501446-70-4Relevant articles and documents
Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication
Skerlj, Renato,Bridger, Gary,Zhou, Yuanxi,Bourque, Elyse,McEachern, Ernest,Langille, Jonathan,Harwig, Curtis,Veale, Duane,Yang, Wen,Li, Tongshong,Zhu, Yongbao,Bey, Michael,Baird, Ian,Sartori, Michael,Metz, Markus,Mosi, Renee,Nelson, Kim,Bodart, Veronique,Wong, Rebecca,Fricker, Simon,Mac Farland, Ron,Huskens, Dana,Schols, Dominique
, p. 6950 - 6954 (2012/01/13)
A series of CCR5 antagonists were optimized for potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells. Compounds that met acceptable ADME criteria, selectivity, human plasma protein binding, potency shift in the presence of α-glycoprotein were evaluated in rat and dog pharmacokinetics.
Piperidine derivatives useful as CCR5 antagonists
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Page/Page column 29; 35, (2010/02/05)
The present invention provides a compound of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R9, R10, A and B are as defined in the specification. The present invention also provides pharmaceutical compositions containing the compound of this invention, and methods of treatment using the compound of this invention. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.