Zobrazeno 1 - 10
of 70
pro vyhledávání: '"Lisa D, Aimone"'
Autor:
Bruce A. Ruggeri, Giorgio Inghirami, Bruce D. Dorsey, Mark A. Ator, Cristina Abele, Rodolfo Machiorlatti, Flavio Cristofani, Lisa D. Aimone, Thelma S. Angeles, Mark S. Albom, Weihua Wan, Lihui Lu, Gregory R. Ott, Diane E. Gingrich, Matthew R. Quail, Mangeng Cheng
PDF file - 102K
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b6a0a50e0c286d90b24603959f90aa4c
https://doi.org/10.1158/1535-7163.22498291
https://doi.org/10.1158/1535-7163.22498291
Autor:
Bruce A. Ruggeri, Giorgio Inghirami, Bruce D. Dorsey, Mark A. Ator, Cristina Abele, Rodolfo Machiorlatti, Flavio Cristofani, Lisa D. Aimone, Thelma S. Angeles, Mark S. Albom, Weihua Wan, Lihui Lu, Gregory R. Ott, Diane E. Gingrich, Matthew R. Quail, Mangeng Cheng
PDF file - 300K
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::36ff3acce277a3f9ee6d65f11bbc8c38
https://doi.org/10.1158/1535-7163.22498288
https://doi.org/10.1158/1535-7163.22498288
Autor:
Robert L. Hudkins, Joanne R. Mathiasen, Rita Raddatz, Edward R. Bacon, Michael J. Marino, Mark A. Ator, Michael Williams, Lisa D. Aimone, John A. Gruner
Publikováno v:
Neuropharmacology. 106:37-45
CEP-32215 is a new, potent, selective, and orally bioavailable inverse agonist of the histamine H3 receptor (H3R) with drug-like properties. High affinity in human (hH3R Ki = 2.0 ± 0.2 nM) and rat (rH3R Ki = 3.6 ± 0.7 nM) H3R radioligand binding as
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c71b30bf6225f22a176e0653fc340cbc
https://doi.org/10.1016/j.neuropharm.2015.09.025
https://doi.org/10.1016/j.neuropharm.2015.09.025
Autor:
Nadine C. Becknell, Joanne R. Mathiasen, Jacquelyn A. Lyons, John A. Gruner, Robert L. Hudkins, Mark A. Olsen, Lisa D. Aimone, Rita Raddatz, R. Curtis Haltiwanger
Publikováno v:
European Journal of Medicinal Chemistry. 95:349-356
A novel series of 3,4-diaza-bicyclo[4.1.0]hept-4-en-2-ones were designed and synthesized as H3R analogs of irdabisant 6. Separation of the isomers, assignment of the stereochemistry by crystallography, and detailed profiling of diastereomers 25 and 2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::006fe633aee98b8159cefa48d14ea763
https://doi.org/10.1016/j.ejmech.2015.03.054
https://doi.org/10.1016/j.ejmech.2015.03.054
Autor:
R. Curtis Haltiwanger, Mark A. Olsen, Mark A. Ator, Emily Kordwitz, Gregory R. Ott, Jason C. Wagner, Bruce D. Dorsey, Zeqi Huang, Mangeng Cheng, Bruce Ruggeri, Eugen F. Mesaros, Weihua Wan, Lihui Lu, Amy J. Landis, Lisa D. Aimone, Mark S. Albom, Thelma S. Angeles
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:1047-1052
The diastereoselective synthesis and biological activity of piperidine-3,4-diol and piperidine-3-ol-derived pyrrolotriazine inhibitors of anaplastic lymphoma kinase (ALK) are described. Although piperidine-3,4-diol and piperidine-3-ol derivatives sho
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0411c50feeaebea97c165e9936080b0e
https://doi.org/10.1016/j.bmcl.2015.01.019
https://doi.org/10.1016/j.bmcl.2015.01.019
Autor:
Sankar Chatterjee, John A. Gruner, Yin G. Lin, Brigitte Lesur, Lisa D. Aimone, Edward R. Bacon, Val R. Marcy
Publikováno v:
Chemical Biology & Drug Design. 81:429-432
In search of a next generation molecule to the novel wake-promoting agent modafinil, a series of aryl-heteroayl-derived wakefulness enhancing agents (in rats) was developed. From this work, compound 16 was separated into its enantiomers to profile th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::53ba61430a469e50038848c3a564a471
https://doi.org/10.1111/cbdd.12083
https://doi.org/10.1111/cbdd.12083
Autor:
Nathan Anderson, Diane E. Gingrich, Arup K. Ghose, Mark S. Albom, Bruce D. Dorsey, Lisa D. Aimone, Elizabeth Bruckheimer, Jason C. Wagner, Matthew A. Curry, Lihui Lu, Jay Friedman, Mark A. Ator, Bruce Ruggeri, Eugen F. Mesaros, Mangeng Cheng, Zeqi Huang, Keith S. Learn, Matthew R. Quail, Thelma S. Angeles, Pawel Dobrzanski, Gregory R. Ott, Sandra V. Fernandez, Joseph G. Lisko, Kevin J. Wells-Knecht, Weihua Wan
Publikováno v:
Journal of medicinal chemistry. 59(16)
Analogues structurally related to anaplastic lymphoma kinase (ALK) inhibitor 1 were optimized for metabolic stability. The results from this endeavor not only led to improved metabolic stability, pharmacokinetic parameters, and in vitro activity agai
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f38d2d8693c2496a71a1241c7558ff6
https://pubmed.ncbi.nlm.nih.gov/27527804
https://pubmed.ncbi.nlm.nih.gov/27527804
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4198-4202
A novel class of benzocinnolinones analogs of irdabisant were designed and synthesized as histamine H3R antagonists/inverse agonists. Modifications to the pyridazinone portion of the core and linker led to the identification of molecules with excelle
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eed73c701c4242cf974b56c9a4fb9596
https://doi.org/10.1016/j.bmcl.2012.04.001
https://doi.org/10.1016/j.bmcl.2012.04.001
Autor:
Robert L. Hudkins, Allison L. Zulli, Rita Raddatz, Lisa D. Aimone, John A. Gruner, Edward R. Bacon, Joanne R. Mathiasen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:2807-2810
Optimization of a series of aminomethyl ketone diamine H3R antagonists to reduce the brain exposure by lowering the pKa, led to molecules with improved pharmacokinetic properties. Compounds 9, 19, and 25 had high affinity for human H3R and demonstrat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec06339451ae51dea3f5d2188b93b94e
https://doi.org/10.1016/j.bmcl.2012.02.081
https://doi.org/10.1016/j.bmcl.2012.02.081
Autor:
Thomas J. Connors, Jie Qian, Zeck Huang, Joanne R. Mathiasen, Edward R. Bacon, Thelma S. Angeles, Mark J. Huffman, Emir Duzic, Joseph M. Salvino, Beth Ann McKenna, Hervé Schaffhauser, Robert J. McHugh, Lily D. Lu, George C. Morton, Beverly P. Holskin, Karla Kopec, Amy DiCamillo, Gerard C. Rosse, Chrysanthe Spais, Rabindranath Tripathy, Lisa D. Aimone
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1421-1426
Serotoninergic neurotransmission has been implicated in modulation of learning and memory. It has been demonstrated that 5-hydroxytryptamine(6) (5-HT(6)) receptor antagonists show beneficial effect on cognition in several animal models. Based on a ph
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::33e912dffb6b9ff1c34528c45a1f47ab
https://doi.org/10.1016/j.bmcl.2011.12.026
https://doi.org/10.1016/j.bmcl.2011.12.026