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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
Authors:Kato Noriyasu  Oka Mitsuru  Murase Takayo  Yoshida Masahiro  Sakairi Masao  Yamashita Satoko  Yasuda Yoshika  Yoshikawa Aya  Hayashi Yuuji  Makino Mitsuhiro  Takeda Motohiro  Mirensha Yakufu  Kakigami Takuji
Affiliation:Central Research Laboratory, Sanwa Kagaku Kenkyusho, Co. Ltd, 363 Shiosaki, Hokusei-cho, Inabe-city, Mie 511-0406, Japan. n_katoh@mb4.skk-net.com
Abstract: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.
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