KIM, In Woo (KR),КИМ Ин У (KR),HAN, Mi Ryeong (KR),ХАН Ми Рион (KR),YOO, Jakyung (KR),Ю Чакён (KR),OH, Yun Ju (KR),О Юн Чу (KR),KIM, Ji Duck (KR),КИМ Чи Дук (KR),KIM, Nam Youn (KR),КИМ Нам Юн (KR),JUN
申请号：
RU2019102376
公开号：
RU0002714206C1
申请日:
2017.06.30
申请国别(地区):
RU
年份:
2020
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: present invention relates to pyrazolopyrimidine derivative of general formula I or its pharmaceutically acceptable salt possessing activity with respect to JAK3 and BTK, as well as to pharmaceutical compositions based on them. In general formula I R1 is benzothiazolyl, isothiazolyl, isoxazolyl, phenyl or pyrazolyl； where R1 is unsubstituted or substituted with a substituent selected from a group consisting of piperazinyl, unsubstituted or substituted C1-4 alkyl； benzyl substituted with C1-4 alkoxy； one or two C1-4 alkyl groups, unsubstituted or substituted morpholino, -N(C1-4 alkyl)2, C1-4 alkoxy, cyano or -CONH(C1-4 alkyl) group； C1-4 haloalkyl； C3-6 cycloalkyl； morpholino； -CO-(morpholino)； morpholino and halogen； -N(C1-4 alkyl)2； -NHCO(C2-4 alkenyl)； -NHCO(pyrrolidinyl)； C1-4 alkoxy, unsubstituted or substituted with -N(C1-4 alkyl)2 group； phenoxy； pyrazolyl unsubstituted or substituted with one or two C1-4 alkyl groups； pyrrolidinyl； and tetrahydropyranyl； R2 is hydrogen, C1-4 alkyl or halogen； R3 is C1-4 alkyl, unsubstituted or substituted with cyano or halogen； C2-6 alkenyl unsubstituted or substituted with one or two substitutes independently selected from a group consisting of cyano, C3-6 cycloalkyl and -N(C1-4 alkyl)2； or C2-4 alkynyl, unsubstituted or substituted C3-6 cycloalkyl, Xl is CR4 or N, where R4 is hydrogen, X2 is CR5, where R5 is hydrogen, C1-4 alkyl, halogen, cyano or C1-4 alkylthio, X3 is NR6, O or S, where R6 is hydrogen or C1-4 alkyl, X4 is CH or N, and X5 is a bond or NH.EFFECT: disclosed are pyrazolopyrimidine derivatives as a kinase inhibitor.13 cl, 5 tbl, 194 exНастоящее изобретение относится к пиразолопиримидиновому производному общей формулы I или его фармацевтически приемлемой соли, обладающим активностью в отношении JAK3 и BTK, а также к фармацевтической композиции на их основе. В общей формуле I R1 представляет собой бензотиазолил, изотиазолил, изоксазолил, фенилил или пиразолил； где R1 является незамещенн
