- Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate
-
Computational modeling was used to direct the synthesis of analogs of previously reported phosphodiesterase 2A (PDE2A) inhibitor 1 with an imidazotriazine core to yield compounds of significantly enhanced potency. The analog PF-05180999 (30) was subsequen
- Helal, Christopher J.,Arnold, Eric,Boyden, Tracey,Chang, Cheng,Chappie, Thomas A.,Fisher, Ethan,Hajos, Mihaly,Harms, John F.,Hoffman, William E.,Humphrey, John M.,Pandit, Jayvardhan,Kang, Zhijun,Kleiman, Robin J.,Kormos, Bethany L.,Lee, Che-Wah,Lu, Jiemin,Maklad, Noha,McDowell, Laura,McGinnis, Dina,O'Connor, Rebecca E.,O'Donnell, Christopher J.,Ogden, Adam,Piotrowski, Mary,Schmidt, Christopher J.,Seymour, Patricia A.,Ueno, Hirokazu,Vansell, Nichole,Verhoest, Patrick R.,Yang, Edward X.
-
p. 1001 - 1018
(2018/02/17)
-
- Imidazo[5,1-f][1,2,4]Triazines for the Treatment of Neurological Disorders
-
The present invention relates to compounds of the Formula and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal.
- -
-
-