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INHIBITEURS DE TYROSINE KINASE DE BRUTON
专利权人:
JOINT STOCK COMPANY "BIOCAD"
发明人:
GAVRILOV, Aleksey Sergeevich,POPKOVA, Aleksandra Vladimirovna,SILONOV, Sergey Aleksandrovich,SMIRNOVA, Svetlana Sergeevna,IAKOVLEV, Pavel Andreevich,ALESHUNIN, Pavel Aleksandrovich,GORBUNOVA, Svetlana
申请号:
IBIB2017/057154
公开号:
WO2018/092047A1
申请日:
2017.11.16
申请国别(地区):
IB
年份:
2018
代理人:
摘要:
The present invention relates to a new compound of formula I: or pharmaceutically acceptable salt, solvate or stereoisomer thereof, wherein: V1 is C or N, V2 is C(R2) or N, whereby if V1 is C then V2 is N, if V1 is C then V2 is C(R2), or if V1 is N then V2 is C(R2); each n, k is independently 0, 1; each R2, R11 is independently H, D, Hal, CN, NR'R", C(O)NR'R", C1-C6 alkoxy; R3 is H, D, hydroxy, C(O)C1-C6 alkyl, C(O)C2-C6 alkenyl, C(O)C2-C6 alkynyl, C1-C6 alkyl; R4 is H, Hal, CN, CONR'R", hydroxy, C1-C6 alkyl, C1-C6 alkoxy; L is CH2, NH, O or chemical bond; R1 is selected from the group of the fragments, comprising: Fragment 1, Fragment 2, Fragment 3 each A1, A2, A3, A4 is independently CH, N, CHal; each A5, A6, A7, A8, A9 is independently C, CH or N; R5 is H, CN, Hal, CONR'R", C1-C6 alkyl, non-substituted or substituted by one or more halogens; each R' and R" is independently selected from the group, comprising H, C1-C6 alkyl, C1-C6 cycloalkyl, aryl; R6 is selected from the group: [formula II] each R7, R8, R9, R10 is independently vinyl, methylacetylenyl; Hal is CI, Br, I, F, which have properties of inhibitor of Bruton's tyrosine kinase (Btk), to pharmaceutical compositions containing such compounds, and their use as pharmaceuticals for treatment of diseases and disorder.La présente invention concerne un nouveau composé représenté par la formule I, ou un sel, un solvate ou un stéréoisomère pharmaceutiquement acceptable de celui-ci, dans laquelle : V1 est C ou N, V2 est C(R2) ou N, ainsi si V1 est C alors V2 est N, si V1 est C alors V2 est C(R2), ou si V1 est N alors V2 est C(R2); chaque n, k est indépendamment 0, 1; chaque R2, R11 est indépendamment H, D, Hal, CN, NR'R", C(O)NR'R", un alkoxy C1-C6; R3 est H, D, un hydroxy, un alkyle en C(O)C1-C6, un alcényle en C(O)C2-C6 , un alcényle en C(O)C2-C6, un alkyle en C1-C6; R4 est H, Hal, CN, CONR'R", un hydroxy, un alkyle en C1-C6, un alkoxy C1-C6; L est CH2, NH, O ou une liaison chimique; R1 est choisi dans le groupe d
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