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JP3959128B2 |
PURPOSE: To effectively obtain the compound useful as an intermediate for an antibacterial agent by a new method in which ring-closure reaction of β- lactam compound and a phosphate reaction are performed in one-pot reaction. CONSTITUTI...
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JP3953274B2 |
A process for the direct crystallization of a compound of formula (I) or a pharmaceutically acceptable salt thereof, is disclosed, wherein R<1> and R<2> represent H, C1-10 alkyl, aryl or heteroaryl, or substituted C1-10 alkyl, aryl or he...
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JP2007039383A |
To provide methods for industrially producing a carbapenem medicament having high antibacterial activity, high in safety and also high in peroral absorbability, and intermediates for the medicament, respectively.The method for producing ...
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JP2007039382A |
To provide methods for industrially producing a carbapenem medicament having high antibacterial activity, high in safety and also high in peroral absorbability, and intermediates for the medicament, respectively.The methods are shown by ...
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JP3878131B2 |
An objective of the present invention is to provide carbapenem derivatives which have strong antibiotic activity also against MRSA, PRSP, Influenzavirus, and beta -lactamase producing bacteria and are stable to DHP-1. The carbapenem deri...
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JP2007001949A |
To provide an improved method for removing a silyl group from a silyl ether compound.The method for removing the silyl group from the silyl ether compound uses a complex comprising titanium tetrachloride and a nitro compound.
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JP3848693B2 |
PURPOSE: To provide the subject new compound having excellent antibacterial activities against various gram-positive and negative bacteria and useful for preventing and treating various bacterial infectious diseases. CONSTITUTION: A comp...
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JP2006298906A |
To find a synthetic route for carbapenem antimicrobial agents being low in cost and high in safety, also suitable for mass synthesis.The carbapenem-based antimicrobial agent is produced by using an amine compound represented by formula (...
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JP2006265235A |
To obtain a medicine comprising a crystal having improved storage stability as an active ingredient in crystals of a compound represented by formula (I) or its pharmaceutically permissible salts.The medicine comprises a crystal of a 1-me...
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JPWO2004089954A1 |
Equation 1(In the formula, R1Is C1-C3C substituted with alkyl or hydroxyl group1-C3Represents alkyl. R represents a hydrogen atom or a group that is hydrolyzed in vivo to regenerate a carboxyl group. G represents any of G1, G2, and G3. )...
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JP2006176418A |
To provide a method for efficiently producing a 1β-methylcarbapenem compound for oral administration.The method for producing a 1β-methylcarbapenem compound comprises reacting a β-lactam compound with a compound (6) represented by the...
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JP2006151815A |
To provide a carbapenem derivative which has a potent antimicrobial effect on pneumococci including MRSA, VRE and PRSP, influenza viruses including BLNAR and β-lactamase-producing strains from among resistant strains bringing about clin...
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JP2006151970A |
To provide a carbapenem derivative which exhibits excellent therapeutic or preventive effects on microbism, particularly on respiratory infectious diseases.The carbapenem compound represented by chemical formula 1 or a pharmacologically ...
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JP2006151814A |
To provide a carbapenem derivative which has a potent antimicrobial effect on pneumococci including MRSA, VRE and PRSP, influenza viruses including BLNAR and β-lactamase-producing strains from among resistant strains bringing about clin...
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JP2006515633A |
A pharmaceutically active compound having a carboxylic acid group -COOH as a part of its chemical structure which -COOH group is in the form of a carboxylic acid ester.
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JP3761096B2 |
PURPOSE: To easily and effectively obtain a 2-alkyl-substituted carbapenem derivative useful as a β-lactam antibiotic substance under mild reaction condition by directly introducing a substituted alkyl group at a specific site of a carb...
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JP3761097B2 |
PURPOSE: To easily and effectively obtain a 2-vinyl-substituted carbapenem derivative useful as a β-lactam antibiotic substance under mild reaction condition by directly introducing a substituted vinyl group at a specific site of a carb...
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JPWO2004043961A1 |
The present invention provides an efficient method for producing a 1β-methylcarbapenem compound for oral administration. That is, the present invention uses a β-lactam compound represented by the general formula (1) as a starting mater...
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JP2006045153A |
To find out an antibacterial agent which has high antibacterial and bactericidal potency and treats or prevents (especially treats) bacterial infections, especially in the respiratory system.The subject medicine contains, as an active in...
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JPWO2004035539A1 |
The present invention is useful as a prodrug-type oral carbapenem according to the following formula (XI) [in formula, R.2Represents a group that is decomposed in vivo and can be easily removed, and R4Represents 1- (1,3-thiazolin-2-yl) a...
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JP2006034950A |
To provide a method and an agent for efficiently cleaning an institution and/or facilities used for manufacturing a substance capable of chemically reacting with a nucleophilic agent and/or a medicine.This is a method for cleaning an ins...
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JP3724854B2 |
To easily obtain 1-azabicyclo [1,1,0] butane useful as a synthetic intermediate for modifying a carbapenem compound excellent in antibacterial activity and used as a synthetic source material for industrial product in high yield by react...
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JP3703146B2 |
Disclosed are a carbapenem compound represented by formula (I) and processes to its preparation.
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JP2005231999A |
To provide a process for industrially and advantageously producing a carbapenem compound having a broad antimicrobial spectrum, a potential antimicrobial activity and resistance to β-lactamase and renal dehydropeptidase-1.A (4R)-hydroxy...
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JPWO2003089431A1 |
Formula: A novel carbapenem compound represented by the following formula or a pharmaceutically acceptable salt thereof. A wide range of Gram-positive and Gram-negative bacteria, especially penicillin-resistant pneumoniae (PRSP) and β-l...
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JPWO2003089432A1 |
A simple method for producing the following carbapenem derivatives. It is represented by the following formula (in the formula, R1 means a protecting group for a hydroxyl group, R2 and R3 mean a hydrogen atom or a lower alkyl group, R4 a...
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JP3684339B2 |
To provide a method of preparing a carbapenem compound exhibiting a strong antibacterial activity. This method prepares (1R,5S,6S)-2-[1-(1,3-thiazoline-2-yl) azethidine-3-yl]thio-6-[(R)-1-hydroxyethyl]-1-methyl-carbape
ne-2-m-3-carboxyli...
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JP3681116B2 |
To provide a crystal of a 1-methylcarbapenem compound having an excellent antimicrobial activity and excellent preservation stability and a medicine, especially an antimicrobial agent comprising the crystal as an active ingredient. This ...
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JP2005200412A |
To provide a medicine effective for an infection-causing bacterium which now becomes a serious clinical problem and includes a pneumococcus including PRSP (penicillin-resistant Streptococcus pneumonie), an influenza bacillus including BL...
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JP2005139088A |
To obtain a carbapenem derivative which has strong and balanced anti-bacterial activities against wide range pathogenic bacteria.This compound is represented by formula (I) [R1 and R8 are each H or a 1 to 6C alkyl; G1 is a single bond, a...
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JP2005514323A |
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 containing imipenem with an organic solvent, wher...
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JP2005104851A |
To obtain a new carbapenem derivative useful as a therapeutic agent for various kinds of bacterial infectious diseases, having a strong antibacterial activity against Streptococcus pneumoniae including PRSP (penicillin-resistant-Streptoc...
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JP2005097278A |
To provide a crystal of a 1-methylcarbapenem compound which has excellent antimicrobial activity and preservative stability, high productivity and easy manipulability, and a medicine especially an antibacterial agent which effectively co...
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JP2005509037A |
The present invention relates to a cost effective and industrially advantageous process for the preparation of imipenem of high purity, which comprises dissolving crude imipenem in warm water to which some base has been added to obtain a...
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JP2005508860A |
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 phosphorohalidate in the presence of a base an...
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JP2005508321A |
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 carbapenem, b) cooling the resulting solution to l...
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JP2004262923A |
To obtain a bactericide having strong antibacterial and bactericidal activities and used for treating or preventing (especially treating) bacterial infectious diseases, especially those to the respiratory system.The carbapenem compound i...
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JPWO2002094829A1 |
Formula (I'): [In the formula, each symbol is synonymous with the specification. ], And an antibacterial agent containing the compound as an active ingredient. The carbapenem compound of the present invention is excellent in gastrointest...
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JP3558684B2 |
PURPOSE: To provide a method for drying a pyrrolidylthiocarbapenem derivative for decreasing a residual solvent, obtain crystals of a pyrrolidylthiocarbapenem derivative, excellent in solubility and stability and provide a method for pro...
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JP2004525084A |
The present invention relates to a cost effective and commercially viable process for the preparation of crystalline N-formimidoyl thienamycin monohydrate (Imipenem monohydrate) of Formula I.
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JPWO2002044178A1 |
Formula [1]: [In the formula, R1 is a lower alkyl group, etc .; R2 is H, a lower alkyl group; X is O, S, NH; m and n are 0 to 5, and the sum is 1 to 5; Y1 is. Halogen, etc .; Y2 is a hydrogen atom, a lower alkyl group that may be substit...
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JP3543016B2 |
PURPOSE: To safely, mildly and simply obtain an intermediate product of an antibiotic substance having a carbapenam or a carbapenem skeleton in β-lactam- based medicines which are antibiotic substances by cyclizing a new azetidinone der...
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JP3532224B2 |
PURPOSE: To enable efficient and inexpensive removal of silyl groups by reaction of a specific silyl ether compound with an inorganic acidic fluoride in the presence of a quaternary ammonium salt, in the production of a specific compound...
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JPWO2002053566A1 |
Carbapenem compounds having a substituted phenyl or a substituted thienyl directly attached to the 3-position of carbapenem nucleus as represented by the formula: wherein Ring E is benzene ring or thiophene ring; R<1> is optionally OH-su...
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JP2004512255A |
This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligan...
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JP2004512339A |
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 compoundin...
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JPWO2002048149A1 |
A novel β-lactam compound having the following structure: [In the formula, R1 is a lower alkyl group or a lower alkyl group substituted with a hydroxyl group, R2 is a hydrogen atom or a lower alkyl group, and R3 is a hydrogen atom, a hy...
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JP2004107288A |
To provide an industrial method for producing an α,β-unsaturated carboxylic acid ester represented by formula (II).The method for producing the α,β-unsaturated carboxylic acid ester represented by formula (II) involves treating a com...
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JP2004107289A |
To provide an industrial method for producing a vinyl sulfide compound represented by formula (II).The method for producing the vinyl sulfide compound represented by formula (II) involves treating a compound represented by formula (I) wi...
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JP2004043445A |
To find a carbapenem derivative having strong and well-balanced antimicrobial activity against pathogenic bacteria in wide range.The carbapenem derivative having strong and well-balanced antimicrobial activity against the pathogenic bact...
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