Cyclin dependent kinase inhibiting drugs, useful for treating tumor cell proliferation, viral infections or neurodegenerative diseases, comprising new or known pyrazolo 1,3,5-triazine derivatives

摘要

The use of 4-substituted pyrazolo (1,5-a)-1,3,5-triazine derivatives (I) as cyclin dependent kinase (CDK) inhibiting medicaments is new. Some compounds (I) are new. The use of pyrazolo-triazine derivatives of formula (I), in the form of racemates, enantiomers or their combinations, or their salts is claimed in the preparation of cyclin dependent kinase (CDK) inhibiting medicaments. A = H, halo, CHO, CN, NO2, guanidinoaminomethylenyl, (1,3-dihydro-2-oxo-indol-3-ylidene)-methyl, alkylcarbonyl, aralkylcarbonyl, heteroaralkylcarbonyl or -L-NR1R2; L = alkylene; R1, R2 = H or alkyl; or NR1R2 = 5-7 membered heterocycle in which the members (other than the bonding N) are selected from CH2, NR3, S or O; R3 = H or alkyl; X = H, alkylthio, aralkylthio, alkylthioxo, aralkylthioxo or NR4R5; R4 = alkyl, hydroxyalkyl, cycloalkyl (optionally substituted by one or more of alkyl, OH and NH2), aralkyl (optionally ring-substituted by one or more of halo, CN, NO2, alkyl and alkoxy), or heteroaryl or heteroaralkyl (both optionally ring-substituted by one or more alkyl); R5 = H; or NR4R5 = ring as defined for NR1R2 (except that R3 can also be hydroxyalkyl); Y = NH or O; Z' = direct bond, alkyl (sic) or alkylthioalkyl (sic); Ar = carbocyclic aryl (optionally substituted by 1-3 of halo, CN, NO2, alkyl, alkoxy or NR7R8); or 5- or 6-membered heteroaryl containing N, O and/or S as heteroatom(s) (optionally substituted by one or more of alkyl, aminoalkyl or mono- or dialkylaminoalkyl); R7, R8 = H or alkyl; or NR7R8 = heterocycle as defined for NR1R2. An Independent claim is included for (I) or their salts as new compounds, provided that if A is other than CN, NO2 or guanidinoaminomethylenyl, then either: (i) Z' = alkyl or thioalkyl (sic); or (ii) X = NR4R5, in which: R4 = 'aralkylthio, aralkylthioxo or hydroxyalkyl, one of the alkyl, alkylthio or alkylthioxo radicals having 2-5C' (sic); or cycloalkyl (optionally substituted as above), aralkyl (optionally ring-substituted by one or more of halo, alkyl and alkoxy), or heteroaryl or heteroaralkyl (both optionally ring-substituted as above); R5 = H; or NR4R5 = ring as defined above.