Patents Assigned to Merck Sharp
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Patent number: 5563150Abstract: 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: GrantFiled: August 9, 1995Date of Patent: October 8, 1996Assignee: Merck, Sharp & Dohme Ltd.Inventors: Neil R. Curtis, Janusz J. Kulagowski, Paul D. Leeson
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Patent number: 5563152Abstract: 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: GrantFiled: August 9, 1995Date of Patent: October 8, 1996Assignee: Merck, Sharp & Dohme Ltd.Inventors: Janusz J. Kulagowski, Paul D. Leeson
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Patent number: 5561130Abstract: 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: GrantFiled: January 24, 1995Date of Patent: October 1, 1996Assignee: Merck Sharp & Dohme LimitedInventors: Eileen M. Seward, Christopher J. Swain
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Patent number: 5559125Abstract: 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: GrantFiled: July 11, 1994Date of Patent: September 24, 1996Assignee: Merck, Sharp & Dohme LimitedInventors: Janusz J. Kulagowski, Paul D. Leeson, Ian M. Mawer, Michael Rowley
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Patent number: 5556969Abstract: 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: GrantFiled: June 29, 1995Date of Patent: September 17, 1996Assignee: Merck Sharp & Dohme Ltd.Inventors: Mark S. Chambers, Stephen R. Fletcher
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Patent number: 5554633Abstract: 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: GrantFiled: January 27, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme, Ltd.Inventor: Martin R. Teall
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Patent number: 5554629Abstract: 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: GrantFiled: June 29, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme Ltd.Inventors: Raymond Baker, Victor G. Matassa, Austin J. Reeve, Francine Sternfeld, Leslie J. Street
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Patent number: 5554627Abstract: 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: GrantFiled: April 27, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme Ltd.Inventors: Richard T. Lewis, Angus M. MacLeod, Kevin J. Merchant
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Patent number: 5552402Abstract: 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: GrantFiled: May 18, 1995Date of Patent: September 3, 1996Assignee: Merck, Sharp & Dohme Ltd.Inventors: V. G. Matassa, L. J. Street, G. A. Showell
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Patent number: 5550126Abstract: Pharmaceutical compositions and methods of using CCK-ligands D,L-glutamic acid and D,L-aspartic acid as antipsychotic, antianxiety, and agents useful in treatment or prevention of withdrawal symptoms caused by withdrawal of chronic or long term use of diazepam, alcohol, cocaine or nicotine and antianxiety agents are described.Type: GrantFiled: January 30, 1995Date of Patent: August 27, 1996Assignee: Merck Sharp and Dohme LimitedInventors: David C. Horwell, John Hughes, Geoff N. Woodruff
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Patent number: 5527817Abstract: 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: GrantFiled: December 7, 1994Date of Patent: June 18, 1996Assignee: Merck Sharp & Dohme LimitedInventors: Raymond Baker, Victor G. Matassa, Alexander R. Guiblin, Kendal G. Pitt, Leslie J. Street, Carole Olive, David E. Storey
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Patent number: 5521175Abstract: 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: GrantFiled: January 26, 1995Date of Patent: May 28, 1996Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose L. Castro Pineiro, Mark S. Chambers, Victor G. Matassa
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Patent number: 5514682Abstract: 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: GrantFiled: November 14, 1994Date of Patent: May 7, 1996Assignee: Merck Sharp & Dohme LimitedInventor: Leslie J. Street
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Patent number: 5514718Abstract: 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: GrantFiled: April 15, 1994Date of Patent: May 7, 1996Assignee: Merck, Sharp & Dohme LimitedInventors: Richard T. Lewis, Kevin J. Merchant, Angus M. MacLeod
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Patent number: 5510362Abstract: A class of substituted imidazole, triazole and tetrazole derivatives of formula (I), 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 (lI); U represents nitrogen or C--R.sup.2 ; B represents oxygen, sulphur or N--R.sup.3 ; 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: GrantFiled: September 8, 1994Date of Patent: April 23, 1996Assignee: Merck, Sharp and Dohme LimitedInventors: Victor G. Matassa, Austin J. Reeve, Francine Sternfeld, Helen Routledge, Leslie Street
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Patent number: 5510359Abstract: 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: GrantFiled: October 7, 1994Date of Patent: April 23, 1996Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose L. Castro Pineiro, Victor G. Matassa
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Patent number: 5496833Abstract: 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: GrantFiled: February 13, 1995Date of Patent: March 5, 1996Assignee: Merck Sharp & Dohme LimitedInventors: Reymond Baker, Tamara Ladduwahetty, Eileen M. Seward, Christopher J. Swain
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Patent number: 5495047Abstract: Fused tricyclic compounds of formula (I) as disclosed herein, and salts and prodrugs thereof, are tachykinin antagonists, useful for treating pain.Type: GrantFiled: April 21, 1994Date of Patent: February 27, 1996Assignee: Merck, Sharp & Dohme (Ltd.)Inventors: Monique B. Van Niel, Brian J. Williams, Walfred S. Saari
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Patent number: 5494926Abstract: 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: GrantFiled: November 18, 1994Date of Patent: February 27, 1996Assignee: Merck Sharp & Dohme Ltd.Inventors: Andrew P. Owens, Martin Teall, Brian Williams
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Patent number: 5475008Abstract: A class of 2(1H)-quinolone derivatives, substituted at the 3-position by a range of carbonyl-containing substitutients or by a five- or six-membered heteroaromatic moiety, 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: GrantFiled: May 25, 1994Date of Patent: December 12, 1995Assignee: Merck Sharp & Dohme LimitedInventors: William R. Carling, Paul D. Leeson, Michael Rowley