SAR Exploration Guided by LE and Fsp3: Discovery of a Selective and Orally Efficacious RORγ Inhibitor-Reference-Cited by-同舟云学术

SAR Exploration Guided by LE and Fsp3: Discovery of a Selective and Orally Efficacious RORγ Inhibitor

Published:2015-11-09 Issue:1 Volume:7 Page:23-27
ISSN:1948-5875
Container-title:ACS Medicinal Chemistry Letters
language:en
Short-container-title:ACS Med. Chem. Lett.

Author:

Hirata Kazuyuki,Kotoku Masayuki,Seki Noriyoshi,Maeba Takaki,Maeda Katsuya,Hirashima Shintaro,Sakai Takayuki,Obika Shingo,Hori Akimi,Hase Yasunori,Yamaguchi Takayuki,Katsuda Yoshiaki,Hata Takahiro,Miyagawa Naoki,Arita Kojo,Nomura Yukihiro,Asahina Kota,Aratsu Yusuke,Kamada Masafumi¹,Adachi Tsuyoshi¹,Noguchi Masato¹,Doi Satoki¹,Crowe Paul²,Bradley Erin²,Steensma Ruo²,Tao Haiyan²,Fenn Morgan²,Babine Robert²,Li Xiaolin²,Thacher Scott²,Hashimoto Hiromasa,Shiozaki Makoto

Affiliation:

1. Pharmaceutical Frontier Research Laboratories, Central Pharmaceutical Research Institute, Japan Tobacco Inc., 1-13-2, Fukuura, Kanazawa-ku, Yokohama, Kanagawa 236-0004, Japan

2. Orphagen Pharmaceuticals, 11558 Sorrento Valley Road, Suite 4, San Diego, California 92121, United States

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Drug Discovery,Biochemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.5b00253

Reference27 articles.

1. Interleukin 17–producing CD4+ effector T cells develop via a lineage distinct from the T helper type 1 and 2 lineages

2. A distinct lineage of CD4 T cells regulates tissue inflammation by producing interleukin 17

3. The Orphan Nuclear Receptor RORγt Directs the Differentiation Program of Proinflammatory IL-17+ T Helper Cells

4. The Benzenesulfoamide T0901317 [N-(2,2,2-Trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide] Is a Novel Retinoic Acid Receptor-Related Orphan Receptor-α/γ Inverse Agonist

5. Identification of SR2211: A Potent Synthetic RORγ-Selective Modulator

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