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filingDate 1995-08-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 1998-09-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4d93739b5ab79e3a579c19d6da88eaea
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publicationDate 1998-09-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-5811431-A
titleOfInvention Spiro-substituted azacyclic derivatives and their use as therapeutic agents
abstract The present invention relates to compounds of formula (I), wherein n is zero, 1, 2 or 3; R represents C 1-6 alkyl, C 1-6 alkoxy, hydroxy, halogen, cyano, trifluoromethyl SO 2 C 1-6 alkyl, NR a R b , NR a COR b or CONR a R b , where R a and R b are each H, C 1-4 alkyl, phenyl or trifluoromethyl; R 1 represents phenyl optionally substituted by 1, 2 or 3 of C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-7 cycloalkyl, C 3-7 cycloalkylC 1-4 alkyl, --O(CH 2 ) p O-- (where p is 1 or 2), halogen, cyano, nitro, trifluoromethyl, trimethylsilyl, OR a , SR a , SOR a , SO 2 R a , NR a R b , NR a COR b , NR a CO 2 R b , COR a , CO 2 R a or CONR a R b ; naphthyl; benzhydryl; or benyl, where the naphthyl group or each phenyl moiety of benzyl and benzhydryl may be substituted by C 1-6 alkyl, C 1-6 alkoxy, halogen or trifluoromethyl; R 2 represents hydogen, a substituent as defined for R 1 or heteroaryl selected from indazolyl, thienyl, furanyl, pyridyl, thiazolyl, tetrazolyl and quinolinyl; wherein each heteroaryl may be substituted by C 1-6 alkyl, C 1-6 alkoxy, halogen or trifluoromethyl; R 3 and R 4 are each H or C 1-6 alkyl or R 3 and R 4 together are linked so as to form a C 1-3 alkylene chain; R 5 represents H, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkylC 1-4 alkyl, phenylC 1-4 alkyl, CO 2 R a , CONR a R b , SOR a or SO 2 R a , wherein the phenyl moiety may be substituted by C 1-6 alkyl, C 1-6 alkoxy, halogen or trifluoromethyl; X and Y are each H, or together represents ═O; and Z represents a bond, O, S, SO, SO 2 , NR 6 , or --(CR 6 R 6 )-- where R 6 is H or C 1-6 alkyl; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia. ##STR1##
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Total number of triples: 729.