Patents Assigned to Beecham Group
  • Patent number: 4666710
    Abstract: An anti-perspirant composition includes 30% by weight of an anti-perspirant agent, aluminium chlorhydrate, 68.5% by weight of ethanol and 1.5% by weight of a long chain fatty acid, myristic acid.The presence of the fatty acid counteracts the reduction in efficacy caused by the high concentration of ethanol.
    Type: Grant
    Filed: February 13, 1980
    Date of Patent: May 19, 1987
    Assignee: Beecham Group P.l.c.
    Inventor: Roy J. Clarkson
  • Patent number: 4665072
    Abstract: Compounds of formula (I): ##STR1## or a salt thereof, in which W is phenyl optionally substituted by halogen or trifluoromethyl, or a benzofuran-2-yl group,R.sup.1 is hydrogen or methyl,R.sup.2 is carboxyl or a group O--Z--CO.sub.2 H or an ester or amide thereof; a group O--E--NR.sup.3 R.sup.4 or a group O--E--OR.sup.5,wherein R.sup.3, R.sup.4 and R.sup.5 each represents hydrogen or C.sub.1-6 alkyl, Z is a C.sub.1-6 straight or branched alkylene chain, n is 1 or 2, a is 2 or 3, and E is a C.sub.2-7 straight or branched alkylene chain with at least two carbon atoms separating the two heteroatoms in the group R.sup.2 ; a process for the production of such compounds and their use in medicine as anti-hyperglycaemic and/or anti-obesity agents.
    Type: Grant
    Filed: May 21, 1986
    Date of Patent: May 12, 1987
    Assignee: Beecham Group p.l.c.
    Inventor: Barrie C. C. Cantello
  • Patent number: 4661480
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolyzable ester thereof: ##STR1## R is phenyl, substituted phenyl, C.sub.3-6 cycloalkyl cyclohexenyl, cyclohexadienyl, or a 5- or 6-membered heterocyclic ring containing up to three hetero-atoms slected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen, substituted amino or C.sub.1-6 alkoxy; Q represents acetoxy, carbamoyloxy, heterocyclylthio group, or a nitrogen containing heterocyclic group bonded via nitrogen; R.sup.1 is hydrogen or a C.sub.1-6 alkyl group and R.sup.2 is an optionally substituted 5- or 6-membered heterocyclic group containing one or two heteroatoms; or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form an optionally substituted five- or six-membered heterocyclic group containing one or two nitrogen heteroatoms; a process for the preparation of such compounds and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 19, 1984
    Date of Patent: April 28, 1987
    Assignee: Beecham Group p.l.c.
    Inventor: Peter H. Milner
  • Patent number: 4661489
    Abstract: A compound of formula (I): ##STR1## in which R is optionally substituted phenyl; C.sub.3-8 cycloalkyl; C.sub.5-8 cycloalkenyl; C.sub.1-8 alkyl which may be straight or branched; C.sub.2-8 alkenyl which may be straight or branched; 5- or 6- membered heterocyclyl; or optionally substituted phenyl C.sub.1-4 alkyl, each of Y and Z, which may be the same or different, is oxygen or sulphur; and X is --CH.sub.2 -- or oxygen, a process for the preparation of such compounds and their use in human and veterinary medicine.
    Type: Grant
    Filed: July 13, 1984
    Date of Patent: April 28, 1987
    Assignee: Beecham Group p.l.c.
    Inventors: Roderick J. Dorgan, Richard L. Elliott
  • Patent number: 4661524
    Abstract: Pharmaceutical compositions with comprise a compound of the formula (I): ##STR1## wherein X is a chlorine or bromine atom or a methoxyl, methylthio or alkyl group of 1-4 carbon atoms; Y is a --CHR.sub.1 --CH.sub.2 -- or --CR.sub.1 .dbd.CH-- group where R.sub.1 is a hydrogen atom or a methyl group and A is a CHOH or CO group, and a pharmaceutically acceptable carrier selected from the group of creams, ointments, lotions, gels, aerosols, sprays, liniments and gel sticks. The compositions possess systemic anti-inflammatory activity when administered topically.
    Type: Grant
    Filed: December 27, 1985
    Date of Patent: April 28, 1987
    Assignee: Beecham Group P.L.C.
    Inventors: Michael J. Thomson, Frank R. Mangan
  • Patent number: 4654371
    Abstract: 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 anti-hyperglycaemic activity.
    Type: Grant
    Filed: October 8, 1985
    Date of Patent: March 31, 1987
    Assignee: Beecham Group p.l.c.
    Inventors: Anthony T. Ainsworth, David G. Smith
  • Patent number: 4652560
    Abstract: The compounds of the formula (II): ##STR1## or pharmaceutically acceptable salts or esters thereof wherein A is a hydrogen atom or an esterifying radical; X is an alkyl group of 1-12 carbon atoms optionally substituted by a hydroxy, amino, acylamino of C.sub.1-6 alkoxy group, which substituents are not on the carbon atom adjacent to the nitrogen atom; or a C.sub.5-7 cycloalkyl group; or a phenylalkyl group wherein the carbon atom content of the alkyl part is 1-6 and the phenyl part is optionally substituted with a fluorine, bromine, chlorine, C.sub.1-6 alkyl, or C.sub.1-6 alkoxy; with the proviso that when X represents an optionally substituted phenylalkyl group and A represents C.sub.1-3 alkyl, then the --CO.sub.2 A group is attached to the alkyl part of the phenylalkyl group; have been found to be .beta.-lactamase inhibitors and antibacterial agents. Their preparation and use is described.
    Type: Grant
    Filed: April 13, 1983
    Date of Patent: March 24, 1987
    Assignee: Beecham Group p.l.c.
    Inventors: Brian P. Clarke, John B. Harbridge, Irene Stirling
  • Patent number: 4650795
    Abstract: The present invention provides the salts of the formula (II): ##STR1## wherein R.sup.1 is a hydrogen atom or a lower alkyl, aralkyl, phenyl or inertly substituted lower alkyl, aralkyl or phenyl group; R.sup.2 is a hydrogen atom or a lower alkyl, aralkyl, phenyl or inertly substituted lower alkyl, aralkyl or phenyl group; and R.sup.3 is lower alkyl, aralkyl, phenyl or inertly substituted lower alkyl, aralkyl or phenyl group; any of said groups R.sup.1, R.sup.2 and R.sup.3 being optionally interlinked to form a ring of 5-7 ring atoms. The compounds are antibacterials.
    Type: Grant
    Filed: October 28, 1985
    Date of Patent: March 17, 1987
    Assignee: Beecham Group p.l.c.
    Inventors: Michael Liberman, Kenneth T. Veal
  • Patent number: 4647558
    Abstract: A monocyclic .beta.-lactam antibiotic having a formamido substituent at the 3S-position, including compounds of the formula (I): ##STR1## and salts thereof wherein R is --SO.sub.3 H; --PO(OH)Y wherein Y is C.sub.1-6 alkoxy, hydroxy, aryloxy, C.sub.1-6 alkyl or aryl; ##STR2## wherein Z represents C.sub.1-6 alkyl or aryl; ##STR3## wherein Z.sup.1 and Z.sup.2 may be the same or different and each represents hydrogen, C.sub.1-6 alkyl, aryl, amino or C.sub.1-6 alkoxy, or Z.sup.1 and Z.sup.2 together form the residue of a heterocyclic ring; --OSO.sub.3 H; or ##STR4## where X is hydrogen or hydroxy; R.sup.1 is an amino, protected amino or carboxylic acylamino group, and R.sup.2 and R.sup.3 are independently selected from hydrogen or a hydrocarbon group of 1 to 18 carbon atoms.
    Type: Grant
    Filed: January 20, 1983
    Date of Patent: March 3, 1987
    Assignee: Beecham Group p.l.c.
    Inventors: Roger J. Ponsford, Michael J. Pearson, Stephen C. Finch
  • Patent number: 4647692
    Abstract: Process for racemization of amino acids by use of a ketone and an organic acid such as acetic acid. In particular, a process for resolution of free .alpha.-amino acids with in situ racemization. The resolution of 4-hydroxyphenylglycine and 3,4-dihydroxyphenylglycine with 3-bromocamphor-9-sulphonic acid with in situ racemization are specifically mentioned.
    Type: Grant
    Filed: August 28, 1985
    Date of Patent: March 3, 1987
    Assignee: Beecham Group p.l.c.
    Inventor: Victor W. Jacewicz
  • Patent number: 4647670
    Abstract: Compounds of formula (I): ##STR1## wherein the various substituents are defined hereinbelow, having anti-hypertensive activity.
    Type: Grant
    Filed: December 10, 1984
    Date of Patent: March 3, 1987
    Assignee: Beecham Group p.l.c.
    Inventors: John M. Evans, Robin E. Buckingham, Kenneth Willcocks
  • Patent number: 4647659
    Abstract: 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: Grant
    Filed: January 22, 1985
    Date of Patent: March 3, 1987
    Assignee: Beecham Group p.l.c.
    Inventors: Michael A. Cook, Alan D. Curzons, Robert B. Wilkins
  • Patent number: 4645671
    Abstract: Tetrazolyl derivatives of clavulanic acid are described, having the formula: ##STR1## wherein X is an optionally substituted tetrazolyl group attached via a nitrogen atom. These compounds are useful as antibiotics and .beta.-lactamase inhibitors.
    Type: Grant
    Filed: July 15, 1985
    Date of Patent: February 24, 1987
    Assignee: Beecham Group p.l.c.
    Inventor: John B. Harbridge
  • Patent number: 4644070
    Abstract: Anti-hypertensive compounds of formula (I): ##STR1## wherein: one of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.1-3 alkylcarbonyl, and the other is methoxy or amino optionally substituted by one or two C.sub.1-6 alkyl or by C.sub.2-7 alkanoyl;one of R.sub.3 and R.sub.4 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl, or R.sub.3 and R.sub.4 together with the carbon atom to which they are attached are C.sub.3-6 spiroalkyl;R.sub.5 is hydrogen, C.sub.1-3 alkyl or C.sub.1-8 acyl; andn is 1 or 2; the lactam group being trans to the OR.sub.5 group; or, when the other of R.sub.1 and R.sub.2 is amino, a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 18, 1984
    Date of Patent: February 17, 1987
    Assignee: Beecham Group p.l.c.
    Inventors: John M. Evans, Robin E. Buckingham, Kenneth Willcocks
  • Patent number: 4640928
    Abstract: 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, benzoyl, 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: Grant
    Filed: October 1, 1985
    Date of Patent: February 3, 1987
    Assignee: Beecham Group p.l.c.
    Inventor: Kenneth Willcocks
  • Patent number: 4639534
    Abstract: Procedure for isolating lithium pseudomonate from a crude preparation containing pseudomonic acid by extracting the crude preparation into a suitable organic solvent in which pseudomonic acid is soluble, treating the extract with a lithium alkanoic acid and separating the resulting crystalline non-hygroscopic lithium pseudomonate, the crude preparation containing pseudomonic acid being a culture medium on or in which pseudomonic acid producing strains of bacteria have been grown, such as Pseudomonas fluorescens.
    Type: Grant
    Filed: December 21, 1984
    Date of Patent: January 27, 1987
    Assignee: Beecham Group p.l.c.
    Inventor: Alan D. Curzons
  • Patent number: 4638066
    Abstract: Compounds of formula (I), ##STR1## or an N-oxide or pharmaceutically acceptable salt thereof, wherein R.sub.1 is hydrogen, C.sub.1-7 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, hydroxy, thiol, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, carboxy, C.sub.1-4 alkoxycarbonyl, C.sub.1-4 alkanoyl, amino optionally substituted by one or two C.sub.1-4 alkyl or by C.sub.4-6 polymethylene optionally containing an oxygen or nitrogen atom, aminocarbonyl optionally N-substituted by one or two C.sub.1-4 alkyl, or benzoyl or phenyl either being optionally ring-substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or trifluoromethyl, R.sub.2 and R.sub.3 are the same or different and are hydrogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen or trifluoromethyl, m is 1 to 3 and n is 1 or 2, the hydrogen atom bonded to the C.sub.a carbon atom being trans to the hydrogen atom bonded to the C.sub.
    Type: Grant
    Filed: December 20, 1984
    Date of Patent: January 20, 1987
    Assignee: Beecham Group p.l.c.
    Inventors: Laramie M. Gaster, Barry S. Orlek
  • Patent number: 4631282
    Abstract: Antihypertensive compounds of formula (I): ##STR1## wherein the various substituents are defined hereinbelow.
    Type: Grant
    Filed: June 20, 1985
    Date of Patent: December 23, 1986
    Assignee: Beecham Group Plc
    Inventor: Frederick Cassidy
  • Patent number: 4629737
    Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereof, in which: W is an optionally substituted phenyl group of the formula ##STR2## wherein R.sup.1 is hydrogen or fluorine, R.sup.2 is hydrogen, C.sub.1-6 alkyl, halogen or trifluoromethyl; or W is a phenoxymethyl or benzofuran-2-yl group;R.sup.3 is C.sub.1-12 alkyl or phenyl C.sub.1-6 alkyl;A is hydrogen or methyl,X is carboxy, --Z--CO.sub.2 H, --Z--OH, T--Z--CO.sub.2 H,--Z--NR.sup.4 R.sup.5, --T--Y--OM, --T--Y--NR.sup.4 R.sup.5, or --T--R.sup.6, in the para- or meta-position with respect to the --(CH.sub.2).sub.n group,whereinR.sup.4 and R.sup.5 are each hydrogen or C.sub.1-6 alkyl,R.sup.6 is C.sub.1-6 alkyl,T is 0, S, --NH or --N--R.sup.7, in which R.sup.7 is C.sub.1-6 alkylZ is C.sub.1-10 straight or branched alkylene optionally containing a carbon-carbon double bond;Y is C.sub.2-10 straight or branched alkylene, provided that the hetero atoms in --T--Y--OM and --T--Y--NR.sup.4 R.sup.
    Type: Grant
    Filed: July 14, 1983
    Date of Patent: December 16, 1986
    Assignee: Beecham Group p.l.c.
    Inventor: Barrie C. C. Cantello
  • Patent number: 4629734
    Abstract: Compounds of formula (I): ##STR1## wherein: R.sub.1 -R.sub.6 are as defined in the specification;X is oxygen or sulphur; and the R.sub.6 NCXR.sub.5 and OCOH moieties are trans and, when one or the other of R.sub.1 and R.sub.2 is an amino group, pharmaceutically acceptable salts thereof, a process and intermediates for preparing them, pharmaceutical compositions containing them, and their use in the treatment of mammals.
    Type: Grant
    Filed: May 16, 1984
    Date of Patent: December 16, 1986
    Assignee: Beecham Group p.l.c.
    Inventor: Valerie A. Ashwood