Heterocyclic derivatives

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United States of America Patent

PATENT NO 5919793
SERIAL NO

08537827

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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Compounds of formula (I) wherein R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen; or R.sup.1 and R.sup.2 are joined together so that CR.sup.1 14 CR.sup.2 is a double bond; X is selected from --Ch.sub.2 CH.sub.2 --, --C.dbd.CH--, --C.tbd.C--, --CH.sub.2 O--, --OCH.sub.2, CH.sub.2 NH--, --NHCH.sub.2 --, --CH.sub.2 CO--, --COCH.sub.2 --, --CH.sub.2 S(O).sub.n -- and --S(O).sub.n CH.sub.2 -- (wherein n is 0, 1 or 2); Ar is phenyl which bears one or more substituents independently selected from the groups (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (1-6C)alkoxy, (1-6C)alkoxycarbonyl, (1-6C)alkoxycarbonyl(1-6C)alkyl, (1-6C)alkoxy(1-6C)alkyl, (1-6C)alkylamino, di-?(1-6C)alkyl!amino, carbamoyl, (1-6C) alkylcarbamoyl, di-?(1-6C)alkyl!carbamoyl, (1-6C)alkenyl and oxime derivatives thereof and O--(1-6C)alkyl ethers of said oximes (1-6C)alkylthio, (1-6C)alkylsulphinyl and (1-6C)alkylsulphonyl when substituted by one or more groups selected from (1-6C)alkoxycarbonyl, (1-6C)alkanoyl and oxime derivatives thereof and O-(1-6C)alkyl ethers of said oxime derivatives, (1-6C)alkanoylamimo, (1-6C)alkanoyloxy, (1-6C)alkanoyloxy(1-6)alkyl, carbamoyl, N-(1-6C)alkylcarbamoyl, N,N-di?(1-6C)alkyl!carbamoyl, amino, (1-6C)alkylamino, di-?(1-6C)alkyl!amino, (1-6C)alkoxy, (2-6C)alkenyloxy, (1-6C)alkylthio, (1-6C)alkylsulphinyl, (1-6C)alkylsulphonyl, halogeno(1-6C)alkyl (2-6C)alkenyl, (2-6C)alkynyl, phenyl, phenoxy, cyano, nitro, hydroxy and carboxy; and wherein Ar may bear further substituents; and their pharmaceutically acceptable salts inhibit squalene synthese and are hence useful in lowering cholesterol levels in blood plasma Processes for preparing compounds of formula (I) are also referred to as well as pharmaceutical compositions containing them and their use in medicine.

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Patent Owner(s)

Patent OwnerAddress
ASTRAZENECA UK LIMITED1 FRANCIS CRICK AVENUE CAMBRIDGE BIOMEDICAL CAMPUS CAMBRIDGE CB2 0AA UNITED KINGDOM

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Brittain, David Robert Bamford, GB 4 42
Brown, George Robert Wilmslow, GB 13 192
Whittamore, Paul Robert Owen Macclesfield, GB 27 175

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