BIPHENYLYLQUINUCLIDINE DERIVATIVES AS SQUALENE SYNTHASE INHIBITORS

摘要

Biphenylylquinuclidine derivatives of Formula (I): Q-Ar1-Ar2, in which Q is of Formula (Ia) or (Ib), in which R?1 and R2¿ are independently selected from hydrogen, alkyl, halogeno and hydroxy; or R?1 and R2¿ when taken together define an oxo group; Xb is selected from -CH¿2?-, =CH- and -CH(OH); Xa is selected from -CH2-, =CH-, CO, -O-, and -S(O)n (wherein n = 0, 1 or 2); Ar?1¿ is a phenylene moiety; Ar2 is phenyl; and wherein one or both of Ar?1 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 pharmaceutically acceptable salts are inhibitors of squalene synthase and hence useful in treating diseases and medical conditions in which a lowering of cholosterol is desirable. The use of these derivatives in medicine is disclosed together with novel compounds, processes for their preparation and pharmaceutical composition containing them.