121443-79-6Relevant articles and documents
N-BIPHENYLMETHYLINDOLE MODULATORS OF PPARG
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Page/Page column 180, (2012/12/14)
The invention provides molecular entities that bind with high affinity to PPARG (PPAR3), inhibit kinase-mediated, e.g., cdk5-mediated, phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. In methods of treatment of these conditions using a compound of the invention, the compound can avoid producing side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, in the patient receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
An efficient preparation of (S)-(-)-1-(2,6-dichlorophenyl)ethylamine
Polniaszek,Lichti
, p. 171 - 178 (2007/10/02)
(S)-(-)-1-(2,6-Dichlorophenyl)ethylamine has been prepared from (S)-α-phenethylamine in 2 steps in 44% overall yield.
Stereoselective Nucleophilic Additions to the Carbon-Nitrogen Double Bond. 2. Chiral Iminium Ions Derived from "Second Generation" Chiral Amines
Polniaszek, Richard P.,Kaufman, Craig R.
, p. 4859 - 4863 (2007/10/02)
"Second generation" chiral amines (1S)-(-)-1-(2-chlorophenyl)ethylamine (4) and (1S)-(-)-1-(2,6-dichlorophenyl)ethylamine (5) have been prepared from commercially available (S)-(-)-α-phenethylamine.These chiral reagents have been incorporated into chiral