Abstract: Compounds of the formula (II): ##STR1## wherein X is sulphur or oxygen and R is hydrogen or alkyl of 1 to 3 carbon atoms, are useful for their antibacterial, .beta.-lactamase inhibitory activity and synergistic activity when combined with a penicillin or cephalosporin.
Abstract: A compound of formula (I): ##STR1## wherein the dotted line indicates an optional double bond and R is a hydrogen atom or a methyl group has topical anti-inflammatory activity.
Abstract: The compounds of the formula (I): ##STR1## and esters thereof wherein R.sub.1 is a lower alkyl group or a phenyl group and R.sub.2 is a hydrogen atom or R.sub.2 together with R.sub.1 represents the residue of a fused benzene ring are .beta.-lactamase inhibitors and anti-bacterial agents. Their preparation and use is described.
Abstract: A dry unit-dose pharmaceutical composition suitable for oral administration which composition comprises 20 mg to 1500 mg of amoxycillin trihydrate, 20 mg to 500 mg of potassium clavulanate and a pharmaceutically acceptable carrier with the proviso that the weight ratio of amoxycillin trihydrate to potassium clavulanate is from 6:1 to 1:1; has favored storage properties. Such compositions are presented in enclosed containers which they also contain a desiccant.
Abstract: Compounds of formula (I): ##STR1## wherein: X is CO, protected CO, CROH in which R is hydrogen or C.sub.1-4 alkyl and in which the OH moiety may be protected;Y is CH.sub.2 CH.sub.2 or CH.dbd.CH;Z is CO or CH.sub.2 ;n is 1 to 8;m is 1, 2 or 3;R.sub.1 is hydrogen, CH.sub.2 OH, CH.sub.2 OH in which the OH moiety is protected, CO.sub.2 W wherein W is hydrogen or CO.sub.2 W represents an ester group in which the ester moiety contains from 1 to 12 carbon atoms, or CONH.sub.2 ;R.sub.2 is hydrogen, C.sub.1-4 alkyl, or taken together with R.sub.3 and the carbon atom to which it is attached represents a carbonyl group;R.sub.3 is hydrogen, hydroxy or protected hydroxy;R.sub.4 is hydrogen or C.sub.1-9 alkyl;and salts thereof--have useful pharmacological properties.
Abstract: Anti-inflammatory naphthyl compounds, their preparation and pharmaceutical compositions containing the same. The anti-inflammatory activity has a wide spectrum coupled with low side effects such as gastrointestinal irritancy or oestrongenicity. The compounds possess a chiral center at C-2 and can exist as mixtures of optical isomers or as substantially pure optical isomers.
Abstract: Compounds of the formula 1: ##STR1## wherein: X is O or S;R.sub.1 is hydrogen, or CO.sub.2 R.sub.1 represents an ester group in which the R.sub.1 moiety contains from 1-12 carbon atoms;R.sub.2 is hydrogen or C.sub.1-4 alkyl;R.sub.4 is C.sub.1-9 alkyl, C.sub.3-8 cycloalkyl or C.sub.3-8 cycloalkyl-C.sub.1-6 alkyl; orR.sub.2 and R.sub.4 taken with the carbon atom to which they are joined represent a C.sub.5-8 cycloalkyl group; andR.sub.5 is C.sub.1-6 alkyl; and salts thereof, having similar activity to natural prostaglandins, a process for their preparation, intermediates useful in that process and pharmaceutical compositions containing them.
Abstract: The compounds of the formula: ##STR1## and salts and esters thereof are useful agents for the treatment of bacterial infections either alone or in combination with a penicillin or cephalosporin derivative. The preceding compounds may be prepared by the hydrogenation of a compound of the formula: ##STR2## wherein R is a hydrogen atom or an acyl group or a salt or ester thereof.
Abstract: A pharmaceutical dispensing container which holds two dosage units which are symptomatic treatment for respiratory tract disorders, the first of these dosage units being indicated for day-time administration and being non-sedative and the second of these dosage units being indicated for night-time administration and being sedative. Indication means include the dosage units being in register with a time chart and a distinguishing visible feature of the dosage units.
Abstract: In vivo hydrolyzable esters of 6.beta.-bromopenicillanic acid when substantially free from the corresponding in vivo hydrolyzable ester of 6.alpha.-bromopenicillanic acid is useful for their .beta.-lactamase inhibitory activity and may be administered either per se or in combination with a penicillin or cephalosporin.
Abstract: Compounds of the formula (I): ##STR1## wherein n is 3 to 5;Y is --CH.sub.2 --CH.sub.2, --CH.dbd.CH-- or C.tbd.C--;L is O or S;R.sub.1 is C.sub.1-4 alkyl;R.sub.2 is hydrogen, C.sub.1-4 alkyl or phenyl;R.sub.3 is hydroxy or protected hydroxy;R.sub.4 is hydrogen, C.sub.1-9 alkyl, C.sub.3-8 cycloalkyl, phenyl, naphthyl, any of which phenyl moieties or naphthyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkoxy, phenyl C.sub.1-6 alkoxy or nitro groups; orR.sub.2 and R.sub.4 taken with the carbon atom to which they are joined represent a C.sub.5-8 cycloalkyl group; and R.sub.5 is C.sub.1-6 alkyl, having similar activity to natural prostaglandins, a process for their preparation, intermediates useful in that process and pharmaceutical compositions containing them.
Abstract: A skin care product such as a cleansing lotion or pre- or aftershave lotion comprising ethanol, water, spherical polymer or copolymer microspheres, e.g. of polyethylene, polystyrene or polymethylmethacrylate, and a suspending agent for the microspheres. The ethanol:water weight ratio is in the range 1:19 to 19:1 and the microspheres, which may be sized from 5 to 7 microns, amount to 3 to 10% by weight of the product. The microspheres have a smoothing and matting effect on the skin, improving the observed degreasing effect of the product.
Abstract: The present invention relates to sodium, thallium, silver or lithium salts of the compoundHS--CH=CHNHC(O).sub.n R.sub.6wherein n is 1 or 2, R.sub.6 is alkyl, phenyl or substituted phenyl. The salts are useful as reagents for the preparation of sulfur containing Clavulanic acid derivatives.
Type:
Grant
Filed:
December 14, 1979
Date of Patent:
October 6, 1981
Assignee:
Beecham Group Limited
Inventors:
Roger J. Ponsford, Andrew J. G. Baxter, Robert Southgate
Abstract: The acute liver toxicity effects of paracetamol are reduced by co-formulating with sustained release ascorbic acid which produces high liver concentrations of ascorbate anion after oral administration of the co-formulation. A suitable form of sustained release ascorbic acid is prepared by microencapsulation of particles of ascorbic acid in membranes which act as microdialysis cells.
Abstract: A process for the preparation of the compounds of the formula (II): ##STR1## and salts and cleavable esters thereof wherein R.sub.1 is a hydrocarbon group of up to 12 carbon atoms and which optionally also contain up to 4 heteratoms selected from oxygen, nitrogen, sulphur or chlorine and bromine which process comprises the reaction of a cleavable ester of a compound of the formula (III): ##STR2## with one equivalent of a strong base of low nucleophilicity and thereafter with a compound of the formula (IV) or (V):R.sup.2 SO.sub.2 SR.sub.1.sup.1 (IV)Cl--S--R.sub.1.sup.1 (V)wherein R.sub.1.sup.1 is a group R.sub.1 in which any amino substituent is protected and R.sup.2 is an alkyl group of 1-4 carbon atoms optionally substituted by a phenyl group or is a phenyl group optionally substituted by an alkyl group of 1-4 carbon atoms and thereafter if desired cleaving the ester moiety to yield the acid of the formula (II) or a salt thereof and removing the protecting group from any protected amino group present in R.
Abstract: The present invention provides a compound of formula (1): ##STR1## wherein G is hydrogen, alkyl, alkenyl, substituted alkyl or substituted alkenyl, R.sub.1 is alkyl or aryl, substituted alkyl or substituted aryl, and R is an organic group such that --CO.sub.2 R is an ester group. The compounds are useful as antibacterial and .beta.-lactamase inhibitory agents.
Abstract: A method for preparing interferon in which MRC-5 cells are induced for 2 to 3 hours with an interferon-inducing medium containing from 0.1 to 50 mg 1.sup.-1 of a ds-RNA, 100 mg 1.sup.-1 of DEAE-Dextran and 250 m.M of sucrose.Other sugars which can be used include glucose, galactose, fructose, mannose and maltose, and a preferred ds-RNA is naturally occurring ds-RNA isolated from P. chrysogenum.
Abstract: An active antibacterial substance from Pseudomonas fluoroescens bacterium designated pseudominic acid and as a co-product a minor amount of a compound having an additional OH group designated as pseudomonic acid I. These two substances obtained are separated and purified. Alkali metal salts and methyl esters can be prepared. The antibacterial activity of pseudomonic acid appears to reside in the free acid form which results from in vivo hydrolysis of the methyl ester which is crystalline.
Abstract: Compounds within formula ##STR1## and their salts wherein X is alkylene of 2-4 carbon atoms; R.sub.1 is hydrogen or alkyl of 1-6 carbon atoms; R.sub.2 is hydrogen, alkyl of 1-6 carbon atoms or benzyl, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a 5-, 6- or 7-membered saturated ring; R.sub.3 is aryl; R.sub.4 is hydrogen or alkyl of 1-4 carbon atoms; and R.sub.5 is hydrogen or alkyl of 1-4 carbon atoms; have been found to possess mood-modifying and anorexia inducing activity.