156 related articles for article (PubMed ID: 22780914)
1. Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disorders.
Verhoest PR; Fonseca KR; Hou X; Proulx-Lafrance C; Corman M; Helal CJ; Claffey MM; Tuttle JB; Coffman KJ; Liu S; Nelson F; Kleiman RJ; Menniti FS; Schmidt CJ; Vanase-Frawley M; Liras S
J Med Chem; 2012 Nov; 55(21):9045-54. PubMed ID: 22780914
[TBL] [Abstract][Full Text] [Related]
2. The selective phosphodiesterase 9 (PDE9) inhibitor PF-04447943 (6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one) enhances synaptic plasticity and cognitive function in rodents.
Hutson PH; Finger EN; Magliaro BC; Smith SM; Converso A; Sanderson PE; Mullins D; Hyde LA; Eschle BK; Turnbull Z; Sloan H; Guzzi M; Zhang X; Wang A; Rindgen D; Mazzola R; Vivian JA; Eddins D; Uslaner JM; Bednar R; Gambone C; Le-Mair W; Marino MJ; Sachs N; Xu G; Parmentier-Batteur S
Neuropharmacology; 2011 Sep; 61(4):665-76. PubMed ID: 21619887
[TBL] [Abstract][Full Text] [Related]
3. Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors.
Claffey MM; Helal CJ; Verhoest PR; Kang Z; Fors KS; Jung S; Zhong J; Bundesmann MW; Hou X; Lui S; Kleiman RJ; Vanase-Frawley M; Schmidt AW; Menniti F; Schmidt CJ; Hoffman WE; Hajos M; McDowell L; O'Connor RE; Macdougall-Murphy M; Fonseca KR; Becker SL; Nelson FR; Liras S
J Med Chem; 2012 Nov; 55(21):9055-68. PubMed ID: 23025719
[TBL] [Abstract][Full Text] [Related]
4. PDE9A inhibition rescues amyloid beta-induced deficits in synaptic plasticity and cognition.
Kroker KS; Mathis C; Marti A; Cassel JC; Rosenbrock H; Dorner-Ciossek C
Neurobiol Aging; 2014 Sep; 35(9):2072-8. PubMed ID: 24746365
[TBL] [Abstract][Full Text] [Related]
5. The Novel Phosphodiesterase 9A Inhibitor BI 409306 Increases Cyclic Guanosine Monophosphate Levels in the Brain, Promotes Synaptic Plasticity, and Enhances Memory Function in Rodents.
Rosenbrock H; Giovannini R; Schänzle G; Koros E; Runge F; Fuchs H; Marti A; Reymann KG; Schröder UH; Fedele E; Dorner-Ciossek C
J Pharmacol Exp Ther; 2019 Dec; 371(3):633-641. PubMed ID: 31578258
[No Abstract] [Full Text] [Related]
6. Phosphodiesterase 9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo.
Kleiman RJ; Chapin DS; Christoffersen C; Freeman J; Fonseca KR; Geoghegan KF; Grimwood S; Guanowsky V; Hajós M; Harms JF; Helal CJ; Hoffmann WE; Kocan GP; Majchrzak MJ; McGinnis D; McLean S; Menniti FS; Nelson F; Roof R; Schmidt AW; Seymour PA; Stephenson DT; Tingley FD; Vanase-Frawley M; Verhoest PR; Schmidt CJ
J Pharmacol Exp Ther; 2012 May; 341(2):396-409. PubMed ID: 22328573
[TBL] [Abstract][Full Text] [Related]
7. Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.
Verhoest PR; Proulx-Lafrance C; Corman M; Chenard L; Helal CJ; Hou X; Kleiman R; Liu S; Marr E; Menniti FS; Schmidt CJ; Vanase-Frawley M; Schmidt AW; Williams RD; Nelson FR; Fonseca KR; Liras S
J Med Chem; 2009 Dec; 52(24):7946-9. PubMed ID: 19919087
[TBL] [Abstract][Full Text] [Related]
8. Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia.
Verhoest PR; Chapin DS; Corman M; Fonseca K; Harms JF; Hou X; Marr ES; Menniti FS; Nelson F; O'Connor R; Pandit J; Proulx-Lafrance C; Schmidt AW; Schmidt CJ; Suiciak JA; Liras S
J Med Chem; 2009 Aug; 52(16):5188-96. PubMed ID: 19630403
[TBL] [Abstract][Full Text] [Related]
9. The selective phosphodiesterase 9 (PDE9) inhibitor PF-04447943 attenuates a scopolamine-induced deficit in a novel rodent attention task.
Vardigan JD; Converso A; Hutson PH; Uslaner JM
J Neurogenet; 2011 Dec; 25(4):120-6. PubMed ID: 22070409
[TBL] [Abstract][Full Text] [Related]
10. Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway.
Ioannidis S; Lamb ML; Wang T; Almeida L; Block MH; Davies AM; Peng B; Su M; Zhang HJ; Hoffmann E; Rivard C; Green I; Howard T; Pollard H; Read J; Alimzhanov M; Bebernitz G; Bell K; Ye M; Huszar D; Zinda M
J Med Chem; 2011 Jan; 54(1):262-76. PubMed ID: 21138246
[TBL] [Abstract][Full Text] [Related]
11. Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.
Certal V; Carry JC; Halley F; Virone-Oddos A; Thompson F; Filoche-Rommé B; El-Ahmad Y; Karlsson A; Charrier V; Delorme C; Rak A; Abecassis PY; Amara C; Vincent L; Bonnevaux H; Nicolas JP; Mathieu M; Bertrand T; Marquette JP; Michot N; Benard T; Perrin MA; Lemaitre O; Guerif S; Perron S; Monget S; Gruss-Leleu F; Doerflinger G; Guizani H; Brollo M; Delbarre L; Bertin L; Richepin P; Loyau V; Garcia-Echeverria C; Lengauer C; Schio L
J Med Chem; 2014 Feb; 57(3):903-20. PubMed ID: 24387221
[TBL] [Abstract][Full Text] [Related]
12. Application of neurophysiological biomarkers for Huntington's disease: evaluating a phosphodiesterase 9A inhibitor.
Nagy D; Tingley FD; Stoiljkovic M; Hajós M
Exp Neurol; 2015 Jan; 263():122-31. PubMed ID: 25315303
[TBL] [Abstract][Full Text] [Related]
13. Molecular dynamics-based discovery of novel phosphodiesterase-9A inhibitors with non-pyrazolopyrimidinone scaffolds.
Li Z; Lu X; Feng LJ; Gu Y; Li X; Wu Y; Luo HB
Mol Biosyst; 2015 Jan; 11(1):115-25. PubMed ID: 25328054
[TBL] [Abstract][Full Text] [Related]
14. Phosphodiesterase 9: insights from protein structure and role in therapeutics.
Singh N; Patra S
Life Sci; 2014 Jun; 106(1-2):1-11. PubMed ID: 24746902
[TBL] [Abstract][Full Text] [Related]
15. C33(S), a novel PDE9A inhibitor, protects against rat cardiac hypertrophy through upregulating cGMP signaling.
Wang PX; Li ZM; Cai SD; Li JY; He P; Huang Y; Feng GS; Luo HB; Chen SR; Liu PQ
Acta Pharmacol Sin; 2017 Sep; 38(9):1257-1268. PubMed ID: 28649129
[TBL] [Abstract][Full Text] [Related]
16. New 2,3-substituted 4,7-dihydro-6-(1'H-pyrazol-3'-yl)pyrazolo[1,5-a] pyrimidin-7-ones and related compounds: synthesis and benzodiazepine receptor binding study.
Selleri S; Bruni F; Costanzo A; Guerrini G; Casilli ML; Giusti L; Lucacchini A; Martini C
Farmaco; 1995 Oct; 50(10):679-87. PubMed ID: 8590575
[TBL] [Abstract][Full Text] [Related]
17. Discovery of ((S)-5-(methoxymethyl)-7-(1-methyl-1H-indol-2-yl)-2-(trifluoromethyl)-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-yl)((S)-2-(3-methylisoxazol-5-yl)pyrrolidin-1-yl)methanone as a potent and selective I(Kur) inhibitor.
Finlay HJ; Lloyd J; Vaccaro W; Kover A; Yan L; Bhave G; Prol J; Huynh T; Bhandaru R; Caringal Y; DiMarco J; Gan J; Harper T; Huang C; Conder ML; Sun H; Levesque P; Blanar M; Atwal K; Wexler R
J Med Chem; 2012 Apr; 55(7):3036-48. PubMed ID: 22409629
[TBL] [Abstract][Full Text] [Related]
18. Characterization of the first potent and selective PDE9 inhibitor using a cGMP reporter cell line.
Wunder F; Tersteegen A; Rebmann A; Erb C; Fahrig T; Hendrix M
Mol Pharmacol; 2005 Dec; 68(6):1775-81. PubMed ID: 16150925
[TBL] [Abstract][Full Text] [Related]
19. Discovery of a phosphodiesterase 9A inhibitor as a potential hypoglycemic agent.
Shao YX; Huang M; Cui W; Feng LJ; Wu Y; Cai Y; Li Z; Zhu X; Liu P; Wan Y; Ke H; Luo HB
J Med Chem; 2014 Dec; 57(24):10304-13. PubMed ID: 25432025
[TBL] [Abstract][Full Text] [Related]
20. Discovery of Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor for the Treatment of Cognitive Disorders.
Mikami S; Nakamura S; Ashizawa T; Nomura I; Kawasaki M; Sasaki S; Oki H; Kokubo H; Hoffman ID; Zou H; Uchiyama N; Nakashima K; Kamiguchi N; Imada H; Suzuki N; Iwashita H; Taniguchi T
J Med Chem; 2017 Sep; 60(18):7677-7702. PubMed ID: 28796496
[TBL] [Abstract][Full Text] [Related]
[Next] [New Search]
