Patents Assigned to Beecham Group p.l.c.
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Patent number: 4957905Abstract: 9-(N'-substituted hydrazone) derivatives of certain erythromycin compounds are novel, antibacterially active compounds which can be prepared by treatment of the corresponding 9-imine derivative with an N'-substituted hydrazine.Type: GrantFiled: September 7, 1988Date of Patent: September 18, 1990Assignee: Beecham Group p.l.c.Inventor: Eric Hunt
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Patent number: 4954489Abstract: Compounds of formula (I) and their salts and esters: ##STR1## wherein X is hydrogen or a group NHR.sup.1, wherein R.sup.1 is hydrogen or an amino protecting group, and R is optionally substituted C.sub.5-8 cycloalkyl or cycloalkenyl, are useful in the treatment of bacterial infections.Type: GrantFiled: April 5, 1989Date of Patent: September 4, 1990Assignee: Beecham Group p.l.c.Inventors: Roger J. Ponsford, Andrew V. Stachulski
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Patent number: 4954532Abstract: A degreasing or moisturizing composition contains silanized silica gel, a humectant such as glycerine, and an inert carrier. The composition is used to treat sebhorreic conditions without causing dry skin.Type: GrantFiled: January 30, 1985Date of Patent: September 4, 1990Assignee: Beecham Group p.l.c.Inventors: Thomas J. Elliott, Susan Dutton
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Patent number: 4952584Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-4 alkyl wherein the phenyl moiety is optionally substituted by one or more C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, hydroxy, C.sub.2-7 alkanoyl, halo, trifluoromethyl, nitro, amino optionally substituted by one or two C.sub.1-6 alkyl groups or by C.sub.2-7 alkanoyl, cyano, carbamoyl or carboxy groups; R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylthio, hydroxy, C.sub.2-7 alkanoyl, chloro, fluoro, trifluoromethyl, nitro, amino optionally substituted by one or two C.sub.1-6 alkyl groups or by C.sub.2-7 alkanoyl, cyano, carbamoyl and carboxy, and phenyl, phenyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkoxy in which any phenyl moiety is optionally substituted by any of these groups; R.sub.5 and R.sub.6 are independently selected from hydrogen, C.sub.Type: GrantFiled: February 6, 1989Date of Patent: August 28, 1990Assignee: Beecham Group p.l.c.Inventors: Mervyn Thompson, Ian T. Forbes
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Patent number: 4946966Abstract: A process for the preparation of a compound of formula (I): ##STR1## which comprises the reactive of a methylating agent with a compound of formula (IV): ##STR2## in a polar solvent in which is dissolved an alkali metal alkoxide, in an inert atmosphere.Type: GrantFiled: December 20, 1988Date of Patent: August 7, 1990Assignee: Beecham Group P.L.C.Inventors: Francis D. King, Thomas W. Ramsay
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Patent number: 4943582Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: X, Y and R.sub.1 -R.sub.6 are as defined have blood pressure lowering activity and K+ channel activator activity and are useful in the treatment of hypertension.Type: GrantFiled: May 1, 1987Date of Patent: July 24, 1990Assignee: Beecham Group p.l.c.Inventors: John M. Evans, Geoffrey Stemp, Frederick Cassidy
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Patent number: 4942166Abstract: A crystalline monohydrate of the compound of formula (A) or a crystalline sodium salt monohydrate of the compound of formula (A): ##STR1## having antiviral activity, processes for their preparation and their use as pharmaceuticals.Type: GrantFiled: June 30, 1989Date of Patent: July 17, 1990Assignee: Beecham Group p.l.c.Inventors: Michael R. Harnden, Richard L. Jarvest, Graham R. Geen
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Patent number: 4942160Abstract: A method of treatment of visceral pain in mammals, including humans, which method comprises the administration to the mammal in need of such treatment, an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof:X--CO--Y--Z (I)whereinX is a group of formula (a), (b), (c), (d) or (e): ##STR1## wherein R.sub.a to R.sub.d are selected from hydrogen, halogen or hydroxy;R.sub.1 is hydrogen and R.sub.2 is a hydrogen or C.sub.1-4 alkyl; orR.sub.1 and R.sub.2 together are a bond;R.sub.3 to R.sub.7 are independently hydrogen or C.sub.1-6 alkyl; andR.sub.4 together with R.sub.2 may be C.sub.2-7 polymethylene when R.sub.1 is hydrogen;either R.sub.8 is C.sub.1-6 alkoxy;R.sub.9 is hydrogen;R.sub.10 is amino or C.sub.1-7 alkanoylamino; andR.sub.11 is halo or C.sub.1-6 alkylthio; orR.sub.8 is hydrogen;R.sub.9 is halo, or C.sub.1-6 alkoxy or C.sub.1-6 alkyl;R.sub.10 is hydrogen or C.sub.1-6 alkoxy; andR.sub.11 is halo, C.sub.1-6 alkoxy or C.sub.Type: GrantFiled: May 5, 1989Date of Patent: July 17, 1990Assignee: Beecham Group p.l.c.Inventors: Gareth J. Sanger, Helen E. Marr
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Patent number: 4940702Abstract: .beta.-Lactam antibiotics are disclosed which have the formulae (Ia) or pharmaceutically acceptable salts or pharmaceutically acceptable in vivo hydrolysable esters thereof: ##STR1## wherein R.sup.1 is phenyl, substituted phenyl, cyclohexenyl, cyclohexadienyl, or an optionally substituted 5- or 6-membered heterocyclic ring containing up to three hetero-atoms selected from oxygen, sulphur or nitrogen; R.sup.2 is hydrogen or optionally substituted C.sub.1-6 alkyl; R.sup.3 is an optionally substituted 5- or 6- membered heterocyclic group containing one or two nitrogen heteroatoms; or R.sup.2 and R.sup.3 together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6- membered heterocyclic group contaning one or two nitrogen heteroatoms; R.sup.4 is a substituted pyridinium group; and CO.sub.2 R is carboxy or a carboxylate anion; and also the use thereof.Processes for the preparation of the compounds are disclosed together with intermediates for use therein.Type: GrantFiled: August 8, 1986Date of Patent: July 10, 1990Assignee: Beecham Group p.l.c.Inventors: Stephen C. Finch, Michael J. Pearson
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Patent number: 4940701Abstract: A pharmaceutical composition for topical administration consisting of two liquid phases designed to be admixed in situ or prior to use. The first phase contains a dissolved drug, and is preferably saturated in the drug, while the second phase is a chemically or physically different liquid from that in the first phase and contains no drug, but is miscible with the first phase. The two liquids are selected so that, on admixture of suitable volumes of the phases, the resultant drug concentration exceeds the saturated drug solubility in the resultant mixture. This produces a liquid mixture supersaturated in drug, which has been found to increase the rate of drug penetration into the skin. The two liquid phases may be gels, and the drug may be hydrocortisone.At least one phase contains an antinucleant to improve stability of the resulting supersaturated solution.Type: GrantFiled: December 10, 1987Date of Patent: July 10, 1990Assignee: Beecham Group p.l.c.Inventor: Adrian F. Davis
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Patent number: 4937243Abstract: Novel compounds of the formula (I), processes for their preparation and their use as collagenase inhibitors are described: ##STR1## in which R.sub.1 is hydroxy; alkoxy; aryloxy; aralkyloxy; --NR.sub.6 R.sub.7 where R.sub.6 and R.sub.7 are hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the N-atom to which they are bonded form a 5- to 7-membered ring with an optional heteroatom; --NHCH(R.sub.8)COR.sub.9 where R.sub.8 is hydrogen; alkyl optionally substituted by hydroxy, alkoxy, --NR.sub.6 R.sub.7, quanidine, CO.sub.2 H, CONH.sub.2, SH, or S-alkyl; or CH.sub.2 -AR where Ar is optionally substituted aryl; and R.sub.9 is hydroxy, alkoxy or --NR.sub.6 R.sub.7.R.sub.2 is hydrogen or acyl.R.sub.3 is C.sub.3-6 alkyl.R.sub.4 is hydrogen; alkyl; --CH.sub.2 R.sub.10 where R.sub.10 is optionally substituted phenyl or heteroaryl; or --CH(R.sub.12)O--R.sub.11 where R.sub.11 is hydrogen; alkyl; or --CH.sub.2 Ph where Ph is optionally substituted phenyl; and R.sub.12 is hydrogen or alkyl.R.sub.Type: GrantFiled: December 22, 1987Date of Patent: June 26, 1990Assignee: Beecham Group p.l.c.Inventors: Roger E. Markwell, Stephen A. Smith, Ian Hughes
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Patent number: 4937247Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is CH or N;Y is NH or O;R.sub.1 is hydrogen or halogen;R.sub.2 is a group of formula (a), (b) or (c) ##STR2## wherein n is 2 or 3; p and q are independently 1 to 3; and R.sub.4 or R.sub.5 is C.sub.1-4 alkyl;R.sub.3 i s C.sub.1-10 acyl, C.sub.1-6 alkoxycarbonyl, optionally substituted phenoxycarbonyl or benzyloxycarbonyl, or R.sub.6 R.sub.7 NCO or R.sub.6 R.sub.7 NS(O).sub.m wherein m is 1 or 2 and R.sub.6 and R.sub.7 are independently C.sub.1-6 alkyl groups or together are C.sub.4-6 polymethylene; having 5-HT.sub.3 antagonist activity, a process for their preparation and their use as pharmaceuticals.Type: GrantFiled: September 25, 1987Date of Patent: June 26, 1990Assignee: Beecham Group p.l.c.Inventor: Francis D. King
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Patent number: 4935404Abstract: Novel compounds of the formula (I), a process for their preparation and their use as collagenase inhibitors are described: ##STR1## in which R.sub.1 is hydrogen or hydroxy; R.sub.2 is hydrogen or alkyl; R.sub.3 is C.sub.3-6 alkyl; R.sub.4 is hydrogen, alkyl, --CH.sub.2 --Z where Z is optionally substituted phenyl or heteroaryl, or R.sub.4 is a group ##STR2## where R.sub.8 is hydrogen, alkyl or --CH.sub.2 --Ph where Ph is optionally substituted phenyl, and R.sub.9 is hydrogen or alkyl; and R.sub.5 is hydrogen or alkyl.Type: GrantFiled: November 14, 1988Date of Patent: June 19, 1990Assignee: Beecham Group p.l.c. of Beecham HouseInventors: David J. Hunter, Roger E. Markwell, Robert W. Ward
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Patent number: 4935465Abstract: A conjugate comprising a pharmaceutically useful protein linked to at least one water-soluble polymer by means of a reversible linking group.Type: GrantFiled: November 27, 1985Date of Patent: June 19, 1990Assignee: Beecham Group p.l.c.Inventor: Andrew J. Garman
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Patent number: 4931434Abstract: Compounds of the general formula (II): ##STR1## in which N.sup.+ denotes an unsubstituted or substituted nitrogen-containing heterocyclyl ring bonded to the remainder of the molecule through a ring nitrogen atom and carrying a positive charge on said nitrogen atom;and the wavy line denotes either the E- or Z-isomeric position,are novel and are useful in the treatment of antibacterial infection in humans or animals.Type: GrantFiled: December 16, 1988Date of Patent: June 5, 1990Assignee: Beecham Group p.l.c.Inventors: Nigel J. P. Broom, Gerald Brooks, Brian P. Clarke
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Patent number: 4923856Abstract: Compounds of the general formula (II): ##STR1## and pharmaceutically acceptable salts and in-vivo hydrolysable esters thereof, in whichR denotes a hydrogen atom or an in vivo hydrolysable acyl group;and the wavy line denotes either the E- or Z-isometric position,are novel compounds which exhibit .beta.-lactamase inhibitory action and have antibacterial properties.Type: GrantFiled: December 16, 1988Date of Patent: May 8, 1990Assignee: Beecham Group p.l.c.Inventors: Nigel J. P. Broom, Gerald Brooks, Steven Coulton
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Patent number: 4921839Abstract: Antibacterially active 11,12-carbonate derivatives of erythromycin 9-(optionally substituted)oxime and 9-imino compounds and their pharmaceutically acceptable ester or acid addition salt thereof: ##STR1## wherein R.sup.1 denotes an oxime group, a substituted oxime group, or an imino group;R.sup.3 denotes a hydrogen atom or an unsubstituted or substituted alkyl group;R.sup.7 denotes hydrogen or methyl;one of R.sup.8 and R.sup.9 denotes hydrogen, hydroxy, alkoxy, alkanoyloxy, amino, substituted amino, or a group of the formula R.sup.A --SO.sub.2 --O--, in which R.sup.A denotes an organic group, and the other of R.sup.8 and R.sup.9 denotes hydrogen, orR.sup.8 and R.sup.9 together denote an oxo group, an oxime group, or a substituted oxime group.Type: GrantFiled: February 22, 1988Date of Patent: May 1, 1990Assignee: Beecham Group p.l.c.Inventors: Edward G. Brain, Eric Hunt, Andrew K. Forrest
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Patent number: 4920127Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein L is NH or O;R.sub.1 is hydrogen, fluoro or chloro;R.sub.2 and R.sub.5 are independently hydrogen or C.sub.1-6 alkyl or together are a bond; orR.sub.2 and R.sub.3 and/or R.sub.4 and R.sub.5, together are C.sub.2-7 polymethylene or --(CH.sub.2).sub.m --O--(CH.sub.2).sub.x -- where m and x. are 1 to 5 such that m+x is 2 to 6;R.sub.4 is C.sub.1-7 acyl, C.sub.1-6 alkoxycarbonyl, hydroxycarbonyl, aminocarbonyl optionally substituted by one or two C.sub.1-6 alkyl groups, CF.sub.3, C.sub.1-6 alkyl substituted by C.sub.1-6 alkoxy, C.sub.1-6 alkylthio or by C.sub.1-6 alkoxycarbonyl, or R.sub.4 is phenyl or phenyl-C.sub.1-4 alkyl optionally substituted in the phenyl ring by one or two of halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy;Z is a group of formula (a), (b) or (c).Type: GrantFiled: February 16, 1988Date of Patent: April 24, 1990Assignee: Beecham Group p.l.c.Inventors: Francis D. King, Karen A. Joiner
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Patent number: 4918083Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereof, or a pharmaceutically acceptable solvate thereof, wherein:Z represents a residue of a substituted or unsubstituted aryl group,A.sup.1 represents a substituted or unsubstituted methylene group or a substituted or unsubstituted ethylene group;A.sup.2 represents a substituted or unsubstituted methylene group or a substituted or unsubstituted ethylene group;providing that at least one of A.sup.1 or A.sup.2 represents a substituted methylene group or a substituted ethylene group,X represents O or NR.sup.o wherein R.sup.Type: GrantFiled: November 24, 1987Date of Patent: April 17, 1990Assignee: Beecham Group p.l.c.Inventors: John M. Berge, Lee J. Beeley
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Patent number: 4918091Abstract: A compound of formula (I): ##STR1## or a tautomeric form thereof, or a pharmaceutically acceptable salt thereof, wherein:R represents hydrogen or alkyl;R.sup.1 represents an alkyl group 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 represents a benzene ring having in total up to five substituents;X represents oxygen, sulphur or a moiety NR.sup.4 wherein R.sup.4 represents hydrogen or alkyl; andn represents an integer in the range of from 2 to 6; a process for preparing such a compound, a composition containing such a compound and the use of the compound and composition in medicine.Type: GrantFiled: June 13, 1988Date of Patent: April 17, 1990Assignee: Beecham Group p.l.c.Inventors: Barrie C. C. Cantello, Richard M. Hindley