Patents Assigned to Beecham Group
  • Patent number: 5130241
    Abstract: A compound having the formula (I): ##STR1## is described, together with salts thereof and an enzymatic process for converting such compounds into clavulanic acid.A process for the preparation of the compound of formula (I) and its salts is disclosed, together with intermediates for use therein. This process involves the use of a novel enzyme system to effect the desired cyclisation, which enzyme system is preferably derived from a micro-organism, in particular a species of Streptomyces.
    Type: Grant
    Filed: December 26, 1990
    Date of Patent: July 14, 1992
    Assignee: Beecham Group plc
    Inventors: Stefan R. Woroniecki, Stephen W. Elson, Keith H. Baggaley
  • Patent number: 5126335
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts and in-vivo hydrolysable esters thereof: ##STR1## wherein X is hydrogen or a group NHR.sup.1, wherein R.sup.1 is hydrogen or an amino protecting group, and R is an optionally substituted 5-membered or 6-membered saturated heterocyclic group containing 1 or 2 heteroatoms selected from oxygen, sulphur or nitrogen, are useful in the treatment of bacterial infections in humans and animals.
    Type: Grant
    Filed: March 21, 1990
    Date of Patent: June 30, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Roger J. Ponsford, Andrew V. Stachulski
  • Patent number: 5126460
    Abstract: A process for the preparation of a pure (3S,4R)-isomer of a compound of formula (A): ##STR1## wherein the substituents are herein defined in which the pyrrolidonyl or piperidonyl ring is formed by cyclizing an appropriate precursor dihydrobenzopyranol compound that has already been resolved to the (3S,4R)-configuration, or a mixture in which the (3S,4R)-configuration predominates with respect to the (3S,4R)-configuration.
    Type: Grant
    Filed: January 30, 1990
    Date of Patent: June 30, 1992
    Assignee: Beecham Group p.l.c.
    Inventor: Erol A. Faruk
  • Patent number: 5124322
    Abstract: Novel compounds of formula (I), salts, solvates and hydrates thereof: ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen; alkyl; alkoxy; halogen; or CF.sub.3 ;R.sub.3 is hydrogen; acyl, such as ##STR2## where Z is optionally substituted aryl; or a group R--S-- where R is an organic residue such that the group R--S-- provides an in vivo-cleavable disulphide bond;R.sub.4 is C.sub.3-6 alkyl;R.sub.5 is hydrogen; alkyl; --CH.sub.2 --R.sub.10 where R.sub.10 is optionally substituted phenyl or heteroaryl; or a group ##STR3## where R.sub.11 is hydrogen; alkyl; or --CH.sub.2 --Ph is optionally substituted phenyl; and R.sub.12 is hydrogen or alkyl; andR.sub.6 is hydrogen; alkyl; or a group ##STR4## where R.sub.13 is hydrogen; or alkyl; and R.sub.14 is hydroxy; alkoxy; or --NR.sub.7a R.sub.8 where each of R.sub.7a and R.sub.8 is hydrogen or alkyl, or R.sub.7a and R.sub.
    Type: Grant
    Filed: June 19, 1989
    Date of Patent: June 23, 1992
    Assignee: Beecham Group p.l.c.
    Inventor: Ian Hughes
  • Patent number: 5116960
    Abstract: Compounds of formula (I) or salts thereof: ##STR1## wherein: each R.sub.1 is independently hydrogen or a silyl protecting group; R.sub.2 is a carboxylic acid or derivative thereof; a ketone or aldehyde function; hydroxymethyl in which the hydroxyl function is optionally silylated, or substituted by hydroxy C.sub.1-4 alkyl, alkoxy C.sub.1-4 alkyl, alkoxycarbonyl C.sub.1-4 alkyl, hydroxycarbonyl C.sub.1-4 alkyl, alkyl, alkanoyl, or optionally substituted aryl or aroyl; one of X and Y is hydrogen, and the other is a sugar residue; hydroxy; optionally substituted C.sub.1-6 alkoxy or C.sub.3-8 cycloalkoxy; alkanoyloxy; thioalkanoyloxy; sulphonyloxy; halogen; or optionally substituted aryloxy, aralkyloxy or aroyloxy; or X and Y together with the carbon atom to which they are bonded are a carbonyl group or derivative thereof, are provided; their use as chemical intermediates and in the treatment of fungal infections is described.
    Type: Grant
    Filed: June 9, 1989
    Date of Patent: May 26, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Michael J. Driver, David T. MacPherson, William S. MacLachlan
  • Patent number: 5114929
    Abstract: An unpressurized container containing a palatable pharmaceutical formulation comprising a homogeneous, non-aqueous suspension of an orally active medicament, an edible oily vehicle, an edible emulsifier and a finely particulate sugar having no oily after taste.
    Type: Grant
    Filed: March 1, 1990
    Date of Patent: May 19, 1992
    Assignee: Beecham Group p.l.c.
    Inventor: Robert R. Vartan
  • Patent number: 5112600
    Abstract: An anti-caries composition has a source of hydrogen citrate ions, preferably an alkali metal hydrogen citrate salt, an oxalate salt and an orally acceptable excipient, and optionally further comprises an ionic fluorine-containing compound. The composition may be in the form of dentifrice when silica is the preferred abrasive, or a mouthwash.
    Type: Grant
    Filed: May 16, 1991
    Date of Patent: May 12, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Robert J. Jackson, Susan A. Duke, Paul Barnett
  • Patent number: 5110828
    Abstract: Novel compounds of formula (I), a process for their preparation, and their use as pharmaceutical agents are described: ##STR1## wherein R.sub.1 represents ##STR2## in which each of p and q independently represents an integer of 2 to 4, r represents an integer of 2 to 4, s represents 1 or 2 and t represents 0 or 1;R.sub.2 is a group OR.sub.4, where R.sub.4 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, a group OCOR.sub.5 where R.sub.5 is hydrogen or R.sub.4, or a group NHR.sub.6 or NR.sub.7 R.sub.8 where R.sub.6, R.sub.7 and R.sub.8 are independently C.sub.1-2 alkyl; andR.sub.3 is hydrogen or C.sub.1-4 alkyl, subject to the proviso that when R.sub.2 is a group OCOR.sub.5 or a group NHR.sub.6, R.sub.3 is C.sub.1-4 alkyl.
    Type: Grant
    Filed: April 13, 1989
    Date of Patent: May 5, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Steven M. Bromidge, Michael S. Hadley, Barry S. Orlek
  • Patent number: 5109000
    Abstract: Novel compounds of the formula (I), processes for their preparation and their use as collagenase inhibitors are described: ##STR1## in which R.sub.1 is hydroxy; alkoxy; aryloxy; aralkyloxy; --NR.sub.6 R.sub.7 where R.sub.6 and R.sub.7 are hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the N-atom to which they are bonded form a 5- to 7-membered ring with an optional heteroatom; --NHCH(R.sub.8)COR.sub.9 is hydrogen; alkyl optionally substituted by hydroxy, alkoxy, --NR.sub.6 R.sub.7, quanidine; CO.sub.2 H, CONH.sub.2, SH, or S-alkyl; or CH.sub.2 --AR where Ar is optionally substituted aryl; and R.sub.9 is hydroxy, alkoxy or --NR.sub.6 R.sub.7.R.sub.2 is hydrogen or acyl.R.sub.3 is C.sub.3-6 alkyl.R.sub.4 is hydrogen; alkyl; --CH.sub.2 R.sub.10 where R.sub.10 is optionally substituted phenyl or heteroaryl; or --CH(R.sub.12) O--R.sub.11 where R.sub.11 is hydrogen; alkyl; or --CH.sub.2 Ph where Ph is optionally substituted phenyl; and R.sub.12 is hydrogen or alkyl.R.sub.5 is hydrogen; alkyl; or --CH(R.
    Type: Grant
    Filed: April 30, 1990
    Date of Patent: April 28, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Roger E. Markwell, Stephen A. Smith, Ian Hughes
  • Patent number: 5108994
    Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is hydroxy or amino;R.sub.2 is hydrogen or amino;R.sub.3 is hydrogen, hydroxymethyl or acyloxymethyl;R.sub.4 is a group of formula: ##STR2## wherein R.sub.5 and R.sub.6 are independently selected from hydrogen, C.sub.1-6 alkyl and optionally substituted phenyl; orR.sub.3 and R.sub.4 together are: ##STR3## wherein R.sub.6 is as defined above;having antiviral activity, processes for their preparation and their pharmaceutical use.
    Type: Grant
    Filed: May 23, 1990
    Date of Patent: April 28, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Michael R. Harnden, Leslie J. A. Jennings
  • Patent number: 5100876
    Abstract: Compounds of the formula (I), or pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is --CH.sub.2 OH; R.sub.2 is hydrogen or C.sub.1-8 alkyl; R.sub.3 is hydrogen or an amine protection group; and each R.sub.4 is hydrogen; their preparation, compositions containing them and their use in the treatment of fungal infections are described.
    Type: Grant
    Filed: December 11, 1989
    Date of Patent: March 31, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Michael J. Driver, William S. MacLachlan, Andrew W. Taylor
  • Patent number: 5098909
    Abstract: A method of treatment of cough and/or bronchoconstriction in mammals, including humans, which method comprises the administration to the mammal in need of such treatment, an effective amount of a 5-HT.sub.3 receptor antagonist.
    Type: Grant
    Filed: July 10, 1989
    Date of Patent: March 24, 1992
    Assignee: Beecham Group, p.l.c.
    Inventor: Andrew J. Williams
  • Patent number: 5093493
    Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof: ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-4 alkyl wherein the phenyl moiety is optionally substituted by one or more C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, hydroxy, C.sub.2-7 alkanoyl, halo, trifluoromethyl, nitro, amino optionally substituted by one or two C.sub.1-6 alkyl groups or by C.sub.2-7 alkanoyl, cyano, carbamoyl or carboxy groups;R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl, trifluoromethyl, cyano, carbamoyl and carboxy, and phenyl or phenyl C.sub.1-4 alkyl in which any phenyl moiety is optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxy carbonyl, C.sub.1-6 alkylthio, hydroxy, C.sub.2-7 alkanoyl, chloro, fluoro, trifluoromethyl, nitro or amino optionally substituted by one or two C.sub.1-6 alkyl groups or by C.sub.
    Type: Grant
    Filed: March 12, 1990
    Date of Patent: March 3, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Mervyn Thompson, Ian T. Forbes, Christopher N. Johnson
  • Patent number: 5091397
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which one of X and Y represents hydrogen and the other represents --CH.sub.2 --Z where Z is a group ##STR2## in which Q represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises one or two heteroatoms selected from oxygen, nitrogen and sulphur, or three nitrogen atoms, any amino nitrogen being optionally substituted by a C.sub.1-2 alkyl, cyclopropyl or propargyl group, and any ring carbon atom being optionally substituted by a group R.sub.1 ; or a group ##STR3## in which A.sub.1, A.sub.2 and A.sub.3 complete a 5-membered aromtic ring and A.sub.1 is oxygen or sulphur, one of A.sub.2 and A.sub.3 is CR.sub.2 and the other is nitrogen or CR.sub.3, or A.sub.2 is oxygen or sulphur, one of A.sub.1 and A.sub.3 is CR.sub.2 and the other is CR.sub.3 ; and R.sub.1, R.sub.2 and R.sub.3 are independently selected from hydrogen, halogen, CN, OR.sub.4, SR.sub.4, N(R.sub.4).sub.2, NHCOR.sub.4, NHCOOCH.sub.
    Type: Grant
    Filed: September 29, 1989
    Date of Patent: February 25, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Harry J. Wadsworth, Michael S. Hadley, Paul A. Wyman, Sarah M. Jenkins
  • Patent number: 5087444
    Abstract: An oral hygiene composition for use in the treatment of dentine hypersensitivity comprises a water soluble strontium salt and a water soluble potassium salt, together with a dentally acceptable excipient. Preferably, the composition is in the form of a dentifrice comprising an abrasive silica and a thickening silica, and optionally includes an ionic fluorine-containing compound.
    Type: Grant
    Filed: March 27, 1990
    Date of Patent: February 11, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Robert J. Jackson, Susan A. Duke, Mark A. Wicks
  • Patent number: 5087626
    Abstract: A method for increasing the weight gain and/or improving the feed utilization of efficiency of livestock which comprises administering to livestock in need thereof an effective amount of a compound of formula (XXII): ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1Z is hydrogen, halogen, or trifluoromethyl; R.sup.2Z is hydrogen or halogen; R.sup.3Z is hydrogen or methyl; R.sup.4Z is --O(CH.sub.2).sup.6 CO.sub.2 H or an ester or amide thereof, O(CH.sub.2).sup..epsilon. M.sup.4 or --CO.sub.2 H or an ester or amide thereof, wherein .delta. is an integer from 1 to 6, .epsilon. is an integer from 2 to 7, and M.sup.4 is hydroxy, alkoxy of 1 to 6 carbon atoms or ##STR2## wherein R.sup.6Z and R.sup.7Z are each hydrogen or alkyl of 1 to 6 carbons or ##STR3## is a 5- or 6-membered ring; R.sup.
    Type: Grant
    Filed: September 7, 1989
    Date of Patent: February 11, 1992
    Assignee: Beecham Group p.l.c
    Inventor: Jonathan R. Arch
  • Patent number: 5082840
    Abstract: A method for increasing the weight gain and/or improving the feed utilization efficiency and/or increasing the lean body mass and/or decreasing birth mortality rate and increasing post-natal survival rate of livestock comprises the administration to livestock of an effective, non-toxic amount of a compound of formula (I), or a veterinarily acceptable acid addition salt thereof: ##STR1## wherein R.sup.1 is phenyl (C.sub.1-6) alkyl or optionally substituted C.sub.1-6 alkyl, andW is optionally substituted phenyl, a heterocyclyl group, or phenoxymethyl optionally substituted on the phenyl group. Certain compounds of formula (I) are novel.
    Type: Grant
    Filed: August 29, 1989
    Date of Patent: January 21, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Jonathan R. Arch, Norman H. Rogers
  • Patent number: D324997
    Type: Grant
    Filed: June 25, 1991
    Date of Patent: March 31, 1992
    Assignee: Beecham Group p.l.c.
    Inventor: Joe Jones
  • Patent number: D325339
    Type: Grant
    Filed: June 25, 1991
    Date of Patent: April 14, 1992
    Assignee: Beecham Group p.l.c.
    Inventor: Joe Jones
  • Patent number: D326182
    Type: Grant
    Filed: November 18, 1988
    Date of Patent: May 19, 1992
    Assignee: Beecham Group p.l.c.
    Inventor: Harriet M. Spry