Discovery and pharmacological characterization of N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor.
In the course of our program for discovery of novel DPP-IV inhibitors, a series of pyrazolo[1,5-a]pyrimidines were found to be novel DPP-IV inhibitors. We identified N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (4a) and described its pharmacological profiles.
Central Research Laboratory, Sanwa Kagaku Kenkyusho, Co. Ltd, 363 Shiosaki, Hokusei-cho, Inabe-city, Mie 511-0406, Japan. n_katoh@mb4.skk-net.com
Noriyasu
N
Kato
Mitsuru
M
Oka
Takayo
T
Murase
Masahiro
M
Yoshida
Masao
M
Sakairi
Satoko
S
Yamashita
Yoshika
Y
Yasuda
Aya
A
Yoshikawa
Yuuji
Y
Hayashi
Mitsuhiro
M
Makino
Motohiro
M
Takeda
Yakufu
Y
Mirensha
Takuji
T
Kakigami
D000818:Animals; D018819:Dipeptidyl Peptidase 4 / Q000378:metabolism; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D004285:Dogs; D006801:Humans; D008297:Male; D011743:Pyrimidines / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D017207:Rats, Sprague-Dawley; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
D054873:Dipeptidyl-Peptidase IV Inhibitors; D011743:Pyrimidines; D018819:Dipeptidyl Peptidase 4; C583175:anagliptin