- Methods of using α-phosphonosulfonate squalene synthetase inhibitors including the treatment of atherosclerosis and hypercholesterolemia
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α-Phosphonosulfonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula STR1 wherein R2 is OR5 or R5a ; R3 and R5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R5a is H, alkyl, arylalkyl or aryl; R4 is H, alkyl, aryl, arylalkyl, or cycloalkyl;, Z is H, halogen, lower alkyl or lower alkenyl; and R1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts and or prodrug esters of the phosphonic (phosphinic) and/or sulfonic acids.
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- Synthesis and Liquid Crystal Behaviour of Further 4,4"-Disubstituted 2'-Fluoro-1,1':4',1"-Terphenyls
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Further to earlier work on the liquid crystal properties of fluoro-1,1':4',1"-terphenyls we have now extended this series to include terminally fluoro- and cyano-substituted 2'-fluoro-1,1':4',1"-terphenyls, chiral 2'-fluoro-1,1':4',1"-terphenyls, and esters derived from 2'-fluoro-1,1':4',1"-terphenyls and incorporating the alkylcyclobutyl group.The preparations and transition temperatures for these series of compounds are presented and their transition temperatures and mesophase types are discussed.An interesting result from this work was the appearence of an S*C phase for one chiral homologue and of SC phases for the esters incorporating the alkylcyclobutyl group.The SC formation is attributed to the presence of the fluoro-substituent.Keywords: terphenyls, fluoroterphenyls, smectic C phases, cyclobutyl esters.
- Chan, L. K. M.,Gray, G. W.,Lacey, D.,Toyne, K. J.
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p. 209 - 240
(2007/10/02)
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