Patents Assigned to Beecham Group p.l.c.
  • Patent number: 5068458
    Abstract: A process for the preparation of a compound of formula (I): ##STR1## in which X and Y are identical and represent halogen, or X is halogen and Y is hydrogen, which comprises halogenating 2-methyl-6-methoxynaphthalene, of formula (II): ##STR2## in the presence of a free radical initiator.
    Type: Grant
    Filed: June 28, 1990
    Date of Patent: November 26, 1991
    Assignee: Beecham Group p.l.c.
    Inventors: John R. M. Dales, Sidney E. Callander
  • Patent number: 5066670
    Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 is methoxy or optionally protected hydroxy have anthelmintic activity and are useful in the treatment of helminthiasis in humans and animals.
    Type: Grant
    Filed: March 9, 1990
    Date of Patent: November 19, 1991
    Assignee: Beecham Group p.l.c.
    Inventors: Roderick J. Dorgan, Graham S. Macaulay
  • Patent number: 5066646
    Abstract: compounds of formula (I) or pharmaceutically acceptable salts thereof; ##STR1## wherein R.sub.1 is a gorup -X-Y where X is a carbonyl group and Y is hydrogen, C.sub.1-8 alkyl, C.sub.2-8 alkenyl, or optionally substituted aryl or heteroaryl; R.sub.2 is hydroxy or C.sub.1-8 alkoxy; 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 as antifungal agents are described.
    Type: Grant
    Filed: December 11, 1989
    Date of Patent: November 19, 1991
    Assignee: Beecham Group p.l.c.
    Inventors: Michael J. Driver, Alexander R. Greenlees, David T. MacPherson
  • Patent number: 5066805
    Abstract: A process for the preparation of a compound of formula (I): ##STR1## which process comprises the reduction of a compound of formula (II): ##STR2## by catalytic hydrogenation using palladium on charcoal as catalyst.
    Type: Grant
    Filed: July 18, 1989
    Date of Patent: November 19, 1991
    Assignee: Beecham Group, p.l.c.
    Inventor: Peter M. Kincey
  • Patent number: 5064649
    Abstract: .beta.-Lactam antibiotics of the formula (Ia) or a pharmaceutically acceptable salt or pharmaceutically acceptable in vivo hydrolysable ester thereof are disclosed: ##STR1## wherein R.sup.1 is hydrogen, methoxy or formamido; R.sup.2 is a acyl group, in particular that of an antibacterially active cephalosporin; CO.sub.2 R.sup.6 is carboxy group or a carboxylate anion; R.sup.4 is a butenolide or butanolide ring, optionally substituted by one or two alkyl, dialkylamino, alkoxy, hydroxy or aryl groups, which may be the same or different, or, wherein two adjacent carbon atoms which are available for substitution define the common bond of an aromatic fused bicyclic system; X is S, SO, SO.sub.2, O or CH.sub.2 ; and the dashed line adjacent to R.sup.4 represents an optional double bond. Processes for the preparation of compounds together with intermediates for use therein are disclosed.
    Type: Grant
    Filed: September 14, 1989
    Date of Patent: November 12, 1991
    Assignee: Beecham Group p.l.c.
    Inventors: George Burton, Stephen C. M. Fell, John H. Bateson
  • Patent number: 5063231
    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 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, 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 7, 1990
    Date of Patent: November 5, 1991
    Assignee: Beecham Group p.l.c.
    Inventors: Gareth J. Sanger, Helen E. Marr
  • Patent number: 5063240
    Abstract: A compound of formula (I): ##STR1## or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof and/or a pharmaceutically acceptable solvate thereof, characterized in that:R.sup.1 represents hydrogen, alkyl, aralkyl or aryl and R.sup.2 represents hydrogen or R.sup.1 and R.sup.2 together represent a bond;R.sup.3 represents hydrogen and R.sup.4 represents hydrogen, akyl, aralkyl or aryl or R.sup.3 and R.sup.4 together represent a bond;X represents a bond, >C.dbd.O, >CHOH, O, S or NR wherein R is an alkyl group;n represents an integer 1, 2 or 3;m represents an integer 1, 2 or 3 andA.sup.1 and A.sup.2 each independently represent a benzene ring having a total up to 5 substituents comprising up to 3 optional substituents; a process for preparing such a compound, a pharmaceutical composition comprising such a compound and the use of such compounds and compositions in medicine.
    Type: Grant
    Filed: May 7, 1990
    Date of Patent: November 5, 1991
    Assignee: Beecham Group p.l.c.
    Inventor: Richard M. Hindley
  • Patent number: 5055458
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is hydroxy, amino, chloro or OR.sub.7 whereinR.sub.7 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 substituents selected from halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy;R.sub.2 amino or, when R.sub.1 is hydroxy or amino, R.sub.2 may also be hydrogen;X is --CH.sub.2 CH.sub.2 -- or a moiety of structure (a), (b) or (c): ##STR2## wherein n is 1 or 2;m is 0, 1 or 2; andR.sub.3 is hydrogen or acyl;R.sub.4 is a group of formula: ##STR3## wherein R.sub.5 and R.sub.6 are independently selected from hydrogen, C.sub.1-6 alkyl and optionally substituted phenyl; having antiviral activity, processes for their preparation and their use as pharmaceuticals.
    Type: Grant
    Filed: July 28, 1989
    Date of Patent: October 8, 1991
    Assignee: Beecham Group P.l.c.
    Inventors: Stuart Bailey, Michael R. Harnden
  • Patent number: 5055596
    Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 is hydrogen or optionally protected hydroxy; R.sup.2 is alkoxy, optionally protected hydroxy, oxo or optionally O-substituted oximino; R.sup.3 is hydrogen, optionally protected hydroxy, or a group 4'-(.alpha.-L-oleandrosyl)-.alpha.-L-oleandrosyloxy or .alpha.-L-oleandrosyloxy wherein the terminal hydroxy group is optionally protected; one or R.sup.4 and R.sup.5 is hydrogen and the other is methyl; and one of R.sup.6 and R.sup.7 is hydrogen and the other is methyl; with the proviso that (a) when R.sup.1 is optionally protected hydroxy, R.sup.3 is hydrogen, and (b) when R.sup.2 is not methoxy or optionally protected hydroxy, R.sup.1 and R.sup.3 are both hydrogen, are new and useful as anthelmintic agents.
    Type: Grant
    Filed: July 30, 1990
    Date of Patent: October 8, 1991
    Assignee: Beecham Group p.l.c.
    Inventors: Geoffrey H. Baker, Roderick J. Dorgan, David O. Morgan, Rhona M. Banks, Simon E. Blanchflower, Mark E. Poulton, Peter R. Shelley
  • Patent number: 5053427
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein a and b together form an --O-- or --CH.sub.2 -- linkage or a bond;either Y is N and R.sub.2 is hydrogen; orY is C-R.sub.1whereineither one of R.sub.1 and R.sub.2 is hydrogen and the other is nitro, cyano, halo, CF.sub.3, formyl, aldoxime, CF.sub.3 O, NO.sub.2 --CH.dbd.CH--, NC--CH.dbd.CH--; a group R.sub.x X-- wherein R.sub.x and C.sub.1-6 alkyl, aryl or heteroaryl either of which may be optionally substituted by one, two or three of C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro, halo, CF.sub.3 and cyano; and X is C.dbd.O, O.C.dbd.O, C.dbd.0.0, CHOH, SO, SO.sub.2, 0.SO, 0.SO.sub.2, CONH, 0.CONH, C.dbd.S, 0.C.dbd.S, C.dbd.S.0, CH.SH, SONH, SO.sub.2 NH, 0.SONH, 0.SO.sub.2 NH, CO--CH.dbd.CH, C.dbd.NHOH, C.dbd.NNH.sub.2 ; or a group R.sub.y R.sub.z NZ-- wherein R.sub.y and R.sub.z are independently hydrogen or C.sub.1-6 alkyl and Z is C.dbd.O, SO or SO.sub.2 ; orR.sub.1 is a C.sub.3-8 cycloalkyl group or a C.sub.
    Type: Grant
    Filed: September 14, 1989
    Date of Patent: October 1, 1991
    Assignee: Beecham Group p.l.c.
    Inventors: Geoffrey Stemp, Gordon Burrell, David G. Smith
  • Patent number: 5049556
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein L is NH or O;X and Y are independently selected from hydrogen or C.sub.1-4 alkyl, or together are a bond;R.sub.1 and R.sub.2 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl-C.sub.1-4 alkyl, or together are C.sub.2-4 polymethylene;R.sub.3 and R.sub.4 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl groups or optionally N-disubstituted by C.sub.
    Type: Grant
    Filed: August 2, 1989
    Date of Patent: September 17, 1991
    Assignee: Beecham Group p.l.c.
    Inventors: Francis D. King, Karen A. Joiner
  • Patent number: 5049588
    Abstract: A method for the treatment and/or prophylaxis of disorders associated with neuronal degeneration resulting from ischaemic events, in mammals, such as humans, which comprises administering to the mammal in need of such treatment an effective amount of a 5-HTl.sub.A agonist.
    Type: Grant
    Filed: May 8, 1989
    Date of Patent: September 17, 1991
    Assignee: Beecham Group p.l.c.
    Inventors: Charles D. Nicholson, Johannes Jukna
  • Patent number: 5045457
    Abstract: Compounds of formula (II): ##STR1## wherein R.sup.3 is optionally protected hydroxy; one of R.sup.4 and R.sup.5 is optionally protected hydroxy; and the other of R.sup.4 and R.sup.5 is hydrogen, which are obtainable by the fermentation of a Streptomyces microorganism, have anthelmintic activity.
    Type: Grant
    Filed: January 23, 1989
    Date of Patent: September 3, 1991
    Assignee: Beecham Group p.l.c. of Beecham House
    Inventors: Rhona M. Banks, Simon E. Blanchflower, Peter R. Shelley
  • Patent number: 5043342
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1##
    Type: Grant
    Filed: December 21, 1989
    Date of Patent: August 27, 1991
    Assignee: Beecham Group p.l.c.
    Inventors: Michael S. Hadley, Paul A. Wyman, Barry S. Orlek
  • Patent number: 5043343
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which Z is a heterocyclic 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 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 aromatic 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.3, NHCOOC.sub.2 H.sub.5, NHOR.sub.4, NHNH.sub.2, NO.sub.2, COR.sub.4, COR.sub.
    Type: Grant
    Filed: August 14, 1990
    Date of Patent: August 27, 1991
    Assignee: Beecham Group p.l.c.
    Inventor: Paul A. Wyman
  • Patent number: 5037850
    Abstract: A skin-care composition comprising a topically acceptable oil-in-water or water-in-oil emulsion base and from 1,000 to 15,000 I Ug.sup.-1 of a C.sub.1-10 alkyl ether or a C.sub.3-10 alkyl ester of retinol is disclosed. The composition preferably contains an anti-oxidant such as butylated hydroxytoluene or butylated hydroxyanisole. The composition is useful in promoting epidermal mitosis.
    Type: Grant
    Filed: October 6, 1989
    Date of Patent: August 6, 1991
    Assignee: Beecham Group p.l.c.
    Inventors: Thomas J. Elliott, Elspeth A. Murrell
  • Patent number: 5034398
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is CO and Y is NH or O, or X is NH and Y is CO;Z is CH.sub.2, O, S or NR.sub.3 wherein R.sub.3 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 alkenyl-methyl, phenyl or phenyl C.sub.1-4 alkyl either of which phenyl moieties may be substituted by one or two of halogen, CF.sub.3, C.sub.1-6 alkoxy or C.sub.1-6 alkyl; and R.sub.a is not present; orZ is CH or N and R.sub.a is as defined for R.sub.3 above;R.sub.b is present when X--Y--R.sub.2 is attached at the phenyl ring and is selected from hydrogen, halogen, CF.sub.3, hydroxy, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;R.sub.1 is hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.
    Type: Grant
    Filed: October 3, 1989
    Date of Patent: July 23, 1991
    Assignee: Beecham Group p.l.c.
    Inventor: Francis D. King
  • Patent number: 5032591
    Abstract: A pharmaceutical product comprising a potassium channel activator antihypertensive agent and a .beta.-blocker antihypertensive agent as a combined preparation for simultaneous, separate or sequential use in therapy of hypertension.
    Type: Grant
    Filed: January 4, 1989
    Date of Patent: July 16, 1991
    Assignee: Beecham Group p.l.c.
    Inventors: John M. Evans, Robin E. Buckingham
  • Patent number: 5032596
    Abstract: A method for the treatment and/or prophylaxis of disorders associated with pulmonary hypertension and/or disorders associated with right heart failure, in mammals, which method comprises administering to the mammal in need of such treatment and/or prophylaxis an effective and/or prophylactic, non-toxic, amount of a compound of formula (I): ##STR1## wherein A.sup.1 represents CR.sub.1, N or N.sup.+ --O.sup.- ; when A.sup.1 represents N or N.sup.+ --O.sup.-, R.sup.2 represents hydrogen;when A.sup.1 represents CR.sub.1 then:either;one of R.sub.1 and R.sub.2 is hydrogen and the other is a group R.sup.a wherein R.sup.a 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 alkylsulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.
    Type: Grant
    Filed: July 5, 1988
    Date of Patent: July 16, 1991
    Assignee: Beecham Group p.l.c.
    Inventor: Andrew J. Williams
  • Patent number: D321759
    Type: Grant
    Filed: December 2, 1988
    Date of Patent: November 19, 1991
    Assignee: Beecham Group p.l.c.
    Inventors: John F. Buswell, Victor C. Cracknell, Noshir J. Khambatta