title: Piperidine-renin inhibitors compounds with improved physicochemical properties.
abstract: Piperidine renin inhibitors with heterocyclic core modifications or hydrophilic attachments show improved physical properties (lower lipophilicity, improved solubility). Tetrahydroquinoline derivative rac-30 with a molecular weight of 517 and a log D(pH 7.4) of 1.9 displays potent and long lasting blood pressure lowering effects after oral administration to sodium depleted conscious marmosets.
authors.affiliation: Pharma Research Department, F. Hoffmann-La Roche Ltd., Basel, Switzerland.
authors.forename: R
authors.initials: R
authors.lastname: Güller
authors.forename: A
authors.initials: A
authors.lastname: Binggeli
authors.forename: V
authors.initials: V
authors.lastname: Breu
authors.forename: D
authors.initials: D
authors.lastname: Bur
authors.forename: W
authors.initials: W
authors.lastname: Fischli
authors.forename: G
authors.initials: G
authors.lastname: Hirth
authors.forename: C
authors.initials: C
authors.lastname: Jenny
authors.forename: M
authors.initials: M
authors.lastname: Kansy
authors.forename: F
authors.initials: F
authors.lastname: Montavon
authors.forename: M
authors.initials: M
authors.lastname: Müller
authors.forename: C
authors.initials: C
authors.lastname: Oefner
authors.forename: H
authors.initials: H
authors.lastname: Stadler
authors.forename: E
authors.initials: E
authors.lastname: Vieira
authors.forename: M
authors.initials: M
authors.lastname: Wilhelm
authors.forename: W
authors.initials: W
authors.lastname: Wostl
authors.forename: H P
authors.initials: HP
authors.lastname: Märki
mesh_terms: D000818:Animals; D000959:Antihypertensive Agents / Q000737:chemistry* / Q000494:pharmacology; D002144:Callithrix; D004305:Dose-Response Relationship, Drug; D006801:Humans; D010880:Piperidines / Q000737:chemistry* / Q000494:pharmacology; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D000092502:Renin Inhibitors
chemical_list: D000959:Antihypertensive Agents; D010880:Piperidines; D011994:Recombinant Proteins; D000092502:Renin Inhibitors