C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 453/02 (2006.01) A61K 31/435 (2006.01)
Patent
CA 2093778
A B S T R A C T HETEROCYCLIC COMPOUNDS Biphenylylquinuclidine derivatives of formula I, Q-Ar1-Ar2, in which Q is of formula Ia or I b, Ia Image Ib in which R1 and R2 are independently selected from hydrogen, alkyl, halogeno and hydroxy; or R1 and R2 when taken together define an oxo group; Xb is selected from -CH2-, =CH- and -CH(OH); Xa is selected from -CH2-, =CH-, CO, -O-, and -S(O)n (wherein n = 0, 1 or 2); Ar1 is a phenylene moiety; Ar2 is phenyl; and wherein one or both of Ar1 and Ar2 is optionally unsubstituted or substituted by one or more substituents independently selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, di-alkylamino, N-carbamoyl, N,N-di-alkylcarbamoyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, halogeno-alkyl, alkanoyl and alkanoylamino; and their pharamaceutically acceptable salts are inhibitors of squalene synthase and hence useful in treating diseases and medical conditions in which a lowering of cholesterol is desirable. The use of these derivatives in medicine is disclosed tohether with novel compounds, processes for their preparation and pharmaceutical composition containing them.
Brown George R.
Harrison Peter J.
Mallion Keith B.
Smart & Biggar
Zeneca Limited
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