Patents Represented by Attorney Robert J. North
  • Patent number: 6080745
    Abstract: A class of fused tricyclic heteroaromatic compounds of formula (I) as defined in claim 1 or a salt thereof or a prodrug thereof, containing a fused pyrazole, oxazole or pyrimidine ring are ligands for dopamine receptor subtypes within the body and are therefore of use in the treatment and/or prevention of disorders of the dopamine system, such as schizophrenia.
    Type: Grant
    Filed: March 12, 1996
    Date of Patent: June 27, 2000
    Assignee: Merck Sharp & Dohme Limited
    Inventors: William Barnaby Davey, Paul David Leeson, Michael Rowley
  • Patent number: 5717104
    Abstract: A process for preparing tryptamine derivatives and related compounds having a 1,2,4-triazol-1-yl moiety within the molecule comprises reacting 4-amino-1,2,4-triazol with a nitrobenzene derivative containing a readily displaceable group; deaminating the aminotriazolium salt thereby obtained by treatment with nitrous acid followed by neutralisation; reducing the triazolyl-ni-trobenzene derivative thereby obtained by transfer hydrogenation; treating the triazolyl-aniline derivative thereby obtained with nitrous acid and then with an alkali metal sulphate, followed by acidification; and subsequently reacting the triazolyl-hydrazine derivative thereby obtained in situ with a suitable carbonyl compound, to obtain the required triazolyl-indole derivative.
    Type: Grant
    Filed: May 20, 1996
    Date of Patent: February 10, 1998
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventor: Peter Grenville Houghton
  • Patent number: 5714498
    Abstract: The invention is directed to substituted benzimidazole compounds which are ligands for dopamine receptor subtypes used in the treatment of the dopamine system.
    Type: Grant
    Filed: September 12, 1995
    Date of Patent: February 3, 1998
    Assignee: Merck, Sharp, & Dohme, Ltd.
    Inventors: Janusz Jozef Kulagowski, Paul David Leeson
  • Patent number: 5712285
    Abstract: A class of pyrrolo?2,3 -b!pyridine derivatives, linked via the 3-position thereof by a methylene group to a tetrahydropyridinyl moiety, the latter moiety being substituted in turn by an aryl- or heteroaryl-substituted divalent monocyclic radical, are ligands for dopamine receptorsubtypes within the body, in particular the D.sub.4 subtype, and are accordingly of use in the treatment and/or prevention of disorders of the dopamine system, including schizophrenia and depression.
    Type: Grant
    Filed: April 3, 1996
    Date of Patent: January 27, 1998
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Paul David Leeson, Mark Peter Ridgill
  • Patent number: 5710161
    Abstract: 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: Grant
    Filed: September 12, 1995
    Date of Patent: January 20, 1998
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: Tamara Ladduwahetty, Angus Murray MacLeod
  • Patent number: 5710015
    Abstract: The present invention relates to the cloning of novel cDNA sequences encoding human and rat inositol monophosphatase (IMP); to the preparation of IMP enzyme by incorporation of the cDNAs into an expression vector and the expression thereof in recombinant host cells; and to the use of the enzyme thereby obtained in designing and developing medicaments which are inhibitors of human or rat IMP.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: January 20, 1998
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: George McAllister, Paul John Whiting
  • Patent number: 5700809
    Abstract: Compounds of formula I are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia.
    Type: Grant
    Filed: August 29, 1995
    Date of Patent: December 23, 1997
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventors: Paul David Leeson, Adrian Leonard Smith, Mark Peter Ridgill, Raymond Baker, Neil Roy Curtis, Janusz Jozef Kulagowski
  • Patent number: 5700802
    Abstract: A class of substituted furo?2,3-b!pyridine derivatives are ligands for dopamine receptor subtypes within the body, in particular the D.sub.4 subtype, and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia or depression.
    Type: Grant
    Filed: October 9, 1996
    Date of Patent: December 23, 1997
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Paul David Leeson
  • Patent number: 5700941
    Abstract: A class of substituted 1,2,3,4,5,6,7,8-octahydronaphthyridine derivatives are ligands for dopamine receptor subtypes within the body, in particular the D.sub.4 subtype, and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia or depression.
    Type: Grant
    Filed: April 3, 1996
    Date of Patent: December 23, 1997
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventor: Janusz Jozef Kulagowski
  • Patent number: 5698573
    Abstract: A class of imidazolone and oxazolone derivatives of Structure I, ##STR1## wherein X represents oxygen or N--R.sup.1 ;Q represents a substituted five-, six- or seven-membered monocyclic heteroaliphatic ring which contains one nitrogen atom as the sole heteroatom and is linked to the imidazolone or oxazolone ring via a carbon atom;R.sup.1 represents hydrogen or C.sub.1-6 alkyl; andone of R.sup.2 and R.sup.3 represents hydrogen or C.sub.1-6 alkyl and the other of R.sup.2 and R.sup.3 represents cycloalkyl or a group of formula (i), (ii) or (iii): ##STR2## in which Z represents oxygen, sulphur or NH; R.sup.4, R.sup.5 and R.sup.
    Type: Grant
    Filed: March 12, 1996
    Date of Patent: December 16, 1997
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: William Robert Carling, Kevin William Moore
  • Patent number: 5696110
    Type: Grant
    Filed: September 5, 1995
    Date of Patent: December 9, 1997
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: Sylvie Bourrain, Stephen Robert Fletcher, Victor Giulio Matassa, Graham Andrew Showell
  • Patent number: 5693640
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: December 2, 1997
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: Tamara Ladduwahetty, Angus Murray MacLeod
  • Patent number: 5686480
    Abstract: A class of fused tricyclic heteroaromatic compounds of formula (I), or a salt thereof or a prodrug thereof containing a fused pyrazole ring are ligands for dopamine receptor subtypes within the body and are therefore of use in the treatment and/or prevention of disorders of the dopamine system, such as schizophrenia.
    Type: Grant
    Filed: March 1, 1996
    Date of Patent: November 11, 1997
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: Ian James Collins, Paul David Leeson, Michael Rowley
  • Patent number: 5686463
    Abstract: 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: Grant
    Filed: March 19, 1987
    Date of Patent: November 11, 1997
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: Raymond Baker, Kevin John Merchant, Angus Murray MacLeod, John Saunders
  • Patent number: 5684006
    Abstract: A class of substituted isoxazole and pyrazole derivatives of formula (I), or a salt thereof of or a prodrug thereof, wherein the broken circle represents two non-adjacent double bonds whereby the five-membered ring containing X and Y is aromatic; one of X and Y represents nitrogen, and the other of X and Y represents oxygen or N--R.sup.5 ; R.sup.1 represents hydrogen, C.sub.1-6 alkyl or trifluoromethyl; R.sup.2 and R.sup.3 independently represent hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, --OR.sup.a, --SR.sup.a, --SOR.sup.a, --SO.sub.2 R.sup.a, --SO.sub.2 NR.sup.a R.sup.b, --NR.sup.a R.sup.a, --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, R.sup.4 represents hydrocarbon or a heterocyclic group; R.sup.5 represents hydrogen or C.sub.1-6 alkyl; and R.sup.a and R.sup.
    Type: Grant
    Filed: May 14, 1996
    Date of Patent: November 4, 1997
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: Sylvie Bourrain, Joseph George Neduvelil, Paul David Leeson, Graham Andrew Showell
  • Patent number: 5681959
    Abstract: The present invention relates to a process for the preparation of azaindole derivatives of the formula ##STR1## wherein Q is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.1-6 alkoxy, hydroxy, aryl or arylC.sub.1-4 alkyl;one of X, Y and Z is --N.dbd. and the others are --CH.dbd.;R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.1-6 alkyl substituted by a group selected from aryl or --NR.sup.2 R.sup.3 where R.sup.2 and R.sup.3 each independently represent C.sub.1-4 alkyl, or R.sup.2 and R.sup.3, together with the nitrogen atom to which they are attached, form a 4-7 membered saturated heterocyclic ring, optionally containing in the ring an oxygen or sulphur atom or a group NR.sup.4 where R.sup.4 is C.sub.1-4 alkyl, aryl or arylC.sub.1-4 alkyl; andR.sup.5 is a hydrogen atom or a group selected from C.sub.1-6 alkyl or aryl.
    Type: Grant
    Filed: February 20, 1996
    Date of Patent: October 28, 1997
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Brian Cchristopher Bishop, Ian Frank Cottrell, Mark Cameron, David Hands
  • Patent number: 5681836
    Abstract: The methanesulfonate salt of a class of antipsychotic compounds comprising a benzo?b!furan moiety and a substituted heterocyclic moiety, linked via the 3-position of the benzo?b!furan moiety by a methylene group, which are antagonists of dopamine receptor subtypes within the brain, being extremely potent antagonists of the human dopamine D.sub.4 receptor subtype and having a selective affinity for the D.sub.4 subtype over other dopamine receptor subtypes, possess advantageous qualities in terms of their improved aqueous solubility relative to the corresponding free base and, as such, provide for greater ease of formulation and display enhanced pharmacokinetic properties, including oral absorption.
    Type: Grant
    Filed: October 9, 1996
    Date of Patent: October 28, 1997
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Paul David Leeson
  • Patent number: 5681833
    Abstract: Compounds of Formula (I), and salts and prodrugs thereof, wherein said formula, R.sup.1 represents certain optionally substituted alkyl or C.sub.3-7 cycloalkyl; R.sup.2 represents (II) or (III), where m is 0, 1, 2 or 3; R.sup.9 is H or C.sub.1-6 alkyl; R.sup.10 is imidazolyl, triazolyl or tetrazolyl, and R.sup.11 is H, C.sub.1-6 alkyl or halo; R.sup.3 is C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; R.sup.4 is C.sub.1-7 alkyl, C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkylC.sub.1-4 alkyl, C.sub.6-10 bicycloalkyl, optionally substituted aryl, or NR.sub.12 R.sub.13 ; R.sup.5 is H or C.sub.1-4 alkyl; n is 0, 1, 2 or 3; which are CCK and/or gastrin antagonists useful in therapy.
    Type: Grant
    Filed: September 20, 1994
    Date of Patent: October 28, 1997
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Mark Stuart Chambers, Sarah Christine Hobbs, Victor Giulio Matassa
  • Patent number: 5674889
    Abstract: 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: Grant
    Filed: August 21, 1995
    Date of Patent: October 7, 1997
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: Fintan Kelleher, Richard Thomas Lewis, Angus Murray Macleod
  • Patent number: 5668153
    Abstract: 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: Grant
    Filed: August 4, 1995
    Date of Patent: September 16, 1997
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventors: Richard Thomas Lewis, Angus Murray MacLeod