Distinct mechanism for antidepressant activity by blockade of central substance P receptors
…, G Liu, D Snavely, E Wyatt-Knowles, JJ Hale… - Science, 1998 - science.org
The localization of substance P in brain regions that coordinate stress responses and receive
convergent monoaminergic innervation suggested that substance P antagonists might …
convergent monoaminergic innervation suggested that substance P antagonists might …
Structural Optimization Affording 2-(R)-(1-(R)-3,5-Bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a Potent …
JJ Hale, SG Mills, M MacCoss, PE Finke… - Journal of medicinal …, 1998 - ACS Publications
Structural modifications requiring novel synthetic chemistry were made to the morpholine
acetal human neurokinin-1 (hNK-1) receptor antagonist 4, and this resulted in the discovery of 2…
acetal human neurokinin-1 (hNK-1) receptor antagonist 4, and this resulted in the discovery of 2…
Potent 1, 3, 4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties
D Kim, L Wang, JJ Hale, CL Lynch, RJ Budhu… - Bioorganic & medicinal …, 2005 - Elsevier
A series of 1, 3, 4-trisubstituted pyrrolidine CCR5 receptor antagonists containing a variety of
fused heterocycles at the 4-position of the piperidine side chain has been discovered, which …
fused heterocycles at the 4-position of the piperidine side chain has been discovered, which …
Discovery of Potent 3,5-Diphenyl-1,2,4-oxadiazole Sphingosine-1-phosphate-1 (S1P1) Receptor Agonists with Exceptional Selectivity against S1P2 and S1P3
Z Li, W Chen, JJ Hale, CL Lynch, SG Mills… - Journal of medicinal …, 2005 - ACS Publications
A class of 3,5-diphenyl-1,2,4-oxadiazole based compounds have been identified as potent
sphingosine-1-phosphate-1 (S1P 1 ) receptor agonists with minimal affinity for the S1P 2 and …
sphingosine-1-phosphate-1 (S1P 1 ) receptor agonists with minimal affinity for the S1P 2 and …
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists
JJ Hale, CL Lynch, W Neway, SG Mills… - Journal of medicinal …, 2004 - ACS Publications
Moderately potent, selective S1P 1 receptor agonists identified from high-throughput
screening have been adapted into lipophilic tails for a class of orally bioavailable amino acid-based …
screening have been adapted into lipophilic tails for a class of orally bioavailable amino acid-based …
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs
JJ Hale, SG Mills, M MacCoss, CP Dorn… - Journal of medicinal …, 2000 - ACS Publications
The regioselective dibenzylphosphorylation of 2 followed by catalytic reduction in the
presence of N-methyl-d-glucamine afforded 2-(S)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(…
presence of N-methyl-d-glucamine afforded 2-(S)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(…
Prolyl hydroxylase domain-containing protein inhibitors as stabilizers of hypoxia-inducible factor: small molecule-based therapeutics for anemia
L Yan, VJ Colandrea, JJ Hale - Expert opinion on therapeutic …, 2010 - Taylor & Francis
Importance of the field: Anemia caused by chronic kidney disease and other chronic
diseases or conditions can be managed by the treatment of biologic-based erythropoiesis …
diseases or conditions can be managed by the treatment of biologic-based erythropoiesis …
1, 3, 8-Triazaspiro [4.5] decane-2, 4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1–3 (HIF PHD1–3) for the treatment of anemia
The discovery of 1,3,8-triazaspiro[4.5]decane-2,4-diones (spirohydantoins) as a structural
class of pan-inhibitors of the prolyl hydroxylase (PHD) family of enzymes for the treatment of …
class of pan-inhibitors of the prolyl hydroxylase (PHD) family of enzymes for the treatment of …
Synthesis and study of alendronate derivatives as potential prodrugs of alendronate sodium for the treatment of low bone density and osteoporosis
P Vachal, JJ Hale, Z Lu, EC Streckfuss… - Journal of medicinal …, 2006 - ACS Publications
Alendronate derivatives were evaluated as potential prodrugs for the osteoporosis drug
alendronate sodium in an attempt to enhance the systemic exposure after oral administration. An …
alendronate sodium in an attempt to enhance the systemic exposure after oral administration. An …
Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720
JJ Hale, W Neway, SG Mills, R Hajdu… - Bioorganic & medicinal …, 2004 - Elsevier
Alteration in lymphocyte trafficking and prevention of graft rejection in rodents observed on
exposure to FTY720 (1) or its corresponding phosphate ester 2 can be induced by the …
exposure to FTY720 (1) or its corresponding phosphate ester 2 can be induced by the …