| 主权项 |
1. A compound of formula I wherein, R1 is H, CONR4R5; R5 is H, (C1-C6)-alkyl or (C3-C10)-cycloalkyl each being optionally substituted once or more with OH, OMe, Cl, F; R4 is H, (C1-C4)-alkyl or CH(R11)COR12; or R4 and R5 taken together with the nitrogen atom to which they are attached form a three to seven membered heterocycle optionally containing a further heteroatom selected from the group consisting of N, O or S; and wherein said heterocycle is optionally substituted once or more by OH, OMe, (C1-C4)-alkyl, optionally substituted phenyl, or benzyl; R11 is a side chain of a natural α-amino acid; R12 is OH, amino, alkylamino or dialkylamino; R2 is a bond, —NH(CO)—, —N(R7)— or —N(R7)CH2—; R7 is H, (C1-C4)-alkyl or CO2R8; R8 is (C1-C4)-alkyl or benzyl; the endocyclic symbols are, for each single compound, all double bonds or all single bonds; m is an integer comprised between 0 and 3; R9 and R11 are independently from each other (C1-C4)-alkyl optionally substituted with OH, cycloalkyl, heterocycloalkyl, OMe, amino, (C1-C6)-alkylamino or (C1-C6)-dialkylamino; heterocycloalkyl optionally substituted once or more by alkyl, amino, (C1-C6)-alkylamino or (C1-C6)-dialkylamino; cycloalkyl; or R9 and R10 taken together with the nitrogen atom to which they are attached form a heterocycle ring chosen from the group consisting of piperidyl, pyrrolidinyl, piperazinyl or morpholinyl, each of them being optionally substituted once or more by F, Cl, Br, OH, OMe, amino, (C1-C6)-alkylamino, (C1-C6)-dialkylamino, (C1-C4)-alkyl, hydroxyalkyl, optionally substituted phenyl, or benzyl; or an imidazole unsaturated heterocycle; R3 is Cl, Et or i-Pr; or a tautomer, a geometrical isomer, an optically active form and a pharmaceutically acceptable salt thereof. |
