title: Potent, selective MCH-1 receptor antagonists.
abstract: This paper describes the lead optimization of a new series of potent, selective, orally bioavailable, brain-penetrant MCH-1 receptor antagonists. A major focus of the work was to achieve a selectivity profile appropriate for in vivo efficacy studies and safety.
authors.affiliation: Discovery Chemistry, Hoffmann-La Roche, Inc., 340 Kingsland Street, Nutley, NJ 07110, USA.
authors.forename: Shawn D
authors.initials: SD
authors.lastname: Erickson
authors.forename: Bruce
authors.initials: B
authors.lastname: Banner
authors.forename: Steven
authors.initials: S
authors.lastname: Berthel
authors.forename: Karin
authors.initials: K
authors.lastname: Conde-Knape
authors.forename: Fiorenza
authors.initials: F
authors.lastname: Falcioni
authors.forename: Irina
authors.initials: I
authors.lastname: Hakimi
authors.forename: Bernard
authors.initials: B
authors.lastname: Hennessy
authors.forename: Robert F
authors.initials: RF
authors.lastname: Kester
authors.forename: Kyungjin
authors.initials: K
authors.lastname: Kim
authors.forename: Chun
authors.initials: C
authors.lastname: Ma
authors.forename: Warren
authors.initials: W
authors.lastname: McComas
authors.forename: Francis
authors.initials: F
authors.lastname: Mennona
authors.forename: Steven
authors.initials: S
authors.lastname: Mischke
authors.forename: Lucy
authors.initials: L
authors.lastname: Orzechowski
authors.forename: Yimin
authors.initials: Y
authors.lastname: Qian
authors.forename: Hamid
authors.initials: H
authors.lastname: Salari
authors.forename: John
authors.initials: J
authors.lastname: Tengi
authors.forename: Kshitij
authors.initials: K
authors.lastname: Thakkar
authors.forename: Rebecca
authors.initials: R
authors.lastname: Taub
authors.forename: Jefferson W
authors.initials: JW
authors.lastname: Tilley
authors.forename: Hong
authors.initials: H
authors.lastname: Wang
mesh_terms: D000577:Amides / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D001562:Benzimidazoles / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D018360:Crystallography, X-Ray; D006801:Humans; D007189:Indans / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D007700:Kinetics; D010880:Piperidines / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D001562:Benzimidazoles; D007189:Indans; C103263:MCHR1 protein, human; D010880:Piperidines; D017481:Receptors, Somatostatin