08-09-2022 дата публикации
Номер: US20220281878A1
Принадлежит:
Provided in the present invention are 1H-[1, 2, 3]triazolo[4, 5-h] quinazoline compounds of general formula (I), which can be used for treating cell proliferative disorders. The new compounds of the present invention are effective inhibitors of cyclin-dependent kinases (CDK). 219.-. (canceled)24. The compound of formula (III) or (111-1) claim 23 , or the pharmaceutically acceptable salt claim 23 , enantiomer claim 23 , diastereomer claim 23 , racemate claim 23 , solvate claim 23 , hydrate claim 23 , polymorph claim 23 , prodrug claim 23 , or isotopic variant thereof claim 23 , or the mixture thereof according to claim 23 , wherein:R1 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, C1-6 alkyl or C1-6 haloalkyl;R2 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, C1-6 alkyl or C1-6 haloalkyl;R3 is selected from H, D, halogen, —CN, —NO2, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 4- to 7-membered heterocyclyl, each of which is optionally substituted with 1, 2 or 3 R8 group(s);R4 is selected from H, D, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl;R5 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, C1-6 alkyl or C1-6 haloalkyl;R6 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, C1-6 alkyl or C1-6 haloalkyl;R7 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, C1-6 alkyl or C1-6 haloalkyl;L is selected from bond, —O—, —NH—, —C(O)—, —C(O)NH— or —NHC(O)—;R8 is selected from H, D, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl or C1-6 haloalkyl; or two R8 groups on the same atom are taken together to form oxo or thioxo;Ra is independently selected from H, —C0-6 alkylene-OR′, —C0-6 alkylene-SR′, —C0-6 alkylene-NR″R′″, —C0-6 alkylene-C(O)R′, —C0-6 alkylene-C(O)OR′, —C0-6 alkylene-C(O)NR″R′″, ...
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