Patents Assigned to Beecham Group
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Patent number: 4859709Abstract: A pharmaceutical composition comprising a freely flowable powder, the powder comprising a porous, high absorption silica or silicate having absorbed therein at least 10% by volume of a liquid, pharmaceutically active composition, based on the weight of powder plus liquid, provided that when the liquid pharmaceutically active composition is a corticoid solution the silica or silicate has a mean particle size of at least 10 .mu.m in diameter.Type: GrantFiled: October 26, 1987Date of Patent: August 22, 1989Assignee: Beecham Group plcInventor: David A. Rawlins
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Patent number: 4857647Abstract: A compound of formula (XXII): ##STR1## or a compound of formula (XXIII): ##STR2## wherein in formula (XXIII), J.sup.1 -1 is 1 to 4; and Q.sub.6 and Q.sub.7 are on the same carbon atom; and wherein, in formulae (XXII) and (XXIII), Q.sub.6 is NH.sub.2 and Q.sub.7 is H and p is 0 to 2; q is 0 to 3; and one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-3 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3 or halogen; and the other of R.sub.5 and R.sub.6 is hydrogen or C.sub.1-6 alkyl.Type: GrantFiled: June 4, 1987Date of Patent: August 15, 1989Assignee: Beecham Group p.l.c.Inventor: Francis D. King
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Patent number: 4853394Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof:Ar--CO--X--Y--Z--OR.sub.1 (I)wherein: Ar is a group of formula (a): ##STR1## wherein either R.sub.2 is C.sub.1-6 alkoxy and one of R.sub.3, R.sub.4 and R.sub.5 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, CX.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-6 alkoxy, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O)n wherein n is 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF.sub.3, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or R.sub.2 is hydrogen and R.sub.3, R.sub.4 and R.sub.5 are independently selected from hydrogen, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio or halo; or any two on adjacent carbon atoms together are C.sub.Type: GrantFiled: November 3, 1986Date of Patent: August 1, 1989Assignee: Beecham Group p.l.c.Inventors: Francis D. King, Roger T. Martin, Eric A. Watts
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Patent number: 4853376Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: X is NH; or O when Ar is of formula (a) and R.sub.2 is hydrogen or when Ar is a group of formula (b);R.sub.1 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-6 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;Ar is a group of formula (a): ##STR2## wherein R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are optional substituents; or Ar is a group of formula (b): ##STR3## wherein Z is CH.sub.2, O, S or NR.sub.7 wherein R.sub.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 alkenyl-methyl, phenyl or phenyl C.sub.1-4 alkyl either of which phenyl moieties may be substituted by one or two of halogen, CF.sub.3, C.sub.1-6 alkoxy or C.sub.1-6 alkyl; and Y is CH or N; or Z is CH or N and Y is NR.sub.a or CHR.sub.a where R.sub.a is as defined for R.sub.7 above;R.sub.b is present when the COX linkage is attached at the phenyl ring, and is selected from hydrogen, halogen, CF.sub.3, hydroxy, C.sub.Type: GrantFiled: October 17, 1986Date of Patent: August 1, 1989Assignee: Beecham Group, p.l.c.Inventor: Francis D. King
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Patent number: 4851407Abstract: A method of treatment of emesis, anxiety and/or IBS in mammals, including humans, which method comprises administering an effective amount of a compound of formula (I) or (II) or a pharmaceutically acceptable salt thereof:Ar--CO--Y--Z (I)wherein Ar is a group of formula (a): ##STR1## wherein: R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-4 alkoxy, hydroxy, amino optionally substituted by one or two C.sub.1-4 alkyl groups, thiol, C.sub.1-4 alkylthio; X is CH.sub.2, NR.sub.3, --O-- or --S-- wherein R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.3-5 alkenyl, phenyl or phenyl C.sub.1-4 alkyl; or Ar is a group of formula (b): ##STR2## wherein R.sub.4 to R.sub.7 are independently hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, amino optionally substituted by one or two C.sub.1-4 alkyl, by C.sub.1-4 alkanoylamino or pyrrolyl, one of R.sub.4 to R.sub.Type: GrantFiled: September 16, 1988Date of Patent: July 25, 1989Assignee: Beecham Group, p.l.c.Inventors: Gordon Wootton, Gareth J. Sanger
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Patent number: 4847280Abstract: A method for the treatment and/or prophylaxis of hyperglycaemia in human or non-human mammals which comprises administering to the mammal in need of such treatment and/or prophylaxis an effective non-toxic amount of:a compound of formula (I): ##STR1## or a pharmaceutically acceptable acid addition salt thereof, or a compound of formula (II): ##STR2## or a pharmaceutically acceptable acid addition salt thereof, and compositions for use in such method.Type: GrantFiled: May 23, 1986Date of Patent: July 11, 1989Assignee: Beecham Group plcInventor: Michael A. Cawthorne
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Patent number: 4847242Abstract: 11-ether derivatives of erythromycin, and corresponding 9-(optionally substituted)-amino, 9-imino, and 9-(optionally substituted)-oxime derivatives are novel antibacterially active compounds, and can be prepared by alkylation of the 11-hydroxy group under mild conditions.Type: GrantFiled: March 10, 1986Date of Patent: July 11, 1989Assignee: Beecham Group p.l.c.Inventor: John S. Davies
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Patent number: 4845092Abstract: A method of treatment of visceral pain in mammals, including humans, which method comprises the administration to the mammal in need of such treatment, an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof:X-CO-Y-Z (I)whereinX is a group of formula (a), (b), (c), (d) or (e): ##STR1## wherein R.sub.a to R.sub.d are selected from hydrogen, halogen or hydroxy;R.sub.1 is hydrogen and R.sub.2 is hydrogen or C.sub.1-4 alkyl; orR.sub.1 and R.sub.2 together are a bond;R.sub.3 and R.sub.7 are independently hydrogen or C.sub.1-6 alkyl; andR.sub.4 together with R.sub.2 may be C.sub.2-7 polymethylene when R.sub.1 is hydrogen;either R.sub.8 is C.sub.1-6 alkoxy;R.sub.9 is hydrogen;R.sub.10 is amino or C.sub.1-7 alkanoylamino; andR.sub.11 is halo or C.sub.1-6 alkylthio; orR.sub.8 is hydrogen;R.sub.9 is halo, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;R.sub.10 is hydrogen or C.sub.1-6 alkoxy; andR.sub.11 is halo, C.sub.1-6 alkoxy or C.sub.Type: GrantFiled: January 19, 1988Date of Patent: July 4, 1989Assignee: Beecham Group plcInventors: Gareth J. Sanger, Helen E. Marr
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Patent number: 4842164Abstract: A nozzle insert for a nozzle of a striped paste dispenser has a hollow cylindrical body through which a first pasty material may be dispensed, the external surface of the hollow body having circumferentially spaced apart plateaus separated by grooves through which a second pasty material may be dispensed, the body preventing contact between the two pasty materials downstream of the discharge end of the insert.Type: GrantFiled: June 25, 1987Date of Patent: June 27, 1989Assignee: Beecham Group p.l.c.Inventors: Adrian F. Davis, Peter R. Watt
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Patent number: 4837238Abstract: Compounds of the formula (I): ##STR1## wherein: X is NR wherein R is hydrogen, C.sub.1-6 alkyl; oxygen; sulphur; SO; or SO.sub.2 ; or R and R.sub.3 taken together are C.sub.4-6 polymethylene;R.sub.1 is hydrogen or C.sub.1-6 alkyl; and R.sub.2 is CN, CR.sub.5 R.sub.6 Y where R.sub.5 and R.sub.6 are independently selected from hydrogen and C.sub.1-4 alkyl and Y is selected from hydrogen, OR.sub.7 or SR.sub.7 where R.sub.7 is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkanoyl, and NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkanoyl or R.sub.8 and R.sub.9 together are C.sub.4-6 polymethylene, or COR.sub.10 where R.sub.10 is C.sub.1-4 alkyl, provided that Y is other than hydrogen when R.sub.1 is hydrogen;orR.sub.2 is hydrogen C.sub.1-6 alkyl or phenyl optionally substituted by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; and R.sub.1 is CN, CR.sub.5 R.sub.6 Y or COR.sub.10 as defined for R.sub.2 above;orR.sub.1 and R.sub.Type: GrantFiled: October 21, 1987Date of Patent: June 6, 1989Assignee: Beecham Group p.l.c.Inventors: Roger E. Markwell, Ian Hughes, Robert W. Ward
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Patent number: 4835150Abstract: .beta.-Lactam antibiotics are disclosed which have the formula (IA) or pharmaceutically acceptable salts or pharmaceutically acceptable in vivo hydrolyzable esters thereof: ##STR1## wherein R.sub.1 is phenyl, 3-hydroxyphenyl, 4-hydroxyphenyl, 3-aminophenyl, 4-aminophenyl, or 3,4-dihydroxyphenyl, the hydroxy and amino groups being optionally protected, and R is C.sub.1-8 alkyl; and also the use thereof.Processes for the preparation of the compounds are disclosed together with intermediates for use therein.Type: GrantFiled: June 23, 1986Date of Patent: May 30, 1989Assignee: Beecham Group p.l.c.Inventors: Clive L. Branch, Arun C. Kaura
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Patent number: 4833136Abstract: A compound of the formula (I) or a salt or solvate thereof: ##STR1## in which: R.sub.0 is hydrogen or C.sub.1-6 alkyl; or together with R.sub.3 is C.sub.4-6 polymethylene;R.sub.1 and R.sub.2 are both hydrogen; orR.sub.1 is hydrogen, C.sub.1-6 alkyl; and R.sub.2 is CN; CR.sub.5 R.sub.6 Y where R.sub.5 and R.sub.6 are independently selected from hydrogen and C.sub.1-4 alkyl and Y is selected from hydrogen, OR.sub.7 or SR.sub.7 where R.sub.7 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkanoyl, and NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkanoyl or together are C.sub.4-6 polymethylene; or COR.sub.10 where R.sub.10 is OH or C.sub.1-4 alkyl, or COR.sub.10 is a pharmaceutically acceptable ester or amide, orR.sub.2 is hydrogen, C.sub.1-6 alkyl, or phenyl optionally substituted by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl, and R.sub.1 is CN, CR.sub.5 R.sub.6 Y or COR.sub.10 as defined for R.sub.2 above; orR.sub.1 and R.sub.Type: GrantFiled: January 29, 1987Date of Patent: May 23, 1989Assignee: Beecham Group p.l.c.Inventors: Roger E. Markwell, Robert W. Ward, Carol R. De Mello
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Patent number: 4831050Abstract: 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, 1-mercapto C.sub.2-7 alkyl, 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: October 21, 1987Date of Patent: May 16, 1989Assignee: Beecham Group p.l.c.Inventors: Frederick Cassidy, Erol A. Faruk
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Patent number: 4826839Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: j is 0 or 1;q is 0, 1 or 2;p is 0 and r is 2 or 3, orp is 1 and r is 2;X is O, S, SO or NR where R is hydrogen, C.sub.1-6 alkyl or C.sub.1-10 carboxylic acyl;Y is NH; or O when R.sub.1 is hydrogen; either R.sub.1 is C.sub.1-6 alkoxy and one of R.sub.2, R.sub.3 and R.sub.4 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O) n wherein n is 0, 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF.sub.3, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or R.sub.1 is hydrogen and R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen, C.sub.Type: GrantFiled: July 17, 1986Date of Patent: May 2, 1989Assignee: Beecham Group p.l.c.Inventors: Francis D. King, Michael S. Hadley, Roger T. Martin
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Patent number: 4826820Abstract: Antibacterially active 6-carbamate erythromycin derivatives of formula I and their pharmaceutically acceptable esters and acid addition salts; ##STR1## wherein: R.sup.1 or R.sup.2 is optionally substituted amino, or R.sup.1 or R.sup.2 +R.sup.5 is --O--C(R.sup.A)(R.sup.B)--O--, and R.sup.2 or R.sup.1 is H, or R.sup.1 +R.sup.2 is oxo, oxime, substituted oxime, or imino;R.sup.3 is carbamoyl or N-substituted carbamoyl;R.sup.4 is H or OH, and R.sup.5 is OH, or etherified hydroxy, or R.sup.4 +R.sup.5 is --O--CO--O-- or --O--C(R.sup.A) (R.sup.B)--O--;R.sup.6 is H, F or OH;R.sup.7 is H or CH.sub.3 ;R.sup.8 or R.sup.9 is H, OH, alkoxy, optionally substituted NH.sub.2, alkanoyloxy, or R.sup.C --SO.sub.2 O--, and R.sup.9 or R.sup.8 is H, or R.sup.8 +R.sup.9 is oxo or optionally substituted oxime;R.sup.A, R.sup.B are H or hydrocarbon; andR.sup.C is organic.Type: GrantFiled: August 26, 1986Date of Patent: May 2, 1989Assignee: Beecham Group p.l.c.Inventor: Edward G. Brain
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Patent number: 4820701Abstract: Antibacterial agents have the formula (I) or are pharmaceutically acceptable salts or in vivo hydrolysable esters thereof: ##STR1## wherein R.sup.3 is phenyl, substituted phenyl, cyclohexenyl, cyclohexadienyl or an optionally substituted 5- or 6-membered heterocyclic ring containing up to three hetero atoms selected from oxygen, sulphur or nitrogen, R.sup.4 is hydrogen or formamido, R.sup.5 is hydrogen, C.sub.1-6 alkyl, substituted alkyl, aryl or aralkyl, R.sup.6 and R.sup.7 are the same or different and represent hydrogen, C.sub.1-6 alkyl, substituted alkyl, halogen, amino, phenyl, substituted phenyl, hydroxyl or C.sub.1-6 alkoxy or R.sup.6 and R.sup.7 form the residue of an optionally substituted 5- or 6-membered carbocyclic ring or a 5- or 6- membered heterocyclic ring containing up to three hetero atoms selected from oxygen, sulphr or nitrogen, and X represents ##STR2## or tautomers thereof wherein R.sup.8 and R.sup.9 are the same or different and each represents hydroxy, or protected hydroxy.Type: GrantFiled: October 21, 1987Date of Patent: April 11, 1989Assignee: Beecham Group p.l.c.Inventors: Robert Southgate, Colin H. Frydrych
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Patent number: 4818754Abstract: A compound of the formula (1) or a salt or solvate thereof: ##STR1## in which: R.sub.0 is hydrogen or C.sub.1-6 alkyl;R.sub.1 and R.sub.2 are both hydrogen; orR.sub.1 is hydrogen, C.sub.1-6 alkyl; and R.sub.2 is CN; CR.sub.5 R.sub.6 Y where R.sub.5 and R.sub.6 are independently selected from hydrogen and C.sub.1-4 alkyl and Y is selected from hydrogen, OR.sub.7 or SR.sub.7 where R.sub.7 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkanoyl, and NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkanoyl or together are C.sub.4-6 polymethylene; or COR.sub.10 is OH or C.sub.1-4 alkyl, or COR.sub.10 is a pharmaceutically acceptable ester or amide; orR.sub.2 is hydrogen, C.sub.1-6 alkyl, or phenyl optionally substituted by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; and R.sub.1 is CN, CR.sub.5 R.sub.6 Y or COR.sub.10 as defined for R.sub.2 above; orR.sub.1 and R.sub.2 together form C.sub.3 -C.sub.Type: GrantFiled: April 16, 1987Date of Patent: April 4, 1989Assignee: Beecham Group p.l.c. of Beecham HouseInventors: Robert W. Ward, Roger E. Markwell, Ian Hughes
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Patent number: 4816453Abstract: Compounds of formula (i) and pharmaceutically acceptable salts thereof: ##STR1## wherein: m and n are independently 1 or 2 and p is 0, 1 or 2 such that m+n+p.gtoreq.3;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-6 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;Ar is a group of formula (a): ##STR2## wherein either R.sub.3 is hydrogen or C.sub.1-7 alkanoyl; and X is chloro, bromo, methylthio or nitro; having gastric motility enhancing activity, anti-emetic activity and/or 5-HT antagonist activity, a process for their preparation, and their use as pharmaceuticals.Type: GrantFiled: September 17, 1986Date of Patent: March 28, 1989Assignee: Beecham Group, p.l.c.Inventor: Eric A. Watts
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Patent number: 4816452Abstract: 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 hydrogen or an amino protecting group and R is substituted methyl; optionally substituted C.sub.2-12 alkyl, 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 organisms.Type: GrantFiled: July 25, 1986Date of Patent: March 28, 1989Assignee: Beecham Group P.L.C.Inventors: Michael J. Pearson, Richard L. Elliott
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Patent number: 4812470Abstract: A compound of the formula (I) ##STR1## wherein R is a group ##STR2## R.sup.1 is hydrogen, phenyl, C.sub.1-20 alkyl, C.sub.2-8 alkenyl or C.sub.2-8 alkynyl each of which may optionally be substituted; or C.sub.3-7 cycloalkyl,X is a divalent group --Y--C.dbd.C--, andY is oxygen or sulphur,have antibacterial and/or antimycoplasmal activity.Type: GrantFiled: February 25, 1983Date of Patent: March 14, 1989Assignee: Beecham Group p.l.c.Inventors: Norman H. Rogers, Peter J. O'Hanlon, Graham Walker, Michael J. Crimmin