发明名称 PYRIDYL- AND PYRIMIDYL-HETEROCYCLIC COMPOUNDS INHIBITING OXIDO SQUALENE-CYCLASE
摘要 This invention concerns heterocyclic derivatives which are useful in inhibiting oxido-squalene cyclase, processes for their preparation and pharmaceutical compositions containing them. The present invention is also concerned with heterocyclic derivatives capable of inhibiting cholesterol biosynthesis and hence in lowering cholesterol levels in blood plasma. The present invention also relates to methods of using such heterocyclic derivatives in treating or preventing diseases and medical conditions such as hypercholesterolemia, atherosclerosis and other medical conditions associated elevated cholesterol levels. In formula (I), G is selected from CH or N; R1 is selected from hydrogen, halogeno, (1-6C)alkyl, halogeno(1-6C)alkyl, cyano, nitro, (1-6C)alkoxycarbonyl, and NR<3>R<4> wherein R<3> and R<4> are independently selected from hydrogen and (1-6C)alkyl, and wherein up to 3 R1 groups may be present; T1 is selected from CH or N; T2 and T3 are independently selected from N and CR, wherein R is selected from hydrogen, hydroxyl and (C1-4)alkyl and wherein either ring containing T2 or T3 is optionally substituted with an oxo group; R2 is selected from hydrogen or (1-4C)alkyl; Q is selected from SO2, CO and CH2; Ar is selected from a five or six-membered heterocycle containing up to 3 heteroatoms selected from nitrogen, oxygen and sulphur, phenyl, phenyl (2-6C)alkenyl and naphthyl in which any Ar group is optinally substituted by one or more substituents selected from (1-6C)alkyl, halogeno, halogeno (1-6C)alkyl, (1-6C)alkoxy, (1-6C)alkoxycarbonyl, cyano, (1-6C)alkylamido, nitro, NR<3>R<4> wherein R<3> and R<4> are independently selected from hydrogen and (1-4C)alkyl; provided that both T2 and T3 are not N and that when T2 si CR then T1 si not CH.
申请公布号 WO9906395(A1) 申请公布日期 1999.02.11
申请号 WO1998GB02196 申请日期 1998.07.23
申请人 ZENECA LIMITED;NEWCOMBE, NICHOLAS, JOHN;JOHNSON, MICHAEL, CLYDE 发明人 NEWCOMBE, NICHOLAS, JOHN;JOHNSON, MICHAEL, CLYDE
分类号 A61K31/4427;A61K31/4545;A61K31/496;A61K31/506;A61P3/06;A61P9/10;C07D401/04;C07D401/06;C07D401/12;C07D401/14;(IPC1-7):C07D401/06;A61K31/495;A61K31/505 主分类号 A61K31/4427
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