Thiazolo[4,5-d]pyrimidine thiones and -ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists

被引:35
作者
Beck, JP
Curry, MA
Chorvat, RJ
Fitzgerald, LW
Gilligan, PJ
Zaczek, R
Trainor, GL
机构
[1] Dupont Pharmaceut Co, Chem & Phys Sci, Wilmington, DE 19880 USA
[2] Dupont Pharmaceut Co, CNS Dis Res, Expt Stn, Wilmington, DE 19880 USA
关键词
D O I
10.1016/S0960-894X(99)00159-6
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of thiazolo[4,5-d]pyrimidine thiones and -ones was prepared and discovered to have good binding affinity to the CRH-R1 receptor, thus showing promise as a new class of potential anxiolytics and/or antidepressants. (C) 1999 DuPont Pharmaceuticals Company. Published by Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1185 / 1188
页数:4
相关论文
共 19 条
[1]   Non-peptide corticotropin-releasing hormone antagonists: Syntheses and structure-activity relationships of 2-anilinopyrimidines and -triazines [J].
Arvanitis, AG ;
Gilligan, PJ ;
Chorvat, RJ ;
Cheeseman, RS ;
Christos, TE ;
Bakthavatchalam, R ;
Beck, JP ;
Cocuzza, AJ ;
Hobbs, FW ;
Wilde, RG ;
Arnold, C ;
Chidester, D ;
Curry, M ;
He, LQ ;
Hollis, A ;
Klaczkiewicz, J ;
Krenitsky, PJ ;
Rescinito, JP ;
Scholfield, E ;
Culp, S ;
De Souza, EB ;
Fitzgerald, L ;
Grigoriadis, D ;
Tam, SW ;
Wong, YN ;
Huang, SM ;
Shen, HL .
JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (05) :805-818
[2]   POTENTIAL ANTI-MICROBIALS .2. SYNTHESIS AND INVITRO ANTIMICROBIAL EVALUATION OF SOME THIAZOLO[4,5-D]PYRIMIDINES [J].
BADAWEY, ESAM ;
RIDA, SM ;
HAZZA, AA ;
FAHMY, HTY ;
GOHAR, YM .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1993, 28 (02) :97-101
[3]   Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists [J].
Beck, JP ;
Arvanitis, AG ;
Curry, MA ;
Rescinito, JT ;
Fitzgerald, LW ;
Gilligan, PJ ;
Zaczek, R ;
Trainor, GL .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1999, 9 (07) :967-972
[4]  
Chen C, 1996, J MED CHEM, V39, P4358
[5]   Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: A centrally active corticotropin-releasing factor(1) receptor antagonist [J].
Chen, YL ;
Mansbach, RS ;
Winter, SM ;
Brooks, E ;
Collins, J ;
Corman, ML ;
Dunaiskis, AR ;
Faraci, WS ;
Gallaschun, RJ ;
Schmidt, A ;
Schulz, DW .
JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (11) :1749-1754
[6]  
CHEN YL, 1998, Patent No. 08847
[7]   Synthesis, corticotropin-releasing factor receptor binding affinity, and pharmacokinetic properties of triazolo-, imidazo-, and pyrrolopyrimidines and -pyridines [J].
Chorvat, RJ ;
Bakthavatchalam, R ;
Beck, JP ;
Gilligan, PJ ;
Wilde, RG ;
Cocuzza, AJ ;
Hobbs, FW ;
Cheeseman, RS ;
Curry, M ;
Rescinito, JP ;
Krenitsky, P ;
Chidester, D ;
Yarem, JA ;
Klaczkiewicz, JD ;
Hodge, CN ;
Aldrich, PE ;
Wasserman, ZR ;
Fernandez, CH ;
Zaczek, R ;
Fitzgerald, LW ;
Huang, SM ;
Shen, HL ;
Wong, YN ;
Chien, BM ;
Quon, CY ;
Arvanitis, A .
JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (05) :833-848
[8]   Corticotrophin-releasing factor receptor antagonists [J].
Christos, TE ;
Arvanitis, A .
EXPERT OPINION ON THERAPEUTIC PATENTS, 1998, 8 (02) :143-152
[9]  
De Souza Errol B., 1995, P505
[10]  
DESOUZA EB, 1995, ANNU REP MED CHEM, V30, P21