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(b) Tagat, J. R.; Steensma, R. W.; McCombie, S. W.; Nazareno, D. V.; Lin, S.; Neustadt, B. R.; Cox, K.; Xu, S.; Wojcik, L.; Murray, M. G.; Vantuno, N.; Baroudy, B. M.; Strizki, J. M. Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II: The discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-trifluoromehtyl)phenyl]ethyl]-1-piperazinyl] piperidine N1-oxide (Sch 350634), an orally bioavailable, potent CCR5 antagonist. J. Med Chem. 2001, 44, 3343-3346.
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50
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(d) Tagat, J. R.; McCombie, S. W.; Nazareno, D.; Labroli, M. A.; Xiao, Y.; Steensma, R. W.; Strizki, J. M.; Baroudy, B. M.; Cox, K.; Lachowicz, J.; Varty, G.; Watkins, R. Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV: Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-[4-{2-methoxy-1(R)- 4-(trifluoromethyl)-phenyl}ethyl-3(S)-methyl-1-piperazinyl]-4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective and orally bioavailable CCR5 antagonist. J. Med. Chem. 2004, 47, 2405-2408.
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