Abstract: .alpha.- Phosphonocarboxylate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.1 is a lipophilic group which contains at least 7 carbons and is substituted alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted arylalkyl or optionally substituted aryl;Z is H, halogen, hydroxy, hydroxyalkyl or lower alkyl;R.sup.2 and R.sup.3 are independently H, metal ion or other pharmaceutically acceptable cation, or a prodrug ester;R.sup.4 is H, metal ion or other pharmaceutically acceptable cation, lower alkyl, lower alkenyl, arylalkyl, aryl or a prodrug ester.

Abstract: Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents are provided which have the structure ##STR1## wherein m is 0, 1, 2 or 3; n is 0, 1, 2, 3 or 4;Y.sup.1 and Y.sup.2 are H or halogen;R.sup.2, R.sup.3 and R.sup.4 may be the same or different and are independently H, metal ion, C.sub.1 to C.sub.8 alkyl or C.sub.3 to C.sub.12 alkenyl;X is O, S, NH or NCH.sub.2 R.sup.15 wherein R.sup.15 is H or C.sub.1 to C.sub.5 alkyl; andR.sup.1 is R.sup.5 --Q.sup.1 --Q.sup.2 --Q.sup.3 -- wherein R.sup.5, Q.sup.1, Q.sup.2 and Q.sup.3 are as defined herein;and when m is o, X is other than S; and if m is o and X is O, then n is 1, 2, 3 or 4; including all stereoisomers thereof.

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: Hydroxyphosphinyl phosphonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2, R.sup.3 and R.sup.4 are independently H, alkyl, metal ion or a prodrug ester; and R.sup.1 is a lipophilic group which contains at least 6 carbons and is alkyl, alkenyl, alkynyl, mixed alkenylalkynyl, a hetero-containing moiety as defined herein, or a phenylalkyl or phenylalkenyl group including those containing a biphenyl group.

Abstract: A pharmaceutical composition containing an hydrophilic aminoglucoside antibiotic coupled with an organic acid. The coupled aminoglucoside antibiotic and organic acid are encapsulated in a liposome. The composition of the invention is self-regulating in that it liberates the active compound in inverse proportion to the concentration of the compound in the external medium. As a result, the composition serves as a long-acting antibiotic while avoiding the release of a toxic or ineffective dose of the antibiotic into the subject.

Abstract: 2,4,5-Tri(4-methoxyphenyl)-4,5-dihydroimidazole, or a pharmaceutically acceptable salt thereof, is employed as a cancer drug potentiator or as an antimetastis drug.

Abstract: A new and substantially improved type of lipid vesicle, called stable plurilamellar vesicles (SPLVs), are described, as well as the process for making the same and X-ray diffraction methods for identifying the same. SPLVs are characterized by lipid bilayers enclosing aqueous compartments containing one or more entrapped solutes, the concentration of such solutes in each aqueous compartment being substantially equal to the emunization of solutes used to prepare the SPLVs. The bilayers of SPLVs are substantially non-compressed. SPLVs are stable during storage and can be used in vivo for the sustained release of compounds and in the treatment of disease.

Abstract: An azole derivative represented by the following formula (I): ##STR1## wherein X is a nitrogen atom or CH, Y is an oxygen atom, a sulfur atom, an imino group, a methylimino group or a group represented by .dbd.N O--, Z is one or two halogen atoms, in stands for a number of 1 to 2, the wavy line means that stereochemistry of the double bond is either E or Z; or an acid adduct thereof.They exhibit strong antifungal activities and are very useful in the therapy for fungus diseases.Also disclosed is an antifungal drug containing said compound as an active ingredient.

Abstract: The invention relates to combination preparations containing chloramphenicol, gentamicin, nystatin and optionally a cortisone as active ingredients for the topical treatment of inflammatory skin disorders. The preparations are present preferably in the form of an ointment and have proved to be surprisingly effective particularly in the case of the treatment of skin disorders which are difficult to heal such as chronic eczema, inflammations in the anal and genital region, and of ulcus cruris and similar disorders.

Abstract: This invention relates to an aminoglycoside composition having reduced nephrotoxicity induced by the aminoglycoside which comprises a selected aminoglycoside and a compound present in an effective amount selected from the group consisting of (a) at least one 7-(oxoalkyl)1,3-dialkyl xanthine of the formula ##STR1## in which R.sub.1 and R.sub.2 are the same or different and are independently selected from the group consisting of straight-chain or branched alkyl radicals with 2 to 6 carbon atoms, cyclohexyl, straight-chain or branched chain alkoxyalkyl and hydroxyalkyl radicals; and A is a hydrocarbon radical with up to 4 carbon atoms which can be substituted by a methyl group; (b) a compound of the formula ##STR2## wherein at least one of R.sub.3 and R.sub.4 is a branched hydroxyalkyl group of the formula ##STR3## with a tertiary alcohol function, which R.sub.6 stands for an alkyl group with 1 to 3 carbon atoms and n stands for a whole number from 2 to 5, the other R.sub.3 or R.sub.

Abstract: An aqueous ophthalmic preparation is described for the treatment of dry and/or irritated eyes. The preparation is comprised of retinol and/or derivatives or precursors thereof, solubilized in water. Certain non-ionic surfactants and propylmethylcellulose are disclosed as solubilizing agents, with propylmethylcellulose also acting as a mucin-like constituent. The vitamin-containing preparation also contains (1) free radical scavenging compounds and (2) compounds capable, in solution, of chelating multivalent metal cations present in human and/or animal external eye tissue or tear film. The preferred free radical scavenger is mannitol. The preferred chelating agent is EDTA, present in minimal quantities for chelating certain catalytically active metallic ions present at or near the surface of the eye. Also described are tonicity adjusting compositions and an ophthalmic solution buffering system comprising citric acid and citrates.

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: Novel external medications comprise, as essential components, the following three components (A) to (C):(A) an .alpha.-monoglyceryl ether represented by the following formula (I): ##STR1## wherein R means an alkyl or alkenyl group having 10 - 24 carbon atoms; (B) a physiologically active material; and(C) an oily material.The external medications have extremely high skin occlusive properties and significantly-improved absorptivity of phosiologically active materials. Therefore, a smaller amount of the medications compared with the conventional ones can give sufficient pharmacological effects and thus side effects can be reduced. The external medications may contain physiologically active materials such as drugs, growth hormones and the like, which are expected to show pharmacological effects upon their percutaneous absorption.

Abstract: Crosslinked copolymers of monomeric aminosaccharides such as aminoglycosidic antibiotics, e.g. neomycin, or of polymeric aminosaccharides, e.g., chitosan, with dialdehydes are useful antihypercholesterolemic agents due to their ability to bind with bile acids. These copolymers are insoluble in acidic solutions but are swellable to at least about 2.times. their original weight.

Abstract: The invention relates to high potency biomass-free avoparcin and a method for its preparation.

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: A novel method and composition are disclosed for the therapeutic and prophylatic treatment of trauma to the skin. In particular, burns, sunburn and frostbite are treated with compounds that have the ability to interfere with the action of calcium calmodulin complex. A preferred compound is trifluoperazine.

Abstract: The invention relates to a synergistic antibiotic composition useful for the treatment of respiratory, gastrointestinal or urinary infections and septicaemia of domestic animals. The composition comprises tiamulin hydrogen fumarate and an aminoglycoside antibiotic or a pharmaceutically acceptable salt thereof in a weight ratio of 5:1 to 1:5. The active components are admixed or diluted with a carrier, used in veterinary therapy, in a weight ratio of 1:1 to 1:50 and formulated for oral or parenteral application.

Abstract: Aminoglycosides and aminoglycoside-aminocyclitols which have been oxygen-radical activated show a broad spectrum of antibacterial activity. The activated compounds are able to penetrate the cell membranes of bacteria and show substantially enhanced activity as compared to the parent unactivated compound.

Abstract: Flavonoid phosphates of aminoglycoside antibiotics are useful sparingly soluble salts, e.g., for achieving a depot effect.

Abstract: 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 of formula I, to pharmaceutically acceptable, easily hydrolyzable esters thereof, including salts of such esters, to pharmaceutical compositions containing the compounds of the invention and dosage units thereof, to methods for the preparation of the compounds of the invention, and to methods of using the said new compounds in the human and veterinary therapy.The 6.beta.-halopenicillanic acids of formula I are potent inhibitors of .beta.-lactamases from a variety of gram-positive and gram-negative bacteria, making the 6.beta.-halopenicillanic acids as well as their salts and easily hydrolyzable esters valuable in human and veterinary medicine.