title: Biarylsulfonamide CCR9 inhibitors for inflammatory bowel disease.
abstract: Inflammatory bowel disease, including Crohn's disease and ulcerative colitis, affects millions of people worldwide. CCR9 has been shown to be a key chemokine receptor mediating the local inflammatory responses in the GI tract. The CCR9 inhibitor Vercirnon advanced to phase 3 clinical trials, but carries several liabilities which we sought to improve.
authors.affiliation: Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States. Electronic address: jackzhang49@yahoo.com.
authors.forename: Jing
authors.initials: J
authors.lastname: Zhang
authors.affiliation: Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
authors.forename: Jan
authors.initials: J
authors.lastname: Romero
authors.affiliation: Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
authors.forename: Audrey
authors.initials: A
authors.lastname: Chan
authors.affiliation: Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
authors.forename: Jennifer
authors.initials: J
authors.lastname: Goss
authors.affiliation: Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
authors.forename: Sabrina
authors.initials: S
authors.lastname: Stucka
authors.affiliation: Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
authors.forename: Jason
authors.initials: J
authors.lastname: Cross
authors.affiliation: Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
authors.forename: Brian
authors.initials: B
authors.lastname: Chamberlain
authors.affiliation: Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
authors.forename: Mustafa
authors.initials: M
authors.lastname: Varoglu
authors.affiliation: Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
authors.forename: Haoqun
authors.initials: H
authors.lastname: Chandonnet
authors.affiliation: Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
authors.forename: Dominic
authors.initials: D
authors.lastname: Ryan
authors.affiliation: Cubist Pharmaceuticals, 65 Hayden Avenue, Lexington, MA 02421, United States.
authors.forename: Blaise
authors.initials: B
authors.lastname: Lippa
mesh_terms: D000818:Animals; D060326:Chemistry Techniques, Synthetic; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006801:Humans; D015212:Inflammatory Bowel Diseases / Q000188:drug therapy*; D020128:Inhibitory Concentration 50; D051379:Mice; D054388:Receptors, CCR / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: C119309:CC chemokine receptor 9; C583420:CCX282-B; D054388:Receptors, CCR; D013449:Sulfonamides
keywords: CCR9; Crohn’s disease; IBD; Sulfonamide; Ulcerative colitis