Phosphorylated Morpholine Acetal Human Neurokinin-1 Receptor Antagonists as Water-Soluble Prodrugs

The regioselective dibenzylphosphorylation of 2 followed by catalytic reduction in the presence of N-methyl-d-glucamine afforded 2-(S)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(5-(2-phosphoryl-3-oxo-4H,-1,2,4-triazolo)methylmorpholine, bis(N-methyl-d-glucamine) salt, 1...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Journal of medicinal chemistry 2000-03, Vol.43 (6), p.1234-1241
Hauptverfasser:	Hale, Jeffrey J, Mills, Sander G, MacCoss, Malcolm, Dorn, Conrad P, Finke, Paul E, Budhu, Richard J, Reamer, Robert A, Huskey, Su-Er W, Luffer-Atlas, Debra, Dean, Brian J, McGowan, Erin M, Feeney, William P, Chiu, Shuet-Hing Lee, Cascieri, Margaret A, Chicchi, Gary G, Kurtz, Marc M, Sadowski, Sharon, Ber, Elzbieta, Tattersall, F. David, Rupniak, Nadia M. J, Williams, Angela R, Rycroft, Wayne, Hargreaves, Richard, Metzger, Joseph M, MacIntyre, D. Euan
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetals - chemical synthesis Acetals - chemistry Acetals - metabolism Acetals - pharmacology Animals Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis Anti-Inflammatory Agents, Non-Steroidal - chemistry Anti-Inflammatory Agents, Non-Steroidal - metabolism Anti-Inflammatory Agents, Non-Steroidal - pharmacology Antiemetics - chemical synthesis Antiemetics - chemistry Antiemetics - metabolism Antiemetics - pharmacology Antineoplastic Agents Aprepitant Biological and medical sciences Cisplatin Dogs Drug Evaluation, Preclinical Ferrets Guinea Pigs Humans Medical sciences Morpholines - chemical synthesis Morpholines - chemistry Morpholines - metabolism Morpholines - pharmacology Neurokinin-1 Receptor Antagonists Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Prodrugs - chemical synthesis Prodrugs - chemistry Prodrugs - metabolism Prodrugs - pharmacology Rats Solubility Stereoisomerism Structure-Activity Relationship Vomiting - chemically induced Vomiting - drug therapy Water
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Schreiben Sie den ersten Kommentar!