Abstract:
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.
Abstract:
Insecticidal compounds having the formula N-(2-R.sup.a -3-R.sup.b -4-R.sup.h -benzoyl)-N'-(2-R.sup.c -3-R.sup.d -4-R.sup.e -5-R.sup.f -benzoyl)-N'-R.sup.g -hydrazine wherein R.sup.a is a halo or lower alkyl; R.sup. b is lower alkoxy, optionally substituted with halo (preferably fluoro); R.sup.c is selected from hydrogen, halo, lower alkyl, lower alkoxy, lower alkoxy lower alkyl, and nitro; R.sup.d, R.sup.e and R.sup.f are each independently selected from hydrogen, bromo, chloro, fluoro, lower alkyl, lower alkoxy, and lower alkoxy lower alkyl; R.sub.g is a (C.sub.4 -C.sub.6)alkyl; R.sup.h is hydrogen, lower alkoxy, lower alkyl, or when taken together with R.sup.b is methylenedioxy (--OCH.sub.2 O--), 1,2-ethylenedioxy (--OCH.sub.2 CH.sub.2 O--), 1,2-ethyleneoxy (--CH.sub.2 CH.sub.2 O--) or 1,3-propyleneoxy (--CH.sub.2 CH.sub.2 CH.sub.2 O--) wherein an oxo atom is located at the R.sup.b position; and the substituents R.sup.c and R.sup.d, or R.sup.d and R.sup.e, or R.sup.e and R.sup.f 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.
Abstract:
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.
Abstract:
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.
Abstract:
This invention relates to a novel process for the preparation of 4-hydroxy-6-methyl-2-pyrone which comprises reacting 3-acetyl-6-methyl-2(H)-pyran-2,4(3H)-dione (dehydroacetic acid, "DHAA") with from 93% to about 99% sulfuric acid (1-7% water content) at temperatures from about 60.degree. to about 140.degree. C. under pressures from about 10 millimeters of mercury to about 75 pounds per square inch wherein the sulfuric acid to pyran weight ratio (H.sub.2 SO.sub.4 :DHAA) is from about 0.8:1 to about 3:1 and isolating the 4-hydroxy-6-methyl-2-pyrone.
Abstract:
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.
Abstract:
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.
Abstract:
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.
Abstract:
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.
Abstract:
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.