N-('-B-hydroxyethylpiperid-4-yl esters and amides

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United States of America Patent

PATENT NO 4853394
SERIAL NO

06926427

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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: Ar--CO--X--Y--Z--OR.sub.1 (I) wherein: Ar is a group of formula (a): ##STR1## wherein either R.sub.2 is C.sub.1-6 alkoxy and one of R.sub.3, R.sub.4 and R.sub.5 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, CX.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-6 alkoxy, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O)n wherein n is 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 or two groups selected from halogen, CF.sub.3, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or R.sub.2 is hydrogen and R.sub.3, R.sub.4 and R.sub.5 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; X is NH; when Ar is of formula (a) and R.sub.2 is hydrogen, Y is a group of formula (c), ##STR2## Z is C.sub.2 or C.sub.3 polymethylene optionally substituted by one or two C.sub.1-4 alkyl groups; and R.sub.1 is hydrogen or C.sub.1-6 alkyl or OR.sub.1 is an in vivo hydrolysable acyloxy group; having gastric motility enhancing activity, anti-emetic activity and/or 5-HT receptor antagonist activity, and their use as pharmaceuticals.

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Patent Owner(s)

Patent OwnerAddress
BEECHAM GROUP P L CSB HOUSE GREAT WEST ROAD BRENTFORD MIDDLESEX TW8 9BD

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
King, Francis D Harlow, GB2 39 667
Martin, Roger T Harlow, GB2 8 195
Watts, Eric A Harlow, GB2 11 275

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