Patents Assigned to Beecham Group
  • Patent number: 4285932
    Abstract: A pharmaceutical composition which comprises a pharmaceutically acceptable carrier together with an in vivo fibrinolytic enzyme as defined herein wherein the catalytic site essential for fibrinolytic activity is blocked by a group which is removable by hydrolysis at a rate such that the pseudo-first order rate constant for hydrolysis is in the range 10.sup.-6 sec.sup.-1 to 10.sup.-3 sec.sup.-1 in isotonic aqueous media at pH 7.4 at 37.degree. C.; is useful in the treatment of venous thrombosis.
    Type: Grant
    Filed: August 20, 1979
    Date of Patent: August 25, 1981
    Assignee: Beecham Group Limited
    Inventor: Richard A. G. Smith
  • Patent number: 4285960
    Abstract: A class of substituted aminoalkyl esters of methicillin have good oral absorption properties.
    Type: Grant
    Filed: September 14, 1978
    Date of Patent: August 25, 1981
    Assignee: Beecham Group Limited
    Inventor: Harry Ferres
  • Patent number: 4284570
    Abstract: This invention relates to antibacterial compounds and in particular to a class of esters which have antibacterial activity against certain Gram-positive and Gram-negative organisms, and also possess antimycoplasmal activity. The compounds are therefore of value in the treatment of human and veterinary infections.
    Type: Grant
    Filed: October 18, 1979
    Date of Patent: August 18, 1981
    Assignee: Beecham Group Limited
    Inventors: Norman H. Rogers, Peter J. O'Hanlon
  • Patent number: 4283412
    Abstract: Esters of an acid of formula: ##STR1## which is termed "monic acid" have activity against Gram-positive and Gram-negative organisms.
    Type: Grant
    Filed: June 11, 1979
    Date of Patent: August 11, 1981
    Assignee: Beecham Group Limited
    Inventors: Kong Luk, John P. Clayton, Norman H. Rogers
  • Patent number: 4283411
    Abstract: Esters of an acid of formula: ##STR1## which is termed "monic acid" have activity against Gram-positive and Gram-negative organisms.
    Type: Grant
    Filed: June 11, 1979
    Date of Patent: August 11, 1981
    Assignee: Beecham Group Limited
    Inventors: Kong Luk, John P. Clayton, Norman H. Rogers
  • Patent number: 4282373
    Abstract: Compounds of the formula (II): ##STR1## wherein X is halogen, hydroxyl or functionalized hydroxyl; Y is halogen, hydroxyl or alkoxy; R.sup.1 is a carboxylic acid group and ester thereof and amide derivative thereof or cyano; and R.sup.2 is hydrogen, a hydrocarbon, a heterocycle, a carboxylic acid group, a carboxylic acid ester, a carboxylic acid amide derivative, acyl, cyano, isocyano or an optionally substituted imine of the formula --CH.dbd.NZ or --N.dbd.CH.sub.2 wherein Z is hydrogen, alkyl, aryl, sulphonyl, --SR.sup.a, sulphoxide --SR.sup.a, or sulphonate --SR.sup.a wherein R.sup.a is alkyl of 1 to 6 carbon atoms or aryl, are useful as intermediates for the ultimate production of penicillins or cephalosporins.
    Type: Grant
    Filed: May 7, 1979
    Date of Patent: August 4, 1981
    Assignee: Beecham Group Limited
    Inventors: Angela W. Guest, Andrew W. Taylor, Robert Ramage
  • Patent number: 4282356
    Abstract: A compound, with hypoglycaemic activity, having formula (II) or a pharmaceutically acceptable quaternary ammonium or acid addition salt thereof: ##STR1## wherein X represents oxygen or sulphur;n represents zero or 1;R.sup.7 represents hydrogen or C.sub.1-6 alkyl;R.sup.1 and R.sup.2 are the same or different and represent hydrogen, C.sub.1-6 alkyl, phenyl, benzyl, or C.sub.3-6 cycloalkyl;R.sup.3 represents hydrogen, C.sub.1-6 alkyl, phenyl or benzyl;R.sup.4 represents hydrogen or C.sub.1-6 alkyl;R.sup.5 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or R.sup.4 and R.sup.5 together represent the remaining members of a 5- or 6-membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C.sub.1-6 alkyl, carboxy or C.sub.1-6 alkoxycarbonyl; andR.sup.
    Type: Grant
    Filed: June 10, 1980
    Date of Patent: August 4, 1981
    Assignee: Beecham Group Limited
    Inventor: Barrie C. C. Cantello
  • Patent number: 4282236
    Abstract: The compounds of the formula (II): ##STR1## and salts and cleavable esters thereof wherein R.sub.1 is a hydrogen atom or a lower alkyl group and R.sub.2 is a CN or CO.sub.2 R.sub.3 group where R.sub.3 is a hydrogen atom or a lower alkyl, aryl, or aralkyl group are antibacterially effective compounds. Their preparation and use is described.R. B. Woodward (Acta Pharm. Suecica 1977, 14 Suppl., p 23-25) disclosed that the compounds of the formula (I): ##STR2## where R was an unspecified group possessed antibacterial activity. No aid in determining the nature of the group R was given by Professor Woodward nor did he describe the preparation of any compounds of the formula (I). However, at the symposium on Current Topics in Drug Research (Uppsala, Sweden October 1977) Professor Woodward described the compound of the formula (I) wherein R is a hydrogen atom. We have prepared this compound and found it to possess a somewhat disappointing degree of antibactrial activity.
    Type: Grant
    Filed: November 7, 1979
    Date of Patent: August 4, 1981
    Assignee: Beecham Group Limited
    Inventor: Nigel J. P. Broom
  • Patent number: 4282202
    Abstract: The stability of an oily intramammary formulation containing a suspension of a solid clavulanic acid salt is improved by incorporation therein of molecular sieve powder.
    Type: Grant
    Filed: October 29, 1979
    Date of Patent: August 4, 1981
    Assignee: Beecham Group Limited
    Inventor: John S. Dowrick
  • Patent number: 4278686
    Abstract: The present invention provides antibiotic compounds of the formula: ##STR1## and salts and cleavable esters thereof wherein X is a SCH.sub.2 CH.sub.2 NH.sub.2 or YNH-COCH.sub.3 group where Y is a SCH.sub.2 CH.sub.2, trans --SO--CH.dbd.-- or cis or trans --S--CH.dbd.CH-- group and R is a lower alkyl, aryl, aralkyl, lower alkenyl, or substituted lower alkyl.
    Type: Grant
    Filed: April 27, 1979
    Date of Patent: July 14, 1981
    Assignee: Beecham Group Limited
    Inventors: David F. Corbett, Alfred J. Eglington
  • Patent number: 4275067
    Abstract: Compounds of the formula (II): ##STR1## wherein X is S, SO or SO.sub.2 ; and R is (a) an alkyl group of up to 4 carbon atoms, (b) an alkyl group of up to 4 carbon atoms substituted by an OR.sup.1, NHR.sup.1, NH.CO.R.sup.1 or CO.sub.2 R.sup.2 group wherein R.sup.1 is a hydrogen atoms, an alkyl group of up to 4 carbon atoms or benzyl group, and R.sup.2 is a moiety such that CO.sub.2 R.sup.2 is a carboxyl, salted carboxyl or esterified carboxyl group, (c) an aryl group or (d) an aralkyl group are useful for their anti-fungal and .beta.-lactamase inhibitory properties.
    Type: Grant
    Filed: August 10, 1978
    Date of Patent: June 23, 1981
    Assignee: Beecham Group Limited
    Inventor: Eric Hunt
  • Patent number: 4273778
    Abstract: This invention relates to novel substituted benzamides having useful pharmacological properties, to pharmaceutical compositions containing them, and to a process for their preparation.N-(2-Diethylaminoethyl)-2-methoxy-4-amino-5-chlorobenzamide, 1-ethyl-2(2-methoxy-5-sulphamoylbenzamidomethyl)pyrrolidine and N-[4'-(1"-benzyl)-piperidyl]-2-methoxy-4-amino-5-chlorobenzamide are well known compounds having useful pharmacological activity such as the ability to regulate the gastro-intestinal function anti-emetic activity and CNS activity.It has now been found that a certain structurally distinct class of substituted benzamides also has useful pharmacological activity, in particular dopamine antagonist activity.
    Type: Grant
    Filed: December 26, 1979
    Date of Patent: June 16, 1981
    Assignee: Beecham Group, Limited
    Inventors: Michael S. Hadley, Francis D. King
  • Patent number: 4272542
    Abstract: In-vivo hydrolysable esters of certain .alpha.-amino penicillins and cephalosporins have been rendered relatively tasteless by formulating into reconstitutable powders with a disodium or dipotassium salt of a di-carboxylic amino acid or tri- or di-sodium or -potassium phosphate, tartrate or citrate.
    Type: Grant
    Filed: July 27, 1976
    Date of Patent: June 9, 1981
    Assignee: Beecham Group Limited
    Inventor: Charles B. Taskis
  • Patent number: 4272445
    Abstract: A process for the preparation of a compound of the formula (A): ##STR1## wherein: R.sub.3 is a C.sub.1-5 alkyl group, a C.sub.3-6 alkenyl group, a C.sub.3-6 cycloalkyl group or an alkylphenyl group in which the alkyl moiety contains 1 to 3 carbon atoms and the phenyl moiety is optionally substituted; R.sub.4 is a hydroxyl group, or a group OR.sub.6 wherein R.sub.6 is a C.sub.2-7 acyl group, a C.sub.1-4 alkyl group, or an optionally substituted benzyl group; R.sub.5 is hydrogen or a C.sub.1-5 alkyl group; or R.sub.4 and R.sub.5 together with the carbon atom to which they are joined represent a carbonyl group; which process comprises the reaction of a compound of the formula (C): ##STR2## wherein Q is a carbonyl group protected by a reagent capable of selectively protecting the 3-carbonyl of androstenedione, and R.sub.3, R.sub.4 and R.sub.5 are as defined in formula (A), to generate an unprotected carbonyl group in place of the protected carbonyl group Q.
    Type: Grant
    Filed: May 19, 1978
    Date of Patent: June 9, 1981
    Assignee: Beecham Group Limited
    Inventors: Paul Smith, Frederick Cassidy
  • Patent number: 4271188
    Abstract: Compounds having hypolipidaemic activity which are substituted aralkylanilines, their preparation and pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 17, 1979
    Date of Patent: June 2, 1981
    Assignee: Beecham Group Limited
    Inventor: Richard M. Hindley
  • Patent number: 4270004
    Abstract: The present invention relates to a process for the preparation of 4-(6.sup.1 -methoxy-2.sup.1 -naphthyl)butan-2-one and to certain compounds for use in that process.British patent specification No. 1,474,377 discloses inter alia that 4-(6.sup.1 -methoxy-2.sup.1 -naphthyl)butan-2-one possesses useful anti-inflammatory activity. A particularly favored process has now been discovered that can be used to produce 4-(6.sup.1 -methoxy-2.sup.1 -naphthyl)butan-2-one in particularly good yield.The present invention provides a process for the preparation of 4-(6.sup.1 -methoxy-2.sup.1 -naphthyl)butan-2-one which process comprises the hydrogenation of a compound of the formula (I): ##STR1## wherein Ar is a 6-methoxy-2-naphthyl group; X and Y are each hydrogen atoms or together represent a second bond between the carbon atoms to which they are attached; and R is a group such that --CO.sub.2 R represents an ester group convertible by hydrogenation to a CO.sub.2 H group.
    Type: Grant
    Filed: October 11, 1979
    Date of Patent: May 26, 1981
    Assignee: Beecham Group Limited
    Inventors: Carl J. Rose, David Miller
  • Patent number: 4268497
    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: November 7, 1979
    Date of Patent: May 19, 1981
    Assignee: Beecham Group Limited
    Inventors: Gerald J. L. Griffin, Malcolm D. Brewer
  • Patent number: 4267273
    Abstract: An enzyme preparation is prepared having terminal non-polar groups incorporated therein so that the enzyme preparation has affinity for a water-immiscible liquid. The enzyme preparation can be separated from an aqueous reaction mixture by contacting the mixture with the water-immiscible liquid, permitting the enzyme preparation to become associated with the water-immiscible liquid and separating the water-immiscible liquid containing the associated enzyme from the reaction mixture.
    Type: Grant
    Filed: April 12, 1979
    Date of Patent: May 12, 1981
    Assignee: Beecham Group Limited
    Inventor: Richard A. G. Smith
  • Patent number: 4267177
    Abstract: The compounds of the formula (II): ##STR1## and salts and esters thereof wherein R.sub.1 is a pyridyl group optionally substituted by one of two lower alkyl groups or lower acyloxy group, have been found to be antibacterial-agents. Their preparation and use is described.
    Type: Grant
    Filed: August 23, 1979
    Date of Patent: May 12, 1981
    Assignee: Beecham Group Limited
    Inventor: Andrew J. G. Baxter
  • Patent number: 4267175
    Abstract: A compound of the formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein: R.sub.1 is a C.sub.1-6 alkoxy group;R.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, CF.sub.3, hydroxy, C.sub.1-6 alkoxy, C.sub.2-7 acyl, amino, amino substituted by one or two C.sub.1-6 alkyl groups, C.sub.2-10 acyl amino, aminosulphone, aminosulphone substituted by one or two C.sub.1-6 alkyl groups, C.sub.1-6 alkyl sulphone or nitro groups; andA is a C.sub.2-4 alkylene group;R.sub.5 and R.sub.6 are joined so that they form with the --N--A--N-- group to which they are attached, a 6, 7 or 8 membered heterocyclic ring;R.sub.7 is a C.sub.1-6 alkyl group, or an aryl --C.sub.1-6 akyl group in which the alkyl moiety is optionally substituted by a C.sub.1-6 alkyl or aryl group; have useful pharmacological activity, such as the ability to regulate the gastrointestinal function and to treat emesis.
    Type: Grant
    Filed: March 8, 1979
    Date of Patent: May 12, 1981
    Assignee: Beecham Group Limited
    Inventor: Eric A. Watts