| 摘要 |
The invention relates to 1,2,5-trisubstituted 1,2-dihydroindazol-3-ones of formula (I)whereinX is -SO2-, -SO-, -(CH2)p-, -(CH2)p-O-, -(CH2)p-(C=O)-, -(CH2)p-(C=O)-NH-, -(CH2)p-CHOH-, -CHOH-(CH2)p-, -(CH2)p-CH=CH-, -CH=CH-(CH2)p-,Y is -(C=O)-, -(C=O)-NH-, -(C=O)-NH-(CH2)p-, -C=O)-(CH2)p-, -(CH2)p-, -(CH2)p-O-, -(CH2)p-(C=O)-, -(CH2)p-(C=O)-NH-, -(CH2)p-(C=O)-NH-(CH2)p-, -(CH2)p-CHOH-, -CHOH-(CH2)p-, -(CH2)p-CH=CH-, -CH=CH-(CH2)p-,Z is -O-, -O-(CH2)p-, -NH-, -NH-(C=O)-, -NH-(C=O)-NH-, -NH-(C=O)-O-, -NH-CH2-(C=O)- and -NH-(C=O)-CH2-,P is a cardinal number from 1 to 4,R1, R2 and R3 can be the same or different and are:mono-, bi- or tricyclic saturated or mono- or polyunsaturated carbocycles having from 5 to 14 ring members; or mono-, bi- or tricyclic saturated or mono- or polyunsaturated heterocycles having from 5 to 15 ring members and from 1 to 6 heteroatoms,in which the carbocycles and the heterocycles can be mono- or polysubstituted by:C1-6-alkyl, -O-C1-6-alkyl, -O-C3-7-cycloalkyl, mono-, bi- or tricyclic saturated or mono- or polyunsaturated carbocycles having from 3 to 14 ring members, mono-, bi- or tricyclic saturated or mono- or polyunsaturated heterocycles having from 5 to 15 ring members and from 1 to 6 heteroatoms,R1 is also H, provided that when X is CH2, then R1 is not H,R3-Z is also NO2,and their pharmaceutically acceptable salts,but excluding compounds of formula (I) in whichif Z is -NH-(C=O)-, -NH-(C=O)-NH-, -NH-(C=O)-O-, -NH-(C=O)-CH2 and at the same time R1 is phenyl, monosubstituted or polysubstituted by -COOH, -COOC1-6-alkyl, -(CH2)p-COOH, -(CH2)p-COOC1-6-alkyl -CONHC1-6-alkyl, -CONHC6-14-aryl, -CONHSO2C1-6-alkyl, -CONHSO2C6-4-aryl, 1H-tetrazol-5-yl, then R2 is not phenyl, monosubstituted or polysubstituted by CN, halogen, C1-4-alkyl, C1-4-alkyloxy, CF3; andif R3-Z is NO2, then R1-X is not benzyl or 4-methoxybenzyl, and R2-Y is not benzyl or 2-picolyl at the same time; and to pharmaceutical treatment processes, and processes for making. |
