Patents Assigned to Beecham Group p.l.c.
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Patent number: 5250688Abstract: 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: GrantFiled: January 22, 1992Date of Patent: October 5, 1993Assignee: Beecham Group p.l.c.Inventors: Michael R. Harnden, Richard L. Jarvest
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Patent number: 5246926Abstract: .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: GrantFiled: March 28, 1990Date of Patent: September 21, 1993Assignee: Beecham Group p.l.c.Inventors: John H. Bateson, George Burton, Stephen C. M. Fell
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Patent number: 5247085Abstract: 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: GrantFiled: May 29, 1992Date of Patent: September 21, 1993Assignee: Beecham Group p.l.c.Inventors: Michael R. Harnden, David M. Duckworth
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Patent number: 5246937Abstract: The present invention provides antiviral compounds of Formula (I): ##STR1## pharmaceutical compositions prepared therefrom, and methods of treatment of viral infections therewith.Type: GrantFiled: January 22, 1992Date of Patent: September 21, 1993Assignee: Beecham Group p.l.c.Inventors: Michael R. Harnden, Richard L. Jarvest
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Patent number: 5239090Abstract: The (3S,4R)-isomer of a compound of formula (E) is disclosed.Type: GrantFiled: February 24, 1992Date of Patent: August 24, 1993Assignee: Beecham Group p.l.c.Inventor: Erol A. Faruk
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Patent number: 5234686Abstract: 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: GrantFiled: May 30, 1991Date of Patent: August 10, 1993Assignee: Beecham Group p.l.c.Inventor: Ian Dodd
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Patent number: 5232925Abstract: 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: GrantFiled: January 15, 1991Date of Patent: August 3, 1993Assignee: Beecham Group p.l.c.Inventor: Richard M. Hindley
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Patent number: 5232938Abstract: 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: GrantFiled: April 21, 1992Date of Patent: August 3, 1993Assignee: Beecham Group p.l.c.Inventors: Geoffrey Stemp, Gordon Burrell
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Patent number: 5220024Abstract: 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: GrantFiled: September 26, 1990Date of Patent: June 15, 1993Assignee: Beecham Group p.l.c.Inventors: Graham R. Geen, Trevor J. Grinter, Stephen Moore
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Patent number: 5217975Abstract: 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: GrantFiled: June 4, 1990Date of Patent: June 8, 1993Assignee: Beecham Group p.l.c.Inventors: Harry J. Wadsworth, Sarah M. Jenkins
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Patent number: 5216161Abstract: 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: GrantFiled: January 16, 1992Date of Patent: June 1, 1993Assignee: Beecham Group p.l.c.Inventor: John C. Hanson
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Patent number: 5212163Abstract: 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: GrantFiled: September 9, 1991Date of Patent: May 18, 1993Assignee: Beecham Group p.l.c.Inventors: Robert W. Ward, Roger E. Markwell, David J. Hunter
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Patent number: 5210234Abstract: 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: GrantFiled: August 22, 1991Date of Patent: May 11, 1993Assignee: Beecham Group p.l.c.Inventors: John M. Evans, Geoffrey Stemp, Frederick Cassidy
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Patent number: 5204330Abstract: 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: GrantFiled: December 6, 1990Date of Patent: April 20, 1993Assignee: Beecham Group p.l.c.Inventors: Michael J. Driver, Alexander R. Greenlees, David T. MacPherson
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Patent number: 5200413Abstract: 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: GrantFiled: August 5, 1991Date of Patent: April 6, 1993Assignee: Beecham Group p.l.c.Inventors: Francis D. King, Karen A. Joiner
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Patent number: 5200179Abstract: 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: GrantFiled: February 13, 1991Date of Patent: April 6, 1993Assignee: Beecham Group p.l.c.Inventors: Dale Bordt, Hans Draayer
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Patent number: 5194443Abstract: 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: GrantFiled: January 24, 1991Date of Patent: March 16, 1993Assignee: Beecham Group p.l.c.Inventor: Richard M. Hindley
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Patent number: 5194250Abstract: 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: GrantFiled: June 26, 1991Date of Patent: March 16, 1993Assignee: Beecham Group p.l.c.Inventors: Edgar Fairhurst, Helen Sayers, Steven Poile
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Patent number: 5190937Abstract: 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: GrantFiled: January 11, 1991Date of Patent: March 2, 1993Assignee: Beecham Group p.l.c.Inventors: Roger E. Markwell, Ian Hughes
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Patent number: 5191093Abstract: 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: GrantFiled: March 12, 1990Date of Patent: March 2, 1993Assignee: Beecham Group p.l.c.Inventors: Geoffrey H. Baker, Merle Beal