Patents Assigned to Beecham Group p.l.c.
  • Patent number: 4918067
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt or in-vivo hydrolysable ester thereof: ##STR1## wherein R.sup.1 is a 5 or 6 membered sulphur and/or nitrogen containing heterocyclic group substituted by an optionally protected amino group, with the proviso that R.sup.1 is not 2-aminothiazol-4-yl, and R is hydrogen; optionally substituted C.sub.1-12 alkyl; optionally substituted C.sub.2-12 alkenyl or alkynyl; carbocyclyl; aryl or heterocyclyl.These compounds have antibacterial properties, and therefore are of use in the treatment of bacterial infections in humans and animals caused by a wide range of organizations.
    Type: Grant
    Filed: July 22, 1987
    Date of Patent: April 17, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Brian C. Gasson, Michael J. Pearson
  • Patent number: 4918079
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein the various substituents are defined hereinbelow, having 5-HT.sub.3 receptor antagonist activity, processes for their preparation and their use as pharmaceuticals.
    Type: Grant
    Filed: September 30, 1988
    Date of Patent: April 17, 1990
    Assignee: Beecham Group p.l.c.
    Inventor: Francis D. King
  • Patent number: 4916155
    Abstract: Crystalline calcium pseudomonate or a hydrate thereof, in particular the dihydrate.Processes for the preparation of these salts and their use in human and veterinary medicine and as a growth promoter in animals are described.
    Type: Grant
    Filed: April 13, 1989
    Date of Patent: April 10, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Geoffrey H. Baker, Merle Beal
  • Patent number: 4914202
    Abstract: A method for inceasing the weight gain and/or improving the feed utilization efficiency and/or increasing the lean body mass and/or decreasing birth mortality rate and increasing post-natal survival rate of livestock comprises the administration to livestock of an effective, non-toxic amount of a compound of formula (I), or a veterinarily acceptable acid addition salt thereof: ##STR1## wherein R.sup.1 is phenyl (C.sub.1-6)alkyl or optionally substituted C.sub.1-6 alkyl, andW is optionally substituted phenyl, a heterocyclyl group, or phenoxymethyl optionally substituted on the phenyl group. Certain compounds of formula (I) are novel.
    Type: Grant
    Filed: March 10, 1988
    Date of Patent: April 3, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Jonathan R. S. Arch, Norman H. Rogers
  • Patent number: 4910307
    Abstract: A process for the preparation of 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.5whereinR.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/or R.sub.3 may be in the form of O-acyl, phosphate, cyclic acetal or cyclic carbonate derivatives thereof;which process comprises the reaction of a compound of formula (II): ##STR2## wherein R.sub.4 ' is R.sub.4 or a group or atom convertible thereto and R.sub.x is amino or protected amino; with a compound of formula (III):R.sub.3 'CHR.sub.2 'CHR.sub.1 'Q (III)wherein Q is a leaving group and R.sub.1 ', R.sub.
    Type: Grant
    Filed: October 20, 1988
    Date of Patent: March 20, 1990
    Assignee: Beecham Group p.l.c.
    Inventor: Paul G. Wyatt
  • Patent number: 4908204
    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: February 22, 1988
    Date of Patent: March 13, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Jeffery H. Robinson, Ian Dodd
  • Patent number: 4904784
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein all the symbols are defined in the specification; having pharmacological activity, including blood pressure lowering activity, a process and intermediates for their preparation and their use as pharmaceuticals.
    Type: Grant
    Filed: February 23, 1989
    Date of Patent: February 27, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: John M. Evans, Geoffrey Stemp, Frederick Cassidy
  • Patent number: 4898580
    Abstract: A syringe for dispensing a liquid pharmaceutical composition has a first chamber (5), adjacent to nozzle (3), which contains a mositure sensitive solid drug, two movable septa (8,9) which together create a second chamber (6) and a third chamber (7) holding a liquid diluent, and a liquid by-pass passage (19) which can connect the third chamber (7) to the first chamber (5) while by-passing second chamber (6).A plunger (4) is depressed to move the septum (9) towards the nozzle (3), thereby causing liquid diluent to flow via by-pass passage (19) into the first chamber (5) to mix with the drug.The second chamber (6) contains moisture sequestering material to insulate the drug from any moisture which might leak through septum (9).
    Type: Grant
    Filed: October 4, 1988
    Date of Patent: February 6, 1990
    Assignee: Beecham Group p.l.c.
    Inventor: Patrick J. Crowley
  • Patent number: 4898728
    Abstract: A process for the production of a sterile composition containing lecithin and polyvinyl pyrrolidone is disclosed in which the lecithin and polyvinyl pyrrolidone, optionally with one or more preservative powders are admixed in a solvent comprising about 75% to 90% methyl isobutyl ketone and about 10% to 25% isopropyl alcohol, and the solution passed through a millipore filter in order to render the ingredients sterile. The process is usefully employed in the production of injectable compositions of amoxycillin and ampicillin.
    Type: Grant
    Filed: April 7, 1988
    Date of Patent: February 6, 1990
    Assignee: Beecham Group p.l.c.
    Inventor: Robert R. Vartan
  • Patent number: 4897476
    Abstract: During the preparation of 6-(substituted methylene)-2-penem compounds (which are known for their anti-bacterial and .beta.-lactamase inhibitory properties) mixtures of the E-isomer and the Z-isomer may be formed. The Z-isomer is, however generally preferred, and the present invention provides a process whereby the E-isomer may be converted into the Z-isomer by reaction with an aromatic heterocyclic thiol in the presence of a base.
    Type: Grant
    Filed: May 12, 1988
    Date of Patent: January 30, 1990
    Assignee: Beecham Group p.l.c.
    Inventor: Nigel J. P. Broom
  • Patent number: 4891380
    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, such as humans, which method comprises administering to the mammal in need of such treatment and/or prophylaxis an effective and/or prophylactic amount of pinacidil; or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof.
    Type: Grant
    Filed: July 5, 1988
    Date of Patent: January 2, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Andrew J. Williams, Derek R. Buckle
  • Patent number: 4886808
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is CO and Y is NH;Z is 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 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.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.
    Type: Grant
    Filed: March 16, 1988
    Date of Patent: December 12, 1989
    Assignee: Beecham Group p.l.c.
    Inventor: Francis D. King
  • Patent number: 4882327
    Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof:Y-CO-L-Z (I)whereinL is NH or O; Y is a group of formula (a), (b) or (c): ##STR1## wherein R.sub.1 and R.sub.2, R.sub.5 and R.sub.6, R.sub.9 and R.sub.10, are independently selected from hydrogen or halogen;X is N or CR.sub.3whereinR.sub.3 is hydrogen or C.sub.1-6 alkoxy;R.sub.4 is hydrogen, halogen, CH.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, C.sub.1-7 acyl, cyano, C.sub.1-6 alkoxycarbonyl, C.sub.1-7 acylamino, hydroxy, nitro or amino, aminocarbonyl, or aminosulphonyl, optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, and C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or disubstituted by C.sub.4 or C.sub.5 polymethylene; phenyl or phenyl C.sub.1-4 alkyl group optionally substituted in the phenyl ring by one or two of halogen, C.sub.1-6 alkoxy or C.sub.1-6 alkyl groups;one of R.sub.7 and R.sub.8 is C.sub.
    Type: Grant
    Filed: April 22, 1988
    Date of Patent: November 21, 1989
    Assignee: Beecham Group p.l.c.
    Inventor: Francis D. King
  • Patent number: 4880776
    Abstract: A hybrid protein which comprises plasmin A-chain linked to urokinase B-chain, the catalytic site of which is blocked by a removable blocking group.
    Type: Grant
    Filed: March 25, 1988
    Date of Patent: November 14, 1989
    Assignee: Beecham Group p.l.c.
    Inventors: Jeffery H. Robinson, Ian Dodd
  • Patent number: 4880834
    Abstract: A method for treating livestock to decrease birth mortality rate and to increase post-natal survival rate by administering ethanolamine derivatives is disclosed.
    Type: Grant
    Filed: October 30, 1986
    Date of Patent: November 14, 1989
    Assignee: Beecham Group p.l.c.
    Inventor: Jonathan R. Arch
  • Patent number: 4879287
    Abstract: Pharmacuetical compositions for topical application to the skin are disclosed comprising the hydrated crystalline calcium salt of mupirocin and a corticosteriod intimately mixed therewith. The compositions are useful for the treatment of skin disorders in humans and domestic animals.
    Type: Grant
    Filed: December 21, 1988
    Date of Patent: November 7, 1989
    Assignee: Beecham Group p.l.c.
    Inventors: Norman A. Orr, Michael J. Greenway
  • Patent number: 4877783
    Abstract: .beta.-Lactam antibiotics having an .alpha.-formamido substituent on the carbon atom adjacent to the carbonyl group of the .beta.-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes for the preparation of the compounds are further disclosed.
    Type: Grant
    Filed: January 24, 1985
    Date of Patent: October 31, 1989
    Assignee: Beecham Group p.l.c.
    Inventor: Peter H. Milner
  • Patent number: 4876086
    Abstract: Injectable pharmaceutical compositions are provided which comprise fine particles of amoxycillin trihydrate coated with a dispersing agent, the ratio of amoxycillin trihydrate to dispersing agent being from 1000:1 to 20:1. A preferred dispersing agent is a mixture of polyvinylpyrrolidone and lecithin. Such compositions give surprising prolonged blood levels of amoxycillin after administration. The compositions can be used in the treatment of both humans and domestic animals.
    Type: Grant
    Filed: September 17, 1987
    Date of Patent: October 24, 1989
    Assignee: Beecham Group p.l.c.
    Inventor: John S. Dowrick
  • Patent number: 4873240
    Abstract: A method for increasing the weight gain and/or improving the feed utilization efficiency of livestock is described which comprises the oral or non-oral administration to livestock of an effective, non-toxic amount of a compound of formula (XX): ##STR1## or a salt thereof, in which W is phenyl optionally substituted by halogen or trifluoromethyl, or a benzofuran-2-yl group, R.sup.1x is hydrogen or methyl, R.sup.2x is carboxyl or a group O--Z.sup.4 --CO.sub.2 H or an ester or amide thereof; a group O--E.sup.1 --NR.sup.3x R.sup.4x or a group O--E.sup.1 --OR.sup.5x, wherein R.sup.3x, R.sup.4x and R.sup.5x each represents hydrogen or C.sub.1-6 alkyl, Z.sup.4 is a C.sub.1-6 straight or branched alkylene chain, x is 1 or 2, y is 2 or 3, and E.sup.1 is C.sub.2-7 straight or branched alkylene chain with at least two carbon atoms separating the two heteroatoms in the group R.sup.2x.
    Type: Grant
    Filed: July 8, 1988
    Date of Patent: October 10, 1989
    Assignee: Beecham Group p.l.c.
    Inventor: Jonathan R. Arch
  • Patent number: 4871744
    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: June 3, 1988
    Date of Patent: October 3, 1989
    Assignee: Beecham Group p.l.c.
    Inventors: Francis D. King, Karen A. Joiner