Functionalized Polymers-Emerging Versatile Tools for Solution-Phase Chemistry and Automated Parallel Synthesis von Kirschning, Andreas, Monenschein, Holger, Wittenberg, Rüdiger

Volltext

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 o... von 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

Volltext

Total Synthesis of Apoptolidin:  Construction of Enantiomerically Pure Fragments von Nicolaou, K. C, Fylaktakidou, Konstantina C, Monenschein, Holger, Li, Yiwei, Weyershausen, Bernd, Mitchell, Helen J, Wei, Heng-xu, Guntupalli, Prasuna, Hepworth, David, Sugita, Kazuyuki

Volltext

2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics von Zeng, Qingping, Bourbeau, Matthew P., Wohlhieter, G. Erich, Yao, Guomin, Monenschein, Holger, Rider, James T., Lee, Matthew R., Zhang, Shiwen, Lofgren, Julie, Freeman, Daniel, Li, Chun, Tominey, Elizabeth, Huang, Xin, Hoffman, Douglas, Yamane, Harvey, Tasker, Andrew S., Dominguez, Celia, Viswanadhan, Vellarkad N., Hungate, Randall, Zhang, Xiaoling

Volltext

S39. GPR139 AN OPHAN GPCR AFFECTING NEGATIVE DOMAINS OF SCHIZOPHRENIA von Atienza, Joy, Reichard, Holly, Mulligan, Victoria, Cilia, Jackie, Monenschein, Holger, Collia, Deanna, Ray, Jim, Kilpatrick, Gavin, Brice, Nicola, Carlton, Mark, Hitchcock, Steve, Corbett, Ged

Volltext

Application of polymer-supported electrophilic reagents for the 1,2-functionalization of glycals von Kirschning, Andreas, Jesberger, Martin, Monenschein, Holger

Volltext

Identification of CVN058, a Novel Brain Penetrant, Selective 5-HT3 Receptor Antagonist That Shows Efficacy in Pre-Clinical Cognition Models von Brice, Nicola, Dawson, Lee A., Margolin, David H., Schiffer, Hans H., Monenschein, Holger, Ray, William J., Hitchcock, Stephen, Carlton, Mark

Volltext

Asymmetric Nucleophilic Acylation of Aldehydes via 1,1-Heterodisubstituted Alkenes von Monenschein, Holger, Dräger, Gerald, Jung, Alexander, Kirschning, Andreas

Volltext

Synthesis and conformational analysis of α,α-difluoroalkyl heteroaryl ethers von Horne, Daniel B., Bartberger, Michael D., Kaller, Matthew R., Monenschein, Holger, Zhong, Wenge, Hitchcock, Stephen A.

Volltext

First-Time Disclosure of CVN424, a Potent and Selective GPR6 Inverse Agonist for the Treatment of Parkinson’s Disease: Discovery, Pharmacological Validation, and Identification of... von Sun, Huikai, Monenschein, Holger, Schiffer, Hans H, Reichard, Holly A, Kikuchi, Shota, Hopkins, Maria, Macklin, Todd K, Hitchcock, Stephen, Adams, Mark, Green, Jason, Brown, Jason, Murphy, Sean T, Kaushal, Nidhi, Collia, Deanna R, Moore, Steve, Ray, William J, English, Nicole Marion, Carlton, Mark Beresford Lewis, Brice, Nicola L

Volltext

S180. THE SELECTIVE GPR139 AGONIST TAK-041 REVERSES ANHEDONIA AND SOCIAL INTERACTION DEFICITS IN RODENT MODELS RELATED TO NEGATIVE SYMPTOMS IN SCHIZOPHRENIA von Schiffer, Hans, Atienza, Josephine, Reichard, Holly, Mulligan, Victoria, Cilia, Jackie, Monenschein, Holger, Collia, Deanna, Ray, Jim, Kilpatrick, Gavin, Brice, Nicola, Carlton, Mark, Hitchcock, Steve, Corbett, Ged, Hodgson, Robert

Volltext

Discovery of TAK-041: a Potent and Selective GPR139 Agonist Explored for the Treatment of Negative Symptoms Associated with Schizophrenia von Reichard, Holly A, Schiffer, Hans H, Monenschein, Holger, Atienza, Josephine M, Corbett, Gerard, Skaggs, Alton W, Collia, Deanna R, Ray, William J, Serrats, Jordi, Bliesath, Joshua, Kaushal, Nidhi, Lam, Betty P, Amador-Arjona, Alejandro, Rahbaek, Lisa, McConn, Donavon J, Mulligan, Victoria J, Brice, Nicola, Gaskin, Philip L. R, Cilia, Jackie, Hitchcock, Stephen

Volltext

Structural insights into the high basal activity and inverse agonism of the orphan receptor GPR6 implicated in Parkinson's disease von Barekatain, Mahta, Johansson, Linda C, Lam, Jordy H, Chang, Hao, Sadybekov, Anastasiia V, Han, Gye Won, Russo, Joseph, Bliesath, Joshua, Brice, Nicola L, Carlton, Mark B L, Saikatendu, Kumar S, Sun, Hukai, Murphy, Sean T, Monenschein, Holger, Schiffer, Hans H, Popov, Petr, Lutomski, Corinne A, Robinson, Carol V, Liu, Zhi-Jie, Hua, Tian, Katritch, Vsevolod, Cherezov, Vadim

Volltext

Development of CVN424: A Selective and Novel GPR6 Inverse Agonist Effective in Models of Parkinson Disease von Brice, Nicola L., Schiffer, Hans H., Monenschein, Holger, Mulligan, Victoria J., Page, Keith, Powell, Justin, Xu, Xiao, Cheung, Toni, Burley, J. Russell, Sun, Huikai, Dickson, Louise, Murphy, Sean T., Kaushal, Nidhi, Sheardown, Steve, Lawrence, Jason, Chen, Yun, Bartkowski, Darian, Kanta, Anne, Russo, Joseph, Hosea, Natalie, Dawson, Lee A., Hitchcock, Stephen H., Carlton, Mark B.

Volltext

Lithiated Dimethoxymethyl Diphenyl Phosphine Oxide, A Versatile Formiate Carbanion Equivalent von Monenschein, Holger, Brünjes, Marco, Kirschning, Andreas

Volltext

Structure guided P1a2 modifications of HEA derived beta -secretase inhibitors for the treatment of Alzheimer's disease von Monenschein, Holger, Horne, Daniel B, Bartberger, Michael D, Hitchcock, Stephen A, Nguyen, Thomas T, Patel, Vinod F, Pennington, Lewis D, Zhong, Wenge

Volltext

The "Resin-Capture-Release" Hybrid Technique: A Merger between Solid- and Solution-Phase Synthesis von Kirschning, Andreas, Monenschein, Holger, Wittenberg, Rüdiger

Volltext

Stable Polymer-Bound Iodine Azide von Kirschning, Andreas, Monenschein, Holger, Schmeck, Carsten

Volltext

Design and Preparation of a Potent Series of Hydroxyethylamine Containing β-Secretase Inhibitors That Demonstrate Robust Reduction of Central β-Amyloid von 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

Volltext

Optimization of Potency and Pharmacokinetic Properties of Tetrahydroisoquinoline Transient Receptor Potential Melastatin 8 (TRPM8) Antagonists von 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

Volltext