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: 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: 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: A pharmaceutical composition which comprises a pharmaceutically acceptable carrier together with an in vivo fibrinolytic enzyme as defined herein wherein the catalytic site essential for fibrinolytic activity is blocked by a group which is removable by hydrolysis at a rate such that the pseudo-first order rate constant for hydrolysis is in the range 10.sup.-6 sec.sup.-1 to 10.sup.-3 sec.sup.-1 in isotonic aqueous media at pH 7.4 at 37.degree. C.; is useful in the treatment of venous thrombosis.
Abstract: This invention relates to antibacterial compounds and in particular to a class of esters which have antibacterial activity against certain Gram-positive and Gram-negative organisms, and also possess antimycoplasmal activity. The compounds are therefore of value in the treatment of human and veterinary infections.
Abstract: The stability of an oily intramammary formulation containing a suspension of a solid clavulanic acid salt is improved by incorporation therein of molecular sieve powder.
Abstract: A compound, with hypoglycaemic activity, having formula (II) or a pharmaceutically acceptable quaternary ammonium or acid addition salt thereof: ##STR1## wherein X represents oxygen or sulphur;n represents zero or 1;R.sup.7 represents hydrogen or C.sub.1-6 alkyl;R.sup.1 and R.sup.2 are the same or different and represent hydrogen, C.sub.1-6 alkyl, phenyl, benzyl, or C.sub.3-6 cycloalkyl;R.sup.3 represents hydrogen, C.sub.1-6 alkyl, phenyl or benzyl;R.sup.4 represents hydrogen or C.sub.1-6 alkyl;R.sup.5 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or R.sup.4 and R.sup.5 together represent the remaining members of a 5- or 6-membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C.sub.1-6 alkyl, carboxy or C.sub.1-6 alkoxycarbonyl; andR.sup.
Abstract: The compounds of the formula (II): ##STR1## and salts and cleavable esters thereof wherein R.sub.1 is a hydrogen atom or a lower alkyl group and R.sub.2 is a CN or CO.sub.2 R.sub.3 group where R.sub.3 is a hydrogen atom or a lower alkyl, aryl, or aralkyl group are antibacterially effective compounds. Their preparation and use is described.R. B. Woodward (Acta Pharm. Suecica 1977, 14 Suppl., p 23-25) disclosed that the compounds of the formula (I): ##STR2## where R was an unspecified group possessed antibacterial activity. No aid in determining the nature of the group R was given by Professor Woodward nor did he describe the preparation of any compounds of the formula (I). However, at the symposium on Current Topics in Drug Research (Uppsala, Sweden October 1977) Professor Woodward described the compound of the formula (I) wherein R is a hydrogen atom. We have prepared this compound and found it to possess a somewhat disappointing degree of antibactrial activity.
Abstract: Compounds of the formula (II): ##STR1## wherein X is halogen, hydroxyl or functionalized hydroxyl; Y is halogen, hydroxyl or alkoxy; R.sup.1 is a carboxylic acid group and ester thereof and amide derivative thereof or cyano; and R.sup.2 is hydrogen, a hydrocarbon, a heterocycle, a carboxylic acid group, a carboxylic acid ester, a carboxylic acid amide derivative, acyl, cyano, isocyano or an optionally substituted imine of the formula --CH.dbd.NZ or --N.dbd.CH.sub.2 wherein Z is hydrogen, alkyl, aryl, sulphonyl, --SR.sup.a, sulphoxide --SR.sup.a, or sulphonate --SR.sup.a wherein R.sup.a is alkyl of 1 to 6 carbon atoms or aryl, are useful as intermediates for the ultimate production of penicillins or cephalosporins.
Type:
Grant
Filed:
May 7, 1979
Date of Patent:
August 4, 1981
Assignee:
Beecham Group Limited
Inventors:
Angela W. Guest, Andrew W. Taylor, Robert Ramage
Abstract: The present invention provides antibiotic compounds of the formula: ##STR1## and salts and cleavable esters thereof wherein X is a SCH.sub.2 CH.sub.2 NH.sub.2 or YNH-COCH.sub.3 group where Y is a SCH.sub.2 CH.sub.2, trans --SO--CH.dbd.-- or cis or trans --S--CH.dbd.CH-- group and R is a lower alkyl, aryl, aralkyl, lower alkenyl, or substituted lower alkyl.
Abstract: Compounds of the formula (II): ##STR1## wherein X is S, SO or SO.sub.2 ; and R is (a) an alkyl group of up to 4 carbon atoms, (b) an alkyl group of up to 4 carbon atoms substituted by an OR.sup.1, NHR.sup.1, NH.CO.R.sup.1 or CO.sub.2 R.sup.2 group wherein R.sup.1 is a hydrogen atoms, an alkyl group of up to 4 carbon atoms or benzyl group, and R.sup.2 is a moiety such that CO.sub.2 R.sup.2 is a carboxyl, salted carboxyl or esterified carboxyl group, (c) an aryl group or (d) an aralkyl group are useful for their anti-fungal and .beta.-lactamase inhibitory properties.
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.