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CP-154,526, a selective, non-peptide antagonist of the corticotropin-releasing factor1 receptor attenuates stress-induced relapse to drug seeking in cocaine- and heroin-trained rats
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(d) Shaham, Y.; Erb, S.; Leung, S.; Buczek, Y.; Stewart, J. CP-154,526, a selective, non-peptide antagonist of the corticotropin-releasing factor1 receptor attenuates stress-induced relapse to drug seeking in cocaine- and heroin-trained rats. Psychopharmacology 1998, 137, 184.
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Role of corticotropin-releasing factor receptor-1 in opiate withdrawal
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In vivo and in vitro characterization of antalarmin, a nonpeptide corticotropin-releasing hormone (CRF) receptor antagonist: Suppression of pituitary ACTH release and peripheral inflammation
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Webster, E. L.; Lewis, D. B.; Torpy, D. J.; Zachman, E. K.; Rice, K. C.; Chrousos, G. P. In vivo and in vitro characterization of antalarmin, a nonpeptide corticotropin-releasing hormone (CRF) receptor antagonist: suppression of pituitary ACTH release and peripheral inflammation. Endocrinology 1996, 137, 5747.
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(b) Bornstein, S. R.; Webster, E. L.; Torpy, D. J.; Richman, S. J.; Mitsiades, N.; Igel, M.; Lewis, D. B.; Rice, K. C.; Joost, H. G.; Tsokos, M.; Chrousos, G. P. Chronic effects of a nonpeptide corticotropin-releasing hormone type I receptor antagonist on pituitary-adrenal function, body weight, and metabolic regulation. Endocrinology 1998, 139, 1546.
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The impact of the nonpeptide corticotropin-releasing hormone antagonist antalarmin on behavioral and endocrine responses to stress
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(c) Deak, T.; Nguyen, K. T.; Ehrlich, A. L.; Watkins, L. R.; Spencer, R. L.; Maier, S. F.; Licinio, J.; Wong, M. L.; Chrousos, G. P.; Webster, E.; Gold, P. W. The impact of the nonpeptide corticotropin-releasing hormone antagonist antalarmin on behavioral and endocrine responses to stress. Endocrinology 1999, 140, 79.
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Synthesis and SAR of 2-aryloxy-4-alkoxy-pyridines as potent orally active corticotrophin-releasing factor 1 antagonists
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ASAP Article, DOI: 10.021/jm070578k
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Chen, Y. L.; Braselton, J.; Forman, J.; Gallaschun, R. J.; Mansbach, R.; Schmidt, A.; Seeger, T. F.; Sprouse, J.; Tingley, F. D.; Winston, E.; Schulz, D. W. Synthesis and SAR of 2-aryloxy-4-alkoxy-pyridines as potent orally active corticotrophin-releasing factor 1 antagonists. J. Med. Chem. 2008, ASAP Article, DOI: 10.021/jm070578k.
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J. Med. Chem
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Chen, Y.L.1
Braselton, J.2
Forman, J.3
Gallaschun, R.J.4
Mansbach, R.5
Schmidt, A.6
Seeger, T.F.7
Sprouse, J.8
Tingley, F.D.9
Winston, E.10
Schulz, D.W.11
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16
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41649116138
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Unpublished data. A representative compound in pyrrolo[2,3-d] pyrimidine series, e.g., 2-[7-(4-bromo-2,6-dimethylphenyl)-2,5-dimethyl7 H-pyrrolo[2,3-d]pyrimidin-4-ylamino]-(S)-butan-1-ol, was found to produce liver toxicity in 90 day toxicology studies in rats and dogs.
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Unpublished data. A representative compound in pyrrolo[2,3-d] pyrimidine series, e.g., 2-[7-(4-bromo-2,6-dimethylphenyl)-2,5-dimethyl7 H-pyrrolo[2,3-d]pyrimidin-4-ylamino]-(S)-butan-1-ol, was found to produce liver toxicity in 90 day toxicology studies in rats and dogs.
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17
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29544452308
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NBI 30775 (R121919), an orally active antagonist of the corticotropin-releasing factor (CRF) type-1 receptor for the treatment of anxiety and depression
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Chen, C.; Grigoriadis, D. E. NBI 30775 (R121919), an orally active antagonist of the corticotropin-releasing factor (CRF) type-1 receptor for the treatment of anxiety and depression. Drug Dev. Res. 2005, 65, 216.
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Chen, C.1
Grigoriadis, D.E.2
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18
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41649093659
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Unpublished phase I data.
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Unpublished phase I data.
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19
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41649120052
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Because the pyridine N-oxide intermediates may show exothermic decomposition, it is recommended to test the differential scanning calorimeter prior to scale-up synthesis. Pyridine N-oxide intermediates are not recommended for large-scale preparation, and caution is required to ensure safety in the laboratory. In general, a 100°C difference between process temperature and decomposition temperature is considered to be acceptable.
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Because the pyridine N-oxide intermediates may show exothermic decomposition, it is recommended to test the differential scanning calorimeter prior to scale-up synthesis. Pyridine N-oxide intermediates are not recommended for large-scale preparation, and caution is required to ensure safety in the laboratory. In general, a 100°C difference between process temperature and decomposition temperature is considered to be acceptable.
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20
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0020525367
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Chlorination yield was improved in the presence of 1 equiv of N,N-diethylaniline. Croisy-Delcey, M.; Bisagni, E. Aza analogs of lucanthone: synthesis and antitumor and bactericidal properties. J. Med. Chem. 1983, 26, 1329.
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Chlorination yield was improved in the presence of 1 equiv of N,N-diethylaniline. Croisy-Delcey, M.; Bisagni, E. Aza analogs of lucanthone: synthesis and antitumor and bactericidal properties. J. Med. Chem. 1983, 26, 1329.
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