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6 results on '"Futamura, Aya"'

1. Discovery of novel indole derivatives as potent and selective inhibitors of proMMP-9 activation

Author

Nishikawa-Shimono, Rie, primary, Kuwabara, Motoi, additional, Fujisaki, Sho, additional, Matsuda, Daisuke, additional, Endo, Mayumi, additional, Kamitani, Masafumi, additional, Futamura, Aya, additional, Nomura, Yusaku, additional, Yamaguchi-Sasaki, Toru, additional, Yabuuchi, Tetsuya, additional, Yamaguchi, Chitose, additional, Tanaka-Yamamoto, Nozomi, additional, Satake, Shunya, additional, Abe-Sato, Kumi, additional, Funayama, Kosuke, additional, Sakata, Mayumi, additional, Takahashi, Shinji, additional, Hirano, Koga, additional, Fukunaga, Takuya, additional, Uozumi, Yoriko, additional, Kato, Sayaka, additional, Tamura, Yunoshin, additional, Nakamori, Tomoaki, additional, Mima, Masashi, additional, Mishima-Tsumagari, Chiemi, additional, Nozawa, Dai, additional, Imai, Yudai, additional, and Asami, Taiji, additional

Published
2023
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3. Discovery of novel indole derivatives as potent and selective inhibitors of proMMP-9 activation

Author

Nishikawa-Shimono, Rie, Kuwabara, Motoi, Fujisaki, Sho, Matsuda, Daisuke, Endo, Mayumi, Kamitani, Masafumi, Futamura, Aya, Nomura, Yusaku, Yamaguchi-Sasaki, Toru, Yabuuchi, Tetsuya, Yamaguchi, Chitose, Tanaka-Yamamoto, Nozomi, Satake, Shunya, Abe-Sato, Kumi, Funayama, Kosuke, Sakata, Mayumi, Takahashi, Shinji, Hirano, Koga, Fukunaga, Takuya, Uozumi, Yoriko, Kato, Sayaka, Tamura, Yunoshin, Nakamori, Tomoaki, Mima, Masashi, Mishima-Tsumagari, Chiemi, Nozawa, Dai, Imai, Yudai, and Asami, Taiji

Published
2024
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5. Discovery of ORN0829, a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia

Author

Tetsuaki Hiyoshi, Dai Nozawa, Sora Kirinuki, Daiji Kambe, Yuichi Tokumaru, Ryo Suzuki, Mari Ohmichi, Hiroshi Kawamoto, Yunoshin Tamura, Futamura Aya, Takeshi Aoki, and Noriko Hino

Subjects
Male, medicine.drug_class, Clinical Biochemistry, Pharmaceutical Science, Pharmacology, 01 natural sciences, Biochemistry, Structure-Activity Relationship, Dogs, Orexin Receptors, Sleep Initiation and Maintenance Disorders, Drug Discovery, medicine, Animals, Humans, Rats, Wistar, Receptor, Molecular Biology, Orexins, Dose-Response Relationship, Drug, Molecular Structure, 010405 organic chemistry, Chemistry, Organic Chemistry, Stereoisomerism, Receptor antagonist, Orexin receptor, 0104 chemical sciences, Orexin, 010404 medicinal & biomolecular chemistry, Drug Design, Lipophilicity, Molecular Medicine, Orexin Receptor Antagonists, Sleep
Abstract

Here, we present the design, synthesis, and SAR of dual orexin 1 and 2 receptor antagonists, which were optimized by balancing the antagonistic activity for orexin receptors and lipophilicity. Based on the prototype compound 1, ring construction and the insertion of an additional heteroatom into the resulting ring led to the discovery of orexin 1 and 2 receptor antagonists, which were 3-benzoyl-1,3-oxazinane derivatives. Within these derivatives, (−)-3h enabled a high dual orexin receptor antagonistic activity and a low lipophilicity. Compound (−)-3h exhibited potent sleep-promoting effects at a po dose of 1 mg/kg in a rat polysomnogram study, and optimal PK properties with a rapid Tmax and short half-lives in rats and dogs were observed, indicating a predicted human half-life of 0.9–2.0 h. Thus, (−)-3h (ORN0829; investigation code name, TS-142) was selected as a viable candidate and is currently in clinical development for the treatment of insomnia.

Published
2020

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