FRI-361 - M480, a novel non-bile acid FXR agonist, shows improvement across multiple parameters in a diet-induced obese mouse model with biopsy-confirmed NASH

Autor: Wagner, B., Brigham, D., Lee, K.-J., Ortiz, A., Lu, N., Douglas, K., Govek, S., Feigh, M., Veidal, S., Vrang, N., Song, K., Smith, N., Dedman, H., Milik, A.

Publikováno v: In Journal of Hepatology 2017 66(1) Supplement:S433-S433

Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer.

Autor: Nagasawa J, Govek S, Kahraman M, Lai A, Bonnefous C, Douglas K, Sensintaffar J, Lu N, Lee K, Aparicio A, Kaufman J, Qian J, Shao G, Prudente R, Joseph JD, Darimont B, Brigham D, Maheu K, Heyman R, Rix PJ, Hager JH, Smith ND

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2018 Sep 13; Vol. 61 (17), pp. 7917-7928. Date of Electronic Publication: 2018 Sep 04.

Discovery, optimization, and evaluation of non-bile acid FXR/TGR5 dual agonists.

Autor: Miyata, Sachiho¹ s-miyata@fujiyakuhin.co.jp, Kawashima, Yuji¹, Sakai, Miku², Matsubayashi, Masaya², Motoki, Keisuke², Miyajima, Yui¹, Watanabe, Yousuke², Chikamatsu, Noriko², Taniguchi, Tetsuya², Tokuyama, Ryukou¹ r-tokuyama@fujiyakuhin.co.jp

Publikováno v: Scientific Reports. 4/28/2021, Vol. 11 Issue 1, p1-11. 11p.

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Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.

Autor: Lai A; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Kahraman M; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Govek S; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Nagasawa J; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Bonnefous C; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Julien J; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Douglas K; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Sensintaffar J; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Lu N; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Lee KJ; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Aparicio A; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Kaufman J; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Qian J; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Shao G; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Prudente R; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Moon MJ; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Joseph JD; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Darimont B; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Brigham D; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Grillot K; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Heyman R; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Rix PJ; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Hager JH; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States., Smith ND; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2015 Jun 25; Vol. 58 (12), pp. 4888-904. Date of Electronic Publication: 2015 May 22.