CGRP receptors antagonist

A major breakthrough in the field was the development of the first highly potent non-peptide CGRP receptor antagonist BIBN-4096BS (Eberlein et al. (Boehringer... 

SmithKIine Beecham is another company with interests in CGRP receptor antagonists and has filed patent applications for two structural classes, the 3,4-dinitrobenzamides (Daines et al., W09809630) and 4-sulfinyl benzanilides (Daines et al., W09856779). 

Daines, R.A., Sham, K.K.C., Tagged, J.J., Kingsbury, W.D., Chan, J., Breen, A., Disa, J., Aiyar, N. Quinine analogs as non-peptide calcitonin gene-related peptide (CGRP) receptor antagonists, Bioorg. Med. Chem. Lett. 1997, 7, 2673-2676. 

Edvinsson, L., Sams, A., Jansen-Olesen, I., Tajti, J., Kane, S.A., Rutledge, R.Z., Koblan, K.S., Hill, R.G., Longmore, J. Characterization of the effects of a non-peptide CGRP receptor antagonist in SK-N-MC cells and isolated human cerebral arteries, Eur. J. Pharmacol. 2001a, 415, 39-44. 

CGRP Receptors Antagonist (Antimigraine Drugs) Enzymatic Preparation of (R)-2-amino-3-(7-methyi-l H-indazoi-5-yi)Propanoic Acid... 

CGRP receptors antagonist enzymatic preparation of (A)-2-amino-3-(7-methyl-1 H-indazol-5-yl)propanoic acid. 

Craig CA., inventor Merck Co, assignee. Bicyclic dihy-droimidazolone CGRP receptor antagonists. W02010033421 A1.2009 Sept 10. 

Merck and Co., Inc., have patented imidazo[4,5-3]pyridines of the general structure 194, which have been found to be antagonists of calcitonin gene-related peptide (CGRP) receptors, which are useful for the treatment of the symptoms for headache, migraine, and cluster headaches <2005W0013894>. Merck have also patented the... 

In 1997 scientists from SmithKIine Beecham published a series of quinine analogs as CGRP antagonists (Daines et al.1997, W09709046). These compounds displayed only weak affinities for the human CGRP receptor in the micromolar range and were therefore not of great importance (Daines et al., 1997). 

Daines, R.A. (SmithKIine Beecham Corporation, USA) Preparation of quinine and quinidine compounds as antagonists of the Calcitonin gene-related Peptide (CGRP) receptor, W09709046 (1997). 

Hasback, P., Sams, A., Schifter, S., Longmore, J., Edvinsson, L. CGRP receptor mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with CompoundV (W09811128), a non-peptide antagonist, Br. J. Pharmacol. 2001, 133, 1405-1413. 

Woolf CJ, Costigan M (1999) Transcriptional and posttranslational plasticity and the generation of inflammatory pain. Proc Natl Acad Sci USA 96 7723-7730 Wu D, Doods H, Arndt K, Schindler M (2002) Development and potential of non-peptide antagonists for calcitonin-gene-related peptide (CGRP) receptors evidence for CGRP receptor... 

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