| 摘要 |
PCT No. PCT/GB93/01648 Sec. 371 Date Jun. 23, 1995 Sec. 102(e) Date Jun. 23, 1995 PCT Filed Aug. 4, 1993 PCT Pub. No. WO94/03451 PCT Pub. Date Feb. 17, 1994Quinuclidine derivatives of formula, and their pharmaceutically acceptable salts, in which: R1 is hydrogen or hydroxy; R2 is hydrogen; pr 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-, -CH2S(O)n- and -S(O)nCH2- wherein n is 0, 1 or 2; and AR is phenyl which may be optionally unsubstituted or substituted by one or more substituents such as halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, dialkylamino, N-alkylcarbamoyl, N,N-di-alkylcarbamoyl, alkoxycarbonyl, alkythio, alkylsulphinyl, alkylsulphonyl, halogeno alkyl, alkanoylamino, alkylenedioxy, alkanoyl and oxime derivatives thereof and O-alkyl ethers of said oximes; provided that when X is selected from -OCH2-, -NHCH2-, and SCH2-, R1 is not hydroxy; inhibit squalene synthase and are useful in treating diseases or medical conditions in which inhibition of squalene synthase is desirable. The use of such heterocyclic derivatives in treating conditions such as hypercholesterolemia, and atherosclerosis is referred to as well as novel compounds, processes for their preparation and pharmaceutical compositions containing them. |
