Patent ID: 8426345

Claim:
A method of identifying biologically active compounds comprising: (a) designing a first library of compounds of formula 1 to scan molecular diversity wherein for each compound of the first library R 2 and one of R 1 , R 3 , R 4 , and R 5 as defined below are pharmacophoric groups and the remainder of R 1 , R 3 , R 4 , and R 5 are non-pharmacophoric groups; (b) assessing the first library of compounds in one or more biological activity assay(s); and (c) designing a second library wherein for each compound of the second library the substituents R 1 to R 5 comprise the two pharmacophoric groups identified in step (b) and a third pharmacophoric group, and wherein the remainder of R 1 , R 3 , R 4 , and R 5 are non-pharmacophoric groups, such that the/each component of the first and second library is a compound of formula 1: wherein the ring of the first library is of the allo configuration; Z is sulphur, oxygen, NH, NR A or hydrogen, in the case where Z is hydrogen then R 1 is not present; R A is selected from the set defined for R 1 , R 3 , R 4 , and R 5 , or wherein Z and R 1 together form a heterocycle; X is oxygen or nitrogen; R 2 is a pharmacophoric group independently selected from the group consisting of C 2 to C 20 alkyl, C 2 to C 20 acyl, wherein said acyl is not acetyl; C 2 to C 20 alkenyl, C 2 to C 20 alkynyl, C 2 to C 20 heteroalkyl, C 5 to C 20 aryl, C 5 to C 20 heteroaryl, C 5 to C 20 arylalkyl and C 5 to C 20 heteroarylalkyl, which is optionally substituted, and can be branched or linear, or wherein NH and R 2 combine to form a heterocycle; R 1 , R 3 , R 4 , and R 5 are each independently selected from (i) non-pharmacophoric groups consisting of H, methyl and acetyl, and (ii) pharmacophoric groups independently selected from the group consisting of C 2 to C 20 alkyl, C 2 to C 20 acyl, wherein said acyl is not acetyl; C 2 to C 20 alkenyl, C 2 to C 20 alkynyl, C 2 to C 20 heteroalkyl; C 5 to C 20 aryl, C 5 to C 20 heteroaryl, C 5 to C 20 arylalkyl and C 5 to C 20 heteroarylalkyl, which is optionally substituted, and can be branched or linear, or wherein X and the corresponding R moiety, R 3 to R 5 respectively, combine to form a heterocycle.