1-Azabicyclo[3,2,2]nonane derivatives having 5-HT receptor antagonist activity

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United States of America Patent

PATENT NO 4798829
SERIAL NO

06896664

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: n is 1, 2, or 3; and m and p are independently 1 or 2 such that m+n+p.gtoreq.4; X is NH; or O when Ar is of formula (a) and R.sub.4 is hydrogen or when Ar is a heteroaromatic group which may be substituted; R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-6 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen; Ar is a group: ##STR2## wherein either R.sub.4 is C.sub.1-6 alkoxy and one of R.sub.5, R.sub.6, and R.sub.7 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O)n wherein n is 0, 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one of two groups selected from halogen, CF.sub.3, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or R.sub.4 is hydrogen and R.sub.5, R.sub.6 and R.sub.7 are independently selected from hydrogen, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio or halo; or any two on adjacent carbon atoms together are C.sub.1-2 alkylenedioxy and the third is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halo; or Ar is a heteroaromatic group which may be substituted; having gastric motility enhancing activity and/or anti-emetic activity and/or 5-HT antagonist activity, a process for their preparation and their use as pharmaceuticals.

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Patent Owner(s)

Patent OwnerAddress
BEECHAM GROUP PLCBRENTFORD MIDDLESEX TW8 9EP

International Classification(s)

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Joiner, Karen A Harlow, GB2 6 74
King, Francis D Harlow, GB2 39 667

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