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Design,synthesis and biological evaluation of novel 7-azaspiro[3.5]nonane derivatives as GPR119 agonists |
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| Authors: | Daisuke Matsuda Madoka Kawamura Yohei Kobashi Fumiyasu Shiozawa Youichirou Suga Keiko Fusegi Shinichi Nishimoto Kayo Kimura Masako Miyoshi Noriko Takayama Hiroyuki Kakinuma Norikazu Ohtake |
| Institution: | 1. Chemistry Laboratories, Taisho Pharmaceutical Co., Ltd., 1-403 Yoshino-cho, Kita-ku, Saitama 331-9530, Japan;2. Pharmaceutical Science Laboratories, Taisho Pharmaceutical Co., Ltd., 1-403 Yoshino-cho, Kita-ku, Saitama 331-9530, Japan;3. Pharmacology Laboratories, Taisho Pharmaceutical Co., Ltd., 1-403 Yoshino-cho, Kita-ku, Saitama 331-9530, Japan;4. Research Support, Taisho Pharmaceutical Co., Ltd., 1-403 Yoshino-cho, Kita-ku, Saitama 331-9530, Japan |
| Abstract: | The design and synthesis of a novel class of 7-azaspiro3.5]nonane GPR119 agonists are described. In this series, optimization of the right piperidine N-capping group (R2) and the left aryl group (R3) led to the identification of compound 54g as a potent GPR119 agonist. Compound 54g showed a desirable PK profile in Sprague-Dawley (SD) rats and a favorable glucose lowering effect in diabetic rats. |
| Keywords: | Corresponding author |
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