Patents Assigned to Merck Sharp & Dohme
  • 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: 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: 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: 5612337
    Abstract: The present invention relates to compounds of formula (I), wherein R.sup.1 is hydrogen, halogen, C.sub.1-6 C alkyl, C.sub.1-6 alkoxy, CF.sub.3, NO.sub.2, CN, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, CO.sub.2 R.sup.a, CONR.sup.a R.sup.b, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl or C.sub.1-4 alkyl substituted by C.sub.1-4 alkoxy, where R.sup.a and R.sup.b are hydrogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen, halogen, C .sub.1-6 alkyl, C.sub.1-6 alkoxy substituted by C.sub.1-4 alkoxy or CF.sub.3 ; R.sup.3 is hydrogen, halogen or CF.sub.3 ; R.sup.4 is selected from the definitions of R.sup.1 ; R.sup.5 is selected from the definitions of R.sup.2 ; R.sup.6 is a 5-membered or 6-membered heterocyclic ring containing 2 or 3 nitrogen atoms optionally substituted by .dbd.O, .dbd.S or a C.sub.1-4 alkyl group, and optionally substituted by an aminoalkyl group; R.sup.9a and R.sup.9b are hydrogen or C.sub.1-4 alkyl, or R.sup.9a and R.sup.9b are joined to form a C.sub.5-7 ring; X is C.sub.
    Type: Grant
    Filed: June 13, 1996
    Date of Patent: March 18, 1997
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Raymond Baker, Timothy Harrison, Angus M. MacLeod, Andrew P. Owens, Eileen M. Seward, Christopher J. Swain, Martin R. Teall
  • 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: 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: 5610159
    Abstract: m is 0 or 1; andn is 0 or 1, where the sum total of n+m is 1 or 2.The compounds are of particular use in the treatment of pain, inflammation, migraine, emesis and postherpetic neuralgia.
    Type: Grant
    Filed: June 19, 1996
    Date of Patent: March 11, 1997
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Jonathan D. Moseley, Christopher J. Swain, Brian J. Williams
  • 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: 5602163
    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: May 25, 1995
    Date of Patent: February 11, 1997
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Victor G. Matassa, Leslie J. Street
  • Patent number: 5602162
    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: May 10, 1995
    Date of Patent: February 11, 1997
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Victor G. Matassa, Leslie J. Street
  • Patent number: 5602125
    Abstract: Thienodiazepine compounds of formula (1) wherein: R.sup.1 represents H, optionally substituted C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; R.sup.2 represents optionally substituted phenyl; or R.sup.2 represents a group (a) where W is CH.sub.2 or NR.sup.9 and W.sup.1 is CH.sub.2 or W and W.sup.1 are each O; R.sup.3 is C.sub.3-7 cycloalkyl optionally substituted by one or more C.sub.1-4 alkyl groups, or R.sup.3 is NR.sup.11 R.sup.12, where R.sup.11 and R.sup.12 are each H; C.sub.1-12 alkyl optionally substituted by NR.sup.9 R.sup.9 or an azacyclic or azabicyclic group; C.sub.4-9 cycloalkyl optionally substituted by one or more C.sub.1-4 alkyl groups; C.sub.4-9 cycloalkylC.sub.1-4 alkyl optionally substituted in the cycloalkyl ring by one or more C.sub.1-4 alkyl groups; optionally substituted aryl; optionally substituted arylC.sub.1-6 alkyl; or azacyclic or azabicyclic groups; or R.sup.11 and R.sup.
    Type: Grant
    Filed: February 28, 1995
    Date of Patent: February 11, 1997
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: William R. Carling, Victor G. Matassa
  • Patent number: 5597915
    Abstract: Compounds of Formula (I), and salts and prodrugs thereof wherein: R.sup.1 is H, certain optionally substituted C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; R.sup.2 represents a group (a) wherein X is O, S or NR.sup.8 where R.sup.8 is H or C.sub.1-4 alkyl; one of Z and Y is C.dbd.O and the other is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-4 alkyl; R.sup.3 is C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; R.sup.4 is C.sub.3-10 cycloalkyl; n is 0, 1, 2 or 3, and are CCK and/or gastrin antagonists, which compounds and compositions thereof are useful in therapy.
    Type: Grant
    Filed: September 15, 1994
    Date of Patent: January 28, 1997
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Mark S. Chambers, Stephen R. Fletcher, Victor G. Matassa, Mark G. Bock
  • Patent number: 5580877
    Abstract: A class of 3,5-dihydro-1H-pyrazolo[3,4-c]quinoline-1,4(2H)-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: April 24, 1995
    Date of Patent: December 3, 1996
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Angus M. MacLeod
  • Patent number: 5576319
    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: August 26, 1994
    Date of Patent: November 19, 1996
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Janusz J. Kulagowski, Neil R. Curtis, Paul D. Leeson, Mark P. Ridgill, Adrian L. Smith
  • Patent number: 5576336
    Abstract: Compounds of formula (I), or a salt or prodrug thereof, wherein R represent hydrogen or C.sub.1-6 alkyl; Q represents a moiety of formula Qa or Qb; they 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: September 13, 1995
    Date of Patent: November 19, 1996
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Raymond Baker, Howard B. Broughton, Janusz J. Kulagowski, Paul D. Leeson, Ian M. Mawer
  • Patent number: 5567819
    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-nitrobenzene 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: January 20, 1995
    Date of Patent: October 22, 1996
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventor: Peter G. Houghton