Discovery of novel (4-piperidinyl)-piperazines as potent and orally active acetyl-CoA carboxylase 1/2 non-selective inhibitors: F-Boc and triF-Boc groups are acid …
…, H Tanaka, A Ohoka-Sugita, F Io, H Koretsune… - Bioorganic & medicinal …, 2011 - Elsevier
Novel (4-piperidinyl)-piperazine derivatives were synthesized and evaluated as ACC1/2 non-selective
inhibitors. Optimization of the substituents on the nitrogen of the piperidine ring …
inhibitors. Optimization of the substituents on the nitrogen of the piperidine ring …
Discovery of novel pyrazolylpyridine derivatives for 20-hydroxyeicosatetraenoic acid synthase inhibitors with selective CYP4A11/4F2 inhibition
…, T Hirata, H Ohara, N Kojima, H Koretsune… - Journal of Medicinal …, 2022 - ACS Publications
20-Hydroxyeicosatetraenoic acid (20-HETE) is one of the major oxidized arachidonic acid (AA)
metabolites produced by cytochrome P450 (CYP) 4A11 and CYP4F2 isozymes in the …
metabolites produced by cytochrome P450 (CYP) 4A11 and CYP4F2 isozymes in the …
TP0463518, a novel prolyl hydroxylase inhibitor, specifically induces erythropoietin production in the liver
…, H Takano, F Io, N Takayama, H Koretsune… - … of Pharmacology and …, 2019 - ASPET
Prolyl hydroxylase (PHD) 1/2/3 pan inhibitors are known to potentially induce erythropoietin
(EPO) production in both the kidney and liver. The 2-[[1-[[6-(4-chlorophenoxy)pyridin-3-yl]…
(EPO) production in both the kidney and liver. The 2-[[1-[[6-(4-chlorophenoxy)pyridin-3-yl]…
Design and synthesis of disubstituted (4-piperidinyl)-piperazine derivatives as potent acetyl-CoA carboxylase inhibitors
…, D Wakasugi, A Ohoka-Sugita, F Io, H Koretsune… - Bioorganic & medicinal …, 2010 - Elsevier
Acetyl-CoA carboxylases (ACCs), the rate limiting enzymes in de novo lipid synthesis, play
important roles in modulating energy metabolism. The inhibition of ACC has demonstrated …
important roles in modulating energy metabolism. The inhibition of ACC has demonstrated …
Introduction of a carboxylic acid group into pyrazolylpyridine derivatives increased selectivity for inhibition of the 20-HETE synthase CYP4A11/4F2
…, K Funayama, T Hirata, H Ohara, H Koretsune… - Bioorganic & Medicinal …, 2023 - Elsevier
20-Hydroxyeicosatetraenoic acid (20-HETE) is a lipid mediator and one of the major
arachidonic acid metabolites whose formation is mainly catalyzed by the enzymes cytochrome …
arachidonic acid metabolites whose formation is mainly catalyzed by the enzymes cytochrome …
(4-Piperidinyl)-piperazine: A new platform for acetyl-CoA carboxylase inhibitors
…, H Tanaka, A Ohoka-Sugita, F Io, H Koretsune… - Bioorganic & medicinal …, 2009 - Elsevier
Acetyl-CoA carboxylases (ACCs), the rate limiting enzymes in de novo lipid synthesis, play
important roles in modulating energy metabolism. The inhibition of ACC has demonstrated …
important roles in modulating energy metabolism. The inhibition of ACC has demonstrated …
Renoprotective Effect of TP0472993, a Novel and Selective 20-Hydroxyeicosatetraenoic Acid Synthesis Inhibitor, in Mouse Models of Renal Fibrosis
T Hirata, H Ohara, N Kojima, H Koretsune… - … of Pharmacology and …, 2023 - ASPET
Kidney fibrosis is considered the essential pathophysiological process for the progression
of chronic kidney disease (CKD) toward renal failure. 20-Hydroxyeicosatetraenoic acid (20-…
of chronic kidney disease (CKD) toward renal failure. 20-Hydroxyeicosatetraenoic acid (20-…
SGL5213, a novel and potent intestinal SGLT1 inhibitor, suppresses intestinal glucose absorption and enhances plasma GLP-1 and GLP-2 secretion in rats
F Io, E Gunji, H Koretsune, K Kato… - European Journal of …, 2019 - Elsevier
Sodium-glucose cotransporter 1 (SGLT1) is the primary transporter for glucose absorption
from digested nutrients in the gastrointestinal tract. Intestinal SGLT1 inhibition reduces post-…
from digested nutrients in the gastrointestinal tract. Intestinal SGLT1 inhibition reduces post-…
Discovery of novel 2-[(4-hydroxy-6-oxo-2, 3-dihydro-1H-pyridine-5-carbonyl) amino] acetic acid derivatives as HIF prolyl hydroxylase inhibitors for treatment of renal …
…, N Takayama, L Okumura-Kitajima, H Koretsune… - Bioorganic & Medicinal …, 2018 - Elsevier
Prolyl hydroxylase domain-containing protein (PHD) inhibitors are useful as orally administered
agents for the treatment of renal anemia. Based on the common structures of known …
agents for the treatment of renal anemia. Based on the common structures of known …
TP0463518, a novel inhibitor for hypoxia-inducible factor prolyl hydroxylases, increases erythropoietin in rodents and monkeys with a good pharmacokinetics …
S Kato, N Takayama, H Takano, H Koretsune… - European Journal of …, 2018 - Elsevier
Hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor stabilizes hypoxia inducible
factor alpha, which increases erythropoietin (EPO) expression via the hypoxia response …
factor alpha, which increases erythropoietin (EPO) expression via the hypoxia response …