Samuel L Graham
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Explore the profile of Samuel L Graham including associated specialties, affiliations and a list of published articles.
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44
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395
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Recent Articles
21.
Burgey C, Paone D, Shaw A, Deng J, Nguyen D, Potteiger C, et al.
Org Lett
. 2008 Jul;
10(15):3235-8.
PMID: 18590336
Two novel routes have been developed to the (3 R,6 S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one 2 of the CGRP receptor antagonist clinical candidate telcagepant (MK-0974, 1). The first employs a ring-closing metathesis of the...
22.
Salvatore C, Hershey J, Corcoran H, Fay J, Johnston V, Moore E, et al.
J Pharmacol Exp Ther
. 2007 Nov;
324(2):416-21.
PMID: 18039958
Calcitonin gene-related peptide (CGRP) is a potent neuropeptide that plays a key role in the pathophysiology of migraine headache. CGRP levels in the cranial circulation are increased during a migraine...
23.
Calcitonin gene-related peptide (CGRP) receptor antagonists: investigations of a pyridinone template
Nguyen D, Paone D, Shaw A, Burgey C, Mosser S, Johnston V, et al.
Bioorg Med Chem Lett
. 2007 Nov;
18(2):755-8.
PMID: 18039571
In our effort to find potent, orally bioavailable CGRP receptor antagonists for the treatment of migraine, a novel series based on a pyridinone template was investigated. After optimizing the privileged...
24.
Paone D, Shaw A, Nguyen D, Burgey C, Deng J, Kane S, et al.
J Med Chem
. 2007 Oct;
50(23):5564-7.
PMID: 17929795
Calcitonin gene-related peptide (CGRP) has been implicated in the pathogenesis of migraine. Herein we describe optimization of CGRP receptor antagonists based on an earlier lead structure containing a (3R)-amino-(6S)-phenylcaprolactam core....
25.
Moore K, Zhu H, Rajapakse H, McGaughey G, Colussi D, Price E, et al.
Bioorg Med Chem Lett
. 2007 Sep;
17(21):5831-5.
PMID: 17827011
This letter describes replacements for the P3 amide moiety present in previously reported tertiary carbinamine macrolactones. Although P-gp efflux issues associated with these amide-macrolactones were solved and full brain penetration...
26.
Shaw A, Paone D, Nguyen D, Stump C, Burgey C, Mosser S, et al.
Bioorg Med Chem Lett
. 2007 Jul;
17(17):4795-8.
PMID: 17616394
Calcitonin gene-related peptide (CGRP) has been implicated in the pathogenesis of migraine. Replacements for the benzodiazepine core of an earlier lead structure 1 including 5-, 6-, and 7-membered lactams were...
27.
Stanton M, Stauffer S, Gregro A, Steinbeiser M, Nantermet P, Sankaranarayanan S, et al.
J Med Chem
. 2007 Jun;
50(15):3431-3.
PMID: 17583334
beta-Secretase inhibition offers an exciting opportunity for therapeutic intervention in the progression of Alzheimer's disease. A series of isonicotinamides derived from traditional aspartyl protease transition state isostere inhibitors has been...
28.
Lindsley S, Moore K, Rajapakse H, Selnick H, Young M, Zhu H, et al.
Bioorg Med Chem Lett
. 2007 May;
17(14):4057-61.
PMID: 17482814
This Letter describes the design and synthesis of tertiary carbinamine macrocyclic inhibitors of the beta-secretase (BACE-1) enzyme. These macrocyclic inhibitors, some of which incorporate novel P2 substituents, display a 2-...
29.
Barrow J, Rittle K, Ngo P, Selnick H, Graham S, Pitzenberger S, et al.
ChemMedChem
. 2007 Apr;
2(7):995-9.
PMID: 17458843
No abstract available.
30.
Stauffer S, Stanton M, Gregro A, Steinbeiser M, Shaffer J, Nantermet P, et al.
Bioorg Med Chem Lett
. 2007 Jan;
17(6):1788-92.
PMID: 17257835
A series of low-molecular weight 2,6-diamino-isonicotinamide BACE-1 inhibitors containing an amine transition-state isostere were synthesized and shown to be highly potent in both enzymatic and cell-based assays. These inhibitors contain...