Patents Assigned to Beecham Group
  • Patent number: 4524075
    Abstract: Topical formulations comprise pseudomonic acid or a salt or ester thereof and a polyethylene glycol or polyethylene glycol analogue or derivative.
    Type: Grant
    Filed: May 26, 1983
    Date of Patent: June 18, 1985
    Assignee: Beecham Group p.l.c.
    Inventor: Joshua Oduro-Yeboah
  • Patent number: 4524073
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R represents an alkyl or aralkyl group, substituted on an alkyl carbon atom other than that adjacent to --NH-- group, with one or more functional groups selected from halogen, non-aromatic heterocyclyl linked through carbon, aromatic heterocyclyl, nitro, oxo, --OR.sup.1, SR.sup.1 --P(O)R.sup.2 R.sup.3, --NR.sup.4 R.sup.5, .dbd.NR.sup.6, or a sulphur linked organic radical, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are various organic radicals.Processes for the preparation of these compounds and pharmaceutical compositions containing them are also disclosed.
    Type: Grant
    Filed: July 20, 1983
    Date of Patent: June 18, 1985
    Assignee: Beecham Group p.1.c.
    Inventors: Irene Stirling, Gordon Bruton, Stephen H. Calvert, Brian P. Clarke
  • Patent number: 4521337
    Abstract: A process for the preparation of a compound of the formulae (Ia) and/or (Ib): ##STR1## wherein R.sup.1 and R.sup.2 are independently substituted or unsubstituted hydrocarbon groups or are joined together so as to form a carbocyclic or heterocyclic ring, and R.sup.3 is a substituted or unsubstituted hydrocarbon group; which process comprises the ring-closing cyclization of a compound of the formula (II): ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined in relation to formulae (Ia) and (Ib).
    Type: Grant
    Filed: March 14, 1983
    Date of Patent: June 4, 1985
    Assignee: Beecham Group p.l.c.
    Inventors: Robert Southgate, Pamela Brown
  • Patent number: 4520014
    Abstract: Vasoconstrictor .alpha.-adrenergic agonists of formula (I)A-B-C (I)wherein, A is a 2-imidazoline group or a guanidine group; B is a chemical bond or a linking group one or two atoms in length; and C is a C.sub.6-10 mono- or bi-cyclic group which is either an aromatic group, a heteroaromatic group containing only one hetero-atom, or a group containing an aromatic moiety; and which group C may be substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or hydroxyl; or salts thereof, are useful in the treatment and prevention of diarrhoea in livestock. Compositions of these compounds are described.
    Type: Grant
    Filed: February 19, 1982
    Date of Patent: May 28, 1985
    Assignee: Beecham Group p.l.c.
    Inventors: Peter M. Newsome, Noel A. Mullan
  • Patent number: 4518606
    Abstract: A pharmaceutical composition for injection which comprises an aqueous sterile solution of a penicillin or salt thereof and from 1 to 10% of benzyl alcohol, a two-pack container or two-part syringe wherein one pack or part contains a penicillin or salt thereof in the form of a dry powder and the second pack or part contains an aqueous solution of benzyl alcohol, such that mixing the contents of the two packs or parts produces an aqueous solution of the penicillin and from 1 to 10% of benzyl alcohol, and a two-pack container or two-part syringe wherein one pack or part contains a penicillin in a solid free acid form, and the second part contains an aqueous solution of benzyl alcohol and substantially one equivalent of a basic pharmaceutically acceptable salt, such that mixing the contents of the two packs or parts produces an aqueous solution of a salt of the penicillin and from 1 to 10% of benzyl alcohol.
    Type: Grant
    Filed: July 9, 1982
    Date of Patent: May 21, 1985
    Assignee: Beecham Group Limited
    Inventor: Edmond Saias
  • Patent number: 4517124
    Abstract: The present invention provides a process for the preparation of a compound of the formula (IV): ##STR1## or salt or ester thereof wherein R.sup.1 and R.sup.2 are independently hydrogen; an organic radical bonded via a carbon atom to the ring carbon atom; a free, etherified or esterified hydroxy or mercapto group; an amino or acylamino group; or together R.sup.1 and R.sup.2 represent a group .dbd.CR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are the same or different and each represent hydrogen or a hydrocarbon or heterocyclic group optionally substituted with a functional group; and R.sup.3 represents an organic radical; which process comprises reacting a compound of the formula (V): ##STR2## wherein R.sup.x is hydrogen or a blocking group and R.sup.4 is an organic radical; with a thiol or reactive derivative thereof. The compounds of the formula (IV) are useful as antibiotics and .beta.-lactamase inhibitors, as are the compounds of the formula (V).
    Type: Grant
    Filed: November 14, 1983
    Date of Patent: May 14, 1985
    Assignee: Beecham Group Limited
    Inventor: Nigel J. P. Broom
  • Patent number: 4510152
    Abstract: Compounds of formula (I): ##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, C.sub.1-6 alkyl-thiolmethyl, 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 ethylenyl 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.sub.2, or one of R.sub.1 and R.sub.
    Type: Grant
    Filed: April 21, 1983
    Date of Patent: April 9, 1985
    Assignee: Beecham Group p.l.c.
    Inventor: Erol A. Faruk
  • Patent number: 4507283
    Abstract: A derivative of streptokinase-human plasminogen activator complex, in which the active catalytic site essential for fibrinolytic activity is blocked by a 2- or 4-aminobenzoyl group, is useful in treating venous thrombosis.The blocking group is removable by hydrolysis such that the first order rate is in the range 0.7.times.10.sup.-5 sec.sup.-1 to 2.5.times.10.sup.-5 sec.sup.-1 in isotonic aqueous media at pH 7.4 at 37.degree. C.
    Type: Grant
    Filed: April 5, 1983
    Date of Patent: March 26, 1985
    Assignee: Beecham Group p.l.c.
    Inventor: Richard A. G. Smith
  • Patent number: 4505926
    Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each is selected from halogen, alkyl, haloalkyl, alkoxy and alkoxyalkyl,R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is alkyl;n is 0,1,2 or 3; andZ is a pharmaceutically or veterinarily acceptable anion, protect animals from death due to enteropathogenic E. coli infection of the gastro-intestinal tract.
    Type: Grant
    Filed: September 15, 1983
    Date of Patent: March 19, 1985
    Assignee: Beecham Group p.l.c.
    Inventors: Peter M. Newsome, Stephen F. Moss, Lee J. Beeley, Malcolm N. Burgess
  • Patent number: 4505894
    Abstract: Compounds of the formula ##STR1## wherein X is S, SO or SO.sub.2 and R is an inert hydrocarbon of up to 20 carbon atoms which will not lead to rapid degradation of the above compound unsubstituted or substituted and A is a group such and CO.sub.2 A represents a carboxylic acid group or a salt or ester thereof, are useful for their antibacterial activity and for their .beta.-lactamase inhibitory activity.
    Type: Grant
    Filed: August 30, 1982
    Date of Patent: March 19, 1985
    Assignee: Beecham Group Limited
    Inventor: Roger J. Ponsford
  • Patent number: 4504480
    Abstract: Compounds of formula (I), ##STR1## or an N-oxide or pharmaceutically acceptable salt thereof, wherein R.sub.1 is hydrogen, C.sub.1-7 alkyl, C.sub.3-7 cycloalkyl, C.sub.4-7 cycloalkenyl or C.sub.1-4 alkyl substituted by C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, C.sub.3-7 cycloalkyl, hydroxy, thiol, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, carboxy, C.sub.1-4 alkoxycarbonyl, C.sub.1-4 alkanoyl, amino optionally substituted by one or two C.sub.1-4 alkyl or by C.sub.4-6 polymethylene optionally containing an oxygen or nitrogen atom, aminocarbonyl optionally N-substituted by one or two C.sub.1-4 alkyl, or benzoyl or phenyl either being optionally ring-substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or trifluoromethyl, R.sub.2 and R.sub.3 are the same or different and are hydrogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alklthio, halogen or trifluoromethyl, m is 1 to 3 and n is 1 or 2, the hydrogen atom bonded to the C.sub.a carbon atom being trans to the hydrogen atom bonded to the C.sub.
    Type: Grant
    Filed: March 4, 1983
    Date of Patent: March 12, 1985
    Assignee: Beecham Group p.l.c.
    Inventors: Laramie M. Gaster, Barry S. Orlek
  • Patent number: 4501696
    Abstract: A process for the preparation of a penam derivative of formula (I): ##STR1## wherein R.sup.A is hydrogen or a group of formula (Ia): ##STR2## wherein X is --CO.sub.2 R.sup.1, or SO.sub.3 R.sup.1 ; R is C.sub.1-6 alkyl, aryl, or heterocyclyl; R.sup.1 is hydrogen, or a pharmaceutically acceptable salt-forming ion or ester-forming radical, and R.sup.2 represents hydrogen or a pharmaceutically acceptable salt-forming ion or in vivo hydrolyzable ester-forming radical; which process comprises reacting a compound of formula (II): ##STR3## wherein R.sup.B is hydrogen, a removable amino blocking group, or a group of formula (IIa): ##STR4## wherein Y is --CO.sub.2 R.sup.x or --SO.sub.3 R.sup.x ; R is as defined with respect to formula (I) above; R.sup.x represents an ester-forming radical, R.sup.Y represents hydrogen, a salt-forming radical or a carboxyl-blocking group, and R.sup.
    Type: Grant
    Filed: July 9, 1982
    Date of Patent: February 26, 1985
    Assignee: Beecham Group p.l.c.
    Inventors: John R. M. Dales, Marguerita A. Vallance
  • Patent number: 4499099
    Abstract: Pharmaceutical compositions comprising compounds of formula (I) or pharmaceutically acceptable salts and/or N-oxides and/or solvates thereof: ##STR1## wherein: R.sub.1 is a C.sub.1-6 alkoxy or C.sub.1-6 alkylthio group; andone of R.sub.2, R.sub.3 and R.sub.4 is hydrogen, the second is C.sub.1-6 alkylthio and the third is selected from the class of substituents consisting of 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 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl or aminosulphonyl optionally N-substituted by one or two C.sub.1-6 alkyl groups; orR.sub.1 is joined to R.sub.2 to form C.sub.1-2 alkylenedioxy; andone of R.sub.3 and R.sub.4 is C.sub.1-6 alkylthio and the other is selected from the class of substituents defined above;R.sub.5 is hydrogen or C.sub.1-6 alkyl;R.sub.6 is C.sub.1-7 alkyl or a group --(CH.sub.2).sub.s R.sub.7 where s is 0 to 2 and R.sub.7 is a C.sub.
    Type: Grant
    Filed: June 9, 1982
    Date of Patent: February 12, 1985
    Assignee: Beecham Group p.l.c.
    Inventor: Eric A. Watts
  • Patent number: 4496565
    Abstract: Compounds of formula (I): ##STR1## a pharmaceutically acceptable salt or solvate thereof having anti-hypertensive activity, a process for their preparation and their use as pharmaceuticals.
    Type: Grant
    Filed: October 17, 1983
    Date of Patent: January 29, 1985
    Assignee: Beecham Group p.l.c.
    Inventors: John M. Evans, Valerie A. Ashwood
  • Patent number: 4490295
    Abstract: The invention provides the compound (2R,5R,Z)-3-(2-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo-[3,2,0]heptane- 2-carboxylic acid and its salts in purified form and pharmaceutical compositions containing them and a process for the purification of such compounds by conversion in aqueous media to the lithium salt of the above acid and precipitation thereof.
    Type: Grant
    Filed: May 7, 1980
    Date of Patent: December 25, 1984
    Assignee: Beecham Group p.1.c.
    Inventors: Ian D. Fleming, David Noble, Hazel M. Noble (formerly Gillett), Wilfred F. Wall
  • Patent number: 4490294
    Abstract: The invention provides the compound (2R,5R,Z)-3-(2-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo-[3,2,0]-heptane -2-carboxylic acid and its salts in purified form and pharmaceutical compositions containing them and a process for the purification of such compounds by conversion in aqueous media to the lithium salt of the above acid and precipitation thereof.
    Type: Grant
    Filed: March 20, 1978
    Date of Patent: December 25, 1984
    Assignee: Beecham Group p.l.c.
    Inventors: Ian D. Fleming, David Noble, Hazel M. Noble, Wilfred F. Wall
  • Patent number: 4490383
    Abstract: A pharmaceutical composition adapted for administration to a human by injection which composition comprises an aqueous solution containing sodium amoxycillin and tri-sodium phosphate, the weight ratio of sodium amoxycillin present to the tri-sodium phosphate present being from 8:1 to 50:1.
    Type: Grant
    Filed: December 9, 1982
    Date of Patent: December 25, 1984
    Assignee: Beecham Group Limited
    Inventor: Stuart A. Hill
  • Patent number: 4485110
    Abstract: A class of 6-alkylidene penem compounds of formula (II) have antibacterial and .beta.-lactamase inhibitory properties: ##STR1## where R.sup.1 and R.sup.2 represent hydrogen or optionally substituted hydrocarbon or heterocyclic, and R.sup.3 represents hydrogen or an organic group.
    Type: Grant
    Filed: April 23, 1981
    Date of Patent: November 27, 1984
    Assignee: Beecham Group Limited
    Inventor: Neal F. Osborne
  • Patent number: 4481209
    Abstract: Ampicillin phthalidyl ester naphthalene-2-sulphonate, its preparation, and its use in pharmaceutical compositions to treat infections.
    Type: Grant
    Filed: November 7, 1980
    Date of Patent: November 6, 1984
    Assignee: Beecham Group Limited
    Inventors: Kenneth Utting, Karrar A. Khan, Sidney E. Callander
  • Patent number: 4481213
    Abstract: A compound of the formula (I): ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1 is hydrogen or C.sub.1-6 alkyl or an acyl group of 1 to 8 carbon atoms; n is 2, 3 or 4; X is halogen; and the OR.sub.1 and HN(CH.sub.2).sub.n X moieties are trans; has anti-hypertensive activity and a low level of cardiac side-effects.
    Type: Grant
    Filed: July 15, 1982
    Date of Patent: November 6, 1984
    Assignee: Beecham Group Limited
    Inventor: John M. Evans