NEW SUBSTITUTED DERIVATIVES OF THIOFEMPIRIMIDINONE IN QUALITY OF INHIBITORS OF 17BETA-HYDROXIESTEROID DESHYDROGENASE.

摘要

A compound of formula (I) ** see formula ** in which R1 and R2 are individually selected from the group consisting of (i) -C1-C12 alkyl, said linear, cyclic, branched or partially unsaturated alkyl being, which is optionally substituted with one, two or three substituents individually selected from the group consisting of hydroxyl, -C1-C12 alkoxy, thiol, C1-C12 alkylthio, aryloxy, arylacyl, -CO-OR, -O-CO-R, heteroaryl-acyloxy and -N (R) 2; wherein the aryl moiety is phenyl or naphthyl, and is optionally substituted with one, two or three halogens; wherein said heteroaryl moiety is thienyl, furyl or pyridinyl; (ii) aryl and aryl- (C1-C12 alkyl), in which the alkyl moiety is optionally substituted with one or two hydroxyl groups, and in which the aryl moiety is optionally substituted with one to five substituents individually selected from the group consisting of halogen, hydroxyl, C1-C12 alkoxy, nitro, nitrile, C1-C12 alkyl, halogenated C1-C12 alkyl, -SO2-N (R) 2, (C1-C12 alkyl) sulfonyl; or said aryl may be optionally substituted with two groups that are attached to adjacent carbon atoms and are combined in a saturated cyclic 5, 6 or 7-membered ring system, optionally containing one, two or three heteroatoms, such as N u Or, the number of atoms of N 0-3 being, and the number of atoms of O each being 0-2, in which the cyclic ring system may also be optionally substituted with an oxo group; (iii) heteroaryl and heteroaryl- (C1-C12 alkyl), in which the heteroaryl group is optionally substituted with one, two or three substituents individually selected from the group consisting of halogen, C1-C12 alkyl, halogenated C1-C8 alkyl, - CO-OR, aryl or aryloxy, in which the aryl group is selected from phenyl or naphthyl, and is optionally substituted with one, two or three halogen atoms; (Iv) cycloheteroalkyl and cycloheteroalkyl (C1-C8), whereby the cycloheteroalkyl moiety is selected from the group consisting of pirrrolidinilo, tetrahydrofuryl, tetrahydrothiophenyl, tetrahydropyridinyl, dioxolyl, azetidinyl, thiazolidinyl, oxazolidinyl, piperidinyl, morpholinyl, thiomorpholinyl, piperazinyl, azepanyl, diazepanyl, oxazepanyl, thiazepanyl, dihydro-1H-pyrrolyl and 1,3-dihydrobenzoimidazolyl; wherein the cycloheteroalkyl moiety is optionally substituted with up to two substituents individually selected from the group consisting of oxo, C1-C12 alkyl, hydroxyl, C1-C12 alkoxy and aryl- (C1-C12 alkyl); or R2 itself is independently selected from -CO-R, -CO-O-R or -CO-N (R) 2; in which R1 and R2 cannot simultaneously be unsubstituted alkyl; R3 and R4 are individually selected from the group consisting of hydrogen, oxo, thio, halogen or dihalogen, -CO-R-, preferably CHO, -CO-OR, nitrile, -CO-N (R) 2, -O-CO -R-, -OR, -SR, -N (R) 2, -C1-C12 alkyl, said linear, cyclic, branched or partially unsaturated alkyl being, and said alkyl is optionally substituted with one, two or three individually selected substituents from the group consisting of hydroxyl, C1-C12 alkoxy, thiol and -N (R) 2; R5 and R6 are individually selected from the group consisting of hydrogen, halogen, -OR, -CO-OR, -CO-R, -C1-C12 alkyl, said linear, cyclic, branched or partially unsaturated alkyl being, and said alkyl is optionally substituted with one, two or three substituents individually selected from the group consisting of hydroxyl, C1-C12 alkoxy, thiol, C1-C12 alkylthio, and -CO-OR; and aryl and aryl- (C1-C12 alkyl), wherein the aryl moiety is optionally substituted with one to five substituents individually selected from the group consisting of halogen, hydroxyl, C1-C12 alkoxy, nitro, nitrile, C1-C12 alkyl, halogenated C1-C12 alkyl, in which R5 and R6 cannot simultaneously be hydrogen, and in which R6 is different from halogen if R5 represents hydrogen; wherein R represents hydrogen, C1-C12 alkyl or phenyl, the phenyl group being optionally substituted with one, two or three substituents selected from the group consisting of halogen, hydroxyl and C1-C4 alkoxy; and the hydrocarbon chain -C (R3) -C (R4) -C (R5) -C (R6) - of the six-membered ring is saturated or contains one or two double bonds between carbon atoms, or its pharmaceutically acceptable salt .