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4956358 |
Tricyclic cepham compounds and use
The compounds having a 4,11-dioxo-3-oxa-8(or 7)-thia-1-azatricyclo[7,2,0,0 2 ,6 ]undecane-2-carboxylic acid skeleton as the base structures, their esters and their salts are useful antibacterial...
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4861768 |
2 β-substituted thiomethylpenicillin derivatives and their preparation and use
Disclosed is a penicillin derivative of the formula: ##STR1## wherein n is an integer of 0, 1 or 2; Y is a cyano group, a lower acyl group, a mono- or di-lower alkylthiocarbamoyl group, ##STR2##...
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4803196 |
Pharmaceutical compositions containing β-lactam antibiotics
A solid pharmaceutical composition comprising one or more β-lactam antibiotics in acid or amphoteric form in association with at least one physiologically acceptable base in the presence of a...
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4760060 |
3-heteroaralkylthio carbacephem compounds and antibacterial pharmaceutical composition
Carbacephem and cephem compounds represented by the formula: ##STR1## [Wherein X is S or CH 2 ; n is an integer of 1 to 5; R 1 is an unsubstituted or substituted heterocyclic group (where the...
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4760059 |
Rectal dosage form
The rectal absorption of the beta-lactam antibiotic ceftriaxone in a solid dosage form is enhanced with chenodeoxycholic acid or its sodium salt, in the presence of a carrier consisting of a...
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4749694 |
Novel lysine esters used as absorption
Novel lysine esters used as absorption enhancing agents for gastrointestinally and rectally administered drugs. Also provided are processes for preparation of said lysine ester compounds as well as...
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4735937 |
8-oxo-5-thia-1-azabicyclo(4,2,0)oct-2-ene compounds
The invention concerns 7-amino-ceph-3-em-4-carboxylic acid compounds of the formula ##STR1## wherein R 1 a represents hydrogen or an amino protective group R 1 A and R 1 b represent hydrogen or...
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4732753 |
Suppository dosage form
Suppositories containing as the active substance a therapeutically effective amount of ceftriaxone, a pharmaceutically compatible salt thereof or a hydrate of one of these compounds, a stabilizer...
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4725591 |
β-lactamase inhibitory composition
Compounds having one or two substituents at the 3-position, represented by the general formula ##STR1## wherein R 1 is an optionally acylated or protected amino group and X is hydrogen atom or...
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4713247 |
Long-acting formulation of cefaclor
Highly potent long-acting formulation of cefaclor for treating bacterial infections in human or animals, comprising a rapid-release and a slow-release component at a ratio of about 3:7 to about 5:5...
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4695467 |
Sustained release tablet
The invention relates to a sustained release tablet which comprises easily disintegrable granules containing (a) a drug, (b) a disintegrating agent selected from the group consisting of...
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4692441 |
Chorine esters as absorption-enhancing agents for drug delivery through mucous membranes of the nasal, buccal, sublingual and vaginal cavities
Choline esters are used as drug absorption enhancing agents for drugs which are poorly absorbed from the nasal, oral, and vaginal cavities.
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4668504 |
Use of substituted propenoates to prevent nephrotoxicity of certain antibiotics
Antibiotics to prevent nephrotoxicity.
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4666899 |
3-(Optionally substituted-but-1-en-3-ynyl) cephalosporins
Compounds of general formula I ##STR1## (wherein R represents NH 2 -- or an acylated or silylated amino group; R 2 represents a hydrogen, halogen, alkyl, aryl, carboxyl or lower alkoxycarbonyl...
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4637999 |
Substituted cephalosporins as anti-inflammatory and antidegenerative agents
Substituted cephalosporins are found to be potent elastase inhibitors and thereby useful antiinflammatory/antidegenerative agents.
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4631274 |
Halovinyl cephem compounds
The invention relates to novel halovinyl cephem derivatives of high antimicrobial activity of the formula: ##STR1## wherein R 1 is a group of the formula: R 4 --A--CONH-- in which R 4 is...
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4623645 |
Substituted cephalosporin sulfoxides as anti-inflammatory and antidegenerative agents
Substituted cephalosporin sulfoxides are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.
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4622318 |
3-(substituted-ethenyl or ethynyl-thiomethyl) cephems
The invention relates to new cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R 1 is amino or a group of the formula: ##STR2## in which R 5 is amino or a protected...
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4619925 |
3-Propenyl cephalosporin derivatives
The present invention relates to 7-[(D)-2-amino-2-(3-hydroxyphenyl)acetamido]-3-[(Z)-1-propen
yl]-3-cephem-4 -carboxylic acid, which is an orally active antibiotic against Gram-positive and...
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4616008 |
Antibacterial solid composition for oral administration
This invention relates to an antibacterial solid composition for oral administration which comprises a lipid soluble cephalosporin compound and a cyclodextrin. The said composition provides much...
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4605651 |
Antibiotic amino acid derivatives of cephalosporins
1. A cephalosporin derivatives of the general formula ##STR1## wherein R 1 is an α-, β- or γ-amino acid residue (bonded by the ester linkage), which may optionally be substituted by one or two...
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4604386 |
3-(alkynylalkyloxy) cephalosporins
3-(alkynylalkyloxy)cephalosporin antibiotics and the intermediates therefor are disclosed. Pharmaceutical compositions for the antibiotics are also disclosed.
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4603050 |
Method for medical treatment of bone tissue defects
The method disclosed herein is applicable in traumatology for treatment of infected false joints, as well as some forms of osteomyelitis. The method consists in administering medicinal solutions to...
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4594246 |
Pharmaceutically-acceptable amine salts of 6-β-halopenicillanic acids
This invention relates to penicillanic acid derviatives of the formula I ##STR1## in which X stands for chlorine, bromine or iodine, to pharmaceutically acceptable, non-toxic salts of the compounds...
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4571334 |
Composition for curing respiratory diseases
A composition for curing respiratory diseases which contains a medicine such as antibiotic, chemotherapeutic and anticancer drug for respiratory disease and lung surfactant.
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4525339 |
Enteric coated oral dosage form
There is presented a method, in the form of a dosage formulation, for transforming substantially orally inactive β-lactam antibiotics or their pharmaceutically acceptable salts or the esters,...
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4524073 |
β-Lactam compounds
A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R represents an alkyl or aralkyl group, substituted on an alkyl carbon atom...
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4501734 |
Promotion of absorption of drugs administered through the alimentary system
An extract from a saponin-containing galenical has the effect of promoting absorption of a pharmacologically active substance or drug such as β-lactam antibiotic administered through the...
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4490370 |
Naphthylglycyl cephalosporin derivatives
Naphthylglycyl and tetrahydronaphthylglycyl cephalosporins are potent antibacterial agents and are particularly useful as oral treatments for upper respiratory infections.
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4425337 |
Adjuvants for rectal delivery of drug
A method and drug form enhancing the rate of absorption of a rectally administered drug from the rectal compartment into the blood stream of a warm blooded animal. The method includes the steps of...
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4421760 |
β-Lactam antibiotic, its preparation and use
The compound of the formula (VI): ##STR1## pharmaceutically acceptable salts and pharmaceutically acceptable esters thereof, are useful for their antibacterial activity and for their β-lactamase...
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4406896 |
Adjuvants for rectal delivery of drug substances
A method and drug form for enhancing the rate of absorption of a rectally administered drug from the rectal compartment into the blood stream of a warm blooded animal. The method includes the steps...
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4381307 |
Soft tertiary amine esters of bio-affecting carboxylic acids
Novel derivatives of known bio-affecting carboxylic acids R-COOH are disclosed, said derivatives having the structural formula ##STR1## wherein Y and Y' are each H or C 1 -C 4 alkyl; n is 0 or 1;...
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4376767 |
Pyridylmethyl esters of selected bio-affecting carboxylic acids
Novel pharmaceutically useful derivatives of selected known bio-affecting carboxylic acids are disclosed, said derivatives having the structural formula ##STR1## wherein R 1 and R 2 , which can be...
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4363807 |
Cepham compounds
This invention relates to novel cepham compounds of antimicrobial activity, useful as intermediates in the preparation of antibiotics, said novel cepham compounds being of the formula: ##STR1##...
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4352800 |
Adjuvant for promoting absorption of therapeutically active substances through the digestive tract
The enamine derivatives having following formula ##STR1## promote absorption of therapeutically active substances through the digestive tract into the blood stream and are able to effectively...
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4342760 |
Cephalosporin analogues
The invention deals with Cephalosporin Analogues of the formula: ##STR1## wherein R 1 is amino or amino substituted with a pharmaceutically acceptable carboxylic acyl protective group for the...
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4267177 |
β-Lactam anti-bacterials, compositions containing them, a process for their preparation, and methods of use thereof
The compounds of the formula (II): ##STR1## and salts and esters thereof wherein R 1 is a pyridyl group optionally substituted by one of two lower alkyl groups or lower acyloxy group, have been...
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4264597 |
Cephalosporin analogues and processes for the preparation thereof
Compounds of the formula ##STR1## wherein X is --O--or --S--; R 1 is amino or a substituted amino group; R 2 is carboxy or a protected carboxy group; and the heavy solid line means single...
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4258040 |
Cephalosporin compounds
Novel cephalosporin compounds having a 3'-α-methyl, a 3-aryl or 3-heterocycle substituent are prepared by total synthesis. The novel cephalosporin compounds are active against gram-negative and...
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4254117 |
7-(α,α-Disubstituted-acetemido)-3-substituted-3-cephem-4-carb oxylic acids
7-(2-Hydroxyimino-2-hydroxyphenyl-acetamido)-3-substituted-3
-cephem-4-carbo xylic acids are disclosed which possess an antibacterial activity.
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4137317 |
Glycerides with antibacterial properties
Triglycerides carrying an anti-bacterial drug moiety in the 2-position and a hydrocarbon acyl moiety in the 1- and 3-positions exhibit excellent anti-bacterial properties without causing the side...
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4132790 |
Antibiotic A16886II
Antibiotic A16886I and antibiotic A16886II and their salts, having antibacterial and anthelmintic activity, prepared by fermentation of Streptomyces clavuligerus NRRL 3585.
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4112087 |
Cephalosporin type antibacterials having a substituted propenyl group in the 3-position
Compounds of the formula ##STR1## wherein R is alkyl having 1 to 4 carbon atoms, β-haloethyl, allyl, propargyl, cyclopentyl or benzyl; R 1 is hydrogen or an α-substituted acetamido group; R 2 ...
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4094978 |
3-Propenyl derivatives of cephalosporin, compositions and their use
3-(3-hydroxyprop-1-(t)-enyl)-7β-(α-substituted acetamido)-ceph-3-em-4-carboxylic acids; 3-(3-carbamoyloxyprop-1-(t)-enyl)-7β-(α-substituted acetamido)-ceph-3-em-4-carboxylic acids; and...
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4089955 |
7-β-[D-2-Amino-2-(1,4-cyclo hexadienyl)-acetylamino]-3-Hal-3-cephem-4-carboxylic acids
7β-[D-2-Amino-2-(1,4-cyclohexadienyl)-acetylamino]-3-Hal-3-
cephem-4-ca rboxylic acids, wherein Hal denotes halogen with an atomic number of up to 35, and pharmaceutically acceptable salts thereof...
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4073902 |
O-Substituted 7β-amino-3-cephem-3-ol-4-carboxylic acid compounds
The invention relates to O-substituted 7β-amino-3-cephem-3-ol-4-carboxylic acid compounds of the formula ##STR1## wherein X represents amino or substituted amino, R 2 represents hydroxyl or a...
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4067977 |
α-AMINO-α-(UREIDOPHENYL)ACETAMIDOCEPHALOSPORINS AND THEIR PHARMACEUTICAL COMPOSITIONS
Cephalosporins with a α-amino-(ureidophenyl)acetamido substituent at position 7 are prepared by acylation of a 7-aminocephalosporin with a derivative of α-amino-p(or m)-ureidophenylacetic acid....
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4060611 |
3-Carbamylbenzyl-7-(phenylglycyl)amino cephalosporin derivatives
Antibacterial 3-carbamoylbenzyl cephems and 3-(carbamoylpyridylmethyl) cephems, pharmaceutically acceptable salts and in vivo hydrolyzable esters thereof; pharmaceutical compositions containing...
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3988450 |
Cephalosporins
Cephalosporin analogues of the formula (I): ##SPC1## and their salts and in-vivo hydrolysable esters (wherein R is an acyl group as found in known antibacterially active penicillins and...
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