title: The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery.
abstract: Ionizable groups were introduced onto the 10,11-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine scaffold of the vasopressin V2-antagonist WAY-VPA-985 in the search for molecules optimized for parenteral formulation. The synthesis and structure activity relationships (SAR) are presented together with solubility data in a model parenteral system. The amine, WAY-140288 (4f), was chosen for further development. p6
authors.affiliation: Wyeth-Ayerst Research, Princeton, NJ 08543, USA. ashwellm@war.wyeth.com
authors.forename: M A
authors.initials: MA
authors.lastname: Ashwell
authors.forename: J F
authors.initials: JF
authors.lastname: Bagli
authors.forename: T J
authors.initials: TJ
authors.lastname: Caggiano
authors.forename: P S
authors.initials: PS
authors.lastname: Chan
authors.forename: A J
authors.initials: AJ
authors.lastname: Molinari
authors.forename: C
authors.initials: C
authors.lastname: Palka
authors.forename: C H
authors.initials: CH
authors.lastname: Park
authors.forename: J F
authors.initials: JF
authors.lastname: Rogers
authors.forename: M
authors.initials: M
authors.lastname: Sherman
authors.forename: E J
authors.initials: EJ
authors.lastname: Trybulski
authors.forename: D K
authors.initials: DK
authors.lastname: Williams
mesh_terms: D065092:Antidiuretic Hormone Receptor Antagonists; D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry*; D001569:Benzodiazepines / Q000737:chemistry*; D006801:Humans; D007263:Infusions, Parenteral; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D065092:Antidiuretic Hormone Receptor Antagonists; D001549:Benzamides; D011758:Pyrroles; D001569:Benzodiazepines; C409452:lixivaptan