- Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit
-
A novel series of pyrrolidine-constrained phenethylamines were developed as dipeptidyl peptidase IV (DPP4) inhibitors for the treatment of type 2 diabetes. The cyclohexene ring of lead-like screening hit 5 was replaced with a pyrrolidine to enable paralle
- Backes, Bradley J.,Longenecker, Kenton,Hamilton, Gregory L.,Stewart, Kent,Lai, Chunqiu,Kopecka, Hana,von Geldern, Thomas W.,Madar, David J.,Pei, Zhonghua,Lubben, Thomas H.,Zinker, Bradley A.,Tian, Zhenping,Ballaron, Stephen J.,Stashko, Michael A.,Mika, Amanda K.,Beno, David W.A.,Kempf-Grote, Anita J.,Black-Schaefer, Candace,Sham, Hing L.,Trevillyan, James M.
-
p. 2005 - 2012
(2008/02/01)
-
- Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
-
The present invention relates to compounds, which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, syndrome X, hyperinsulinemia, obesity, atherosclerosis, various immunomodulatory diseases, and other diseases.
- -
-
Page/Page column 24
(2010/11/24)
-