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Discovery of potent liver-selective stearoyl-CoA desaturase-1 (SCD1) inhibitors, thiazole-4-acetic acid derivatives, for the treatment of diabetes, hepatic steatosis, and obesity.
Iida T, Ubukata M, Mitani I, Nakagawa Y, Maeda K, Imai H, Ogoshi Y, Hotta T, Sakata S, Sano R, Morinaga H, Negoro T, Oshida S, Tanaka M, Inaba T. Iida T, et al. Among authors: tanaka m. Eur J Med Chem. 2018 Oct 5;158:832-852. doi: 10.1016/j.ejmech.2018.09.003. Eur J Med Chem. 2018. PMID: 30248655
Discovery of (1S,2R,3R)-2,3-dimethyl-2-phenyl-1-sulfamidocyclopropanecarboxylates: novel and highly selective aggrecanase inhibitors.
Shiozaki M, Maeda K, Miura T, Kotoku M, Yamasaki T, Matsuda I, Aoki K, Yasue K, Imai H, Ubukata M, Suma A, Yokota M, Hotta T, Tanaka M, Hase Y, Haas J, Fryer AM, Laird ER, Littmann NM, Andrews SW, Josey JA, Mimura T, Shinozaki Y, Yoshiuchi H, Inaba T. Shiozaki M, et al. Among authors: tanaka m. J Med Chem. 2011 Apr 28;54(8):2839-63. doi: 10.1021/jm101609j. Epub 2011 Mar 21. J Med Chem. 2011. PMID: 21417219
Synthesis, SAR studies, and pharmacological evaluation of 3-anilino-4-(3-indolyl) maleimides with conformationally restricted structure as orally bioavailable PKCbeta-selective inhibitors.
Tanaka M, Sagawa S, Hoshi J, Shimoma F, Yasue K, Ubukata M, Ikemoto T, Hase Y, Takahashi M, Sasase T, Ueda N, Matsushita M, Inaba T. Tanaka M, et al. Bioorg Med Chem. 2006 Sep 1;14(17):5781-94. doi: 10.1016/j.bmc.2006.05.033. Epub 2006 Jun 9. Bioorg Med Chem. 2006. PMID: 16762554
Discovery of 6-phenylpyrimido[4,5-b][1,4]oxazines as potent and selective acyl CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitors with in vivo efficacy in rodents.
Fox BM, Sugimoto K, Iio K, Yoshida A, Zhang JK, Li K, Hao X, Labelle M, Smith ML, Rubenstein SM, Ye G, McMinn D, Jackson S, Choi R, Shan B, Ma J, Miao S, Matsui T, Ogawa N, Suzuki M, Kobayashi A, Ozeki H, Okuma C, Ishii Y, Tomimoto D, Furakawa N, Tanaka M, Matsushita M, Takahashi M, Inaba T, Sagawa S, Kayser F. Fox BM, et al. Among authors: tanaka m. J Med Chem. 2014 Apr 24;57(8):3464-83. doi: 10.1021/jm500135c. Epub 2014 Apr 8. J Med Chem. 2014. PMID: 24670009
Discovery of pyrrolopyridazines as novel DGAT1 inhibitors.
Fox BM, Iio K, Li K, Choi R, Inaba T, Jackson S, Sagawa S, Shan B, Tanaka M, Yoshida A, Kayser F. Fox BM, et al. Among authors: tanaka m. Bioorg Med Chem Lett. 2010 Oct 15;20(20):6030-3. doi: 10.1016/j.bmcl.2010.08.066. Epub 2010 Aug 18. Bioorg Med Chem Lett. 2010. PMID: 20833038
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