Discovery of Clinical Candidate 2‑(4-(2-((1H‑Benzo[d]imidazol-2-yl)thio)ethyl)piperazin-1-yl)‑N‑(6-methyl-2,4-bis(methylthio)pyridin-3-yl)acetamide Hydrochloride [K-604], an Aqueous-Soluble Acyl-CoA:Cholesterol O‑Acyltransferase‑1 Inhibitor
Shibuya, Kimiyuki, Kawamine, Katsumi, Ozaki, Chiyoka, Ohgiya, Tadaaki, Edano, Toshiyuki, Yoshinaka, Yasunobu, Tsunenari, Yoshihiko
Published in Journal of medicinal chemistry (13.12.2018)
Published in Journal of medicinal chemistry (13.12.2018)
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Esterification of 24S-OHC induces formation of atypical lipid droplet-like structures, leading to neuronal cell death[S]
Takabe, Wakako, Urano, Yasuomi, Vo, Diep-Khanh Ho, Shibuya, Kimiyuki, Tanno, Masaki, Kitagishi, Hiroaki, Fujimoto, Toyoshi, Noguchi, Noriko
Published in Journal of lipid research (01.11.2016)
Published in Journal of lipid research (01.11.2016)
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New CETP inhibitor K-312 reduces PCSK9 expression: a potential effect on LDL cholesterol metabolism
Miyosawa, Katsutoshi, Watanabe, Yuichiro, Murakami, Kentaro, Murakami, Takeshi, Shibata, Haruki, Iwashita, Masaya, Yamazaki, Hiroyuki, Yamazaki, Koichi, Ohgiya, Tadaaki, Shibuya, Kimiyuki, Mizuno, Ken, Tanabe, Sohei, Singh, Sasha A, Aikawa, Masanori
Published in American journal of physiology: endocrinology and metabolism (15.07.2015)
Published in American journal of physiology: endocrinology and metabolism (15.07.2015)
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Optimization of a novel series of potent and orally bioavailable GPR119 agonists
Koshizawa, Tomoaki, Morimoto, Toshiharu, Watanabe, Gen, Watanabe, Toshiaki, Yamasaki, Nao, Sawada, Yoshikazu, Fukuda, Tomoaki, Okuda, Ayumu, Shibuya, Kimiyuki, Ohgiya, Tadaaki
Published in Bioorganic & medicinal chemistry letters (01.08.2017)
Published in Bioorganic & medicinal chemistry letters (01.08.2017)
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Journal Article
A selective ACAT-1 inhibitor, K-604, suppresses fatty streak lesions in fat-fed hamsters without affecting plasma cholesterol levels
Ikenoya, Mami, Yoshinaka, Yasunobu, Kobayashi, Hideyuki, Kawamine, Katsumi, Shibuya, Kimiyuki, Sato, Fumiyasu, Sawanobori, Kimio, Watanabe, Takuya, Miyazaki, Akira
Published in Atherosclerosis (01.04.2007)
Published in Atherosclerosis (01.04.2007)
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Brain Targeting of Acyl-CoA:Cholesterol O‑Acyltransferase‑1 Inhibitor K‑604 via the Intranasal Route Using a Hydroxycarboxylic Acid Solution
Shibuya, Kimiyuki, Morikawa, Shigeru, Miyamoto, Masayoshi, Ogawa, Shin-ichiro, Tsunenari, Yoshihiko, Urano, Yasuomi, Noguchi, Noriko
Published in ACS omega (15.10.2019)
Published in ACS omega (15.10.2019)
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A selective ACAT-1 inhibitor, K-604, stimulates collagen production in cultured smooth muscle cells and alters plaque phenotype in apolipoprotein E-knockout mice
Yoshinaka, Yasunobu, Shibata, Haruki, Kobayashi, Hideyuki, Kuriyama, Hiroki, Shibuya, Kimiyuki, Tanabe, Sohei, Watanabe, Takuya, Miyazaki, Akira
Published in Atherosclerosis (01.11.2010)
Published in Atherosclerosis (01.11.2010)
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Journal Article
Three derivatives of 4-fluoro-5-sulfonylisoquinoline
Ohba, Shigeru, Gomi, Noriaki, Ohgiya, Tadaaki, Shibuya, Kimiyuki
Published in Acta crystallographica. Section C, Crystal structure communications (01.10.2012)
Published in Acta crystallographica. Section C, Crystal structure communications (01.10.2012)
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Synthesis of oxidative metabolites of K-115, a novel Rho-kinase inhibitor
Gomi, Noriaki, Shibuya, Kimiyuki, Kawamura, Kiyoshi, Kabeya, Mototsugu
Published in Tetrahedron letters (16.02.2022)
Published in Tetrahedron letters (16.02.2022)
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Syntheses and pharmacokinetic evaluations of four metabolites of 2-(4-(2-((1H-benzo[d]imidazol-2-yl)thio)ethyl)piperazin-1-yl)-N-(6-methyl-2,4-bis-(methylthio)pyridin-3-yl)acetamide hydrochloride [K-604], an acyl-CoA:cholesterol O-acyltransferase-1 inhibitor
Shibuya, Kimiyuki, Miura, Toru, Ohgiya, Tadaaki, Omichi, Kozo, Tsunenari, Yoshihiko
Published in Bioorganic & medicinal chemistry (01.06.2020)
Published in Bioorganic & medicinal chemistry (01.06.2020)
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Journal Article
Discovery of Clinical Candidate 2-(4-(2-((1H-Benzo[d]imidazol-2-yl)thio)ethyl)piperazin-1-yl)-N-(6-methyl-2,4-bis(methylthio)pyridin-3-yl)acetannide Hydrochloride [K-604], an Aqueous-Soluble Acyl-CoA:Cholesterol O-Acyltransferase-1 Inhibitor
Shibuya, Kimiyuki, Kawamine, Katsumi, Ozaki, Chiyoka, Ohgiya, Tadaaki, Edano, Toshiyuki, Yoshinaka, Yasunobu, Tsunenari, Yoshihiko
Published in Journal of medicinal chemistry (13.12.2018)
Published in Journal of medicinal chemistry (13.12.2018)
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Journal Article
Design, synthesis and pharmacology of aortic-selective acyl-CoA: Cholesterol O-acyltransferase (ACAT/SOAT) inhibitors
Shibuya, Kimiyuki, Kawamine, Katsumi, Miura, Toru, Ozaki, Chiyoka, Edano, Toshiyuki, Mizuno, Ken, Yoshinaka, Yasunobu, Tsunenari, Yoshihiko
Published in Bioorganic & medicinal chemistry (07.08.2018)
Published in Bioorganic & medicinal chemistry (07.08.2018)
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Journal Article
Determination of the Absolute Configuration and a Practical Chiral Synthesis of 5-[5-(1-Methylethoxy)pyridin-2-yl]-5-methylimidazolidine-2,4-dione as a Novel Liver X Receptor -Selective Agonist
Koura, Minoru, Sumida, Hisashi, Shibuya, Kimiyuki, Ohba, Shigeru
Published in Synthesis (Stuttgart) (01.05.2017)
Published in Synthesis (Stuttgart) (01.05.2017)
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Discovery of novel spiro[chromane-2,4′-piperidine] derivatives as potent and orally bioavailable G-protein-coupled receptor 119 agonists
Koshizawa, Tomoaki, Morimoto, Toshiharu, Watanabe, Gen, Fukuda, Tomoaki, Yamasaki, Nao, Hagita, Sumihiko, Sawada, Yoshikazu, Okuda, Ayumu, Shibuya, Kimiyuki, Ohgiya, Tadaaki
Published in Bioorganic & medicinal chemistry letters (15.10.2018)
Published in Bioorganic & medicinal chemistry letters (15.10.2018)
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Journal Article
Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists
Koura, Minoru, Matsuda, Takayuki, Okuda, Ayumu, Watanabe, Yuichiro, Yamaguchi, Yuki, Kurobuchi, Sayaka, Matsumoto, Yuuki, Shibuya, Kimiyuki
Published in Bioorganic & medicinal chemistry letters (01.07.2015)
Published in Bioorganic & medicinal chemistry letters (01.07.2015)
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