Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma.

Sturdivant, Jill M; Royalty, Susan M; Lin, Cheng-Wen; Moore, Lori A; Yingling, Jeffrey D; Laethem, Carmen L; Sherman, Bryan; Heintzelman, Geoffrey R; Kopczynski, Casey C; deLong, Mitchell A

Sturdivant, Jill M; Royalty, Susan M; Lin, Cheng-Wen; Moore, Lori A; Yingling, Jeffrey D; Laethem, Carmen L; Sherman, Bryan; Heintzelman, Geoffrey R; Kopczynski, Casey C; deLong, Mitchell A.

Affiliation

Sturdivant JM; Aerie Pharmaceuticals, Inc., 4301 Emperor Boulevard, Suite 400, Durham, NC 27703, United States. Electronic address: jsturdivant@aeriepharma.com.
Royalty SM; Aerie Pharmaceuticals, Inc., 4301 Emperor Boulevard, Suite 400, Durham, NC 27703, United States.
Lin CW; Aerie Pharmaceuticals, Inc., 4301 Emperor Boulevard, Suite 400, Durham, NC 27703, United States.
Moore LA; Aerie Pharmaceuticals, Inc., 4301 Emperor Boulevard, Suite 400, Durham, NC 27703, United States.
Yingling JD; Aerie Pharmaceuticals, Inc., 4301 Emperor Boulevard, Suite 400, Durham, NC 27703, United States.
Laethem CL; Aerie Pharmaceuticals, Inc., 4301 Emperor Boulevard, Suite 400, Durham, NC 27703, United States.
Sherman B; Aerie Pharmaceuticals, Inc., 4301 Emperor Boulevard, Suite 400, Durham, NC 27703, United States.
Heintzelman GR; Aerie Pharmaceuticals, Inc., 4301 Emperor Boulevard, Suite 400, Durham, NC 27703, United States.
Kopczynski CC; Aerie Pharmaceuticals, Inc., 4301 Emperor Boulevard, Suite 400, Durham, NC 27703, United States.
deLong MA; Aerie Pharmaceuticals, Inc., 4301 Emperor Boulevard, Suite 400, Durham, NC 27703, United States.

Bioorg Med Chem Lett ; 26(10): 2475-2480, 2016 05 15.

Article in En | MEDLINE | ID: mdl-27072905

Subject(s)

Benzoates/pharmacology; Glaucoma, Open-Angle/drug therapy; Protein Kinase Inhibitors/chemistry; Protein Kinase Inhibitors/pharmacology; beta-Alanine/analogs & derivatives; rho-Associated Kinases/antagonists & inhibitors; Animals; Disease Models, Animal; Drug Evaluation, Preclinical/methods; Humans; Intraocular Pressure/drug effects; Molecular Structure; Norepinephrine Plasma Membrane Transport Proteins/antagonists & inhibitors; Protein Kinase Inhibitors/chemical synthesis; Rabbits; Serotonin Plasma Membrane Transport Proteins/metabolism; Structure-Activity Relationship; Trabecular Meshwork/drug effects; beta-Alanine/pharmacology

Key words

AR-13324; Glaucoma; Intraocular pressure (IOP); Rho kinase (ROCK); Trabecular meshwork

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Benzoates / Glaucoma, Open-Angle / Beta-Alanine / Protein Kinase Inhibitors / Rho-Associated Kinases Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Year: 2016 Document type: Article

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