New beta-alanylamino-substituted dihydropyrimidinone derivatives, useful as antibacterial agents with strong activity against Gram positive bacteria, including methicillin-resistant Staphylococcus aureus

摘要

5-( beta -Alanyl-amino)-3,4,5,6-tetrahydro-2-(acylamino or ureido)-pyrimidin-4-one derivatives (I) are new. Dihydropyrimidinones of formula (I) and their salts are new; Y = 1-5C linear or branched alkanediyl (optionally having one C replaced by O or NH); Z = NRz1Rz2, 5-6 atom aromatic heterocycle containing 1-3 heteroatoms selected from O, S or N, phenyl, 1-6C alkyl optionally substituted with a 5 or 6 (un)saturated or aromatic heterocyclic with 1-3 heteroatoms selected from O, S or N, or phenyl, both can be optionally substituted by 1-6C alkyl, trifluoromethyl, amino-1-4C (di)alkylamino; Rz1 = H, 1-4C alkyl optionally substituted by pyridyl or NRz3Rz4; Rz3 or Rz4 = H, 1-4C alkyl, 3-6C cycloalkyl, 1-6 aromatic heterocycle (optionally substituted by 1-4C alkoxy, halogen, trifluoromethyl or phenoxy); Rz1 and Rz2 = along with the N they are attached to form 4-6 ring containing 1-2 heteroatoms optionally substituted by 1-3 halogen or alkyl, where the alkyl is optionally substituted by amino, 1-4C (di)alkylamino; Q1 = H, U (optionally substituted by pyridyl or NQ3Q4), 3-6C cycloalkyl or 5- or 6-membered aromatic heterocycle (optionally substituted by OU, halo, CF3 or OPh); or NQ1Q2 = 4-6 membered ring (optionally containing 1 or 2 further heteroatom(s) and optionally substituted by 1-3 of halo or alkyl (itself optionally substituted by NH2, NHU or NU2)); Q3, Q4 = H or U; R1 = H or T; R2 = H or T (optionally substituted by OH, OU or COOU); R4 = H; or R2 + R4 = group completing a 5- or 6-membered ring (optionally containing a further O, S or N heteroatom); R3 = -C (O)R'3; R'3 = U, 3-6C cycloalkyl, OT, NH2, NHU, NU2 or a 5- or 6-membered aromatic heterocycle containing 1-3 of O, S and N as heteroatom(s); T = 1-6C alkyl and; U = 1-4C alkyl. An Independent claim is also included for the preparation of (I).