Abstract: Methods and compositions are disclosed utilizing the optically pure (S)-isomer of lomefloxacin to treat bacterial infection. In particular, this compound is a potent drug for the treatment of Mycobacteria infection.

Abstract: Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of &bgr;-lactamase enzymes.

Abstract: The present invention relates to cephem-derivatives and to a process for their preparation, having proper substituents at C-2 position, i.e. heterocyclylthio or acyloxy group. They are potent protease inhibitors, in particular human leucocyte elastase (HLE) inhibitors.

Abstract: A method for the prophylaxis or treatment of infectious diseases caused by helicobacter pyloir, by administering a pharmacologically effective amount of a 1-methoylcarbapenem coumpund of formula (I) or a pharmacologically acceptable salt or ester thereof: R1 represents a group of the following formula: R2 is a hydrogen atom or a C1-C6 alkyl group, and R3 is a hydrogen atom or a C1-C6 alkyl group.

Abstract: A phloroglucide derivative having the following formula: ##STR1## wherein Q is halogen; X is CH.sub.2 or C.dbd.O; Y is cephalosporin having a formula of ##STR2## wherein Ph is phenyl, Ac is acetoxy, or pharmaceutically acceptable salts thereof, and an antibacterial pharmaceutical composition derived thereof.

Abstract: New 2-oxo-1-azetidine sulfonic acid derivatives with an aminoalkyl substituted "anti" (E-isomer) oxyimino group in the acylamino substituent at the 3 position of the monobactam ring. These compounds are potent inhibitors of bacterial .beta.-lactamases. These compounds can be used in combination with .beta.-lactam antibiotics to increase the effectiveness of the .beta.-lactam antibiotics in fighting infection caused by .beta.-lactamase producing bacteria.

Abstract: The present invention relates to the use of 7-alkylidene derivatives of cephalosporin esters, such as sulfides, sulfoxides, and sulfones, as inhibitors of human leukocyte elastase. These materials are therefore useful as anti-inflammatory and anti-degenerative agents.

Abstract: A dry solid mixture of a hydroxypolycarboxylic acid and a cephalosporin where the hydroxypolycarboxylic acid of the formula ##STR1## where x and y are 0 or 1 and z is 0 to 3, in the weight ration of hydroxypolycarboxylic acid to cephalosporin of at least 1.8. The invention comprises a solution made from the dry solid mixture and a process of treating animals with cephalosporin by including the solution in the water fed to the animals so that the animals can ingest the cephalosporin. A particularly preferred mixture is one of citric acid and cephalexin.

Abstract: Cephalosporins with an exocyclic allene in the 7-position and their pharmaceutically active salts are potent inhibitors of .beta.-lactamases and are therefore useful in the treatment of penicillin resistant infections.

Abstract: The present invention provides a method of diagnosing and treating a pregnant female at risk for impending preterm delivery. The method comprises the step of diagnosing imminent preterm delivery by testing with a method that has a sensitivity of at least 80% and a specificity of at least 80%, or by testing for fetal fibronectin in the female's vaginal or cervical secretions. If imminent preterm delivery is indicated by the test, the next step comprises administering to the female a combination of a tocolytic agent, at least one urinastatin-like compound, and at least one antibiotic. Also provided is a pharmaceutical composition of MGMTSRYFYNGTSMA (SEQ ID NO:1), RAFIQLWAFDAVKGK (SEQ ID NO:2) and an antibiotic.

Abstract: Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of .beta.-lactamase enzymes.

Abstract: Cephalosporins with an exocyclic allene in the 7-position and their pharmaceutically active salts are potent inhibitors of .beta.-lactamases and are therefore useful in the treatment of penicillin resistant infections.

Abstract: The present invention provides cephalosporin sulphones or formula (I), and pharmaceutically or veterinarily acceptable salts thereof; ##STR1## wherein n is zero, one or two; R.sub.1 is hydrogen, halogen or an optionally substituted C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio or C.sub.1 -C.sub.4 carboxamido group;R.sub.2 is hydrogen or an optionally substituted C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.2 -C.sub.5 alkenyl or C.sub.3 -C.sub.6 cycloalkyl group;R.sub.3 is hydrogen or acetoxymethyl, methoxymethyl, methyl or an optionally substituted heterocyclylthiomethyl group;R.sub.4 is an optionally substituted C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.6 alkenyl, aryl(C.sub.1 -C.sub.8)alkyl or heterocyclyl(C.sub.1 -C.sub.8)alkyl group; andR.sub.5 is an optionally substituted C.sub.6 -C.sub.10 aryl or a heterocyclyl group.The compounds of formula I and the pharmaceutically and veterinarily acceptable salts thereof are elastase inhibitors.

Abstract: A method and composition for topically treating acne and acneiform dermal disorders includes applying an amount of a cephalosporin antibiotic effective to treat the acne and acneiform dermal disorders. The antibiotic is blended with a carrier suitable for topical application to dermal tissues. The carrier is selected from the group consisting of an aqueous liquid, an alcohol base, a water soluble gel, a lotion, an ointment, a nonaqueous liquid base, a mineral oil base, a blend of mineral oil and petrolatum, liposomes, a time-release patch, and a liquid-absorbed wipe. The cephalosporin can also be combined with benzoyl peroxide in a gel carrier.

Abstract: A method of killing microorganisms which form a biofilm on a tissue or implant surfaces in a patient, and which are refractory to a biocide at a dose which is effective to kill the microorganism in planktonic form. The effect of the biocide is potentiated, to an effective killing level, by applying an electric field across the surface containing the biofilm.

Abstract: The invention relates to a novel stable form of cephradine, processes for its production and intermediates used therein.

Abstract: New cycloalkano[b]dihydroindoles and -indolesulphonamides, substituted by heterocycles, of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different andrepresent hydrogen, nitro, cyano, halogen, trifluoromethyl, carboxyl, hydroxyl or trifluoromethoxy, orrepresent a group of the formula --S(O).sub.w R.sup.5, in whichR.sup.5 denotes alkyl or optionally substituted aryl,w denotes the number 0, 1 or 2, orrepresents alkoxy or alkoxycarbonyl, or benzyloxy, orrepresents a group of the formula --NR.sup.6 R.sup.7, in whichR.sup.6 and R.sup.7 are identical or different anddenote hydrogen, alkyl or acyl ordenote aryl, ordenote a group of the formula --S(O).sub.w R.sup.5, in which R.sup.

Abstract: Anti-thrombobenic, anti-microbial compositions containing heparin reacted with quaternary ammonium components and bound with water-insoluble polymers are disclosed. Such compositions may also contain additional quaternary ammonium compounds not reacted with heparin and may also contain quaternary ammonium compound(s) reacted with antibiotics.

Abstract: Cephalosporin compounds of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and are a hydrogen atom or a lower alkyl group of 1-5 carbon atoms and A is a hydrogen atom or a nucleophilic compound residue or pharmacologically acceptable salts thereof have excellent antibacterial activity against Gram positive and Gram negative microorganisms.

Abstract: This invention provides cephalosporin compounds represented by the following general formula: ##STR1## wherein R.sup.1 and R.sup.2 are same or different hydrogen atom or a lower alkyl group of 1 to 5 carbon atoms; R.sup.3 is a lower alkyl group which may optionally be substituted with a halogen atome (or atoms), an alkenyl group, or a cycloalkylmethyl group of 3 to 6 carbon atoms; and A is hydrogen atom or residue of a nucleophilic compound and pharmacologically acceptable salts thereof. These compounds have broad-spectrum antibacterial activity against Gram-positive and -negative bacteria including Pseudomonas aeruginosa, as well as against a great variety of .beta.-lactamase-producing strains.

Abstract: Antibacterially active novel cephalosporins of the formula ##STR1## in which R.sup.1 represents alkyl, alkenyl, alkoxy, alkylthio, halogen, trifluoromethyl or trifluoromethoxy,R.sup.2 represents hydrogen or an organic radical,R.sup.3 represents hydrogen, alkyl, alkenyl, alkoxy, alkylthio, halogen, hydroxymethyl or ethers or esters thereof, or various organothiomethyl or substituted aminomethyl radicals, andR.sup.4 represents COO.sup.- or COOH, or salts thereof.

Abstract: Acylcarnitine used as a nasal, buccal, sublingual and vaginal drug absorption enhancing vehicle for poorly absorbed drugs.

Abstract: Choline ester salts are used as drug absorption enhancing agents for orally and rectally administered drugs.

Abstract: Cephalosporin esters of the formula ##STR1## wherein R.sup.2 is hydrogen or acyl and R.sup.1 is a group which is readily removable by hydrolysis,and pharmaceutically acceptable acid addition salts of basic compounds of formula I in which R.sup.2 is an acyl group, may be prepared by reacting 7-amino-3-methyl-3-cephem-4-carboxylic acid (7-ADCA) in a partially chlorinated lower alkane with a bicyclic amidine of the formula ##STR2## wherein n is the integer 3, 4 or 5, and a halide of the formulaX--R.sup.1 IIIwherein X is halogen and R.sup.1 has the above significance,if desired, treating the resulting compound of formula I in which R.sup.2 is hydrogen with an unprotected or optionally protected acylating agent, cleaving off a protecting group which may be present and, if desired, treating a resulting basic compound of formula I in which R.sup.2 is an acyl group into a pharmaceutically acceptable acid addition salt.

Abstract: Choline esters are used as drug absorption enhancing agents for drugs which are poorly absorbed from the nasal, oral, and vaginal cavities.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 stands for hydrogen or formylamino, R.sup.2 is a residue of amino acid selected from the group consisting of serine and alanine, or a peptide of at least one of these amino acids, or hydrogen, R.sup.3 stands for --NH--C(.dbd.NH)--NH.sub.2 or --CH.sub.2 NH.sub.2, or its salt, which can be produced by cultivating a microorganism belonging to the genus Xanthomonas, is useful as a therapeutic agent against infectious disease caused by bacteria.

Abstract: This invention relates to the hybridization of streptolydigin, tirandamycin and sorbic acid to penicillin and cephalosporin nuclei.

Abstract: 1. A cephalosporin derivatives of the general formula ##STR1## wherein R.sup.1 is an .alpha.-, .beta.- or .gamma.-amino acid residue (bonded by the ester linkage), which may optionally be substituted by one or two lower alkyl groups at the amino group thereof, R.sup.2 is an 1-alkanoyloxyalkyl, 1-alkoxycarbonyloxyalkyl, phthalidyl or 5-methyl-1,3-dioxolen-2-on-4-ylmethyl group, R.sup.3 is a carbamoyloxymethyl group, which may optionally be substituted by one or two lower alkyl groups, or a heterocyclothiomethyl group, which may optionally be substituted by one or more appropriate substituents, and R.sup.4 is a hydrogen atom or a hydroxy group, or its non-toxic salt are found to be useful as orally administrable antibiotics having broad antimicrobial activities against both gram-positive and gram-negative bacteria.

Abstract: 3-[(Z)-1-Propen-1-yl]-7-acylamido cephalosporins in which the 7-acyl group is phenylglycyl or substituted phenylglycyl are orally active antibiotics against Gram+ and Gram- bacteria.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 stands for hydrogen or formylamino, R.sup.2 stands for hydrogen, alanyl or alanyl-alanyl, or its salt, which can be produced by cultivating a microorganism belonging to the genus Lysobacter, is useful as a therapeutic agent against infectious disease caused by bacteria.

Abstract: A cephalosporin derivative having an antibacterial activity similar to a cephalosporin antibiotic in living bodies without affecting the intestinal bacterial colonies, a method for preparing the derivative and a pharmaceutical composition in a dosage unit form containing the derivative as an active ingredient are disclosed.