André Erdling - Research Outputs - Lund University

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Institutionen för kliniska vetenskaper, Lund - Forskningsoutput

The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. 2021-04-03 Telcagepant (MK-0974) displays affinity (K i) for the canine and rat receptors, with values of 1204 nM and 1192 nM (n=10), respectively.Telcagepant (MK-0974) potently blocks human α-CGRP-stimulated cAMP responses in human CGRP receptor expressing HEK293 cells with an IC 50 of 2.2 nM.Telcagepant (MK-0974) displays saturable binding to SK-N-MC membranes with a K D of 1.9 nM and B max of 479 TELCAGEPANT DrugBank Drug Name 781649-09-0 CAS Number CHEMBL236593 ChEMBL ID Drug Info: Drug Type small molecule Drug Groups investigational Publications: Chan KY et al., 2010, Characterization of the calcitonin gene-related peptide receptor antagonist telcagepant (MK-0974) in human isolated coronary arteries., J Pharmacol Exp Ther Identification Name Telcagepant Accession Number DB12228 Description. Telcagepant has been investigated for the treatment of Migraine. It is an antagonist of the receptor for calcitonin gene-related peptide (CGRP), a primary neuropeptide involved in the pathophysiology of migraine.

Telcagepant synthesis

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On His Wings Travels knows how. Request a free consultation now Figure 9: The total synthesis of telcagepant by Merck. - "Domino and one-pot syntheses of biologically active compounds using diphenylprolinol silyl ether" Weitere E-Angebote Science of Synthesis Pharmaceutical Substances Two novel routes have been developed to the (3 R,6 S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one 2 of the CGRP receptor antagonist clinical candidate telcagepant (MK-0974, 1). The first employs a ring-closing metathesis of the styrene 7 as the key reaction, while the second makes use of a highly diastereoselective Hayashi-Miyaura Rh-catalyzed arylboronic acid addition Thieme E-Books & E-Journals. Full-text search Full-text search; Author Search; Title Search; DOI Search Thieme E-Books & E-Journals.

André Erdling - Research Outputs - Lund University

Telcagepant has been investigated for the treatment of Migraine. It is an antagonist of the receptor for calcitonin gene-related peptide (CGRP), a primary neuropeptide involved in the pathophysiology of migraine. Chemvon Biotechnology Co. Ltd. is supplier for Telcagepant.

Institutionen för kliniska vetenskaper, Lund - Forskningsoutput

Chemvon Biotechnology Co. Ltd. is supplier for Telcagepant.

of Merck Rahway disclose their efforts towards an improved multikilogram synthesis of telcagepant, a CGRP receptor antagonist for the treatment of migraines (J. Org. Chem.
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Full-text search Full-text search; Author Search; Title Search; DOI Search Thieme E-Books & E-Journals. Jahre (Archiv) 2010 Isolating only three intermediates, the overall yield of this cost-effective synthesis was up to 27%. This environmentally responsible synthesis contains all of the elements required for a manufacturing process and prepares telcagepant (1) with the high quality required for pharmaceutical use.

The key to the success of this organocatalytic transformation was the … Disclosed is an efficient synthesis for the manufacture of the caprolactam intermediate (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one: Formula and salts thereof, and an efficient preparation of telcagepant using the caprolactam intermediate.
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André Erdling - Research Outputs - Lund University

- Mechanism of Action & Protocol. Telcagepant Accession Number DB12228 Description. Telcagepant has been investigated for the treatment of Migraine. It is an antagonist of the receptor for calcitonin gene-related peptide (CGRP), a primary neuropeptide involved in the pathophysiology of migraine.