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1.
Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.
Bioorg Med Chem Lett
; 25(3): 444-50, 2015 Feb 01.
Article
in English
| MEDLINE | ID: mdl-25577040
2.
Shaping suvorexant: application of experimental and theoretical methods for driving synthetic designs.
J Comput Aided Mol Des
; 28(1): 5-12, 2014 Jan.
Article
in English
| MEDLINE | ID: mdl-24488306
3.
2-Aminopyridines as Potent and Selective Nav1.8 Inhibitors Exhibiting Efficacy in a Nonhuman Primate Pain Model.
ACS Med Chem Lett
; 15(6): 917-923, 2024 Jun 13.
Article
in English
| MEDLINE | ID: mdl-38894930
4.
Fluorinated Isoindolinone-Based Glucosylceramide Synthase Inhibitors with Low Human Dose Projections.
ACS Med Chem Lett
; 15(1): 123-131, 2024 Jan 11.
Article
in English
| MEDLINE | ID: mdl-38229758
5.
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Bioorg Med Chem Lett
; 22(18): 5903-8, 2012 Sep 15.
Article
in English
| MEDLINE | ID: mdl-22892116
6.
Promotion of sleep by suvorexant-a novel dual orexin receptor antagonist.
J Neurogenet
; 25(1-2): 52-61, 2011 Mar.
Article
in English
| MEDLINE | ID: mdl-21473737
7.
Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation.
Nat Commun
; 12(1): 815, 2021 02 05.
Article
in English
| MEDLINE | ID: mdl-33547286
8.
Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis.
J Med Chem
; 46(22): 4790-8, 2003 Oct 23.
Article
in English
| MEDLINE | ID: mdl-14561098
9.
The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey.
Neuropharmacology
; 64: 215-23, 2013 Jan.
Article
in English
| MEDLINE | ID: mdl-22750078
10.
Pharmacological characterization of MK-6096 - a dual orexin receptor antagonist for insomnia.
Neuropharmacology
; 62(2): 978-87, 2012 Feb.
Article
in English
| MEDLINE | ID: mdl-22019562
11.
Discovery of [(2R,5R)-5-{[(5-fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties.
ChemMedChem
; 7(3): 415-24, 337, 2012 Mar 05.
Article
in English
| MEDLINE | ID: mdl-22307992
12.
Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia.
J Med Chem
; 53(14): 5320-32, 2010 Jul 22.
Article
in English
| MEDLINE | ID: mdl-20565075
13.
Discovery of a potent, CNS-penetrant orexin receptor antagonist based on an n,n-disubstituted-1,4-diazepane scaffold that promotes sleep in rats.
ChemMedChem
; 4(7): 1069-74, 2009 Jul.
Article
in English
| MEDLINE | ID: mdl-19418500
14.
Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-n-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory cancer.
J Med Chem
; 51(14): 4239-52, 2008 Jul 24.
Article
in English
| MEDLINE | ID: mdl-18578472
15.
Kinesin spindle protein (KSP) inhibitors. Part V: discovery of 2-propylamino-2,4-diaryl-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by beta-fluorination to overcome cellular efflux by P-glycoprotein.
Bioorg Med Chem Lett
; 17(10): 2697-702, 2007 May 15.
Article
in English
| MEDLINE | ID: mdl-17395460
16.
Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP.
Bioorg Med Chem Lett
; 16(12): 3175-9, 2006 Jun 15.
Article
in English
| MEDLINE | ID: mdl-16603356
17.
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP.
Bioorg Med Chem Lett
; 15(8): 2041-5, 2005 Apr 15.
Article
in English
| MEDLINE | ID: mdl-15808464
18.
Non-peptide alpha v beta 3 antagonists. Part 7: 3-Substituted tetrahydro-naphthyridine derivatives.
Bioorg Med Chem Lett
; 14(4): 1049-52, 2004 Feb 23.
Article
in English
| MEDLINE | ID: mdl-15013021
19.
Non-peptide alphavbeta3 antagonists. Part 6: design and synthesis of alphavbeta3 antagonists containing a pyridone or pyrazinone central scaffold.
Bioorg Med Chem Lett
; 13(10): 1809-12, 2003 May 19.
Article
in English
| MEDLINE | ID: mdl-12729670
20.
Nonpeptide alpha V beta 3 antagonists. Part 10: In vitro and in vivo evaluation of a potent 7-methyl substituted tetrahydro-[1,8]naphthyridine derivative.
Bioorg Med Chem Lett
; 14(17): 4515-8, 2004 Sep 06.
Article
in English
| MEDLINE | ID: mdl-15357983