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Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.
Schnute ME, Wennerstål M, Alley J, Bengtsson M, Blinn JR, Bolten CW, Braden T, Bonn T, Carlsson B, Caspers N, Chen M, Choi C, Collis LP, Crouse K, Färnegårdh M, Fennell KF, Fish S, Flick AC, Goos-Nilsson A, Gullberg H, Harris PK, Heasley SE, Hegen M, Hromockyj AE, Hu X, Husman B, Janosik T, Jones P, Kaila N, Kallin E, Kauppi B, Kiefer JR, Knafels J, Koehler K, Kruger L, Kurumbail RG, Kyne RE Jr, Li W, Löfstedt J, Long SA, Menard CA, Mente S, Messing D, Meyers MJ, Napierata L, Nöteberg D, Nuhant P, Pelc MJ, Prinsen MJ, Rhönnstad P, Backström-Rydin E, Sandberg J, Sandström M, Shah F, Sjöberg M, Sundell A, Taylor AP, Thorarensen A, Trujillo JI, Trzupek JD, Unwalla R, Vajdos FF, Weinberg RA, Wood DC, Xing L, Zamaratski E, Zapf CW, Zhao Y, Wilhelmsson A, Berstein G. Schnute ME, et al. Among authors: hu x. J Med Chem. 2018 Dec 13;61(23):10415-10439. doi: 10.1021/acs.jmedchem.8b00392. Epub 2018 Sep 9. J Med Chem. 2018. PMID: 30130103
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.
Meyers MJ, Arhancet GB, Hockerman SL, Chen X, Long SA, Mahoney MW, Rico JR, Garland DJ, Blinn JR, Collins JT, Yang S, Huang HC, McGee KF, Wendling JM, Dietz JD, Payne MA, Homer BL, Heron MI, Reitz DB, Hu X. Meyers MJ, et al. Among authors: hu x. J Med Chem. 2010 Aug 26;53(16):5979-6002. doi: 10.1021/jm100505n. J Med Chem. 2010. PMID: 20672822
Discovery of LYC-55716: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ) Agonist for Use in Treating Cancer.
Aicher TD, Van Huis CA, Hurd AR, Skalitzky DJ, Taylor CB, Beleh OM, Glick G, Toogood PL, Yang B, Zheng T, Huo C, Gao J, Qiao C, Tian X, Zhang J, Demock K, Hao LY, Lesch CA, Morgan RW, Moisan J, Wang Y, Scatina J, Paulos CM, Zou W, Carter LL, Hu X. Aicher TD, et al. Among authors: hu x. J Med Chem. 2021 Sep 23;64(18):13410-13428. doi: 10.1021/acs.jmedchem.1c00731. Epub 2021 Sep 9. J Med Chem. 2021. PMID: 34499493
Identification of a novel, non-tetrahydroquinoline variant of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib, with improved aqueous solubility.
Kalgutkar AS, Frederick KS, Hatch HL, Ambler CM, Perry DA, Garigipati RS, Chang GC, Lefker BA, Clark RW, Morehouse LA, Francone O, Hu X. Kalgutkar AS, et al. Among authors: hu x. Xenobiotica. 2014 Jul;44(7):591-605. doi: 10.3109/00498254.2013.874611. Epub 2013 Dec 31. Xenobiotica. 2014. PMID: 24380613
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