Research Topics
| Hong C ShenSummaryAffiliation: Merck Research Laboratories Country: USA Publications
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Detail Information
Publications
On the diastereoselectivity of ru-catalyzed [5 + 2] cycloadditionsBarry M Trost
Department of Chemistry, Stanford University, Stanford, California 94305 5080, USA
Org Lett 5:4149-51. 2003..reaction: see text]. Ru-catalyzed cycloisomerization of cyclopropylenynes proceeds with good to high diastereoselectivities to form hexahydroazulenes...
Novel patent publications on high-affinity nicotinic acid receptor agonistsHong C Shen
Department of Medicinal Chemistry, Merck Research Laboratories, Merck and Co Inc, 126 East Lincoln Avenue, Rahway, NJ 07065 0900, USA
Expert Opin Ther Pat 19:957-67. 2009....- Discovery of spirocyclic secondary amine-derived tertiary ureas as highly potent, selective and bioavailable soluble epoxide hydrolase inhibitorsHong C Shen
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065 0900, USA
Bioorg Med Chem Lett 19:3398-404. 2009..This study posed the question as to whether sEH inhibition provides a robust mechanism leading to a significant antihypertensive effect... - Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in ratsHong C Shen
Departments of Medicinal Chemistry, Merck Research Laboratories, Merck and Co, Inc, Rahway, New Jersey 07065 0900, USA
J Med Chem 52:2587-602. 2009.... - Acyl hydroxypyrazoles as novel agonists for high-affinity nicotinic acid receptor GPR109A: WO2008051403Hong C Shen
Research Fellow Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065 0900, USA
Expert Opin Ther Pat 19:1149-55. 2009..The fused bicyclic core contains a hydroxypyrazole that mimics the anthranilide moiety described in their earlier patents and patent publications... - Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagementHong C Shen
Merck Research Laboratories, Merck and Co, Inc, Rahway, NJ 07065 0900, USA
J Med Chem 52:5009-12. 2009..With minimal off-target activity and a good PK profile, the benchmark 2d exhibited remarkable in vitro and ex vivo target engagement. The eutomer entA-2d also elicited vasodilation effect in rat mesenteric artery... - Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109AHong C Shen
Department of Medicinal Chemistry, Merck Research Laboratories, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065 0900, USA
Bioorg Med Chem Lett 18:4948-51. 2008..In addition to its intrinsic activity, compound 9n significantly enhances nicotinic acid binding to the receptor, thereby potentiating the functional efficacy of nicotinic acid... - Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109AHong C Shen
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065 0900, USA
Bioorg Med Chem Lett 17:6723-8. 2007..Compound 1a displayed good PK, better in vivo efficacy in reducing FFA in mouse than niacin, and no vasodilation in a mouse model. Compound 1q demonstrated equal affinity to GPR109A as niacin... - Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptorHong C Shen
Merck Research Laboratories, Merck and Co, Inc, Rahway, New Jersey 07065 0900, USA
J Med Chem 50:6303-6. 2007..Compound 2i exhibited good in vivo antilipolytic efficacy while providing a significantly improved therapeutic index over vasodilation (flushing) with respect to niacin in the mouse model... - Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitorsHong C Shen
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065 0900, USA
Bioorg Med Chem Lett 19:5314-20. 2009..This observation further challenges the premise that sEH inhibition can provide a viable approach to the treatment of hypertensive patients... - Alpha-heteroarylation of esters, lactones, amides, and lactams by nucleophilic aromatic substitutionHong C Shen
Department of Medicinal Chemistry, Merck Research Laboratories, Merck and Company, Inc, P O Box 2000, Rahway, New Jersey 07065 0900, USA
Org Lett 8:1447-50. 2006..The choice of NaHMDS in toluene gave the best results. A tandem alpha-heteroarylation and hydroxylation protocol using air as the oxidant afforded tertiary alcohols in good yields... - A strategy of employing aminoheterocycles as amide mimics to identify novel, potent and bioavailable soluble epoxide hydrolase inhibitorsHong C Shen
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065 0900, USA
Bioorg Med Chem Lett 19:5716-21. 2009..The strategy of employing aminoheterocycles as amide replacements may represent a general approach to develop mimics of known hydrolase or protease inhibitors containing an amide moiety... - Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidateHong C Shen
Department of Medicinal Chemistry, Merck Research Laboratories, Merck and Co, Inc, Rahway, New Jersey 07065 0900, USA mail
J Med Chem 53:2666-70. 2010.... - Soluble epoxide hydrolase inhibitors: a patent reviewHong C Shen
Merck and Co, Inc, Merck Research Laboratories, Department of Medicinal Chemistry RY800 C114, 126 East Lincoln Avenue, PO Box 2000, Rahway, NJ 07065 0900, USA
Expert Opin Ther Pat 20:941-56. 2010..It has been claimed that sEH inhibitors can be used to treat hypertension, diabetes, stroke, dyslipidemia, pain, immunological disorders, eye diseases, neurological diseases and other indications... - Discovery of benzimidazole pyrrolidinyl amides as prolylcarboxypeptidase inhibitorsHong C Shen
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065 0900, USA
Bioorg Med Chem Lett 21:1299-305. 2011..Compound 9b was also studied in vivo for its effect on weight loss and food intake in an eDIO mouse model and the results will be discussed... - Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109AFa Xiang Ding
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065 0900, USA
Bioorg Med Chem Lett 20:3372-5. 2010..The structure-activity relationship (SAR) studies were aimed to improve activity on GPR109A, reduce Cytochrome P450 2C8 (CYP2C8) and Cytochrome P450 2C9 (CYP2C9) inhibition, reduce serum shift and improve pharmacokinetic (PK) profiles... - Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of potent niacin receptor agonistsSubharekha Raghavan
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 18:3163-7. 2008..Several compounds were identified that were potent against the niacin receptor, had enhanced cytochrome P450 selectivity against subtypes CYP2C8 and CYP2C9, and improved oral exposure in mice... - Discovery of benzodihydroisofurans as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase inhibitorsHong C Shen
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065 0900, USA
Bioorg Med Chem Lett 22:1550-6. 2012..In the established diet-induced obese (eDIO) mouse model, compound ent-3a displayed target engagement both in plasma and in brain. However, this compound failed to induce significant body weight loss in eDIO mice in a five-day study... - The discovery of non-benzimidazole and brain-penetrant prolylcarboxypeptidase inhibitorsThomas H Graham
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065 0900, USA
Bioorg Med Chem Lett 22:658-65. 2012..The compounds were also cell permeable and demonstrated in vivo brain exposure. The in vivo effect of compound (S)-6e on weight loss in an established diet-induced obesity (eDIO) mouse model was studied... - Synthesis and biological evaluation of platensimycin analogsHong C Shen
Departments of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065 0900, USA
Bioorg Med Chem Lett 19:1623-7. 2009..The medicinal chemistry efforts were focused on the modification of the enone moiety of platensimycin and several analogs showed significant activity against FabF and possess antibacterial activity... - Palladium-catalyzed Suzuki-Miyaura coupling of pyridyl-2-boronic esters with aryl halides using highly active and air-stable phosphine chloride and oxide ligandsDavid X Yang
Department of Medicinal Chemistry, Merck Research Laboratories, Merck and Co, Inc, P O Box 2000, Rahway, New Jersey 07065 0900, USA
Org Lett 11:381-4. 2009..The convenient reaction protocol demonstrates its potentially wide applications in medicinal chemistry... - Gold(I)-catalyzed regioselective cyclizations of silyl ketene amides and carbamates with alkynesEllen C Minnihan
Department of Medicinal Chemistry, Merck Research Laboratories, Merck and Co Inc, P O Box 2000, Rahway, NJ 07065, USA
J Org Chem 72:6287-9. 2007..The gold(I)-catalyzed regioselective cyclizations of silyl ketene amides or carbamates with alkynes were utilized to construct cyclopentanes or dehydro-delta-lactams... - A formal [3 + 3] cycloaddition reaction. Improved reactivity using alpha,beta-unsaturated iminium salts and evidence for reversibility of 6pi-electron electrocyclic ring closure of 1-oxatrienesHong C Shen
Department of Chemistry, University of Minnesota, Minneapolis, Minnesota 55455, USA
J Org Chem 68:1729-35. 2003..Most significantly, experimental evidence is provided to support the mechanism of this reaction that involves a sequential Knoevenagel condensation and a reversible 6pi-electron electrocyclic ring-closure of 1-oxatrienes... - An enantioselective biomimetic total synthesis of (-)-siccaninBarry M Trost
Department of Chemistry, Stanford University, Stanford, CA 94305-5080, USA
Angew Chem Int Ed Engl 42:3943-7. 2003 - Synthesis of chiral chromans by the Pd-catalyzed asymmetric allylic alkylation (AAA): scope, mechanism, and applicationsBarry M Trost
Department of Chemistry, Stanford University, Stanford, California 94305 5080, USA
J Am Chem Soc 126:11966-83. 2004.... - Biomimetic enantioselective total synthesis of (-)-siccanin via the Pd-catalyzed asymmetric allylic alkylation (AAA) and sequential radical cyclizationsBarry M Trost
Department of Chemistry, Stanford University, Stanford, California 94305 5080, USA
J Am Chem Soc 126:12565-79. 2004..These studies may shed light on the biosynthesis of this novel family of compounds... - Syntheses of seven-membered rings: ruthenium-catalyzed intramolecular [5+2] cycloadditionsBarry M Trost
Department of Chemistry, Stanford University, Stanford, CA 94305 5080, USA
Chemistry 11:2577-90. 2005..The potential power of this methodology towards natural product total synthesis is demonstrated by the formation of several polycyclic systems with the chosen reaction conditions and readily available cyclopropylenyne substrates... - A synthesis of trisubstituted alkenes by a Ru-catalyzed additionBarry M Trost
Department of Chemistry, Stanford University Stanford, CA 94305 5080, USA
Chemistry 8:2341-9. 2002..The first C-C bond formation generally involves sterically less hindered carbons of the alkenes and alkynes. Modest to very high regioselectivity can be achieved depending on the steric difference of the two substituents of alkynes...