Zobrazeno 1 - 10
of 32
pro vyhledávání: '"Hiromasa Hashimoto"'
Autor:
Yasunori Hase, Kazutaka Ikegashira, Hiromasa Hashimoto, Takayuki Yamasaki, Iichiro Kawahara, Taku Ikenogami, Yoshihisa Koga, Koji Inagaki, Naoki Miyagawa, Takahiro Oka
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:873-877
Optimization of novel azetidine compounds, which we had found as colony stimulating factor-1 receptor (CSF-1R) Type II inhibitors, provided JTE-952 as a clinical candidate with high cellular activity (IC50 = 20 nM) and good pharmacokinetics profile.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f442336db72895a98e9e75673b64cf0
https://doi.org/10.1016/j.bmcl.2019.02.006
https://doi.org/10.1016/j.bmcl.2019.02.006
Autor:
Takuya Orita, Masafumi Inoue, Tomoya Miura, Yoshinori Hara, Makoto Shiozaki, Hiroshi Yamamoto, Shingo Obika, Hiroshi Yamanaka, Chika Oki, Yukari Kimoto, Yoshihiro Ogawa, Tsuyoshi Adachi, Atsuo Tanimoto, Akimi Hori, Satoru Noji, Hiromasa Hashimoto, Yasunori Hase, Tamotsu Negoro, Satoki Doi, Katsuya Maeda
Publikováno v:
Journal of medicinal chemistry. 63(13)
Dermatologic disorders such as atopic dermatitis arise from genetic and environmental causes and are complex and multifactorial in nature. Among possible risk factors, aberrant immunological reactions are one of the leading etiologies. Immunosuppress
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd05e59507e421fd4174fd9eaec2f08d
https://pubmed.ncbi.nlm.nih.gov/32511913
https://pubmed.ncbi.nlm.nih.gov/32511913
Autor:
Akihiro Nomura, Kojo Arita, Paul D. Crowe, Kazuyuki Hirata, Makoto Shiozaki, Keisuke Ito, Naoki Miyagawa, Yoshiaki Katsuda, Kota Asahina, Hiromasa Hashimoto, Yoshihiro Suwa, Masayuki Kotoku, Haiyan Tao, Yasunori Hase, Yokota Masahiro, Seki Noriyoshi, Fujioka Shingo, Satoki Doi, Tsuyoshi Adachi, Masato Noguchi, Scott M. Thacher, Takayoshi Suzuki, Taku Ikenogami, Takaki Maeba
Publikováno v:
Journal of medicinal chemistry. 62(5)
Starting from a previously reported RORγ inhibitor (1), successive efforts to improve in vivo potency were continued. Introduction of metabolically beneficial motifs in conjunction with scaffold hopping was examined, resulting in discovery of the se
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0d47ae0da2d592b09541af2e19b99f9f
https://pubmed.ncbi.nlm.nih.gov/30776227
https://pubmed.ncbi.nlm.nih.gov/30776227
Autor:
Yasunori Hase, Kazutaka Ikegashira, Takayuki Yamasaki, Satoki Doi, Taku Ikenogami, Koji Inagaki, Tsuyoshi Adachi, Hiromasa Hashimoto, Takayuki Yamaguchi, Yoshihisa Koga
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(1)
We report the discovery of a novel azetidine scaffold for colony stimulating factor-1 receptor (CSF-1R) Type II inhibitors by using a structure-based drug design (SBDD) based on a docking model. The work leads to the representative compound 4a with h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4d709947508bc3b3d064a15b58e90d84
https://pubmed.ncbi.nlm.nih.gov/30442420
https://pubmed.ncbi.nlm.nih.gov/30442420
Autor:
Masanobu Koga, Hiromasa Hashimoto
Publikováno v:
2017 International Automatic Control Conference (CACS).
The purpose of this study was developing useful calculation tool running on smart device and enlarging the width of utility by cooperating with smart watch. On this research, we suggest a function which can receive notification of calculation result
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::88f9250951dd3139e7d8e44c3b5d104d
https://doi.org/10.1109/cacs.2017.8284235
https://doi.org/10.1109/cacs.2017.8284235
Autor:
Fukuda Kenji, Shuichi Kimura, Takashi Nakagawa, Toshihiro Kiguchi, Hiromasa Hashimoto, Yushi Matsuo, Kazuhito Harada, Mariko Maekawa, Soejima Yuki, Masanori Shindo, Masaki Takagi, Mikio Hayashi, Naoki Ogawa, Kazuyuki Hirata, Taku Ikenogami, Yuko Shinagawa, Takeo Katsushima, Mitsuru Takahashi, Teruhiko Inoue
Publikováno v:
ACS Medicinal Chemistry Letters. 2:238-242
Short-acting oral calcilytics, calcium-sensing receptor (CaSR) antagonists, have been considered as alternatives for parathyroid hormone (PTH), an injectable bone anabolic drug used in the treatment of osteoporosis. Previously, we identified aminopro
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::289ed30b7d81d9b069c946c2cc22f545
https://doi.org/10.1021/ml100268k
https://doi.org/10.1021/ml100268k
Autor:
Masanori Shindo, Kazuyuki Hirata, Yuko Shinagawa, Teruhiko Inoue, Yushi Matsuo, Takeo Katsushima, Takashi Nakagawa, Hiromasa Hashimoto
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3809-3813
Synthesis and structure-activity relationship studies on a new aminopropandiol class of derivatives as calcium-sensing receptor antagonists are described. Modification of the phenolic moiety of a calcilytic compound NPS 2143 led to the identification
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7171d4a9a8d0abacd66a62e8b76d9db4
https://doi.org/10.1016/j.bmcl.2010.04.035
https://doi.org/10.1016/j.bmcl.2010.04.035
Autor:
Yoshinori Hara, Satoru Noji, Satoru Ikeda, Hiroshi Yamanaka, Shintaro Hirashima, Kazutaka Ikegashira, Hiromasa Hashimoto, Yasushi Niwa, Ryo Mizojiri, Toru Noguchi, Takahiro Oka, Izuru Ando, Hiroyuki Goto
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3181-3186
Following the discovery of JTK-109 ( 1 ) as a potent inhibitor of hepatitis C virus NS5B RNA-dependent RNA polymerase, [(a) Hirashima, S.; Suzuki, T.; Ishida, T.; Noji, S.; Yata, S.; Ando, I.; Komatsu, M.; Ikeda, S.; Hashimoto, H. J. Med. Chem. 2006
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b11e7639c944fbb3c6d7112ca415762c
https://doi.org/10.1016/j.bmcl.2007.03.027
https://doi.org/10.1016/j.bmcl.2007.03.027
Autor:
Naoki Miyagawa, Kota Asahina, Shintaro Hirashima, Scott Thacher, Satoki Doi, Masayuki Kotoku, Yukihiro Nomura, Katsuya Maeda, Shingo Obika, Haiyan Tao, Erin Bradley, Yoshiaki Katsuda, Paul Crowe, Seki Noriyoshi, Ruo Steensma, Takahiro Hata, Tsuyoshi Adachi, Robert Babine, Sakai Takayuki, Makoto Shiozaki, Kojo Arita, Masato Noguchi, Takaki Maeba, Xiaolin Li, Yasunori Hase, Morgan Fenn, Kazuyuki Hirata, Masafumi Kamada, Yusuke Aratsu, Akimi Hori, Takayuki Yamaguchi, Hiromasa Hashimoto
A novel series of RORγ inhibitors was identified starting with the HTS hit 1. After SAR investigation based on a prospective consideration of two drug-likeness metrics, ligand efficiency (LE) and fraction of sp(3) carbon atoms (Fsp(3)), significant
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2a980bfa040ac0bdac6e9c6c9a5fd8c0
https://europepmc.org/articles/PMC4716592/
https://europepmc.org/articles/PMC4716592/
Autor:
Satoru Ikeda, Hiromasa Hashimoto, Shintaro Hirashima, Tomio Ishida, Izuru Ando, Takayoshi Suzuki, Atsuhito Yoshida, Tsuyoshi Adachi, Mizutani Kenji
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1859-1863
A series of 1-cycloalkyl-2-phenyl-1H-benzimidazole-5-carboxylic acid derivatives was synthesized and evaluated for inhibitory activity against HCV NS5B RNA-dependent RNA polymerase (RdRp). A SAR study was performed and led to identify the 2-[(4-diary
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::90f38ee4a8d02efbdc56a9826e8d3647
https://doi.org/10.1016/j.bmcl.2006.01.032
https://doi.org/10.1016/j.bmcl.2006.01.032