Patents Represented by Attorney Robert J. North
  • Patent number: 5665722
    Abstract: A class of chemical 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, are antagonists of dopamine receptor subtypes within the brain, being extremely potent antagonists of the human dopamine D.sub.4 subtype over other dopamine receptor subtypes, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders such as schizophrenia while manifesting fewer side-effects than those associated with classical neuroleptic drugs.
    Type: Grant
    Filed: October 18, 1996
    Date of Patent: September 9, 1997
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: Janusz Jozef Kulagowski, Paul David Leeson, Ian Michael Mawer
  • Patent number: 5665732
    Abstract: A class of chemical compounds comprising a 1-H-indazole moiety and a substituted heterocyclic moiety, linked via the 3-position of the indazole moiety by a methylene group, 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. In formula (I) R represents hydrogen or C.sub.1-6 alkyl, Q represents a moiety of formula Qa, Qb, or Qc.
    Type: Grant
    Filed: September 8, 1995
    Date of Patent: September 9, 1997
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Janusz Jozef Kulagowski, Paul David Leeson, Adrian Leonard Smith
  • Patent number: 5641787
    Abstract: The present invention accordingly provides the use of a compound of formula I, or a pharmaceutically acceptable salt thereof or a prodrug thereof: ##STR1## wherein R.sup.1 represents hydrogen or C.sub.1-6 alkyl;Z represents --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --;R.sup.2 represents hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, aryl(C.sub.1-6)alkyl or halogen;R.sup.3, R.sup.4 and R.sup.5 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.sub.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 ; andR.sup.a and R.sup.b independently represent hydrogen, hydrocarbon or a heterocyclic group;for the manufacture of a medicament for the treatment and/or prevention of psychotic disorders such as schizophrenia.
    Type: Grant
    Filed: September 12, 1995
    Date of Patent: June 24, 1997
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Ian Michael Mawer, Howard Barff Broughton, Janusz Jozef Kulagowski, Paul David Leeson
  • Patent number: 5633281
    Abstract: Compounds of formula (I), or a salt or prodrug thereof, wherein R.sup.1 represents H, C.sub.1-4 alkyl or CH.sub.2 COOH; R.sup.2 represents H or C.sub.1-4 alkyl, with the proviso that R.sup.1 and R.sup.2 are not both H; R.sup.3 and R.sup.4 each independently rely resent H, C.sub.1-, alkyl. C.sub.2-6 alkenyl C.sub.1-6 alkoxy, halo or trifluoromethyl; A.sup.1, A.sup.2, A.sup.3, and A.sup.4 each independently represent H, C.sub.1-6 alkyl, C.sub.1-6 alkenyl, C.sub.1-6 alkoxy, halo or trifluoromethyl; and A.sup.5 and A.sup.6 each independently represent H or C.sub.
    Type: Grant
    Filed: December 8, 1995
    Date of Patent: May 27, 1997
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Martin R. Teall, Brian J. Williams
  • Patent number: 5629347
    Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is R.sup.9 CR.sup.10 R.sup.11 or CH.sub.2 R.sup.9 CR.sup.10 R.sup.11 where R.sup.9 is H or OH and R.sup.10 and R.sup.11 are optionally substituted phenyl, optionally substituted benzyl, C.sub.5-7 cycoalkyl or (C.sub.5-7 cycloalkyl)methyl; R.sup.1 and R.sup.2 are H, optionally substituted C.sub.1-6 alkyl, optionally substituted phenyl(C.sub.1-4 alkyl), C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, COR.sup.a, COOR.sup.a, COC.sub.1-6 alkylhalo, COC.sub.1-6 alkylNR.sup.a R.sup.b, CONR.sup.12 C.sub.1-6 alkylCONR.sup.a R.sup.b, CONR.sup.a R.sup.b, or SO.sub.2 R.sup.a, or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.q optionally substituted by oxo where one methylene group may optionally be replaced by O or NR.sup.x ; R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; R.sup.4 is optionally substituted phenyl(C.sub.1-3 alkyl); X and Y are H, or X and Y together are .dbd.O; and Z is O, S, or NR.sup.7 ; are tachykinin antagonists.
    Type: Grant
    Filed: December 22, 1993
    Date of Patent: May 13, 1997
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Christopher J. Swain, Martin R. Teall, Brian J. Williams
  • Patent number: 5629336
    Abstract: Compounds capable of interacting with the strychnine-insensitive glycine modulatory site of the N-methyl-D-aspartate (NMDA) receptor are active in preventing or reducing dependence on dependence-inducing agents such as morphine, but lack the undesirable side-effects of agents hitherto employed for this purpose.
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: May 13, 1997
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventor: Peter H. Hutson
  • Patent number: 5624947
    Abstract: Compounds of formula (I), or a salt or prodrug thereof are tachykinin antagonists.
    Type: Grant
    Filed: June 20, 1995
    Date of Patent: April 29, 1997
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Linda E. Keown, Tamara Ladduwahetty, Monique B. Van Niel
  • Patent number: 5622950
    Abstract: A class of pyrrolo[2,3-b]pyridine derivatives, substituted at the 3-position by a substituted piperazinylmethyl moiety, are antagonists of dopamine receptor subtypes within the brain, having a selective affinity for the dopamine D.sub.4 receptor subtype over other dopamine receptor subtypes, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders such as schizophrenia whilst manifesting fewer side-effects than those associated with classical neuroleptic drugs.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: April 22, 1997
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Neil R. Curtis, Janusz J. Kulagowski, Paul D. Leeson, Mark P. Ridgill, Adrian L. Smith
  • Patent number: 5620972
    Abstract: Benzapines of the formula (I) ##STR1## and salts and prodrugs thereof useful as CCK antagonists.
    Type: Grant
    Filed: June 20, 1995
    Date of Patent: April 15, 1997
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Monique B. van Niel
  • Patent number: 5618812
    Abstract: Compounds of Formula (I), and salts and prodrugs thereof, wherein R.sup.1 represents H, optionally substituted C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; R.sup.2 is NHR.sup.12 or (CH.sub.2).sub.s R.sup.13 where 5 is 0, 1 or 2; R.sup.3 represents C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; R.sup.4 and R.sup.5 are H, C.sub.1-12 alkyl optionally substituted by NR.sup.9 R.sup.9' or an azacyclic or azabicyclic group, optionally substituted C.sub.4-9 cycloalkyl, C.sub.4-9 cycloalkyl C.sub.1-4 alkyl, aryl, arylC.sub.1-6 alkyl or azacyclic or azabicyclic groups, or R.sup.4 and R.sup.5 together form the residue of an optionally substituted azacyclic or azabicyclic ring system; x is 0, 1, 2 or 3; R.sup.12 is optionally substituted phenyl or pyridyl; R.sup.13 represents a group (A) wherein R.sup.14 is H or C.sub.1-6 alkyl; R.sup.15 is H, C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; and the dotted line is an optional covalent bond; are CCK and/or gastrin antagonists useful in therapy.
    Type: Grant
    Filed: January 26, 1995
    Date of Patent: April 8, 1997
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventors: Jose L. Castro Pineiro, William R. Carling, Mark S. Chambers, Stephen R. Fletcher, Sarah C. Hobbs, Victor G. Matassa, Kevin W. Moore, Graham A. Showell, Michael G. Russell
  • Patent number: 5614524
    Abstract: A class of substituted piperazine derivatives of formula I ##STR1## are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated conditions, for which a selective agonist of these receptors is indicated.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: March 25, 1997
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: V. G. Matassa, L. J. Street, A. J. Reeve
  • Patent number: 5614532
    Abstract: A class of 2-(1H)-quinolone derivatives, substituted at the 3-position by an optionally substituted aryl substituent, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA receptor antagonist.
    Type: Grant
    Filed: May 25, 1994
    Date of Patent: March 25, 1997
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: William R. Carling, Paul D. Leeson, Michael Rowley, Kevin W. Moore
  • Patent number: 5614518
    Abstract: A class of substituted morpholine derivatives of formula ##STR1## wherein Y represents an optionally substituted bicyclic heteroaromatic ring system containing one or two nitrogen atoms, the ring system comprising a six-membered aromatic or heteroaromatic ring fused to a five- or six-membered heteroaromatic ring; and Z represents an optionally substituted arylalkyl, aryloxymethyl or arylalkoxymethyl group, 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: May 20, 1996
    Date of Patent: March 25, 1997
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Paul D. Leeson, Graham A. Showell
  • Patent number: 5612362
    Abstract: Compounds of formula (I) and salts and prodrugs wherein Q.sup.1 is a specified aryl group, the dotted line is an optional double bond, Z is O or NR.sup.3, R.sup.1 and R.sup.3 are H or specified optionally substituted alkyl or other substituents and R.sup.2 is an optionally substituted phenyl or group are tachykinin receptor antagonists useful in medicine.
    Type: Grant
    Filed: April 18, 1995
    Date of Patent: March 18, 1997
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Angus M. MacLeod
  • Patent number: 5612336
    Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q.sup.1 is phenyl substituted by one or more halo; optionally substituted naphthyl, indolyl, benzothiophenyl, benzofuranyl, benzyl or fluorenyl; the dotted line represents an optional covalent bond; one of X and Y is H and the other is hydroxy or C.sub.1-6 alkoxy, or X and Y together form a group .dbd.O or .dbd.NOR.sup.5 where R.sup.5 is H or C.sub.1-6 alkyl; R.sup.1 is H or C.sub.1-6 alkyl. R.sup.2 is CO--W--R.sup.6 where W represents a bond or a hydrocarbon chain of 1-6 carbon atoms and R.sup.6 is an azacyclic or azabicyclic group; R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; and R.sup.4 is phenyl optionally substituted by 1-3 of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, OR.sup.a, SR.sup.a, SOR.sup.a, NR.sup.a R.sup.b, NR.sup.a COR.sup.b, NR.sup.a CO.sub.2 R.sup.b, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b, where R.sup.a and R.sup.b are H, C.sub.
    Type: Grant
    Filed: January 13, 1995
    Date of Patent: March 18, 1997
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Richard J. Lewis, Angus M. MacLeod, Kevin J. Merchant
  • Patent number: 5610183
    Abstract: Compounds of Formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein Q is optionally substituted phenyl or naphthyl;X and Y are each H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or X and Y are together .dbd.O;Z is O or S;R.sup.1 is H, optionally substituted C.sub.1-6 alkyl, optionally substituted phenyl (C.sub.1-4 alkyl), C.sub.2-6 alkenyl, COC.sub.1-6 alkylhalo, COR.sup.a, COOR.sup.a, CONHR.sup.a, COC.sub.1-6 alkylNR.sup.a R.sup.b or CONR.sup.a C.sub.1-6 alkylCONR.sup.a R.sup.b ;R.sup.2 is substituted C.sub.1-6 alkyl, optionally substituted phenyl(C.sub.1-4 alkyl), C.sub.2-6 alkenyl, C.sub.1-6 alkylhalo, COR.sup.a, COOR.sup.a, CONHR.sup.a, COC.sub.1-6 alkylNR.sup.a R.sup.b or CONR.sup.a C.sub.1-6 alkylCONR.sup.a R.sup.b ;or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.p optionally substituted by oxo;R.sup.3 is H [or C.sub.1-6 alkyl];R.sup.4 is H, C.sub.1-6 alkyl or phenyl; andR.sup.5 is optionally substituted (CH.sub.2).sub.
    Type: Grant
    Filed: December 17, 1993
    Date of Patent: March 11, 1997
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Andrew P. Owens, Brian J. Williams
  • Patent number: 5607946
    Abstract: A class of chemical compounds comprising a 2(1H)-quinolone moiety and a substituted heterocyclic moiety, linked via the 3-position of the 2(1H)-quinolone moiety by a methylene group, are antagonists of dopamine receptor subtypes within the brain, having a selective affinity for the dopamine D4 receptor subtype over other dopamine receptor subtypes, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders such as schizophrenia whilst manifesting fewer side-effects than those associated with classical neuroleptic drugs.
    Type: Grant
    Filed: August 30, 1995
    Date of Patent: March 4, 1997
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Janusz J. Kulagowski, Paul D. Leeson, Ian M. Mawer
  • Patent number: 5607957
    Abstract: A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.
    Type: Grant
    Filed: September 29, 1994
    Date of Patent: March 4, 1997
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose L. Castro Pineiro, Victor G. Matassa
  • Patent number: 5604240
    Abstract: A class of substituted pyrrolo[2,3-c]pyridine derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.
    Type: Grant
    Filed: November 16, 1995
    Date of Patent: February 18, 1997
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: Mark S. Chambers, Victor G. Matassa
  • Patent number: D379223
    Type: Grant
    Filed: September 13, 1995
    Date of Patent: May 13, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth A. Kramer, Ashok V. Katdare