Abstract: Compounds are provided of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group and A.sub.1 is a hydrogen atom or a methyl group. These compounds possess antibacterial activity. The preparation of these compounds is described.
Type:
Grant
Filed:
October 19, 1981
Date of Patent:
August 30, 1983
Assignee:
Beecham Group Limited
Inventors:
Andrew J. G. Baxter, Patricia M. Roberts, Robert Southgate
Abstract: Compounds having the formula: ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, Y and X are as defined hereinbelow, are useful for the reduction of abnormally high blood glucose and lipid levels in the treatment of obesity or hyperglycaemia.
Abstract: Compounds of the formula (I): ##STR1## and pharmaceutically acceptable salts and pro-drugs thereof, wherein: Ar is a phenyl group optionally substituted by one or two moieties selected from halogen, C.sub.1-4 alkyl, methoxy, methylthio or trifluoromethyl, or a 2-thienyl group or N-methyl-2-pyrryl group optionally substituted by one or two C.sub.1-4 alkyl groups;R is hydrogen or methyl; andn is 0 or 1having useful anti-inflammatory and/or analgesic activity, pharmaceutical compositions containing them, and processes for their preparation.
Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R is phenyl, 4-hydroxyphenyl, or a 5- or 6-membered heterocyclic ring containing up to three heteroatoms selected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen or C.sub.1-6 alkoxy;R.sup.1 represents hydrogen or C.sub.1-6 alkyl;R.sup.2 and R.sup.3 are the same or different and represent hydrogen, C.sub.1-6 alkyl, halogen, amino, hydroxy, or C.sub.1-6 alkoxy;X represents oxygen or sulphur; andA represents hydrogen, pyridyl, acetoxy, carbamoyloxy or a heterocyclicthio group;Their preparation and use is described.
Type:
Grant
Filed:
June 5, 1981
Date of Patent:
July 19, 1983
Assignee:
Beecham Group Limited
Inventors:
Peter H. Bentley, Kenneth D. Hardy, Peter H. Milner
Abstract: Anti-inflammatory compositions are prepared which comprise a therapeutically effective amount of a compound of the formula ##STR1## wherein X is CO or CHOH; Y is CO; the dotted line represents a double bond which is present or absent; R.sub.1 is hydrogen or methyl; R.sub.2 is hydrogen, fluorine, chlorine, bromine, methyl, trifluoromethyl, methoxyl, hydroxyl, acetoxyl, nitro or amino; R.sub.3 is alkyl of 3 to 8 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, alkenyl of 3 to 8 carbon atoms, cycloalkenyl of 5 to 8 carbon atoms or phenyl unsubstituted or substituted by 1 or 2 substituents selected from the group consisting of fluorine, chlorine, bromine, methyl, ethyl, methoxyl, ethoxyl, benzyloyl, hydroxyl, acetoxyl, trifluoromethyl, nitro, amino, acetyl, methylthiol, methylsulphonyl, methylamino and dimethylamino. Compounds of formula I above are also novel.
Type:
Grant
Filed:
December 15, 1976
Date of Patent:
July 12, 1983
Assignee:
Beecham Group Limited
Inventors:
William G. Cole, Alexander C. Goudie, Carl J. Rose
Abstract: 2,2-Dimethyl-3,4-dihydro-2H-benzo[b]pyran-3-ols bearing an amino group in the 4-position and a cyano group in the benzo ring, their salts, esters and ethers, demonstrate excellent vasodilatory activity. The compounds, of which trans-2,2-dimethyl-4-isopropylamino-6-cyano-3,4-dihydro-2H-benzo[b]pyran-3 -ol is a representative embodiment, can be prepared from the corresponding 3,4-epoxy derivative upon treatment with an amine.
Abstract: Compounds of formula (I) in the 1-form ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each is selected from hydrogen, optionally substituted (C.sub.1-7) alkyl, optionally substituted aryl and aromatic heterocyclyl and the dotted line is an optional direct bond, and acid addition salts thereof, are useful in treating worm infections in mammals. Compounds (I) are produced by forming the amide of m-aminotetramisole or by closing the dihydroimidazoline ring.
Abstract: Compounds of formula (II): ##STR1## wherein R is C.sub.1-20 alkyl; C.sub.3-8 cycloalkyl; C.sub.3-20 alkenyl; aralkyl; cycloalkylalkyl; heterocyclyl or heterocyclylalkyl; each being substituted with formyl; ##STR2## have activity against human and veterinary bacteria and mycoplasma. They may be produced by conventional methods and are used in conventional formulations.
Abstract: The compounds of the formula (II): ##STR1## wherein R.sub.3 and R.sub.4 are as defined in relation to formula (I) and R.sub.7 is a nitro, cyano, amino or aminomethyl group, are antibacterial agents and .beta.-lactamase inhibitors. Their use and a process for their preparation are described.
Abstract: The present invention provides the compounds of the formula (II): ##STR1## and pharmaceutically acceptable salts and esters thereof wherein R.sup.3 is a hydrogen atom, a group HO.sub.3 S-- or a group R.sup.5 CO wherein R.sup.5 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, aryl, aryl(C.sub.1-6)alkyl or aryloxy(C.sub.1-6)alkyl; and R.sup.4 is an organic group other than methyl bonded to the --CO--NH-- moiety via a carbon atom; with the proviso that when R.sup.3 is a hydrogen atom or a group R.sup.5 CO the stereochemical configuration at the .alpha.-carbon atom of the C-6 substituent is S, and with the further proviso that when R.sup.3 is a group HO.sub.3 S-- the hydrogen atoms at C-5 and C-6 are cis. Their use is described as are processes for their preparation. Compounds wherein the R.sup.4 CO-- moiety is replaced by a hydrogen atom are also prepared.
Type:
Grant
Filed:
October 28, 1980
Date of Patent:
June 7, 1983
Assignee:
Beecham Group Limited
Inventors:
David F. Corbett, Robert Southgate, Alfred J. Eglington
Abstract: The present invention provides a process for the preparation of a compound of the formula (O): ##STR1## wherein R.degree. is SCH.sub.2 CH.sub.2 NH.sub.2 which process comprises the reaction of a cleavable ester of a compound of the formula (O) wherein R.degree. is H with an optionally protected compound XCH.sub.2 CH.sub.2 NH.sub.2 wherein X is a displaceable group.
Abstract: A compound of formula (I): ##STR1## wherein: R is C.sub.1-4 alkyl;R.sub.1 is hydrogen or C.sub.1-4 alkyl;one of A and B is sulphur, and the other of A and B is carbon doubly bound to the carbon spacing A and B; andthe dotted line represents an optionally present double bond;and pro-drugs thereof; and pharmaceutically acceptable salts thereof;have useful anti-inflammatory and analgesic activity.
Type:
Grant
Filed:
March 5, 1981
Date of Patent:
May 24, 1983
Assignee:
Beecham Group Limited
Inventors:
Alexander C. Goudie, Robert W. Ward, Howard E. Rosenberg
Abstract: 6.beta.-[2-(2'-methylphenoxycarbonyl)-2-thien-3'-ylacetamido] penicillanic acid of formula (II): ##STR1## and pharmaceutically acceptable salts and in vivo hydrolyzable esters thereof, are active against Gram-positive and Gram-negative bacteria which makes them useful as therapeutic and prophylactic agents against bacterial infections in animals, including man and poultry. A process for the preparation and pharamceutical compositions comprising the penicillin, are also described.
Abstract: Compounds of formula (II): ##STR1## or a pharmaceutically acceptable salt, lower alkyl or aralkyl ester or amide thereof, wherein R.sup.1 and R.sup.2, which may be the same or different, are each of a hydrogen atom or a methyl group, n is 1, 2 or 3, and Z is a C.sub.1-6 alkyl or C.sub.1-6 alkoxy group, or a halogen or hydrogen atom are useful in treating obesity and/or hyperglycaemia and/or inflammation in mammals.
Abstract: The compound of formula (I): ##STR1## wherein X is CFCl; and C.sub.1-6 alkanoyl esters and/or phosphate esters thereof, is active against herpes viruses.
Type:
Grant
Filed:
September 21, 1981
Date of Patent:
May 17, 1983
Assignee:
Beecham Group Limited
Inventors:
Paul L. Coe, Albert S. Jones, Stewart A. Noble, Richard T. Walker
Abstract: 4-(6-Methoxy-2-naphthyl)-3-hydroxybutan-2-one and 4-(6-methoxy-2-naphthyl)buta-2,3-diol have good degrees of anti-inflammatory and analgesic activity coupled with an advantageous therapeutic ratio based on gastric irritancy and are non-oestrogenic. Their preparation and use are described.
Abstract: A compound of formula (I): ##STR1## or a salt thereof; wherein R.sup.1 is hydrogen, methyl or ethyl; R.sup.2 is hydrogen, methyl or ethyl; R.sup.3 is hydrogen, fluorine, chlorine, bromine or trifluoromethyl; each of R.sup.4 and R.sup.5 is hydrogen, fluorine, chlorine, bromine, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; n is 1 or 2; and X is C.sub.1-12 straight or branched alkylene, and salts thereof, are anti-obesity, hypoglycaemic, anti-inflammatory and platelet aggregation inhibiting agents.
Abstract: The compounds of the formula (II): ##STR1## and salts and esters theereof wherein R.sub.1 is an inert organic group of up to 14 carbon atoms and R.sub.2 is an inert organic group of up to 16 carbon atoms, the group NR.sub.1 R.sub.2 containing up to 22 carbon atoms, are antibacterial agents able to enhance the effectiveness of penicillins and cephalosporins against certain .beta.-lactamase producing bacteria.
Abstract: A compound of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: Ar is phenyl, optionally substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, cyano, nitro, hydroxy, CONH.sub.2, CO.sub.2 W wherein W is C.sub.1-6 alkyl or C.sub.1-4 alkylphenyl which phenyl may be substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or halogen, NR.sub.1 R.sub.2 wherein R.sub.1 and R.sub.2 are selected from hydrogen or C.sub.1-6 alkyl, NHCO C.sub.1-6 alkyl or C.sub.1-6 alkylcarbonyloxy; phenyl disubstituted on adjacent carbon atoms by methylenedioxy; furyl or thienyl;the dotted lines represent an optionally present double bond; andX is CO or CR.sub.1 OH wherein R.sub.1 is hydrogen or C.sub.1-4 alkyl, having useful pharmacological activity, processes for their preparation and their use.
Abstract: Analgesic tablets which comprise an analgesic Medicament and metoclopramide or an acid addition salt thereof, the weight ratio of analgesic to metoclopramide or acid addition salt thereof lying in the range of 50:1 to 250:1, and a process for their preparation.