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Pirazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
专利权人:
F. Hoffmann-La Roche AG
发明人:
WANG, Xiaojing
申请号:
ES11713749
公开号:
ES2601004T3
申请日:
2011.04.06
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound chosen from the formula I: ** Formula ** and the stereoisomers, geometric isomers, tautomers or pharmaceutically acceptable salts thereof, wherein: R1 is H, C1-C12 alkyl, C2-C8 alkenyl, C2-C8 alkynyl , C6-C20 aryl, C3-C12 carbocyclyl, heterocyclyl of 3 to 20 ring atoms or heteroaryl of 5 to 20 ring atoms; R2 is H, heterocyclyl of 3 to 20 ring atoms, heteroaryl of 5 to 20 ring atoms, - (heteroaryl of 5 to 20 ring atoms) - (heterocyclyl of 3 to 20 ring atoms), aryl C6-C20, C3-C12 carbocyclyl, NR4R5 or OR4; or R1 and R2 together form a heterocyclyl of 3 to 20 ring atoms or a heteroaryl of 5 to 20 ring atoms; X is chosen from the structures: in which the wavy line indicates the site of the junction; R3 is H, Cl, Br, C1-C12 alkyl, - (C1-C12 alkylene) - (C3-C12 carbocyclyl), - (C1-C12 alkylene) - (heterocyclyl of 3 to 20 ring atoms), - ( C2-C8 alkenylene) - (C3-C12 carbocyclyl), - (C2-C8 alkenylene) - (heterocyclyl of 3 to 20 ring atoms), C6-C20 aryl, - (C6-C20 arylene) - (3-heterocyclyl at 20 ring atoms), - (C6-C20 arylene) - (C1-C12 alkylene) - (3 to 20 ring heterocyclyl), C3-C12 carbocyclyl, 3 to 20 ring heterocyclyl or heteroaryl of 5 to 20 ring atoms; R4 and R5 are independently selected from H, C1-C12 alkyl, C6-C20 aryl, C3-C12 carbocyclyl, heterocyclyl of 3 to 20 ring atoms, heteroaryl of 5 to 20 ring atoms, - (C1- alkylene C12) - (C6-C20 aryl), - (C1-C12 alkylene) - (C3-C12 carbocyclyl), - (C1-C12 alkylene) - (heterocyclyl of 3 to 20 ring atoms), - (C1- alkylene C12) - (heteroaryl of 5 to 20 ring atoms); or R4 and R5 together form a heterocyclyl of 3 to 20 ring atoms or a heteroaryl of 5 to 20 ring atoms; R6 is H or -NH2; R7 is H, F, CH2F, CHF2 and CF3; and said alkyl, alkenyl, alkynyl, alkylene, carbocyclyl, heterocyclyl, aryl and heteroaryl are optionally substituted by one or more groups independently selected from F, Cl, Br, I, -CH3, -CH2CH3, -CH (CH3) 2, -CH2CH (CH3) 2, -CH2NH2, -CH2CH2NH2, -CH2CHCH2NH2, -CH2CH (CH3) NH2, -CH2OH, -CH2CH2OH, -C (CH3
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