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7538212 |
Intermediate for carbapenem compound for oral administration and process for producing the same
The present invention provides a novel intermediate represented by formula (1), (3), or (4) for efficiently producing a 1β-methylcarbapenem compound for oral administration, and a process for...
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7459551 |
Method for preparing cyclic compounds
The present invention provides a method for preparing a β-lactam compound of the following Formula (3), which comprises the step of reacting a compound of the following Formula (1) with a trialkyl...
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7148356 |
Process for the catalytic synthesis of biaryls and polymers from aryl compounds
A process for producing organic substituted aromatic or heteroaromatic compounds including biaryl and biheteroaryl compounds in a two-step reaction. In the first step, the aromatic or...
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7115595 |
Carbapenem compounds
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...
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7045619 |
2-(pyrazol-3-yl)carbapenem derivatives
A compound of formula (I):
wherein
R α is hydrogen, optionally substituted (C 1-6 )alkyl or optionally substituted aryl;
R β is hydrogen, optionally substituted (C 1-6 )alkyl or...
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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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6908913 |
Carbapenem derivatives
An objective of the present invention is to provide carbapenem derivatives which have strong antibiotic activity also against MRSA, PRSP, Influenzavirus, and β-lactamase producing bacteria and are...
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6867302 |
Process for the catalytic synthesis of biaryls and polymers from aryl compounds
A process for producing organic substituted aromatic or heteroaromatic compounds including biaryl and biheteroaryl compounds in a two-step reaction. In the first step, the aromatic or...
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6825187 |
Carbapenem derivatives of quarternary salt type
An objective of the present invention is to provide carbapenem derivatives which have potent antibiotic activity against MRSA, PRSP, Influenzavirus, and β-lactamase-producing bacteria and are...
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6680313 |
Carbapenum derivatives
An objective of the present invention is to provide carbapenem derivatives which have potent antibiotic activity against MRSA, PRSP, Influenzavirus, and β-lactamase-producing bacteria and are...
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6531466 |
Tricyclic carbapenem compounds
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 ...
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6495539 |
B-lactam-like chaperone inhibitors
Compounds of the formula and the salts, esters and amides thereof wherein Z is S, SO, SO 2 or O; each of R 1 , R 2 and R 3 is independently H or substituted or unsubstituted alkyl (1-10C),...
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6489471 |
Process for the synthesis of carbapenem intermediates, and compounds produced
A process of synthesizing a carbapenem compound of formula (6) is disclosed, wherein R represents H or methyl, P and P* independently represent H or protecting groups and each R 1 is independently...
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6489318 |
Ethylidene derivatives of tricyclic carbapenems
Disclosed are novel ethylidene derivatives of tricyclic carbapenems of the formula I wherein the ring marked C and X have the meaning as in the description, in the form of pure diastereoisomers...
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6399597 |
1,8-naphthosultamylmethyl carbapenem antibacterial compounds, compositions containing such compounds and methods treatment
Compounds of formula I are disclosed. as well as pharmaceutically acceptable salts thereof. The naphthosultam is substituted with various substituent groups including at least one cationic group...
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6395894 |
Process for the synthesis of carbapenem intermidiates, and compounds produced
A process of synthesizing a compound of structural formula 6 is disclosed wherein R 1 represents H or a suitable protecting group for an alcohol; R 2 represents a benzyl, C 1-6 alkyl or aryl;...
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6346617 |
Crystalline 2-hydroxymethyl carbapenem intermediate compounds and process for synthesis thereof
A process for preparation of a compound of formula I: wherein: R 1 represents CH 3 or H; and P represents a protecting group; comprising reacting a compound of formula IV: wherein R 1 and P...
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6346526 |
Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
Compounds of formula I: as well as pharmaceutically acceptable salts thereof useful as carbapenem antibacterial agents are disclosed wherein X is CH 2 or C═O.
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6310055 |
Halophenoxy substituted carbapenem antibacterial compounds
The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2 -position with a iodophenoxy linked through a group --Z--CH 2 --; The...
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6294529 |
Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
Compounds of formula I are disclosed. ##STR1## as well as pharmaceutically acceptable salts thereof. The naphthosultam is substituted with various substituent groups including at least one cationic...
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6288054 |
Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
The present invention relates to tricyclic carbapenem antibacterial agents in which the carbapenem nucleus is fused to a 6 membered carbocyclic ring. The compound is further substituted with...
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6255479 |
Process for the preparation of α-oxolactams
A method for preparing an α-oxolactam comprising, reacting a corresponding α-diazolactam with an oxygen donor, in the presence of a transition metal catalyst, to yield the corresponding...
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6252063 |
Crystalline salts of a carbapenem antibiotic
Crystalline salts of an amorphous, unstable carbapenem antibiotic having the formula: ##STR1## are disclosed, wherein R - represents beyslate, tosylate, napsylate, saccharate or alizarate.
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6235898 |
Process for the synthesis of carbapenem intermediated and compounds produced
A process of synthesizing a carbapenem compound of formula 6: ##STR1## is disclosed using a compound of formula 4': ##STR2## The intermediate compounds that are described herein are also included...
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6194568 |
Process for synthesizing carbapenem intermediates
The invention describes an improved process for synthesizing 1-β-methyl-2-hydroxymethyl substituted carbapenems as key intermediates for the synthesis of anti-MRSA carbapenem antibiotics. The...
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6150350 |
Antimicrobial compositions
The invention relates to antimicrobial compositions comprising a combination of (1) a therapeutically effective amount of a compound of formula I ##STR1## with (2) a second ingredient selected from...
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6025487 |
Isomerisation process
A process for the preparation of a compound (I) ##STR1## wherein R is a hydroxyl protecting group which comprises isomerising a compound of formula (I) wherein R is a hydroxyl protecting group by...
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6011150 |
Azetidinone compound and process for preparation thereof
There is disclosed an azetidinone compound of the formula [I]: ##STR1## wherein Ring B is a benzene ring which may have substituent(s), R 1 is a hydroxy-substituted lower alkyl group which may...
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6008212 |
Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
Compounds of formula I: ##STR1## as well as pharmaceutically acceptable salts thereof are disclosed. R 2 is H and R 3 is C1-3 alkyl, or R 2 and R 3 taken in combination represent C 1 -3...
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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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5990101 |
Carbapenem derivatives
Novel carbapenem derivatives, represented by the following formula (I), having a substituted or unsubstituted imidazo[5,1-b]thiazolium-6-ylmethyl group at the 2-position are disclosed. The...
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5880111 |
Therapeutic derivations of diphosphonates
Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by...
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5869477 |
β-methylcarbapenem derivatives, process for the preparation thereof and pharmaceutical composition comprising same
A β-methylcarbapenem compound of formula (I), a salt or an ester thereof, a process for the preparation thereof and a anti-bacterial composition containing same: ##STR1## wherein: R 1 is a C 1 -6...
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5856475 |
4-thia-1-azabicyclo/3.2.0/Heptane-3-Imino-2-isopropylidene-7-oxo-analogon s of beta-lactams, processes for their preparation and the use thereof
The object of the present invention are 4-thia-1-azabicyclo 3.2.0!heptane-3-imino-2-isopropylidene-7-oxo beta-lactamic analogons of general formula I ##STR1## wherein the radicals have the...
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5854227 |
Therapeutic derivatives of diphosphonates
Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, infectious urinary tract stones, and bone cancer, are...
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5849907 |
Chemical process
A process for the preparation of the antibacterial compound ##STR1## or a salt thereof which comprises hydrogenolysis of the novel compound of formula (II) ##STR2## and if necessary or desired...
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5840885 |
Processes for the production of 6-α-aminoacyl-penicillin and 7-.alpha .
A new process is described for the production of 6-alpha-amino-penicillins and 7-alpha-amino-desacetoxy-cephalosporins free from halogen-containing solvents by acylating 6-APA, 7-ADCA or a...
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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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5811374 |
3-aryl-pyrrolidine-2,4-dione derivatives
New 3-arylpyrrolidine-2,4-dione derivatives of the formula (I): ##STR1## in which the variables A, B, E, R, X, Y, Z and n are set forth in the specification, are useful as insecticides, acaricides,...
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5801242 |
Process for making quinolonyl lactam antimicrobials and novel intermediate compounds
The present invention provides processes for making compounds of the structure (Q--L 1 )--L--(L 2 --B) wherein (I) Q is a quinolone moiety; (II) B is a lactam moiety; and (III) L, L 1 ,...
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5756725 |
Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
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...
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5719276 |
Beta lactam production
A new process is described for the production of 6-alpha-amino-penicillins and 7-alpha-amino-desacetoxy-cephalosporins free from halogen-containing solvents by acylating 6-APA, 7-ADCA or a...
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5705636 |
Cyclohexene derivatives
Compounds of the formula ##STR1## wherein R 1 represents hydrogen or a nitrogen protecting group, useful as intermediates in the preparation of compounds having antibacterial activity.
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5703231 |
Process for making antimicrobial compounds
The present invention provides a process for making a compound having a structure according to Formula (I) ##STR1## wherein A 1 , A 2 and A 3 are independently carbon or nitrogen and R 1 , R 3 ,...
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5693634 |
Urea derivatives for use in treating bacterial infections
The present invention relates to compounds of formula (I) ##STR1## and salts and metabolically labile esters thereof. These compounds and compositions containing them have antibacterial activity....
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5646139 |
Antimicrobial carbapenem quinolones
Compounds of Structure: ##STR1## as well as their pharmaceutically-acceptable salts and biohydrolyzable esters, and hydrates thereof, are effective antiinfective agents, useful in treating and...
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5612477 |
2-(pyrazol-3-yl)carbapenem derivatives
Disclosed are a carbapenem compound represented by formula (I) and processes to its preparation.
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5607928 |
Carbapenem derivatives containing a bicyclic ketone substituent and their use as anti-infectives
The present invention relates to carbapenems and provides a compound of the formula (I) ##STR1## wherein R 1 is hydroxymethyl, 1-hydroxyethyl or 1-fluoroethyl; R 2 is hydrogen or C 1 -4 alkyl;...
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5587374 |
10(1-hydroxyethyl)-11-oxo-1-azatricyclo/7.2.0.0..sup.3.8/ undec-2-ene-2-carboxylic acid esters and a process for preparing thereof
A compound of the formula 1-cyclohexyloxycarbonyloxethyl (4S, 8S, 9R 10S, 12R)-4-methoxy-10-(1-hydroxyethyl)-11-oxo-1-azatricyclo[7.2.
0.0. 3 ,8 ]undec-2-ene-2-carboxylate which is useful as a...
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5580976 |
Preparation of β-lactam compounds, and intermediates therefor
A process for preparing a β-lactam compound of the formula (I): ##STR1## which comprises cyclization of an azetidinone derivative of the formula: ##STR2## is provided in which R 1 is hydrogen,...
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