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JP3040600B2 |
PURPOSE: To obtain a high-purity carbapenem derivative useful for infectious diseases, having excellent antimicrobial properties and stability simply and efficiently by reacting a specific azetidine derivative with a specific organic pho...
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JP3037827B2 |
PURPOSE: To obtain a new compound effective for various kinds of infectious diseases, having excellently antibacterial action on Escherichia coli, Pseudomonas aeruginosa, etc., and stability to decomposing enzymes such as DHP. CONSTITUTI...
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JP3035325B2 |
Compounds of the general formula (I) in which:- R1 represents a hydroxyl protecting group; and R2 represents a hydrogen or halogen atom, an azido group, a C1-3 alkyl group, a group (CH2)mOR3 wherein m is zero or one and R3 represents a h...
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JP2000086660A |
To obtain a new carbapenem compound highly resistant to β-lactamase and nephrodehydropeptidase and excellent in antibacterial activity as well. This new compound is a carbapenem compound (salt) of formula I [R1 and R2 are each H or a (n...
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JP3025788B2 |
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JP3018442B2 |
Compounds of the general formula (I) in which:- R1 represents a hydroxyl protecting group; and R2 represents a hydrogen or halogen atom, an azido group, a C1-3 alkyl group, a group (CH2)mOR3 wherein m is zero or one and R3 represents a h...
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JP3019486B2 |
Compounds of formula in which R1 is hydrogen or a hydroxyl protecting group and -X-Y- is -CH=CH- or useful as intermediates in the preparation of antibacterially active compounds.
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JP3019407B2 |
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JP2000053681A |
To obtain an antimicrobial agent having excellent stability to dehydropeptidase I, having a high recovery ratio in urine, low toxicity, capable of exhibiting excellent antimicrobial activity, useful for treating and preventing bacteriosi...
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JP2000038387A |
To provide a novel compound that has high anti-microbial activity, is stable to dehydropeptidase I and shows high urinary content. This is a novel compound represented by formula I [A is a heteroaryl monocyclic thio group that is represe...
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JP3005045B2 |
NEW MATERIAL:A compound expressed by formula I [R<0> is H or OH protecting group; R<1> is lower alkyl; R<2> is carboxyl protecting group or negative charge; R<3> is H or amino protecting group; R<4> is (substituted) lower alkyl; k is 0-4...
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JP2999216B2 |
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JP2000007676A |
To provide a method for effectively producing a carbapenem compound useful as an intermediate for (producing the important isomers of) carbapenem- based antibiotic excellent in antimicrobial property in high yield by reacting a specific ...
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JPH11513979A |
A process of synthesizing a compound of formula (1) or (2) is disclosed wherein R represents H or methyl and P represents triethylsilyl or trimethylsilyl. A compound of formula (3) or (4) is reacted with P-C1 wherein P is as defined abov...
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JP2979235B2 |
beta -Lactam compounds of the formula (Ia) including pharmaceutically acceptable salts and in vivo hydrolysable esters, processes for their preparation and their use as antibiotics: wherein R<1> is hydrogen, methoxy or formamido; R<2> is...
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JP2977212B2 |
Antimicrobial quinolonyl lactam compounds comprising a lactam-containing moiety linked, by a non-ester linking moiety, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula: wherein (1) R<3>, R<4>, and R<5>, to...
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JP2969616B2 |
PURPOSE: To obtain a 4-mercaptopyrrolidine compound useful as a synthetic intermediate for carbapenem-based antimicrobial agents, etc., in high yield at a low cost by reacting a specific halogenobutyric acid compound (salt) with an amine...
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JP2965922B2 |
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JP2958835B2 |
PURPOSE: To obtain the subject compound by deesterification and decarboxylation, starting from, as raw material, a 4-(1,1-dialkoxycarbonylalkyl) azetidin-2-one derivative having such a structure that a malonic acid derivative is bonded t...
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JP2955276B2 |
To obtain a composition having strong antimicrobial activity, stable to dehydropeptidase I and β-lactamase, having high recovery rate in urine and low nephrotoxicity and useful for preventing or treating infectious diseases by including...
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JPH11510801A |
PCT No. PCT/EP96/03374 Sec. 371 Date Mar. 27, 1998 Sec. 102(e) Date Mar. 27, 1998 PCT Filed Aug. 1, 1996 PCT Pub. No. WO97/06174 PCT Pub. Date Feb. 20, 1997A process for the preparation of a compound (I) wherein R is a hydroxyl protectin...
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JPH11509871A |
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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JP2940836B2 |
Disclosed are 6- and 4-substituted-1-azabicyclo-[3.2.0]heptan-3.7-dione-2-carboxy
lic acid esters and salts (I) which are useful in the preparation of 6-, 1- and 2- substituted carbapenem antibiotics.wherein R5 is a pharmaceutically acce...
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JP2934274B2 |
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JP2934283B2 |
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JPH11193232A |
To obtain a composition for prevention or treatment for infection having potent antimicrobial activity and weak toxicity to kidney by including a specific 1-methylcarbapenem compound as an active ingredient. This composition includes a 1...
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JP2910356B2 |
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JPH11506430A |
PCT No. PCT/US96/05202 Sec. 371 Date Nov. 7, 1997 Sec. 102(e) Date Nov. 7, 1997 PCT Filed Apr. 18, 1996 PCT Pub. No. WO96/35691 PCT Pub. Date Nov. 14, 1996A compound of structural Formula I or II which is useful for treating microbial in...
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JP2897153B2 |
There is disclosed an azetidinone compound of the formula [I]: wherein Ring B is a benzene ring which may have substituent(s), R<1> is a hydroxy-substituted lower alkyl group which may have substituent(s), X is oxygen atom and the like, ...
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JPH11504910A |
A compound of formula (I), wherein R is selected from the group consisting of isobutyryloxymethyl, (5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl, and benzoyloxymethyl, is useful in the treatment of bacterial infections.
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JPH11504912A |
A compound of general formula (I) in which R is (a); wherein R< alpha > is hydrogen, optionally substituted (C1-6)alkyl or optionally substituted aryl; R< beta > is hydrogen, optionally substituted (C1-6)alkyl or optionally substituted a...
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JPH1180158A |
To provide a method for simply producing the subject compound useful as an intermediate for β-lactam-based antibiotics by reacting a carbapenem derivative with iodobenzene dichloride and then with a base. This method reacts with a compo...
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JP2875015B2 |
Antimicrobial dithiocarbamoyl quinolone compounds of the general formula: wherein (1) A<1>, A<2>, A<3>, R<1>, R<3>, R<4>, and R<6> form any of a variety of quinolone and related heterocyclic structures similar to those known in the art t...
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JPH1160576A |
To obtain the subject new derivative strong in antimicrobial activities, stable to dehydropeptidase I, high in proportion in urine and useful as an antimicrobial agent. The subject derivative is a tricyclic heterocyclic derivative of for...
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JP2860379B2 |
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JP2847693B2 |
PURPOSE:To efficiently remove a protecting group by treating a beta-lactam compound having carboxyl protected with a substituted or unsubstituted allyl with a Pd catalyst in the presence of an allyl group scavenger. CONSTITUTION:A p-lact...
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JP2848552B2 |
PURPOSE: To obtain a stable new compound exhibiting excellent antibacterial activity and useful as an antibacterial agent for peroral administration. CONSTITUTION: This derivative is a crystalline compound of (1R,5S,6S)-2[(4R)-2- oxo-4-p...
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JP2843444B2 |
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JPH10279581A |
To obtain the subject new compound good in stability against a dehydropeptidase-I, exhibiting an excellent antibacterial activity, high in recovery rate in urine and useful as an antibacterial agent for treating or preventing a bacterial...
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JP2792103B2 |
A compound of the formula : in which R<1> is carboxy or protected carboxy, R<2> is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl, R<3> is hydrogen or lower alkyl, R<4> is unsaturated heterocyclic group which may be substituted by ...
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JPH10508285A |
Carbapenems of the formula: I are disclosed as useful antibacterial agents. Pharmaceutical compositions and methods of use are also disclosed.
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JP2783683B2 |
PCT No. PCT/KR93/00114 Sec. 371 Date Jul. 21, 1995 Sec. 102(e) Date Jul. 21, 1995 PCT Filed Dec. 20, 1993 PCT Pub. No. WO94/14811 PCT Pub. Date Jul. 7, 1994The present invention relates to 2-(2-substituted pyrrolidin-4-yl)-thio-carbapene...
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JPH10507185A |
Compounds of general formula (I), in which R or R alone is hydrogen, optionally substituted (C1-6)alkyl or together form a 5 or 6 membered heterocyclic ring which may contain at least one additional heteroatom selected from oxygen, nitro...
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JPH10168081A |
To obtain a new subject carbapenem derivative that contains a specific 1-methylcarbapaenem derivative, is excellent in antimicrobial activity, stable to dehydropeptidase I with high urinary recovery and is useful as an antimicrobial agen...
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JP2767171B2 |
A method of crystallizing (1R,5S,6S)-2-[(6,7-dihydro-5H-pyrazolo[1,2-a][1,2,4]triazoli
um-6-yl)]t hio-6-[(R)-1-hydroxyethyl]-1-methyl-carbapenem-3-carboxylate
(hereinafter simply referred to as L-627), which is characterized by maintain...
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JP2754679B2 |
A compound of the formula : in which R<1> is carboxy or protected carboxy, R<2> is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl, R<3> is hydrogen or lower alkyl, R<4> is aliphatic heterocyclic group which may be substituted by su...
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JPH10130270A |
To obtain the subject derivative having antimicrobial activity in a high quality and in a high yield by carrying out reaction in the presence of an organic base and a metal salt. (A) A compound of formula I [R1 is a group of formula a II...
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JP2752143B2 |
NEW MATERIAL:A compound shown by formula I [R<1> is H or methyl; l, m and n are 0-3 and m+n are 2-6; Y is direct single bond and O, S or =NR<6> (R<6> is H, alkyl, etc.); R<2> is H (substituted) alkyl, halogen, OH, alkoxy, amino, alkanoyl...
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JP2748500B2 |
A compound of the formula : in which R<1> is carboxy or protected carboxy, R<2> is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl, R<3> and R<4> are each hydrogen or lower alkyl, and R<5> is aliphatic heterocyclic group, which may ...
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JPH1087665A |
To efficiently obtain the subject compound useful as an antibiotic substance excellent in antimicrobial activities and stability in a short process by reacting an α,β-unsaturated ester with a sulfenyl chloride compound. A compound repr...
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