Abstract: The acute liver toxicity effects of paracetamol are reduced by co-formulating with ascorbic acid derivatives (ascorbate anion bioprecursors) which produce high liver concentrations of ascorbate anion after oral administration of the co-formulation. A suitable ascorbate anion bioprecursor is ascorbyl 6-palmitate.
Abstract: The compounds of the formula (II): ##STR1## and salts and esters thereof wherein R.sub.1 is a pyrimidyl group, or a pyrimidyl group substituted by one or two lower alkyl groups, or by a lower alkoxy group or by a lower acyloxy group; and R.sub.2 is a hydrogen atom or a group CR.sub.3 R.sub.4 R.sub.5 wherein R.sub.3 is a hydrogen atom or a hydroxy group; R.sub.4 is a hydrogen atom or a lower alkyl group; and R.sub.5 is a hydrogen atom or a lower alkyl group, a benzyl group, a phenyl group or is joined to R.sub.4 to form part of a C.sub.5-7 carbocyclic ring, have been found to be anti-bacterial-agents. Their preparation and use is described.
Abstract: Compounds of the formula (II): ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is phenyl or naphthyl or substituted phenyl or naphthyl group; R.sub.2 is: ##STR2## wherein R.sub.5 is hydrogen or C.sub.1-6 alkyl, R.sub.6 is hydrogen or C.sub.1-6 alkyl, phenyl, tolyl or benzyl and R.sub.7 is hydrogen; R.sub.3 and R.sub.4 are each hydrogen atom or C.sub.1-4 alkyl, and X is CO, CHOH, CHCI or C.dbd.C R.sub.8 R.sub.9 wherein R.sub.8 and R.sub.9 are each hydrogen or C.sub.1-4 alkyl; or CR.sub.10 OH or CHR.sub.10, wherein R.sub.10 is C.sub.1-4 alkyl, have been found to be mood-modifying agents and anorexic agents.
Abstract: Compounds of formula (I) ##STR1## wherein: R.sup.1 is C.sub.1-6 alkyl or C.sub.5-7 cycloalkyl;R.sup.2 is hydrogen or C.sub.1-6 alkyl; orNR.sup.1 R.sup.2 represents a heterocyclic ring having 5 to 7 ring atoms and only one hetero-atom; andR.sup.3 is C.sub.1-4 alkyl, one carbon atom of which is di- or tri-halogenatedor salts thereof are useful in promoting growth of ruminants. Processes for their production, veterinary formulations and treatments are described.
Abstract: Compounds of the formula (II): ##STR1## and pharmaceutically acceptable acid-addition salts thereof wherein Ar is a pyridyl or optionally substituted phenyl group of the sub-formula --C.sub.6 H.sub.3 R.sub.1 R.sub.2 wherein R.sub.1 is a hydrogen, fluorine, chlorine or bromine atom or a lower alkyl, lower alkoxyl, lower acyl, lower acyloxyl or lower alkoxycarbonyl group; and R.sub.2 is a hydrogen, fluorine or chlorine atom or a lower alkyl or lower alkoxy group having useful anti-hypertension activity, their preparation, and pharmaceutical compositions containing them.
Abstract: Compounds of the formula (II): ##STR1## and pharmaceutically acceptable acid-addition salts thereof wherein Ar is a pyrimidyl group having useful anti-hypertension activity, their preparation, and pharmaceutical compositions containing them.
Abstract: Compounds of the formula (I): ##STR1## wherein: n is 3 to 5;Y is --CH.sub.2 --CH.sub.2 or --CH.dbd.CH-- or --C.tbd.C--R.sub.1 is C.sub.1-4 alkyl;R.sub.2 is hydrogen, C.sub.1-4 alkyl or phenyl;R.sub.3 is hydroxy or protected hydroxy;R.sub.4 is hydrogen, C.sub.1-9 alkyl, C.sub.3-8 cycloalkyl, phenyl, naphthyl, any of which phenyl moieties or naphthyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkoxy, phenyl C.sub.1-6 alkoxy or nitro groups; andR.sub.5 is C.sub.1-6 alkyl having useful pharmacological activity, compositions containing them and processes for their preparation.
Abstract: Compounds of the formula (I): ##STR1## having pharmacological activities similar to those of natural prostaglandins wherein:n is 0 to 5;X is CO, CS or CH.sub.2 ;Y is --CH.sub.2 --CH.sub.2 --; or, when n is 1 to 5, --CH.dbd.CH-- or --C.tbd.C--;R.sub.1 is either CH.sub.2 NR.sub.5 R.sub.6, wherein R.sub.5 and R.sub.6 are separately hydrogen or C.sub.1-6 alkyl, or R.sub.5 is hydrogen and R.sub.6 is (CH.sub.2).sub.m CO.sub.2 R.sup.1.sub.9 wherein m is 0 to 4 and R.sup.1.sub.9 is optionally substituted C.sub.1-6 alkyl or benzyl, optionally substituted in the phenyl ring by chlorine or bromine atoms or by nitro or CF.sub.3 groups; or R.sub.5 and R.sub.6 are both the same (CH.sub.2).sub.m CO.sub.2 R.sup.1.sub.9 as hereinbefore defined; or C(NH.sub.2).dbd.NOH; or C(OR.sub.7).dbd.NH.sub.2.sup.+ B.sup.- wherein R.sub.7 is C.sub.1-6 alkyl and B.sup.- is a salting ion; or CH.sub.2 NHR.sub.8, wherein R.sub.8 is SO.sub.2 R.sup.1.sub.9, COR.sup.1.sub.9 or CZNHR.sub.9 and R.sup.1.sub.9 is as hereinbefore defined, R.sub.
Abstract: The compound of the formula (I): ##STR1## and pharmaceutically acceptable salts and esters thereof, are useful for their .beta.-lactamase inhibitory activity and synergized penicillins and cephalosporins in the treatment of bacterial infections.
Abstract: Compounds of formula (II): ##STR1## Z represents a divalent radical derived from a C.sub.1-20 alkane, C.sub.3-8 cycloalkane, C.sub.2-20 alkene, arene, aralkane, cycloalkylalkane, heterocycle, or heterocylylalkane; and R.sup.x and R.sup.y are the same or different and each represent (a) hydrogen, or (b) C.sub.1-20 alkyl, C.sub.2-8 alkenyl, either of which may be optionally substituted with C.sub.3-7 cycloalkyl, halogen, carboxy, C.sub.1-6 alkoxycarbonyl, carbamyl, aryl, heterocyclyl, hydroxy, C.sub.1-6 alkanoyloxy, amino, mono- or di-(C.sub.1-6) alkylamino; or (c) C.sub.3-7 cycloalkyl optionally substituted with C.sub.1-6 alkyl; or (d) aryl; or (e) heterocyclyl; or (f) R.sup.x and R.sup.y together with the nitrogen atom to which they are attached represent a C.sub.5-7 heterocyclic ring, are useful as antibacterial and antimycoplasma agents.
Abstract: Compounds which are clinically important cephalosporins and salts and esters thereof having a wide spectrum of activity against Gram-positive bacteria but especially against Gram-negative bacteria such as Pseudomonas spp. against which commercially available cephalosporins are normally inactive. Preferred compounds of the invention are also active against Gram-negative cephalosporinase-producing organisms such as Enterobacter spp., Serratia spp. and indole-positive Proteus; methods of preparation are described.
Abstract: Compounds of the formula (I): ##STR1## wherein: Y is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --C.dbd.C--n is 1 to 5;R.sub.1 is hydrogen, or CO.sub.2 R.sub.1 represents an ester group in which the R.sub.1 moiety contains from 1 to 12 carbon atoms;R.sub.2 is hydrogen, C.sub.1-4 alkyl, trifluoromethyl, or phenyl;R.sub.3 is hydroxy or protected hydroxy;R.sub.5 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-6 alkyl, any of which phenyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or nitro groups; andX is CH.sub.2 andR.sub.4 is C.sub.1-9 alkyl, C.sub.3-8 cycloalkyl--C.sub.1-6 alkyl, phenyl--C.sub.1-6 alkyl or naphthyl--C.sub.1-6 alkyl, any of which groups may have one acyclic carbon-carbon bond interrupted by an oxygen atom; hydrogen, C.sub.3-8 cycloalky, phenyl or naphthyl, any of which phenyl of naphthyl moieties in R.sub.4 may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkoxy or nitro groups; or R.
Abstract: A ketone of formula (II): ##STR1## wherein Y represents ##STR2## and R represents a C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, aryl, aralkyl or cycloalkylalkyl group, optionally substituted with halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, carboxy or C.sub.1-6 alkoxy carbonyl, or represents a 5 or 6 membered heterocyclic group containing a nitrogen, oxygen or sulphur atom, has antibacterial and antimycloplasmal activity and is of value in the treatment of bacterial and mycoplasma-induced human and veterinary diseases.
Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable ester, amide or salt thereof wherein R.sub.1 is a hydrogen, fluorine, chlorine or bromine atom or a hydroxyl, hydroxymethyl, methyl, methoxyl, amino, formamido, acetamido, methylsulphonylamido, nitro, benzyloxy, methylsulphonylmethyl, ureido, trifluoromethyl or p-methoxybenzylamino group; R.sub.2 is a hydrogen, fluorine, chlorine or bromine atom or a hydroxyl group; R.sub.3 is a hydrogen, chlorine or bromine atom or a hydroxyl group; R.sub.4 is a hydrogen, chlorine or fluorine atom or a methyl, methoxyl or hydroxyl group or a carboxylic acid group or a salt, ester or amide thereof; R.sub.5 is a hydrogen atom or a methyl group; R.sub.6 is a hydrogen atom or a methyl group; R.sub.7 is a hydrogen atom or a methyl or ethyl group; R.sub.
Abstract: Effervescent analgesic powders which comprise paracetamol D.C., and metoclopramide or an acid addition salt thereof, the weight ratio of paracetamol D.C. to metoclopramide or the acid addition salt thereof lying in the range 50:1 to 250:1, and a process for their preparation.
Abstract: A device for oral administration to a ruminant animal includes a veterinary medicament, such as an anthelmintic, uniformly dispersed throughout an erodable sheet comprising an ethylene-vinylacetate copolymer. The sheet is rolled up and stuck together with adhesive backed paper strips for administration, and unrolls in the rumen to take up a planar configuration which is retained in the rumen. The sheet may be placed within a plastics netting envelope to give more controlled erosion and release of medicament.
Type:
Grant
Filed:
December 9, 1980
Date of Patent:
December 29, 1981
Assignee:
Beecham Group Limited
Inventors:
Gerald J. L. Griffin, Malcolm D. Brewer
Abstract: A penicillin of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R is C.sub.1-6 alkyl; an optionally substituted 5-membered heterocyclic ring containing one or two heteroatoms selected from oxygen, sulphur and nitrogen; phenyl; mono-substituted phenyl where the substituent is halogen, hydroxy, C.sub.1-6 alkoxy, nitro, amino, C.sub.1-6 alkyl, or C.sub.1-6 haloalkyl, C.sub.1-6 alkylcarbonyloxy, or C.sub.1-6 alkyl sulphonylamino; or di-substituted phenyl where the substituents are selected from hydroxy, halogen, methoxy, acetoxy and amino; and X represents a group of formula: ##STR2## wherein R.sup.1 represents C.sub.1 to C.sub.6 alkyl, or C.sub.1 to C.sub.6 alkoxy.Their preparation and use is described.
Abstract: A compound of the general formula (III), having anorexic activity: ##STR1## or a salt thereof, wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be the same or different and are each a hydrogen or halogen atom, or a trifluoromethyl, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, hydroxyl, carboxyl, C.sub.1 to C.sub.4 alkoxycarbonyl, amino or acetamido group; R.sub.6 is a hydrogen atom or a C.sub.1 to C.sub.4 alkyl group; X is a straight or branched alkylene group of up to 4 carbon atoms; and R.sub.7 and R.sub.8 which may be the same or different are each a hydrogen atom or a C.sub.1 to C.sub.4 alkyl group, or R.sub.7 is joined to R.sub.8 so that NR.sub.7 R.sub.8 forms a 5-7 membered heterocyclic ring.
Abstract: Sodium amoxycillin is obtained by spray drying a solution of sodium amoxycillin in aqueous isopropyl alcohol, wherein the initial ratio of isopropyl alcohol to sodium amoxycillin present in the solution to be spray dried is from 5:3 to 3:1 w/w.