-
2
-
-
1542286029
-
CGRP-receptor antagonists - A fresh approach to migraine therapy?
-
Durham PL. CGRP-receptor antagonists - a fresh approach to migraine therapy? N Engl J Med 2004;350: 1073-1075
-
(2004)
N Engl J Med
, vol.350
, pp. 1073-1075
-
-
Durham, P.L.1
-
3
-
-
0842283227
-
Migraine
-
Silberstein SD. Migraine. Lancet 2004;363:381-391
-
(2004)
Lancet
, vol.363
, pp. 381-391
-
-
Silberstein, S.D.1
-
4
-
-
0027103157
-
Calcitonin gene-related peptide: Multiple actions, multiple receptors
-
Poyner DR. Calcitonin gene-related peptide: multiple actions, multiple receptors. Pharmacol Ther 1992;56:23-51
-
(1992)
Pharmacol Ther
, vol.56
, pp. 23-51
-
-
Poyner, D.R.1
-
6
-
-
1542346238
-
Calcitonin gene-related peptide receptor antagonist BIBN 4096 BS for the acute treatment of migraine
-
Olesen J, Diener H.-C, Husstedt IW, et al. Calcitonin gene-related peptide receptor antagonist BIBN 4096 BS for the acute treatment of migraine. N Engl J Med 2004;350:1104-1110
-
(2004)
N Engl J Med
, vol.350
, pp. 1104-1110
-
-
Olesen, J.1
Diener, H.-C.2
Husstedt, I.W.3
-
7
-
-
36148978527
-
Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: Discovery of N-[(3R,6S)-6- 2,3-Difluorophenyl)- 2-oxo-1- 2,2,2-trifluoroethyl)azepan- 3-yl]-4-(2-oxo-2,3- dihydro-1H-imidazo [4,5-b]pyridin-1-yl) piperidine-1-carboxamide (MK-0974)
-
Paone DV, Shaw AW, Nguyen DN, et al. Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-Difluorophenyl)- 2-oxo-1- (2,2,2-trifluoroethyl)azepan- 3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo [4,5-b]pyridin-1-yl) piperidine-1-carboxamide (MK-0974). J Med Chem 2007;50:5564-5567
-
(2007)
J Med Chem
, vol.50
, pp. 5564-5567
-
-
Paone, D.V.1
Shaw, A.W.2
Nguyen, D.N.3
-
8
-
-
0038717244
-
New therapeutic target in primary headaches - Blocking the CGRP receptor
-
and references cited therein
-
Edvinsson L. New therapeutic target in primary headaches - blocking the CGRP receptor. Expert Opin Ther Targets 2003;7:377-383 and references cited therein
-
(2003)
Expert Opin Ther Targets
, vol.7
, pp. 377-383
-
-
Edvinsson, L.1
-
9
-
-
0025143541
-
Vasoactive peptide release in the extracerebral circulation of humans during migraine attack
-
Goadsby PJ, Edvinsson L, Ekman R. Vasoactive peptide release in the extracerebral circulation of humans during migraine attack. Ann Neurol 1990;28:183-187
-
(1990)
Ann Neurol
, vol.28
, pp. 183-187
-
-
Goadsby, P.J.1
Edvinsson, L.2
Ekman, R.3
-
10
-
-
56749157338
-
CGRP blockers in migraine therapy: Where do they act?
-
Edvinsson L. CGRP blockers in migraine therapy: where do they act? Br J Pharmacol 2008;155:967-969
-
(2008)
Br J Pharmacol
, vol.155
, pp. 967-969
-
-
Edvinsson, L.1
-
11
-
-
51549089370
-
Clinical and preclinical rationale for CGRP-receptor antagonists in the treatment of migraine
-
Tepper SJ, Stillman MJ. Clinical and preclinical rationale for CGRP-receptor antagonists in the treatment of migraine. Headache 2008;48:1259-1268
-
(2008)
Headache
, vol.48
, pp. 1259-1268
-
-
Tepper, S.J.1
Stillman, M.J.2
-
12
-
-
0036671940
-
Interaction of calcitonin-gene-related peptide with its receptors
-
Conner AC, Hay DL, Howitt SG, et al. Interaction of calcitonin-gene- related peptide with its receptors. Biochem Soc Trans 2002;30:451-455
-
(2002)
Biochem Soc Trans
, vol.30
, pp. 451-455
-
-
Conner, A.C.1
Hay, D.L.2
Howitt, S.G.3
-
13
-
-
0036266044
-
The mammalian calcitonin gene-related peptides, adrenomedullin, amylin, and calcitonin receptors
-
International Union of Pharmacology. XXXII.
-
Poyner DR, Sexton PM, Marshall I, et al. International Union of Pharmacology. XXXII. The mammalian calcitonin gene-related peptides, adrenomedullin, amylin, and calcitonin receptors. Pharmacol Rev 2002;54:233-246
-
(2002)
Pharmacol Rev
, vol.54
, pp. 233-246
-
-
Poyner, D.R.1
Sexton, P.M.2
Marshall, I.3
-
15
-
-
24944552764
-
Development of human calcitonin gene-Related Peptide (CGRP) receptor antagonists. 1. Potent and selective small molecule CGRP antagonists. 1-[N2- [3,5-Dibromo-N-[[4-(3,4-dihydro-2 (1H)-oxoquinazolin-3-yl)-1-piperidinyl] carbonyl]-D-tyrosyl]-L-lysyl]-4- (4-pyridinyl)piperazine: The first CGRP antagonist for clinical trials in acute migraine
-
Rudolf K, Eberlein W, Engel W, et al. Development of human calcitonin gene-Related Peptide (CGRP) receptor antagonists. 1. Potent and selective small molecule CGRP antagonists. 1-[N2- [3,5-Dibromo-N-[[4-(3,4-dihydro-2 (1H)-oxoquinazolin-3-yl)-1-piperidinyl] carbonyl]-D-tyrosyl]-L-lysyl]-4- (4-pyridinyl)piperazine: the first CGRP antagonist for clinical trials in acute migraine. J Med Chem 2005;48:5921-5931
-
(2005)
J Med Chem
, vol.48
, pp. 5921-5931
-
-
Rudolf, K.1
Eberlein, W.2
Engel, W.3
-
16
-
-
0033970471
-
Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist
-
Doods H, Hallermayer G, Wu Dm, et al. Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol 2000;129:420-423
-
(2000)
Br J Pharmacol
, vol.129
, pp. 420-423
-
-
Doods, H.1
Hallermayer, G.2
Dm, W.3
-
17
-
-
0037134498
-
Receptor activity-modifying protein 1 determines the species selectivity of non-peptide CGRP receptor antagonists
-
Mallee JJ, Salvatore CA, LeBourdelles B, et al. Receptor activity-modifying protein 1 determines the species selectivity of non-peptide CGRP receptor antagonists. J Biol Chem 2002;277:14294-14298
-
(2002)
J Biol Chem
, vol.277
, pp. 14294-14298
-
-
Mallee, J.J.1
Salvatore, C.A.2
Le Bourdelles, B.3
-
18
-
-
0028801446
-
Trigeminal ganglion stimulation increases facial skin blood flow in the rat: A major role for calcitonin gene-related peptide
-
Escott KJ, Beattie DT, Connor HE, et al. Trigeminal ganglion stimulation increases facial skin blood flow in the rat: a major role for calcitonin gene-related peptide. Brain Res 1995;669:93-99
-
(1995)
Brain Res
, vol.669
, pp. 93-99
-
-
Escott, K.J.1
Beattie, D.T.2
Connor, H.E.3
-
19
-
-
2942512592
-
Safety, tolerability and pharmacokinetics of BIBN 4096 BS, the first selective small molecule calcitonin gene-related peptide receptor antagonist, following single intravenous administration in healthy volunteers
-
Iovino M, Feifel U, Yong C-L, et al. Safety, tolerability and pharmacokinetics of BIBN 4096 BS, the first selective small molecule calcitonin gene-related peptide receptor antagonist, following single intravenous administration in healthy volunteers. Cephalalgia 2004;24:645-656
-
(2004)
Cephalalgia
, vol.24
, pp. 645-656
-
-
Iovino, M.1
Feifel, U.2
Yong, C.-L.3
-
23
-
-
71449097958
-
-
Boehringer Ingelheim CGRP antagonists US 2007/ 0244099; 2007, continuation of US 2004/0132716; 2004 (abandoned)
-
Boehringer Ingelheim. CGRP antagonists. US 2007/0244099; 2007, continuation of US 2004/0132716; 2004 (abandoned)
-
-
-
-
30
-
-
71449084949
-
-
Boehringer Ingelheim DE102006039038 2008
-
Boehringer Ingelheim. DE102006039038; 2008
-
-
-
-
33
-
-
71449121882
-
-
Boehringer Ingelheim. X = O: selected CGRP-antagonists process for preparing them and their use as pharmaceutical compositions. US7279471 2007; X = NH: selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions. US7547694 2009
-
Boehringer Ingelheim. X = O: selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions. US7279471; 2007; X = NH: selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions. US7547694; 2009.
-
-
-
-
36
-
-
71449116427
-
-
Boehringer Ingelheim.US2008/045705
-
Boehringer Ingelheim. Production method. US2008/045705; 2008.
-
(2008)
Production Method
-
-
-
37
-
-
71449084485
-
-
Boehringer Ingelheim.WO2009/021942
-
Boehringer Ingelheim. Novel preparation process. WO2009/021942; 2009.
-
(2009)
Novel Preparation Process
-
-
-
38
-
-
71449088441
-
-
Boehringer Ingelheim.WO2009/043797
-
Boehringer Ingelheim. Novel compounds. WO2009/043797; 2009.
-
(2009)
Novel Compounds
-
-
-
39
-
-
71449117386
-
-
Boehringer Ingelheim Pharmaceuticals BI 44370 TA in acute migraine attack ClinicalTrials.gov identifier NCT00751803
-
Boehringer Ingelheim Pharmaceuticals. BI 44370 TA in acute migraine attack. ClinicalTrials.gov identifier NCT00751803
-
-
-
-
40
-
-
71449103951
-
-
Boehringer Ingelheim. (a) Substituted piperidines pharmaceutical compositions containing these compounds their use and processes for the preparation thereof. US702631 2006. (b) Substituted piperidines, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof. US7538115 2009
-
Boehringer Ingelheim. (a) Substituted piperidines, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof. US7026312; 2006. (b) Substituted piperidines, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof. US7538115; 2009.
-
-
-
-
41
-
-
71449090144
-
-
Boehringer Ingelheim. Substituted piperidines pharmaceutical compositions containing these compounds their use and processes for the preparation thereof. US6949541 2005
-
Boehringer Ingelheim. Substituted piperidines, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof. US6949541; 2005.
-
-
-
-
42
-
-
71449084253
-
-
Boehringer Ingelheim. Arylalkane arylalkene and aryl azaalkane medicaments containing said compounds and method for the production thereof. US7230001 2007
-
Boehringer Ingelheim. Arylalkane, arylalkene and aryl azaalkane, medicaments containing said compounds and method for the production thereof. US7230001; 2007.
-
-
-
-
43
-
-
71449087262
-
-
Boehringer Ingelheim. Cyclopropane CGRP antagonists medicaments containing these compounds and method for the production thereof. US7407963 2008
-
Boehringer Ingelheim. Cyclopropane CGRP antagonists, medicaments containing these compounds, and method for the production thereof. US7407963; 2008.
-
-
-
-
44
-
-
71449102500
-
-
Boehringer Ingelheim. Novel compounds. WO2009/034028 2009
-
Boehringer Ingelheim. Novel compounds. WO2009/034028; 2009.
-
-
-
-
45
-
-
71449122589
-
-
Boehringer Ingelheim. Novel compounds. WO2009/034029 2009
-
Boehringer Ingelheim. Novel compounds. WO2009/034029; 2009.
-
-
-
-
46
-
-
71449116118
-
-
Boehringer Ingelheim. CGRP antagonists. WO2009/050232 2009
-
Boehringer Ingelheim. CGRP antagonists. WO2009/050232; 2009.
-
-
-
-
47
-
-
71449120653
-
-
Boehringer Ingelheim. CGRP antagonists. WO2009/050234 2009
-
Boehringer Ingelheim. CGRP antagonists. WO2009/050234; 2009.
-
-
-
-
48
-
-
71449116429
-
-
Boehringer Ingelheim. CGRP antagonists. WO2009/050235 2009
-
Boehringer Ingelheim. CGRP antagonists. WO2009/050235; 2009.
-
-
-
-
49
-
-
71449112653
-
-
Boehringer Ingelheim. CGRP antagonists. WO2009/050237 2009
-
Boehringer Ingelheim. CGRP antagonists. WO2009/050237; 2009.
-
-
-
-
50
-
-
71449094704
-
-
Boehringer Ingelheim. Novel compounds. WO2009/065919 2009
-
Boehringer Ingelheim. Novel compounds. WO2009/065919; 2009.
-
-
-
-
51
-
-
71449127303
-
-
Boehringer Ingelheim. Novel compounds. WO2009/065920 2009
-
Boehringer Ingelheim. Novel compounds. WO2009/065920; 2009.
-
-
-
-
52
-
-
71449100501
-
-
Boehringer Ingelheim. Novel compounds. WO2009/065922 2009
-
Boehringer Ingelheim. Novel compounds. WO2009/065922; 2009.
-
-
-
-
53
-
-
71449120654
-
-
Boehringer Ingelheim. Novel compounds. WO2009/065921 2009
-
Boehringer Ingelheim. Novel compounds. WO2009/065921; 2009.
-
-
-
-
54
-
-
33645886051
-
Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepine lead
-
Williams TM, Stump CA, Nguyen DN, et al. Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepine lead. Bioorg Med Chem Lett 2006;16:2595-2598
-
(2006)
Bioorg Med Chem Lett
, vol.16
, pp. 2595-2598
-
-
Williams, T.M.1
Stump, C.A.2
Nguyen, D.N.3
-
55
-
-
71449089657
-
-
Merck and Co., IncBenzodiazepine CGRP receptor antagonists. US7196079 2007
-
Merck and Co., IncBenzodiazepine CGRP receptor antagonists. US7196079; 2007
-
-
-
-
56
-
-
71449114934
-
-
Merck and Co., Inc. CGRP receptor antagonists.WO2006/078554 2006
-
Merck and Co., Inc. CGRP receptor antagonists. WO2006/078554; 2006
-
-
-
-
57
-
-
71449086320
-
-
Merck and Co., IncBenzodiazepine CGRP receptor antagonists. US7476665 2009
-
Merck and Co., IncBenzodiazepine CGRP receptor antagonists. US7476665; 2009
-
-
-
-
58
-
-
33747336251
-
Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: Optimization of the 4-substituted piperidine
-
Burgey CS, Stump CA, Nguyen DN, et al. Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: optimization of the 4-substituted piperidine. Bioorg Med Chem Lett 2006;16:5052-5056
-
(2006)
Bioorg Med Chem Lett
, vol.16
, pp. 5052-5056
-
-
Burgey, C.S.1
Stump, C.A.2
Nguyen, D.N.3
-
59
-
-
71449109769
-
-
Merck and Co., Inc. Heterocyclic benzodiazepine CGRP receptor antagonists. WO2007/016087 2007
-
Merck and Co., Inc. Heterocyclic benzodiazepine CGRP receptor antagonists. WO2007/016087; 2007
-
-
-
-
60
-
-
34547533721
-
Caprolactams as potent CGRP receptor antagonists for the treatment of migraine
-
Shaw AS, Paone DV, Nguyen DN, et al. Caprolactams as potent CGRP receptor antagonists for the treatment of migraine. Bioorg Med Chem Lett 2007;17:4795-4798
-
(2007)
Bioorg Med Chem Lett
, vol.17
, pp. 4795-4798
-
-
Shaw, A.S.1
Paone, D.V.2
Nguyen, D.N.3
-
61
-
-
71449126178
-
-
Merck and Co., IncCGRP receptor antagonists. US7205292 2007
-
Merck and Co., IncCGRP receptor antagonists. US7205292; 2007
-
-
-
-
62
-
-
71449116901
-
-
Merck and Co., Inc. CGRP receptor antagonists. US7491, 713 2009
-
Merck and Co., Inc. CGRP receptor antagonists. US7491,713; 2009
-
-
-
-
63
-
-
71449113438
-
-
Merck and Co., Inc. CGRP receptor antagonists. US6953790 2005. See also continuation patents (a) US7235545 2007 (b) US7452903; 2008, and (c) US7534784; 2009
-
Merck and Co., Inc. CGRP receptor antagonists. US6953790; 2005. See also continuation patents (a) US7235545; 2007 (b) US7452903; 2008, and (c) US7534784; 2009
-
-
-
-
64
-
-
38749114993
-
Pharmacological characterization of MK-0974 N-[(3R,6S)-6- 2,3- Difluorophenyl)-2-oxo-1- 2,2,2- trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b] pyridin-1-yl)piperidine-1-carboxamide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment of migraine
-
Salvatore CA, Hershey JC, Corcoran HA, et al. Pharmacological characterization of MK-0974 N-[(3R,6S)-6-(2,3- Difluorophenyl)-2-oxo-1-(2,2,2- trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b] pyridin-1-yl)piperidine-1-carboxamide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment of migraine. J Pharmacol Exp Ther 2008;324:416-421
-
(2008)
J Pharmacol Exp Ther
, vol.324
, pp. 416-421
-
-
Salvatore, C.A.1
Hershey, J.C.2
Corcoran, H.A.3
-
65
-
-
13144251165
-
Investigation of the species selectivity of a nonpeptide CGRP receptor antagonist using a novel pharmacodynamic assay
-
Hershey JC, Corcoran HA, Baskin EP, et al. Investigation of the species selectivity of a nonpeptide CGRP receptor antagonist using a novel pharmacodynamic assay. Regul Pept 2005;127:71-77
-
(2005)
Regul Pept
, vol.127
, pp. 71-77
-
-
Hershey, J.C.1
Corcoran, H.A.2
Baskin, E.P.3
-
66
-
-
71449090386
-
-
Merck and Co., Inc. CGRP receptor antagonists. WO2006/041830 2006
-
Merck and Co., Inc. CGRP receptor antagonists. WO2006/041830; 2006
-
-
-
-
67
-
-
71449098828
-
-
Merck and Co., Inc. Benzazepine compounds as CGRP receptor antagonists. WO2008/085317 2008
-
Merck and Co., Inc. Benzazepine compounds as CGRP receptor antagonists. WO2008/085317; 2008
-
-
-
-
68
-
-
71449118074
-
-
Merck and Co., Inc. CGRP receptor antagonists. WO2006/044449 2006
-
Merck and Co., Inc. CGRP receptor antagonists. WO2006/044449; 2006
-
-
-
-
69
-
-
71449116673
-
-
Merck and Co., Inc. CGRP receptor antagonists. WO2006/047196 2006
-
Merck and Co., Inc. CGRP receptor antagonists. WO2006/047196; 2006
-
-
-
-
70
-
-
71449084006
-
-
Merck and Co., Inc. CGRP receptor antagonists. WO2006/044504 2006
-
Merck and Co., Inc. CGRP receptor antagonists. WO2006/044504; 2006
-
-
-
-
72
-
-
71449100254
-
-
Merck and Co., Inc. CGRP receptor antagonists. WO2006/099268 2006
-
Merck and Co., Inc. CGRP receptor antagonists. WO2006/099268; 2006
-
-
-
-
73
-
-
38149000824
-
Calcitonin gene-related peptide (CGRP) receptor antagonists: Investigations of a pyridinone template
-
Nguyen DN, Paone DV, Shaw AS, et al. Calcitonin gene-related peptide (CGRP) receptor antagonists: investigations of a pyridinone template. Bioorg Med Chem Lett 2008;18:755-758
-
(2008)
Bioorg Med Chem Lett
, vol.18
, pp. 755-758
-
-
Nguyen, D.N.1
Paone, D.V.2
Shaw, A.S.3
-
74
-
-
71449111226
-
-
Merck and Co., IncCarboxamide spirohydantoin CGRP receptor antagonists. US7288559 2007
-
Merck and Co., IncCarboxamide spirohydantoin CGRP receptor antagonists. US7288559; 2007
-
-
-
-
75
-
-
71449095155
-
-
Merck and Co., IncBenzodiazepine spirohydantoin CGRP receptor antagonists. US7205293 2007
-
Merck and Co., IncBenzodiazepine spirohydantoin CGRP receptor antagonists. US7205293; 2007
-
-
-
-
76
-
-
71449117142
-
-
Merck and Co., IncAryl spirohydantoin CGRP receptor antagonists. US7189722 2007
-
Merck and Co., IncAryl spirohydantoin CGRP receptor antagonists. US7189722; 2007
-
-
-
-
77
-
-
71449099784
-
-
Merck and Co., IncMonocyclic anilide spirohydantoin CGRP receptor antagonists. US7192954 2007
-
Merck and Co., IncMonocyclic anilide spirohydantoin CGRP receptor antagonists. US7192954; 2007
-
-
-
-
78
-
-
71449113200
-
-
Merck and Co., Inc. Monocyclic anilide spirolactam CGRP receptor antagonists. WO2008/112159 2008
-
Merck and Co., Inc. Monocyclic anilide spirolactam CGRP receptor antagonists. WO2008/112159; 2008
-
-
-
-
79
-
-
71449101204
-
-
Merck and Co., Inc. CGRP receptor antagonists with tertiary amide, sulfonamide, carbamate, and urea end groups. WO2008/127584 2008
-
Merck and Co., Inc. CGRP receptor antagonists with tertiary amide, sulfonamide, carbamate, and urea end groups. WO2008/127584; 2008
-
-
-
-
80
-
-
71449088920
-
-
Merck and Co., IncBicyclic anilide spirohydantoin CGRP receptor antagonists. US7202251 2007
-
Merck and Co., IncBicyclic anilide spirohydantoin CGRP receptor antagonists. US7202251; 2007
-
-
-
-
81
-
-
33750704948
-
Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists
-
Bell IM, Bednar RA, Fay JF, et al. Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists. Bioorg Med Chem Lett 2006;16:6165-6169
-
(2006)
Bioorg Med Chem Lett
, vol.16
, pp. 6165-6169
-
-
Bell, I.M.1
Bednar, R.A.2
Fay, J.F.3
-
82
-
-
71449114142
-
-
Merck and Co., Inc. Tricyclic anilide spirohydantoin CGRP receptor antagonists. WO2006/031676 2006
-
Merck and Co., Inc. Tricyclic anilide spirohydantoin CGRP receptor antagonists. WO2006/031676; 2006
-
-
-
-
83
-
-
55549139050
-
Potent benzimidazolone-based CGRP receptor antagonists
-
Theberge CR, Bednar RA, Bell IM, et al. Potent benzimidazolone-based CGRP receptor antagonists. Bioorg Med Chem Lett 2008;18:6122-6125
-
(2008)
Bioorg Med Chem Lett
, vol.18
, pp. 6122-6125
-
-
Theberge, C.R.1
Bednar, R.A.2
Bell, I.M.3
-
84
-
-
57849129258
-
The discovery of highly potent CGRP receptor antagonists
-
Stump CA, Bell IM, Bednar RA, et al. The discovery of highly potent CGRP receptor antagonists. Bioorg Med Chem Lett 2009:19:214-217
-
(2009)
Bioorg Med Chem Lett
, vol.19
, pp. 214-217
-
-
Stump, C.A.1
Bell, I.M.2
Bednar, R.A.3
-
85
-
-
71449095582
-
-
Merck and Co., Inc. Bicyclic anilide spirolactam CGRP receptor antagonists. WO2006/031610 2006
-
Merck and Co., Inc. Bicyclic anilide spirolactam CGRP receptor antagonists. WO2006/031610; 2006
-
-
-
-
86
-
-
71449083498
-
-
Merck and Co., Inc. Tricyclic anilide spirolactam CGRP receptor antagonists. WO2006/031491 2006
-
Merck and Co., Inc. Tricyclic anilide spirolactam CGRP receptor antagonists. WO2006/031491; 2006
-
-
-
-
87
-
-
67651102827
-
The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists
-
Bell IM, Bednar RA, Corcoran HA, et al. The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists. Bioorg Med Chem Lett 2009;19:4740-4742
-
(2009)
Bioorg Med Chem Lett
, vol.19
, pp. 4740-4742
-
-
Bell, I.M.1
Bednar, R.A.2
Corcoran, H.A.3
-
88
-
-
71449118299
-
-
Merck and Co., Inc. Bicyclic anilide heterocyclic CGRP receptor antagonists. WO2008/130512 2008
-
Merck and Co., Inc. Bicyclic anilide heterocyclic CGRP receptor antagonists. WO2008/130512; 2008
-
-
-
-
89
-
-
71449094928
-
-
Merck and Co., Inc. Tricyclic anilide heterocyclic CGRP receptor antagonists. WO2008/153852 2008
-
Merck and Co., Inc. Tricyclic anilide heterocyclic CGRP receptor antagonists. WO2008/153852; 2008
-
-
-
-
90
-
-
71449095154
-
-
Merck and Co., Inc. Aryl spirolactam CGRP receptor antagonists. WO2006/031513 2006
-
Merck and Co., Inc. Aryl spirolactam CGRP receptor antagonists. WO2006/031513; 2006
-
-
-
-
91
-
-
71449115174
-
-
Merck and Co., Inc. Aryl heterocyclic CGRP receptor antagonists. WO2008/130524; 2008
-
Merck and Co., Inc. Aryl heterocyclic CGRP receptor antagonists. WO2008/130524; 2008
-
-
-
-
92
-
-
71449100973
-
-
Merck and Co., Inc. Monocyclic anilide spirolactam CGRP receptor antagonists. WO2006/029153; 2006
-
Merck and Co., Inc. Monocyclic anilide spirolactam CGRP receptor antagonists. WO2006/029153; 2006
-
-
-
-
93
-
-
71449098829
-
-
Merck and Co., Inc. Constrained spirocyclic compounds as CGRP receptor antagonists. WO2008/073251; 2008
-
Merck and Co., Inc. Constrained spirocyclic compounds as CGRP receptor antagonists. WO2008/073251; 2008
-
-
-
-
94
-
-
71449085923
-
-
Merck and Co., Inc. Substituted spirocyclic CGRP receptor antagonists. WO2008/020902 2008
-
Merck and Co., Inc. Substituted spirocyclic CGRP receptor antagonists. WO2008/020902; 2008
-
-
-
-
96
-
-
71449083006
-
-
Merck and Co., IncCarboxamide spirolactam CGRP receptor antagonists. US7390798 2008
-
Merck and Co., IncCarboxamide spirolactam CGRP receptor antagonists. US7390798; 2008
-
-
-
-
97
-
-
71449100747
-
-
Merck and Co., Inc. Carboxamide heterocyclic CGRP receptor antagonists. WO2008/153849 2008
-
Merck and Co., Inc. Carboxamide heterocyclic CGRP receptor antagonists. WO2008/153849; 2008
-
-
-
-
98
-
-
71449109299
-
-
Merck and Co. Inc. Bicyclic spirohydantoin CGRP receptor antagonists. WO2007/061695; 2007
-
Merck and Co. , Inc. Bicyclic spirohydantoin CGRP receptor antagonists. WO2007/061695; 2007
-
-
-
-
99
-
-
71449110007
-
-
Merck and Co., Inc. Spirohydantoin tricyclic CGRP receptor antagonists. WO2007/061694; 2007
-
Merck and Co., Inc. Spirohydantoin tricyclic CGRP receptor antagonists. WO2007/061694; 2007
-
-
-
-
100
-
-
71449099783
-
-
Merck and Co., Inc. Spirolactam aryl CGRP receptor antagonists. WO2007/061677; 2007
-
Merck and Co., Inc. Spirolactam aryl CGRP receptor antagonists. WO2007/061677; 2007
-
-
-
-
101
-
-
71449102498
-
-
Merck and Co., Inc. Spirolactam tricyclic CGRP receptor antagonists. WO2007/061692; 2007
-
Merck and Co., Inc. Spirolactam tricyclic CGRP receptor antagonists. WO2007/061692; 2007
-
-
-
-
102
-
-
71449116897
-
-
Merck and Co., Inc. Spirohydantoin aryl CGRP receptor antagonists. WO2007/061676; 2007
-
Merck and Co., Inc. Spirohydantoin aryl CGRP receptor antagonists. WO2007/061676; 2007
-
-
-
-
103
-
-
71449124524
-
-
Merck and Co., Inc. Spirolactam bicyclic CGRP receptor antagonists. WO2007/061696; 2007
-
Merck and Co., Inc. Spirolactam bicyclic CGRP receptor antagonists. WO2007/061696; 2007
-
-
-
-
104
-
-
71449109072
-
-
Merck and Co., Inc. Hydroxypyridine CGRP receptor antagonists. WO2005/009962; 2005
-
Merck and Co., Inc. Hydroxypyridine CGRP receptor antagonists. WO2005/009962; 2005
-
-
-
-
105
-
-
71449099058
-
-
Merck and Co., IncBenzimidazolinyl piperidines as CGRP ligands. US6552043; 2003
-
Merck and Co., IncBenzimidazolinyl piperidines as CGRP ligands. US6552043; 2003
-
-
-
-
106
-
-
71449122117
-
-
Bristol-Myers Squibb. Novel beta-turn mimetics as calcitonin gene related peptide receptor antagonists. US20050209256; 2005
-
Bristol-Myers Squibb. Novel beta-turn mimetics as calcitonin gene related peptide receptor antagonists. US20050209256; 2005.
-
-
-
-
107
-
-
71449106293
-
-
Bristol-Myers Squibb. Calcitonin gene related peptide receptor antagonists. WO03/104326; 2003
-
Bristol-Myers Squibb. Calcitonin gene related peptide receptor antagonists. WO03/104326; 2003.
-
-
-
-
108
-
-
71449125719
-
-
Bristol-Myers Squibb. Heterocyclic anti-migraine agents. US2005/0153959; 2005
-
Bristol-Myers Squibb. Heterocyclic anti-migraine agents. US2005/0153959; 2005.
-
-
-
-
109
-
-
71449095797
-
-
Bristol-Myers Squibb. CGRP antagonists. US2007/0049577; 2007
-
Bristol-Myers Squibb. CGRP antagonists. US2007/0049577; 2007.
-
-
-
-
110
-
-
71449087500
-
-
Bristol-Myers Squibb US2007/0149502; 2007
-
Bristol-Myers Squibb. US2007/0149502; 2007
-
-
-
-
111
-
-
71449110248
-
-
Bristol-Myers Squibb US2007/0149503; 2007
-
Bristol-Myers Squibb. US2007/0149503; 2007
-
-
-
-
112
-
-
71449109768
-
-
Bristol-Myers Squibb. Constrained compounds as CGRP-receptor antagonists. US7380930; 2008
-
Bristol-Myers Squibb. Constrained compounds as CGRP-receptor antagonists. US7380930; 2008.
-
-
-
-
113
-
-
71449123306
-
-
Bristol-Myers Squibb. Constrained compounds as CGRP-receptor antagonists. US7380931; 2008
-
Bristol-Myers Squibb. Constrained compounds as CGRP-receptor antagonists. US7380931; 2008.
-
-
-
-
114
-
-
71449101203
-
-
Bristol-Myers Squibb. Constrained compounds as CGRP-receptor antagonists. US7544680; 2009
-
Bristol-Myers Squibb. Constrained compounds as CGRP-receptor antagonists. US7544680; 2009.
-
-
-
-
115
-
-
71449098187
-
-
Bristol-Myers Squibb. Constrained compounds as CGRP-receptor antagonists. US7470679; 2008
-
Bristol-Myers Squibb. Constrained compounds as CGRP-receptor antagonists. US7470679; 2008.
-
-
-
-
116
-
-
71449115646
-
-
Bristol-Myers Squibb. Constrained compounds as CGRP-receptor antagonists. US7470680; 2008
-
Bristol-Myers Squibb. Constrained compounds as CGRP-receptor antagonists. US7470680; 2008.
-
-
-
-
117
-
-
71449124274
-
-
Bristol-Myers Squibb. (a) Anti-migraine treatments. US7314883; 2008
-
Bristol-Myers Squibb. (a) Anti-migraine treatments. US7314883; 2008.
-
-
-
-
118
-
-
50249096199
-
Discovery of (R)-4-(8-Fluoro-2-oxo-1,2- dihydroquinazolin-3-(4H)-yl-N-(3- (7-methyl-1H-indazol-5-yl)-1-oxo- 1-(4-(piperidin-1-yl)piperidn-1-yl) propan-2-yl)piperidine-1-carboxamide (BMS-694153): A potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and efficient intranasal exposure
-
Degnan AP, Chaturvedula PV, Conway CM, et al. Discovery of (R)-4-(8-Fluoro-2-oxo-1,2- dihydroquinazolin-3-(4H)-yl-N-(3- (7-methyl-1H-indazol-5-yl)-1-oxo- 1-(4-(piperidin-1-yl)piperidn-1-yl) propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and efficient intranasal exposure. J Med Chem 2008;51:4858-4861
-
(2008)
J Med Chem
, vol.51
, pp. 4858-4861
-
-
Degnan, A.P.1
Chaturvedula, P.V.2
Conway, C.M.3
-
119
-
-
71449088698
-
-
Bristol-Myers Squibb. Novel therapeutic agents for the treatment of migraine. US2005/0215576; 2005
-
Bristol-Myers Squibb. Novel therapeutic agents for the treatment of migraine. US2005/0215576; 2005.
-
-
-
-
120
-
-
66349123811
-
Carbamates as potent calcitonin gene-related peptide antagonists with improved solution stability
-
Degnan AP, Conway CM, Dalterio RA, et al. Carbamates as potent calcitonin gene-related peptide antagonists with improved solution stability. Bioorg Med Chem Lett 2009;19:3555-3558
-
(2009)
Bioorg Med Chem Lett
, vol.19
, pp. 3555-3558
-
-
Degnan, A.P.1
Conway, C.M.2
Dalterio, R.A.3
-
121
-
-
71449089656
-
-
Bristol-Myers Squibb. Calcitonin gene related peptide receptor antagonists. US7220862; 2007
-
Bristol-Myers Squibb. Calcitonin gene related peptide receptor antagonists. US7220862; 2007.
-
-
-
-
122
-
-
71449124013
-
-
Bristol-Myers Squibb. Calcitonin gene related peptide receptor antagonists. WO2005/065779; 2005
-
Bristol-Myers Squibb. Calcitonin gene related peptide receptor antagonists. WO2005/065779; 2005.
-
-
-
-
123
-
-
71449097476
-
-
SmithKline Beecham Corporation. Compounds and methods. WO97/09046; 1997
-
SmithKline Beecham Corporation. Compounds and methods. WO97/09046; 1997.
-
-
-
-
124
-
-
0030708674
-
Quinine analogs as non-peptide calcitonin gene-related peptide (CGRP) receptor antagonists
-
Daines RA, Sham KKC, Taggart JJ, et al. Quinine analogs as non-peptide calcitonin gene-related peptide (CGRP) receptor antagonists. Bioorg Med Chem Lett 1997;7:2673-2676
-
(1997)
Bioorg Med Chem Lett
, vol.7
, pp. 2673-2676
-
-
Daines, R.A.1
Sham, K.K.C.2
Taggart, J.J.3
-
125
-
-
71449104969
-
-
SmithKline Beecham Corporation. Compounds and methods. WO98/09630; 1998
-
SmithKline Beecham Corporation. Compounds and methods. WO98/09630; 1998.
-
-
-
-
126
-
-
71449097475
-
-
SmithKline Beecham Corporation. 4-Sulfinyl benzamides as calcitonin gene-related peptide receptor antagonists. WO98/56779; 1998
-
SmithKline Beecham Corporation. 4-Sulfinyl benzamides as calcitonin gene-related peptide receptor antagonists. WO98/56779; 1998.
-
-
-
-
127
-
-
0035129463
-
Pharmacology of SB-273779, a nonpeptide calcitonin gene-related peptide 1 receptor antagonist
-
Aiyar N, Daines RA, Disa J, et al. Pharmacology of SB-273779, a nonpeptide calcitonin gene-related peptide 1 receptor antagonist. J Pharmacol Exp Ther 2001;296:768-775
-
(2001)
J Pharmacol Exp Ther
, vol.296
, pp. 768-775
-
-
Aiyar, N.1
Daines, R.A.2
Disa, J.3
-
128
-
-
71449112652
-
-
Glaxo Group Limited. 5-Phenyl-1, 3,4-oxadiazol-2-yl-acetyl- 4-piperidinyl derivatives as CGRP receptor antagonists. WO2009/000819; 2009
-
Glaxo Group Limited. 5-Phenyl-1,3,4-oxadiazol-2-yl-acetyl- 4-piperidinyl derivatives as CGRP receptor antagonists. WO2009/000819; 2009.
-
-
-
-
129
-
-
71449124273
-
-
Glaxo Group Limited Pyrrolo[ 2,3-d] pyrimidine derivatives as CGRP receptor antagonists. WO2009/060682; 2009
-
Glaxo Group Limited. Pyrrolo[2,3-d] pyrimidine derivatives as CGRP receptor antagonists. WO2009/060682; 2009.
-
-
-
-
130
-
-
71449085671
-
-
Vertex Pharmaceuticals Incorporated. CGRP receptor antagonists. WO2008/011190; 2008
-
Vertex Pharmaceuticals Incorporated. CGRP receptor antagonists. WO2008/011190; 2008.
-
-
-
-
131
-
-
71449084252
-
-
Vertex Pharmaceuticals Incorporated. CGRP receptor antagonists. WO2007/146349; 2007
-
Vertex Pharmaceuticals Incorporated. CGRP receptor antagonists. WO2007/146349; 2007.
-
-
-
-
132
-
-
71449103950
-
-
Neurogen Corporation. Biaryl ketone-substituted piperidines. WO2008/070014; 2008
-
Neurogen Corporation. Biaryl ketone-substituted piperidines. WO2008/070014; 2008.
-
-
-
-
133
-
-
71449125717
-
-
Neurogen Corporation. Amide-substituted aryl piperidines. WO2008/060568; 2008
-
Neurogen Corporation. Amide-substituted aryl piperidines. WO2008/060568; 2008.
-
-
-
-
134
-
-
71449101781
-
-
Grünenthal GmbH. Substituted cyclopentene compounds. US7109214; 2006
-
Grünenthal GmbH. Substituted cyclopentene compounds. US7109214;2006.
-
-
-
-
135
-
-
42249087655
-
Randomized controlled trial of an oral CGRP receptor antagonist, MK-0974, in acute treatment of migraine
-
Ho TW, Mannix LK, Fan X, et al. Randomized controlled trial of an oral CGRP receptor antagonist, MK-0974, in acute treatment of migraine. Neurology 2008;70:1304-1312
-
(2008)
Neurology
, vol.70
, pp. 1304-1312
-
-
Ho, T.W.1
Mannix, L.K.2
Fan, X.3
-
136
-
-
57649233374
-
Efficacy and tolerability of MK-0974 (telcagepant), a new oral antagonist of calcitonin gene-related peptide receptor, compared with zolmitriptan for acute migraine: A randomised, placebo-controlled, parallel-treatment trial
-
Ho TW, Ferrari MD, Dodick DW, et al. Efficacy and tolerability of MK-0974 (telcagepant), a new oral antagonist of calcitonin gene-related peptide receptor, compared with zolmitriptan for acute migraine: a randomised, placebo-controlled, parallel-treatment trial. Lancet 2008;372:2115-2123
-
(2008)
Lancet
, vol.372
, pp. 2115-2123
-
-
Ho, T.W.1
Ferrari, M.D.2
Dodick, D.W.3
-
137
-
-
67650688361
-
Telcagepant is a new oral treatment for migraine
-
Doggrell SA. Telcagepant is a new oral treatment for migraine. Expert Opin Pharmacother 2009;10:1523-1526
-
(2009)
Expert Opin Pharmacother
, vol.10
, pp. 1523-1526
-
-
Doggrell, S.A.1
-
138
-
-
71449116898
-
-
Boehringer Ingelheim. Use of selected CGRP-antagonists in combination with other antimigraine drugs for the treatment of migraine. US2006/0142273; 2006
-
Boehringer Ingelheim. Use of selected CGRP-antagonists in combination with other antimigraine drugs for the treatment of migraine. US2006/0142273; 2006.
-
-
-
-
139
-
-
71449127302
-
-
Boehringer Ingelheim. CGRP-antagonist in combination with serotonin-reuptake inhibitor for the treatment of migraine. US2005/0233980; 2005
-
Boehringer Ingelheim. CGRP-antagonist in combination with serotonin-reuptake inhibitor for the treatment of migraine. US2005/0233980; 2005.
-
-
-
-
140
-
-
71449085422
-
-
Boehringer Ingelheim DE10314617; 2004
-
Boehringer Ingelheim. DE10314617; 2004
-
-
-
-
141
-
-
71449114389
-
-
Rita Dobmeyer. Medication for the treatment or prevention of migraine. EP1374870; 2004
-
Rita Dobmeyer. Medication for the treatment or prevention of migraine. EP1374870; 2004.
-
-
-
|