01-01-2015 дата публикации
Номер: US20150005256A1
Принадлежит:
The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. 15-. (canceled)7. The method of claim 6 , wherein the compound is of the specified formula and:X and X′ are O; [{'sub': 1', '4', '1', '4', '1', '4, '(a) substituted or unsubstituted phenyl wherein the substituents are independently 1-5 H, (C-C)alkyl, (C-C)alkoxy, halo (F, Cl, Br, I), (C-C)haloalkyl, cyano, or nitro; or'}, {'sub': 1', '4', '1', '4', '1', '4, '(b) substituted or unsubstituted 2-pyridyl, 3-pyridyl, or 4-pyridyl, wherein the substituents are independently 1-4 H, (C-C)alkyl, (C-C)alkoxy, halo (F, Cl, Br, I), (C-C)haloalkyl, cyano, or nitro;'}], 'Y is{'sup': '3', 'Ris H, methyl, ethyl, or cyano;'}{'sup': 4', '7', '8, 'sub': 1', '4', '1', '4', '1', '4, 'R, R, and Rare independently: H, (C-C)alkyl, (C-C)alkoxy, halo (F, Cl, Br, I), (C-C)haloalkyl, cyano, or nitro; and'}{'sup': 5', '6, 'sub': 1', '4', '1', '4', '1', '4, 'Rand Rare independently: H, (C-C)alkyl, halo (F, Cl, Br, I), C-Chaloalkyl, (C-C)alkoxy, hydroxy, amino, cyano, or nitro.'}8. (canceled)9. The method of claim 7 , wherein the compound is of the specified formula and: [{'sub': 1', '4', '1', '4', '1', '4, '(a) substituted or unsubstituted phenyl wherein the substituents are independently 1-5 H, (C-C)alkyl, (C-C)alkoxy, halo (F, Cl, Br, I), (C-C)haloalkyl; or'}, {'sub': 1', '4', '1', '4', '1', '4, '(b) substituted or unsubstituted 3-pyridyl, wherein the substituents are independently 1-4 H, (C- ...
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