Hypolipidaemic condensed 1,4-thiazepines

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United States of America Patent

PATENT NO 5817652
SERIAL NO

08505232

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The invention provides a compound of formula (I), wherein n is an integer of from 0 to 2; R is an optional substituent; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is an atom or group selected from hydrogen, C.sub.1-4 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.1-4 alkoxy, pyrryl, thienyl, pyridyl, 1,3-benzodioxolo, phenyl and naphthyl, which groups are optionally substituted; R.sup.3 is hydrogen, OH, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or --O C.sub.1-6 acyl; R.sup.4 is a group independently selected from C.sub.1-6 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.2-6 alkenyl, and C.sub.2-6 -alkynyl which groups are optionally substituted; R.sup.5 is a group independently selected from C.sub.2-6 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.2-6 alkenyl and C.sub.2-6 alkynyl, which groups are optionally substituted; or R.sup.4 and R.sup.5, together with the carbon atom to which they are attached, form a C.sub.3-7 spiro cycloalkyl group which is optionally substituted; R.sup.6 and R.sup.7 are independently selected from hydrogen and C.sub.1-6 alkyl; and X is an aromatic or non-aromatic monocyclic or bicyclic ring system having from 5 to 10 carbon atoms (including the two carbon atoms forming part of the thiazepine ring) wherein optionally one or more of the carbon atoms is/are replaced by heteroatom(s) independently selected from nitrogen, oxygen and sulphur, or X is an aromatic or non-aromatic monocyclic or bicyclic ring system having from 5 to 10 carbon atoms (including the two carbon atoms forming part of the thiazepine ring) wherein one or more of the carbon atoms is/are replaced by heteroatom(s) independently selected from nitrogen, oxygen and sulphur; and salts, solvates and physiologically functional derivatives thereof, pharmaceutical formulations comprising such compounds, processes for their preparation and their use in reducing bile acid uptake and hence as hypolipidaemic compounds. ##STR1##

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Patent Owner(s)

Patent OwnerAddress
BURROUGHS WELLCOME COA CORP OF NC RESEARCH TRIANGLE PARK NC

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Brieaddy, Lawrence Edward Raleigh, NC 6 290
Hodgson, Jr Gordon Lewis Durham, NC 3 171

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