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Items: 1 to 20 of 166

1.

Highly potent, selective, and orally active phosphodiesterase 10A inhibitors.

Malamas MS, Ni Y, Erdei J, Stange H, Schindler R, Lankau HJ, Grunwald C, Fan KY, Parris K, Langen B, Egerland U, Hage T, Marquis KL, Grauer S, Brennan J, Navarra R, Graf R, Harrison BL, Robichaud A, Kronbach T, Pangalos MN, Hoefgen N, Brandon NJ.

J Med Chem. 2011 Nov 10;54(21):7621-38. doi: 10.1021/jm2009138.

PMID:
21988093
2.

Novel triazines as potent and selective phosphodiesterase 10A inhibitors.

Malamas MS, Stange H, Schindler R, Lankau HJ, Grunwald C, Langen B, Egerland U, Hage T, Ni Y, Erdei J, Fan KY, Parris K, Marquis KL, Grauer S, Brennan J, Navarra R, Graf R, Harrison BL, Robichaud A, Kronbach T, Pangalos MN, Brandon NJ, Hoefgen N.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5876-84. doi: 10.1016/j.bmcl.2012.07.076.

PMID:
22902656
3.

Use of structure-based design to discover a potent, selective, in vivo active phosphodiesterase 10A inhibitor lead series for the treatment of schizophrenia.

Helal CJ, Kang Z, Hou X, Pandit J, Chappie TA, Humphrey JM, Marr ES, Fennell KF, Chenard LK, Fox C, Schmidt CJ, Williams RD, Chapin DS, Siuciak J, Lebel L, Menniti F, Cianfrogna J, Fonseca KR, Nelson FR, O'Connor R, MacDougall M, McDowell L, Liras S.

J Med Chem. 2011 Jul 14;54(13):4536-47. doi: 10.1021/jm2001508.

PMID:
21650160
4.

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 27;52(16):5188-96. doi: 10.1021/jm900521k.

PMID:
19630403
5.

Discovery of potent, selective, and metabolically stable 4-(pyridin-3-yl)cinnolines as novel phosphodiesterase 10A (PDE10A) inhibitors.

Hu E, Kunz RK, Rumfelt S, Chen N, Bürli R, Li C, Andrews KL, Zhang J, Chmait S, Kogan J, Lindstrom M, Hitchcock SA, Treanor J.

Bioorg Med Chem Lett. 2012 Mar 15;22(6):2262-5. doi: 10.1016/j.bmcl.2012.01.086.

PMID:
22365755
6.

The SAR development of dihydroimidazoisoquinoline derivatives as phosphodiesterase 10A inhibitors for the treatment of schizophrenia.

Ho GD, Michael Seganish W, Bercovici A, Tulshian D, Greenlee WJ, Van Rijn R, Hruza A, Xiao L, Rindgen D, Mullins D, Guzzi M, Zhang X, Bleickardt C, Hodgson R.

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2585-9. doi: 10.1016/j.bmcl.2012.01.113.

PMID:
22377514
7.

Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors.

Höfgen N, Stange H, Schindler R, Lankau HJ, Grunwald C, Langen B, Egerland U, Tremmel P, Pangalos MN, Marquis KL, Hage T, Harrison BL, Malamas MS, Brandon NJ, Kronbach T.

J Med Chem. 2010 Jun 10;53(11):4399-411. doi: 10.1021/jm1002793.

PMID:
20450197
8.

Inhibition of the striatum-enriched phosphodiesterase PDE10A: a novel approach to the treatment of psychosis.

Siuciak JA, Chapin DS, Harms JF, Lebel LA, McCarthy SA, Chambers L, Shrikhande A, Wong S, Menniti FS, Schmidt CJ.

Neuropharmacology. 2006 Aug;51(2):386-96.

PMID:
16780899
9.

Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).

Hu E, Chen N, Bourbeau MP, Harrington PE, Biswas K, Kunz RK, Andrews KL, Chmait S, Zhao X, Davis C, Ma J, Shi J, Lester-Zeiner D, Danao J, Able J, Cueva M, Talreja S, Kornecook T, Chen H, Porter A, Hungate R, Treanor J, Allen JR.

J Med Chem. 2014 Aug 14;57(15):6632-41. doi: 10.1021/jm500713j.

PMID:
25062128
10.

Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors.

Chappie TA, Humphrey JM, Allen MP, Estep KG, Fox CB, Lebel LA, Liras S, Marr ES, Menniti FS, Pandit J, Schmidt CJ, Tu M, Williams RD, Yang FV.

J Med Chem. 2007 Jan 25;50(2):182-5.

PMID:
17228859
11.

Pharmacology of JNJ-42314415, a centrally active phosphodiesterase 10A (PDE10A) inhibitor: a comparison of PDE10A inhibitors with D2 receptor blockers as potential antipsychotic drugs.

Megens AA, Hendrickx HM, Hens KA, Fonteyn I, Langlois X, Lenaerts I, Somers MV, de Boer P, Vanhoof G.

J Pharmacol Exp Ther. 2014 Apr;349(1):138-54. doi: 10.1124/jpet.113.211904.

12.

Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.

Kehler J, Ritzen A, Langgård M, Petersen SL, Farah MM, Bundgaard C, Christoffersen CT, Nielsen J, Kilburn JP.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3738-42. doi: 10.1016/j.bmcl.2011.04.067.

PMID:
21602043
13.

The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey.

Smith SM, Uslaner JM, Cox CD, Huszar SL, Cannon CE, Vardigan JD, Eddins D, Toolan DM, Kandebo M, Yao L, Raheem IT, Schreier JD, Breslin MJ, Coleman PJ, Renger JJ.

Neuropharmacology. 2013 Jan;64:215-23. doi: 10.1016/j.neuropharm.2012.06.013.

PMID:
22750078
14.

Preclinical characterization of selective phosphodiesterase 10A inhibitors: a new therapeutic approach to the treatment of schizophrenia.

Schmidt CJ, Chapin DS, Cianfrogna J, Corman ML, Hajos M, Harms JF, Hoffman WE, Lebel LA, McCarthy SA, Nelson FR, Proulx-LaFrance C, Majchrzak MJ, Ramirez AD, Schmidt K, Seymour PA, Siuciak JA, Tingley FD 3rd, Williams RD, Verhoest PR, Menniti FS.

J Pharmacol Exp Ther. 2008 May;325(2):681-90. doi: 10.1124/jpet.107.132910.

15.

Current landscape of phosphodiesterase 10A (PDE10A) inhibition.

Chappie TA, Helal CJ, Hou X.

J Med Chem. 2012 Sep 13;55(17):7299-331. doi: 10.1021/jm3004976. No abstract available.

PMID:
22834877
16.

Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia.

Grauer SM, Pulito VL, Navarra RL, Kelly MP, Kelley C, Graf R, Langen B, Logue S, Brennan J, Jiang L, Charych E, Egerland U, Liu F, Marquis KL, Malamas M, Hage T, Comery TA, Brandon NJ.

J Pharmacol Exp Ther. 2009 Nov;331(2):574-90. doi: 10.1124/jpet.109.155994.

17.

Use of structure based design to increase selectivity of pyridyl-cinnoline phosphodiesterase 10A (PDE10A) inhibitors against phosphodiesterase 3 (PDE3).

Hu E, Kunz RK, Rumfelt S, Andrews KL, Li C, Hitchcock SA, Lindstrom M, Treanor J.

Bioorg Med Chem Lett. 2012 Nov 15;22(22):6938-42. doi: 10.1016/j.bmcl.2012.09.010.

PMID:
23044369
18.

Discovery of 4-hydroxy-1,6-naphthyridine-3-carbonitrile derivatives as novel PDE10A inhibitors.

Bauer U, Giordanetto F, Bauer M, O'Mahony G, Johansson KE, Knecht W, Hartleib-Geschwindner J, Carlsson ET, Enroth C.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1944-8. doi: 10.1016/j.bmcl.2012.01.046.

PMID:
22321214
19.

Discovery of benzo[d]imidazo[5,1-b]thiazole as a new class of phosphodiesterase 10A inhibitors.

Banerjee A, Narayana L, Raje FA, Pisal DV, Kadam PA, Gullapalli S, Kumar H, More SV, Bajpai M, Sangana RR, Jadhav S, Gudi GS, Khairatkar-Joshi N, Merugu RR, Voleti SR, Gharat LA.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6747-54. doi: 10.1016/j.bmcl.2013.10.027.

PMID:
24231362
20.

Discovery of 1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one (TAK-063), a highly potent, selective, and orally active phosphodiesterase 10A (PDE10A) inhibitor.

Kunitomo J, Yoshikawa M, Fushimi M, Kawada A, Quinn JF, Oki H, Kokubo H, Kondo M, Nakashima K, Kamiguchi N, Suzuki K, Kimura H, Taniguchi T.

J Med Chem. 2014 Nov 26;57(22):9627-43. doi: 10.1021/jm5013648.

PMID:
25384088
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