Publication in detail

Bioorg Med Chem Lett. 2015 Nov 17. pii: S0960-894X(15)30258-4. doi: 10.1016/j.bmcl.2015.11.050. [Epub ahead of print]

Discovery of the imidazole-derived GPR40 agonist AM-3189.

Ma, Z; Lin, DC; Sharma, R; Liu, J; Zhu, L; Li, AR; Kohn, T; Wang, Y; Liu, JJ; Bartberger, MD; Medina, JC; Zhuang, R; Li, L; Zhang, J; Luo, J; Wong, S; Tonn, GR; Houze, JB

Amgen Inc., South San Francisco, CA, USA.

As a follow-up to the GPR40 agonist AMG 837, which was evaluated in clinical trials for the treatment of type II diabetes, further optimization led to the discovery of AM-3189 (13k). AM-3189 is representative of a new class of compounds with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837.

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