Heterocyclic derivatives

• Main Authors: BRITTAIN; DAVID ROBERT, WHITTAMORE; PAUL ROBERT OWEN, BROWN; GEORGE ROBERT
• Format: Patent
• Language: English
• Published: 06.07.1999
• Edition: 6
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

PCT No. PCT/GB94/00910 Sec. 371 Date Oct. 26, 1995 Sec. 102(e) Date Oct. 26, 1995 PCT Filed Apr. 28, 1994 PCT Pub. No. WO94/25459 PCT Pub. Date Nov. 10, 1994Compounds of formula (I) wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 are joined together so that CR114 CR2 is a double bond; X is selected from -Ch2CH2-, -C=CH-, -C 3BOND C-, -CH2O-, -OCH2, CH2NH-, -NHCH2-, -CH2CO-, -COCH2-, -CH2S(O)n- and -S(O)nCH2- (wherein n is 0, 1 or 2); Ar is phenyl which bears one or more substituents independently selected from the groups (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (1-6C)alkoxy, (1-6C)alkoxycarbonyl, (1-6C)alkoxycarbonyl(1-6C)alkyl, (1-6C)alkoxy(1-6C)alkyl, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, carbamoyl, (1-6C) alkylcarbamoyl, di-[(1-6C)alkyl]carbamoyl, (1-6C)alkenyl and oxime derivatives thereof and O-(1-6C)alkyl ethers of said oximes (1-6C)alkylthio, (1-6C)alkylsulphinyl and (1-6C)alkylsulphonyl when substituted by one or more groups selected from (1-6C)alkoxycarbonyl, (1-6C)alkanoyl and oxime derivatives thereof and O-(1-6C)alkyl ethers of said oxime derivatives, (1-6C)alkanoylamimo, (1-6C)alkanoyloxy, (1-6C)alkanoyloxy(1-6)alkyl, carbamoyl, N-(1-6C)alkylcarbamoyl, N,N-di[(1-6C)alkyl]carbamoyl, amino, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, (1-6C)alkoxy, (2-6C)alkenyloxy, (1-6C)alkylthio, (1-6C)alkylsulphinyl, (1-6C)alkylsulphonyl, halogeno(1-6C)alkyl (2-6C)alkenyl, (2-6C)alkynyl, phenyl, phenoxy, cyano, nitro, hydroxy and carboxy; and wherein Ar may bear further substituents; and their pharmaceutically acceptable salts inhibit squalene synthese and are hence useful in lowering cholesterol levels in blood plasma Processes for preparing compounds of formula (I) are also referred to as well as pharmaceutical compositions containing them and their use in medicine.