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WO/1998/057973A1 |
A stabilized carbapenem intermediate compound represented by formula (1) or a salt thereof is disclosed, wherein P represents a carboxyl protecting group and X represents a charge balancing group. In addition, a process for synthesizing ...
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WO/1998/052918A1 |
An efficient process for the stereoselective production of (2S,4S)-2-[[(R)-hydroxy-(3R)-cyclic amin-3-yl]methyl]pyrrolidine-4-thiol or its salts, which are intermediates useful in producing carbapenem, by reacting a compound represented ...
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WO/1998/046566A1 |
The present invention relates to novel $g(b)-lactam compounds, their pharmacologically acceptable salts and prodrugs, which exhibit antibiotic activity against a broad spectrum of organisms, especially bacteria which are resistant to con...
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WO/1998/034936A1 |
Carbapenem compounds represented by general formula (I) or pharmaceutically acceptable salts thereof, wherein each symbol has the meaning as defined in the specification. Because of being excellent in absorbability in the digestive tract...
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WO/1998/027094A1 |
Disclosed are novel ethylidene derivatives of tricyclic carbapenems of formula (I), wherein the ring marked C and X have the meaning as in the description, in the form of pure diastereoisomers and in the form of pure geometric isomers. N...
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WO/1998/023623A1 |
Compounds exhibiting a wide and potent antimicrobial activity against gram-positive and gram-negative bacteria, a potent antimicrobial activity against various $g(b)-lactamase producing bacteria, MRSA and resistant Pseudomonas aeruginosa...
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WO/1998/021210A1 |
A compound of formula (I), salts and metabolically labile esters thereof, wherein R represents optionally substituted aryl or heteroaryl group; A represents a propylene chain or A is a chain of 3 members one of which is selected from an ...
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WO/1998/018800A1 |
A method is presented for stabilizing carbapenem antibiotics by carboxylating the pyrrolidinyl amino with a carbon dioxide source. The resulting compounds and pharmaceutical compositions thereof can be used in the treatment of infectious...
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WO/1998/014421A1 |
A method for esterifying carboxylic compounds, characterized by treating either a mixture of a carboxylic compound and a base or a salt of a carboxylic compound with a compound represented by the formula R?1�-X (wherein R?1� represen...
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WO/1998/010761A1 |
The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH�2? group. The naphthosultam is further substituted with various ...
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WO/1998/011108A1 |
The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a sulfonamide containing ring system linked to the carbapenem nucleus through a CH�2? group. The com...
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WO/1998/009965A1 |
$g(b)-Lactam compounds represented by general formula (1) and salts and esters thereof, wherein R?1� represents a lower alkyl or an OH-substituted lower alkyl; R?2� represents H or a lower alkyl; X represents O, S, or NH; n is 1 to 3...
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WO/1998/002439A1 |
A process for synthesizing a coumpond of formula (I) or a pharmaceutically acceptable salt or ester thereof, wherein each P independently represents H or a protecting group, and R?1� and R?2� independently represent H, C�1-10? alky...
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WO/1997/047621A1 |
The invention provides a process for the preparation of compounds of formula (I) wherein R1, R2, R3 R4 and R5 are as defined in the specification; and wherein any functional groups are optionally protected; and salts thereof; which proce...
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WO/1997/045430A1 |
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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WO/1997/041853A1 |
1-Methylcarbapenem derivatives of general formula (I) and pharmacologically acceptable salts and esters thereof, useful as the active ingredient of anti-Helicobacter pylori compositions (such as therapeutic or preventive agents for Helic...
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WO/1997/041123A1 |
Constitution: 1-Methylcarbapenem compounds of general formula (I) and pharmacologically acceptable salts and derivatives thereof, wherein R1 is hydrogen or lower alkyl; R2 is hydrogen or lower alkyl; and R3 is hydrogen, lower alkyl, subs...
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WO/1997/040048A1 |
The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH2 group. The naphthosultam is further substituted with various subs...
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WO/1997/033888A1 |
Carbapenem compounds of formula (1), wherein R1: an optionally substituted lower alkyl group; R2: H or a lower alkyl group; Y: a bond or an optionally substituted lower alkylene group; R: optionally hydrogenated condensed oxazine or thia...
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WO/1997/025325A1 |
A cephem compound of formula (I) wherein R1 stands for an optionally substituted lower alkyl group, R2 stands for H or a lower alkyl group, R3 stands for H, an optionally substituted hydrocarbon group, cyano group, a lower alkyloxy group...
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WO/1997/023483A1 |
Constitution: 1-methylcarbapenem compounds having general formula (1) or pharmacologically acceptable salts thereof wherein R1 represents hydrogen or lower alkyl; R2 represents hydrogen or an ester residue; and A represents substituted p...
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WO/1997/021712A1 |
(1R,5S,6S)-2-[(1-(1,3-thiazolin-2-yl)azetidin-3-yl)thio]-6-[
(R)-1-hydroxyethyl]-1-methyl-carbapen-2-em-3-carboxylic acid ester derivatives of formula (I) wherein R1 is a hydrogen atom or a lower alkyl group; R2 is an alkyl group which m...
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WO/1997/020844A1 |
A 'beta'-methylcarbapenem compound of formula (I), a salt or an ester thereof, a process for the preparation thereof and a pharmaceutical composition containing same, wherein R1 is a C1-16 alkyl, C1-16 alkenyl, cycloalkyl, aryl or hetero...
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WO/1997/006174A1 |
A process for the preparation of a compound of formula (I), wherein R is a hydroxyl protecting group which comprises isomerisation of a compound of formula (II), wherein R is a hydroxyl protecting group.
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WO/1997/004770A1 |
Carbapenems are disclosed in which the 2-position sidechain contains a fluorenone moiety that is substituted by a bis cationic group. The compounds are of general formula (I). The compounds are effective for treating methicillin resistan...
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WO/1997/001564A1 |
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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WO/1996/038450A1 |
The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which...
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WO/1996/038448A1 |
The compounds of formulae A-D, wherein: X is selected from the group consisting of CH2, S, and O; T is selected from the group consisting of CH2 and O; U is selected from the group consisiting of CH2, S, O, and CH(alkyl), where alkyl is ...
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WO/1996/035691A1 |
A compound of structural Formula (I or II) useful for treating microbial infections in humans or other warm-blooded animals, or pharmaceutically acceptable salts thereof as defined herein.
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WO/1996/034846A1 |
Compounds of 1,3-propane diol linked structure (I), when for use in therapy, where R1 is an acyl or fatty alcohol group derived from a C12-30 preferably C16-30 fatty acid desirably with two or more cis or trans double bonds, and R2 is hy...
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WO/1996/034855A1 |
Compounds of structure (I), and when for use in therapy: where R1 is an acyl group derived from a C16-30 fatty acid with two or more cis or trans double bonds and particularly an n-6 or n-3 series EFA or conjugated linoleic acid, or colu...
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WO/1996/034869A1 |
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 aryl;...
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WO/1996/034868A1 |
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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WO/1996/028455A1 |
Novel carbapenem derivatives represented by general formula (I) which have an optionally substituted imidazo[5,1-b]thiazolium-6-ylmethyl group at the 2-position. The compounds have a broad and potent antibacterial activity on Gram-positi...
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WO/1996/026939A1 |
A Carbapenem compound of formula: (I) wherein R1 is an optionally substituted lower alkyl group, R2 is H or a lower alkyl group, Y is a bond or an optionally substituted alkylene group, and W is a group of formula: (a) or (b) wherein rin...
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WO/1996/011932A1 |
Compounds of general formula (I), in which Ra or Rb 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, nit...
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WO/1996/008491A1 |
A compound represented by general formula (I), a process for producing the same, and the use thereof as an antibacterial wherein R1 either represents hydrogen or lower alkyl, or forms a heterocyclic ring together with R3; R2 represents h...
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WO/1996/007655A1 |
A novel compound represented by general formula [I], a process for producing the same, and the use thereof as an antibacterial (wherein R1 represents hydrogen or lower alkyl; R2 represents hydrogen, ester residue or alkali metal; and R3 ...
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WO/1996/004286A1 |
The present invention provides processes for making compounds of the structure (Q-L1)-L-(L2-B), wherein (I) Q is a quinolone moiety; (II) B is a lactam moiety; and (III) L, L1, and L2 together comprise a linking moiety; comprising the st...
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WO/1996/004282A1 |
Carbapenems of formula (I) are disclosed as MRSA active agents. R1 represents hydrogen or methyl; CO2M represents a carboxylic acid, a carboxylate anion with or without a pharmaceutically acceptable counterion, a pharmaceutically accepta...
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WO/1996/001261A1 |
A carbapenem compound represented by general formula (I) or a salt thereof, wherein ring A represents a three- to seven-membered ring having at least one nitrogen atom and may have a substituent(s) in addition to R6; R1 represents hydrog...
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WO/1995/031461A1 |
The present invention is directed to a process of making 2-aryl carbapenems of formula (1) from a compound of formula (2), wherein compound (A) is reacted with a silyl protected boronic acid compound of formula (B) and wherein Ar is sele...
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WO/1995/029913A1 |
Crystal of (1R, 5S, 6S)-6-[(1R)-1-hydroxyethyl]-2-[(3S, 5S)-5-sulfamoylaminomethyl-1-pyrrolidin-3-yl]thio-1-methyl-1
-carba-2-penem-3-carboxylic acid represented by formula (I). The process for producing a lyophilized preparation contain...
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WO/1995/026966A1 |
The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which...
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WO/1995/026335A1 |
Novel n-arylaliphatic-n-alkyl-functionalised amides of formula (I), wherein Am is in particular a substituted piperidyl group. A method for preparing these compounds, and pharmaceutical compositions containing them are also disclosed. Th...
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WO/1995/025108A1 |
Carbapenems of formula (I) are disclosed as useful antibacterial agents. Pharmaceutical compositions and methods of use are also disclosed.
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WO/1995/023150A1 |
A compound represented by general formula (I), a medicinally acceptable salt or ester thereof, a process for producing the same, and an antibacterial containing the same as the active ingredient: wherein R1 represents hydrogen or lower a...
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WO/1995/023149A1 |
Compounds of general formula (I), salts and metabolically labile esters thereof; wherein R1 represents hydrogen or a hydroxyl protecting group; R2 represents hydrogen or a carboxyl protecting group; R3 represents hydrogen or a nitrogen p...
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WO/1995/021841A1 |
A carbapenem antibiotic of formula (I) is disclosed. The variable (a) represents a counterion. Pharmaceutical compositions and methods of use are also disclosed.
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WO/1995/019979A1 |
This invention relates to the synthesis of a bicyclic ketoester compound of formula (1) obtained by cyclizing a diazo compound of formula (2) in the presence of a rhodium catalyst. By adding an effective amount of a Lewis acid to the cyc...
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