| 摘要 |
The present invention is based on the use of a broad family of 5-imino-1,2,4-thiadiazoles as potential new drugs for the treatment of diseases in which PDE7 inhibition is important, specially inflammatory diseases, autoimmune and neurodegenerative disorders. On the other hand, compounds of the 5-imino-1,2,4-thiadiazole family are here described, as well as their synthetic procedures, and they may have great application as drug or drug candidates.;Therefore, a first aspect of the present invention is related to a compound of formula (I):; |
| 主权项 |
1. A method for inhibiting phosphodiesterase (PDE7) activity comprising the administration to a patient in need thereof a therapeutically effective amount of a compound of formula (II): Wherein: R1 is a group X1—R1′ wherein X1 is a single bond; R1′ is C1-C6 alkyl, aryl, R1′ being optionally substituted with one or more groups X1′—R8 which may be identical or different; X1′ is a single bond or a group selected from C1-C6 alkylene, X1′ being optionally substituted with at least one or more groups which may be identical or different and are selected from F, Cl, Br, I; R8 is H, —OH, ═O, —NO2, CN, F, Cl, Br, I, C1-C4 alkyl, —CO2R6a, —C(═O)R6a, C(═S)R6a, SO2R6a, SOR6a, SO3R6a, SR6a, OR6a, C(═O)NR6aR7a, C(═S)NR6aR7a, C(═N—CN)NR6aR7a, C(═N—SO2NH2)NR6aR7a, C(═CH—NO2)NR6aR7a, SO2NR6aR7a, C(═NR6a)NHR7a, C(═NR6a)R7a or NR6aR7a, R6a and R7a being independently selected from R4 and R5; R2 is aryl, R2 being optionally substituted with at least one or more groups which may be identical or different and are selected from —NO2, OR6b, R6b being independently selected from R4 and R5; R3′ is selected from pyridyl, —(CH2)n—(C5-C7-heterocycloalkyl), (CH2)n—OR12 or —(CH2)n—C(O)OR12, n is a number between 0 and 20; R12 is independently selected from the groups defined for R10; R4 and R5 are independently selected from: C1-C6 alkyl; and R10 is independently selected from H and C1-C6 alkyl; or a pharmaceutically acceptable salt thereof. |
