Patents Assigned to Beecham Group
  • Patent number: 4812459
    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: June 6, 1986
    Date of Patent: March 14, 1989
    Assignee: Beecham Group p.l.c.
    Inventors: John M. Evans, Geoffrey Stemp, Frederick Cassidy
  • Patent number: 4808588
    Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein: Het is monocyclic heteroaryl having two adjacent carbon atoms, a and b, depicted in formula (I); p1 R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl and C.sub.1-6 Alkoxy;R.sub.3 is hydroxy, C.sub.1-6 alkoxy, C.sub.3-7 alkenyl-methoxy, phenoxy or phenyl C.sub.1-4 alkoxy in which either phenyl moiety may be substituted by one or two C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halo; CO.sub.2 R.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl, CONR.sub.7 R.sub.8 or SO.sub.2 NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are independently hydrogen or C.sub.1-6 alkyl or together are C.sub.4-6 polymethylene, NO.sub.2, (CH.sub.2).sub.m OR.sub.9 wherein m is 1 or 2 and R.sub.9 is C.sub.1-6 alkyl or S(O).sub.n R.sub.10 wherein n is 0, 1 or 2 and R.sub.10 is C.sub.
    Type: Grant
    Filed: July 30, 1987
    Date of Patent: February 28, 1989
    Assignee: Beecham Group, p.l.c.
    Inventor: Francis D. King
  • Patent number: 4808405
    Abstract: A binary complex between streptokinase and plasminogen is prepared in which the catalytic site essential for fibrinolytic activity is blocked by a group which is removable by hydrolysis such that the pseudo-first order rate constant for hydrolysis of the complex is in the range 10.sup.-6 sec.sup.-1 to 10.sup.-3 sec.sup.-1 in isotonic aqueous media at pH 7.4 at 37.degree. C. The complex is preferably a p-anisoyl streptokinase/plasminogen complex without internal peptide bond cleavage. The complex is useful in the treatment of venous thrombosis.
    Type: Grant
    Filed: August 29, 1986
    Date of Patent: February 28, 1989
    Assignee: Beecham Group p.l.c.
    Inventors: Richard A. G. Smith, John G. Winchester
  • Patent number: 4808619
    Abstract: Compounds of the formula ##STR1## as defined in the specification, and processes for their preparation and methods of using the compounds for the treatment of hypertension in mammals, such as humans and for the treatment and/or prophylaxis of cerebrovascular disorders and/or disorders associated with cerebral senility in mammals, such as humans.
    Type: Grant
    Filed: July 30, 1986
    Date of Patent: February 28, 1989
    Assignee: Beecham Group p.l.c.
    Inventors: John M. Evans, Geoffrey Stemp, Charles D. Nicholson, Dieter Angersbach
  • Patent number: 4803293
    Abstract: Compounds of formula (I): ##STR1## or a pharmaceutically acceptable salt thereof,in whichR.sup.1 is hydrogen, halogen, or trifluoromethyl,R.sup.2 is hydrogen or halogen,R.sup.3 is hydroxyl, C.sub.1-6 alkoxy or ##STR2## where R.sup.8 and R.sup.9 are each hydrogen or C.sub.1-6 alkyl; R.sup.4 is hydrogen or C.sub.1-6 alkyl; R.sup.5 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyl optionally substituted by hydroxy; cyano, C.sub.1-6 alkenyl or C.sub.1-6 alkynyl optionally substituted by carboxy or esters and amides thereof, phenyl, C.sub.1-6 alkyl phenyl or a group ##STR3## wherein R.sup.12 and R.sup.13 are each hydrogen or C.sub.1-6 alkyl or together, along with the nitrogen to which they are attached, form a 5- or 6-membered ring and m is 1 or 2;R.sup.6 is hydrogen or methyl:R.sup.7 is --O(CH.sub.2).sub.a CO.sub.2 H, --O(CH.sub.2).sub.b M, --CO.sub.2 H; or amide thereof in whicha is an integer from 1 to 6,b is an integer from 2 to 7, andM is hydroxy, C.sub.1-6 alkoxy or ##STR4## in which R.sup.10 and R.sup.
    Type: Grant
    Filed: February 18, 1987
    Date of Patent: February 7, 1989
    Assignee: Beecham Group plc
    Inventors: John Berge, Richard M. Hindley
  • Patent number: 4800225
    Abstract: A pure, crystalline hydrate of (.+-.)endo-4-amino-5-chloro-2-methoxy-N-(1'-azabicyclo[3.3.1]non-4'-yl)-be nzamide hydrochloride, having useful pharmacological activity namely gastric motility enhancing activity, anti-emetic activity and 5-HT M-receptor antagonist activity.
    Type: Grant
    Filed: March 20, 1987
    Date of Patent: January 24, 1989
    Assignee: Beecham Group, p.l.c.
    Inventor: Paul Smith
  • Patent number: 4800212
    Abstract: Compounds of formula (I) or when a compound of formula (I) contain a salifiable group, a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 -R.sub.7 and X are as defined, are useful as anti-hypertensive agents.
    Type: Grant
    Filed: June 10, 1985
    Date of Patent: January 24, 1989
    Assignee: Beecham Group p.l.c.
    Inventors: John M. Evans, Geoffrey Stemp
  • Patent number: 4798828
    Abstract: Compounds of the general formula I: ##STR1## and their pharmaceutically acceptable salts and in vivo hydrolyzable esters, in whichone of R.sup.1 and R.sup.2 denotes hydrogen,the other of R.sup.1 and R.sup.2 denotes an unsubstituted or substituted five-membered hetero-aromatic ring bonded through a carbon atom thereof and having one hetero-atom selected from nitrogen, oxygen and sulphur and additionally having from one to three nitrogen atoms, andR.sup.3 denotes hydrogen or an organic group,are novel compounds with .beta.-lactamase inhibitory and antibacterial properties.
    Type: Grant
    Filed: January 24, 1985
    Date of Patent: January 17, 1989
    Assignee: Beecham Group p.l.c.
    Inventor: Neal F. Osborne
  • Patent number: 4798829
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: n is 1, 2, or 3; and m and p are independently 1 or 2 such that m+n+p.gtoreq.4;X is NH; or O when Ar is of formula (a) and R.sub.4 is hydrogen or when Ar is a heteroaromatic group which may be substituted;R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-6 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;Ar is a group: ##STR2## wherein either R.sub.4 is C.sub.1-6 alkoxy and one of R.sub.5, R.sub.6, and R.sub.7 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O)n wherein n is 0, 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally 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 or phenyl C.sub.
    Type: Grant
    Filed: August 14, 1986
    Date of Patent: January 17, 1989
    Assignee: Beecham Group plc.
    Inventors: Francis D. King, Karen A. Joiner
  • Patent number: 4797387
    Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein L is NH or O;X is a moiety capable of hydrogen bonding to the NH group depicted in formula (I);R.sub.1 and R.sub.2 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, carboxy, C.sub.1-6 alkoxycarbonyl, 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.4-5 polymethylene; andZ 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; and R.sub.3 or R.sub.4 is C.sub.1-7 alkyl, C.sub.
    Type: Grant
    Filed: January 14, 1987
    Date of Patent: January 10, 1989
    Assignee: Beecham Group, p.l.c.
    Inventor: Francis D. King
  • Patent number: 4795809
    Abstract: A compound having the formula (I): ##STR1## is described, together with salts thereof and an enzymatic process for converting such compounds into clavulanic acid.A process for the preparation of the compound of formula (I) and its salts is disclosed, together with intermediates for use therein. This process involves the use of a novel enzyme system to effect the desired cyclization, which enzyme system is preferably derived from a micro-organism, in particular a species of Streptomyces.
    Type: Grant
    Filed: August 27, 1986
    Date of Patent: January 3, 1989
    Assignee: Beecham Group plc
    Inventors: Stefan R. Woroniecki, Stephen W. Elson, Keith H. Baggaley
  • Patent number: 4790989
    Abstract: Certain formulations of pseudomonic acids and their salts have good antifungal activity.
    Type: Grant
    Filed: April 10, 1987
    Date of Patent: December 13, 1988
    Assignee: Beecham Group p.l.c.
    Inventors: Pamela A. Hunter, Valerie Berry, Joshua Oduro-Yeboah, Norman A. Orr
  • Patent number: 4789679
    Abstract: A method for the treatment and/or prophylaxis of incontinence in mammals, which method comprises administering to the mammal an effective amount of the compound pinacidil or a pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: July 17, 1987
    Date of Patent: December 6, 1988
    Assignee: Beecham Group p.l.c.
    Inventors: Thomas C. Hamilton, Robin E. Buckingham
  • Patent number: 4786742
    Abstract: This invention relates to a novel salt of an antibacterial compound and to a process for its preparation.
    Type: Grant
    Filed: August 8, 1986
    Date of Patent: November 22, 1988
    Assignee: Beecham Group p.l.c.
    Inventor: Alan D. Curzons
  • Patent number: 4786639
    Abstract: A method for the treatment and/or prophylaxis of reversible airways obstruction and asthma 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: November 4, 1986
    Date of Patent: November 22, 1988
    Assignee: Beecham Group p.l.c.
    Inventor: John M. Evans
  • Patent number: 4786643
    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: November 19, 1987
    Date of Patent: November 22, 1988
    Assignee: Beecham Group p.l.c.
    Inventors: Gareth J. Sanger, Wesley D. Miner
  • Patent number: 4783478
    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: July 9, 1987
    Date of Patent: November 8, 1988
    Assignee: Beecham Group p.l.c.
    Inventors: Gordon Wootton, Gareth J. Sanger
  • Patent number: 4783460
    Abstract: Compounds of formula (I): ##STR1## or a salt thereof, in which W is phenyl optionally substituted by halogen or trifluoromethyl, or a benzofuran-2-yl group,R.sup.1 is hydrogen or methyl,R.sup.2 is carboxyl or a group O--Z--CO.sub.2 H or an ester or amide thereof; a group O--E--NR.sup.3 R.sup.4 or a group O--E--OR.sup.5, wherein R.sup.3, R.sup.4 and R.sup.5 each represents hydrogen or C.sub.1-6 alkyl, Z is a C.sub.1-6 straight or branched alkylene chain, n is 1 or 2, a is 2 or 3, and E is a C.sub.2-7 straight or branched alkylene chain with at least two carbon atoms separating the two heteroatoms in the group R.sup.2 ; a process for the production of such compounds and their use in treating hyperglycaemia and/or obesity.
    Type: Grant
    Filed: March 17, 1987
    Date of Patent: November 8, 1988
    Assignee: Beecham Group p.l.c.
    Inventor: Barrie C. C. Cantello
  • Patent number: 4782083
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: one of R.sub.1 and R.sub.2 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl or R.sub.1 and R.sub.2 together are C.sub.2-5 -polymethylene;either R.sub.3 is hydrogen, hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy and R.sub.4 is hydrogen or R.sub.3 and R.sub.4 together are a bond;R.sub.5 is hydrogen C.sub.1-6 alkyl optionally substituted by halogen hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, carboxy or amino optionally substituted by one or two independent C.sub.1-6 alkyl groups, or C.sub.2-6 alkenyl, amino optionally substituted by a C.sub.1-6 alkyl or C.sub.1-6 alkenyl group or by a C.sub.1-6 alkanoyl group optionally substituted by up to three halo atoms, by a phenyl group optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen, or aryl or hetroaryl, either being optionally substituted by one or more groups or atoms selected from the class of C.sub.1-6 alkyl, C.sub.
    Type: Grant
    Filed: August 29, 1986
    Date of Patent: November 1, 1988
    Assignee: Beecham Group P.L.C.
    Inventors: Frederick Cassidy, Geoffrey Stemp, John M. Evans
  • Patent number: 4774238
    Abstract: (5R) (Z)-6-(1-methyl,1,2,3-triazol-4-yl-methylene)-penem-3-carboxylic acid and its salts are provided in analytically pure crystalline form, and the salts in hydrated form, for example (5R) sodium (Z)-6-(1-methyl-1,2,3-triazol-4-yl-methylene)penem-3-carboxylate monohydrate.
    Type: Grant
    Filed: July 21, 1986
    Date of Patent: September 27, 1988
    Assignee: Beecham Group plc
    Inventors: Nigel J. P. Broom, Anthony C. Marshall