Search Results - "Horne, Daniel B"

Discovery of TRPM8 Antagonist (S)‑6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine by Horne, Daniel B, Biswas, Kaustav, Brown, James, Bartberger, Michael D, Clarine, Jeffrey, Davis, Carl D, Gore, Vijay K, Harried, Scott, Horner, Michelle, Kaller, Matthew R, Lehto, Sonya G, Liu, Qingyian, Ma, Vu V, Monenschein, Holger, Nguyen, Thomas T, Yuan, Chester C, Youngblood, Beth D, Zhang, Maosheng, Zhong, Wenge, Allen, Jennifer R, Chen, Jian Jeffrey, Gavva, Narender R

“…Transient-receptor-potential melastatin 8 (TRPM8), the predominant mammalian cold-temperature thermosensor, is a nonselective cation channel expressed in a…”
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Total Synthesis of (+)-Frondosin A. Application of the Ru-Catalyzed [5+2] Cycloaddition by Trost, Barry M, Hu, Yimin, Horne, Daniel B

“…The first total synthesis of (+)-frondosin A was accomplished in 19 longest linear and 21 total steps from commercially available materials. The key features…”
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Palladium-Catalyzed DYKAT of Butadiene Monoepoxide: Enantioselective Total Synthesis of (+)-DMDP, (−)-Bulgecinine, and (+)-Broussonetine G by Trost, Barry M., Horne, Daniel B., Woltering, Michael J.

“…Palladium catalyzed asymmetric allylic alkylation reaction of an amine with two equivalents of butadiene monoxide allows for the expedient synthesis of trans‐…”
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Syntheses of Seven-Membered Rings: Ruthenium-Catalyzed Intramolecular [5+2] Cycloadditions by Trost, Barry M., Shen, Hong C., Horne, Daniel B., Toste, F. Dean, Steinmetz, Bernhard G., Koradin, Christopher

“…The Ru‐catalyzed intramolecular [5+2] cycloaddition of cyclopropylenynes is investigated with respect to the regio‐ and diastereoselectivity as well as the…”
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Palladium-Catalyzed DYKAT of Vinyl Epoxides: Enantioselective Total Synthesis and Assignment of the Configuration of (+)-Broussonetine G by Trost, Barry M., Horne, Daniel B., Woltering, Michael J.

“…A potential general approach to potent N‐heterocyclic glycosidase inhibitors is illustrated by the first total synthesis of (+)‐broussonetine G (1). The key…”
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Design and Preparation of a Potent Series of Hydroxyethylamine Containing β-Secretase Inhibitors That Demonstrate Robust Reduction of Central β-Amyloid by Weiss, Matthew M, Williamson, Toni, Babu-Khan, Safura, Bartberger, Michael D, Brown, James, Chen, Kui, Cheng, Yuan, Citron, Martin, Croghan, Michael D, Dineen, Thomas A, Esmay, Joel, Graceffa, Russell F, Harried, Scott S, Hickman, Dean, Hitchcock, Stephen A, Horne, Daniel B, Huang, Hongbing, Imbeah-Ampiah, Ronke, Judd, Ted, Kaller, Matthew R, Kreiman, Charles R, La, Daniel S, Li, Vivian, Lopez, Patricia, Louie, Steven, Monenschein, Holger, Nguyen, Thomas T, Pennington, Lewis D, Rattan, Claire, San Miguel, Tisha, Sickmier, E.Allen, Wahl, Robert C, Wen, Paul H, Wood, Stephen, Xue, Qiufen, Yang, Bryant H, Patel, Vinod F, Zhong, Wenge

“…A series of potent hydroxyethyl amine (HEA) derived inhibitors of β-site APP cleaving enzyme (BACE1) was optimized to address suboptimal pharmacokinetics and…”
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Optimization of Potency and Pharmacokinetic Properties of Tetrahydroisoquinoline Transient Receptor Potential Melastatin 8 (TRPM8) Antagonists by Horne, Daniel B, Tamayo, Nuria A, Bartberger, Michael D, Bo, Yunxin, Clarine, Jeffrey, Davis, Carl D, Gore, Vijay K, Kaller, Matthew R, Lehto, Sonya G, Ma, Vu V, Nishimura, Nobuko, Nguyen, Thomas T, Tang, Phi, Wang, Weiya, Youngblood, Beth D, Zhang, Maosheng, Gavva, Narender R, Monenschein, Holger, Norman, Mark H

“…Transient receptor potential melastatin 8 (TRPM8) is a nonselective cation channel expressed in a subpopulation of sensory neurons in the peripheral nervous…”
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Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility by Rzasa, Robert M., Frohn, Michael J., Andrews, Kristin L., Chmait, Samer, Chen, Ning, Clarine, Jeffrey G., Davis, Carl, Eastwood, Heather A., Horne, Daniel B., Hu, Essa, Jones, Adrie D., Kaller, Matthew R., Kunz, Roxanne K., Miller, Silke, Monenschein, Holger, Nguyen, Thomas, Pickrell, Alexander J., Porter, Amy, Reichelt, Andreas, Zhao, Xiaoning, Treanor, James J.S., Allen, Jennifer R.

“…[Display omitted] We report the discovery of a novel series of 2-(3-alkoxy-1-azetidinyl) quinolines as potent and selective PDE10A inhibitors…”
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Design and Synthesis of Potent, Orally Efficacious Hydroxyethylamine Derived β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE1) Inhibitors by Dineen, Thomas A, Weiss, Matthew M, Williamson, Toni, Acton, Paul, Babu-Khan, Safura, Bartberger, Michael D, Brown, James, Chen, Kui, Cheng, Yuan, Citron, Martin, Croghan, Michael D, Dunn, Robert T, Esmay, Joel, Graceffa, Russell F, Harried, Scott S, Hickman, Dean, Hitchcock, Stephen A, Horne, Daniel B, Huang, Hongbing, Imbeah-Ampiah, Ronke, Judd, Ted, Kaller, Matthew R, Kreiman, Charles R, La, Daniel S, Li, Vivian, Lopez, Patricia, Louie, Steven, Monenschein, Holger, Nguyen, Thomas T, Pennington, Lewis D, San Miguel, Tisha, Sickmier, E. Allen, Vargas, Hugo M, Wahl, Robert C, Wen, Paul H, Whittington, Douglas A, Wood, Stephen, Xue, Qiufen, Yang, Bryant H, Patel, Vinod F, Zhong, Wenge

“…We have previously shown that hydroxyethylamines can be potent inhibitors of the BACE1 enzyme and that the generation of BACE1 inhibitors with CYP 3A4…”
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Structure guided P1′ modifications of HEA derived β-secretase inhibitors for the treatment of Alzheimer’s disease by Monenschein, Holger, Horne, Daniel B., Bartberger, Michael D., Hitchcock, Stephen A., Nguyen, Thomas T., Patel, Vinod F., Pennington, Lewis D., Zhong, Wenge

“…The structure–activity relationship of the P1′ region of hydroxyethylamine inhibitors of β-secretase (BACE-1) is described. The synthesis and SAR of a series…”
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Synthesis and conformational analysis of α,α-difluoroalkyl heteroaryl ethers by Horne, Daniel B., Bartberger, Michael D., Kaller, Matthew R., Monenschein, Holger, Zhong, Wenge, Hitchcock, Stephen A.

“…We report the efficient synthesis of difluoroalkyl aryl ethers from the rearrangement of heteroaryl ketones and aldehydes, mediated by xenon difluoride and…”
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Structure guided P1a2 modifications of HEA derived beta -secretase inhibitors for the treatment of Alzheimer's disease by Monenschein, Holger, Horne, Daniel B, Bartberger, Michael D, Hitchcock, Stephen A, Nguyen, Thomas T, Patel, Vinod F, Pennington, Lewis D, Zhong, Wenge

“…The synthesis and SAR of a series of BACE-1 hydroxyethyl amine inhibitors containing substitutions on a spirocyclobutyl moiety is described. Selectivity…”
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Palladium-Catalyzed DYKAT of Vinyl Epoxides: Enantioselective Total Synthesis and Assignment of the Configuration of (+)-Broussonetine G by Trost, Barry M., Horne, Daniel B., Woltering, Michael J.

“…Der potente N‐heterocyclische Glycosidaseinhibitor (+)‐Broussonetin G (1) wurde erstmals durch Totalsynthese hergestellt. Der Pyrrolidinkern wurde dabei durch…”
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