Bioorganic and Medicinal Chemistry Letters p. 1036 - 1040 (2011)
Update date:2022-08-05
Topics:
Stock, Nicholas
Volkots, Deborah
Stebbins, Karin
Broadhead, Alex
Stearns, Brian
Roppe, Jeffrey
Parr, Timothy
Baccei, Christopher
Bain, Gretchen
Chapman, Charles
Correa, Lucia
Darlington, Janice
King, Christopher
Lee, Catherine
Lorrain, Daniel S.
Prodanovich, Pat
Santini, Angelina
Evans, Jilly F.
Hutchinson, John H.
Prasit, Peppi
Compound 21 (AM432) was identified as a potent and selective antagonist of the DP2 receptor (CRTH2). Modification of a bi-aryl core identified a series of tri-aryl antagonists of which compound 21 proved a viable clinical candidate. AM432 shows excellent potency in a human whole blood eosinophil shape change assay with prolonged incubation, a comparatively long off-rate from the DP2 receptor, excellent pharmacokinetics in dog and in vivo activity in two mouse models of inflammatory disease after oral dosing.
View MoreLonzeal Pharmaceuticals Co., Ltd.
website:http://www.lonzeal.com
Contact:+86-13381011962
Address:RM 801, Yue MOMA, No. 26 Anningzhuang Rd. Haidian District, Beijing, China
Contact:0086 371 65711996
Address:Jalan 4/3, Kawasan Perindustrian Serendah, 48000 Rawang,
Contact:+86-371-86058576
Address:NO.32, Jingsan Road, Zhengzhou, China
Contact:86-27-84888681
Address:Wuhan economic & technology development zone
hangzhou verychem science and technology co.ltd
website:http://www.verypharm.com
Contact:+86-571-88162785; 88162786
Address:F1502, 753 Shenhua road, Hangzhou, China
Doi:10.1007/BF00481520
(1989)Doi:10.1016/S0040-4039(00)94542-8
(1990)Doi:10.1016/S0040-4039(01)80579-7
(1989)Doi:10.1021/jm00376a024
(1984)Doi:10.1016/j.tetlet.2006.08.060
(2006)Doi:10.1021/acs.orglett.0c01032
(2020)