecting group, and n represents...
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WO/1982/003218A1 |
Carba-2-penem compounds represented by the following general formula: (FORMULA) (wherein R1 represents an alkyl group, an aryl group, an alkylthio group, an arylthio group or an acylaminoalkylthio group, R2 and R3 each represent an alkox...
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WO/1982/001875A1 |
New (Beta)-lactams of the general structure: (FORMULA) wherein R represents H or an acyl moiety known from the penicillin or cephalosporin art, R' is hydrogen, lower alkoxy, lower alkoxyalkyl, lower alkyl, phenylthio or lower alkylmercap...
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WO/1982/001705A1 |
4-substituted-2-oxoazetidine derivatives represented by the following general formula (I): (FORMULA) (wherein R1 represents a hydrogen atom, an alkyl group optionally having a hydroxy group, a phthalimido group or a halogen atom, R2 repr...
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WO/1982/000291A1 |
Carba-2-penem compounds represented by the following general formula (I): (FORMULA) (wherein R1 represents an alkyl group, an aryl group, an alkylthio group, an arylthio group, or an acylaminoalkylthio group, R2 and R3 each represents an...
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JP7430256B2 |
Provided are a continuous post-treatment method and device for a penem compound. The method includes the following steps: S1, performing continuous extraction on a reaction crude product of a penem compound, to obtain an extraction heavy...
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JP7326164B2 |
The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such ...
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JP7309607B2 |
The disclosure is directed to new crystalline tebipenem pivoxil salt forms, including a crystalline tebipenem pivoxil ethane sulfonate salt form (Form A), a crystalline tebipenem pivoxil ketoglutarate salt form (Form A), tebipenem pivoxi...
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JP2023504485A |
The present invention relates to probes for the detection of β-lactamase-type enzymatic activity. In particular, the present invention relates to novel fluorogenic substrates and detection methods using such substrates for detecting the...
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JP7213173B2 |
This invention relates to carbapenem compounds of the following formula:wherein A, Z, X, R1, and R4 are as described herein, as well as stereoisomers, pharmaceutically acceptable salts or N-oxides thereof, which may be useful for the tre...
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JP6738918B2 |
The present invention provides novel derivative of β-lactam antibiotics, such as meropenem. The inventive compounds include compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, ta...
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JP6477728B2 |
This invention relates to a novel doripenem crystal, a solvate thereof, and a preparation method thereof and, more specifically, to a novel doripenem anhydride crystal, a method of preparing the doripenem anhydride crystal using various ...
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JP6321735B2 |
Provided is a crystalline form E of ertapenem sodium. Further provided is a method for preparing a crystalline form E of ertapenem sodium, characterized by using an aqueous ertapenem sodium solution at a low concentration as a raw materi...
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JP2018058865A |
To provide a novel doripenem anhydride crystal with improved solubility and stability of the doripenem.A doripenem anhydride crystal has peaks at diffraction angles of 11.00±0.2, 12.55±0.2, 15.05±0.2, 16.18±0.2, 17.81±0.2, 18.83±0....
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JP6227147B2 |
A polymer containing a carboxyl group, a preparation method and an application thereof, a supported catalyst and a preparation method thereof and preparation methods of a penem antibiotic intermediate are disclosed. The polymer is prepar...
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JP6192739B2 |
Provided is a process for the preparation of meropenem trihydrate in high purity and high yield, including using a dry methanol solvate of meropenem, which can remarkably reduce the amount of residual solvents in the resulting product, t...
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JP6085339B2 |
Intermediates of Ertapenem of formula 2a wherein Np represents (I) or (II), and P 1 and P 2 represent carboxyl protecting groups, and their preparation methods. Compound 2a prepared by the present methods in solid form is amorphous. The ...
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JP2016517435A |
The present invention provides the new derivative of beta* lactam antibiotics, such as Meropenem . The compound concerning the present invention contains the compound of formula (I), its salt permitted pharmacologically, solvent Hydrate ...
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JP5922110B2 |
The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The inventio...
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JP5920601B2 |
Chromogenic or fluorescent carbapenems according to formula I, wherein Ar is a mono or disubstituted carbocyclic aromatic group or an optionally mono or disubstituted heterocyclic aromatic group, are useful compounds for the detection of...
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JP2016501259A |
The present invention relates to a method for producing dripenem monohydrate, and more specifically, a step of reacting dripenem-PNB with zinc powder in a mixed solvent composed of an organic solvent and an aqueous phosphate solution to ...
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JP2015533142A |
The present invention relates to the production of compounds, in particular compounds and salts thereof that can be used as intermediates for the production of antibiotics, preferably carbapenem antibiotics, more preferably ertapenem.
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JP5656881B2 |
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JP5646328B2 |
The present disclosure provides engineered ketoreductase enzymes having improved properties as compared to a naturally occurring wild-type ketoreductase enzyme. Also provided are polynucleotides encoding the engineered ketoreductase enzy...
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JP5408876B2 |
The present invention provides ²-methyl carbapenem compounds and/or pharmaceutical compositions thereof. The present also provides carbapenem compounds and/or pharmaceutical compositions thereof for use in methods of treatment for bacte...
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JP2014501265A |
Provided is a crystalline form E of ertapenem sodium. Further provided is a method for preparing a crystalline form E of ertapenem sodium, characterized by using an aqueous ertapenem sodium solution at a low concentration as a raw materi...
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JP5373390B2 |
The present invention has its object to provide an easy process for producing (4R,5S,6S)-3-[[(3S,5S)-5-(dimethylaminocarbonyl)-3-pyrrolid inyl]thio]-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicy clo[3.2.0]hept-2-ene-2-carboxylic acid,...
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JP5328170B2 |
To provide an intermediate synthesizing step using non or a reduced amount of a halogen-containing solvent and/or avoiding or decreasing extremely high temperatures and/or low temperatures, in a method for synthesizing a pyrrolidylthioca...
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JP5285130B2 |
This invention described an ICE inhibitor prodrug (I) having good bioavailability. Compound of formula (I) is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerativ...
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JP5255983B2 |
A pharmaceutical composition is disclosed which contains a compound of formula (I) or a pharmaceutically acceptable salt, prodrug or hydrate thereof, in the stabilized form and/or in combination with a carbon dioxide source.
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JP5247449B2 |
The present invention provides a novel process for the preparation of the meropenem trihydrate of formula (I).
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JP2012525339A |
Intermediates of Ertapenem of formula 2a wherein Np represents (I) or (II), and P 1 and P 2 represent carboxyl protecting groups, and their preparation methods. Compound 2a prepared by the present methods in solid form is amorphous. The ...
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JP5019389B2 |
An object of the present invention is to provide a carbapenem synthetic intermediate which is advantageous in an industrial process. There are provided a process for producing Compound (I), or a pharmaceutically acceptable salt, or a sol...
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JP5013795B2 |
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JP2012153686A |
To provide a method for preparing an antibiotic compound.The method for preparing a carbapenem antibiotic compound solution and the application thereof can be used for vein injection or intramuscular injection.
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JP2012149079A |
To provide new compounds which show broad and excellent antimicrobial activities against Gram positive and Gram negative bacteria, including various resistant bacteria.The compounds are represented by formula (I), wherein R1 represents a...
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JP4890719B2 |
This invention described an ICE inhibitor prodrug (I) having good bioavailability. Compound of formula (I) is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerativ...
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JP4854899B2 |
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 formula (II). The process entails compoun...
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JP2011241212A |
To provide a process for improving carbapenem antibiotics using carbapenem intermediates, and to provide a method for retrieving carbapenems in the process.The method for retrieving products (carbapenems) from a carbapenem crystal mother...
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JP4801049B2 |
A 2-arylmethylazetidine carbapenem derivative of formula (I) or a pharmaceutically acceptable salt thereof exhibits a wide spectrum of antibacterial activities against Gram-positive and Gram-negative bacteria and excellent antibacterial ...
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JPWO2009093638A1 |
(R in the formula1Is a lower alkyl group, etc., R2Is a hydrogen atom, etc., R3Is a carboxyl-protecting group, L is a hydroxyl-active ester, and R is.4Is a hydrogen atom, etc., R5Indicates a hydrogen atom or the like. ) A carbapenem repre...
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JPWO2009075323A1 |
Has desirable properties as a drug substance (4R, 5S, 6S) -6-[(1R) -1-hydroxyethyl] -4-methyl-3-({4-[(5S) -5-methyl-2, 5-Dihydro-1H-pyrrole-3-yl] -1,3-thiazole-2-yl} thio) -7-oxo-1-azabicyclo [3.2.0] Stability of hepto-2-en-2-carboxylic ...
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JP4667542B2 |
PCT No. PCT/JP96/03540 Sec. 371 Date Jul. 17, 1997 Sec. 102(e) Date Jul. 17, 1997 PCT Filed Dec. 4, 1996 PCT Pub. No. WO97/21712 PCT Pub. Date Jun. 19, 1997Disclosed are carbapenem-3-carboxylic acid ester derivatives of formula (I), wher...
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