226228-88-2Relevant academic research and scientific papers
PIPERAZINYL 3-AMINOPYRROLIDINE DERIVATIVES AS A CCR2 ANTAGONIST
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, (2012/07/31)
The present invention relates to compounds of chemical formula 1 and having CCR2 (chemokine receptor 2) antagonistic effects, and salts or isomers thereof. These compounds are very useful for treating, preventing, or relieving rheumatoid arthritis, arteri
Discovery of INCB3284, a potent, selective, and orally bioavailable hCCR2 antagonist
Xue, Chu-Biao,Feng, Hao,Cao, Ganfeng,Huang, Taisheng,Glenn, Joseph,Anand, Rajan,Meloni, David,Zhang, Ke,Kong, Lingquan,Wang, Anlai,Zhang, Yingxin,Zheng, Changsheng,Xia, Michael,Chen, Lihua,Tanaka, Hiroyuki,Han, Qi,Robinson,Modi, Dilip,Storace, Lou,Shao, Lixin,Sharief, Vaqar,Li, Mei,Galya, Laurine G.,Covington, Maryanne,Scherle, Peggy,Diamond, Sharon,Emm, Tom,Yeleswaram, Swamy,Contel, Nancy,Vaddi, Kris,Newton, Robert,Hollis, Greg,Friedman, Steven,Metcalf, Brian
, p. 450 - 454 (2011/08/22)
We report the identification of 13 (INCB3284) as a potent human CCR2 (hCCR2) antagonist. INCB3284 exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC 50 of 4.7 nM in antagonism of c
Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists
Lim, Jee Woong,Oh, Youna,Kim, Jong-Hoon,Oak, Min-Ho,Na, Yongho,Lee, Jung-Ok,Lee, Seung-Woo,Cho, Heeyeong,Park, Woo-Kyu,Choi, Gildon,Kang, Jongmin
scheme or table, p. 2099 - 2102 (2010/07/06)
Novel 3-aminopyrrolidine derivatives were synthesized and evaluated for their antagonistic activity against human chemokine receptor 2. Structure-activity studies on 3-aminopyrrolidine incorporating heteroatomic carbocycle moieties led to piperidine compo
Potent antagonists of the CCR2b receptor. Part 3: SAR of the (R)-3-aminopyrrolidine series
Moree, Wilna J.,Kataoka, Ken-ichiro,Ramirez-Weinhouse, Michele M.,Shiota, Tatsuki,Imai, Minoru,Tsutsumi, Takaharu,Sudo, Masaki,Endo, Noriaki,Muroga, Yumiko,Hada, Takahiko,Fanning, Dewey,Saunders, John,Kato, Yoshinori,Myers, Peter L.,Tarby, Christine M.
, p. 1869 - 1873 (2008/09/19)
SAR studies were conducted around lead compound 1 using high-throughput parallel solution and solid phase synthesis. Our lead optimization efforts led to the identification of several CCR2b antagonists with potent activity in both binding and functional a
