Abstract: The compounds of the formula (II): ##STR1## pharmaceutically acceptable salts thereof, esters thereof and acid addition salts thereof wherein X is a C.sub.1-6 alkylene group, a C.sub.3-8 cycloalkylene group or a C.sub.3-8 cycloalkyl C.sub.1-4 alkylene group, have been found to be .beta.-lactamase inhibitors and antibacterial agents. Their preparation and use is described.
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 an can exist as mixtures of optical isomers or as substantially pure optical isomers.
Abstract: Antacid dosage units comprising a finely divided solid antacid such as aluminium hydroxide dispersed in a fondant confectionary base are provided. Each dosage unit is sealed against moisture evaporation and may include antibacterial or antifungal preservatives as well as humectants and other adjuvants.
Abstract: Process for the preparation of compounds of the formula (I): ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 which may be the same or different, represent hydrogen, halogen, nitro, lower alkyl or lower alkoxy, where lower means of up to six carbon atoms, or any adjacent two of R.sub.1 to R.sub.4 taken together represent an alkylene group containing from 3 to 5 carbon atoms or a 1,4-buta-1,3-dienylene group, by removal of CH.sub.2 R.sub.5 wherein R.sub.5 is phenyl optionally substituted with one or two groups selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro from a compound of formula (II): ##STR2## with an alkali metal C.sub.1-4 primary alkoxide. The compounds are used to inhibit allergic responses.
Abstract: An injectable formulation containing a soluble salt of amoxycillin has its stability on reconstitution improved by the incorporation therein of PVP.
Abstract: The compound of the formula (VI): ##STR1## pharmaceutically acceptable salts and pharmaceutically acceptable esters thereof, are useful for their antibacterial activity and for their .beta.-lactamase inhibitory activity. They may be combined in a synergistically effective amount with a penicillin or cephalosporin for the treatment of bacterial infections in humans and animals.
Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R is phenyl, 4-hydroxy phenyl, or a 5- or 6-membered heterocyclic ring containing up to three heteroatoms selected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen or C.sub.1-6 alkoxy;R.sup.1 represents hydrogen or C.sub.1-6 alkyl;R.sup.2 and R.sup.3 are the same or different and represent hydrogen, C.sub.1-6 alkyl, halogen, amino, hydroxy, or C.sub.1-6 alkoxy.Their preparation and use is described.
Abstract: Compounds of the formula (II): ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms, CO.sub.2 R.sub.2 is a carboxyl group, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable esterified carboxyl group, are useful for their .beta.-lactamase inhibitory activity and to synergize the antibacterial activity of penicillins and cephalosporin.
Abstract: A process for the preparation of a compound of formula (I): ##STR1## wherein R.sup.1 is hydrogen, hydroxy, mercapto radical, a substituted or unsubstituted methoxy, ethoxy, methyl, ethyl, methyl thio, or ethylthio radical, a carbamoyloxy, carbamoylthio, C.sub.1-6 alkanoyloxy, C.sub.1-6 alkanoylthio, cyano, carboxy or carbamoyl radical; andR.sup.2 represents an acyl group which comprises hydrolysis of a compound of formula (II): ##STR2## wherein R.sup.1 and R.sup.2 are as defined with respect to formula (I) hereinbefore and R.sup.3 represents benzyl or substituted benzyl; wherein the hydrolysis is catalyzed by a microbial serine proteinase.
Type:
Grant
Filed:
October 19, 1981
Date of Patent:
November 1, 1983
Assignee:
Beecham Group Limited
Inventors:
Ian R. Chester, Lawson W. Powell, David G. Roberts
Abstract: The present invention provides the compounds of the formula (II): ##STR1## and salts and esters thereof wherein R.sup.3 is a hydrogen atom or is an organic bonded via a carbon atom to the carbapenem ring, n is zero or one, X is a saturated or unsaturated hydrocarbon radical optionally substituted by bromo or chloro, and R.sup.4 is a C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.1-10 aralkyl or aryl group, any of such groups R.sup.4 being optionally substituted. These compounds are useful as antibacterial agents.
Abstract: Compounds of formula (I), or salts thereof: ##STR1## wherein: X is oxygen or sulphur, or >C.dbd.X represents ##STR2## Y is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--; n is 1 to 5;R.sub.1 is hydrogen or C.sub.1-6 alkyl;R.sub.2 is hydrogen or C.sub.1-4 alkyl; andR.sub.3 is C.sub.4-9 alkyl, C.sub.5-8 cycloalkyl, or C.sub.5-8 cycloalkyl --C.sub.1-6 alkyl; orR.sub.2 and R.sub.3 taken with the carbon atom to which they are joined represent a C.sub.5-8 cycloalkyl group, having useful pharmacological activity, pharmaceutical compositions containing them and a process for their preparation.
Abstract: Compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: R.sub.1 is C.sub.1-6 alkyl;R.sub.2 is hydrogen or C.sub.1-7 acyl;R.sub.3 is C.sub.1-6 alkyl;R.sub.4 is a group CH.sub.2 R.sub.5 wherein R.sub.5 is hydrogen, C.sub.3-8 cycloalkyl or phenyl optionally substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.1-4 alkoxy, trifluoromethyl and halogen, having useful anti-emetic activity.
Abstract: The compound of the formula (I): ##STR1## and salts and esters thereof may be used as a .beta.-lactamase inhibitor to enhance the effectiveness of penicillins or cephalosporins.
Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: R.sub.1 is a C.sub.1-6 alkoxy group;R.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, CF.sub.3, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkyl-S(O).sub.n wherein n is 0, 1 or 2, nitro, or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two C.sub.1-6 alkyl groups;or R.sub.1 and R.sub.2 taken together are methylendioxy or ethylenedioxy in which case R.sub.3 is any one of the groups given for R.sub.1 and R.sub.2 above;R.sub.4 is hydrogen or C.sub.1-6 alkyl;R.sub.5 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-6 alkyl, either of which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3 or halogen, and R.sub.6 is hydrogen; or R.sub.5 and R.sub.6 are attached to two adjacent carbon atoms and form together with these two carbon atoms a fused benzene ring, which benzene ring may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.
Abstract: A compound, with hypoglycaemic activity, having formula (II) or a pharmaceutically acceptable acid addition salt thereof: ##STR1## wherein X represents oxygen or sulphur;R.sup.1 R.sup.2 are the same or different and represent hydrogen, halogen, C.sub.1-6 alkyl, phenyl, benzyl,C.sub.3-6 cycloalkyl, carbo-C.sub.1-6 alkoxy or C.sub.1-6 carboxy or R.sup.1 and R.sup.2 represent the remaining members of a benzene ring;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; andR.sup.
Abstract: The present invention provides the compounds of the formula (II): ##STR1## and pharmaceutically acceptable salts and cleavable esters thereof wherein RCONH is an organic acylamino group and E is a carboxy group or pharmaceutically acceptable salt or ester thereof or is a cyano group. Their preparation is described as is their use in compositions containing them. Compounds wherein RCONH is replaced by an azido group are described as useful intermediates.
Abstract: Compounds of the formula (I), or pharmaceutically acceptable salts thereof ##STR1## wherein X is phenyl, optionally substituted by one halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy; or pyridyl; R.sub.1 is hydrogen or C.sub.1-6 alkyl; and n is 1 to 6, pharmaceutical compositions containing them and a process for their preparation. These compounds are useful in the prophylaxis or treatment of diseases due to a histamine-mediated allergic response.
Abstract: Compounds are described of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group; A.sub.1 is a hydrogen atom; and A.sub.2 is a group CR.sub.2 R.sub.3 R.sub.4 wherein R.sub.2 is a hydrogen atom or a hydroxyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, a benzyl group, a phenyl group or is joined to R.sub.3 to form part of a C.sub.5-7 carboxylic ring or is a group of the formula CH(OH)R.sub.5 or CHX wherein R.sub.5 is a hydrogen atom or lower alkyl group and X is an oxygen atom or a CR.sub.6 R.sub.7 group where R.sub.6 is a hydrogen atom or a lower alkyl, phenyl, CN, CO.sub.2 R.sub.8 where R.sub.8 is a lower alkyl, phenyl or benzyl group and R.sub.7 is a hydrogen atom or a lower alkyl group or is joined to R.sub.6 to form part of a C.sub.5-7 carbocyclic ring. These compounds have been found to possess antibacterial properties. The preparation of these compounds is described.
Type:
Grant
Filed:
September 28, 1981
Date of Patent:
September 20, 1983
Assignee:
Beecham Group Limited
Inventors:
Kay H. Dickinson nee Berryman, Terence C. Smale, Robert Southgate
Abstract: Compounds are provided of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group and A.sub.1 is a hydrogen atom or a methyl group. These compounds possess antibacterial activity. The preparation of these compounds is described.
Type:
Grant
Filed:
October 19, 1981
Date of Patent:
August 30, 1983
Assignee:
Beecham Group Limited
Inventors:
Andrew J. G. Baxter, Patricia M. Roberts, Robert Southgate