757247-82-8Relevant academic research and scientific papers
N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation
Nirschl, Alexandra A.,Zou, Yan,Krystek Jr., Stanley R.,Sutton, James C.,Simpkins, Ligaya M.,Lupisella, John A.,Kuhns, Joyce E.,Seethala, Ramakrishna,Golla, Rajasree,Sleph, Paul G.,Beehler, Blake C.,Grover, Gary J.,Egan, Donald,Fura, Aberra,Vyas, Viral P.,Li, Yi-Xin,Sack, John S.,Kish, Kevin F.,An, Yongmi,Bryson, James A.,Gougoutas, Jack Z.,DiMarco, John,Zahler, Robert,Ostrowski, Jacek,Hamann, Lawrence G.
supporting information; experimental part, p. 2794 - 2798 (2010/02/28)
A novel selective androgen receptor modulator (SARM) scaffold was discovered as a byproduct obtained during synthesis of our earlier series of imidazolidin-2-ones. The resulting oxazolidin-2-imines are among the most potent SARMs known, with many analogue
Discovery of potent and muscle selective androgen receptor modulators through scaffold modifications
Li, James J.,Sutton, James C.,Nirschl, Alexandra,Zou, Yan,Wang, Haixia,Sun, Chongqing,Pi, Zulan,Johnson, Rebecca,Krystek Jr., Stanley R.,Seethala, Ramakrishna,Golla, Rajasree,Sleph, Paul G.,Beehler, Blake C.,Grover, Gary J.,Fura, Aberra,Vyas, Viral P.,Li, Cindy Y.,Gougoutas, Jack Z.,Galella, Michael A.,Zahler, Robert,Ostrowski, Jacek,Hamann, Lawrence G.
, p. 3015 - 3025 (2008/02/06)
A novel series of imidazolin-2-ones were designed and synthesized as highly potent, orally active and muscle selective androgen receptor modulators (SARMs), with most of the compounds exhibiting low nM in vitro potency in androgen receptor (AR) binding and functional assays. Once daily oral treatment with the lead compound 11a (AR Ki = 0.9 nM, EC50 = 1.8 nM) for 14 days induced muscle growth with an ED50 of 0.09 mg/kg, providing approximately 50-fold selectivity over prostate growth in an orchidectomized rat model. Pharmacokinetic studies in rats demonstrated that the lead compound 11a had oral bioavailability of 65% and a plasma half-life of 5.5 h. On the basis of their preclinical profiles, the SARMs in this series are expected to provide beneficial anabolic effects on muscle with minimal androgenic effects on prostate tissue.
BICYCLIC MODULATORS OF ANDROGEN RECEPTOR FUNCTION
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Page/Page column 27, (2008/06/13)
The present invention relates to bicyclic compounds according to formula I, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of androgen receptor-associated conditions, such as age-related diseases, for example sarcopenia, wherein R1, R2, R5, X, Y and n are defined herein.
