Discovery of the Orally Effective Thyrotropin-Releasing Hormone Mimetic: 1‑{N‑[(4S,5S)‑(5-Methyl-2-oxooxazolidine-4-yl)carbonyl]-3-(thiazol-4-yl)‑l‑alanyl}-(2R)‑2-methylpyrrolidine Trihydrate (Rovatirelin Hydrate)

• Naotake Kobayashi,
• Norihito Sato,
• Yuko Fujimura,
• Tsuyoshi Kihara,
• Katsuji Sugita,
• Kouji Takahashi,
• Katsumi Koike,
• Tamio Sugawara,
• Yukio Tada,
• Hiroshi Nakai,
• Takayoshi Yoshikawa

Affiliations

Naotake Kobayashi

†Medicinal Chemistry Research Laboratory, Shionogi & Co., Ltd., Toyonaka-shi, Osaka, Japan

Norihito Sato

‡Research Laboratory for Development, Shionogi & Co., Ltd., Toyonaka-shi, Osaka, Japan

Yuko Fujimura

†Medicinal Chemistry Research Laboratory, Shionogi & Co., Ltd., Toyonaka-shi, Osaka, Japan

Tsuyoshi Kihara

Business Search & Evaluation, Shionogi & Co., Ltd., Osaka-shi, Osaka, Japan

Katsuji Sugita

‡Research Laboratory for Development, Shionogi & Co., Ltd., Toyonaka-shi, Osaka, Japan

Kouji Takahashi

DMPK Services, Shionogi Techno Advance Research Co., Ltd., Toyonaka-shi, Osaka, Japan

Katsumi Koike

⊥Drug Discovery & Disease Research Laboratory, Shionogi & Co., Ltd., Toyonaka-shi, Osaka, Japan

Tamio Sugawara

†Medicinal Chemistry Research Laboratory, Shionogi & Co., Ltd., Toyonaka-shi, Osaka, Japan

Yukio Tada

†Medicinal Chemistry Research Laboratory, Shionogi & Co., Ltd., Toyonaka-shi, Osaka, Japan

Hiroshi Nakai

†Medicinal Chemistry Research Laboratory, Shionogi & Co., Ltd., Toyonaka-shi, Osaka, Japan

Takayoshi Yoshikawa

Pharmacovigilance Japan, Allergan Japan K.K., Shibuya-ku, Tokyo, Japan