| 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 in all possible isomeric forms and selected from the group consisting of glycine, alanine, phenylalanine, valine, leucine, isoleucine, aspartic acid, asparagine, glutamic acid, glutamine, serine, lysine, histidine, methionine, proline, cysteine, threonine, tryptophan, arginine and tyrosine; 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 and their racemate forms, as well as their pharmaceutically acceptable salts thereof. |
