Patents Assigned to Merck Sharp
  • Patent number: 6060469
    Abstract: The present invention relates to compounds of formula (I), ##STR1## wherein R.sup.1 represents halogen, hydroxy, C.sub.1-6 alkyl group optionally substituted by one or three fluorine atoms, C.sub.1-6 alkoxy group optionally substituted by one to three fluorine atoms, or C.sub.1-6 alkylthio optionally substituted by one to three fluorine atoms; R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or when R.sup.2 is adjacent to R.sup.1, they may be joined together such that there is formed a 5- or 6-membered saturated or unsaturated ring containing one or two oxygen atoms; R.sup.3 represents an optionally substituted 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur; m is 0-3 and n is 0-3, with the proviso that the sum total of m+n is 2 or 3; p is zero or 1; q is 1 or 2; and when m is 1 and n is 1 or 2, the broken line represents an optional double bond; R.sup.4, R.sup.5, R.sup.6, R.sup.9 and R.sup.
    Type: Grant
    Filed: May 18, 1998
    Date of Patent: May 9, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Timothy Harrison, Christopher John Swain, Brian John Williams
  • Patent number: 6054469
    Abstract: Compounds having formula I, or salts or prodrugs thereof: ##STR1## are selective agonists of the 5-HT.sub.1D.alpha. receptor and are useful in the treatment of migraine and associated conditions.
    Type: Grant
    Filed: April 29, 1998
    Date of Patent: April 25, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Sylvie Bourrain, Angus Murray MacLeod, Graham Andrew Showell
  • Patent number: 6054456
    Abstract: The present invention provides a compound of formula I, or a pharmaceutically acceptable salt thereof: ##STR1## wherein Z, E, Q, T, U, V and L are as defined herein; processes for its preparation and its use in the treatment of conditions for which the administration of an agonist selective for the 5-HT.sub.1D.alpha. receptor subtype is indicated, such as migraine.
    Type: Grant
    Filed: May 26, 1998
    Date of Patent: April 25, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Tamara Ladduwahetty, Angus Murray MacLeod, Michael Rowley
  • Patent number: 6051591
    Abstract: A class of 2,7-diazabicyclo[3.3.0]octane derivatives represented by formula I are selective agonists of the 5-HT.sub.1D.alpha. receptor. The compounds are useful in the treatment of migraine and related conditions.
    Type: Grant
    Filed: March 12, 1998
    Date of Patent: April 18, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Andrew Madin
  • Patent number: 6051572
    Abstract: A class of azetidine, pyrrolidine and piperidine derivatives, substituted by inter alia a phenylmorpholinyl, phenylpiperidinyl or benzimidazolone moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
    Type: Grant
    Filed: April 28, 1998
    Date of Patent: April 18, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Jose Luis Castro Pineiro
  • Patent number: 6048878
    Abstract: A compound of formula (I), or a salt or prodrug thereof, is described, wherein G is attached at position 3 or 4 of the piperidine ring and represents halogen or C.sub.1-6 alkoxy; R1 represents C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, aryl(C.sub.1-6)alkyl or heteroaryl (C.sub.1-6)alkyl, any of which groups may be optionally substituted; processes for its preparation and its use in therapy, particularly in the treatment of migraine.
    Type: Grant
    Filed: May 13, 1998
    Date of Patent: April 11, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Ian James Collins, Angus Murray MacLeod, Christopher Richard Moyes, Michael Rowley, Graham Andrew Showell
  • Patent number: 6046325
    Abstract: The present invention relates to a process for the preparation of a compound of formula (I): ##STR1## wherein R.sup.1 is a C.sub.1-6 alkyl or arylC.sub.1-4 alkyl group; and R.sup.2 is a hydrogen atom, a halogen atom, or a group selected from C.sub.1-6 alkyl, CF.sub.3 or C.sub.1-6 alkoxy substituted by C.sub.1-4 alkoxy; which comprises reacting an anhydrous or hydrated glyoxal of formula (II) with a compound of formula (III): ##STR2## in the presence of an acid.
    Type: Grant
    Filed: September 8, 1999
    Date of Patent: April 4, 2000
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Michael Stewart Ashwood, Brian Christopher Bishop, Ian Frank Cottrell
  • Patent number: 6046195
    Abstract: The present invention relates to certain spiro-azacyclic derivatives which are tachykinin antagonists and are useful, for example, in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
    Type: Grant
    Filed: March 23, 1999
    Date of Patent: April 4, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Karen Elizabeth Haworth, Eileen Mary Seward, Christopher John Swain
  • Patent number: 6046196
    Abstract: A class of substituted 7,8-ring fused 1,2,4-triazolo[4,3-b]pyridazine derivatives, as shown in Formula I possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and a substituted alkoxy moiety at the 6-position, are selective ligands for GABA.sub.A receptors, in particular having high affinity for the .alpha.2 and/or .alpha.3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of muscle spasm or spasticity, e.g. in paraplegic patients.
    Type: Grant
    Filed: December 9, 1998
    Date of Patent: April 4, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Franz Fridolin Hefti
  • Patent number: 6025374
    Abstract: A class of substituted azetidine, pyrrolidine and piperidine derivatives are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
    Type: Grant
    Filed: May 28, 1997
    Date of Patent: February 15, 2000
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventors: Jose Luis Castro Pineiro, Caroline Henry, Victor Giulio Matassa, Austin John Reeve, Francine Sternfeld, Leslie Joseph Street
  • Patent number: 5998416
    Abstract: A class of N-substituted piperazine, piperidine, and tetrahydropyridine derivatives, further subltitutedat the 4-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
    Type: Grant
    Filed: October 26, 1998
    Date of Patent: December 7, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Sylvie Bourrain, Angus Murray MacLeod, Graham Andrew Showell, Leslie Joseph Street
  • Patent number: 5998415
    Abstract: A class of piperazinones, homopiperazinones and thione analogues thereof, substituted at the 1-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, and linked at the 4-position via an alkylene spacer to a fused bicyclic heteroaromatic moiety, typically indolyl, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
    Type: Grant
    Filed: April 17, 1998
    Date of Patent: December 7, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Mark Stuart Chambers, Sarah Christine Hobbs, Leslie Joseph Street
  • Patent number: 5994374
    Abstract: A class of 1-[3-(1H-indol-3-yl)propyl]-4-benzyl-1,2,5,6-tetrahydropyridine derivatives, substituted at the 5-position of the indole nucleus by a 1,2,4-triazol-4-yl moiety, and on the methylene linkage of the benzyl moiety by an alkyl, alkoxy, or alkoxy-alkoxy substituent, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype while possessing at least a 10-fold selective affinity for the 5HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype. They are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D.alpha. receptors is indicated, and are expected to have fewer undesirable cardiovascular and other side effects.
    Type: Grant
    Filed: May 8, 1998
    Date of Patent: November 30, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Sylvie Bourrain, Angus Murray MacLeod, Joseph George Neduvelil, Graham Andrew Showell
  • Patent number: 5985874
    Abstract: The present invention relates to the compound of formula (I) or a pharmaceutically acceptable salt thereof.The compounds are of particular use in the treatment or prevention of pain or inflammation, migraine, emesis, postherpetic neuralgia, depression or anxiety.
    Type: Grant
    Filed: May 7, 1999
    Date of Patent: November 16, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Simon Neil Owen, Christopher John Swain, Brian John Williams
  • Patent number: 5985896
    Abstract: The present invention provides compounds of formula (I), wherein R.sup.1 is phenyl or a 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur, which aryl or heteroaryl group is optionally substituted; R.sup.2 is hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3, OCF.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 each independently represent hydrogen or C.sub.1-4 alkyl; R.sup.4, R.sup.5, R.sup.6, R.sup.9a and R.sup.9b, A, X, and Y are as defined in the specification; the dotted line is an optional double bond; Q.sup.1 is oxygen, sulphur or --NH--; Q.sup.2 is --N.dbd., --NH--, --CH.dbd. or --CH.sub.2 --; and m is zero or 1; and pharmaceutically acceptable salts and prodrugs thereof.
    Type: Grant
    Filed: December 18, 1997
    Date of Patent: November 16, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Jason Matthew Elliott, Graeme Irvine Stevenson, Christopher John Swain
  • Patent number: 5981526
    Abstract: The present invention relates to a method for the treatment or prevention of migraine, which method comprises administration to a patient in need of such treatment an amount of a tachykinin antagonist and an amount of rizatriptan such that together they give effective relief. There is also provided pharmaceutical compositions and products comprising a tachykinin antagonist and rizatriptan.
    Type: Grant
    Filed: October 3, 1997
    Date of Patent: November 9, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Richard John Hargreaves
  • Patent number: 5981529
    Abstract: A class of 1-[3-(1H-indol-3-yl)propyl]-4-(2-phenylethyl)piperazine derivatives, substituted at the 5-position of the indole nucleus by a five-membered heteroaromatic moiety, on one or other of the ethylene carbon atoms of the phenethyl moiety by halogen, trifluoromethyl, alkyl, hydroxyalkyl or alkoxyalkyl, and optionally on the phenyl ring of the phenethyl moiety by halogen, trifluoromethyl, alkoxy or an oxazolidinone group and optionally by one or two further substituents, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D .alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D .alpha. receptor subtype relative to the 5-HT.sub.1D .beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.
    Type: Grant
    Filed: March 18, 1998
    Date of Patent: November 9, 1999
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Raymond Baker, Mark Stuart Chambers, Sarah Christine Hobbs, Angus Murray MacLeod, Austin John Reeve, Francine Sternfeld, Leslie Joseph Street
  • Patent number: 5977104
    Abstract: The present invention provides methods for the treatment or prevention of bipolar disorder without concomitant therapy with other antidepressant or anti-anxiety agents which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such a NK-1 receptor antagonist.
    Type: Grant
    Filed: June 11, 1998
    Date of Patent: November 2, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Neil Roy Curtis, Jason Matthew Elliott, Timothy Harrison, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Nadia Melanie Rupniak, Eileen May Seward, Christopher John Swain, Brian John Williams
  • Patent number: 5977116
    Abstract: A class of N-substituted piperazine, piperidine and tetrahydropyridine derivatives, linked by a fluoro-substituted alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 4-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D recptor agonists.
    Type: Grant
    Filed: May 12, 1998
    Date of Patent: November 2, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Angus Murray MacLeod, Michael Rowley, Monique Bodil Van Niel
  • Patent number: 5973156
    Abstract: A class of substituted piperidine and tetrahydropyridine derivatives, linked through the 4-position thereof via an alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 1-position by an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl-alkyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.spsb..alpha. receptor subtype whilst processing at least a 10-fold selective affinity for the 5-HT.sub.1D.spsb..alpha. receptor subtype relative to the 5-HT.sub.1D.spsb..beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
    Type: Grant
    Filed: May 13, 1998
    Date of Patent: October 26, 1999
    Assignee: Merck Sharp & Dome Ltd.
    Inventors: Mark Stuart Chambers, Sarah Christine Hobbs, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant