Patents Assigned to Beecham Group p.l.c.
  • Patent number: 5250688
    Abstract: A compound of formula (I) ##STR1## or a salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, acyl or phosphate, provided that when one of R.sub.1 or R.sub.2 is phosphate, the other is hydrogen; or R.sub.1 and R.sub.2 are joined together to form a cyclic acetal group, a cyclic carbonate group or a cyclic phosphate group.Processes for preparing these compounds and their use in therapy is also described.
    Type: Grant
    Filed: January 22, 1992
    Date of Patent: October 5, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Michael R. Harnden, Richard L. Jarvest
  • Patent number: 5246926
    Abstract: .beta.-Lactam compounds of the formula (Ia) including pharmaceutically acceptable salts and in vivo hydrolysable esters, processes for their preparation and their use as antibiotics: ##STR1## wherein R.sup.1 is hydrogen, methoxy or formamido;R.sup.2 is an acyl group, in particular that of an antibacterially active cephalosporin;CO.sub.2 R.sup.6 is a carboxy group or a carboxylate anion;R.sup.3 is a Y-lactone ring optionally containing an endocyclic double bond, which ring is optionally substituted at any carbon atom by alkyl, dialkylamino, alkoxy, hydroxy, halogen or aryl, which in the case of more than one substituent may be the same or different, or is optionally di-substituted at two adjacent carbon atoms, which are available for substitution, to form an aromatic fused bicyclic system; and X is S, SO, SO.sub.2, O or CH.sub.2.
    Type: Grant
    Filed: March 28, 1990
    Date of Patent: September 21, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: John H. Bateson, George Burton, Stephen C. M. Fell
  • Patent number: 5247085
    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 is amino or, when R.sub.1 is hydroxy or amino, R.sub.2 may also be hydrogen;R.sub.3 is hydrogen, hydroxymethyl or acyloxymethyl;R.sub.4 is a group of formula: ##STR2## R.sub.5 and R.sub.6 are independently selected from hydrogen, C.sub.1-6 alkyl and optionally substituted phenyl; orR.sub.3 and R.sub.4 together are: ##STR3## wherein R.sub.6 is as defined above;having antiviral activity, to processes for their preparation and their use as pharmaceuticals.
    Type: Grant
    Filed: May 29, 1992
    Date of Patent: September 21, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Michael R. Harnden, David M. Duckworth
  • Patent number: 5246937
    Abstract: The present invention provides antiviral compounds of Formula (I): ##STR1## pharmaceutical compositions prepared therefrom, and methods of treatment of viral infections therewith.
    Type: Grant
    Filed: January 22, 1992
    Date of Patent: September 21, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Michael R. Harnden, Richard L. Jarvest
  • Patent number: 5239090
    Abstract: The (3S,4R)-isomer of a compound of formula (E) is disclosed.
    Type: Grant
    Filed: February 24, 1992
    Date of Patent: August 24, 1993
    Assignee: Beecham Group p.l.c.
    Inventor: Erol A. Faruk
  • Patent number: 5234686
    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: May 30, 1991
    Date of Patent: August 10, 1993
    Assignee: Beecham Group p.l.c.
    Inventor: Ian Dodd
  • Patent number: 5232925
    Abstract: Compounds of formula (I): ##STR1## or a tautomeric form thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceuticallyacceptable solvate thereof, wherein:A.sup.1 represents a substituted or unsubstituted aromatic heterocyclyl group;R.sup.1 represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group;R.sup.2 and R.sup.3 each represent hydrogen, or R.sup.2 and R.sup.3 together represent a bond;A.sup.2 represents a benzene ring having in total up to five substituents; andn represents an integer in the range of from 2 to 6; pharmaceutical compositions containing such compounds and the use of such compounds and compositions in medicine.
    Type: Grant
    Filed: January 15, 1991
    Date of Patent: August 3, 1993
    Assignee: Beecham Group p.l.c.
    Inventor: Richard M. Hindley
  • Patent number: 5232938
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein a, b, J, Y and R.sub.2 -R.sub.8 are as defined herein are potassium channel activators, a process for their preparation and their pharmaceutical use.
    Type: Grant
    Filed: April 21, 1992
    Date of Patent: August 3, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Geoffrey Stemp, Gordon Burrell
  • Patent number: 5220024
    Abstract: A process for the preparation of a compound of formula (A): ##STR1## wherein X is hydrogen, hydroxy, chloro, C.sub.1-6 alkoxy or phenyl C.sub.1-6 alkoxy and R.sub.a and R.sub.b are hydrogen, including acyl and phosphate derivatives thereof; which process comprises:i) the preparation of a compound of formula (I): ##STR2## wherein R.sub.1 is C.sub.1-6 alkyl, or phenyl C.sub.1-6 alkyl in which the phenyl group is optionally substituted; R.sub.2 is hydrogen, hydroxy, chlorine, C.sub.1-6 alkoxy, phenyl C.sub.1-6 alkoxy or amino; and R.sub.3 is halogen, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphonyl, azido, an amino group or a protected amino group, which process comprises the reaction of a compound of formula (II): ##STR3## with a compound of formula (VII): ##STR4## wherein Q is a leaving group, J is hydrogen or halo and R.sub.
    Type: Grant
    Filed: September 26, 1990
    Date of Patent: June 15, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Graham R. Geen, Trevor J. Grinter, Stephen Moore
  • Patent number: 5217975
    Abstract: A compound of formula (I) useful for treating dementia or a pharmaceutically acceptable salt thereof: ##STR1## in which one of X and Y represents hydrogen and the other represents Z, where Z is a group in which Q represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises two or three nitrogen atoms, any amino nitrogen being substituted by a C.sub.1-2 alkyl, cyclopropyl or propargyl group, r represents the integer of 2 or 3, s represents an integer of 1 or 2 and t represents 0, with the proviso that when Y is hydrogen s is 1.
    Type: Grant
    Filed: June 4, 1990
    Date of Patent: June 8, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Harry J. Wadsworth, Sarah M. Jenkins
  • Patent number: 5216161
    Abstract: A process for the preparation of 2,5-diamino-4,6-dichloropyrimidine, which process comprises the chlorination of 2,5-diamino-4,6-dihydroxypyrimidine with phosphorus oxychloride and a quaternary ammonium chloride or a weak tertiary amine base hydrochloride.
    Type: Grant
    Filed: January 16, 1992
    Date of Patent: June 1, 1993
    Assignee: Beecham Group p.l.c.
    Inventor: John C. Hanson
  • Patent number: 5212163
    Abstract: Novel compounds of formula (I) and salts, solvates and hydrates thereof, processes for their preparation and their use in the treatment of conditions in which degradation of connective tissue and other proteinaceous components of the body occurs: ##STR1## in which, R is hydrogen, C.sub.1-6 alkyl or optionally substituted benzyl; R.sub.1 is hydrogen or C.sub.1-6 alkyl; R.sub.2 is C.sub.3-6 alkyl; R.sub.3 is hydrogen, alkyl, --CH.sub.2 --Z where Z is optionally substituted phenyl or heteroaryl, or R.sub.3 is a group ##STR2## where R.sub.7 is hydrogen, alkyl or --CH.sub.2 --Ph where Ph is optionally substituted phenyl and R.sub.8 is hydrogen or alkyl; and R.sub.4 is --CH.sub.2 --(CH.sub.2).sub.n OR.sub.5 or --CH.sub.2 --(CH.sub.2).sub.n OCOR.sub.6 or --CH(R.sub.9)COR.sub.10, where n is an integer from 1 to 6; R.sub.5, R.sub.6 and R.sub.9 are hydrogen or C.sub.1-6 alkyl; and R.sub.10 is hydroxy or --O--C.sub.1-6 alkyl or --NR.sub.5 R.sub.6 (where R.sub.5 and R.sub.
    Type: Grant
    Filed: September 9, 1991
    Date of Patent: May 18, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Robert W. Ward, Roger E. Markwell, David J. Hunter
  • Patent number: 5210234
    Abstract: A compound of the following formula: ##STR1## wherein: R.sub.1 and R.sub.2 is hydrogen or C.sub.1-4 alkyl or R.sub.1 and R.sub.2 together are C.sub.2-5 polymethylene; R.sub.3 is hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 alkylcarbonyloxy; R'.sub.4 is ethyl, isopropyl, t-butyl or cyclopentyl, and R.sup.1.sub.6 is hydrogen or C.sub.1-6 alkyl.
    Type: Grant
    Filed: August 22, 1991
    Date of Patent: May 11, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: John M. Evans, Geoffrey Stemp, Frederick Cassidy
  • Patent number: 5204330
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is a group --CH.sub.2 --X where X is hydrogen, halogen, --CN, --N.sub.3, --OC(O)R.sub.5, --S(O).sub.n R.sub.5, --SH, --OC(O)NHR.sub.5, --NHCONHR.sub.5 or --NR.sub.6 R.sub.7, where R.sub.5 is hydrogen optionally substituted C.sub.1-8 alkyl, or aryl, heteroaryl, aryl C.sub.1-4 alkyl or heteroaryl C.sub.1-4 alkyl in each of which the aromatic moiety is optionally substituted with the proviso that when X is --S(O).sub.n R.sub.5, R.sub.5 does not represent hydrogen, R.sub.6 and R.sub.7 are independently hydrogen or C.sub.116 alkyl, or one of R.sub.6 and R.sub.7 is hydrogen and the other is --formyl, C.sub.2-8 alkanoyl, dialkoxyphosphoryl, aroyl, heteroaroyl, aryl C.sub.1-4 alkanoyl, heteroaryl C.sub.1-4 alkanoyl, C.sub.1-8 alkylsulphonyl, arylsulphonyl, heteroarylsulphonyl, aryl C.sub.1-4 alkylsulphonyl or heteroaryl C.sub.1-4 alkylsulphonyl, where any aromatic moiety in R.sub.6 or R.sub.
    Type: Grant
    Filed: December 6, 1990
    Date of Patent: April 20, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Michael J. Driver, Alexander R. Greenlees, David T. MacPherson
  • Patent number: 5200413
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein L is NH;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 5, 1991
    Date of Patent: April 6, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Francis D. King, Karen A. Joiner
  • Patent number: 5200179
    Abstract: Sterile pharmaceutical compositions for use in therapy especially inactivated vaccines for use in prophylaxis, are prepared by inactivating a live virus or bacterium with ascorbic acid and/or a salt thereof in the presence of oxygen and a source of heavy metal ions. Methods of treating animals, including humans, with such compositions are also disclosed.
    Type: Grant
    Filed: February 13, 1991
    Date of Patent: April 6, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Dale Bordt, Hans Draayer
  • Patent number: 5194250
    Abstract: A skin- or hair-care composition containing silica additionally comprises a C.sub.2-4 alkyl ester of a di, tri- or tetrabasic carboxylic acid or hydroxy-carboxylic acid (optionally acetylated). The alkyl ester may be dissolved in an aqueous solvent system.
    Type: Grant
    Filed: June 26, 1991
    Date of Patent: March 16, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Edgar Fairhurst, Helen Sayers, Steven Poile
  • Patent number: 5194443
    Abstract: Compounds of formula (I): ##STR1## or a tautomeric form thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein:A.sup.1 represents a substituted or unsubstituted aromatic heterocyclyl group;R.sup.1 represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group;R.sup.2 and R.sup.3 each represent hydrogen, or R.sup.2 and R.sup.3 together represent a bond;A.sup.2 represents a benzene ring having in total up to five substituents; andn represents an integer in the range of from 2 to 6; pharmaceutical compositions containing such compounds and the use of such compounds and compositions in medicine.
    Type: Grant
    Filed: January 24, 1991
    Date of Patent: March 16, 1993
    Assignee: Beecham Group p.l.c.
    Inventor: Richard M. Hindley
  • Patent number: 5191093
    Abstract: 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: March 12, 1990
    Date of Patent: March 2, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Geoffrey H. Baker, Merle Beal
  • Patent number: 5190937
    Abstract: Novel compounds of formula (I), and pharmaceutically acceptable salts thereof; their preparation; compositions containing them; and their use in the treatment of conditions in which degradation of connective tissue and other proteinaceous components of the body occurs: ##STR1## in which, R.sub.1 is --OH; alkoxy; aryloxy or aralkyloxy in each of which the aryl group is optionally substituted; --NR.sub.6 R.sub.7, where each of R.sub.6 and R.sub.7 is independently hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are bonded form a 5-, 6- or 7-membered ring with an optional oxygen or sulphur atom or an optionally substituted second nitrogen atom in the ring; or a group:--NH--CH(R.sub.8)--C(O)--R.sub.9where R.sub.8 is hydrogen; alkyl optionally substituted by --OH, alkoxy, --NR.sub.6 R.sub.7 as defined for R.sub.1, guanidine, --CO.sub.2 H, --CONH.sub.2, --SH, or --S--alkyl; or --CH.sub.2 --Ar where Ar is optionally substituted aryl or heteroaryl; and R.sub.
    Type: Grant
    Filed: January 11, 1991
    Date of Patent: March 2, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Roger E. Markwell, Ian Hughes