Author/Authors :
Karen E Sexton، نويسنده , , Helen T Lee، نويسنده , , Mark Massa، نويسنده , , Janak Padia، نويسنده , , William C. Patt، نويسنده , , Peggy Liao، نويسنده , , Jason K Pontrello، نويسنده , , Bruce D. Roth، نويسنده , , Mark A. Spahr، نويسنده , , Randy Ramharack، نويسنده ,
Abstract :
Compounds of the general structure A and B were investigated for their activity as lipoprotein(a), [Lp(a)], assembly (coupling) inhibitors. SAR around the amino acid derivatives (structure A) gave compound 14-6 as a potent coupling inhibitor. Oral dosing of compound 14-6 to Lp(a) transgenic mice and cymologous monkeys resulted in a>30% decrease in plasma Lp(a) levels after 1–2 weeks of treatment at 100 mg/kg/day.
