90905-33-2Relevant articles and documents
Physical and chemical rationalization for asymmetric amplification in aatocatalytic reactions
Buono, Frederic G.,Iwamura, Hiroshi,Blackmond, Donna G.
, p. 2099 - 2103 (2004)
Selective precipitation of the product alkoxide 2′ is observed at higher conversions of substrate in the asymmetric autocatalytic alkylation of pyrimidyl aldehyde 1. Enrichment or depletion of the enantiomeric excess in solution can result, depending on the solvent employed in the reaction. Asymmetric amplification may be effected by a synergistic combination of chemical and physical processes, leading to a homochiral reaction environment.
KETOLIDE COMPOUNDS
-
Page/Page column 56-57, (2012/06/30)
The invention relates to ketolide compounds of Formula (I) and their pharmaceutically acceptable salts, solvates, hydrates, polymorphs and stereoisomers having antimicrobial activity. The invention also provides pharmaceutical compositions containing the compounds of invention and methods of treating or preventing microbial infections with the compounds of invention, wherein, T is -C*H(R1)-P-Q; R1 is hydrogen; unsubstituted or substituted lower alkyl, cycloalkyl or aryl; P is heteroaryl ring; Q is unsubstituted or substituted aryl or heteroaryl ring; and P is attached to Q via carbon-carbon link; and R3 is hydrogen or fluorine, With the provision that when R1 is hydrogen, R3 is fluorine.
Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis.
Coleman, Paul J,Brashear, Karen M,Askew, Ben C,Hutchinson, John H,McVean, Carol A,Duong,Feuston, Bradley P,Fernandez-Metzler, Carmen,Gentile, Michael A,Hartman, George D,Kimmel, Donald B,Leu, Chih-Tai,Lipfert, Lorraine,Merkle, Kara,Pennypacker, Brenda,Prueksaritanont, Thomayant,Rodan, Gideon A,Wesolowski, Gregg A,Rodan, Sevgi B,Duggan, Mark E
, p. 4829 - 4837 (2007/10/03)
3-(S)-Pyrimidin-5-yl-9-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-nonanoic acid (5e) and 3-(S)-(methylpyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-nonanoic acid (5f) were identified as potent and selective antagonists of the alpha(v)beta(3) receptor. These compounds have excellent in vitro profiles (IC(50) = 0.07 and 0.08 nM, respectively), significant unbound fractions in human plasma (6 and 4%), and good pharmacokinetics in rat, dog, and rhesus monkey. On the basis of the efficacy shown in an in vivo model of bone turnover following once-daily oral administration, these two compounds were selected for clinical development for the treatment of osteoporosis.