Patents Assigned to Beecham Group
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Patent number: 4481214Abstract: Compounds of formula (I): ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, C.sub.1-6 alkyl-thiolmethyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.Type: GrantFiled: May 19, 1983Date of Patent: November 6, 1984Assignee: Beecham Group p.l.c.Inventor: John M. Evans
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Patent number: 4481210Abstract: A method of treatment of bacterial infections in humans which comprises administering to a patient one or two unit dosages per day of a compound of formula (I): ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically acceptable salting ion or a pharmaceutically acceptable ester-forming radical, andR.sup.2 is hydrogen, a pharmaceutically acceptable salting ion or an in vivo hydrolyzable ester-forming radical.Type: GrantFiled: March 30, 1982Date of Patent: November 6, 1984Assignee: Beecham Group p.l.c.Inventors: Robert Sutherland, Brian Slocombe
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Patent number: 4480099Abstract: A compound of formula (I), and 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, amino, C.sub.1-7 acyl amino, aminocarbonyl or aminosulphone optionally substituted by one or two C.sub.1-6 alkyl groups; C.sub.1-6 alkyl-SO.sub.n wherein n is 1 or 2; or nitro;R.sub.4 is hydrogen or C.sub.1-6 alkyl;R.sub.5 is C.sub.1-6 alkyl or a group --(CH.sub.2).sub.s R.sub.6 wherein s is 1 or 2 and R.sub.6 is C.sub.3-8 cycloalkyl or phenyl, which phenyl may optionally be substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.1-4 alkoxy, CF.sub.3 and halogen;n is 0 to 3;p is 3 to 6; andr plus s is 2 to 5; may be used for the treatment of disorders of the gastro-intestinal function.Type: GrantFiled: June 21, 1982Date of Patent: October 30, 1984Assignee: Beecham Group P.L.C.Inventor: Michael S. Hadley
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Patent number: 4478849Abstract: The compounds of the formula (II): ##STR1## and their pharmaceutically acceptable salts wherein R.sub.1 is a hydrogen, fluorine or chlorine atom or a hydroxyl, hydroxymethyl, methyl, methoxyl, amino, formamido, acetamido, methylsulphonylamido, nitro, benzyloxy, methylsulphonylmethyl, ureido, trifluoromethyl or p-methoxybenzylamino group; R.sub.2 is a hydrogen, fluorine or chlorine atom or a hydroxyl group; R.sub.3 is a hydrogen or chlorine atom or a hydroxyl group; R.sub.4 is a carboxylic acid group or a salt, ester or amide thereof; R.sub.5 is a hydrogen, chlorine or fluorine atom or a methyl, methoxyl or hydroxyl group or a carboxylic acid group or a salt, ester or amide thereof; R.sub.6 is a hydrogen atom or a methyl, or propyl group; X is an oxygen atom or a bond; and Y is an alkylene group of up to 6 carbon atoms or a bond have been found to possess anti-obesity and/or antihyperglycaemic activity.Type: GrantFiled: March 10, 1983Date of Patent: October 23, 1984Assignee: Beecham Group LimitedInventors: Anthony T. Ainsworth, David G. Smith
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Patent number: 4477662Abstract: A process for the preparation of an antibacterially active compound of the formula (I): ##STR1## and salts and esters thereof wherein R.sup.1 and R.sup.2 independently are hydrogen or an organic group, and R.sup.3 is an organic group bonded via a carbon atom to the sulphur atom, which comprises reacting a compound of the formula (II): ##STR2## wherein R.sup.4 is an organic group different to R.sup.3 and R.sup.a is hydrogen or a carboxy-blocking group, with a thiol R.sup.3 SH or reactive derivative thereof. In addition certain compounds within the formula (II) are novel and useful antibacterial agents in their own right.Type: GrantFiled: February 3, 1982Date of Patent: October 16, 1984Assignee: Beecham Group p.l.c.Inventors: David F. Corbett, Pamela Brown nee Davis, Roger J. Ponsford
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Patent number: 4473578Abstract: The compounds of the formula: ##STR1## and pharmaceutically acceptable salts and in-vivo hydrolysable esters thereof wherein R.sup.1 is a hydrogen atom or a group selected from OH, OSO.sub.3 H or a pharmaceutically acceptable salt or C.sub.1-4 alkyl ester thereof, OR.sup.2, SR.sup.3, OCOR.sup.2, OCO.sub.2 R.sup.3 or OCONHR.sup.3, where R.sup.2 is a C.sub.1-6 alkyl group or an optionally substituted benzyl group and R.sup.3 is a C.sub.1-6 alkyl group or an optionally substituted benzyl or an optionally substituted phenyl group; and R.sup.22 is a hydrogen atom, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 alkynyl wherein the triple bond is not present on the carbon adjacent to the sulphur atom, aralkyl, C.sub.1-6 alkanoyl, aralkanoyl, aryloxyalkanoyl or arylcarbonyl, any of such R.sup.22 groups being optionally substituted; with the proviso that when R.sup.22 is 2-aminoethyl R.sup.1 must be SR.sup.3 or OSO.sub.3 H or a pharmaceutically acceptable salt of C.sub.Type: GrantFiled: July 29, 1982Date of Patent: September 25, 1984Assignee: Beecham Group LimitedInventor: David F. Corbett
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Patent number: 4472413Abstract: Compounds of formula (I): ##STR1## wherein X is methoxy or ethoxy, Y is amino or C.sub.1-6 alkanoylamino, Z is hydrogen, chloro or bromo and R.sub.1 is methyl, chloro or fluoro, have anti-psychotic activity, and are useful in the treatment of CNS disorders.Type: GrantFiled: September 30, 1982Date of Patent: September 18, 1984Assignee: Beecham Group p.l.c.Inventors: Michael S. Hadley, Francis E. Blaney
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Patent number: 4472374Abstract: An intramammary composition containing a siloxane elastomer with incorporated antibacterial agent. The composition is of sufficiently low viscosity to facilitate application to the teat of a cow via the streak canal, and the composition remains sufficiently elastic to enable it to remain in place during the dry period and to allow it to be readily milked-out at the onset of lactation. The composition is useful in reducing mammary infections in cattle during their dry period and is compatible with conventional mastitis treatments at the end of lactation.Type: GrantFiled: September 24, 1982Date of Patent: September 18, 1984Assignee: Beecham Group p.l.c.Inventors: John S. Dowrick, Peter Balderstone
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Patent number: 4469697Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein: X is CH.sub.2, O, S or NR.sub.4 wherein R.sub.4 is hydrogen or C.sub.1-4 alkyl;one of Y and Z is NR.sub.5 and the other is CR.sub.6 R.sub.7 wherein R.sub.5 is hydrogen, C.sub.1-4 alkyl or C.sub.1-4 acyl and R.sub.6 and R.sub.7 are either both hydrogen or together form an oxo group;R.sub.1 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.4-7 cycloalkenyl or C.sub.1-4 alkyl substituted by C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, C.sub.3-7 cycloalkyl, amino optionally substituted by one or two C.sub.1-4 alkyl or by C.sub.4-6 polymethylene optionally containing an oxygen atom or by phenyl C.sub.1-4 alkyl optionally substituted in the phenyl ring by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or trifluoromethyl; andR.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, hydroxy, C.sub.1-4 alkyl C.sub.Type: GrantFiled: March 25, 1983Date of Patent: September 4, 1984Assignee: Beecham Group p.l.c.Inventors: Derek V. Gardner, Trevor J. White
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Patent number: 4465689Abstract: Esters of an acid of formula: ##STR1## which is termed "monic acid" have activity against Gram-positive and Gram-negative organisms.Type: GrantFiled: January 25, 1979Date of Patent: August 14, 1984Assignee: Beecham Group LimitedInventors: Kong Luk, John P. Clayton, Norman H. Rogers
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Patent number: 4463010Abstract: A 1-aza[3.2.0]bicycloheptan-2-carboxylic acid or salt or ester thereof having a substituent at position 7 of the formula:.dbd.CR.sup.1 R.sup.2wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen or an organic group.Type: GrantFiled: May 12, 1982Date of Patent: July 31, 1984Assignee: Beecham Group p.l.c.Inventor: Martin L. Gilpin
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Patent number: 4460594Abstract: Compounds of the formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein: R.sub.1 is hydroxy, C.sub.1-4 alkoxy or an in-vivo hydrolysable acyloxy group:R.sub.2 is hydrogen, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy or an in-vivo hydrolysable acyloxy group;R.sub.4 is benzofuryl, benzothienyl, indolyl, quinolyl, isoquinolyl,2,3-dihydrobenzofuryl, 2,3-dihydrobenzylthienyl or 2,3-dihydroindolyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, hydroxy or acyloxy, trifluoromethyl, halogen or nitro; andA is a bond or C.sub.1-6 alkylene,a process for their preparation, and pharmaceutical compositions containing them.Type: GrantFiled: September 15, 1982Date of Patent: July 17, 1984Assignee: Beecham Group p.l.c.Inventor: Roger E. Markwell
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Patent number: 4460582Abstract: The present invention provides a compound of the formula (I): ##STR1## and pharmaceutically acceptable salts and in-vivo hydrolysable esters thereof wherein R.sup.1 is carboxy, R.sup.2 is hydrogen or carboxy, R.sup.3 is hydrogen, acyl, C.sub.1-6 akyl or C.sub.2-6 alkenyl, any of such R.sup.3 groups being optionally substituted, and R.sup.4 is an amino or protected amino group.Processes for the preparation of these compounds are described as is their use in the treatment of bacterial infection.Type: GrantFiled: March 1, 1982Date of Patent: July 17, 1984Assignee: Beecham Group P.L.C.Inventor: John H. C. Nayler
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Patent number: 4460595Abstract: Compounds of the formula (I) ##STR1## wherein; n is 1 to 5Y is --CH.sub.2 --CH.sub.2 or --CH.dbd.CH--;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, 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, C.sub.3-8 cycloalkyl-C.sub.1-6 alkyl, phenyl, phenyl -C.sub.1-6 alkyl, naphthyl, naphthyl C.sub.1-6 alkyl, 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;R.sub.5 is hydrogen, C.sub.1-6 alkyl, C.sub.5-8 cycloalkyl, phenyl, phenyl-C.sub.1-6 alkyl or phenyl C.sub.3-6 cycloalkyl, any of which phenyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or nitro groups; orR.sub.2 and R.sub.Type: GrantFiled: April 23, 1982Date of Patent: July 17, 1984Assignee: Beecham Group LimitedInventors: David R. Adams, Alexander C. Goudie
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Patent number: 4459300Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: n, p and q independently are 0 to 2;R.sub.5 is hydrogen or C.sub.1-6 alkyl;R.sub.6 is C.sub.1-7 alkyl or a group --(CH.sub.2).sub.s R.sub.7 where s is 0 to 2 and R.sub.7 is a C.sub.3-8 cycloalkyl group, or a group --(CH.sub.2).sub.t R.sub.8 where t is 1 or 2 and R.sub.8 is C.sub.2-5 alkenyl or a phenyl group optionally substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.1-4 alkoxy, trifluoromethyl and halogen, or a thienyl group;R.sub.12 is C.sub.1-6 alkylsulphonyl;and eitherR.sub.1 is C.sub.1-6 alkoxy or C.sub.1-6 alkylthio; and one of R.sub.2 and R.sub.11 is hydrogen and the other is C.sub.1-6 alkoxy, C.sub.1-6 alkyl or hydroxy; or R.sub.1 and R.sub.2 together are C.sub.1-3 alkylenedioxy; and R.sub.11 is hydrogen, halogen, CF.sub.3, C.sub.1-6 alkoxy,hydroxy, nitro, C.sub.1-7 acyl, amino, C.sub.1-7 acylamino, aminocarbonyl optionally substituted by one or two C.sub.1-6 alkyl, C.sub.Type: GrantFiled: June 17, 1982Date of Patent: July 10, 1984Assignee: Beecham Group p.l.c.Inventor: Eric A. Watts
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Patent number: 4455314Abstract: The preparation and use of 6,.alpha.-methoxy-6,.beta.-[2-(2-methylphenoxycarbonyl)-2-(thien-3-yl) acetamido] penicillanic acid of formula (II): ##STR1## or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof.Type: GrantFiled: January 20, 1983Date of Patent: June 19, 1984Assignee: Beecham Group p.l.c.Inventors: George Burton, Desmond J. Best
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Patent number: 4454136Abstract: Compounds of the formula (I): ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is hydrogen or C.sub.1-6 alkyl, and R.sub.2 is hydroxy, C.sub.1-4 alkylsulphonyloxy or p-toluenesulphonyloxy are useful for the prophylaxis and treatment of diseases due to allergic response in mammals. Processes for their preparation are described.Type: GrantFiled: September 15, 1981Date of Patent: June 12, 1984Assignee: Beecham Group LimitedInventors: Derek R. Buckle, Harry Smith
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Patent number: 4454069Abstract: This invention provides a novel process for the preparation of clavulanic acid and pharmaceutically acceptable salts and esters thereof which process utilizes the preparation of the tertiary-butylamine salt of clavulanic acid optionally in the form of an acetone solvate and subsequently converting said salt into the desired product.Type: GrantFiled: December 24, 1981Date of Patent: June 12, 1984Assignee: Beecham Group LimitedInventors: Michael A. Cook, Alan D. Curzons, Robert B. Wilkins
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Patent number: 4450170Abstract: Compounds A - B - C wherein A is 2 imidazolinyl or N-alkyl derivative thereof, B is oxygen, sulphur, CR.sup.1 R.sup.2 wherein R.sup.1 and R.sup.2 are hydrogen or alkyl, or NR.sup.3 wherein R.sup.3 is hydrogen or alkyl, and C is a 5 - or 6 - membered carbo- or heterocyclic group having a nitrogen containing substituent and up to two other substituents, are useful in treatment of diarrhoea or scours. Certain compounds A - B - C are novel.Type: GrantFiled: June 24, 1981Date of Patent: May 22, 1984Assignee: Beecham Group LimitedInventors: Lee J. Beeley, Peter M. Newsome
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Patent number: 4447422Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R.sup.1 is phenyl, 4-hydroxy phenyl, 3,4-dihydroxyphenyl, 3,4-diacetoxyphenyl 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; and R.sup.2 is a sub-group of formula (A):--NH--R.sup.3 (A)wherein R.sup.3 is an optionally substituted C.sub.1-10 alkyl or C.sub.3-7 cycloalkyl group; or R.sup.2 is a sub-group of formula (B):--NH--CO--R.sup.4 (B)wherein R.sup.4 is an aryl group, an optionally substituted C.sub.1-10 alkyl group or a C.sub.1-6 alkyloxy group optionally substituted by an aryl group.Type: GrantFiled: June 7, 1982Date of Patent: May 8, 1984Assignee: Beecham Group p.1.c.Inventors: Andrew W. Taylor, Richard G. Adams