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 use is described of both (i) ranitidine bismuth citrate and (ii) one or more Helicobacter pylori-inhibiting antibiotics in treating or preventing gastrointestinal disorders.Pharmaceutical compositions containing both (i) and (ii) and methods for the preparation of pharmaceutical compositions containing (i) and (ii) are also described.

Abstract: Compounds represented by the following formula (I), that is, cephem derivatives having substituted or unsubstituted 3-(imidazo[5,1-b]thiazolium-6-yl)-1-propenyl as a substituent at the 3-position of the cephem ring: ##STR1##

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: Disclosed is a pharmaceutical composition intended for the topical application to human skin, comprising(A) as an effective ingredient, a mixture comprising(1) an antibiotic medication;(2) an antihistamine; and(B) a physiologically acceptable carrier.Also disclosed is a method for treatment using this composition.

Abstract: A formulation comprising amoxycillin or a veterinarily acceptable derivative thereof, clavulanic acid or a veterinarily acceptable derivative thereof, and a veterinarily acceptable carrier is used in the treatment of farrowing fever and/or bacterial pneumonia in pigs.

Abstract: .beta.-Phenethanolamines are effective in promoting growth and improving feed efficiency and leanness in animals.

Abstract: A cosmetic composition for treating skin includes by weight percent from 50-99.5% cosmetically acceptable vehicle for topical administration, 0.5-20% collagenase/elastase inhibitor, 0-10% moisturizer, 0-25% emollient, 0-10% humectant and 0-0.5% fragrance. A method for treating skin to reduce evidence of wrinkles and aging includes topically applying a cosmetic composition including a cosmetically effective amount of a collagenase/elastase inhibitor as an active ingredient.

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 compounds of formula (I) and pharmaceutically or veterinarily salts thereof; ##STR1## wherein R.sub.1 is hydrogen or halogen or an organic group; R.sub.2 is hydrogen or an optionally substituted C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.14 aralkyl group;R.sub.3 is hydrogen or halogen, or an organic groupR.sub.4 is hydrogen or a group defined as R.sub.2 above or R.sub.4 taken together with R.sub.3 constitutes a C.sub.2 -C.sub.6 alkanediyl or an alkanediyl radical optionally substituted by methyl or phenyland X is either oxygen or sulphur or NR.sub.6, wherein R.sub.6 is either hydrogen or a group as defined for R.sub.2. A process for their preparation by cyclization of appropriate intermediates is also described.The compounds of formula I and the pharmaceutically and veterinarily acceptable salts thereof are elastase inhibitors.

Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.

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: The present invention provides a method of inhibiting protein kinase C in a mammal having a tumor system which contains protein kinase C, which mammal is undergoing cytostatic therapy. The method comprises administering to the mammal a protein kinase C inhibitor.

Abstract: Thrombin inhibitors are provided which have the formula ##STR1## wherein Z is a thrombin inhibitor substructure containing distal and proximal binding site residues; andR.sup.1 is cyano, hydroxyl, alkoxy, amino, aminoalkyl or nitro.

Abstract: The present invention provides a method for inhibiting endometriosis comprising administering to a woman in need of treatment an effective amount of a compound of formula I ##STR1## wherein R is hydrogen or methyl;R.sup.1 and R.sup.2 each are methyl or ethy, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached represent a saturated heterocyclic group; andX is bromo, chloro, fluoro, or hydrogen; or a pharmaceutically acceptable salt thereof.

Abstract: The oral delivery of many classes of drugs is facilitated by converting drugs having suitable functional groups to 1-O-alkyl-, 1-O-acyl-, 1-S-acyl, and 1-S-alkyl-sn-glycero-3-phosphate derivatives. The method confers the ability to be absorbed through the digestive tract to drugs that are not orally bioavailable in the non-derivatized state, and enhances the effectiveness of drugs that are poorly absorbed or rapidly eliminated. The method provides orally bioavailable lipid prodrugs of zaxol and taxol-related compounds. Potency of the lipid prodrugs is comparable to that of the corresponding nonderivatized drugs. In a preferred embodiment, taxol or substituted taxol is covalently bound to a phospholipid.

Abstract: The invention relates to various methodologies for diagnosing Kawasaki syndrome. Various bacteria, including TSST-1 producing Staphylococcus aureus, and SPEB and SPEC producing streptococcus have been found to be indicative of the pathological condition. Also described is a Kawasaki syndrome implicated isolate of S. aureus, and therapeutic methodologies for preventing treating the condition. These involve the administration of anti-TSST-1 agents which are not gamma globulin.

Abstract: 2-spiro (2'-spirocycloalkyl) cyclopropyl cephalosporin sulfone compounds, methods of treating patients for elastase inhibition, and processes for preparing such compounds.

Abstract: The oral delivery of many classes of drugs is facilitated by converting drugs having suitable functional groups to 1-O-alkyl-, 1-O-acyl-, 1-S-acyl, and 1-S-alkyl-sn-glycero-3-phosphate derivatives. The method confers the ability to be absorbed through the digestive tract to drugs that are not orally bioavailable in the non-derivatized state, and enhances the effectiveness of drugs that are poorly absorbed or rapidly eliminated. The method provides orally bioavailable lipid prodrugs of pharmaceutical compounds having diverse physiological activities, including anticancer and antiviral agents, anti-inflammatory agents, antihypertensives and antibiotics. Potency of the lipid prodrugs is comparable to that of the corresponding non-derivatized drugs.

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: Inhibitors of sex steroid activity, for example those having the general structure ##STR1## may be used as part of a pharmaceutical composition to provide antiestrogenic effects and/or to suppress estrogen synthesis. Such pharmaceutical compositions are useful for the treatment of breast cancer or other diseases whose progress is aided by activation of sex steroid receptors.

Abstract: There are provided compounds I ##STR1## wherein A is a hydrogen atom or an organic group,R.sub.1 is hydrogen or halogen atom or an organic group,R.sub.2 is hydrogen or halogen atom, C.sub.1 -C.sub.4 alkyl or acyloxy group,R.sub.3 is hydrogen atom, C.sub.1 -C.sub.4 alkyl or alkoxy, benzyl group or a methylene andR.sub.4 is chloro, fluoro, hydrogen atom or an organic group.The compounds I are elastase inhibitors. A process for their preparation is also provided, as are pharmaceutical compositions containing them.

Abstract: A cephalosporinase testing agent comprising a cephalosporin antibiotic, a penicillinase inhibitor in an amount of 20% by weight or less based on the weight of the cephalosporin-antibiotic, and a pH indicator which may be bromcresol purple is provided. A cephalosporinase producing bacteria can be judged by smearing a sample containing bacteria to be tested on the testing agent and observing the color tone change. According to this agent, cephalosporinase-active penicillinase producing bacteria are judged cephalosporinase-negative owing to the action of the penicillinase inhibitor, which may be clavulanic acid. Therefore, since only cephalosporinase producing bacteria are judged cephalosporinase-positive, this agent enables error free judgment.

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: A novel colorimetric method for beta-lactamase assay and its applications are disclosed. The novel assay method for beta-lactamase is based on the discovery described in this invention. The chromophore formed by oxidation of either the N-alkyl derivative of p-phenylenediamine or the 3,3',5,5'-tetraalkyl derivative of benzidine can be decolorized by the open beta-lactam ring end product resulting from the hydrolysis of a penicillin in the presence of a mercury-containing compound. The same chromophore can be decolorized by the open beta-lactam ring end product resulting from the hydrolysis of a cephalosporin in either the presence or the absence of the mercury-containing compound. None of the intact beta-lactam antibiotics can decolorize the chromophore in either the presence or the absence of the mercury-containing compound. The final concentration of the mercury-containing compound in the decolorization mixture ranges from approximately 0.

Abstract: Methods, for the treatment of humans and lower animal subjects having a gastrointestinal disorder, comprising administering bismuth and administering an antimicrobial. From about 50 to about 5000 milligrams of bismuth are administered, per day, for from 3 to 56 days. A safe and effective amount of antimicrobial is administered for from 1 to 21 days. Preferred processes also include a step for performing a diagnostic test on the subject for detection of a campylobacter-like organism infection of the subject. The invention also provides compositions containing a safe and effective amount of bismuth and a safe and effective amount of antimicrobial.

Abstract: Lactoferrin can be used to increase the efficacy of beta-lactam antibiotics. There is a potentiating effect when lactoferrin is administered either simultaneous with or shortly before or after the administration of beta-lactam antibiotics. The dosage of lactoferrin administered is usually 0.5-100 mg/kg and preferably 1-10 mg/kg.

Abstract: Oral pharmaceutical compositions in unit dosage form suitable for swallowing (especially capsules) comprising a safe and effective amount of solid Colloidal Bismuth Subcitrate (CBS), and optionally one or more pharmaceutically-acceptable carrier materials, wherein the packing density of the dosage unit is less than about 1 g/ml.

Abstract: The absorption of antibiotics given through oral and rectal routes of administration is significantly enhanced by use of the antibiotic in conjunction with a two-component absorption enhancing system made up of an ether of a C.sub.6 to C.sub.18 alcohol and a polyoxyethylene glycol together with a second component selected from among polyoxyethylene glycol C.sub.6 to C.sub.18 glyceride esters, C.sub.6 to C.sub.18 carboxylic acids or salts thereof, and esters of two or more C.sub.6 to C.sub.18 carboxylic acids, glycerol and a polyoxyethylene glycol. A carrier and adjuvants are usually included. These compositions can be administered in any convenient oral or rectal dosage form, including tablets, capsules, beadlets and suppositories.

Abstract: Process for the preparation of 7.beta.-amino-3-substituted methyl-3-cephem-4-carboxylic acid derivatives, new intermediates comprising 7.beta.-(cyclo)alkylideneammonio-3-halomethyl-3-cephem-4-carbox ylic acid derivatives and 7.beta.-amino/ammonio-3-bromomethyl-3-cephem-4-carboxylic acid derivatives and the processes for the preparation of these intermediates.

Abstract: An unpressurized container containing a palatable pharmaceutical formulation comprising a homogeneous, non-aqueous suspension of an orally active medicament, an edible oily vehicle, an edible emulsifier and a finely particulate sugar having no oily after taste.

Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are:(a) compounds of the formula[D-DHC] (I)wherein [D] is a centrally acting drug species, and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine.revreaction.pyridinium salt redox carrier, with the proviso that when [DHC] is ##STR1## wherein R is a lower alkyl or benzyl and [D] is a drug species containing a single NH.sub.2 or OH functional group, the single OH group when present being a primary or secondary OH group, said drug species being linked directly through said NH.sub.

Abstract: This invention provides compositions comprising a physiologically-active agent and a compound having the structural formula ##STR1## Wherein X may represent sulfur or two hydrogen atoms; R' is H or a lower alkyl group having 1-4 carbon atoms; m is 2-6; n is 0-18 and R is --Ch.sub.3, ##STR2## wherein R" is H or halogen, in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.

Abstract: The compounds having a 4,11-dioxo-3-oxa-8(or 7)-thia-1-azatricyclo[7,2,0,0.sup.2,6 ]undecane-2-carboxylic acid skeleton as the base structures, their esters and their salts are useful antibacterial agents.

Abstract: 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## wherein R.sub.1 is a hydrogen atom, a lower alkyl group, a phenyl group, a group --(CH.sub.2).sub.m --OR.sub.2 or --(CH.sub.2).sub.m COOR.sub.2 (m is an integer of 1 to 6 and R.sub.2 is a hydrogen atom or a penicillin carboxyl ester-forming group which is commonly used for penicillin derivatives) or a phenyl group substituted by at least one member selected from the class consisting of lower alkyl group, halogen atom and lower alkoxy group; and R is a hydrogen atom or a penicillin carboxyl ester-forming group, or a salt thereof. They are useful as .beta.-lactamase inhibitors.

Abstract: A solid pharmaceutical composition comprising one or more .beta.-lactam antibiotics in acid or amphoteric form in association with at least one physiologically acceptable base in the presence of a gaseous atmosphere containing a stabilizing amount of carbon dioxide at a concentration greater than that of atmospheric air. The compositions exhibit enhanced stability. A preferred antibiotic for the compositions is ceftazidime or a hydrate thereof, and a preferred base is sodium cabonate or a mixture thereof with one or more other bases.

Abstract: 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 mixture of two or more glycerides of C.sub.12 to C.sub.18 fatty acids.

Abstract: Carbacephem and cephem compounds represented by the formula: ##STR1## [Wherein X is S or CH.sub.2 ; n is an integer of 1 to 5; R.sub.1 is an unsubstituted or substituted heterocyclic group (where the heterocyclic group is a 5- or 6-membered heterocyclic group having 1 to 4 of O, S and N); R.sub.2 is a group represented by the formula: ##STR2## (where R.sub.4 is an unsubstituted or substituted phenyl or 2-aminothiazolyl) or a group represented by the formula: ##STR3## (where R.sub.5 is an unsubstituted or substituted lower alkyl); R.sub.3 is hydrogen, an alkali metal, an alkaline earth metal, an organic ammonium group or an ester residue, and R.sub.1 may be a quaternary ammonium group, where --CO.sub.2 R.sub.3 represents --CO.sub.2.sup.- ] have strong antibacterial activity against Gram-positive and Gram-negative bacteria, and are useful for treating various infections.

Abstract: 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 pharmaceutical formulations and methods for their use as absorption enhancing agents.

Abstract: The invention concerns 7-amino-ceph-3-em-4-carboxylic acid compounds of the formula ##STR1## wherein R.sub.1.sup.a represents hydrogen or an amino protective group R.sub.1.sup.A and R.sub.1.sup.b represent hydrogen or an acyl group AC, or R.sub.1.sup.A and R.sub.1.sup.b together denote a bivalent amino protective group, and R.sub.2 represents hydrogen or an organic radical R.sub.2.sup.A which together with the --C(.dbd.O)--O-- grouping forms a protected carboxyl group, or salts such compounds which possess salt-forming groups; these compounds have antibiotic properties.

Abstract: 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 consisting of a mono-, di- or triglyceride of a C.sub.12 -C.sub.18 -fatty acid or of a mixture of such glycerides, a potentiator consisting of an aliphatic C.sub.2 -C.sub.18 -fatty acid, a mono-, di- or triglyceride of a C.sub.2 -C.sub.12 -fatty acid, a partial ester or complete ester of propylene glycol, polyethylene glycol or a carbohydrate with a C.sub.2 -C.sub.12 -fatty acid, a pharmaceutically compatible ester or ether thereof or of a mixutre of the said potentiators and, if desired, customary therapeutically inert adjuvants for suppositories, and their manufacture are described. These have valuable antimicrobial properties.

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: Compounds having one or two substituents at the 3-position, represented by the general formula ##STR1## wherein R.sub.1 is an optionally acylated or protected amino group and X is hydrogen atom or methoxy group, or a pharmaceutically acceptable salt thereof; when used either alone or in combination with a .beta.-lactam antibiotic, show excellent .beta.-lactamase inhibitory activity and can be used as drugs for use in humans and domestic animals.

Abstract: 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 by potency of cefaclor, convenient for administration or carrying about.

Abstract: 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 starch derivatives, gums, cellulose derivatives and ion-exchange resins, and(c) a water soluble polymer selected from the group consisting of cellulose derivatives, synthetic water soluble polymers and polysaccharides, the surfaces of which granules are treated solely with a wax selected from the group consisting of plant or animal wax, hydrogenated oils and paraffin.

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 cephalosporin derivative of the formula I: ##STR1## in which X is S, O, CH.sub.2 or SO, R1 is (optionally-substituted)imidazol-2-yl or one of the C-7 acyl groups known in the cephalosporin art, R2 is hydrogen or methoxy, R3 is carboxy or a biodegradable ester thereof and --R4 is of the formula XII, XIII or XIV: ##STR2## in which R32-R40 inclusive are as defined in the specification; and the salts thereof. Pharmaceutical compositions, methods of manufacture and intermediates are also described.

Abstract: Compounds of general formula I ##STR1## (wherein R represents NH.sub.2 -- or an acylated or silylated amino group;R.sup.2 represents a hydrogen, halogen, alkyl, aryl, carboxyl or lower alkoxycarbonyl group;R.sup.3 is hydrogen or a carboxyl blocking group;B is >Sor>S.fwdarw.O (.alpha.- or .beta.-); and the dotted line represents .DELTA..sup.2 or .DELTA..sup.3 unsaturation) and salts, solvates and esters thereof are described.Compounds where R.sup.3 is hydrogen, the dotted line represents .DELTA..sup.3 unsaturation and R is a group of formula ##STR2## (where R.sup.a is an optionally substituted heterocyclic aryl group having one or more hetero atoms selected from S, N and O in the ring, R.sup.b is an optionally substituted aryl group, R.sup.c is hydrogen, acyl, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.d is as defined for R.sup.

Abstract: Substituted cephalosporins are found to be potent elastase inhibitors and thereby useful antiinflammatory/antidegenerative agents.