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Original Article

Patent Update: ACAT Inhibitors

Pages 151-160 | Published online: 03 Mar 2008

References

  • FRICK MH, ELO H, HAAPA K et al.: HelsinkiHeart Study: primary prevention trial with gemfibrozil in middle aged men with dyslip-idaemia. N. Engl. J. Med. (1987) 317:1237.
  • O'BRIEN PM, SusKovic DR: ACAT in-hibitors: A potential new approach to the treatment of hypercholesterolaemia and ath-erosclerosis. Curr Opin. Thera. Patents (1992) 2:507.
  • SLISKOVIC DR, WHITE AD: Therapeutic po-tential of ACAT inhibitors as lipid lowering and anti-atherosclerotic agents. Trends Phar-macol. Sci. (1990) 12:194.
  • An excellent review covering ACAT inhibitors and their therapeutic potential.
  • MCCARTHY PA, HAMANAKA ES, MARZETTA CA et al.: CP-113,818 and CP105,191 are po-tent and selective inhibitors of acyl Coen-zyme A:cholesterol acyl transferase (ACAT). I I th International Symposium on Drugs Affect-ing Lipid Metabolism. Florence, Italy (1992) pp.113.
  • INSICEEP PB, CONNOLLY AG, DAVIS KM: •Pharmacokinetics in beagle dogs of CP-105,191 and CP-113,818, potent inhibitors of acyl coenzyme A:cholesterol acyl trans-ferase (ACAT). I I th International Symposium on Drugs Affecting Lipid Metabolism. Flo-rence, Italy (1992) pp.88.
  • An interesting bioavailabifity study of Pfizer's ACAT in-hibitors.
  • PARROTT DP, BRIGHT CP, BURTON B, RIDDELL D, Sims AFG: RP64477: a potent in-hibitor of ACAT in human cells. 11th Inter-national Symposium on Drugs Affecting Lipid Metabolism. Florence, Italy (1992) pp.89.
  • SLISKOVIC DR, PICARD JA, ROARK WH et al.: Malonester amide ACAT inhibitors: synthe-sis and biological activity. 204th ACS Meet-ing. Washington DC (1992) MEDI 38.
  • YAMADA K, ODA S, SHIRAKURA S et al.: KF-17828: a novel inhibitor of acyl CoA choles-terol acyl transferase (ACAT). 11th Inter-national Symposium on Drugs Affecting Lipid Metabolism. Florence, Italy (1992) pp.89.
  • MOCHIZUKI T, TANABE H, OTA M et al.: A potent acyl-CoA:cholesterol acyl trans-ferase (ACAT) inhibitor with inhibitory ac-tivity toward macrophage foam cell forma-tion in vitro and anti-hypercholesterolemic effect in vivo. 11th International Symposium on Drugs Affecting Lipid Metabolism. Florence, Italy (1992) pp.89.
  • WILDE RG, BILLHEIMER JT, GILLEES PJ et • at.: Acyl CoA-cholesterol acyltransferase (ACAT) inhibitors: imidazole ureas with ether and amine linking elements. 204th ACS Meeting. Washington DC (1992) MEDI 18.
  • Discussion of DuP128, newer analogues, and approaches to bioavailable compounds.
  • MADUSKLTIE TP, BILLHEIMER J, GILLIES PJ et al.: Design, synthesis and structure ac-tivity relationship studies for a new imida-zole series of J774 macrophage specific acyl-CoA:cholesterol acyl transferase (ACAT) inhibitors. 204th ACS Meeting. Washington DC (1992) MEDI 39.
  • MADUSKUIE TP, BILLHEIMER 3, GILLEES PJ et al.: Design, synthesis and structure activ-ity relationship of a new diphenylamide and phenolic series of acyl-CoA:cholesterol acyl transferase (ACAT) inhibitors. 204th ACS Meeting. Washington DC (1992) MEDI 40.
  • WILDE RG, BILLHEIMER JT, GIMES PJ et al.: Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: ureas bearing hetero-cyclic groups bioisosteric for an imidazole. 204th ACS Meeting. Washington DC (1992) MEDI 41.
  • KOGUSHI M, OHTSUKA I, TANAKA H et al.: E5324: a potent and novel inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT). 11th International Symposium on Drugs Affecting Lipid Metabolism. Florence, Italy (1992) pp.88.
  • NOSE K, HAYASI K, IwAsE T, SAWA Y, HOFUE T: Pharmacokinetics and metabolic fate of the acyl-CoA:cholesterol acyl transferase (ACAT) inhibitor N-butyl-N'4243-(5-ethyl-4-phenyl-1H-imidazole-1-yl)propoxy]-6-me-thyl-phenyllurea, E5324. 11th International Symposium on Drugs Affecting Lipid Metabo-lism. Florence, Italy (1992) pp.89.
  • TANAKA H, OHTSUKA I, KOGUSHI M et al.: Ef-fect of a novel ACAT inhibitor (E5324) on the experimental atherosclerosis in rabbits. 11th International Symposium on Drugs Affect-ing Lipid Metabolism. Florence, Italy (1992) pp.89.
  • WHILE AD, CRESWELL MC, ESSENBURG AD et at.: Heterocyclic ureas potent inhibitors of acyl CoA:cholesterol acyltransferase (ACAT). Part 2. 203rd ACS Meeting. San Francisco (1992) MEDI 141.
  • WHITE AD, CRESWELL MC, WILSON MW et at.: Heterocyclic ureas potent inhibitors of acyl CoA:cholesterol acyltransferase (ACAT). Part 3. 203rd ACS Meeting. San Francisco (1992) MEDI 142.
  • O'BRIEN PM, SLISKOVIC DR, WILSON MW et at.: Novel ACAT inhibitors derived from amino acids: synthesis and biological activ-ity. 203rd ACS Meeting. San Francisco (1992) MEDI 140.
  • O'BRIEN PM, SLISKOVIC DR, BLANKLEY CJ et al.: ACAT inhibitors: urea derivatives con-taining alkyl substituted amide or amine functionalities. 201st ACS Meeting. Atlanta (1991) MEDI 119.
  • O'BRIEN PM, SLISKOVIC DR, BLANKLEY CJ et at.: ACAT inhibitors: urea derivatives con-taining aryl or heteroaryl substituted amide or amine functionalities. 201st ACS Meeting. Atlanta (1991) MEDI 120.
  • PICARD JA, HAMELEHLE KL, KRAUSE BR et at.: The synthesis and biological evalua-tion of several series of acyl-CoA:cholesterol acyl transferase (ACAT) inhibitors derived from N-(chlorocarbonyl) isocyanate. 204th ACS Meeting. Washington DC (1992) MEDI 42.
  • PROZIALECK DE, FOBARE WF, MCKEAN ML, ADELMAN SJ: Inhibition of cellular choles-terol (C) esterification and hypercholes-terolemia (hyperC) by Meldrum's acid deriva- •• fives - novel inhibitors of acylCoA-choles-terol acyltransferase (A CAT). FASEB J. (1992) 6:1388.
  • FOBARE WF, MCKEAN ML, LEE MC et al.: •• WAY-125,147: a novel inhibitor of acyl-CoA: cholesterol acyl-transferase (A CAT) which also inhibits LDL modification. 11th International Symposium on Drugs Affect-ing Lipid Metabolism. Florence, Italy (1992) pp.113.
  • Novel modification of ureas that retains ACAT activity.

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