INDOLE DERIVATIVES INHIBITORS OF ENZYME LACTATE DEHYDROGENASE (LDH)

摘要

The present invention encompasses compounds having general formula (I) able to inhibit the lactate production (lactic acid) involved in the angiogenesis of tumoral tissues, in the glycolytic metabolic process of tumoral cells, of immune system cells in asthmatic diseases, in vascular cells in the pulmonary hypertension, in the treatment of chronic back pain or hyperoxaluria, and in the process by which the parasites protozoan causing malaria obtain most of the necessary energy.;

主权项

1. A compound, having the general formula (I): wherein: R is F or CF3; R1 is H; C1-C4 alkyl; C1-C4 alkyl substituted by phenyl, wherein the phenyl may optionally be substituted with one or more groups selected from halogen, nitro, methoxy, CF3 or phenyl; C1-C4 alkyl substituted by C3-C7 cycloalkyl, wherein the C3-C7 cycloalkyl may optionally be substituted by C1-C4 alkyl; or piperidine, optionally substituted by C1-C4 alkyl or C1-C4 alkyl substituted by phenyl; R2 is H or CH3; R3, R4, R3′, R4′ and R5 are independently selected from H, Cl, or OCF3; R6 is H or C6H5; R7 is H, wherein Q is selected from H or CH3C(O); or a stereoisomer, tautomer, hydrate, solvate, or a pharmaceutically acceptable salt thereof; with the exclusion of the following compounds; wherein R═CF3 and: R1, R2, R3, R4, R3′, R4′, R5, R6, and R7═H; R1, R2, R3, R4, R3′, R4′, R5, and R7═H; R6═C6H5; R1, R2, R3, R4, R3′, R4′, R6, and R7═H; R5═Cl; R1, R3, R4, R3′, R4′, R5, R6 and R7═H; R2═CH3; R1, R3, R4, R3′, R4′, R6, and R7═H; R2═CH3; R5═Cl; and R1, R2, R3′, R4′, R4, R6, and R7═H; R3, R5═Cl.