Patents Assigned to Beecham Group Limited
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Patent number: 4444783Abstract: The compounds of the formulaes (IV), (V) and (VI): ##STR1## and salts and esters thereof where X is a bromine or chlorine atom, and n is 0 or 1; are antibacterial agents. Their preparation and use is described.Type: GrantFiled: October 1, 1981Date of Patent: April 24, 1984Assignee: Beecham Group LimitedInventor: Alfred J. Eglington
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Patent number: 4444981Abstract: A compound of formula (II): ##STR1## wherein R is a C.sub.1-4 alkyl group;R.sub.1 is a hydrogen atom or a C.sub.1-4 alkyl group;R.sub.2 is a hydrogen or halogen atom, or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 alkylthio group;and pro-drugs thereof; and the pharmaceutically acceptable salts of the compounds of formula (II) and of their pro-drugs; has useful anti-inflammatory and analgesic activity.Type: GrantFiled: July 25, 1980Date of Patent: April 24, 1984Assignee: Beecham Group LimitedInventor: Alexander C. Goudie
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Patent number: 4444754Abstract: 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.Type: GrantFiled: March 10, 1981Date of Patent: April 24, 1984Assignee: Beecham Group LimitedInventors: Irene Stirling, Brian P. Clarke
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Patent number: 4441609Abstract: 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.Type: GrantFiled: March 5, 1979Date of Patent: April 10, 1984Assignee: Beecham Group LimitedInventor: Patrick J. Crowley
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Patent number: 4442098Abstract: Compounds of formula (I): ##STR1## wherein: X is CH.sub.2, O, S or NR wherein R is hydrogen or C.sub.1-4 alkyl;Y and Z are independently selected from hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or CF.sub.3 ;R.sub.1 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-4 alkyl any of which phenyl moieties may be substituted by one or more of C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or CF.sub.3 ;R.sub.2 is hydrogen, OH, C.sub.1-6 alkoxy, phenyl-C.sub.1-4 alkoxy, C.sub.1-7 acyloxy or NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are independently selected from hydrogen or C.sub.1-6 alkyl; R.sub.4 is hydrogen and R.sub.5 is OH or C.sub.1-4 alkoxy; or R.sub.4 and R.sub.5 together form C.sub.3-6 polymethylene optionally interrupted by O or NR.sub.6 where R.sub.6 is hydrogen or C.sub.1-4 alkyl; or together with R.sub.1 forms an oxo group or .dbd.NOR.sub.7 wherein R.sub.7 is hydrogen or C.sub.1-6 alkyl; andR.sub.3 is hydrogen or C.sub.Type: GrantFiled: December 18, 1981Date of Patent: April 10, 1984Assignee: Beecham Group LimitedInventors: Derek V. Gardner, Laramie M. Gaster
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Patent number: 4438036Abstract: The present invention provides a process for inversion of the absolute stereochemistry at the .alpha.-carbon atom of a C-6 substituent of a bicyclic carbapenem antibiotic via a phosphorus - azodicarboxylate mediated reaction. Novel azides, amines and formates are described as useful intermediates and as antibacterial agents.Type: GrantFiled: October 13, 1981Date of Patent: March 20, 1984Assignee: Beecham Group LimitedInventors: David F. Corbett, Robert Southgate, Steven Coulton
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Patent number: 4438101Abstract: 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.Type: GrantFiled: September 22, 1978Date of Patent: March 20, 1984Assignee: Beecham Group LimitedInventors: Roger J. Ponsford, Thomas T. Howarth
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Patent number: 4436751Abstract: Compounds of formula (II): ##STR1## wherein Y is --CH.dbd.CH--CH.sub.2 --CH-- or ##STR2## R.sup.1 is hydrogen or C.sub.1-4 alkyl, R.sup.2 is hydrogen or C.sub.1-6 alkyl,R.sup.3 is hydrogen, nitro or C.sub.1-6 alkyl and, when Y represents ##STR3## and R.sup.2 and R.sup.3 are hydrogen, the nitro radical is in the meta- or para- position on the benzene ring.are novel and have antimycoplasmal activity. They may be produced by esterification of the corresponding carboxylic acid salt.Type: GrantFiled: December 11, 1981Date of Patent: March 13, 1984Assignee: Beecham Group LimitedInventors: Peter J. O'Hanlon, Graham Walker
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Patent number: 4435565Abstract: Secondary amines of clavulanic acid are useful as beta-lactamase inhibitors that enhance the effectiveness of penicillins or cephalosphorins and also have antibacterial properties in their own right.Type: GrantFiled: March 16, 1981Date of Patent: March 6, 1984Assignee: Beecham Group LimitedInventors: Irene Stirling, Brian P. Clarke
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Patent number: 4435414Abstract: A pharmaceutical composition, which on reconstitution with water yields an injectable solution, which comprises:(a) sodium dicloxacillin, and(b) polyethylene glycol or propylene glycol.Type: GrantFiled: August 23, 1982Date of Patent: March 6, 1984Assignee: Beecham Group LimitedInventor: Michael J. Greenway
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Patent number: 4432993Abstract: A compound of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or methyl,R.sup.3 is hydroxy, hydroxyalkoxy, benzyloxy orX--Y--Zwherein (i)X is a bond or oxygen,Y is C.sub.1-6 straight or branched alkylene, andZ is hydrogen or carboxy;or (ii)X is a bond or moiety --O--CH.sub.2 --,Y is C.sub.2-6 straight or branched alkenylene, andZ is carboxy; andR.sup.4 is an optional substituent, and n is 1, 2 or 3,their esters, amides and salts, are anti-obesity, hypoglycaemic, anti-inflammatory and platelet aggregation inhibiting agents.Type: GrantFiled: September 24, 1981Date of Patent: February 21, 1984Assignee: Beecham Group LimitedInventor: Michael J. Ferris
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Patent number: 4431587Abstract: 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: GrantFiled: December 14, 1981Date of Patent: February 14, 1984Assignee: Beecham Group LimitedInventors: Kay H. Dickinson nee Berryman, Terence C. Smale, Robert Southgate
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Patent number: 4428937Abstract: 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.Type: GrantFiled: December 15, 1980Date of Patent: January 31, 1984Assignee: Beecham Group LimitedInventor: Thomas T. Howarth
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Patent number: 4428958Abstract: Compounds of the formula ##STR1## wherein X is S, SO or SO.sub.2 and R is an organic group of up to 20 carbon atoms and A is a group such that CO.sub.2 A represents a carboxylic acid group or a salt or ester thereof, are useful for their antibacterial activity and for their .beta.-lactamase inhibitory activity.Type: GrantFiled: January 24, 1977Date of Patent: January 31, 1984Assignee: Beecham Group LimitedInventor: Roger J. Ponsford
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Patent number: 4428961Abstract: The present invention provides a compound of formula (I): ##STR1## wherein R.sup.1 is a group such that COOR.sup.1 is a carboxyic acid group or a salt or ester thereof;R.sup.3 is hydrogen or an organic radical;n is zero or 1;R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 -C.sub.3 alkyl;X is C.sub.1 -C.sub.6 alkylene optionally substituted by hydroxy or a carboxylic acid group or a salt or ester thereof;Y is an amino, or substituted amino, wherein the substituent is carboxylic acyl, C.sub.1 -C.sub.6 alkyl or a group .dbd.C(R.sup.14)NR.sup.15 R.sup.16 wherein R.sup.15 and or C.sub.1 -C.sub.6 alkyl and R.sup.14 is hydrogen or C.sub.1 -C.sub.6 alkyl, or a group --NR.sup.A R.sup.B wherein R.sup.A and R.sup.B are independently hydrogen or C.sub.1 -C.sub.6 alkyl.Type: GrantFiled: January 23, 1981Date of Patent: January 31, 1984Assignee: Beecham Group LimitedInventors: Robert Southgate, Terence C. Smale, Roger J. Ponsford
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Patent number: 4428932Abstract: A pharmaceutical composition, for use in the desensitization therapy of humans allergic to non-infective allergens, comprises a non-infective allergen and an adjuvant consisting of a C.sub.10-22 alkyl ester of tyrosine or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 29, 1982Date of Patent: January 31, 1984Assignee: Beecham Group LimitedInventor: Brain G. Overell
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Patent number: 4427686Abstract: A compound of the formula (I): ##STR1## wherein R.sub.1 is hydrogen or C.sub.1-6 alkyl;R.sub.2, R.sub.3 and R.sub.4 are the same or different and are chosen from hydrogen, hydroxyl, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy and C.sub.1-4 alkanoyl;G is H or OH; andm and n are independently 1 to 3; with the proviso that when G is OH, one of m or n is 1; is useful 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.Type: GrantFiled: December 8, 1981Date of Patent: January 24, 1984Assignee: Beecham Group LimitedInventors: Derek R. Buckle, Harry Smith
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Patent number: 4427690Abstract: A new antibacterially active agent has been isolated from Streptomyces clavuligerus. This new compound which is designated clavulanic acid has the formula (I): ##STR1## In addition to being a broad spectrum antibiotic of medium potency, clavulanic acid and its salts and esters have the ability to enhance the effectiveness of .beta.-lactam antibiotics against many .beta.-lactamase producing bacteria.Type: GrantFiled: September 24, 1976Date of Patent: January 24, 1984Assignee: Beecham Group LimitedInventors: Martin Cole, Thomas T. Howarth, Christopher Reading
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Patent number: 4427689Abstract: The compounds of the formula (I): ##STR1## and salts and esters thereof wherein R.sub.1 is a hydrogen atom or a lower alkyl, aryl or aralkyl group, R.sub.2 and R.sub.3 are independently hydrogen, aryl, aralkyl, lower alkyl or substituted lower alkyl, or R.sub.3 is joined to R.sub.1 to form a 5- or 6- membered ring and X is S, SO or SO.sub.2 ; have been found to be .beta.-lactamase inhibitors and antibacterial agents. Their preparation and use is described.Type: GrantFiled: August 31, 1979Date of Patent: January 24, 1984Assignee: Beecham Group LimitedInventors: Iskander I. Zomaya, John S. Davies
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Patent number: 4426392Abstract: 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.Type: GrantFiled: July 27, 1981Date of Patent: January 17, 1984Assignee: Beecham Group LimitedInventor: Alexander C. Goudie