GIANNINI, GIUSEPPE,CABRI, WALTER,VESCI, LOREDANA,CERVONI, MARIA LUISA,PISANO, CLAUDIO,TADDEI, MAURIZIO,FERRINI, SERENA
申请号：
ES11805449
公开号：
ES2536980T3
申请日:
2011.12.13
申请国别(地区):
ES
年份:
2015
代理人:
摘要：
A compound of general formula I ** Formula ** in which, R1 is H, CONR4R5； R5 is H, (C1-C6) -alkyl or (C3-C10) -cycloalkyl each of which is optionally substituted one or more times with OH, OMe, Cl, F； R4 is H, (C1-C4) -alkyl or CH (R11) COR12； or R4 and R5 together with the nitrogen atom to which they are attached form a three to seven membered heterocycle optionally containing another heteroatom chosen from the group consisting of N, O or S； and wherein said heterocycle is optionally substituted one or more times with 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； Endocyclic symbols --- are, for each compound, all double bonds or all simple bonds； m is an integer between 0 and 3； R9 and R10 are independently of each other (C1-C4) -alkyl optionally substituted with OH, cycloalkyl, heterocycloalkyl, OMe, amino, (C1-C6) -alkylamino or (C1-C6) -dialkylamino； heterocycloalkyl optionally substituted one or more times with alkyl, amino, (C1-C6) -alkylamino or (C1-C6) -dialkylamino； cycloalkyl； or R9 and R10 together with the nitrogen atom to which they are attached form a heterocyclic ring selected from the group consisting of piperidyl, pyrrolidinyl, piperazinyl or morpholinyl, each of which is optionally substituted one or more times with F, Cl, Br , OH, OMe, amino, (C1-C6) -alkylamino, (C1-C6) -dialkylamino, (C1-C4) -alkyl, hydroxyalkyl, optionally substituted phenyl or benzyl； or an unsaturated imidazole heterocycle； R3 is Cl, Et or i-Pr； their tautomers, their geometric isomers, their optically active forms such as their enantiomers, diastereoisomers and racemates, as well as their pharmaceutically acceptable salts.Un compuesto de fórmula general I**Fórmula** en la que, R1 es H, CONR4R5； R5 es H, (C1-C6)-alquilo o (C3-C10)-cicloalquilo cad
