Patents Represented by Attorney Robert J. North
  • 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: 5550288
    Abstract: A novel process for the preparation of .alpha.-aminoacylanilides comprises the treatment of the corresponding .alpha.-haloacylanilides with a solution of ammonium carbamate in aqueous ammonia. The process is especially useful in the preparation of certain active cardiac antiarrhythmic agents, such as tocainide.
    Type: Grant
    Filed: November 14, 1994
    Date of Patent: August 27, 1996
    Assignee: Merck & Co., Inc.
    Inventor: James W. McManus
  • Patent number: 5543417
    Abstract: Described is a combination method using selective inhibitors of 5.alpha.-reductase 1 and/or 2 including 7.beta.-substituted 4-aza-5.alpha.-cholestan-3-ones and related 4-aza-5.alpha.-androstan-3-one compounds which are useful in the treatment of acne vulgaris in combination with at least one agent selected from an antibacterial, keratolytic, and/or an anti-inflammatory.
    Type: Grant
    Filed: October 21, 1994
    Date of Patent: August 6, 1996
    Assignee: Merck & Co., Inc.
    Inventor: Joanne Waldstreicher
  • 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: 5510362
    Abstract: 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: Grant
    Filed: September 8, 1994
    Date of Patent: April 23, 1996
    Assignee: Merck, Sharp and Dohme Limited
    Inventors: Victor G. Matassa, Austin J. Reeve, Francine Sternfeld, Helen Routledge, Leslie Street
  • 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: 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
  • Patent number: 5475008
    Abstract: 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: Grant
    Filed: May 25, 1994
    Date of Patent: December 12, 1995
    Assignee: Merck Sharp & Dohme Limited
    Inventors: William R. Carling, Paul D. Leeson, Michael Rowley
  • Patent number: 5472978
    Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q represents optionally substituted phenyl, naphthyl, indolyl, benzothiophenyl, benzofuranyl, benzyl or indazolyl; Z represents O, S or NR.sup.8 ; X and Y are H or are together .dbd.O; R.sup.1 and R.sup.2 are H; optionally substituted C.sub.1-6 alkyl; optionally substituted phenyl(C.sub.1-4 alkyl); COR.sup.c ; CO.sub.2 R.sup.c ; CONR.sup.c R.sup.d ; CONR.sup.c COOR.sup.d ; or SO.sub.2 R.sup.c ; R.sup.3 is H or C.sub.1-6 alkyl, R.sup.4 is H , C.sub.1-6 alkyl or optionally substituted phenyl; and R.sup.5 represents optionally substituted phenyl; are tachykinin antagonists. They and compositions thereof are useful in therapy.
    Type: Grant
    Filed: December 10, 1993
    Date of Patent: December 5, 1995
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Angus M. MacLeod, Kevin J. Merchant, Christopher J. Swain
  • Patent number: 5462932
    Abstract: Disclosed is a therapy protocol for treating and for preventing bone loss in patients who have difficulty in swallowing by administering a liquid formulation of alendronate which can be easily swallowed. Also described are pharmaceutical dosage forms of a syrup, aqueous solution, a solution formed from a reconstituted powder, of alendronate, for carrying out the therapeutic method.
    Type: Grant
    Filed: May 17, 1994
    Date of Patent: October 31, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Gerald S. Brenner, Ashok V. Katdare, Denise Pretzer, Donna T. Whiteford
  • Patent number: 5461063
    Abstract: Compounds of formula (I), and salts and prodrugs thereof: ##STR1## wherein X represents O or S;Y represents (CH.sub.2).sub.m, where m is 0 or 1;Z represents (CH.sub.2).sub.n, where n is 0 or 1;R.sup.1 represents optionally substituted phenyl;R.sup.2 is phenyl, naphthyl, indazolyl, thienyl, furyl, pyridyl, thiazolyl, tetrazolyl, quinolyl, benzhydryl or benzyl;R.sup.3 is H, COR.sup.a, CO.sub.2 R.sup.a C(COOR).sub.2, C(CONR.sup.a R.sup.b).sub.2, COCONR.sup.a R.sup.b, COCO.sub.2 R.sup.a, C.sub.1-6 alkyl optionally substituted by a group selected from (CO.sub.2 R.sup.a, CONR.sup.a R.sup.b, hydroxy, cyano, COR.sup.a, NR.sup.a R.sup.b, C(NOH)NR.sup.a R.sup.b, CONHphenyl(C.sub.1-4 alkyl), COCO.sub.2 R.sup.a, 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 R.sup.13 COR.sup.
    Type: Grant
    Filed: August 5, 1993
    Date of Patent: October 24, 1995
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Fintan Kelleher, Richard T. Lewis
  • Patent number: 5459239
    Abstract: This invention discloses novel immunogenic peptide sequences, derived from the human cyclooxygenase-1 and cyclooxygenase-2 cDNAs which elicit specific non cross-reactive antibody responses. Assays are also disclosed for selectively and independently detecting cyclooxygenase-1 or cyclooxygenase-2 proteins present in a given biological sample.
    Type: Grant
    Filed: January 24, 1994
    Date of Patent: October 17, 1995
    Assignee: Merck Frosst Canada Inc.
    Inventors: Gary O'Neill, Philip J. Vickers, Stacia Kargman, Jillian F. Evans
  • Patent number: 5451588
    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: November 22, 1993
    Date of Patent: September 19, 1995
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Victor G. Matassa, Leslie J. Street
  • Patent number: 5451582
    Abstract: Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein: R.sup.1 is H, certain optionally substituted C.sub.1.6 alkyl, or C.sub.3-7 cycloalkyl;R.sup.2 is (CH.sub.2).sub.q -tetrazolyl optionally substituted in the tetrazole ring by C.sub.1-4 alkyl, (CH.sub.2).sub.q -imidazolyl (where q is 0, 1, 2 or 3), CONHSO.sub.2 R.sup.9, SO.sub.2 NHCOR.sup.9 (where R.sup.9 is C.sub.1-6 alkyl, optionally substituted aryl or trifluoromethyl). SO.sub.2 NHR.sup.10 (where R.sup.10 is a nitrogen containing heterocycle), cyclopropyl or (CH.sub.2), CO.sub.2 H, where n is 1 or 2;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 straight or branched chain alkyl; andx is 0, 1, 2 or 3;are CCK and/or gastrin receptor antagonists. They and compositions thereof are useful in therapy.
    Type: Grant
    Filed: February 12, 1993
    Date of Patent: September 19, 1995
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Mark S. Chambers, Victor G. Matassa, Stephen R. Fletcher