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Publication number: 20120149679Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.Type: ApplicationFiled: February 20, 2012Publication date: June 14, 2012Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Publication number: 20130338111Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.Type: ApplicationFiled: August 16, 2013Publication date: December 19, 2013Applicants: Icagen, Inc., Pfizer LimitedInventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Publication number: 20100197655Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.Type: ApplicationFiled: January 12, 2010Publication date: August 5, 2010Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Patent number: 5830892Abstract: The present invention provides compounds of formula (I), wherein R.sup.1 is a 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms selected from nitrogen, oxygen and sulphur, which 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 substitued by C.sub.1-4 alkoxy, where R.sup.a and R.sup.a R.sup.b each independently represent hydrogen or C.sub.1-4 alkyl; R.sup.3 is hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 -alkoxy substituted by C.sub.1-4 alkoxy or CF.sub.3 ; R.sup.4, R.sup.5, R.sup.6, R.sup.9a, R.sup.9b, A, X and Y are as defined in the specification; and m is zero or , and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and pos therpetic neuralgia.Type: GrantFiled: December 18, 1997Date of Patent: November 3, 1998Assignee: Merck Sharp & Dohme Ltd.Inventors: Raymond Baker, Jason Matthew Elliott, Graeme Irvine Stevenson, Christopher John Swain
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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