Patents Assigned to Beecham Group p.l.c.
  • Patent number: 4762847
    Abstract: A topical composition for application to skin affected by acne containing from 0.05 to 2% by weight of Octopirox together with a non-irritant topically acceptable carrier. The composition is particularly useful for treating acne vulgaris.
    Type: Grant
    Filed: October 2, 1986
    Date of Patent: August 9, 1988
    Assignee: Beecham Group p.l.c.
    Inventors: Peter J. Edwards, Carol A. Jeffryes, Fiona M. Swain
  • Patent number: 4758677
    Abstract: 2,2-Dimethyl-3,4-dihydro-2H-benzo[b]pyran-3-ols bearing an amino group in the 4-position and a cyano group in the benzo ring, their salts, esters and ethers, demonstrate excellent vasodilatory activity. The compounds, of which trans-2,2-dimethyl-4-isopropylamino-6-cyano-3,4-dihydro-2H-benzo[b]pyran-3 -ol is a representative embodiment, can be prepared from the corresponding 3,4-epoxy derivative upon treatment with an amine.
    Type: Grant
    Filed: November 17, 1982
    Date of Patent: July 19, 1988
    Assignee: Beecham Group p.l.c
    Inventor: John M. Evans
  • Patent number: 4755525
    Abstract: A compound of the general formula I: ##STR1## or a salt or solvate thereof, in which, R.sup.1 represents hydrogen or a lower alkyl group,R.sup.2 represents hydrogen, a lower alkyl group, or ##STR2## R.sup.3 represents hydrogen, a lower alkyl group, or ##STR3## R.sup.4 represents a lower alkyl group substituted by one or more fluorine atoms,R.sup.5 represents hydrogen, halogen or lower alkyl, andR.sup.6 represents a lower alkyl or a substituted or unsubstituted carbocyclic aryl group. The compounds are useful as inhibitors of 5-lipoxygenase.
    Type: Grant
    Filed: June 17, 1986
    Date of Patent: July 5, 1988
    Assignee: Beecham Group p.l.c.
    Inventors: Roger E. Markwell, Stephen A. Smith
  • Patent number: 4753962
    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: December 1, 1986
    Date of Patent: June 28, 1988
    Assignee: Beecham Group p.l.c.
    Inventors: Anthony T. Ainsworth, David G. Smith
  • Patent number: 4752581
    Abstract: A fibrinolytically active hybrid protein which comprises one chain of a 2-chain protease linked to a chain of a different 2-chain protease, or to the same chain of the same protease, at least one of the chains in the hybrid protein being derived from a fibrinolytically active protease, such that the hybrid protein has a catalytic site essential for fibrinolytic activity which is optionally blocked by a removable blocking group.
    Type: Grant
    Filed: December 21, 1984
    Date of Patent: June 21, 1988
    Assignee: Beecham Group p.l.c.
    Inventors: Jeffery H. Robinson, Ian Dodd
  • Patent number: 4745115
    Abstract: Compounds of the general formula I ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl or together are a group X which is C.sub.3-6 polymethylene optionally in which one carbon atom is replaced by O, S or NR.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl;R.sub.3 is a mono- or fused bi-cyclic heteroaromatic group having up to ten atoms in the aromatic ring(s), not more than four of which are selected from nitrogen, oxygen or sulphur, optionally C-substituted by one or more substituents selected from halogen, CF.sub.3, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl or cyano; or is phenyl or naphthyl, optionally substituted by one or more substituents selected from halogen, CF.sub.3, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl, carboxyl, C.sub.1-6 alkoxycarbonyl, cyano, CONR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are selected from hydrogen or C.sub.1-6 alkyl or together are a group X; NR.sub.9 R.sub.
    Type: Grant
    Filed: October 18, 1985
    Date of Patent: May 17, 1988
    Assignee: Beecham Group p.l.c.
    Inventors: Roger E. Markwell, Stephen A. Smith, David J. Hunter
  • Patent number: 4743593
    Abstract: An antibacterially active 9,11-O-methylene derivative of 9-dihydroerythromycin wherein the methylene group is optionally substituted by one or two hydrocarbon groups. In particular, compounds of formula I and their pharmaceutically acceptable esters and acid addition salts: ##STR1## wherein: R.sup.1 and R.sup.2 are each H, optionally substituted hydrocarbon, or optionally substituted 5 or 6-membered O or S heterocyclyl, orR.sup.1 +R.sup.2 is optionally substituted divalent hydrocarbon,R.sup.3 is H or OH;R.sup.4 is H, F or OH;R.sup.5 and R.sup.6 are each H of CH.sub.3 ;one of R.sup.7 and R.sup.8 is H, OH, alkoxy, alkanoyloxy optionally substituted NH.sub.2, or R.sup.9 --SO.sub.2 --O--, and the other of R.sup.7 and R.sup.8 is H, orR.sup.7 +R.sup.8 is oxo, oxime or substituted oxime; and R.sup.9 is organic.
    Type: Grant
    Filed: December 6, 1985
    Date of Patent: May 10, 1988
    Assignee: Beecham Group p.l.c.
    Inventor: Eric Hunt
  • Patent number: 4741903
    Abstract: A derivative of a fibrinolytic enzyme in which the catalytic site on the enzyme which is responsible for fibrinolytic activity is blocked by a human protein attached thereto by way of a reversible linking group.
    Type: Grant
    Filed: April 15, 1987
    Date of Patent: May 3, 1988
    Assignee: Beecham Group p.l.c.
    Inventor: Richard A. G. Smith
  • Patent number: 4738963
    Abstract: A method for the treatment and/or prophylaxis of incontinence in mammals, which method comprises administering to the mammal in need of said treatment an effective amount of a compound of formula (I): ##STR1## wherein R.sub.1 -R.sub.8 and X are as set forth herein.
    Type: Grant
    Filed: May 27, 1986
    Date of Patent: April 19, 1988
    Assignee: Beecham Group p.l.c.
    Inventors: Thomas C. Hamilton, Robin E. Buckingham
  • Patent number: 4737487
    Abstract: Peptides comprising, in sequence, units selected from the amino acid residues 11 to 23 of vasoactive intestinal peptide (VIP) and consisting at least of the amino acid residues 15 to 20, or an analogue thereof wherein one or more of the amino acid residues is replaced by an equivalent other amino acid, or a pharmaceutically acceptable salt thereof; having pharmacological activity, a process for their preparation and their use as pharmaceuticals.
    Type: Grant
    Filed: October 31, 1985
    Date of Patent: April 12, 1988
    Assignee: Beecham Group p.l.c.
    Inventors: Eric A. Watts, Gordon Wootton, Christine Summers
  • Patent number: 4732901
    Abstract: Compounds of formula (I): ##STR1## in which R.sub.1 is hydrogen or C.sub.1-6 alkyl;R.sub.2 is hydrogen or a group --CO.sub.2 R.sub.3 where R.sub.3 is hydrogen or C.sub.1-6 alkyl;n is an integer of from 2 to 12;X represents a double or triple bond, and each of A and B represents hydrogen when X is a double bond, or both A and B are absent when X is a triple bond; and ##STR2## represents an aromatic heterocyclic ring, are disclosed as inhibitors of 5-lipoxygenase.
    Type: Grant
    Filed: February 27, 1986
    Date of Patent: March 22, 1988
    Assignee: Beecham Group p.l.c.
    Inventor: Derek R. Buckle
  • Patent number: 4730050
    Abstract: A derivative of a fibrinolytic enzyme in which the catalytic site on the enzyme which is responsible for fibrinolytic activity is blocked by a human protein attached thereto by way of a reversible linking group.
    Type: Grant
    Filed: April 3, 1987
    Date of Patent: March 8, 1988
    Assignee: Beecham Group p.l.c.
    Inventor: Richard A. G. Smith
  • Patent number: 4725603
    Abstract: A method of treatment of migraine, cluster headaches and trigeminal neuralgia, radiation or cytotoxic agent induced nausea and vomiting and/or cardiac arrhythmia in mammals, including humans, which method comprises administering an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is C.sub.1-6 alkyl;R.sub.2 is amino or C.sub.1-7 acylamino;R.sub.3 is halo;one of R.sub.4 and R.sub.5 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-3 alkyl, which phenyl moieties may be substituted by one or more substituents selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3 or halogen;the other of R.sub.4 and R.sub.5 is hydrogen or C.sub.1-6 alkyl;p is 0 to 2; andq is 0 to 3.
    Type: Grant
    Filed: June 20, 1986
    Date of Patent: February 16, 1988
    Assignee: Beecham Group, p.l.c.
    Inventors: Gareth J. Sanger, Wesley D. Miner
  • Patent number: 4721720
    Abstract: A method of treatment of emesis, anxiety and/or IBS in mammals, including humans, which method comprises administering an effective amount of a compound of formula (I) or (II) or a pharmaceutically acceptable salt thereof:Ar--Co--Y--Z (I)wherein Ar is a group of formula (a): ##STR1## wherein: R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-4 alkoxy, hydroxy, amino optionally substituted by one or two C.sub.1-4 alkyl groups, thiol, C.sub.1-4 alkylthio; X is CH.sub.2, NR.sub.3, --O-- or --S-- wherein R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.3-5 alkenyl, phenyl or phenyl C.sub.1-4 alkyl; or Ar is a group of formula (b): ##STR2## wherein R.sub.4 to R.sub.7 are independently hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, amino optionally substituted by one or two C.sub.1-4 alkyl, by C.sub.1-4 alkanoylamino or pyrrolyl, one of R.sub.4 to R.sub.
    Type: Grant
    Filed: March 12, 1986
    Date of Patent: January 26, 1988
    Assignee: Beecham Group p.l.c.
    Inventors: Gordon Wootton, Gareth J. Sanger
  • Patent number: 4721723
    Abstract: The invention provides crystalline paroxetine hydrochloride hemihydrate, processes for its preparation, compositions containing the same and its therapeutic use as an anti-depressant.
    Type: Grant
    Filed: October 23, 1986
    Date of Patent: January 26, 1988
    Assignee: Beecham Group p.l.c.
    Inventors: Roger D. Barnes, Marian W. Wood-Kaczmar, Alan D. Curzons, Ian R. Lynch, John E. Richardson, Philip C. Buxton
  • Patent number: 4719217
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is C.sub.1-6 alkyl;R.sub.2 is amino or C.sub.1-7 acylamino;R.sub.3 is halo or C.sub.1-6 alkythio;R.sub.4 and R.sub.5 are independently selected from 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 two of halo, CF.sub.3, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;R.sub.6 is C.sub.1-7 alkyl, --(CH.sub.2).sub.s R.sub.7, s being 0 to 2 andR.sub.7 being C.sub.3-8 cycloalky, --(CH.sub.2).sub.t R.sub.8, t being 1 or 2 andR.sub.8 being thienyl or phenyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy and C.sub.1-4 alkyl optionally substituted by hydroxy, C.sub.
    Type: Grant
    Filed: June 26, 1986
    Date of Patent: January 12, 1988
    Assignee: Beecham Group p.l.c.
    Inventors: Francis D. King, Michael S. Hadley
  • Patent number: 4716160
    Abstract: Compounds of formula (I) ##STR1## wherein: R is hydrogen or C.sub.1-6 alkyl;R.sub.1 and R.sub.2 are both hydrogen; orR.sub.1 is hydrogen, C.sub.1-6 alkyl; and R.sub.2 is CN; CR.sub.5 R.sub.6 Y where R.sub.5 and R.sub.6 are independently selected from hydrogen and C.sub.1-4 alkyl and Y is selected from hydrogen, OR.sub.7 or SR.sub.7 where R.sub.7 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkanoyl, and NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkanoyl or together are C.sub.4-6 polymethylene, or COR.sub.10 where R.sub.10 is OH or C.sub.1-4 alkyl, or COR.sub.10 is a pharmaceutically acceptable ester or amide; orR.sub.2 is hydrogen, C.sub.1-6 alkyl, or phenyl optionally substituted by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; and R.sub.1 is CN, CR.sub.5 R.sub.6 Y or COR.sub.10 as defined for R.sub.2 above; orR.sub.1 and R.sub.2 together form C.sub.3 -C.sub.6 polymethylene optionally substituted by C.sub.1 -C.sub.4 alkyl;R.
    Type: Grant
    Filed: April 25, 1986
    Date of Patent: December 29, 1987
    Assignee: Beecham Group p.l.c.
    Inventors: Roger E. Markwell, Robert W. Ward, Carol R. de Mello
  • Patent number: 4713486
    Abstract: A compound of formula (I): ##STR1## or a salt, ester or amide thereof, in whichY is a group --O(CH.sub.2).sub.m --, --(CH.sub.2).sub.m -- or --CH.dbd.CH-- where m is an integer of from 1 to 5 n is an integer of from 4 to 14X represents a double or triple bond, and each of A and B represents hydrogen when X is a double bond, or both A and B are absent when X is a triple bond,is useful in the treatment of allergic diseases.
    Type: Grant
    Filed: October 21, 1985
    Date of Patent: December 15, 1987
    Assignee: Beecham Group p.l.c.
    Inventor: Derek R. Buckle
  • Patent number: 4707474
    Abstract: Compositions comprising a cloxacillin salt and liquid paraffin, arachis oil or fractionated coconut oil are useful in treating infectious keratoconjunctivitis in cattle and domestic animals.
    Type: Grant
    Filed: May 6, 1983
    Date of Patent: November 17, 1987
    Assignee: Beecham Group p.l.c.
    Inventor: Robert J. Bywater
  • Patent number: D294119
    Type: Grant
    Filed: April 16, 1985
    Date of Patent: February 9, 1988
    Assignee: Beecham Group p.l.c.
    Inventor: Geoffrey A. Ryder