title: Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of tertiary alcohol-bearing piperidines.
abstract: The design and optimization of a novel series of renin inhibitor is described herein. Strategically, by committing the necessary resources to the development of synthetic sequences and scaffolds that were most amenable for late stage structural diversification, even as the focus of the SAR campaign moved from one end of the molecule to another, highly potent renin inhibitors could be rapidly identified and profiled.
authors.affiliation: Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Highway, Kirkland, Québec, Canada H9H 3L1. austin.chihyu.chen@gmail.com
authors.forename: Austin
authors.initials: A
authors.lastname: Chen
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Cauchon
authors.forename: Amandine
authors.initials: A
authors.lastname: Chefson
authors.forename: Sarah
authors.initials: S
authors.lastname: Dolman
authors.forename: Yves
authors.initials: Y
authors.lastname: Ducharme
authors.forename: Daniel
authors.initials: D
authors.lastname: Dubé
authors.forename: Jean-Pierre
authors.initials: JP
authors.lastname: Falgueyret
authors.forename: Pierre-André
authors.initials: PA
authors.lastname: Fournier
authors.forename: Sébastien
authors.initials: S
authors.lastname: Gagné
authors.forename: Michel
authors.initials: M
authors.lastname: Gallant
authors.forename: Erich
authors.initials: E
authors.lastname: Grimm
authors.forename: Yongxin
authors.initials: Y
authors.lastname: Han
authors.forename: Robert
authors.initials: R
authors.lastname: Houle
authors.forename: Jing-Qi
authors.initials: JQ
authors.lastname: Huang
authors.forename: Gregory
authors.initials: G
authors.lastname: Hughes
authors.forename: Hélène
authors.initials: H
authors.lastname: Jûteau
authors.forename: Patrick
authors.initials: P
authors.lastname: Lacombe
authors.forename: Sophie
authors.initials: S
authors.lastname: Lauzon
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Lévesque
authors.forename: Susana
authors.initials: S
authors.lastname: Liu
authors.forename: Dwight
authors.initials: D
authors.lastname: Macdonald
authors.forename: Bruce
authors.initials: B
authors.lastname: Mackay
authors.forename: Dan
authors.initials: D
authors.lastname: McKay
authors.forename: M David
authors.initials: MD
authors.lastname: Percival
authors.forename: René
authors.initials: R
authors.lastname: St-Jacques
authors.forename: Sylvie
authors.initials: S
authors.lastname: Toulmond
mesh_terms: D000438:Alcohols / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D015195:Drug Design; D006973:Hypertension / Q000188:drug therapy*; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D051381:Rats; D012083:Renin / Q000737:chemistry; D013329:Structure-Activity Relationship; D000092502:Renin Inhibitors
chemical_list: D000438:Alcohols; D000959:Antihypertensive Agents; D010880:Piperidines; D012083:Renin; D000092502:Renin Inhibitors