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Publikationer i urvalet

13 träffar

Bibliografisk träff 2020-07-08

Structure-Based Drug Discovery of N-((R)-3-(7-Methyl-1H-indazol-5-yl)-1-oxo-1-(((S)-1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2'-oxo-1',2'-dihydrospiro[piperidine-4,4'-pyrido[2,3-d][1,3]oxazine]-1-carboxamide (HTL22562): A Calcitonin Gene-Related Peptide Receptor Antagonist for Acute Treatment of Migraine.

Bucknell SJ, Ator MA, Brown AJH, Brown J, Cansfield AD, Cansfield JE, Christopher JA, Congreve M, Cseke G, Deflorian F, Jones CR, Mason JS, O'Brien MA, Ott GR, Pickworth M, Southall SM.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.0c01003

Bibliografisk träff 2020-02-20

Blocking the CGRP Pathway for Acute and Preventive Treatment of Migraine: The Evolution of Success.

Dubowchik GM, Conway CM, Xin AW.

J Med Chem · review; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.9b01810

Bibliografisk träff 2019-11-04

Applications of fluorine-containing amino acids for drug design.

Mei H, Han J, Klika KD, Izawa K, Sato T, Meanwell NA, Soloshonok VA.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2019.111826

Bibliografisk träff 2014-06-24

Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.

Bell IM.

J Med Chem · review; journal article · DOI 10.1021/jm500364u

Bibliografisk träff 2014-04-18

Serendipitous oxidation product of BIBN4096BS: a potent CGRP receptor antagonist.

Dasgupta B, Kozlowski E, Schroeder DR, Torrente JR, Xu C, Pin S, Conway CM, Dubowchik GM, Macor JE, Vrudhula VM.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2014.04.033

Bibliografisk träff 2013-12-26

Identification of potent CNS-penetrant thiazolidinones as novel CGRP receptor antagonists.

Joshi P, Anderson C, Binch H, Hadida S, Yoo S, Bergeron D, Decker C, terHaar E, Moore J, Garcia-Guzman M, Termin A.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2013.12.089

Bibliografisk träff 2013-04-12

Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migraine through intranasal delivery.

Chaturvedula PV, Mercer SE, Pin SS, Thalody G, Xu C, Conway CM, Keavy D, Signor L, Cantor GH, Mathias N, Moench P, Denton R, Macci R, Schartman R, Whiterock V, Davis C, Macor JE, Dubowchik GM.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2013.04.012

Bibliografisk träff 2012-06-09

Design and synthesis of potent antagonists containing rigid spirocyclic privileged structures for the CGRP receptor.

Chaturvedula PV, Pin S, Tholady G, Conway CM, Macor JE, Dubowchik GM.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2012.05.118

Bibliografisk träff 2012-04-30

MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.

Bell IM, Stump CA, Gallicchio SN, Staas DD, Zartman CB, Moore EL, Sain N, Urban M, Bruno JG, Calamari A, Kemmerer AL, Mosser SD, Fandozzi C, White RB, Zrada MM, Selnick HG, Graham SL, Vacca JP, Kane SA, Salvatore CA.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2012.04.105

Bibliografisk träff 2012-02-27

Discovery of BMS-846372, a Potent and Orally Active Human CGRP Receptor Antagonist for the Treatment of Migraine.

Luo G, Chen L, Conway CM, Denton R, Keavy D, Gulianello M, Huang Y, Kostich W, Lentz KA, Mercer SE, Schartman R, Signor L, Browning M, Macor JE, Dubowchik GM.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/ml300021s

Bibliografisk träff 2011-09-21

Identification of a novel RAMP-independent CGRP receptor antagonist.

Zartman CB, Bell IM, Gallicchio SN, Graham SL, Kane SA, Mallee JJ, Rutledge RZ, Salvatore CA, Vacca JP, Williams TM.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2011.09.056

Bibliografisk träff 2008-04-21

Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.

Obach RS, Lombardo F, Waters NJ.

Drug Metab Dispos · journal article · DOI 10.1124/dmd.108.020479

Bibliografisk träff 2006-03-09

Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead.

Williams TM, Stump CA, Nguyen DN, Quigley AG, Bell IM, Gallicchio SN, Zartman CB, Wan BL, Penna KD, Kunapuli P, Kane SA, Koblan KS, Mosser SD, Rutledge RZ, Salvatore C, Fay JF, Vacca JP, Graham SL.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2006.02.051