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US 12,760,024 B2Granted
Substituted benzo[d][1,3]dioxoles as BTK and/or JAK3 kinase inhibitors
AssigneeXi'an Xintong Pharmaceutical Research Co., Ltd.
InventorsYungen Xu, Tingting Liang, Qihua Zhu, Junjie Wang, Lifang Cen, Wenjie Wang, Jiaming Jin
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Abstract
Disclosed herein is a 1,3-benzodioxol derivative as shown in general formula (I). Results of pharmacological experiments indicate that the compound of Formula (I) can exert excellent inhibition on both BTK and JAK3 kinases, and can be used to prepare medicines for treating rheumatoid arthritis caused by over-activation of BTK and/or JAK3 pathways. The disclosure further describes a preparation method for the 1,3-benzodioxol derivative.
Claims15
A compound of formula (I):
- or a pharmaceutically acceptable salt or stereoisomer thereof,
- wherein:
- A represents —NHC(O)—, —NHC(O)CH2—, —NHS(O)2—, —O—, or —S—;
- R1 represents:
- Y1 represents CR5 or N;
- Y2 represents CR5 or N;
- Y3 represents CR5 or N;
- Y4 represents CR5 or N;
- each R5 independently represents H, F, Cl, Br, I, CN, CH3, CF3, OH, OCH3, or OCF3;
- Z represents —NR6—, —O—, or —S—;
- R6 represents H, CH3, CH2CH3, or cyclopropyl;
- each R4 independently represents H, F, Cl, Br, I, CN, NO2, C1-C6 alkyl, CF3, C(O)NH2, C(O)NHCH3, C(O)NHCH2CF3, NH2, NHC1-C6 alkyl, NHC(O)CH3, N(CH3)2, N(CH2CH3)2, OH, OC1-C6 alkyl, OCF3, OCH2CH2OCH3, pyrrolidin-1-yl, piperazin-1-yl, 4-methylpiperazin-1-yl, morpholin-4-yl, or phenyl;
- X represents CH or N;
- m represents 0 or 1;
- n represents 0 or 1;
- R2 represents H, Cl, Br, or CN;
- and
- R3 represents H, C1-C6 alkyl, or C2-C6 heterocycloalkyl;
- wherein the C2-C6 heterocycloalkyl is a saturated 4-, 5-, or 6-membered ring containing one, two, or three heteroatoms or heteroatomic groups independently selected from the group consisting of N, NH, O, and S;
- and
- wherein the C1-C6 alkyl or C2-C6 heterocycloalkyl is substituted with one or more substituents independently selected from the group consisting of NH2, NHCH3, NHC(O)CH3, OH, and OCH3.
18 more elements
A compound selected from the group consisting of:
- or a planimetrically acceptable salt thereof.
Dependencies are inferred from the claim text.