- Bioavailable diacylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex
-
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.
- -
-
Page/Page column 5
(2008/06/13)
-
- Insecticidal N'-substituted-N,N'-diacylhydrazines
-
Insecticidal compounds having the formula N-(2-Ra -3-Rb -4-Rh -benzoyl)-N'-(2-Rc -3-Rd -4-Re -5-Rf -benzoyl)-N'-Rg -hydrazine wherein Ra is a halo or lower alkyl; R b is lower alkoxy, optionally substituted with halo (preferably fluoro); Rc is selected from hydrogen, halo, lower alkyl, lower alkoxy, lower alkoxy lower alkyl, and nitro; Rd, Re and Rf are each independently selected from hydrogen, bromo, chloro, fluoro, lower alkyl, lower alkoxy, and lower alkoxy lower alkyl; Rg is a (C4 -C6)alkyl; Rh is hydrogen, lower alkoxy, lower alkyl, or when taken together with Rb is methylenedioxy (--OCH2 O--), 1,2-ethylenedioxy (--OCH2 CH2 O--), 1,2-ethyleneoxy (--CH2 CH2 O--) or 1,3-propyleneoxy (--CH2 CH2 CH2 O--) wherein an oxo atom is located at the Rb position; and the substituents Rc and Rd, or Rd and Re, or Re and Rf when taken together can be methylenedioxy or 1,2-ethylenedioxy as well as compositions comprising an agronomically acceptable carrier and an insecticidally effective amount of such compounds; and methods of using such compounds and compositions. Also, methods for the production of the compounds and their intermediates, which methods comprise either admixing a 3-amino-2-(substituted)-benzoic acid, sodium nitrite and methanol under acidic conditions or admixing a 3,4-fused heterocyclic benzoic acid and an alkyl lithium reagent followed by subsequent reaction with an electrophilic reagent.
- -
-
-