Abstract: A pharamceutical composition comprises a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein A is C1-6alkyl, C2-6alkenyl, C2-6-alkynyl, C3-6-cycloalkyl, arylC1-6alkyl, aryl, S(O)pR1.
Type:
Grant
Filed:
April 16, 1999
Date of Patent:
July 17, 2001
Assignee:
Merck Sharp & Dohme Limited
Inventors:
Howard Barff Broughton, Mark Stewart Chambers, Sarah Christine Hobbs, Angus Murray MacLeod, Austin John Reeve
Abstract: Substituted triazolo-pyridazine derivative compounds represented by
wherein the variables are disclosed herein are selective ligands for GABA-A receptors, particularly for the &agr;2 and/or &agr;3 subunits.
Type:
Grant
Filed:
November 10, 1998
Date of Patent:
July 3, 2001
Assignee:
Merck Sharp & Dohme Limited
Inventors:
Howard Barff Broughton, William Robert Carling, Jose Luis Castro Pineiro, Alexander Richard Guiblin, Andrew Madin, Kevin William Moore, Michael Geoffrey Russell, Leslie Joseph Street
Abstract: This system comprises a compacted bag, in particular under vacuum, having an appendage into which a spacer device is inserted (2) which forms a pocket (140) separating two facing flexible partition sections from each other (120,121) of which one (121) is adapted to be applied when placed under vacuum against a set of heatable blades with closed outline linked to each other (51, 61) the interior blade (61) being carried by a mobile part (6) of which the end is able to penetrate into the cut pocket (140) with a view to the inflation of the bag with air brought by a channel (600′) through a sterilizing filter (8).
Abstract: Substituted spiro-azacyclic derivatives of structural formula I are tachykinin receptor antagonists of use, for example, in the treatment of pain, inflammation, migraine, emesis and posttherpetic neuralgia
Wherein A is a pyridyl, X is —CH2—, Y is —CH2— or —CH═ and q is 2.
Type:
Grant
Filed:
November 18, 1999
Date of Patent:
May 1, 2001
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Janusz Jozef Kulagowski, Piotr Antoni Raubo, Christopher John Swain, Christopher George Thomson
Abstract: The present invention relates to compounds of formula (I), wherein R1 represents a fluoroC1-2alkoxy group; and R2 represents a hydrogen or halogen atom or a C1-4alkyl, C1-4alkoxy, fluoroC1-4alkyl or fluoroC1-4alkoxy group; 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.
Abstract: A class of substituted aminocyclohexane derivatives are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1D&agr; receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT1D&agr; receptor subtype relative to the 5-HT1D&bgr; 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-HT1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.
Type:
Grant
Filed:
January 4, 1999
Date of Patent:
April 3, 2001
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Angus Murray MacLeod, Graham Andrew Showell, Leslie Joseph Street
Abstract: Substituted 1,2,4-Triazolo[3,4-A]phthalazine derivatives are GABA Alpha 5 ligands and are represented by the formula
Type:
Grant
Filed:
November 12, 1998
Date of Patent:
March 13, 2001
Assignee:
Merck Sharp & Dohme Limited
Inventors:
William Robert Carling, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Kevin William Moore, Francine Sternfeld, Leslie Joseph Street
Abstract: Three classes of indole and indoline derivatives are disclosed as ligands selective for the 5-HT6 receptors, and hence of value in the treatment or prevention of CNS disorders, including Alzheimer's disease, Parkinson's disease, schizophrenia, depression and anxiety. A particular class, 1-substituted-4-(&ohgr;-N,N-dialkyl-aminoalkyl)indoles, are claimed as novel compounds.
Type:
Grant
Filed:
September 9, 1999
Date of Patent:
February 13, 2001
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Jose Luis Castro Pineiro, George Mc Allister, Michael Geoffrey Neil Russel
Abstract: Pyrazolo[4,3-c]pyridazin-3-one analogues, represented by
are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, are useful in the treatment of anxiety and convulsions.
Abstract: This invention relates to methods and compositions for treating pain and nociception in a patient by administering a combination of a morpholine or thiomorpholine tachykinin antagonist and an opioid analgesic.
Abstract: A class of substituted or 7,8-ring fused 1,2,4-triazolo[4,3-b]pyridazine derivatives, 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 GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders including schizophrenia.
Type:
Grant
Filed:
November 12, 1998
Date of Patent:
January 16, 2001
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Jose Luis Castro Pineiro, Ruth McKernan, Paul John Whiting
Abstract: The present invention is directed to substituted spiro-azacyclic derivatives of the formula (I):
(wherein R1, R2, R3, R4, R5, R6, R9, R10, X, Y, p and q are defined herein) 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:
October 22, 1999
Date of Patent:
January 9, 2001
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Neil Roy Curtis, Jason Matthew Elliott, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Eileen Mary Seward, Christopher John Swain, Brian John Williams
Abstract: The present invention relates to the use of an NK-1 receptor antagonist and a selective serotonin reuptake inhibitor for the treatment or prevention of obesity.
Abstract: The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 antagonist for the manufacture of a medicament for oral administration for the treatment or prevention of movement disorders, methods of treatment using such a NK-1 receptor antagonist and pharmaceutical compositions comprising it.
Abstract: There is disclosed a method for increasing retinal and optic nerve head oxygen tension by application of a composition comprising carbonic anhydrase inhibitors to the eye.
Type:
Grant
Filed:
January 19, 1999
Date of Patent:
December 5, 2000
Assignee:
Merck Sharp & Dohme B.V.
Inventors:
Einae Stefansson, Jens Dollerup, Kurt Bang
Abstract: The present invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof: ##STR1## where A is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, arylC.sub.1-6 alkyl, aryl, S(O),R.sup.1, OR.sup.1 or NR.sup.1 R.sup.6 ;R.sup.1 is hydrogen; C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkenyl each of which is optionally substituted by amino, C.sub.1-6 alkylamino, di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkoxy, C.sub.1-6 alkylaminocarbonyl, one, two or three hydroxy groups, one, two or three halogen atoms or a four, five or six-membered saturated heterocyclic ring containing a nitrogen atom and optionally either an oxygen atom or a further nitrogen atom which ring is optionally substituted by C.sub.1-4 alkyl on the further nitrogen atom; aryl, arylC.sub.1-6 alkyl, arylC.sub.2-6 alkenyl or arylC.sub.2-6 alkynyl optionally substituted on the aryl ring by halogen, nitro, cyano, C.sub.
Type:
Grant
Filed:
April 22, 1999
Date of Patent:
December 5, 2000
Assignee:
Merck Sharp & Dohme Limited
Inventors:
Howard Barff Broughton, Mark Stuart Chambers
Abstract: Compounds having formula I, or pharmaceutically acceptable 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:
July 21, 1998
Date of Patent:
November 21, 2000
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Jose Luis Castro Pineiro, Michael Geoffrey Russell
Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein A is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, arylC.sub.1-6 alkyl, aryl, S(O).sub.p R.sup.1, OR.sup.1 or NR.sup.1 R.sup.12 ;B is optionally substituted 5- or 6-membered heteroaromatic ring or C(O)NR.sup.10 R.sup.11 ;R.sup.1 is hydrogen, optionally substituted C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkenyl, optionally substituted aryl, arylC.sub.1-6 alkyl, arylC.sub.2-6 alkenyl or arylC.sub.2-6 alkynyl or an optionally substituted 5- or 6-membered heteroaromatic ring;R.sup.2 and R.sup.3 are hydrogen or C.sub.1-6 alkyl;R.sup.4 is hydrogen, C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, aryl or CH.sub.2 (CO).sub.m NR.sup.8 R.sup.9 ;R.sup.5 is NR.sup.6 R.sup.7, C.sub.1-6 alkyl or C.sub.1-6 alkoxy;R.sup.6 is independently as defined for R.sup.4 ;R.sup.
Type:
Grant
Filed:
April 22, 1999
Date of Patent:
November 7, 2000
Assignee:
Merck Sharp & Dohme Limited
Inventors:
Howard Barff Broughton, Mark Stuart Chambers
Abstract: The present invention relates to the use of a tachykinin antagonist and a muscarinic antagonist and/or an antihistamine for the treatment or prevention of motion sickness. There is also provided pharmaceutical compositions and products comprising a tachykinin antagonist and a muscarinic antagonist and/or an antihistamine.
Abstract: A class of compounds of formula (I) wherein Z, E, Q, T, U, V, W, M, R.sup.1, R.sup.7 and R.sup.8 are as defined herein; 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 14, 1998
Date of Patent:
October 31, 2000
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Jose Luis Castro Pineiro, Andrew Madin, Joseph George Neduvelil, Graham Andrew Showell, Leslie Joseph Street, Monique Bodil Van Niel