| abstract |
A pyrazol pyrimidinone compound according to formula (1), a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein: R1 is H or C1-6 alkyl in which R1 binds well to N1 or N2; R2 is C1-6 alkyl optionally substituted with hydroxy or alkoxy; C3-7 cycloalkyl optionally substituted with alkyl, hydroxy or alkoxy; a saturated 5-6 membered heterocycle optionally substituted with alkyl, hydroxy or alkoxy, het1 or Ar1; R3 is C1-6 alkyl optionally substituted with 1 or 2 groups independently selected from: Ar2, C3-7 cycloalkyl optionally substituted with C1-6 alkyl; OAr2, SAr2; NHC (O) C1-6 alkyl; het2; xanthene; and naphthalene; wherein Ar1 and Ar2 are independently groups of formula (2), in which R4, R5 and R6 are independently selected from: hydrogen, halo, phenoxy, phenyl, CF3, OCF3, R7, SR7 and OR7, in which R7 is C1-6 alkyl optionally substituted with het3 or by a phenyl group optionally substituted with 1, 2 or 3 groups independently selected from halo, CF3, OCF3, C1-6 alkyl and C1-6 alkoxy: or in which R4 and R5 they combine to form a union of 3 or 4 atoms, and in the said union 1 or 2 heteroatoms independently selected from O, S and N can be incorporated; and wherein het1, het2 and het3, which may be the same or different, are 5-6 membered aromatic heterocycles containing 1, 2 or 3 heteroatoms, independently selected from O, S and N, the said heterocycles optionally substituted by 1 , 2 or 3 substituents, are independently selected from C1-6 alkyl, halo and phenyl optionally substituted with 1, 2 or 3 groups independently selected from halo and C1-6 alkyl; with the conditions that when: a) R1 is attached to N1, R1 is C1-6 alkyl and R2 is propyl, then R3 is not ethyl substituted with Ar1, and b) is attached to N1, R1 is C1-6 alkyl and R2 it is methyl, then R3 is not C1-4alkyl substituted with Ar1, processes for the preparation thereof, pharmaceutical compositions thereof and use thereof in the preparation of medicaments useful for treating cardiovascular disorders. |