Abstract: 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:
Grant
Filed:
December 22, 1987
Date of Patent:
June 26, 1990
Assignee:
Beecham Group p.l.c.
Inventors:
Roger E. Markwell, Stephen A. Smith, Ian Hughes
Abstract: A conjugate comprising a pharmaceutically useful protein linked to at least one water-soluble polymer by means of a reversible linking group.
Abstract: 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:
Grant
Filed:
November 14, 1988
Date of Patent:
June 19, 1990
Assignee:
Beecham Group p.l.c. of Beecham House
Inventors:
David J. Hunter, Roger E. Markwell, Robert W. Ward
Abstract: 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:
Grant
Filed:
December 16, 1988
Date of Patent:
June 5, 1990
Assignee:
Beecham Group p.l.c.
Inventors:
Nigel J. P. Broom, Gerald Brooks, Brian P. Clarke
Abstract: Compounds of the general formula I ##STR1## or pharmaceutically acceptable salts or solvates thereof, in which R.sup.1 represents hydrogen or a lower alkyl group,R.sub.2 represents hydrogen, a lower alkyl group, or ##STR2## R.sup.3 represents hydrogen, a lower alkyl group, or ##STR3## R.sup.4 represents hydrogen or a lower alkyl group, R.sup.5 represents hydrogen or a lower alkyl group,R.sup.6 represents hydrogen, a lower alkyl, a substituted or unsubstituted aryl group, or --COOR.sup.15,R.sup.7 represents hydrogen, halogen or lower alkyl,R.sup.8 represents a lower alkyl or a substituted or unsubstituted carbocyclic aryl group,R.sup.15 represents hydrogen or a lower alkyl, and n is 0 to 8, n being 0 when R.sup.6 represents lower alkyl, are disclosed as an active therapeutic substances for the treatment of inflammatory conditions, allergic conditions and disorders related to loss of gastro-intestinal integrity.
Abstract: 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:
Grant
Filed:
December 16, 1988
Date of Patent:
May 8, 1990
Assignee:
Beecham Group p.l.c.
Inventors:
Nigel J. P. Broom, Gerald Brooks, Steven Coulton
Abstract: 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:
Grant
Filed:
February 22, 1988
Date of Patent:
May 1, 1990
Assignee:
Beecham Group p.l.c.
Inventors:
Edward G. Brain, Eric Hunt, Andrew K. Forrest
Abstract: 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).
Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt or in-vivo hydrolysable ester thereof: ##STR1## wherein R.sup.1 is a 5 or 6 membered sulphur and/or nitrogen containing heterocyclic group substituted by an optionally protected amino group, with the proviso that R.sup.1 is not 2-aminothiazol-4-yl, and R is hydrogen; optionally substituted C.sub.1-12 alkyl; optionally substituted C.sub.2-12 alkenyl or alkynyl; carbocyclyl; aryl or heterocyclyl.These compounds have antibacterial properties, and therefore are of use in the treatment of bacterial infections in humans and animals caused by a wide range of organizations.
Abstract: 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:
Grant
Filed:
June 13, 1988
Date of Patent:
April 17, 1990
Assignee:
Beecham Group p.l.c.
Inventors:
Barrie C. C. Cantello, Richard M. Hindley
Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein the various substituents are defined hereinbelow, having 5-HT.sub.3 receptor antagonist activity, processes for their preparation and their use as pharmaceuticals.
Abstract: 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.
Abstract: Crystalline calcium pseudomonate or a hydrate thereof, in particular the dihydrate.Processes for the preparation of these salts and their use in human and veterinary medicine and as a growth promoter in animals are described.
Abstract: A method for inceasing the weight gain and/or improving the feed utilization efficiency and/or increasing the lean body mass and/or decreasing birth mortality rate and increasing post-natal survival rate of livestock comprises the administration to livestock of an effective, non-toxic amount of a compound of formula (I), or a veterinarily acceptable acid addition salt thereof: ##STR1## wherein R.sup.1 is phenyl (C.sub.1-6)alkyl or optionally substituted C.sub.1-6 alkyl, andW is optionally substituted phenyl, a heterocyclyl group, or phenoxymethyl optionally substituted on the phenyl group. Certain compounds of formula (I) are novel.
Abstract: A process for the preparation of compounds of formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is hydrogen or CH.sub.2 OH;R.sub.2 is hydrogen or, (when R.sub.1 is hydrogen), hydroxy or CH.sub.2 OH;R.sub.3 is CH.sub.2 OH or, (when R.sub.1 and R.sub.2 are both hydrogen), CH(OH)CH.sub.2 OH;R.sub.4 is hydrogen, hydroxy, amino or OR.sub.5whereinR.sub.5 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 halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy groups;and in which any OH groups in R.sub.1, R.sub.2 and/or R.sub.3 may be in the form of O-acyl, phosphate, cyclic acetal or cyclic carbonate derivatives thereof;which process comprises the reaction of a compound of formula (II): ##STR2## wherein R.sub.4 ' is R.sub.4 or a group or atom convertible thereto and R.sub.x is amino or protected amino; with a compound of formula (III):R.sub.3 'CHR.sub.2 'CHR.sub.1 'Q (III)wherein Q is a leaving group and R.sub.1 ', R.sub.
Abstract: A fibrinolytically active hybrid protein which comprises one chain of a 2-chain protease linked to a chain of a different 2-chain protease, or to the same chain of the same protease, at least one of the chains in the hybrid protein being derived from a fibrinolytically active protease, such that the hybrid protein has a catalytic site essential for fibrinolytic activity which is optionally blocked by a removable blocking group.
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:
February 23, 1989
Date of Patent:
February 27, 1990
Assignee:
Beecham Group p.l.c.
Inventors:
John M. Evans, Geoffrey Stemp, Frederick Cassidy
Abstract: A process is disclosed for the preparation of a compound of formula (I): ##STR1## wherein Ar is aryl or substituted aryl and R.sup.3 is hydrogen, alkyl or aralkyl, which process comprises reducing a compound of formula (II): ##STR2## wherein Ar and R.sup.3 are as defined with respect to formula (I) and R.sup.4 is alkyl. Compounds of formula (I) are useful as chemical intermediates.
Abstract: A process for the production of a sterile composition containing lecithin and polyvinyl pyrrolidone is disclosed in which the lecithin and polyvinyl pyrrolidone, optionally with one or more preservative powders are admixed in a solvent comprising about 75% to 90% methyl isobutyl ketone and about 10% to 25% isopropyl alcohol, and the solution passed through a millipore filter in order to render the ingredients sterile. The process is usefully employed in the production of injectable compositions of amoxycillin and ampicillin.
Abstract: A syringe for dispensing a liquid pharmaceutical composition has a first chamber (5), adjacent to nozzle (3), which contains a mositure sensitive solid drug, two movable septa (8,9) which together create a second chamber (6) and a third chamber (7) holding a liquid diluent, and a liquid by-pass passage (19) which can connect the third chamber (7) to the first chamber (5) while by-passing second chamber (6).A plunger (4) is depressed to move the septum (9) towards the nozzle (3), thereby causing liquid diluent to flow via by-pass passage (19) into the first chamber (5) to mix with the drug.The second chamber (6) contains moisture sequestering material to insulate the drug from any moisture which might leak through septum (9).