Abstract: The compounds of the formula (II): ##STR1## and salts and esters thereof wherein R.sub.1 is a pyridyl group optionally substituted by one of two lower alkyl groups or lower acyloxy group, have been found to be antibacterial-agents. Their preparation and use is described.
Abstract: A compound of formula (I): ##STR1## and pharmaceutically acceptable salts thereof, wherein R is hydrogen or an alkyl group containing up to 6 carbon atoms; X is a bond or oxygen; Y is --(CH.sub.2).sub.n -- where n is 0 or an integer from 1 to 5 wherein one carbon atom not bound to the nitrogen atom may be optionally substituted with a hydroxy group; and Z is hydrogen or halogen; may be used in the prophylaxis and treatment of diseases whose symptoms are controlled by the mediators of the allergic response, for example asthma, hay-fever, rhinitis and allergic eczema.
Abstract: The present invention provides the antibacterial agents of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is a carboxylic acid group or a salt thereof or is a group of the formula CO.sub.2 R.sub.1.sup.1 wherein R.sub.1.sup.1 is a group such that CO.sub.2 R.sub.1.sup.1 is an ester group, R.sub.2 is a hydrogen atom or a lower alkyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a phenyl group or a phenyl group substituted by one or two groups selected from fluorine, chlorine, OR.sub.5, NH.CO.R.sub.5, NH.CO.sub.2 R.sub.5 or CO.sub.2 R.sub.5 where R.sub.5 is a lower alkyl or benzyl group.A process for their preparation and their use in pharmaceutical compositions is also described.
Type:
Grant
Filed:
January 19, 1979
Date of Patent:
April 21, 1981
Assignee:
Beecham Group Limited
Inventors:
Roger J. Ponsford, Robert Southgate, Patricia M. Roberts
Abstract: Compounds of 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, 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 are disclosed together with a method for their preparation. The compounds are useful as anti-allergic agents. With the exception of 4,9-dioxo-1H-naphtho-[2,3-d]-triazole, and its salts, all compounds of formula (I) are novel.
Abstract: A novel antibiotic designated herein MM 17880 may be obtained from the cultivation of strains of Streptomyces olivaceus and related organisms. In addition to being potent antibacterial agents, MM 17880 and its salts inhibit .beta.-lactamase obtained from many organisms so that it shows a synergistic antibacterical effect when combined with .beta.-lactam antibiotics.
Abstract: A compound of formula (I): ##STR1## wherein: A is >CH-- and n is 1 to 6; orA is >C.dbd.CH-- and n is 0 to 5; orA is >CH--CH.dbd.CH and n is 0 to 4; andR.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.5-7 cycloalkyl or C.sub.5-7 cycloalkyl-C.sub.1-6 alkyl; and salts thereof, has antiplatelet aggregation and bronchodilation activity.
Type:
Grant
Filed:
October 9, 1979
Date of Patent:
April 14, 1981
Assignee:
Beecham Group Limited
Inventors:
Frederick Cassidy, Keith H. Baggaley, Arthur W. R. Tyrrell
Abstract: 7.alpha.-Methoxy-7.beta.-acylamino cephalosporins are prepared from 7.beta.-acylamino cephalosporins through formation of a ketenimine by the action of an acid halide, formation of an addition reaction adduct of this ketenimine, treatment of the adduct with a methoxide to form a 7.alpha.-methoxy ketenimine and hydrolysis of the latter ketenimine.
Type:
Grant
Filed:
October 15, 1979
Date of Patent:
April 7, 1981
Assignee:
Beecham Group Limited
Inventors:
Andrew W. Taylor, George Burton, John P. Clayton
Abstract: A class of penicillins with antibacterial activity having formula (I): ##STR1## wherein R.sup.2 is hydrogen or a pharmaceutically acceptable salting ion or in vivo hydrolyzable ester radical and R.sup.1 is hydrogen, a pharmaceutically acceptable salting ion or a pharmaceutically acceptable ester forming radical.
Abstract: Compounds of the formula (II): ##STR1## wherein A is a group such that CO.sub.2 A is carboxylic acid, a non-toxic salt thereof or non-toxic ester thereof; R.sub.1 is COR.sub.4 or OR.sub.5 wherein R.sub.4 is lower alkyl, lower alkenyl, lower alkyl aryl or aryl and R.sub.5 is CO.sub.2 R.sub.6, COR.sub.6 or SO.sub.2 R.sub.6 wherein R.sub.6 is lower alkyl, lower alkenyl, lower alkyl aryl or aryl; and R.sub.2 is COR.sub.8 wherein R.sub.8 is lower alkyl, lower alkenyl, lower alkyl aryl or aryl; when R.sub.1 is COR.sub.4 and R.sub.2 is COR.sub.8, R.sub.4 and R.sub.8 are joined so that the N(COR.sub.4) COR.sub.8 moiety is a 5-,6-, or 7-membered heterocyclic ring or said ring to which is fused a phenyl ring unsubstituted or substituted by one or two lower alkyl, lower alkoxyl, fluorine or chlorine; when R.sub.1 is OR.sub.5 and R.sub.2 is COR.sub.8, R.sub.5 and R.sub.8 are joined so that the N(OR.sub.5) COR.sub.
Abstract: The compounds of the formula (II): ##STR1## and salts and esters thereof wherein R.sub.1 is an inert organic group of up to 14 carbon atoms and R.sub.2 is an inert organic group of up to 16 carbon atoms, the group NR.sub.1 R.sub.2 containing up to 22 carbon atoms, are antibacterial agents able to enhance the effectiveness of penicillins and cephalosporins against certain .beta.-lactamase producing bacteria.
Abstract: The present invention provides the antibacterial agents of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is a carboxylic acid group or a salt thereof or is a group of the formula CO.sub.2 R.sub.1.sup.1 wherein R.sub.1.sup.1 is a group such that CO.sub.2 R.sub.1.sup.1 is an ester group, R.sub.2 is a hydrogen atom or a lower alkyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a NH. CO.sub.n R.sub.6 group where R.sub.6 is a lower alkyl group, a phenyl group or a phenyl group substituted by one or two halogen atoms, lower alkyl or lower alkoxyl groups; and n is 1 or 2.A process for their preparation and their use in pharmaceutical compositions is also described.
Type:
Grant
Filed:
January 19, 1979
Date of Patent:
March 10, 1981
Assignee:
Beecham Group Limited
Inventors:
Roger J. Ponsford, Andrew J. G. Baxter, Robert Southgate
Abstract: The present invention provides a process for the preparation of potassium clavulanate which process comprises contacting a concentrated solution of lithium clavulanate with a concentrated solution of potassium fluoride, potassium orthophosphate, potassium metaphosphate potassium carbonate or potassium bicarbonate, separating off the resulting precipitated lithium fluoride, lithium orthophosphate, lithium metaphosphate or lithium carbonate and thereafter recovering the potassium clavulanate from solution.
Abstract: A process for the preparation of 3-substituted thiophenes which involves cyclization of a novel intermediate, avoids the use of previously employed expensive starting materials. The thiophenes are useful for the preparation of penicillins and cephalosporins.The process is for the preparation of a thiophene of formula (I): ##STR1## where R.sup.1 represents a carboxylic acid group, or an ester or amide thereof or a nitrile group; R.sup.2 represents a group suitable for use as an .alpha.-substituent in the side-chain of a penicillin or cephalosporin; which comprises treating a compound of formula (II): ##STR2## wherein X represents halogen or optionally functionalized hydroxyl, Y represents halogen, hydroxyl, or alkoxy; with a source of nucleophilic sulphur under basic conditions.
Type:
Grant
Filed:
July 21, 1978
Date of Patent:
February 24, 1981
Assignee:
Beecham Group Limited
Inventors:
Angela W. Guest, Andrew W. Taylor, Robert Ramage
Abstract: The compounds of the formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, a trityl group or an acyl group as found in known antibacterially active penicillins or cephalosporins; R.sup.2 is a hydrogen atom, a lower alkyl group or an aryl group; R.sup.3 is a hydrogen atom, a lower alkyl group, a substituted lower alkyl or a thiosubstituted lower alkyl group; and R.sup.4 is a group such that CO.sub.2 R.sup.4 is a carboxylic acid group or a salt or readily removable ester thereof; are antibiotics. The compounds may be formulated in pharmaceutical compositions.Processes for the preparation of the compounds (I) are also described.
Abstract: Amino chromanols, their preparation and anti-hypertensive compositions containing the compounds in hypotensive amounts with a pharmaceutically acceptable carrier for oral or parenteral administration. Pharmaceutically acceptable salts and O-acyl, particularly O-acetyl, derivatives are described. The compounds exist as racemates and optically active isomers.
Abstract: A compound, with hypolgycaemic activity, having formula (II) or a pharmaceutically acceptable quaternary ammonium or acid addition salt thereof: ##STR1## wherein X represents oxygen or sulphur; n.sub.7 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.
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 anti-mycoplasmal activity. The compounds are therefore of value in the treatment of human and veterinary infections.
Abstract: 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 of different, represent hydrogen, halogen, nitro, lower alkyl, and lower alkoxy, 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 are disclosed. The compounds are useful as anti-allergic agents.