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Dive into the research topics where Dennis Heyer is active.

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Featured researches published by Dennis Heyer.


Bioorganic & Medicinal Chemistry Letters | 2008

Synthesis of 3-alkyl naphthalenes as novel estrogen receptor ligands

Jing Fang; Adwoa Akwabi-Ameyaw; Jonathan E. GlaxoSmithKline Britton; Subba Reddy Katamreddy; Frank Navas; Aaron B. Miller; Shawn P. Williams; David W. Gray; Lisa A. Orband-Miller; Jean Shearin; Dennis Heyer

A series of estrogen receptor ligands based on a 3-alkyl naphthalene scaffold was synthesized using an intramolecular enolate-alkyne cycloaromatization as the key step. Several of these compounds bearing a C6-OH group were shown to be high affinity ligands. All compounds had similar ERalpha and ERbeta binding affinity ranging from micromolar to low nanomolar.


Neuropeptide Y and Drug Development | 1997

Chapter 7 – Peptide antagonists of neuropeptide Y: Design, structure and pharmacological characterization

Alejandro J. Daniels; Dennis Heyer; Andrew Spaltenstein

Publisher Summary This chapter discusses design, structure, and pharmacological characterization of peptide antagonists of neuropeptide. The structure-affinity pattern found for the pentapeptide series agrees well with reported structural requirements at the N-terminus of neuropeptide Y (NPY). Incorporation of the residues into appropriately substituted pentapeptides is sufficient to allow interaction, with modest affinity, to NPY rat brain Y2 receptors. The improvement in the affinity/activity of the native C-terminal decapeptide of NPY following introduction of the critical Tyr-6 and Leu-8 residues is analyzed. It has been proposed that the C-terminal α-helical domain of NPY provides an additional receptor recognition site and may play a role in receptor-subtype selectivity. The ability of the dimers and their monomeric counterparts to inhibit the NPY-induced increase in cytosolic calcium in HEL cells is examined. The inhibitory potency of the dimers in HEL cells correlates well with their potency in antagonizing the pressor effect of NPY in anesthetized rats. HEL cells may constitute a good model to screen for NPY receptor antagonists as potential antihypertensive agents. It is suggested that the possible reasons commonly proposed for enhanced receptor affinity upon ligand dimerization includes increased local concentration of the ligand at the receptor and co-operative binding to multiple sites on the same receptor.


Journal of Medicinal Chemistry | 2012

Discovery of 6,7-Dihydro-5H-pyrrolo[2,3-a]pyrimidines as Orally Available G Protein-Coupled Receptor 119 Agonists

Subba Reddy Katamreddy; Andrew J. Carpenter; Carina Ammala; Eric E. Boros; Ron L. Brashear; Celia P. Briscoe; Sarah R. Bullard; Richard Dana Caldwell; Christopher R. Conlee; Dallas K. Croom; Shane M. Hart; Dennis Heyer; Paul R. Johnson; Jennifer A. Kashatus; Doug Minick; Gregory Peckham; Sean Ross; Shane Roller; Vicente Samano; Howard Sauls; Sarva M. Tadepalli; James B. Thompson; Yun Xu; James M. Way

GPR119 is a 7-transmembrane receptor that is expressed in the enteroendocrine cells in the intestine and in the islets of Langerhans in the pancreas. Indolines and 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines were discovered as G protein-coupled receptor 119 (GPR119) agonists, and lead optimization efforts led to the identification of 1-methylethyl 4-({7-[2-fluoro-4-(methylsulfonyl)phenyl]-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)-1-piperidinecarboxylate (GSK1104252A) (3), a potent and selective GPR119 agonist. Compound 3 showed excellent pharmacokinetic properties and sufficient selectivity with in vivo studies supporting a role for GPR119 in glucose homeostasis in the rodent. Thus, 3 appeared to modulate the enteroinsular axis, improve glycemic control, and strengthen previous suggestions that GPR119 agonists may have utility in the treatment of type 2 diabetes.


Tetrahedron Letters | 1999

Solid phase synthesis of 1,3,5-trisubstituted pyridin-2-ones

James A. Linn; Samuel W. Gerritz; Anthony L. Handlon; Clifton E. Hyman; Dennis Heyer

Abstract The solid phase synthesis of 1,3,5-trisubsituted pyridin-2-ones is reported via selective 1 NH- alkylation of 3-amino-5-carbomethoxy-1 H -pyridin-2-one with a solid-supported halo-acid. Coupling of an acid to solid-supported 3-aminopyridinone was followed by saponification of the methyl ester to give the acid. Activation of the acid via the pentafluorophenyl ester allowed reaction with an amine, and cleavage from the solid support with TFA:H 2 O (95:5) provided 1,3,5-trisubstituted pyridin-2-ones.


Journal of Medicinal Chemistry | 1995

Novel modified carboxy terminal fragments of neuropeptide Y with high affinity for Y2-type receptors and potent functional antagonism at a Y1-type receptor.

Johann Leban; Dennis Heyer; Antonio Landavazo; Jessica E. Matthews; Ann Aulabaugh; Alejandro J. Daniels


Regulatory Peptides | 2002

Food intake inhibition and reduction in body weight gain in lean and obese rodents treated with GW438014A, a potent and selective NPY-Y5 receptor antagonist.

Alejandro J. Daniels; M.K. Grizzle; R.P. Wiard; Jessica E. Matthews; Dennis Heyer


Archive | 2004

Triphenylethylene compounds as selective estrogen receptor modulators

John F. Eaddy; Dennis Heyer; Amarjit Sab Randhawa; Vicente Samano; John A. Ray; Subba Reddy Katamreddy; Michael Tolar Martin; Michael Scott GlaxoSmithKline Mcclure


Archive | 1997

Pharmacologically active compounds and use

Eric E. Boros; Morton Harfenist; Dennis Heyer; Helen L. White


Archive | 1997

Phenoxathiin derivatives as inhibitors of monoamine oxidase

Morton Harfenist; Helen L. White; Eric E. Boros; Dennis Heyer


Archive | 2009

Indulines derivatives and gpr119 agonists

Dana Caldwell Richard; Dennis Heyer; Vincente Samano; Benjamin Thompson James; Eugene Boros Eric

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Jing Fang

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