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Volumn 18, Issue 13, 2008, Pages 3778-3782

Design, synthesis, and structure-activity relationship study of a novel class of ORL1 receptor antagonists based on N-biarylmethyl spiropiperidine

Author keywords

Antagonist; hERG channel; N Biarylmethyl spiropiperidine; ORL1

Indexed keywords

1' [[1 (3 CHLOROPYRIDIN 2 YL) 1H PYRAZOL 4 YL]METHYL] 3H SPIRO 2 BENZOFURAN 1,4' PIPERIDINE; OPIATE ANTAGONIST; OPIATE RECEPTOR; PIPERIDINE DERIVATIVE; POTASSIUM CHANNEL;

EID: 44849137530     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.05.036     Document Type: Article
Times cited : (13)

References (29)
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    • Ito, F.; Noguchi, H.; Ohashi, Y.; Kondo, H.; Yamagishi, T. WO 99/36421, 1999.
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    • Kyle, D.; Goehring, R. R.; Shao, B. WO 01/39775 A1, 2001.
    • Kyle, D.; Goehring, R. R.; Shao, B. WO 01/39775 A1, 2001.
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    • Ito, F.; Ohashi, Y. EP 0997464 A1, 2000.
    • Ito, F.; Ohashi, Y. EP 0997464 A1, 2000.
  • 23
    • 44849116685 scopus 로고    scopus 로고
    • Yoshizumi, T.; Takahashi, H.; Miyazoe, H.; Sugimoto, Y.; Tsujita, T.; Kato, T.; Ito, H.; Kawamoto, H.; Hirayama, M.; Ichikawa, D.; Azuma-Kanoh, T.; Ozaki, S.; Shibata, Y.; Tani, T.; Chiba, M.; Ishii, Y.; Okuda, S.; Tadano, K.; Fukuroda, T.; Okamoto, O.; Ohta, H. J. Med. Chem., in press.
    • Yoshizumi, T.; Takahashi, H.; Miyazoe, H.; Sugimoto, Y.; Tsujita, T.; Kato, T.; Ito, H.; Kawamoto, H.; Hirayama, M.; Ichikawa, D.; Azuma-Kanoh, T.; Ozaki, S.; Shibata, Y.; Tani, T.; Chiba, M.; Ishii, Y.; Okuda, S.; Tadano, K.; Fukuroda, T.; Okamoto, O.; Ohta, H. J. Med. Chem., in press.
  • 24
    • 44849135910 scopus 로고    scopus 로고
    • note
    • Seventy-eight kinds of aldehydes consist of the following structures: pyridine-substituted benzaldehydes (8 kinds), pyrimidine substituted benzaldehydes (4 kinds), 4-(1-pyrro)benzaldehyde, 4-(2-thiazolyl)benzaldehyde, 4-(1,2,3-thiadiazol-4-yl)benzaldehyde, 2-methyl-3-formyl-5-phenylfuran, 3-methyl-4-formyl-5-phenyl-1,2-oxazole, 2-methyl-3-formyl-4-phenyl-1,2-oxazole, 2-formyl-5-phenylthiophene, 2-formyl-5-(2-pyridyl)thiophene, 2-formyl-thiazoles with aromatic substituent (11 kinds), 4-formyl-2-phenylthiazole, 2-formylpyrroles with aromatic substituent at the 1-position (37 kinds), 1-(2-cyanophenyl)-3-formylpyrrole, 3-formylpyrazoles with aromatic substituent at the 1-position (6 kinds), 1-phenyl-5-formylpyrazole, 1-phenyl-4-formyl-1,2,3-triazole.
  • 27
    • 44849122023 scopus 로고    scopus 로고
    • note
    • Rat microsomal (RM) and human microsomal (HM) stabilities were determined by percentage parent compound (1 μM) remaining after 30 min (37 °C) incubation with rat/human liver microsomes (0.25 mg protein/ml).
  • 28
    • 44849094911 scopus 로고    scopus 로고
    • note
    • +.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.