Patent ID: 7795255
Filing Date: 2010-09-14
Classification: A61K,A61P

Abstract:
1. A rigidified compound having the general Formula Va: wherein: the compound has a core structure which consists of a rhodanine analog being covalently attached to a first aryl or heteroaryl and of 1-5 linking moieties, at least one of said linking moieties connecting at least two radicals of E and X, such that said core structure has one or zero free-to-rotate bonds, wherein the wavy lines indicate a part of said rhodanine analog and a part of said first aryl or heteroaryl which are included in said core structure, wherein: the dashed lines indicate either a Z-configuration or an E-configuration of B with respect to Y; A is N; X is NRb; Y, Z and W are each independently O or S; M is C; B is selected from the group consisting of hydroxy, thiohydroxy, alkoxy, thioalkoxy, amine, hydrogen, a substituted or unsubstituted alkyl, a substituted or unsubstituted cycloalkyl, a substituted or unsubstituted aryl and a substituted or unsubstituted heteroaryl; E and G are each independently CRs; J and K are absent; Rb and Rs are each independently hydrogen, a substituted or unsubstituted alkyl, a substituted or unsubstituted cycloalkyl, and a substituted or unsubstituted aryl; R and R wherein: each of R Rq is selected from the group consisting of hydrogen, alkyl and Q Q each of said substituted alkyl, substituted cycloalkyl, substituted alkenyl, substituted allyl, substituted aryl and substituted heteroaryl independently comprises at least one substituent selected from the group consisting of halo, nitro, alkoxy, aryloxy, hydroxy, thiohydroxy, thioalkoxy, thioaryloxy, alkyl, aryl, heteroaryl, heteroalicyclic, trihaloalkyl, C-carboxylate, O-carboxylate, oxo, C-amide, N-amide, S-sulfonamide and N-sulfonamide, wherein when R with the proviso that the rigidified compound is not 2-(3-methoxy-phenyl)-5-(3-morpholin-4-yl-propyl)-4-thioxo-4,5-dihydro-1-thia-3b,5-diaza-cyclopenta[a]pentalen-6-one or 5-(3-morpholin-4-yl-propyl)-2-(3-nitro-phenyl)-4-thioxo-4,5-dihydro-1-thia-3b,5-diaza-cyclopenta[a]pentalen-6-one.