Patents by Inventor Angus Murray MacLeod
Angus Murray MacLeod has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 6048878Abstract: A compound of formula (I), or a salt or prodrug thereof, is described, wherein G is attached at position 3 or 4 of the piperidine ring and represents halogen or C.sub.1-6 alkoxy; R1 represents C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, aryl(C.sub.1-6)alkyl or heteroaryl (C.sub.1-6)alkyl, any of which groups may be optionally substituted; processes for its preparation and its use in therapy, particularly in the treatment of migraine.Type: GrantFiled: May 13, 1998Date of Patent: April 11, 2000Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose Luis Castro Pineiro, Ian James Collins, Angus Murray MacLeod, Christopher Richard Moyes, Michael Rowley, Graham Andrew Showell
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Patent number: 5998416Abstract: A class of N-substituted piperazine, piperidine, and tetrahydropyridine derivatives, further subltitutedat the 4-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.Type: GrantFiled: October 26, 1998Date of Patent: December 7, 1999Assignee: Merck Sharp & Dohme Ltd.Inventors: Sylvie Bourrain, Angus Murray MacLeod, Graham Andrew Showell, Leslie Joseph Street
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Patent number: 5998440Abstract: A class of substituted azetidine, pyrrolidine and piperidine derivatives, linked by a fluoro-substituted alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.Type: GrantFiled: May 8, 1998Date of Patent: December 7, 1999Assignee: Merck Sharpe & Dohme Ltd.Inventors: Jose Luis Castro Pineiro, Angus Murray MacLeod, Monique Bodil Van Niel
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Patent number: 5994374Abstract: A class of 1-[3-(1H-indol-3-yl)propyl]-4-benzyl-1,2,5,6-tetrahydropyridine derivatives, substituted at the 5-position of the indole nucleus by a 1,2,4-triazol-4-yl moiety, and on the methylene linkage of the benzyl moiety by an alkyl, alkoxy, or alkoxy-alkoxy substituent, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype while possessing at least a 10-fold selective affinity for the 5HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype. They are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D.alpha. receptors is indicated, and are expected to have fewer undesirable cardiovascular and other side effects.Type: GrantFiled: May 8, 1998Date of Patent: November 30, 1999Assignee: Merck Sharp & Dohme Ltd.Inventors: Sylvie Bourrain, Angus Murray MacLeod, Joseph George Neduvelil, Graham Andrew Showell
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Patent number: 5981529Abstract: A class of 1-[3-(1H-indol-3-yl)propyl]-4-(2-phenylethyl)piperazine derivatives, substituted at the 5-position of the indole nucleus by a five-membered heteroaromatic moiety, on one or other of the ethylene carbon atoms of the phenethyl moiety by halogen, trifluoromethyl, alkyl, hydroxyalkyl or alkoxyalkyl, and optionally on the phenyl ring of the phenethyl moiety by halogen, trifluoromethyl, alkoxy or an oxazolidinone group and optionally by one or two further substituents, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D .alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D .alpha. receptor subtype relative to the 5-HT.sub.1D .beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.Type: GrantFiled: March 18, 1998Date of Patent: November 9, 1999Assignee: Merck Sharp & Dohme LimitedInventors: Raymond Baker, Mark Stuart Chambers, Sarah Christine Hobbs, Angus Murray MacLeod, Austin John Reeve, Francine Sternfeld, Leslie Joseph Street
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Patent number: 5977116Abstract: A class of N-substituted piperazine, piperidine and tetrahydropyridine derivatives, linked by a fluoro-substituted alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 4-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D recptor agonists.Type: GrantFiled: May 12, 1998Date of Patent: November 2, 1999Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose Luis Castro Pineiro, Angus Murray MacLeod, Michael Rowley, Monique Bodil Van Niel
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Patent number: 5973156Abstract: A class of substituted piperidine and tetrahydropyridine derivatives, linked through the 4-position thereof via an alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 1-position by an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl-alkyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.spsb..alpha. receptor subtype whilst processing at least a 10-fold selective affinity for the 5-HT.sub.1D.spsb..alpha. receptor subtype relative to the 5-HT.sub.1D.spsb..beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.Type: GrantFiled: May 13, 1998Date of Patent: October 26, 1999Assignee: Merck Sharp & Dome Ltd.Inventors: Mark Stuart Chambers, Sarah Christine Hobbs, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant
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Patent number: 5889008Abstract: A class of 1-?3-(1H-indol-3-yl)propyl!-4-(2-phenylethyl) piperazine derivatives, substituted at the 5-position of the indole nucleus by a five-membered heteroaromatic moiety, and on the phenyl ring of the phenethyl moiety by fluoro, chloro, trifluoromethyl, alkoxy or an oxazolidinone group and optionally by one or two further substituents, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D .alpha. receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT.sub.1D .alpha. receptor subtype relative to the 5-HT.sub.1D .alpha. subtype; they are therefore usefull in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.Type: GrantFiled: February 5, 1998Date of Patent: March 30, 1999Assignee: Merck Sharp & Dohme, Ltd.Inventors: Richard Alexander Jelley, Angus Murray MacLeod, Austin John Reeve, Francine Sternfeld, Leslie Joseph Street
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Patent number: 5885999Abstract: The present invention relates to compounds of formula (I): ##STR1## wherein m is zero, 1 or 2; and n is zero or 1, with the proviso that the sum total of m+n is 1 or 2;R.sup.1 represents phenyl; naphthyl; benzhydryl; or benzyl, where the naphthyl group or any phenyl moiety may be substituted;R.sup.2 represents hydrogen; phenyl; heteroaryl selected from indazolyl, thienyl, furanyl, pyridyl, thiazolyl, tetrazolyl and quinolinyl; naphthyl; benzhydryl; or benzyl; wherein each heteroaryl, the naphthyl group and any phenyl moiety may be substituted;R.sup.3 and R.sup.4 each independently represents hydrogen or C.sub.1-6 alkyl or R.sup.3 and R.sup.4 together are linked so as to form a C.sub.1-3 alkylene chain;Q represents CR.sup.5 R.sup.6 or NR.sup.5 ;X and Y each independently represents hydrogen, or together form a group .dbd.O; andZ represents a bond, O, S, SO, SO.sub.2, NR.sup.c or --(CR.sup.c R.sup.d)--, where R.sup.c and R.sup.d each independently represent hydrogen or C.sub.Type: GrantFiled: January 21, 1997Date of Patent: March 23, 1999Assignee: Merck Sharp & Dohme Ltd.Inventors: Jason Matthew Elliott, Angus Murray MacLeod, Graeme Irvine Stevenson
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Patent number: 5849746Abstract: A class of 1,4-disubstituted piperazine derivatives, further substituted on one of the carbon atoms of the piperazine ring, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.Type: GrantFiled: July 22, 1997Date of Patent: December 15, 1998Assignee: Merck Sharp & Dohme Ltd.Inventors: Mark Stuart Chambers, Angus Murray MacLeod, Victor Giulio Matassa
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Patent number: 5811431Abstract: The present invention relates to compounds of formula (I), wherein n is zero, 1, 2 or 3; R represents C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halogen, cyano, trifluoromethyl SO.sub.2 C.sub.1-6 alkyl, NR.sup.a R.sup.b, NR.sup.a COR.sup.b or CONR.sup.a R.sup.b, where R.sup.a and R.sup.b are each H, C.sub.1-4 alkyl, phenyl or trifluoromethyl; R.sup.1 represents phenyl optionally substituted by 1, 2 or 3 of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, --O(CH.sub.2).sub.p O-- (where p is 1 or 2), halogen, cyano, nitro, trifluoromethyl, trimethylsilyl, OR.sup.a, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, NR.sup.a R.sup.b, NR.sup.a COR.sup.b, NR.sup.a CO.sub.2 R.sup.b, COR.sup.a, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b ; naphthyl; benzhydryl; or benyl, where the naphthyl group or each phenyl moiety of benzyl and benzhydryl may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or trifluoromethyl; R.sup.Type: GrantFiled: January 7, 1997Date of Patent: September 22, 1998Assignee: Merck Sharp & Dohme Ltd.Inventors: Tamara Ladduwahetty, Richard Thomas Lewis, Angus Murray MacLeod, Kevin John Merchant
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Patent number: 5760018Abstract: The present invention is directed to certain compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, A.sup.1, A.sup.2, X, m and n are defined herein. The compounds of this invention are tachykinin receptor antagonists and are of particular use in the treatment of pain, inflammation, migraine and emesis.Type: GrantFiled: July 11, 1996Date of Patent: June 2, 1998Assignee: Merck Sharp & Dohme Ltd.Inventors: Raymond Baker, Richard Thomas Lewis, Angus Murray MacLeod, Graeme Irvine Stevenson
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Patent number: 5719149Abstract: The present invention relates to compounds of formula (I) wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are selected from a variety of suitable aromatic substituents; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, or C.sub.2 -alkyl substituted by C.sub.1-4 alkoxy or hydroxy; R.sup.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, C.sub.2-4 alkyl substituted by C.sub.1-4 alkoxy or hydroxy, or the group C(.dbd.NR.sup.c)NR.sup.a R.sup.b ; or R.sup.6 and R.sup.7, together with the nitrogen atom to which they are attached, form an optionally substituted saturated heterocyclic ring of 4 to 7 ring atoms which may optionally contain in the ring one oxygen or sulphur atom or a group selected from NR.sup.8, S(O) or S(O).sub.2 ; or R.sup.6 and R.sup.Type: GrantFiled: February 27, 1997Date of Patent: February 17, 1998Assignee: Merck Sharp & Dohme Ltd.Inventors: Paul Finke, Timothy Harrison, Richard Thomas Lewis, Angus Murray MacLeod, Andrew Pate Owens
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Patent number: 5710161Abstract: The present invention relates to compounds of the formula (I): ##STR1## wherein Ar.sup.1 represents optionally substituted phenyl; Ar.sup.2 represents aryl; benzhydryl; or benzyl; wherein each aryl and heteroaryl and each phenyl moiety of benzyl and benzhydryl may be substituted;R.sup.1 represents H or a group of the formula Z-R.sup.2 ;R.sup.2 represents H, CO.sub.2 R.sup.7, CONR.sup.7 R.sup.8, NR.sup.7 R.sup.8, NR.sup.7 COR.sup.9, NR.sup.7 SO.sub.2 R.sup.8, trifluoromethyl, heteroaryl or --O-heteroaryl, each of which heteroaryl groups are as previously defined and may be optionally substituted, or R.sup.2 represents a group selected from phenyl, piperazinyl, piperidinyl, spiro-fused piperidinyl, tetrahydroquinolinyl or tetrahydroisoquinolinyl, each of which may be substituted;R.sup.3, R.sup.4, R.sup.5 and R.sup.6 each independently represent H or C.sub.1-4 alkyl;R.sup.7 and R.sup.8 each independently represent H, C.sub.Type: GrantFiled: September 12, 1995Date of Patent: January 20, 1998Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Tamara Ladduwahetty, Angus Murray MacLeod
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Patent number: 5693640Abstract: A class of pyridazino?4,5-b!indole-1,4-dione derivatives, substituted in the 2-position by an optionally substituted phenyl moiety, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment and/or prevention of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA antagonist.Type: GrantFiled: June 6, 1995Date of Patent: December 2, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Tamara Ladduwahetty, Angus Murray MacLeod
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Patent number: 5686463Abstract: A class of novel oxadiazoles, substituted on one of the ring carbon atoms with a non-aromatic azacyclic or azabicyclic ring, and substituted on the other ring carbon atom with a substituent of low lipophilicity; are potent muscarinic agonists, and have good CNS penetrability. The compounds are therefore useful in the treatment of neurological and mental illnesses.Type: GrantFiled: March 19, 1987Date of Patent: November 11, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Raymond Baker, Kevin John Merchant, Angus Murray MacLeod, John Saunders
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Patent number: 5674889Abstract: The present invention relates to compounds of formula (I) and salts and prodrugs thereof, wherein Q.sup.1 represents a phenyl group substituted by one or more halo optionally substituted naphthyl, optionally substituted indolyl, optionally substituted benzthiophenyl, optionally substituted benzofuranyl, optionally substituted benzyl or optionally substituted fluorenyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; Z.sup.1 represents a group selected from (a) or (b). The compounds are tachykinin antagonists useful for treating pain or inflammation, migraine or emesis.Type: GrantFiled: August 21, 1995Date of Patent: October 7, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Fintan Kelleher, Richard Thomas Lewis, Angus Murray Macleod
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Patent number: 5668153Abstract: Compounds of formula (I) ##STR1## exemplified by formulae (Ia) and (Ib) ##STR2## are tachykinin receptor antagonists useful in the treatment of disorders associated with the presence of an excess of tachykinins such as pain, inflammation, migraine, emesis and post herpetic neuralgia.Type: GrantFiled: August 4, 1995Date of Patent: September 16, 1997Assignee: Merck Sharp & Dohme, Ltd.Inventors: Richard Thomas Lewis, Angus Murray MacLeod
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Patent number: 5665883Abstract: The present invention relates to compounds of formula (I) wherein n is 3 and where any carbon atom of (CH.sub.2).sub.n may be substituted by R.sup.4 and/or R.sup.5 ; X represents O or S; R.sup.1 represents (CH.sub.2).sub.q phenyl, wherein q is 0, 1 , 2 or 3 which may be optionally substituted in the phenyl ring; R.sup.2 represents aryl selected from phenyl and naphthyl; heteroaryl selected from indazolyl, thienyl, furyl, pyridyl, thiazolyl, tetrazolyl and quinolyl; benzhydryl; or benzyl; wherein each aryl or heteroaryl moiety may be substituted; R.sup.4 and R.sup.5 each independently represent H, halo, C.sub.1-6 alkyl, oxo, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b ; R.sup.6 represents H or C.sub.1-6 alkyl; R.sup.7 represents trifluoromethyl, C.sub.2-6 alkenyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, (CH.sub.2).sub.p NR.sup.9 R.sup.10, CO.sub.2 R.sup.16, CONR.sup.9 R.sup.10, (CH.sub.2).sub.p CO.sub.2 R.sup.16, (CH.sub.2).sub.p CONR.sup.9 R.sup.10, (CH.sub.2).sub.p NR.sup.9 COR.sup.16, (CH.sub.Type: GrantFiled: September 26, 1996Date of Patent: September 9, 1997Assignee: Merck Sharp & Dohme LimitedInventors: Raymond Baker, Angus Murray MacLeod, Eileen Mary Seward, Christopher John Swain
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Patent number: 5663352Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts and prodrugs thereof, wherein X represents a propylene or propenylene chain optionally substituted by one or more of R.sup.4, R.sup.5, R.sup.6 and R.sup.7 ; m is 2, 3 or 4; n is 0, 1 or 2 when m is 2 or 3, and n is 0 or 1 when m is 4; R.sup.1 represents optionally substituted phenyl; R.sup.2 represents optionally substituted phenyl, heteroaryl, benzhydryl or benzyl; R.sup.3 represents H, COR.sup.9, CO.sub.2 R.sup.10, COCONR.sup.10 R.sup.11, COCO.sub.2 R.sup.10, SO.sub.2 R.sup.15, CONR.sup.10 SO.sub.2 R.sup.15, C.sub.1-6 alkyl optionally substituted by a group selected from (CO.sub.2 R.sup.10, CONR.sup.10 R.sup.11, hydroxy, cyano, COR.sup.9, NR.sup.10 R.sup.11, C(NOH)NR.sup.10 R.sup.11, CONHphenyl(C.sub.1-4 alkyl), COCO.sub.2 R.sup.10, COCONR.sup.10 R.sup.11, SO.sub.2 R.sup.15, CONR.sup.10 SO.sub.2 R.sup.15 and optionally substituted phenyl), Y--R.sup.8 or CO--Z--(CH.sub.2).sub.q --R.sup.12 ; R.sup.4 and R.sup.Type: GrantFiled: January 19, 1996Date of Patent: September 2, 1997Assignee: Merck Sharp & Dohme LimitedInventors: Angus Murray MacLeod, Kevin John Merchant, Graeme Irvine Stevenson