| 摘要 |
HETEROCYCLIC DERIVATIVES Quinuclidine derivatives of formula I, and their pharmaceutically acceptable salts, in which R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 are joined together so that CR1-CR2 is a double bond; Ar1 is a phenylene moiety; Ar2 is a 6-membered heteroaryl moiety containing one or two nitrogen atoms; and wherein one or both of Ar1 and Ar2 may optionally bear one or more substituents such as halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, di-alkylamino, N-alkylcarbamoyl, di-N,N-alkylcarbamoyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, alkanoylamino, alkylenedioxy, alkanoyl and oxime derivatives thereof and 0-alkyl ethers of said oxime derivatives; inhibit squalene synthase and are therefore useful in treating treating diseases and medical conditions where inhibition of squalene synthase is desirable, for example in treating hypercholesterolemia and atherosclerosis. Processes for the preparation of these derivatives and pharmaceutical compositions containing them are also referred to as well as their use in medicine.
|
