Patents Assigned to Beecham Group
  • Patent number: 4987138
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##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, 1-mercapto C.sub.2-7 alkyl, 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 ethenyl 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.
    Type: Grant
    Filed: August 11, 1988
    Date of Patent: January 22, 1991
    Assignee: Beecham Group p.l.c.
    Inventors: Frederick Cassidy, Geoffrey Stemp
  • Patent number: 4980153
    Abstract: An oral hygiene composition in the form of a dentifrice or a mouthwash, comprising: (a) from 0.01 to 2% by weight of the composition of an antibacterial compound of formula (I): ##STR1## in which R.sup.1 is oxygen, sulphur or an alkylene group of from 1 to 6 carbon atoms, each of R.sub.2 to R.sub.6 and R.sup.2 ' to R.sup.6 ' is hydrogen, hydroxyl or halogen; (b) from 0 to 90% by weight of a dentally acceptable abrasive, (c) from 0.1% to 15% by weight of a dialkali or tetra-alkali metal pyrophosphate salt or a mixture thereof and (d) water.
    Type: Grant
    Filed: March 15, 1989
    Date of Patent: December 25, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Robert J. Jackson, Nicholas A. Berrill, Shawn V. Robbins
  • Patent number: 4971975
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which X represents R.sub.1 OOC-- in which R.sub.1 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl; R.sub.2 O-- in which R.sub.2 is C.sub.1-2 alkyl, C.sub.1-2 alkylcarbonyl or aminocarbonyl optionally substituted by one or two methyl groups;a group ##STR2## in which Y represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises one or two heteroatoms selected from oxygen, nitrogen and sulphur, any amino nitrogen optionally substituted by a C.sub.1-2 alkyl group, Y being optionally C-substituted by a methyl group; or a group ##STR3## in which A.sub.1 is oxygen or sulphur, one of A.sub.2 and A.sub.3 is CR.sub.3 and the other is nitrogen or CR.sub.4 where R.sub.3 and R.sub.4 are independently selected from hydrogen and methyl; and each of p and q independently represents an integer of 2 to 4.
    Type: Grant
    Filed: April 15, 1988
    Date of Patent: November 20, 1990
    Assignee: Beecham Group plc
    Inventors: Michael S. Hadley, Paul A. Wyman, Barry S. Orlek
  • Patent number: 4970159
    Abstract: A purified fibrinolytically active degraded species of tissue-type plasminogen activator comprising a fibrinolytically intact B chain of native t-PA linked to kringle 2 as the only functionally and structurally intact domain of native t-PA A chain.
    Type: Grant
    Filed: April 1, 1986
    Date of Patent: November 13, 1990
    Assignee: Beecham Group p.l.c.
    Inventor: Ian Dodd
  • Patent number: 4968691
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which X represents a group ##STR2## in which p represents an integer of 2 to 4; r represents an integer of 1 or 2; s represents 0 or 1; and A represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises one or two heteroatoms selected from oxygen, nitrogen and sulphur, any amino nitrogen optionally substituted by a C.sub.1-4 alkyl group, and when (p,r,s) is (2,2,0) or (2,2,1) any A comprising 2 heteroatoms is optionally C-substituted by a methyl group, and when (p,r,s) is (2,1,0), (2,1,1) or (3,1,0) any A comprising 2 heteroatoms is optionally C-substituted by C.sub.1-2 alkyl and any A comprising one heteroatom is optionally C-substituted by a methyl group, and wherein compounds of formula (I) having two asymetric centers have the stereo-chemical configuration in which the group X and the (CH.sub.2).sub.
    Type: Grant
    Filed: March 7, 1989
    Date of Patent: November 6, 1990
    Assignee: Beecham Group P.L.C.
    Inventors: Barry S. Orlek, Michael S. Hadley, Howard E. Rosenberg, Harry J. Wadsworth
  • Patent number: 4965270
    Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is hydrogen or CH.sub.2 OH;R.sub.2 is hydrogen or, when R.sub.1 is hydrogen, hydroxy or CH.sub.2 OH;R.sub.3 is CH.sub.2 OH or, when R.sub.1 and R.sub.2 are both hydrogen, CH(OH)CH.sub.2 OH;R.sub.4 is hydrogen, hydroxy, amino or OR.sub.5 whereinR.sub.5 is C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-2 alkyl either of which phenyl moieties may be substituted by one or two halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy groups;and in which any OH groups in R.sub.1, R.sub.2 and R.sub.3 may be in the form of O-acyl, phosphate, cyclic acetal or cyclic carbonate derivatives thereof; having antiviral activity.
    Type: Grant
    Filed: November 7, 1989
    Date of Patent: October 23, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Michael R. Harnden, Paul G. Wyatt, Stuart Bailey
  • Patent number: 4959374
    Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereif, wherein: Z represents a residue of a substituted or unsubstituted aryl group,X represents o or NR.sup.o wherein R.sup.0 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, an alkanoyl group substituted or unsubstituted in the alkyl moiety, or an arylalkyl moiety substituted or unsubstituted in the aryl moiety,n represents an integer 1 or 2,m represents an integer 1 or 2,p represents an integer 2 or 3,andq represents an integer in the range of from 1 to 12; pharmaceutical compositions containing such compounds and the use of such compounds and compositions in medicine.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: September 25, 1990
    Assignee: Beecham Group P.L.C.
    Inventor: John M. Berge
  • Patent number: 4959367
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is N or CH;R.sub.1 and R.sub.2 are the same or different and are hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-7 acyl, C.sub.1-7 acylamino, or amino, aminocarbonyl or aminosulphonyl, optionally substituted by one or two C.sub.1-6 alkyl or C.sub.3-8 cycloalkyl groups, or by C.sub.4-5 polymethylene or by phenyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsuphinyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, hydroxy or nitro; or R.sub.1 and R.sub.2 taken together are methylenedioxy or ethylenedioxy;Z is a group of formula (a), (b) or (c) ##STR2## wherein n is 2 or 3; p is 1 or 2; q is 1 to 3; r is 1 to 3; andR.sub.3 or R.sub.4 is C.sub.1-4 alkyl;having 5-HT.sub.3 receptor antagonist activity, a process for their preparation and their use as pharmaceuticals.
    Type: Grant
    Filed: November 2, 1988
    Date of Patent: September 25, 1990
    Assignee: Beecham Group P.L.C.
    Inventor: Francis D. King
  • Patent number: 4957733
    Abstract: Pharmaceutical product comprising an interferon and a compound of formula (A) ##STR1## or a pro-drug, or a pharmaceutically acceptable salt, phosphate ester and/or acyl derivative or either of the foregoing as a combined preparation for simultaneous, separate or sequential use in antiviral therapy.
    Type: Grant
    Filed: November 30, 1987
    Date of Patent: September 18, 1990
    Assignee: Beecham Group P.L.C.
    Inventors: Martin Cole, Malcolm R. Boyd, David Sutton
  • 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: 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: 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: 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: 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: 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: 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