Patents Assigned to Merck Sharp & Dohme Ltd.
  • 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: 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: 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: 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
  • 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: 5652100
    Abstract: The present invention relates to stably co-transfected eukaryotic cell lines capable of expressing a recombinant GABA.sub.A receptor, particularly a recombinant human GABA.sub.A receptor, which comprises at least one alpha, one beta and one gamma subunit; and to the use of the cell line and/or membrane preparation in selecting compounds and designing medicaments which interact with the respective human recombinant GABA.sub.A receptor.
    Type: Grant
    Filed: November 17, 1994
    Date of Patent: July 29, 1997
    Assignee: Merck Sharpe & Dohme Ltd.
    Inventors: Karen Hadingham, Paul John Whiting
  • 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: 5633266
    Abstract: The present invention relates to compounds of formula (I), and salts and prodrugs thereof, wherein n is 1 , 2 or 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 optionally substituted (CH.sub.2).sub.q phenyl, wherein q is 0, 1, 2 or 3; R.sup.2 represents optionally substituted aryl, heteroaryl, benzhydryl or benzyl; 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 C.sub.1-6 alkyl or optionally substituted phenyl; R.sup.8 represents H, COR.sup.a, CO.sub.2 R.sup.a, COCONR.sup.a R.sup.b, COCO.sub.2 R.sup.a, C.sub.1-6 alkyl optionally substituted by a variety of substituents, or C.sub.1-6 alkyl, optionally substituted by oxo, substituted by an optionally substituted aromatic heterocycle. The compounds are tachykinin antagonists useful for treating pain or inflammation, migraine or emesis.
    Type: Grant
    Filed: July 26, 1995
    Date of Patent: May 27, 1997
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Christopher J. Swain, Brian J. Williams