mk-0429 and Osteoporosis

mk-0429 has been researched along with Osteoporosis* in 2 studies

Reviews

1 review(s) available for mk-0429 and Osteoporosis

Article	Year
Emerging targets in osteoporosis disease modification. Journal of medicinal chemistry, 2010, Jun-10, Volume: 53, Issue:11 Topics: Animals; Biomarkers; Bone Density; Bone Resorption; Humans; Osteoporosis	2010

Other Studies

1 other study(ies) available for mk-0429 and Osteoporosis

Article	Year
Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis. Journal of medicinal chemistry, 2003, Oct-23, Volume: 46, Issue:22 3(S)-(6-methoxypyridin-3-yl)-3-[2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)propyl]imidazolidin-1-yl]propionic acid 6 was identified as a potent and selective antagonist of the alpha(v)beta(3) receptor. This compound has an excellent in vitro profile (IC(50) = 0.08 nM), a significant unbound fraction in human plasma (12%), and good pharmacokinetics in rat, dog, and rhesus monkey. On the basis of the efficacy shown in three in vivo models of bone turnover, the compound was selected for clinical development. To support the ongoing metabolism and safety studies, a novel strategy was employed in which a series of oxidized derivatives of 6 were prepared by exposure of 6 (or the methyl ester) to chemical oxidizing agents. These products proved useful in the identification of active metabolites generated by either in vitro or in vivo metabolism. Topics: Animals; Bone Density; Bone Resorption; Dogs; Female; Humans; Integrin alphaVbeta3; Macaca mulatta; Male; Naphthyridines; Osteoporosis; Ovariectomy; Oxidation-Reduction; Propionates; Rats; Rats, Sprague-Dawley; Stereoisomerism; Structure-Activity Relationship	2003

Article

Year

Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis.

Journal of medicinal chemistry, 2003, Oct-23, Volume: 46, Issue:22

3(S)-(6-methoxypyridin-3-yl)-3-[2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)propyl]imidazolidin-1-yl]propionic acid 6 was identified as a potent and selective antagonist of the alpha(v)beta(3) receptor. This compound has an excellent in vitro profile (IC(50) = 0.08 nM), a significant unbound fraction in human plasma (12%), and good pharmacokinetics in rat, dog, and rhesus monkey. On the basis of the efficacy shown in three in vivo models of bone turnover, the compound was selected for clinical development. To support the ongoing metabolism and safety studies, a novel strategy was employed in which a series of oxidized derivatives of 6 were prepared by exposure of 6 (or the methyl ester) to chemical oxidizing agents. These products proved useful in the identification of active metabolites generated by either in vitro or in vivo metabolism.

Topics: Animals; Bone Density; Bone Resorption; Dogs; Female; Humans; Integrin alphaVbeta3; Macaca mulatta; Male; Naphthyridines; Osteoporosis; Ovariectomy; Oxidation-Reduction; Propionates; Rats; Rats, Sprague-Dawley; Stereoisomerism; Structure-Activity Relationship

2003