199942-73-9Relevant articles and documents
Antagonists of gonadotropin releasing hormone
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, (2008/06/13)
PCT No. PCT/US97/08479 Sec. 371 Date Nov. 12, 1998 Sec. 102(e) Date Nov. 12, 1998 PCT Filed May 16, 1997 PCT Pub. No. WO97/44321 PCT Pub. Date Nov. 27, 1997There are disclosed compounds of formula (I) and pharmaceutical acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related conditions.
Investigation of the 4-O-alkylamine substituent of non-peptide quinolone GnRH receptor antagonists
DeVita, Robert J.,Goulet, Mark T.,Wyvratt, Matthew J.,Fisher, Michael H.,Lo, Jane-L,Yang, Yi Tien,Cheng, Kang,Smith, Roy G.
, p. 2621 - 2624 (2007/10/03)
Synthesis and in vitro activity of the enantiomers of quinolone GnRH antagonist (±)-1 are reported. Chiral amino alcohols were prepared from the appropriate cyclic D- or L-amino acids by the Arndt-Eistert homologation followed by reduction of the resulting esters. Incorporation of these pharmacophores was achieved via a novel Mitsunobu alkylation of 4-hydroxyquinolones. The key amine pharmacophore for binding to the rat GnRH receptor was most active in the S-configuration. Ring size was not important for potency with 4, 5, 6, and 7-membered ring amines exhibiting similar potency.