Ligands for nematode nuclear receptors and uses thereof
AssigneeBoard of Regents, The University of Texas System
InventorsDavid J. Mangelsdorf, Richard J. Auchus, Daniel L. Motola, Carolyn L. Cummins, Kamalesh K. Sharma
Life of this patent
Estimating the term…
Abstract
An effective anti-nematode methodology entails contacting nematodes with a biologically effective amount of at least one compound according to formula I: where Q, Q′, R1, R2, and n are defined herein, or with a stereoisomer, solvate, or pharmaceutically acceptable salt of such compound.
Claims9
A method for controlling the growth of a nematode, comprising contacting the nematode with a biologically effective amount of at least one compound according to formula I or a stereoisomer, or pharmaceutically acceptable salt thereof:
- wherein each instance of independently is a single bond or a double bond;
- one of Q or Q′ is OH or SH and the other of Q or Q′ is hydrogen, or Q and Q′ together with the carbon atom to which they are attached form a carbonyl or thiocarbonyl group;
- R1 is selected from the group consisting of:
- wherein each instance of independently is a single bond, or a double bond;
- and wherein R1 is optionally substituted with 1 to 2 substituents, each of which is independently selected from the group consisting of halo, (C1-C8)alkyl, NRR′, OR, and SR;
- R2 is a substituent on one or more carbon atoms in rings A, B, C, and D and, in each instance, is independently selected from the group consisting of halo, (C1-C8)alkyl, (C1-C8)haloalkyl, (C1-C8)hydroxyalkyl, NRR′, oxo, thione, OR, and SR;
- R and R′ are independently selected from the group consisting of hydrogen, (C1-C8)alkyl, (C1-C8)fluoroalkyl, and (C1-C8)hydroxyalkyl;
- and n is selected from the group consisting of 0, 1, or 2.
A method of reducing nematode infestation of a plant that is infested or susceptible to infestation by a nematode population, comprising administering to the plant a biologically effective amount of at least one compound according to formula I or a stereoisomer, or pharmaceutically acceptable salt thereof:
- wherein each instance of independently is a single bond or a double bond;
- one of Q or Q′ is OH or SH and the other of Q or Q′ is hydrogen, or Q and Q′ together with the carbon atom to which they are attached form a carbonyl or thiocarbonyl group;
- R1 is selected from the group consisting of:
- wherein each instance of independently is a single bond, or a double bond and wherein R1 is optionally substituted with 1 to 2 substituents, each of which is independently selected from the group consisting of halo, (C1-C8)alkyl, (C1-C8)haloalkyl, (C1-C8)hydroxyalkyl, NRR′, OR, and SR;
- R2 is a substituent on one or more carbon atoms in rings A, B, C, and D and, in each instance, is independently selected from the group consisting of halo, (C1-C8)alkyl, (C1-C8)haloalkyl, (C1-C8)hydroxyalkyl, NRR′, oxo, thione, OR, and SR;
- R and R′ are independently selected from the group consisting of hydrogen, (C1-C8)alkyl, (C1-C8)fluoroalkyl, and (C1-C8)hydroxyalkyl;
- and n is selected from the group consisting of 0, 1, or 2.
A method of reducing a nematode infestation in a mammal, comprising administering to the mammal a therapeutically effective amount of at least one compound according to formula I or a stereoisomer, or pharmaceutically acceptable salt thereof:
- wherein each instance of independently is a single bond or a double bond;
- one of Q or Q′ is OH or SH and the other of Q or Q′ is hydrogen, or Q and Q′ together with the carbon atom to which they are attached form a carbonyl or thiocarbonyl group;
- R1 is selected from the group consisting of:
- wherein each instance of independently is a single bond, or a double bond and wherein R1 is optionally substituted with 1 to 2 substituents, each of which is independently selected from the group consisting of halo, (C1-C8)alkyl, (C1-C8)haloalkyl, (C1-C8)hydroxyalkyl, NRR′, OR, and SR;
- R2 is a substituent on one or more carbon atoms in rings A, B, C, and D and, in each instance, is independently selected from the group consisting of halo, (C1-C8)alkyl, (C1-C8)haloalkyl, (C1-C8)hydroxyalkyl, NRR′, oxo, thione, OR, and SR;
- R and R′ are independently selected from the group consisting of hydrogen, (C1-C8)alkyl, (C1-C8)fluoroalkyl, and (C1-C8)hydroxyalkyl;
- and n is selected from the group consisting of 0, 1, or 2.
Dependencies are inferred from the claim text.