主权项 |
1. A compound having the general Formula (I) wherein, R1 is H, (C1-C6)-alkyl or aryl; or alternatively R1 and one R4, each being linked to two adjacent carbon atoms, in case n is 2 or 3, are taken together to form a cyclopropane ring; R2 is phenyl optionally substituted with halogen, benzyloxy, (C1-C3)-alkyl or CF3; (C3-C6)-cycloalkyl; aryl-(C1-C6)-alkyl wherein the aryl is optionally substituted with benzyloxy, (C1-C3)-alkyl or CF3; R3 is H, PO(OH)2, or a group of Formula (II)
—(CO)—R7 Formula II R7 is (C1-C7)-alkyl, (C1-C6)-alkoxy or —CH(NH2)R8; R8 is H, or the side chain of a natural α-amino acid; R4 and R5 are at any occurrence independently H, halogen, (C1-C6)-alkyl, or alternatively, when n is 2 or 3, one R4 and one R5, each being linked to two adjacent carbon atoms, are taken together to form a cyclopropane ring; R6 is H or alternatively, R2 and R6 are taken together to form a five- to six-membered heterocycle which can be optionally fused with an aryl moiety; -A-E- is —(CO)—(NR9)— or —(NR9)—(CO)—; R9 is H or (C1-C3)-alkyl; m is an integer comprised between 0 to 3; n is an integer comprised between 0 to 3 with the proviso that when is 2 or 3, each of R4 and R5 can adopt different meaning at each occurrence; the symbol means that the carbon atom bearing said symbol can adopt a R or S configuration; the symbol ◯ can be absent, but if present it means that the cycle can be partially unsaturated with the proviso that when the carbon atom bearing R4 is involved in a double bond, R5 is absent; their tautomers, their geometrical isomers, their optically active forms such as enantiomers, diastereomers and their racemate forms, as well as their pharmaceutically acceptable salts thereof. |