| 摘要 |
DISCLOSED ARE COMPOUNDS OF THE FORMULA WHERE IN : R2 IS HYDROGEN, ALKYL, OR CYCLOALKYL ; R3 IS HYDROGEN, LOWER ALKYL, LOWER ALKOXY, HALOGEN, TRIFLUOROMETHYL, LOWER ALKYNYL, LOWER ALKENYL, NITRILE, NITRO, -COR4, -CO2R4, -CONR4R5, -CONR4OR5, -SO2NR4R5, -SO2R4, -SO3R4, P(O)(OR4)(OR5), Y IS N OR CR7 ; R9 IS LOWER ALKYL, HALOALKYL, OR ARYL ; X AND Z ARE INDEPENDENTLY HYDROGEN, HALOGEN, LOWER ALKYL, LOWER ALKOXY,TRIFLUOROMETHYL, HYDROXY, NITRILE, NITRO, -NR4R5, -N(O)R4R5, -NR4R5R6W, -SR4, -C(O)R4, -CO2R4, -CONR4R5, -SO2NR4R5, -SO2R4, -SO3R4, P(O)(OR4)(OR5), -T(CH2)mQR4, -C(O)T(CH2)mQR4, OR –NR4C(O)T(CH2)mQR5 ; m IS 1 TO 6 ; T IS O, S, NR4, N(O)R4, NR4R5W, OR CR4R5 ; Q IS O, S, NR4, N(O)R4, NR4R5W, CO2, OR A CARBOCYCLIC GROUP CONTAINING FROM 3 TO 7 MEMBERS, UP TO FOUR OF WHICH MEMBERS ARE OPTIONALLY HETEROATOMS INDEPENDENTLY SELECTED FROM OXYGEN, SULFUR, AND NITROGEN, WHEREIN THE CARBOCYCLIC GROUP IS UNSUBSTITUTED OR SUBSTITUTED WITH ONE, TWO, OR THREE GROUPS INDEPENDENTLY SELECTED FROM HALOGEN, HYDROXY, HYDROXYALKYL, LOWER ALKYL, LOWER ALKOXY ALKOXYCARBONYL, ALKYLCARBONYL, ALKYLCARBONYLAMINO, AMINOALKYL, TRIFLUOROMETHYL, N-HYDROXYACETAMIDE, TRIFLUOROMETHYLALKYL, AMINO, OR MONO OR DIALKYLAMINO ; R6 LOWER ALYL, HALOALKYL OR ARYL; R7 IS –NR4R5, -N(O)R4R5, -NR4R5R9X, -OH, -OR4, -SR4, HALO, -COR4, (CH2)nR4, CO2R4, CONR4R5, -C(O)NR4SO2R5, -S(O)R4, -SO2R4, -SO2NR4R5, -SO3R4, -(CH2)nP(O)(OR4)2, -NR4SO2R5, ALDEHYDE, NITRILE, NITRO, ALKYL ALKOXYALKYL, -T(CH2)mQR4, -C(O)T(CH2)mQR4, -NR4C(O)T(CH2)mQR5, OR –T(CH2)CO2R4 ; n IS 0 TO 6 ; W IS AN ANION ; R4 AND R5 ARE INDEPENDENTLY HYDROGEN, LOWER ALKYL, LOWER ALKENYL, LOWER ALKYNYL, (CH2) nAr, ARYLALKYL, ARYL, HETEROARYL, HETEROARYLALKYL, CYCLOALKYL, HETEROCYCLOALKYL, OR HETEROARYL, OR R4 AND R5 TOGETHER WITH THE NITROGEN TO WHICH THEY ARE ATTACHED FORM A CARBOCYCLIC RING CONTAINING 3 TO 8 MEMBERS, UP TO FOUR OF WHICH MEMBERS ARE OPTIONALLY CARBONYL GROUPS OR HETEROATOMS INDEPENDENTLY SELECTED FROM O, S, SO, S(O)2, AND N; AND WHEN Y IS CR7 , IT IS PART OF THE PORT STRUCTURE …….. WHEREIN R7 AND Z ARE AS DEFINED ABOVE, OR CAN BE TAKEN TOGETHER WITH THE CARBONS TO WHICH THEY ARE ATTACHED TO FORM… WHEREIN : G AND J ARE INDEPENDENTLY CH2, NH, OR O; B IS NH, S, CH2, OR O; D IS C OR N, PROVIDED THAT R10 IS NOTHING WHEN D IS N; AND R10 AND R11 ARE INDEPENDENTLY HYDROGEN, HALOGEN, LOWER ALKYL, LOWER ALKOXY, OR ALKYLCARBONYL; THESE COMPOUNDS ARE USEFUL FOR TREATING CELL PROLIFERATIVE DISORDERS, SUCH AS CANCER, ATHEROSCLEROSIS, AND RESTENOSIS. THESE COMPOUNDS ARE POTENT INHIBITORS OF CYCLIN-DEPENDENT KINASES (CDKS) AND GROWTH FACTOR-MEDIATED KINASES; THE PRESENT INVENTION ALSO PROVIDES A METHOD OF TREATING CELL PROLIFERATIVE DISORDERS; ALSO PROVIDED BY THE PRESENT INVENTION IS A PHARMACEUTICAL COMPOSITION COMPRISING A COMPOUND OF FORMULA I TOGETHER WITH A CARRIER OR EXCIPIENT |
