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7335681 |
Amino ceramide-like compounds and therapeutic methods of use
Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of...
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7220737 |
Noribogaine in the treatment of pain and drug addiction
The present invention is directed to methods of treating patients for pain by administering noribogaine. Noribogaine may also be used to treat patients for the symptoms associated with withdrawal...
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7202236 |
Modified release pharmaceutical formulation
A modified release pharmaceutical composition comprising, as active ingredient, a compound of formula (I), wherein R 1 represents C?1-2#191 alkyl substituted by one or more fluoro substituents; R...
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7148251 |
Amino ceramide-like compounds and therapeutic methods of use
Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of...
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7138414 |
Heterocyclically substituted benzoylureas, process for their preparation and their use as pharmaceuticals
The invention relates to heterocyclically substituted benzoylureas and also to their physiologically tolerated salts and physiologically functional derivatives. Compounds are described of the...
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6967196 |
Sulfonamide compounds and uses thereof
In accordance with the present invention, there is provided a novel class of sulfonamide compounds. Compounds of the invention contain a core sulfonamide group. Variable moieties connected to the...
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6831078 |
Azetidinecarboxamide derivatives for treating CNS disorders
A compound of formula (1) wherein R 1 is aryl; and R 2 is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and their use in therapy, particularly for the treatment and...
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6514962 |
Stabilized preparations of β-lactam antibiotic
Stabilized preparations which contain a β-lactam antibiotic having an esterified carboxyl group attached directly to the mother nucleus, an oil and a phosphate.
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6482818 |
C-2 S/O-and S/N formaldehyde acetal derivatives of carbapenem-3-carboxylic acids and their use as antibiotics and β-lactamase inhibitors
The compounds of the general formula I wherein R 1 denotes hydrogen, hydroxymethyl or 1-hydroxyethyl, R 2 denotes hydrogen or methyl and R 3 denotes a pharmaceutically acceptable group which...
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6426342 |
Use of β-lactamase inhibitors as neuroprotectants
Novel neuroprotectant methods are described. β-Lactamase inhibitors are used to prevent or reduce loss of neuronal cells and neuronal cell function in patients afflicted with or susceptible to...
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6251891 |
Carbapenem derivatives
A compound represented by the general formula ##STR1## wherein R 1 either represents a hydrogen atom or a lower alkyl group, R 2 represents a hydrogen atom, an ester residue, an alkali metal or...
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6225305 |
Substituted urea and isothiorea derivatives as no synthase inhibitors
The use of an N-substituted urea derivative for the manufacture of a medicament for the treatment of a condition where there is an advantage in inhibiting the NO synthase enzyme, in particular...
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5273973 |
Antimicrobial quinolonyl esters
Antimicrobial quinolnyl 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 the formula: ##STR1##...
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5242914 |
2-(heterocyclylthio) carbapenem derivatives, their preparation and their use as antibiotics
Compounds of formula (I): ##STR1## in which R a is a group of formula (II): ##STR2## where one of R' is a bond to the remainder of the compound, one more of R' is R 2 and the others of R' are all...
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5116833 |
Antibiotic C-3 dithioacetal-substituted carbapenem compounds, compositions, and methods of use thereof
A dithioacetal carbapenem of the formula ##STR1## in which R 1 is hydrogen or C 1 -6 alkyl; n is 0, 1 or 2; R 3 is hydrogen or C 1 -6 alkyl; R 2 is C 1 -6 alkyl, phenyl optionally...
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4863916 |
Substituted 6-hydroxymethyl-carbapenem antibiotics
Substituted 6-hydroxymethyl-carbapenem antibiotics of the formula ##STR1## in which R 1 is --OR 4 , ##STR2## A is a direct bond, or an alkylene and/or cycloalkylene radical, R 2 is a group of the...
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4771046 |
Carbapenem derivatives
Carbapenem derivatives useful as antibacterial agents have the formula ##STR1## wherein: X represents a hydrogen atom or a methyl group; and Y represents a group of the formula: ##STR2## in...
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4720491 |
Fluoralkylatedcarbapenem derivatives
Compounds of formula I ##STR1## wherein, R 1 represents hydrogen or methyl, R 2 represents hydrogen or lower alkyl, lower alkenyl, lower alkynyl or cycloalkyl each of which may be...
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4698339 |
Carbapenems, their production and use
A compound of the general formula: ##STR1## wherein X is a lower alkylene group which may optionally be substituted by a hydroxyl group, or a lower alkenylene group, Y is (1) a lower alkyl group,...
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4683226 |
6-hydroxyalkyl-2-(substituted-thio)penem-3-carboxylic acids
6-substituted-hydrocarbon-2-(substituted-thio)penem-3-carbox
ylic acids and cogeners having useful antibacterial activity are disclosed. The compounds are prepared in a reaction sequence starting...
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4495197 |
N-Carboxyl-thienamycin esters and analogs thereof as anti-inflammatory agents
Derivatives of N-carboxyl-thienamycin esters and analogs thereof are found to be potent elastase inhibitors and thereby useful anti-inflammatory agents.
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4493839 |
1-Carbapenem-3-carboxylic esters as anti-inflammatory agents
Derivatives of 1-carbapenem-3-carboxylic esters are found to be potent elastase inhibitors and therefore are useful anti-inflammatory agents.
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4473578 |
β-Lactam antibiotics and their use
The compounds of the formula: ##STR1## and pharmaceutically acceptable salts and in-vivo hydrolysable esters thereof wherein R 1 is a hydrogen atom or a group selected from OH, OSO 3 H or a...
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4446146 |
β-Lactam containing compounds, their preparation and use
The compounds of the formula (II): ##STR1## wherein R 1 is a group such that CO 2 R 1 is a carboxylic acid group or a salt or ester thereof; R 2 is a group of the sub-formula (a) or (b): --CR...
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4444783 |
β-Lactam antibacterial agents, a process for the preparation and use in pharmaceutical compositions
The compounds of the formulaes (IV), (V) and (VI): ##STR1## and salts and esters thereof where X is a bromine or chlorine atom, and n is 0 or 1; are antibacterial agents. Their preparation and use...
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4426390 |
Novel β-lactam compounds, process for producing thereof, and use thereof as medicines
A compound of the formula ##STR1## wherein R 1 represents a hydrogen atom, --OH or --OSO 3 H, and R 2 represents a hydrogen atom or an unsubstituted or substituted benzyl group; and a salt...
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4413000 |
β-Lactam antibiotics, their preparation and use
The present invention provides the compounds of the formula (II): ##STR1## and salts and esters thereof wherein R 3 is a hydrogen atom or is an organic bonded via a carbon atom to the carbapenem...
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4404218 |
Antibiotic SF-2103A substance and process for production thereof
An antibiotic SF-2103A substance or a salt thereof, and a process for the production thereof are described, and the process comprises cultivating an antibiotic SF-2103A substance-producing strain...
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4397861 |
N- And carboxyl derivatives of thienamycin
Disclosed are N-acyl and carboxyl derivatives of the antibiotic thienamycin, which has the following structure: ##STR1## Such derivatives are useful as antibiotics. Also disclosed are processes for...
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4382949 |
2-(Amino acid-thio)-1-carbapen-2-em-3-carboxylic acids and congeners
2-(Amino acid-thio)-1-carbapen-2-em-3-carboxylic acids and congeners having useful antibacterial activity are disclosed. The compounds are prepared in a reaction sequence starting with a...
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4376774 |
Antibiotic N-heterocyclyl thienamycin
This invention relates to a new class of thienamycins (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics: ##STR1## wherein the stylized radical (hereafter...
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4374144 |
β-Lactam compounds, their preparation and use
The present invention relates to the preparation of compounds of the formula: ##STR1## wherein CO 2 R 1 is a free, salted or esterified carboxyl group, n is 0 or 1, and R 2 is hydrogen or an...
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4372965 |
6-, 1- And 2-substituted-thio-1-carbadethiapen-2-em-3-carboxylic acid S-oxides
Disclosed are S-oxides of 6-, 1- and 2-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein: n is 1 or 2; and R 1 , R 6 , R 7 and R 8 are, inter alia,...
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4368203 |
Antibiotics and derivatives thereof having β-lactamase inhibitory activity and production thereof
A novel antibiotic substance of the formula ##STR1## wherein R 1 is CH 3 and R 2 is --CH 2 --CH 2 -- or R 1 is H and R 2 is --CHCH--; and R 3 represents hydrogen, lower alkyl or...
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4341791 |
6-, 2- and 1,1-Disubstituted-1-carbadethiapen-2-em-3-carboxylic acid S-oxides
Disclosed are S-oxides of 6-, 2- and 1,1-disubstituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein: n is 1 or 2; and R 1 , R 2 , R 6 , R 7 and R 8 are, inter...
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4318916 |
Antibiotic PS-5 and derivatives having β-lactamase inhibitory activity and production thereof
A novel antibiotic substance and derivatives thereof, having strong antibiotic activity and β-lactamase inhibiting effect and a method for producing the same by aerobic cultivation of Streptomyces...
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4312871 |
6-, 1- And 2-substituted-1-carbadethiapen-2-em-3-carboxylic acids
Disclosed are 6-, 1- and 2-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein: R 1 , R 2 , R 6 , R 7 and R 8 are, inter alia, independently selected from...
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4281002 |
3-(2-Aminoethylthio)-6-amido-7-oxo-1-azabicyc lo(3.2.0)-hept-2-ene-2-carboxylic acid
Disclosed are 3-(2-aminoethylthio)-6-amido-7-oxo-1-azabicyclo [3.2.0]hept-2-ene-2-carboxylic acids having the structure: ##STR1## wherein R 1 is hydrogen or acyl. Such compounds as well as their...
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4278686 |
Carbapenum derivatives, a process for their preparation and their use in pharmaceutical compositions and intermediates
The present invention provides antibiotic compounds of the formula: ##STR1## and salts and cleavable esters thereof wherein X is a SCH 2 CH 2 NH 2 or YNH-COCH 3 group where Y is a SCH 2 CH 2 ,...
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4277482 |
3-Substituted thio-6-amido-7-oxo-1-azabicyclo[3.2.0]-hept-2-ene-2-carboxylic acid s-oxides
Disclosed are S-oxides of 3-substituted thio-6-amido-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxyli
c acids having the structure: ##STR1## wherein: n is 1 or 2; R 1 is hydrogen or acyl; and R 8 ...
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4264621 |
5-Substituted-3 -(2-aminoethylthio)-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-en e-2-carboxylic acid
Antibiotic 5-substituted-3-(2-aminoethylthio)-6-(1-hydroxyethyl)-7-oxo-
1-azabicyclo[3 .2.0]hept-2-ene-2-carboxylic acids (I) are disclosed: ##STR1## wherein R is alkyl, cycloalkyl,...
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4255441 |
β-Lactam antibiotics, a process for their prepaeration and their use in pharmaceutical compositions
The present invention provides the antibacterial agents of the formula (II): ##STR1## wherein R 1 is a group such that CO 2 R 1 is a carboxylic acid group or a salt thereof or is a group of the...
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4235922 |
3-(2-Aminoethylthio)-6-ethyl-7-oxo-1-azabicyclo [3.2.0]hept-2-ene-2-carboxylic acid
The antibiotic 3-(2-Aminoethylthio)-6-ethyl-7-oxo-1-azabicyclo[3.2.0]hept-2
-ene-2-carboxy lic acid(I) and processes for its preparation are disclosed: ##STR1## Also disclosed are pharmaceutical...
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4235920 |
N-Alkylated derivatives of thienamycin
Disclosed are N-alkylated derivatives of the antibiotic thienamycin, which has the following structure: ##STR1## Such compounds and their pharmaceutically acceptable salt, ester and amide...
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4235917 |
N-Alkyl-N-acyl derivatives of thienamycin
Disclosed are N-alkyl- N-acyl derivatives of the antibiotic thienamycin having the following structural formula: ##STR1## wherein R 1 is, inter alia, alkyl, alkenyl, aryl or aralkyl; and R 2 is...
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4234596 |
3-(2-Aminoethyl thio)-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid
Isomeric forms of 3-(2-aminoethylthio)-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3
.2.0]hept-2-en e-2-carboxylic acid (I) ##STR1## are disclosed; also disclosed is a process for their total synthesis;...
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4232030 |
Substituted N-methylene derivatives of thienamycin sulfoxide and sulfone
Disclosed are substituted N-methylene derivatives of thienamycin sulfoxide (I, n=1) and sulfone (I, n=2) which may be represented by the following structural formula: ##STR1## wherein X and Y are...
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4224336 |
3-(2-Aminoethylthio)-6-amido-7-oxo-1-azabicyclo[3.2.0]- hept-2-ene-2-carboxylic acid
Disclosed are 3-(2-aminoethylthio)-6-amido-7-oxo-1-azabicyclo[3.2.0]hept-2
-ene-2-carboxy lic acids having the structure: ##STR1## wherein R 1 is hydrogen or acyl. Such compounds as well as their...
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4223038 |
Bicyclic β-lactam antibiotics
Compounds of the formula (I): ##STR1## wherein G is hydrogen, alkyl, alkenyl, substituted alkyl or substituted alkenyl, R 1 is alkyl or aryl, substituted alkyl or substituted aryl, and R is an...
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4218462 |
6-(1-Hydroxyethyl)-2-(2-aminoeth ylthio)-1-substituted-1-carbade-thiapen-2-em-3-carboxylic acids
Disclosed are 1-substituted-6-(1-hydroxyethyl)-2-(2-aminoethylthio)-1-carb
adethiapen-2-e m-3-carboxylic acids (I) and their pharmaceutically acceptable salts and esters which are useful as...
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