C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 453/02 (2006.01) A61K 31/435 (2006.01)
Patent
CA 2085913
ABSTRACT HETEROCYCLIC DERIVATIVES Quinuclidine compounds of the formula I: Image R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 are joined together so that CR1-CR2 is a double bond; X is selected from -CH2CH2-, -CH=CH-, -C?C-, -CH2O-, -OCH2-, -CH2NH-, -NHCH2-, -CH2CO-, -COCH2-, -CH=N-, -N=CH-, -CH2S-, -SCH2-, wherein the sulphur atom in the latter two groups may optionally bear one or two oxygen atoms; and wherein one or both of ring A and ring B may be optionally unsubstituted or independently substituted by one or more substituents selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkoxy, alkylamino, di-alkyl]amino, N-alkyl]carbamoyl, N,N-di-alkyl]carbamoyl, alkoxycarbonyl, alkylthic, alkylsulphinyl, alkylsulphonyl and halogeno-alkyl; are inhibitors of squalene synthase and are hence useful in treating diseases or medical conditions such as hypercholesterolemia, atherosclerosis and fungal diseases. Methods of using these compounds to treat such conditions, novel compounds, processes for making these compounds and pharmaceutical compositions containing them are claimed.
Brown George R.
Harrison Peter J.
Mallion Keith B.
Imperial Chemical Industries Plc
Smart & Biggar
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