Patent ID: 7994140
Filing Date: 2011-08-09
Classification: A61K,A61P

Abstract:
1. A method of identifying a candidate therapeutic agent comprising: i) contacting a membrane comprising a G-Protein Coupled Receptor (GPCR) with a compound of general formula 1, or a pharmaceutically acceptable salt thereof wherein the ring may be of any configuration; Z is selected from the group consisting of: sulphur, oxygen, and NR A wherein R A is selected from the set defined for R 1 to R 5 or C1 to C15 acyl, C4 to C15 arylacyl or C4 to C15 heteroarylacyl, with the proviso that both R 1 and R A are not hydrogen, X is selected from the group consisting of: oxygen and NR A providing that: i) X of XR 2 is NR A , ii) X of XR 3 is oxygen and R 3 is not hydrogen, iii) X of R 4 is oxygen or NR A , and X of XR 5 is oxygen, wherein at least one of OR 4 and OR 5 is OH, R 1 to R 5 are independently selected from the group consisting of: H, C1 to C12 alkyl, C1 to C12 alkenyl, C1 to C12 alkynyl, C1 to C12 heteroalkyl, C4 to C15 aryl, C4 to C15 heteroaryl, C4 to C15 arylalkyl and C4 to C15 heteroarylalkyl substituent, wherein, when X is NR A , both R A and the corresponding R 2 or R 4 is not hydrogen, and ii) determining whether said compound inhibits or effects signal transduction activity of said GPCR, wherein a compound that inhibits or effects said activity of said GPCR is a candidate therapeutic agent.