Small-molecule modulators of TRP-p8 activity
AssigneeDendreon Corporation
InventorsOfir Moreno, Sateesh Natarajan, David F. Duncan
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Abstract
Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.
Claims9
A compound of Formula I-E:
- wherein A, B, C, and D are independently selected from CR1 and N;
- wherein at least one of A, B, C, and D is CR1;
- wherein R1 is selected from H, alkyl, heteroalkyl, aryl, arylalkyl, halogen;
- and wherein when two adjacent of A, B, C, and D are CR1, the two R1's may combine to form a single aryl, cycloalkyl, or heterocycloalkyl group;
- and
- R2 is ethylene, propylene or butylene;
- and R3 is H, methyl or —C═NH(NH2).
The compound 1-(2-Amino-ethyl)-1-(2-isopropyl-5-methyl-cyclohexanecarbonyl)-1,3-dihydro-benzoimidazol-2-one.
The compound 3-(2-Amino-ethyl)-1-(2-isopropyl-5-methyl-cyclohexanecarbonyl)-2-oxo-2,3-dihydro-1H-benzoimidazole-5-carboxylic acid amide.
Dependencies are inferred from the claim text.