Tetrahydroquinoline derivatives as CRTH2 antagonists.
A series of tetrahydroquinoline-derived inhibitors of the CRTH2 receptor was discovered by a high throughput screen. Optimization of these compounds for potency and pharmacokinetic properties led to the discovery of potent and orally bioavailable CRTH2 antagonists.
Liu
Jiwen
J
Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. jiwenl@amgen.com
Wang
Yingcai
Y
Sun
Ying
Y
Marshall
Derek
D
Miao
Shichang
S
Tonn
George
G
Anders
Penny
P
Tocker
Joel
J
Tang
H Lucy
HL
Medina
Julio
J
D018926:Anti-Allergic Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D002460:Cell Line; D048430:Cell Shape / Q000187:drug effects; D055808:Drug Discovery; D004804:Eosinophils / Q000187:drug effects / Q000276:immunology; D006801:Humans; D011804:Quinolines / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors*; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors*
D018926:Anti-Allergic Agents; D011804:Quinolines; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; C542964:1,2,3,4-tetrahydroquinoline; C036293:prostaglandin D2 receptor