| abstract |
1. New derivatives of (azetidin-1-ylalkyl) lactams of general formula (I) in which R is C1-C6-akyl substituted with C3-C7-cycloalkyl, phenyl or pyridyl, where phenyl is optionally substituted with 1 or 2 substituents selected from the group consisting of C1-C4-alkyl, halogen, C1-C4-alkoxy, phenyl, C2-C5-alkanoyl, fluoro-C1-C4-alkyl and -SO2N (C1-C4-alkyl) 2; and the C 3 -C 7 -cycloalkyl is optionally substituted with 1 or 2 substituents independently selected from the group consisting of C 1 -C 4 -alkyl and fluoro; R1 is phenyl optionally substituted with 1 or 2 halogen atoms; R2 is -CO NR3 R4, -CONH (C3-C7-cycloalkyl) -, -NR3 R4, imidazole or the group of formula R3 and R4 are independently hydrogen or C1-C4-alkyl optionally substituted with hydroxyl or C1-C 4- alkoxy; R5 and R6 are independently hydrogen or C1 -C4-alkyl; R7 is hydrogen, hydroxyl, or phenyl; R8 is hydrogen, hydroxy or C2-C5alkyoyloxy; X is C1 -C4-alkylene; X1 means direct binding; X2 is a direct bond or CO; W is methylene, CH (OH), CH (C1 -C4-alkoxy), CHNH (C1 -C4 -alkyl), CHN (C1 -C4 -alkyl) 2, CHNR5 SO2 (C1 -C4 -alkyl), O, S (O) p, NH, N (C1 -C4 -alkyl), NSO2 (C1 -C4-alkyl), NSO2 NH2, NSO2 NH (C1 -C4 -alkyl), NSO2 NH (C1 -C4 -alkyl) 2, NCONH2, NCONH (C1-C4-alkyl), NCON (C1-C4-alkyl) 2, or NC02 (C1 -C4-alkyl); n is 1 or 2 when W is not methylene and n is 0 or 1 when W is methylene; p is 0, 1 or 2; and pharmaceutically acceptable salts thereof. PL PL PL PL PL PL PL PL |