Patents Assigned to Beecham Group p.l.c.
  • Patent number: 4957905
    Abstract: 9-(N'-substituted hydrazone) derivatives of certain erythromycin compounds are novel, antibacterially active compounds which can be prepared by treatment of the corresponding 9-imine derivative with an N'-substituted hydrazine.
    Type: Grant
    Filed: September 7, 1988
    Date of Patent: September 18, 1990
    Assignee: Beecham Group p.l.c.
    Inventor: Eric Hunt
  • Patent number: 4954489
    Abstract: Compounds of formula (I) and their salts and esters: ##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 optionally substituted C.sub.5-8 cycloalkyl or cycloalkenyl, are useful in the treatment of bacterial infections.
    Type: Grant
    Filed: April 5, 1989
    Date of Patent: September 4, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Roger J. Ponsford, Andrew V. Stachulski
  • Patent number: 4954532
    Abstract: A degreasing or moisturizing composition contains silanized silica gel, a humectant such as glycerine, and an inert carrier. The composition is used to treat sebhorreic conditions without causing dry skin.
    Type: Grant
    Filed: January 30, 1985
    Date of Patent: September 4, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Thomas J. Elliott, Susan Dutton
  • Patent number: 4952584
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt 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 alkoxy, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylthio, hydroxy, C.sub.2-7 alkanoyl, chloro, fluoro, trifluoromethyl, nitro, amino optionally substituted by one or two C.sub.1-6 alkyl groups or by C.sub.2-7 alkanoyl, cyano, carbamoyl and carboxy, and phenyl, phenyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkoxy in which any phenyl moiety is optionally substituted by any of these groups; R.sub.5 and R.sub.6 are independently selected from hydrogen, C.sub.
    Type: Grant
    Filed: February 6, 1989
    Date of Patent: August 28, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Mervyn Thompson, Ian T. Forbes
  • Patent number: 4946966
    Abstract: A process for the preparation of a compound of formula (I): ##STR1## which comprises the reactive of a methylating agent with a compound of formula (IV): ##STR2## in a polar solvent in which is dissolved an alkali metal alkoxide, in an inert atmosphere.
    Type: Grant
    Filed: December 20, 1988
    Date of Patent: August 7, 1990
    Assignee: Beecham Group P.L.C.
    Inventors: Francis D. King, Thomas W. Ramsay
  • Patent number: 4943582
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: X, Y and R.sub.1 -R.sub.6 are as defined have blood pressure lowering activity and K+ channel activator activity and are useful in the treatment of hypertension.
    Type: Grant
    Filed: May 1, 1987
    Date of Patent: July 24, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: John M. Evans, Geoffrey Stemp, Frederick Cassidy
  • Patent number: 4942166
    Abstract: A crystalline monohydrate of the compound of formula (A) or a crystalline sodium salt monohydrate of the compound of formula (A): ##STR1## having antiviral activity, processes for their preparation and their use as pharmaceuticals.
    Type: Grant
    Filed: June 30, 1989
    Date of Patent: July 17, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Michael R. Harnden, Richard L. Jarvest, Graham R. Geen
  • Patent number: 4942160
    Abstract: A method of treatment of visceral pain in mammals, including humans, which method comprises the administration to the mammal in need of such treatment, an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof:X--CO--Y--Z (I)whereinX is a group of formula (a), (b), (c), (d) or (e): ##STR1## wherein R.sub.a to R.sub.d are selected from hydrogen, halogen or hydroxy;R.sub.1 is hydrogen and R.sub.2 is a hydrogen or C.sub.1-4 alkyl; orR.sub.1 and R.sub.2 together are a bond;R.sub.3 to R.sub.7 are independently hydrogen or C.sub.1-6 alkyl; andR.sub.4 together with R.sub.2 may be C.sub.2-7 polymethylene when R.sub.1 is hydrogen;either R.sub.8 is C.sub.1-6 alkoxy;R.sub.9 is hydrogen;R.sub.10 is amino or C.sub.1-7 alkanoylamino; andR.sub.11 is halo or C.sub.1-6 alkylthio; orR.sub.8 is hydrogen;R.sub.9 is halo, or C.sub.1-6 alkoxy or C.sub.1-6 alkyl;R.sub.10 is hydrogen or C.sub.1-6 alkoxy; andR.sub.11 is halo, C.sub.1-6 alkoxy or C.sub.
    Type: Grant
    Filed: May 5, 1989
    Date of Patent: July 17, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Gareth J. Sanger, Helen E. Marr
  • Patent number: 4940702
    Abstract: .beta.-Lactam antibiotics are disclosed which have the formulae (Ia) or pharmaceutically acceptable salts or pharmaceutically acceptable in vivo hydrolysable esters thereof: ##STR1## wherein R.sup.1 is phenyl, substituted phenyl, cyclohexenyl, cyclohexadienyl, or an optionally substituted 5- or 6-membered heterocyclic ring containing up to three hetero-atoms selected from oxygen, sulphur or nitrogen; R.sup.2 is hydrogen or optionally substituted C.sub.1-6 alkyl; R.sup.3 is an optionally substituted 5- or 6- membered heterocyclic group containing one or two nitrogen heteroatoms; or R.sup.2 and R.sup.3 together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6- membered heterocyclic group contaning one or two nitrogen heteroatoms; R.sup.4 is a substituted pyridinium group; and CO.sub.2 R is carboxy or a carboxylate anion; and also the use thereof.Processes for the preparation of the compounds are disclosed together with intermediates for use therein.
    Type: Grant
    Filed: August 8, 1986
    Date of Patent: July 10, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Stephen C. Finch, Michael J. Pearson
  • Patent number: 4940701
    Abstract: A pharmaceutical composition for topical administration consisting of two liquid phases designed to be admixed in situ or prior to use. The first phase contains a dissolved drug, and is preferably saturated in the drug, while the second phase is a chemically or physically different liquid from that in the first phase and contains no drug, but is miscible with the first phase. The two liquids are selected so that, on admixture of suitable volumes of the phases, the resultant drug concentration exceeds the saturated drug solubility in the resultant mixture. This produces a liquid mixture supersaturated in drug, which has been found to increase the rate of drug penetration into the skin. The two liquid phases may be gels, and the drug may be hydrocortisone.At least one phase contains an antinucleant to improve stability of the resulting supersaturated solution.
    Type: Grant
    Filed: December 10, 1987
    Date of Patent: July 10, 1990
    Assignee: Beecham Group p.l.c.
    Inventor: Adrian F. Davis
  • Patent number: 4937243
    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 where R.sub.8 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.
    Type: Grant
    Filed: December 22, 1987
    Date of Patent: June 26, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Roger E. Markwell, Stephen A. Smith, Ian Hughes
  • Patent number: 4937247
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is CH or N;Y is NH or O;R.sub.1 is hydrogen or halogen;R.sub.2 is a group of formula (a), (b) or (c) ##STR2## wherein n is 2 or 3; p and q are independently 1 to 3; and R.sub.4 or R.sub.5 is C.sub.1-4 alkyl;R.sub.3 i s C.sub.1-10 acyl, C.sub.1-6 alkoxycarbonyl, optionally substituted phenoxycarbonyl or benzyloxycarbonyl, or R.sub.6 R.sub.7 NCO or R.sub.6 R.sub.7 NS(O).sub.m wherein m is 1 or 2 and R.sub.6 and R.sub.7 are independently C.sub.1-6 alkyl groups or together are C.sub.4-6 polymethylene; having 5-HT.sub.3 antagonist activity, a process for their preparation and their use as pharmaceuticals.
    Type: Grant
    Filed: September 25, 1987
    Date of Patent: June 26, 1990
    Assignee: Beecham Group p.l.c.
    Inventor: Francis D. King
  • Patent number: 4935404
    Abstract: Novel compounds of the formula (I), a process for their preparation and their use as collagenase inhibitors are described: ##STR1## in which R.sub.1 is hydrogen or hydroxy; R.sub.2 is hydrogen or alkyl; R.sub.3 is C.sub.3-6 alkyl; R.sub.4 is hydrogen, alkyl, --CH.sub.2 --Z where Z is optionally substituted phenyl or heteroaryl, or R.sub.4 is a group ##STR2## where R.sub.8 is hydrogen, alkyl or --CH.sub.2 --Ph where Ph is optionally substituted phenyl, and R.sub.9 is hydrogen or alkyl; and R.sub.5 is hydrogen or alkyl.
    Type: Grant
    Filed: November 14, 1988
    Date of Patent: June 19, 1990
    Assignee: Beecham Group p.l.c. of Beecham House
    Inventors: David J. Hunter, Roger E. Markwell, Robert W. Ward
  • Patent number: 4935465
    Abstract: A conjugate comprising a pharmaceutically useful protein linked to at least one water-soluble polymer by means of a reversible linking group.
    Type: Grant
    Filed: November 27, 1985
    Date of Patent: June 19, 1990
    Assignee: Beecham Group p.l.c.
    Inventor: Andrew J. Garman
  • Patent number: 4931434
    Abstract: Compounds of the general formula (II): ##STR1## in which N.sup.+ denotes an unsubstituted or substituted nitrogen-containing heterocyclyl ring bonded to the remainder of the molecule through a ring nitrogen atom and carrying a positive charge on said nitrogen atom;and the wavy line denotes either the E- or Z-isomeric position,are novel and are useful in the treatment of antibacterial infection in humans or animals.
    Type: Grant
    Filed: December 16, 1988
    Date of Patent: June 5, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Nigel J. P. Broom, Gerald Brooks, Brian P. Clarke
  • Patent number: 4923856
    Abstract: Compounds of the general formula (II): ##STR1## and pharmaceutically acceptable salts and in-vivo hydrolysable esters thereof, in whichR denotes a hydrogen atom or an in vivo hydrolysable acyl group;and the wavy line denotes either the E- or Z-isometric position,are novel compounds which exhibit .beta.-lactamase inhibitory action and have antibacterial properties.
    Type: Grant
    Filed: December 16, 1988
    Date of Patent: May 8, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Nigel J. P. Broom, Gerald Brooks, Steven Coulton
  • Patent number: 4921839
    Abstract: Antibacterially active 11,12-carbonate derivatives of erythromycin 9-(optionally substituted)oxime and 9-imino compounds and their pharmaceutically acceptable ester or acid addition salt thereof: ##STR1## wherein R.sup.1 denotes an oxime group, a substituted oxime group, or an imino group;R.sup.3 denotes a hydrogen atom or an unsubstituted or substituted alkyl group;R.sup.7 denotes hydrogen or methyl;one of R.sup.8 and R.sup.9 denotes hydrogen, hydroxy, alkoxy, alkanoyloxy, amino, substituted amino, or a group of the formula R.sup.A --SO.sub.2 --O--, in which R.sup.A denotes an organic group, and the other of R.sup.8 and R.sup.9 denotes hydrogen, orR.sup.8 and R.sup.9 together denote an oxo group, an oxime group, or a substituted oxime group.
    Type: Grant
    Filed: February 22, 1988
    Date of Patent: May 1, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Edward G. Brain, Eric Hunt, Andrew K. Forrest
  • Patent number: 4920127
    Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein L is NH or O;R.sub.1 is hydrogen, fluoro or chloro;R.sub.2 and R.sub.5 are independently hydrogen or C.sub.1-6 alkyl or together are a bond; orR.sub.2 and R.sub.3 and/or R.sub.4 and R.sub.5, together are C.sub.2-7 polymethylene or --(CH.sub.2).sub.m --O--(CH.sub.2).sub.x -- where m and x. are 1 to 5 such that m+x is 2 to 6;R.sub.4 is C.sub.1-7 acyl, C.sub.1-6 alkoxycarbonyl, hydroxycarbonyl, aminocarbonyl optionally substituted by one or two C.sub.1-6 alkyl groups, CF.sub.3, C.sub.1-6 alkyl substituted by C.sub.1-6 alkoxy, C.sub.1-6 alkylthio or by C.sub.1-6 alkoxycarbonyl, or R.sub.4 is phenyl or phenyl-C.sub.1-4 alkyl optionally substituted in the phenyl ring by one or two of halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy;Z is a group of formula (a), (b) or (c).
    Type: Grant
    Filed: February 16, 1988
    Date of Patent: April 24, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Francis D. King, Karen A. Joiner
  • Patent number: 4918083
    Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereof, or a pharmaceutically acceptable solvate thereof, wherein:Z represents a residue of a substituted or unsubstituted aryl group,A.sup.1 represents a substituted or unsubstituted methylene group or a substituted or unsubstituted ethylene group;A.sup.2 represents a substituted or unsubstituted methylene group or a substituted or unsubstituted ethylene group;providing that at least one of A.sup.1 or A.sup.2 represents a substituted methylene group or a substituted ethylene group,X represents O or NR.sup.o wherein R.sup.
    Type: Grant
    Filed: November 24, 1987
    Date of Patent: April 17, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: John M. Berge, Lee J. Beeley
  • Patent number: 4918091
    Abstract: A compound of formula (I): ##STR1## or a tautomeric form thereof, or a pharmaceutically acceptable salt thereof, wherein:R represents hydrogen or alkyl;R.sup.1 represents an alkyl group or a substituted or unsubstituted aryl group;R.sup.2 and R.sup.3 each represent hydrogen, or R.sup.2 and R.sup.3 together represent a bond;A represents a benzene ring having in total up to five substituents;X represents oxygen, sulphur or a moiety NR.sup.4 wherein R.sup.4 represents hydrogen or alkyl; andn represents an integer in the range of from 2 to 6; a process for preparing such a compound, a composition containing such a compound and the use of the compound and composition in medicine.
    Type: Grant
    Filed: June 13, 1988
    Date of Patent: April 17, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Barrie C. C. Cantello, Richard M. Hindley