New 2,5-diamino-3,4,5,6-tetrahydro-6-pyrimidinone derivatives useful for treating bacterial infections

摘要

2,5-Diamino-3,4,5,6-tetrahydro-6-pyrimidinone derivatives (I) are new. Compounds of formula (I) and their salts are new: Y = 1-5C alkanediyl, optionally with a C atoms replaced by O or NH; Z' = NZ1Z2, NZ5-CQ-NZ6Z7 or NZ5-C(NZ9)-Z8; heteroaryl or phenyl optionally substituted with 1-3 of 1-6C alkyl, halo, CF3, 1-4C aminoalkyl or 1-4C dialkylamino; or 1-6C alkyl optionally substituted with heterocyclyl; Z1 = H; 6-10C aryl substituted with 1-3 of CF3, OCF3, OPh, 1-4C alkoxy, halo, CN or SO2NZ11Z12; or 1-4C alkyl optionally substituted with 1-3 of 3-6C cycloalkyl, pyridyl or NZ3Z4; Z3, Z4 = H, 1-4C alkyl, 3-6C cycloalkyl or heteroaryl optionally substituted with 1-4C alkoxy, halo, CF3 or OPh, or NZ3Z4 is a heterocycle optionally substituted with 1-3 of halo or R; R = alkyl optionally substituted with 1-3 of amino, 1-4C alkylamino or 1-4C dialkylamino; Z11 = H or 1-4C alkyl; Z12 = H, 1-4C alkyl or Ph; Z5-Z7 = H, 1-6C alkyl, 1-6C alkanoyl, benzyl or pyridylmethyl; Z8 = H or 1-6C alkyl; Q = O, S or NZ9; Z9 = H, 1-6C alkyl, 1-6C alkanoyl, benzyl or pyridylmethyl; R1 = H or 1-6C alkyl; R2 = H or 1-6C alkyl optionally substituted with 1-3 of OH, 1-4C alkoxy or 1-4C alkoxycarbonyl; R3 = COR31 or heteroaryl; R31 = 1-4C alkyl, 3-6C cycloalkyl, 1-6C alkoxy, NH2, 1-4C alkylamino, 1-4C dialkylamino or heteroaryl; R4 = H; alternatively, NZ1Z2 is a heterocycle optionally substituted with 1-3 of halo or R and/or R2+R4 forms a 5- or 6-membered ring. Independent claims are also included for: (1) a process for preparing compounds (I); (2) a pharmaceutical composition comprising a compound (I) and a carrier or excipient.