title: Water-soluble PDE4 inhibitors for the treatment of dry eye.
abstract: PDE4 inhibitors have the potential to alleviate the symptoms and underlying inflammation associated with dry eye. Disclosed herein is the development of a novel series of water-soluble PDE4 inhibitors. Our studies led to the discovery of coumarin 18, which is effective in a rabbit model of dry eye and a tear secretion test in rats.
authors.affiliation: Kalypsys, Inc., 10420 Wateridge Circle, San Diego, CA 92121, United States. sgovek@san.rr.com
authors.forename: Steven P
authors.initials: SP
authors.lastname: Govek
authors.forename: Guy
authors.initials: G
authors.lastname: Oshiro
authors.forename: John V
authors.initials: JV
authors.lastname: Anzola
authors.forename: Clay
authors.initials: C
authors.lastname: Beauregard
authors.forename: Jasmine
authors.initials: J
authors.lastname: Chen
authors.forename: Avery R
authors.initials: AR
authors.lastname: Coyle
authors.forename: Daniel A
authors.initials: DA
authors.lastname: Gamache
authors.forename: Mark R
authors.initials: MR
authors.lastname: Hellberg
authors.forename: Jennifer N
authors.initials: JN
authors.lastname: Hsien
authors.forename: Julia M
authors.initials: JM
authors.lastname: Lerch
authors.forename: John C
authors.initials: JC
authors.lastname: Liao
authors.forename: James W
authors.initials: JW
authors.lastname: Malecha
authors.forename: Lena M
authors.initials: LM
authors.lastname: Staszewski
authors.forename: David J
authors.initials: DJ
authors.lastname: Thomas
authors.forename: John M
authors.initials: JM
authors.lastname: Yanni
authors.forename: Stewart A
authors.initials: SA
authors.lastname: Noble
authors.forename: Andrew K
authors.initials: AK
authors.lastname: Shiau
mesh_terms: D015761:4-Aminopyridine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D001665:Binding Sites; D003198:Computer Simulation; D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4 / Q000378:metabolism; D004195:Disease Models, Animal; D015352:Dry Eye Syndromes / Q000188:drug therapy; D058988:Phosphodiesterase 4 Inhibitors; D011817:Rabbits; D051381:Rats; D014867:Water / Q000737:chemistry*
chemical_list: D000893:Anti-Inflammatory Agents; D003374:Coumarins; D058988:Phosphodiesterase 4 Inhibitors; D014867:Water; D015761:4-Aminopyridine; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4