Patents Assigned to Merck Sharp & Dohme
  • Patent number: 5567726
    Abstract: Imidazole, triazole and tetrazole derivatives of formula (I) 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, wherein the broken circle represents two non-adjacent double bonds in any position in the five-membered ring; two, three or four of V, W, X, Y and Z represent nitrogen and the remainder represent carbon provided that, when two of V, W, X, Y and Z represent nitrogen and the remainder represent carbon, then the said nitrogen atoms are in non-adjacent positions within the five-membered ring; E represents a bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; F represents a group of formula (a); U represents nitrogen or C--R.sup.2 ; B represents oxygen, sulphur or N--R.sup.3 ; R.sup.1 represents a group of formula (i), (ii) or (iii).
    Type: Grant
    Filed: January 24, 1995
    Date of Patent: October 22, 1996
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Jose L. Castro Pineiro, Alexander R. Guiblin, Austin J. Reeve, Francine Sternfeld, Victor G. Matassa, Leslie J. Street
  • Patent number: 5563161
    Abstract: Compounds of formula (I), and salt and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; 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; C.sub.2-6 alkynyl; COR.sup.a ; COOR.sup.a ; COHet; 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 ; R.sup.2 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.q optionally substituted by oxo where q is 4 or 5 and where one methylene group may optionally be replaced by an oxygen atom or a group NR.sup.x, where R.sup.x is H or C.sub.1-6 alkyl; R.sup.3 is C.sub.1-3 alkyl substituted by optionally substituted phenyl; R.sup.4 and R.sup.5 are each H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; and Z represents O or S; are tachykinin receptor antagonists useful in therapy.
    Type: Grant
    Filed: March 10, 1995
    Date of Patent: October 8, 1996
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Ian T. Huscroft, Graeme I. Stevenson, Brain J. Williams
  • Patent number: 5563152
    Abstract: A class of chemical compounds comprising a pyrrolo[2,3-b]pyridine moiety and a carboxamido-substituted heterocyclic moiety, linked via the 3-position of the pyrrolo[2,3-b]pyridine 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.
    Type: Grant
    Filed: August 9, 1995
    Date of Patent: October 8, 1996
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Janusz J. Kulagowski, Paul D. Leeson
  • Patent number: 5563150
    Abstract: A class of chemical compounds comprising a pyrrolo[2,3-b]pyridine moiety and a halo-substituted heterocyclic moiety, linked via the 3-position of the pyrrolo[2,3-b]pyridine 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.
    Type: Grant
    Filed: August 9, 1995
    Date of Patent: October 8, 1996
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Neil R. Curtis, Janusz J. Kulagowski, Paul D. Leeson
  • Patent number: 5561130
    Abstract: Compounds of Formula (I), and salts and prodrugs thereof, wherein n is 1, 2 or 3; X represents O or S; R.sup.1 is optionally substituted phenyl; R.sup.2 is aryl or heteroaryl; R.sup.4 and R.sup.5 are independently H, halo, C.sub.1-6 alkyl, oxo, CH.sub.2 OR.sup.a, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b ; R.sup.8 represents C(COOR.sup.a).sub.2, C(CONR.sup.a R.sup.b).sub.2 or C.sub.1-6 alkyl substituted by C(.dbd.NR.sup.a)NR.sup.b NR.sup.c CO.sub.2 R.sup.d, CONHNR.sup.a R.sup.b, C(S)NR.sup.a R.sup.b, CONR.sup.a C.sub.1-6 alkylR.sup.12, CONR.sup.13 C.sub.2-6 alkynyl, CONR.sup.13 C.sub.2-6 alkenyl, COCONR.sup.a R.sup.b, CONR.sup.a C(NR.sup.b)NR.sup.c R.sup.d, CONR.sup.13 SO.sub.2 R.sup.a, SO.sub.2 NR.sup.13 COR.sup.a, CONR.sup.a heteroaryl or COR.sup.q ; R.sup.a, R.sup.b, R.sup.c and R.sup.d are each H, C.sub.1-6 alkyl, phenyl or trifluoromethyl. R.sup.12 represents OR.sup.a, CONR.sup.a R.sup.b or heteroaryl; R.sup.13 represents H or C.sub.1-6 alkyl; and R.sup.
    Type: Grant
    Filed: January 24, 1995
    Date of Patent: October 1, 1996
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Eileen M. Seward, Christopher J. Swain
  • Patent number: 5559125
    Abstract: A class of 4-hydroxy-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: July 11, 1994
    Date of Patent: September 24, 1996
    Assignee: Merck, Sharp & Dohme Limited
    Inventors: Janusz J. Kulagowski, Paul D. Leeson, Ian M. Mawer, Michael Rowley
  • Patent number: 5556969
    Abstract: Compounds of the formula (I): ##STR1## wherein R.sub.1 is hydrogen or specified optionally substituted alkyl, R.sup.2 is specified optionally substituted phenyl or pyridyl, x is 0, 1, 2 or 3, R.sup.3 is a specified alkyl, halo or amino and R.sup.4 is specified cycoalkyl or bicycloalkyl; and salts and prodrugs thereof, are useful as antagonists of cholecystokin and gastrin receptors.
    Type: Grant
    Filed: June 29, 1995
    Date of Patent: September 17, 1996
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Mark S. Chambers, Stephen R. Fletcher
  • Patent number: 5554633
    Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-6 alkyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents C.sub.1-6 alkyl substituted by CONR.sup.7 (CH.sub.2).sub.p R.sup.8 (where R.sup.7 is H or C.sub.1-6 alkyl, R.sup.8 is optionally substituted heteroaryl and p is 0, 1, 2, 3, 4, 5 or 6); R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkynyl; R.sup.4 represents H, C.sub.1-6 alkyl or optionally substitute phenyl; R.sup.5 represents optionally substituted phenyl; R.sup.6 is H or C.sub.1-6 alkyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.
    Type: Grant
    Filed: January 27, 1995
    Date of Patent: September 10, 1996
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventor: Martin R. Teall
  • Patent number: 5554629
    Abstract: A discrete class of 4-substituted 1,2,4-triazole 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: June 29, 1995
    Date of Patent: September 10, 1996
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Victor G. Matassa, Austin J. Reeve, Francine Sternfeld, Leslie J. Street
  • Patent number: 5554627
    Abstract: Compounds of formula (I), wherein Q.sup.1 represents an aryl group; the dotted line represents an optional covalent bond; one of X and Y represents H and the other represents 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; Z represents O, S or NR.sup.2, where R.sup.2 is H or C.sub.1-6 alkyl; W represents a bond or a saturated or unsaturated hydrocarbon chain of 1, 2, 3, 4, 5 or 6 carbon atoms; R.sup.1 represents H or C.sub.1-6 alkyl. R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; R.sup.4 represents an optionally substituted phenyl group; and R.sup.6 represents a specified amino group or an optionally substituted aromatic or non-aromatic azacyclic or azabicyclic group; and salts and prodrugs are tachykinin receptor antagonists.
    Type: Grant
    Filed: April 27, 1995
    Date of Patent: September 10, 1996
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Richard T. Lewis, Angus M. MacLeod, Kevin J. Merchant
  • Patent number: 5552402
    Abstract: A class of substituted five-membered heteroaromatic compounds 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 18, 1995
    Date of Patent: September 3, 1996
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: V. G. Matassa, L. J. Street, G. A. Showell
  • Patent number: 5527817
    Abstract: The sulphate salt of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine is a selective agonist of 5-HT.sub.1 -like receptors and is 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: December 7, 1994
    Date of Patent: June 18, 1996
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Raymond Baker, Victor G. Matassa, Alexander R. Guiblin, Kendal G. Pitt, Leslie J. Street, Carole Olive, David E. Storey
  • Patent number: 5521175
    Abstract: Compounds of Formula (I), and salts and prodrugs thereof, wherein R.sup.1 represents C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; R.sup.2 optionally substituted phenyl or R.sup.2 represents a group (A) where W is CH.sub.2 or NR.sup.10, and W.sup.1 is CH.sub.2, or W and W.sup.1 each represent 0; R.sup.3 is C.sub.1-6 alkyl, halo or NR.sup.13 R.sup.14 ; R.sup.4 is H, C.sub.1-4 alkyl, optionally substituted phenyl or optionally substituted benzyl; R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are H or C.sub.1-4 alkyl; or any two of R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 together form a chain (CH.sub.2).sub.t, and any other two of R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 optionally form a chain (CH.sub.2).sub.s where s and t are independently 1, 2 or 3; m is 2, 3, 4, 5, 6, 7, 8 or 9; n is 0, 1, 2, 3 or 4; and x is 0, 1, 2 or 3; are CCK and/or gastrin antagonists useful in therapy.
    Type: Grant
    Filed: January 26, 1995
    Date of Patent: May 28, 1996
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose L. Castro Pineiro, Mark S. Chambers, Victor G. Matassa
  • Patent number: 5514682
    Abstract: Compounds of formula (I) wherein F represents a Group of the formula (a) ; E represents a bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; and the rest of the variables are defined in the specification are selective agonists of 5HT.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 14, 1994
    Date of Patent: May 7, 1996
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Leslie J. Street
  • Patent number: 5514718
    Abstract: Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein Q.sup.1 is halo substituted phenyl; naphthyl; indolyl; benzthiophenyl; benzofuranyl; benzyl; or fluorenyl;. . is 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 are together .dbd.O or .dbd.NOR.sup.5 ;R.sup.1 and R.sup.2 are H; C.sub.1-6 alkyl optionally substituted by hydroxy, cyano, COR.sup.c, CO.sub.2 R.sup.c, CONR.sup.c R.sup.d, or NR.sup.c R.sup.d (where R.sup.c and R.sup.d are H, C.sub.1-6 alkyl or phenyl(C.sub.0-4 alkyl) optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo and trifluoromethyl); phenyl(C.sub.1-4 alkyl) (optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo or trifluoromethyl); COR.sup.c ; CO.sub.2 R.sup.c ; CONR.sup.c R.sup.d ; COC.sub.1-6 alkylNR.sup.c R.sup.d ; CONR.sup.c COOR.sup.d ; or SO.sub.2 R.sup.c ;R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; andR.sup.4 is phenyl optionally substituted by C.sub.1-6 alkyl, C.sub.
    Type: Grant
    Filed: April 15, 1994
    Date of Patent: May 7, 1996
    Assignee: Merck, Sharp & Dohme Limited
    Inventors: Richard T. Lewis, Kevin J. Merchant, Angus M. MacLeod
  • Patent number: 5510359
    Abstract: A class of substituted five-membered heteroaromatic compounds possessing an imino spacer group 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: October 7, 1994
    Date of Patent: April 23, 1996
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose L. Castro Pineiro, Victor G. Matassa
  • Patent number: 5496833
    Abstract: Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein n is 1, 2 or 3;X represents O or S;Y represents a hydrocarbon chain of 1, 2, 3 or 4 carbon atoms optionally substituted by oxo;R.sup.1 is phenyl optionally substituted by 1, 2 or 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, 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, --CO.sub.2 R.sup.a or --CONR.sup.a R.sup.b ;R.sup.2 is phenyl, indazolyl, thienyl, furyl, pyridyl, thiazolyl, tetrazolyl, quinolyl, benzhydryl, or benzyl;R.sup.4 and R.sup.5 each independently represent H, halo, C.sub.1-6 alkyl, oxo, CH.sub.2 OR.sup.a, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b ;R.sup.8 represents an optionally substituted aromatic heterocycle; andR.sup.a and R.sup.b are H, trifluoromethyl, C.sub.1-6 alkyl or phenyl optionally substituted by C.sub.
    Type: Grant
    Filed: February 13, 1995
    Date of Patent: March 5, 1996
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Reymond Baker, Tamara Ladduwahetty, Eileen M. Seward, Christopher J. Swain
  • Patent number: 5494926
    Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q represents phenyl or benzhydryl; X and Y each represent H or X and Y together form a group =0; Z is O, S or NR.sup.8 (R.sup.8 is H or C.sub.1-6 alkyl); R.sup.1 is H, optionally substituted C.sub.1-6 alkyl, phenyl(C.sub.1-4 alkyl), C.sub.2-6 alkylene, COR.sup.a, COOR.sup.a, CONHR.sup.a, COC.sub.1-4 alkylNR.sup.a R.sup.b, or CONR.sup.a C.sub.1-4 alkylCONR.sup.a R.sup.b ; R.sup.2 is C.sub.1-4 alkyl substituted by an optionally substituted aromatic heterocycle; R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; R.sup.4 is H, C.sub.1-6 alkyl or optionally substituted phenyl; R.sup.5 represents optionally substituted phenyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.
    Type: Grant
    Filed: November 18, 1994
    Date of Patent: February 27, 1996
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Andrew P. Owens, Martin Teall, Brian Williams
  • Patent number: 5495047
    Abstract: Fused tricyclic compounds of formula (I) as disclosed herein, and salts and prodrugs thereof, are tachykinin antagonists, useful for treating pain.
    Type: Grant
    Filed: April 21, 1994
    Date of Patent: February 27, 1996
    Assignee: Merck, Sharp & Dohme (Ltd.)
    Inventors: Monique B. Van Niel, Brian J. Williams, Walfred S. Saari
  • Patent number: 5478933
    Abstract: Disclosed are new benzodiazepine compounds which are useful as cholecystokinin and gastrin receptor antagonists and are useful in the treatment of anxiety, panic and pain.
    Type: Grant
    Filed: April 8, 1994
    Date of Patent: December 26, 1995
    Assignee: Merck Sharpe & Dohme Ltd.
    Inventor: Graham A. Showell