Patents Assigned to Beecham Group
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Patent number: 4524075Abstract: Topical formulations comprise pseudomonic acid or a salt or ester thereof and a polyethylene glycol or polyethylene glycol analogue or derivative.Type: GrantFiled: May 26, 1983Date of Patent: June 18, 1985Assignee: Beecham Group p.l.c.Inventor: Joshua Oduro-Yeboah
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Patent number: 4524073Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R represents an alkyl or aralkyl group, substituted on an alkyl carbon atom other than that adjacent to --NH-- group, with one or more functional groups selected from halogen, non-aromatic heterocyclyl linked through carbon, aromatic heterocyclyl, nitro, oxo, --OR.sup.1, SR.sup.1 --P(O)R.sup.2 R.sup.3, --NR.sup.4 R.sup.5, .dbd.NR.sup.6, or a sulphur linked organic radical, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are various organic radicals.Processes for the preparation of these compounds and pharmaceutical compositions containing them are also disclosed.Type: GrantFiled: July 20, 1983Date of Patent: June 18, 1985Assignee: Beecham Group p.1.c.Inventors: Irene Stirling, Gordon Bruton, Stephen H. Calvert, Brian P. Clarke
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Patent number: 4521337Abstract: A process for the preparation of a compound of the formulae (Ia) and/or (Ib): ##STR1## wherein R.sup.1 and R.sup.2 are independently substituted or unsubstituted hydrocarbon groups or are joined together so as to form a carbocyclic or heterocyclic ring, and R.sup.3 is a substituted or unsubstituted hydrocarbon group; which process comprises the ring-closing cyclization of a compound of the formula (II): ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined in relation to formulae (Ia) and (Ib).Type: GrantFiled: March 14, 1983Date of Patent: June 4, 1985Assignee: Beecham Group p.l.c.Inventors: Robert Southgate, Pamela Brown
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Patent number: 4520014Abstract: Vasoconstrictor .alpha.-adrenergic agonists of formula (I)A-B-C (I)wherein, A is a 2-imidazoline group or a guanidine group; B is a chemical bond or a linking group one or two atoms in length; and C is a C.sub.6-10 mono- or bi-cyclic group which is either an aromatic group, a heteroaromatic group containing only one hetero-atom, or a group containing an aromatic moiety; and which group C may be substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or hydroxyl; or salts thereof, are useful in the treatment and prevention of diarrhoea in livestock. Compositions of these compounds are described.Type: GrantFiled: February 19, 1982Date of Patent: May 28, 1985Assignee: Beecham Group p.l.c.Inventors: Peter M. Newsome, Noel A. Mullan
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Patent number: 4518606Abstract: A pharmaceutical composition for injection which comprises an aqueous sterile solution of a penicillin or salt thereof and from 1 to 10% of benzyl alcohol, a two-pack container or two-part syringe wherein one pack or part contains a penicillin or salt thereof in the form of a dry powder and the second pack or part contains an aqueous solution of benzyl alcohol, such that mixing the contents of the two packs or parts produces an aqueous solution of the penicillin and from 1 to 10% of benzyl alcohol, and a two-pack container or two-part syringe wherein one pack or part contains a penicillin in a solid free acid form, and the second part contains an aqueous solution of benzyl alcohol and substantially one equivalent of a basic pharmaceutically acceptable salt, such that mixing the contents of the two packs or parts produces an aqueous solution of a salt of the penicillin and from 1 to 10% of benzyl alcohol.Type: GrantFiled: July 9, 1982Date of Patent: May 21, 1985Assignee: Beecham Group LimitedInventor: Edmond Saias
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Patent number: 4517124Abstract: The present invention provides a process for the preparation of a compound of the formula (IV): ##STR1## or salt or ester thereof wherein R.sup.1 and R.sup.2 are independently hydrogen; an organic radical bonded via a carbon atom to the ring carbon atom; a free, etherified or esterified hydroxy or mercapto group; an amino or acylamino group; or together R.sup.1 and R.sup.2 represent a group .dbd.CR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are the same or different and each represent hydrogen or a hydrocarbon or heterocyclic group optionally substituted with a functional group; and R.sup.3 represents an organic radical; which process comprises reacting a compound of the formula (V): ##STR2## wherein R.sup.x is hydrogen or a blocking group and R.sup.4 is an organic radical; with a thiol or reactive derivative thereof. The compounds of the formula (IV) are useful as antibiotics and .beta.-lactamase inhibitors, as are the compounds of the formula (V).Type: GrantFiled: November 14, 1983Date of Patent: May 14, 1985Assignee: Beecham Group LimitedInventor: Nigel J. P. Broom
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Patent number: 4510152Abstract: Compounds of formula (I): ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, C.sub.1-6 alkyl-thiolmethyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.Type: GrantFiled: April 21, 1983Date of Patent: April 9, 1985Assignee: Beecham Group p.l.c.Inventor: Erol A. Faruk
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Patent number: 4507283Abstract: A derivative of streptokinase-human plasminogen activator complex, in which the active catalytic site essential for fibrinolytic activity is blocked by a 2- or 4-aminobenzoyl group, is useful in treating venous thrombosis.The blocking group is removable by hydrolysis such that the first order rate is in the range 0.7.times.10.sup.-5 sec.sup.-1 to 2.5.times.10.sup.-5 sec.sup.-1 in isotonic aqueous media at pH 7.4 at 37.degree. C.Type: GrantFiled: April 5, 1983Date of Patent: March 26, 1985Assignee: Beecham Group p.l.c.Inventor: Richard A. G. Smith
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Patent number: 4505926Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each is selected from halogen, alkyl, haloalkyl, alkoxy and alkoxyalkyl,R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is alkyl;n is 0,1,2 or 3; andZ is a pharmaceutically or veterinarily acceptable anion, protect animals from death due to enteropathogenic E. coli infection of the gastro-intestinal tract.Type: GrantFiled: September 15, 1983Date of Patent: March 19, 1985Assignee: Beecham Group p.l.c.Inventors: Peter M. Newsome, Stephen F. Moss, Lee J. Beeley, Malcolm N. Burgess
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Patent number: 4505894Abstract: Compounds of the formula ##STR1## wherein X is S, SO or SO.sub.2 and R is an inert hydrocarbon of up to 20 carbon atoms which will not lead to rapid degradation of the above compound unsubstituted or substituted and A is a group such and CO.sub.2 A represents a carboxylic acid group or a salt or ester thereof, are useful for their antibacterial activity and for their .beta.-lactamase inhibitory activity.Type: GrantFiled: August 30, 1982Date of Patent: March 19, 1985Assignee: Beecham Group LimitedInventor: Roger J. Ponsford
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Patent number: 4504480Abstract: Compounds of formula (I), ##STR1## or an N-oxide or pharmaceutically acceptable salt thereof, wherein R.sub.1 is hydrogen, C.sub.1-7 alkyl, C.sub.3-7 cycloalkyl, C.sub.4-7 cycloalkenyl or C.sub.1-4 alkyl substituted by C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, C.sub.3-7 cycloalkyl, hydroxy, thiol, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, carboxy, C.sub.1-4 alkoxycarbonyl, C.sub.1-4 alkanoyl, amino optionally substituted by one or two C.sub.1-4 alkyl or by C.sub.4-6 polymethylene optionally containing an oxygen or nitrogen atom, aminocarbonyl optionally N-substituted by one or two C.sub.1-4 alkyl, or benzoyl or phenyl either being optionally ring-substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or trifluoromethyl, R.sub.2 and R.sub.3 are the same or different and are hydrogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alklthio, halogen or trifluoromethyl, m is 1 to 3 and n is 1 or 2, the hydrogen atom bonded to the C.sub.a carbon atom being trans to the hydrogen atom bonded to the C.sub.Type: GrantFiled: March 4, 1983Date of Patent: March 12, 1985Assignee: Beecham Group p.l.c.Inventors: Laramie M. Gaster, Barry S. Orlek
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Patent number: 4501696Abstract: A process for the preparation of a penam derivative of formula (I): ##STR1## wherein R.sup.A is hydrogen or a group of formula (Ia): ##STR2## wherein X is --CO.sub.2 R.sup.1, or SO.sub.3 R.sup.1 ; R is C.sub.1-6 alkyl, aryl, or heterocyclyl; R.sup.1 is hydrogen, or a pharmaceutically acceptable salt-forming ion or ester-forming radical, and R.sup.2 represents hydrogen or a pharmaceutically acceptable salt-forming ion or in vivo hydrolyzable ester-forming radical; which process comprises reacting a compound of formula (II): ##STR3## wherein R.sup.B is hydrogen, a removable amino blocking group, or a group of formula (IIa): ##STR4## wherein Y is --CO.sub.2 R.sup.x or --SO.sub.3 R.sup.x ; R is as defined with respect to formula (I) above; R.sup.x represents an ester-forming radical, R.sup.Y represents hydrogen, a salt-forming radical or a carboxyl-blocking group, and R.sup.Type: GrantFiled: July 9, 1982Date of Patent: February 26, 1985Assignee: Beecham Group p.l.c.Inventors: John R. M. Dales, Marguerita A. Vallance
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Patent number: 4499099Abstract: Pharmaceutical compositions comprising compounds of formula (I) or pharmaceutically acceptable salts and/or N-oxides and/or solvates thereof: ##STR1## wherein: R.sub.1 is a C.sub.1-6 alkoxy or C.sub.1-6 alkylthio group; andone of R.sub.2, R.sub.3 and R.sub.4 is hydrogen, the second is C.sub.1-6 alkylthio and the third is selected from the class of substituents consisting of 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 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl or aminosulphonyl optionally N-substituted by one or two C.sub.1-6 alkyl groups; orR.sub.1 is joined to R.sub.2 to form C.sub.1-2 alkylenedioxy; andone of R.sub.3 and R.sub.4 is C.sub.1-6 alkylthio and the other is selected from the class of substituents defined above;R.sub.5 is hydrogen or C.sub.1-6 alkyl;R.sub.6 is C.sub.1-7 alkyl or a group --(CH.sub.2).sub.s R.sub.7 where s is 0 to 2 and R.sub.7 is a C.sub.Type: GrantFiled: June 9, 1982Date of Patent: February 12, 1985Assignee: Beecham Group p.l.c.Inventor: Eric A. Watts
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Patent number: 4496565Abstract: Compounds of formula (I): ##STR1## a pharmaceutically acceptable salt or solvate thereof having anti-hypertensive activity, a process for their preparation and their use as pharmaceuticals.Type: GrantFiled: October 17, 1983Date of Patent: January 29, 1985Assignee: Beecham Group p.l.c.Inventors: John M. Evans, Valerie A. Ashwood
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Patent number: 4490295Abstract: The invention provides the compound (2R,5R,Z)-3-(2-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo-[3,2,0]heptane- 2-carboxylic acid and its salts in purified form and pharmaceutical compositions containing them and a process for the purification of such compounds by conversion in aqueous media to the lithium salt of the above acid and precipitation thereof.Type: GrantFiled: May 7, 1980Date of Patent: December 25, 1984Assignee: Beecham Group p.1.c.Inventors: Ian D. Fleming, David Noble, Hazel M. Noble (formerly Gillett), Wilfred F. Wall
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Patent number: 4490294Abstract: The invention provides the compound (2R,5R,Z)-3-(2-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo-[3,2,0]-heptane -2-carboxylic acid and its salts in purified form and pharmaceutical compositions containing them and a process for the purification of such compounds by conversion in aqueous media to the lithium salt of the above acid and precipitation thereof.Type: GrantFiled: March 20, 1978Date of Patent: December 25, 1984Assignee: Beecham Group p.l.c.Inventors: Ian D. Fleming, David Noble, Hazel M. Noble, Wilfred F. Wall
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Patent number: 4490383Abstract: A pharmaceutical composition adapted for administration to a human by injection which composition comprises an aqueous solution containing sodium amoxycillin and tri-sodium phosphate, the weight ratio of sodium amoxycillin present to the tri-sodium phosphate present being from 8:1 to 50:1.Type: GrantFiled: December 9, 1982Date of Patent: December 25, 1984Assignee: Beecham Group LimitedInventor: Stuart A. Hill
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Patent number: 4485110Abstract: A class of 6-alkylidene penem compounds of formula (II) have antibacterial and .beta.-lactamase inhibitory properties: ##STR1## where R.sup.1 and R.sup.2 represent hydrogen or optionally substituted hydrocarbon or heterocyclic, and R.sup.3 represents hydrogen or an organic group.Type: GrantFiled: April 23, 1981Date of Patent: November 27, 1984Assignee: Beecham Group LimitedInventor: Neal F. Osborne
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Patent number: 4481209Abstract: Ampicillin phthalidyl ester naphthalene-2-sulphonate, its preparation, and its use in pharmaceutical compositions to treat infections.Type: GrantFiled: November 7, 1980Date of Patent: November 6, 1984Assignee: Beecham Group LimitedInventors: Kenneth Utting, Karrar A. Khan, Sidney E. Callander
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Patent number: 4481213Abstract: A compound of the formula (I): ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1 is hydrogen or C.sub.1-6 alkyl or an acyl group of 1 to 8 carbon atoms; n is 2, 3 or 4; X is halogen; and the OR.sub.1 and HN(CH.sub.2).sub.n X moieties are trans; has anti-hypertensive activity and a low level of cardiac side-effects.Type: GrantFiled: July 15, 1982Date of Patent: November 6, 1984Assignee: Beecham Group LimitedInventor: John M. Evans